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Natural compounds derived from plants could yield hundreds of new drugs

NYBG scientist says the plant world has “great potential” as a source of new medicines

There are probably at least 500 medically useful chemicals awaiting discovery in plant species whose chemical constituents have not yet been evaluated for their potential to cure or treat disease, according to a new analysis by a New York Botanical Garden scientist who has more than 15 years of experience in collecting plants for natural-products discovery programs.

Currently, 135 drugs on the market are derived directly from plants; the analysis indicates that at least three times as many disease-fighting substances have yet to be found that could be developed into drugs or used as the basis for further drug research.

“Clearly, plant diversity has not been exhausted, and there is still great potential in the plant world,” said James S. Miller, Ph.D., Dean and Vice President for Science at the Botanical Garden.

Dr. Miller’s analysis, “The Discovery of Medicines from Plants: A Current Biological Perspective,” is published in the December issue of the peer-reviewed journal Economic Botany.

To arrive at his estimate, Dr. Miller used a formula based on the ratio of the number of drugs that have been developed from plants to the number of plants that were screened to find those drugs. He then applied that ratio to the number of plant species that have not yet been screened.

Because of uncertainties in some of those numbers, the formula yields a range of potential drug discoveries. While there is no general agreement among botanists about the number of plant species that are likely to exist, Dr. Miller concluded that there are 300,000 to 350,000 species of plants. Of those, he determined that the chemistry of only 2,000 species has been thoroughly studied, and perhaps only 60,000 species have been evaluated even partially for medicinally useful chemicals.

Working with those numbers, Dr. Miller calculated that there are likely to be a minimum of 540 to 653 new drugs waiting to be discovered from plants; the actual number could be much greater.

“These calculations indicate that there is significant value in continuing to screen plants for the discovery of novel bioactive medicinally useful compounds,” concludes Dr. Miller, who has run natural-products discovery programs that have collected specimens in North America, Central and Southeast Asia, and Africa for government agencies, pharmaceutical companies, and academic programs.

As part of his Economic Botany paper, Dr. Miller reviews the disappointing history of past plant-screening efforts and evaluates the potential for future programs.

Technological advances in the 1970s and 1980s gave medical researchers the capacity to evaluate large numbers of plant samples. That prompted the federal government and large pharmaceutical companies to institute aggressive plant collecting and screening programs. Those programs led to the development of several important drugs such as Taxol from Taxus brevifolia (used in cancer treatment) and Camptothecin from Camptotheca acuminata (derivatives of which are used to treat cancer). Other drugs indirectly trace their discovery to natural-products research, including the anti-viral Oseltamivir, which derives from Illicium anisatum and is marketed in the United States as Tamiflu.

The number of drug discoveries, however, was substantially less than anticipated. By the early 2000s, many of the large pharmaceutical companies had abandoned their efforts.

Dr. Miller argues that one possible explanation for the low yield is the relatively crude way in which plant extracts were tested for their pharmaceutical potential. Plants may contain as many as 500 to 800 different chemical compounds, but the screening programs of the late 20th century used extracts made from a whole plant or at best extracts that contained many hundreds of compounds.

Under those circumstances, one compound may interfere with the action of another, or the amount of one compound may be too small to register in a mix of hundreds of chemicals.

To correct this problem, new technologies now allow researchers to separate complex mixtures of natural products into a “library” of relatively pure compounds that can be tested individually. A 2002 study demonstrated that testing such libraries dramatically improves discovery rates.

Bringing these advances together with refinements in collecting strategies could lead to what Dr. Miller calls a “second renaissance” of natural-products discovery.

Miller undertook his analysis to highlight the fact that despite past collecting programs, the plant world represents a poorly explored source of potentially lifesaving drugs. That adds urgency, he said, to efforts to conserve natural habitats so that species are not driven to extinction before they can be studied.

“The natural world has a great and diverse array of interesting chemicals that have been only minimally studied and still hold considerable potential,” he writes.

Contact: Stevenson Swanson
718-817-8512
The New York Botanical Garden

Source: http://www.eurekalert.org/pub_releases/2011-12/tnyb-nmc121211.php

Links related to natural compounds and plant extracts:

Natural Compounds

Plant Extracts

Natural and Natural Derivatives Libraries

Ancient Chinese cures translate into modern Western medicines

The Chem-TCM is the most comprehensive database of its kind and translates more than 12,000 chemicals from more than 300 Chinese herbs used in traditional Chinese medicine (TCM) into Western terminology.

“Future researchers will now be able to better understand the chemical basis of remedies that have been in use for thousands of years,” says David Barlow of King’s College London (KCL), who has helped to develop the database.

TCM chemicals are rarely used as raw materials to develop Western drugs because their complex nature makes the registration process difficult.

The database may also answer one of TCM’s regulatory challenges in the United Kingdom. An EU directive came into effect in the UK this May that makes it illegal for individual practitioners to sell TCM over the counter, except for varieties registered with the UK drug safety watchdog, the Medicines and Healthcare Products Agency.

read more…

BioFocus to Offer IMD’s Natural Product Libraries through Drug Discovery Services

    BioFocus and InterMed Discovery (IMD) inked a marketing collaboration that will allow BioFocus to offer IMD’s natural product screening libraries through its drug discovery services. IMD will in addition provide follow-on services to BioFocus.

    “We have been impressed with the scale of IMD’s natural product discovery capabilities, and we believe that when InterMed’s natural product libraries and services are combined with our screening services, our engine for drug discovery will be substantially enhanced and more cost-effective for our clients,” comments Chris Newton, Ph.D., BioFocus MD.

    IMD was established as a management buyout from Bayer HealthCare in Germany. The firm’s expertise is based on its natural compound libraries and related databases, which are being exploited to offer compound discovery and consultancy to the pharmaceutical, crop science, and food industries. IMD claims to offer the largest collections of pure compounds, sample fractions, and mixtures as its source for potential natural product leads.

    The firm is in addition generating a pipeline of early-stage pharmaceuticals and functional ingredients based on compounds it says have shown interesting in vitro or in vivo potential. Biologically characterized product leads are identified using the IMD Bioprofiling and Npsilico technologies, which together comprise a bioinformatics platform that draws on years worth of screening results, complemented by primary biological and chemical research on natural products.

    The Npsilico platform is composed of literature and proprietary information about bioactive natural products. IMD claims that this enables the identification of lead structures without de novo wet lab identification, through systematic, focused, and structure-driven research.

    Source: http://genengnews.com/gen-news-highlights/biofocus-to-offer-imd-s-natural-product-libraries-through-drug-discovery-services/81245443/

Iona Chemistry Professor Researches Cure For ALZ

New Rochelle, NY – Do curry spice, wine and apple skins hold the answer for finding a cure for Alzheimer’s disease, Parkinson’s disease and other neurological disorders?

The results of a laboratory research project, recently published in the Journal of Neurochemistry, show that a chemical compound derived from these natural products may be used in neutralizing the toxic effects of chemicals associated with some debilitating and life-threatening neurological diseases.

The findings are the result of a four-year study undertaken by Terrence Gavin, Ph.D., a chemistry professor at Iona College and Richard M. LoPachin, Ph.D, a neurochemist and director of research in the Department of Anesthesiology at Montefiore Medical Center and the Albert Einstein College of Medicine.

In lab experiments it was found that the compound, called 2-ACP, completely protects nerve cells from the harmful effects of type-2 alkenes. There is growing evidence that exposure to type 2-alkenes, which are found in the smoke inhaled from cigarettes, the exhaust of automobiles and even in French fried potatoes, can increase the chances of developing Alzheimer’s and otherneurological conditions. In addition, studies
have shown type-2 alkenes are being produced within the nerve endings during the disease process that presumably initiates Alzheimer’s.

Dr. Gavin said: “The research Dr. LoPachin and I undertook is promising because chemical compounds extracted from curry spice, red wine and apple skins, which are widely used natural products, have already been clinically demonstrated to have neuroprotective properties. This suggests it would be safe and effective to treat humans with the 2-ACP compound.”

He added: “But, these molecular findings worked in laboratory cultures. We now need to confirm the effects of 2-ACP in animal studies. That will be the focus of our efforts in the coming months.”

In addition, Dr. Gavin and some of his students
at Iona will be looking for new compounds that will be as good or better than 2-ACP in combating the effects of type 2-alkenes. “Our goal is to have new compounds ready for testing in six months. This is a very exciting scientific exploration,” Dr. Gavin stated.

Dr. Gavin has been a chemistry professor at Iona since 1982. He holds a doctoral degree in chemistry from the State University of New York at Stony Brook and attended the State University of New York at New Paltz where he earned a B.A. degree. He and his family live in New Paltz.

Source: westchester.com

Pomegranate ‘can combat MRSA and other superbugs’

Scientists have discovered the power of fruit as a potential new weapon in the fight against MRSA and other hospital superbugs. A team from the University of Kingston, in Surrey, have shown that pomegranate can be used to create an ointment with the power to tackle the drug-resistant infections.

In a series of tests conducted over three years, academics found that mixing the fruit’s rind with two other natural products – metal salts and vitamin C – greatly enhanced its infection-fighting properties. The discovery could pave the way for a lotion to be developed for patients or perhaps, in time, a new antibiotic.

Declan Naughton, professor of biomolecular sciences at Kingston, described the breakthrough as “significant”.

Naughton said scientists were searching for a way to create new antibiotics because of the rise in infections resistant to drugs on the market. One way to go about it was to screen natural products, he said.

“A great deal of medicines come from plants, but the normal approach taken by the pharmaceutical industry is to try to find one particular active molecule,” he said. “After a considerable number of screening experiments, we found that combining three ingredients – pomegranate rind, vitamin C and a metal salt – gave a much more potent effect: killing off or inhibiting drug-resistant microbes from growing.

“It was the mix that fantastically increased the activity – there was synergy, where the combined effects were much greater than those exhibited by individual components. It shows nature still has a few tricks up its sleeve.”

The tests were conducted using microbes taken from hospital patients. Scientists found that pomegranate rind mixed with metal salts were most effective against MRSA, while adding vitamin C helped tackle other common hospital infections.

Naughton said the idea of using foodstuffs was unusual but meant that the body should be more able to cope with its application. “Patients are less likely to experience any major side-effects,” he added.

It is not the first time pomegranate has been shown to have medical benefits. The fruit has already been hailed a super-food with claims that its juice can help protect against a range of ailments, from heart disease to male impotence.

Other scientists welcomed the findings but pointed out that they were limited to tests in the laboratory – and had yet to be developed for use on people.

Anthony Coates, professor of medical microbiology at St George’s in London, said: “What is the significance of all of this? Well, there is no doubt that these natural products like pomegranate are of interest. This observation – the fact it has acted against MRSA and other drug-resistant infections – is potentially significant. But we need to remember it is early research, of an observational nature, in vitro.” Coates said much more work needed to be done to answer questions such as which component was the most active and to look at toxicity when applying the treatment to humans.

However, he pointed to other studies that had also highlighted the benefits of the fruit. One trial on 60 patients found that it had an anti-dental plaque effect, for instance.

Any discovery that was a potential step towards a new antibiotic was a positive thing, he added.

“The need for new antibiotics is acute,” said Coates. “To put it in context, about 20 new classes of antibiotics were marketed between 1940 and 1962 yet only three have been marketed since. In all classes, resistance has arisen. Most antibiotics come from nature, so it is very valid to look at natural sources.”

■ The leaves and bark of the willow tree have been talked about for centuries as a remedy for some illnesses. This is because they contain salicylic acid – the precursor to aspirin. The Royal Society published findings about the medicinal properties of the natural ingredient in the 18th century.

â–  Taxol (paclitaxel) is a chemotherapy drug that has been in use for many years. It is extracted from yew bark and needles. The white powder is turned into a clear, colourless liquid and administered intravenously. It is used in the treatment of ovarian, testicular and lung cancer among others.

■ The same scientists who discovered that pomegranate rind could counter MRSA also discovered that white tea could help prevent cancer and heart disease. It comes from the same plant as other teas, but the leaves are picked and harvested before fully open – when the buds are covered by fine, white hair.

â–  Rhubarb root has naturally occurring anthraquinones (organic compounds) which have a laxative effect.

â–  Animals can also provide medicines. For example, a series of antibiotic peptides were extracted from the skin of the African clawed frog.

Source: guardian.co.uk

Astellas and REGiMMUNE to Collaborate on New Vaccine Technology

TOKYO and MOUNTAIN VIEW, CA–(Marketwire – July 22, 2009) – REGiMMUNE Corporation today announced that Astellas Pharma Inc. and REGiMMUNE have entered into a collaboration agreement to jointly research and develop a novel vaccine-platform technology. The partnership will combine Astellas’ broad range of capabilities in screening and developing natural source-derived compounds with REGiMMUNE’s immune liposome technology. Terms of the agreement have not been disclosed.

“Our goal is to develop a potent vaccine-platform technology that enables effective vaccination with novel adjuvant and immune liposome technologies, increasing the efficiency of delivery to immune cells. Our approach will eliminate many of the current limitations for vaccine development,” explained Haru Morita, CEO of REGiMMUNE. “This is particularly important for responding to new or changing virus strains. Astellas has a strong presence in immunology and is one of the largest vaccine distributors in Japan,” Mr. Morita continued. “We believe this collaboration can produce a technology that will allow a rapid response to various viral outbreaks spreading around the world.”

“We are pleased to initiate our first partnership with REGiMMUNE,” stated Masafumi Nogimori, President and Chief Executive Officer of Astellas. “Disease prevention through timely and adequate vaccination is a key to maintaining human health. Astellas is committed to developing a new vaccine platform and this collaboration with REGiMMUNE will strengthen our position in this important area of disease prevention.”

About Vaccines

Prophylactic vaccines need to elicit sufficient immune responses to protect individuals from the challenge by infectious agents. Most commonly, attenuated live viral particles are used to develop effective vaccines; however, development of live viral particles requires significant lead time and lengthy, costly manufacturing processes. While efforts have been made to develop improved adjuvants to enhance the potency of non-viral vaccines, Alum remains the only adjuvant approved by the U.S. FDA for use in humans. The Astellas-REGiMMUNE collaboration is expected to address these obstacles and provide a number of benefits over currently marketed products.

About REGiMMUNE

REGiMMUNE, with research and development operations in Tokyo, Japan, and Mountain View, CA, is a biotechnology company focused on the discovery, development and commercialization of immune-regulatory therapeutics to treat life-threatening and debilitating conditions including allergies, autoimmune diseases and transplantation. The company’s proprietary platform technology, reVax, induces immune tolerance in an antigen-specific manner through pharmacological induction of regulatory T (Treg) cells. Treg cells are believed to play a central role in inducing and maintaining immune tolerance. Using its reVax technology, REGiMMUNE is developing a broad range of pipeline products. The lead compound, RGI-2001, which is in late preclinical stage, has the potential to become a first-in-class Treg-cell-inducing drug.

About Astellas

Astellas Pharma Inc., located in Tokyo, Japan, is a pharmaceutical company dedicated to improving the health of people around the world through the provision of innovative and reliable pharmaceutical products. The organization is committed to becoming a global category leader by combining outstanding R&D and marketing capabilities and continuing to grow in the world pharmaceutical market. For more information about Astellas Pharma Inc., please visit our website at www.astellas.com/en/.

Source: REGiMMUNE

Drug Discovery Latin America, February 26-27, 2009 – Rio de Janeiro, Brazil

The inaugural Drug Discovery Latin America conference and exhibition will be held in the colourful city of Rio de Janeiro in the days immediately following the world famous carnival.

The purpose of this meeting is to review the status of drug discovery activities in Latin America and to assist its future development. Business and research leaders from both developed markets and BRIC countries will bring their knowledge and experience to share. Participants will be encouraged to network and explore partnering opportunities.

Full conference passes include admission to all sessions and the exhibition as well as conference documentation.
Lunch, coffee breaks and the drinks reception provide ample time for networking and to continue discussions from the question and answer sessions.

http://www.selectbiosciences.com/conferences/DDLA2009

Agenda

Day One – 26 February 2009

Screening

09:00

Using Drug Molecules as Probes and Probe Molecules as Drug Precursors
Ralph Garippa, Research Leader, Roche Discovery Technologies
This talk will highlight some examples of Pharma’s HT screened molecules which became popular commercialized reagents, and some promising molecules which have been published in the public domain (PubMed) as a result of academic screening.

09:30

Title to be Confirmed
Jeremy Caldwell, Director of Cell Based Screening, GNF

10:00

Using in vitro Screening Assays to Profile the Biology of Chemical Entities
John Watson, Director, Pharmacology and Biotechnology, Promega
Profiling of a compound’s impact on cell signaling pathways, ADME properties and cellular toxicity early in the discovery process can help prioritize compounds to help assure the final drug has maximal target activity and minimal off target effects.

10:30

Coffee and Networking in the Exhibition Hall

11:15

Nuclear Receptor Activation Assessment: Improving Safety and Directing Chemistry
Kyle Kramer, Vice President, Business Development, Puracyp
The presentation includes introduction to key nuclear receptors (NR) involved in drug metabolism. The construction and use of stable cell lines with reporter genes is explained. Finally, the utility of these systems in drug safety screening is presented.

11:45

Functional Genome-Wide Screening for Genes that Regulate p53 in Endothelial Cells
Michael Edel, Principle Investigator, Centre of Regenerative Medicine in Barcelona
Angiogenesis requires an increase in endothelial cell proliferation to support an increase in mass of blood vessels. An in vitro cell model has been designed that can be used for screening gene or chemical libraries that regulate endothelial cell proliferation.

12:15

Presentation to be Announced

12:45

Lunch and Networking in the Exhibition Hall

Tropical Disease Drug Development

14:00

Prolyl Oligopeptidase of Trypanosoma cruzi (POP Tc80) : A Target for the Design of New Weapons Against Chagas Desease
Bernard Maigret, CNRS Research Director, LORIA – Nancy University
The group has recently demonstrated that the activity of POPTc80, a prolyl endopeptidase that mediates native collagen and fibronectin hydrolysis, is required for trypomastigotes entry into host cells. Using a tridimentionnel model of this target built from homology modelling, molecular docking and screening assays they were able to identify possible new compounds active against Chagas desease.

14:30

Novel Drug Targets for the Malaria Parasite
Asif Mohmmed, Staff Research Scientist, International Centre for Genetic Engineering and Biotechnology

15:00

Title to be Confirmed
Leila de Mendonça Lima, Senior Researcher and Head of Lab. for Functional Genomics and Bioinformatics, Oswaldo Cruz Foundation, FIOCRUZ

15:30

Coffee and Networking in the Exhibition Hall

16:15

Drug Discovery of Fluorinated Drugs Against Neglected Diseases and HIV/AIDS
Núbia Boechat, Head of R&D Group in Medicinal Chemistry, Oswaldo Cruz Foundation, FIOCRUZ
Organic synthesis of fluorinated compounds in medicinal chemistry against AIDS and neglected diseases; innovation and technological management in public health.

Drug Discovery in Emerging Markets

16:45

Drug Development and Discovery
Christopher Bianca, Professor of Chemistry, Clinical Consultant, Keystone College Academia
This presentation discusses all the relevant information required to develop a new drug or a lead compound drug, from toxicology, to pharmacodynamics, to pharmacokinetics, and all the way to clinical trials including FDA approval.

17:15

Stem Cells in Drug Discovery
Chris Kendrick-Parker, Chief Commercial Officer, Cellular-Dynamics International

17:45

Drinks Reception

Day Two – 27 February 2009

Drug Discovery in Emerging Markets (continued)

09:00

Title to be Confirmed
Marcelo Criscuolo, Executive Director, Bio Sidus

09:30

Ranbaxy’s Quest to Become a Research Based International Pharmaceutical Company
Abhijit Ray, Director, New Drug Discovery Research, Ranbaxy Laboratories
Ranbaxy has worked hard to create physical infrastructure, science base and a sustainable strategy for drug discovery research. How this effort has borne fruit will be discussed.

10:00

Taking Companies from Concept to Market
Paul Morril, Co-Founder, Execute Technologies

10:30

Coffee and Networking in the Exhibition Hall

11:15

Title to be Confirmed
Jose Krieger, Heart Institute (InCor), University of Sao Paulo

11:45

Comparative Proteomics Identification of Diagnostic and Prognostic Biomarkers in Leukemias
Eliana Abdelhay, Head of the Bone Marrow Transplantation Laboratory, National Cancer Institute (INCA)
Through proteomics the group analyzed the modifications in the protein profile of bone marrow MNCs from patients in CML phases and in Imatinib Mesylate treatment. They could identify several putative biomarkers of diagnostic, evolution and treatment response that can be use in drug design.

12:15

NFAT Transcription Factors: A Putative New Target in Cancer
João Viola, Head, Division of Cell Biology, National Cancer Institute (INCA)
The Nuclear Factor of Activated T Cells (NFAT) family of transcription factors is activated upon different stimuli that lead to increased intracellular calcium levels. NFAT proteins regulate genes that control many aspects of malignant cell transformation and tumour development. The group investigates the molecular mechanisms by which NFAT regulate tumour-related events and its involvement in oncogenesis.

12:45

Lunch and Networking in the Exhibition Hall

Natural Products

14:00

ChemBioBank, an Academic Project for Drug Discovery in Latin America
Fernando Albericio, Executive Director, Barcelona Science Park, University of Barcelona
The goal of the Latin American ChemBioBank project (LA-CBB) is to build a chemico-biological database, annotated with both biological and bioinformatic data, addressed to the scientific community and to the pharmaceutical and biotech industries.

14:30

High Content Screens for Novel Antipoxviral Agents: Natural Products to the Rescue
Hakim Djaballah, Director, Memorial Sloan Kettering Cancer Centre
The group have developed and validated a high content assay to screen for compounds that would preferentially block viral entry, viral replication, or viral spread upon infecting cell monolayer seeded in 384-well plates with a recombinant vaccinia virus which expresses karyophilic GFP under the control of a viral early/late promoter.

15:00

Using a Luciferase Based Screening Assay to Identify Traditional Chinese Medicine Targeting Nuclear Hormone Receptors
Chiwai Wong, Principal Investigator, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences
Since the activities of nuclear hormone receptors (NHRs) are regulated by small molecule compounds and that Traditional Chinese Medicine (TCM) extracts contain a diverse array of naturally derived chemicals, the group investigated if selective TCM extracts modulate the activities of NHRs.

15:30

Coffee and Networking in the Exhibition Hall

16:15

Bourreria huanita Flowers, a New Antidepressant?
Miguel Torres, Biological Chemist, University of San Carlos
Ethnobotanical and pharmacological studies have preliminarily demonstrated an antidepressant effect in ethanolic extract of dried Bourreria huanita (Boraginaceae) flowers from Guatemala. It’s possible this natural product contains a medically useful molecule and funding is required to continue the chemical analysis and elucidation.

16:45

Post Absorption and Metabolism Compounds: A New Approach to Discover Drug Candidates from Chinese Herbal Medicine
William Jia, VP Research and Associate Professor, Shanghai Innovative Research Centre/University of British Columbia
In a recent study the group has isolated compounds post absorption/metabolism (PAM) of orally taken ginseng. The study showed that those compounds are highly active for neuroprotection and anti-depression.

TimTec and Collaborative Drug Discovery Team Up to Provide Chemically Searchable Natural Products and Derivatives Available to the Scientific Community

TimTec LLC., the international distributor of synthetic organic and natural compounds, and Collaborative Drug Discovery, Inc. (CDD), the community based research information management enterprise, announced today that the CDD web-based software now hosts TimTec’s Natural Product Library and Natural Derivatives Library. The TimTec natural product and derivative compounds are now available as a structure searchable database in the CDD Web2.0 collaborative research information system.

The CDD-TimTec Natural Products Library (NPL-480) and Natural Derivatives Library (NDL-3000) databases comprise almost 3,500 compounds available from TimTec. NPL-480 is a new library of 480 natural compounds composed of pure natural products as lead identifying materials. NDL-3000 elaborates on structural variety of pure natural compounds and includes synthetic compounds and synthetically modified pure natural compounds including, but not limited to, alkaloids, natural phenols, nucleoside analogs, carbohydrates, purines, pyrimidines, flavonoids, steroidal compounds and natural amino acids.

“The growing number of research institutions world-wide now investigating natural products will buoy the discovery of novel chemistry leading to a wealth of therapeutic breakthroughs,” said Dr. Barry Bunin, President of Collaborative Drug Discovery. “It’s natural that TimTec’s laboratories complement CDD’s academic partners in natural products research with a unique commercial source of natural products and diverse derivatives.”

“Beyond our successful compounds libraries, chemical software and drug discovery services, TimTec immediately appreciates the unique advantage and elegance of the CDD system to share our natural product compounds with the growing CDD community,” said Dr. Murat Niyazymbetov founder and President of TimTec.

The TimTec databases join 14 other publicly available data sources in the CDD system with chemical and biological data for over 42,000 agents including:

* 1,700 FDA approved drugs with indications and sponsors
* Over 15,000 compounds with Malaria assay data from 5 public data sources
* More than 850 compounds with Tuberculosis antibacterial activity information
* Over 47,000 Ki values against 699 GPCR targets from the NIMH Psychoactive Drug Screening Program (PDSP) Database
* 25,000 plus compounds available for purchase

About TimTec LLC.
TimTec LLC. – http://www.timtec.net – is a privately held company located in Newark Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. The company has developed strong in-house expertise assembling general and targeted library collections for variety of research purposes. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.

For further information please contact:

Barry Bunin, Ph.D.
President & CEO
Collaborative Drug Discovery (CDD)
1818 Gilbreth Road, Suite 220
Burlingame, CA 94010
650-204-3084
info(at)collaborativedrug.com

Kay Denisova
Business Development
TimTec LLC.
Harmony Business Park Building 301-A
Newark, DE 19711
Tel 302 292 8500
Fax 302 292 8520
info(at)timtec.net

http://www.timtec.net

Direct Screening of Natural Products Extracts Using Mass Spectrometry

Present advances in screening and separation technologies reveal extracts bioactivity with great efficiency and accuracy. Recently reported method of Direct Screening of Natural Products Extracts Using Mass Spectrometry does not require any preparation or fractionation work. Several hundred crude extracts can be screened per one day. Direct bioaffinity screening mass spectrometry method followed by the use of ligand mass information for mass-directed purification makes screen of crude extracts and identification of active compounds precisely possible.

Vu, H., et. al. Direct Screening of Natural Product Extracts Using Mass Spectrometry. J. of Biomol. Screening. 2008, v. 13, 4, 265-275

Plants and plant extracts from Timtec

Mumie – Description and Origin

Though Mumie has been used in folk medicine of different countries for almost two thousand years, there are still many legends regarding its mysterious origin. In Russia serious research has been conducted on Mumie since 1910. This research became even more intense during the past twenty years Government financing supported research that was conducted at major laboratories within the national science and medicine academies of the republics from Mumie’s origin (Middle Asia region of the former USSR (Kirgysia, Tajikistan, and Uzbekistan).

Health organizations aren’t the only groups interested in Mumie. In Russia and many of the former USSR republics, Mumie is considered a strategic material and is used extensively as a performance enhancer within the armed forces (Spetnaz and other elite fighting groups) to help prepare cosmonauts before and during space travel, and as an important part in the restoration programs of national and Olympic-level athletes. It was surprising to me that Mumie was unknown to American athletes until recently when it was introduced by a Russian/American company in 1991.

To locate the origin for the word Mumie, one would have to go back 2,500 years to the time of the ancient philosopher and scientist Aristotle. He proposed the first procedures for testing the compound as well as its initial preparation in grape juice, honey and milk. Mumie is often used by ordinary persons to treat bone fractures and strains of muscles and ligaments, stomach disorders, nervous and cardiovascular problems, the inflammation of joints, and impotence. It is a good bio-stimulator, serves to elevate the immune system and neuro-hormonal regulation, controls oxidation-reduction processes, and has a positive influence on mineral metabolism. The most recent survey of the practical applications of Mumie have come from Moscow through the efforts of Drs. A.A. Altamyshev and B.K. Kortshubelkov and supported by the Russian Committee of Cosmonautics. To date, several hundreds research investigations have been conducted on Mumie which clearly point to its mechanisms of action and its usefulness.

Article about Mumie

Gossypol Biological Properties

Gossypol:

  • is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes.
  • is antimalarial being the selective inhibitor of Plasmodium falciparum (pfLDH over hLDHs), an essential enzyme for energy generation within malarial parasite.
  • posesses proapoptotic properties, probably due to the regulation of the Bax and Bcl2.
  • reversibly inhibits Calcineurin and binds to calmodulin.
  • inhibits replication of the HIV-1 virus.
  • an effective protein kinase C inhibitor.

Read more about Gossypol

MerLion Pharmaceuticals Pte Ltd Announces The Completion Of Merger With Combinature Biopharm AG And Athelas SA; Closure Of US $30 Million Financing Round

MerLion Pharmaceuticals Pte Ltd (MerLion) of Singapore, the world’s leading natural products based drug discovery company, announces that it has completed a merger by exchange of shares with Combinature Biopharm AG (Berlin, Germany) and Athelas SA (Geneva, Switzerland).

SINGAPORE, Singapore | Aug 21, 2006 |
MerLion Pharmaceuticals Pte Ltd (MerLion) of Singapore, the world’s leading natural products based drug discovery company, announces that it has completed a merger by exchange of shares with Combinature Biopharm AG. (Berlin, Germany) and Athelas SA (Geneva, Switzerland). Both European companies become 100% subsidiaries of MerLion whose headquarters and drug discovery research centre is based in Singapore. Drug development of its anti-infective programmes and nuclear magnetic resonance screening activities will be conducted from Berlin.

Dr Tony Buss, CEO of MerLion said “This major expansion of our capabilities, combined with proven drug discovery technologies and promising clinical candidates, position MerLion for its next exciting phase of growth. The company will continue its lead discovery activities in a range of therapeutic areas and will focus on the clinical development of anti-infective drugs.”

Dr Harald Labischinski, CEO of Combinature Biopharm and the new Chief Scientific Officer of MerLion, said “Combinature is very pleased to enter into such a strategic agreement with the leading natural compound research company and is now for the first time in the position to forward the new company’s most advanced antibiotic compounds from late stage pre-clinical development through phase I and phase II clinical. We expect to start our first clinical programmes with a novel mode of action resistance breaker antibiotic as well as with a new subclass of a broad spectrum antibiotic class within a few months from now.”

Dr Christine Deuschel, CEO of Athelas, said “MerLion offers Athelas an exceptional opportunity to progress the development of our novel anti-pathogenicity platform. The integration of Athelas’ DiVi Technology will provide MerLion with a broad and completely novel way of discovering new molecules based on a mechanism of action unexploited to date”.

The company has also completed the first closure of US$ 25M from a US$30M round of financing, which will be completed in full during the fourth quarter of 2006. This funding will propel the company towards an initial public offering within two years. The round, led by Aravis Venture of Switzerland and Bio*One Capital Pte Ltd of Singapore, represents one of the largest private rounds of funding raised for a drug discovery and development company in the region.

Ms. Swee Yeok Chu, CEO of Bio*One Capital and Mr. Jean-Philippe Tripet, Managing Partner of Aravis stated: “We believe that this cross border merger and financing is a landmark deal in Asia that confirms the ability of biotechnology companies to successfully develop from Singapore, capitalising on international alliances, funding from international investors, as well as strong local infrastructure that supports the growth of the company. With this financing and acquisitions, MerLion has now built a profile that compares with the best emerging biotechnology companies globally.”

Other participants in this round of funding include Nomura Research and Advisory, Aurelia Private Equity, Brandenburg Capital, Bioveda Capital, Novartis Venture Fund Mitsubishi Corporation and 3i Group Investment LP.

Michael Toenes of BC Venture GmbH , Juergen Leschke, Management Partner Aurelia Private Equity, Dr. Clemens Doppler of 3i Group Investment LP and Dr Dirk Honold, former CFO of Combinature stated: “The new company is now in the exciting position to further fill and advance the pipeline and to start clinical testing with very promising antibiotic drugs which have already shown exciting profiles. By the transaction the combined entity will have a strategic position to enter into the highly attractive and growing markets in the important area of novel anti-infectives.” In addition to progressing at least two anti-infective candidates into clinical proof of concept studies and developing the growing portfolio of earlier candidates towards the clinic, MerLion will retain its strong partnership alliances in natural products drug discovery and will expand in two main areas;

Novel Anti-Infectives Discovery The acquisition of the anti-infectives DiVi discovery platform of Athelas, which received an award at the 2005 Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), provides MerLion with strong target generation capabilities and proprietary drug discovery screening systems in the area of bacterial pathogenicity.

Nuclear Magnetic Resonance (NMR) Screening The experienced NMR screening group based in Berlin will continue to utilise their expertise and technology with existing partners and in support of ongoing MerLion portfolio projects. This technology is the subject of increasing interest to the industry and is capable of advancing discovery by closely identifying how active compounds interact with drug targets and how these interactions may be optimised. MerLion would like to recognise the professional services provided during this complex transaction by Jones Day, CMS, Wong Partnership, Schellenburg-Wittmer, Vischer, PriceWaterhouseCoopers, Ernst & Young and Maidavale Consulting.

For more information, please visit http://www.merlionpharma.com Contact Chris Molloy, MerLion Pharmaceuticals Pte Ltd, The Capricorn #05-01, Singapore Science Park II, Singapore 117528 Tel: +65 6829 5606 Fax: +65 6829 5601 enquiries@merlionpharma.com

SOURCE: MerLion Pharmaceuticals Pte Ltd

Elsevier MDL and Key Organics partner to improve chemical sourcing

San Ramon, CA, May 8, 2006 – Elsevier MDL, producer of the MDL® Available Chemicals Directory and MDL® Screening Compounds Directory databases, and Key Organics Ltd., a leading supplier of screening compounds and chemical building blocks, have partnered in an effort to provide improved access to timely, accurate information for chemical sourcing and procurement for pharmaceutical, biotechnology and chemistry researchers.

Through its Bionet Research Intermediates catalog, Key Organics supplies novel building blocks for customers to utilize within their discovery chemistry programs. “By working closely with Elsevier MDL, we’re able to ensure that customers are viewing accurate information in Available Chemicals Directory, the most widely used sourcing database,” says Dr. Colin Piper, Business Development Manager, Key Organics.

“Chemists rely on the unmatched coverage of MDL Available Chemicals Directory to find compounds from suppliers, including specialty suppliers, from around the globe,” said Trevor Heritage, Senior Vice President and Chief Science Officer at Elsevier MDL. “For this reason, currency and accuracy are paramount. Our partnership with Key Organics facilitates regular updates of their latest products, including unique compounds that aren’t available elsewhere.”

The partnership between the companies includes an exchange of information that makes it easy and quick for mutual customers to order products from Key Organics using the MDL number from the databases.

The structure-searchable Available Chemicals Directory and the Screening Compounds Directory databases from Elsevier MDL compile detailed product and pricing information for millions of chemical products from hundreds of suppliers around the globe. The databases are accessible via the online DiscoveryGate® platform (allowing researchers to view chemical sourcing information linked with synthetic methodology, bioactivity, metabolism, toxicity, and health and safety information) and are available for in-house installation. Researchers can also leverage the value of Available Chemicals Directory and close supplier relationships with companies like Key Organics through the new MDL® Logistics application, a cradle-to-grave solution for sourcing reagents and managing in-house chemical inventories.

About Key Organics Ltd.

Key Organics was formed in 1986, supplying schemes of novel small-molecule chemistry to customers under confidentiality agreements. Over the last 20 years Key has provided companies worldwide with screening compounds, building blocks and chemistry services. In recent years custom and contract synthesis and lead optimization programs have become an increasingly important part of Key Organics business for clients worldwide. Based at a well-equipped multi-lab site in Camelford, Cornwall, UK, Key Organics employs graduate and Ph.D. chemists, including medicinal chemists, with experience in a wide range of chemical techniques and technologies. Key Organics is able to supply milligram to kilogram quantities of compounds to a high specification. For more information visit www.keyorganics.ltd.uk.

About Elsevier MDL

Elsevier MDL provides informatics, database and workflow solutions that accelerate successful life sciences R&D by improving the speed and quality of scientists’ decision making. Researchers around the world depend on Elsevier MDL for innovative and reliable discovery informatics software solutions and services augmented by 400 Elsevier chemistry and life sciences journals and related products. For more information, visit www.mdl.com. Elsevier is a world-leading publisher of scientific, technical and medical information products and services. For more information visit www.elsevier.com.

Elsevier is part of Reed Elsevier Group plc, a world-leading publisher and information provider. Reed Elsevier’s ticker symbols are REN (Euronext Amsterdam), REL (London Stock Exchange), RUK and ENL (New York Stock Exchange). For more information visit www.reedelsevier.com.

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MDL, DiscoveryGate and Available Chemicals Directory are registered trademarks or trademarks of MDL Information Systems, Inc. (‘Elsevier MDL’) in the United States. All rights reserved. All other trademarks mentioned in this document are the property of their respective owners.

Plant Compounds Inhibit Blood Clotting

After screening hundreds of phytochemicals found in a variety of plants, an ARS scientist has identified, characterized, and synthesized two potentially heart-healthy natural compounds.

These compounds, either in foods or as dietary supplements, may be important for alleviating the symptoms of heart disease related to blood clots. Rigorous testing and regulatory approval is prerequisite.

The research was conducted by ARS biochemist Jae B. Park at the Beltsville ( Maryland) Human Nutrition Research Center’s Phytonutrients Laboratory. Park presented the findings at the 2005 annual meeting of the Federation of American Societies for Experimental Biology, in San Diego, California. The chemical structures of the compounds and their biological activities were filed in a 2005 patent application.

The natural compounds that were synthesized are N-caffeoyldopamine and N-coumaroyldopamine, and their analogs, which are found in sweet peppers, Chinese wolfberry, and cocoa. When tested in larger quantities than likely found in foods, these compounds suppress the mechanism whereby blood platelets stick to blood vessel walls.

Platelets play an important role in blood clotting. They release chemicals that cause the cascade of events that form plugs at the site of injury within blood vessel walls.

Park found that the compounds significantly suppress an adhesive molecule, P-selectin, that glues platelets to white blood cells and blood vessel walls. White blood cells, or leukocytes, move through vessel walls to damaged areas, where they surround and isolate dead tissue and foreign bodies and also produce antibodies.

During the aging process, fatty substances in blood plasma can accumulate inside blood vessel walls. These fat deposits trigger cells to release molecules that cause a chain of events in which immune cells, proteins, and calcium in the bloodstream also adhere to the blood vessel’s inner wall. All these substances combine to form plaque.

Plaque buildup can obstruct arteries and lead to blood clotting. “Blood clotting causes the artery to narrow even more, and in some cases, prevents the blood from supplying the heart muscle, which results in a condition called ¡®acute coronary syndrome,” says Park.

To test the biological activities of the compounds, Park collected blood from mice and exposed it to the compounds. He then studied the compounds’ effects on P-selectin expression and platelet-leukocyte interactions.

“The compounds were found to be potent in their ability to inhibit chemical reactions that lead to blood clotting, such as platelet activation and platelet-leukocyte interaction,” says Park.

While it’s long been known that plant chemicals promote health, they have not been measured in foods to the extent that the essential vitamins have. Therefore, it is unknown whether the quantity of the newly studied compounds normally present in foods is enough to elicit the suppression response. Park is now measuring the compounds in plant sources using newly developed analytical methods. – By Rosalie Marion Bliss, Agricultural Research Service Information Staff.

This research is part of Human Nutrition, an ARS National Program (#107) described on the World Wide Web at www.nps.ars.usda.gov.

Jae B. Park is with the USDA-ARS Phytonutrients Laboratory, 10300 Baltimore Ave., Bldg. 307-C, Room 133, Beltsville, MD 20705; phone (301) 504-8365, fax (301) 504-9456.

Source: ARS USDA

Gossypol. What is it?

What is it?

Gossypol is an herbal medicine used to treat cancer and a female problem called endometriosis. It may also be used by women and men to prevent pregnancy.

Other names for Gossypol include: Gossypium hirsutum and Cottonseed oil.

Ask your doctor, nurse, or pharmacist if you need more information about this medicine or if any information in this leaflet concerns you.

Before Using: Tell your doctor if you.

* are taking medicine or are allergic to any medicine (prescription or over-the-counter (OTC) or dietary supplement)
* are pregnant or plan to become pregnant while using this medicine
* are breastfeeding
* have other health problems, such as high blood pressure or heart or blood vessel disease

Dosage: There are many doses for this medicine. The most common doses for Gossypol are listed below. Ask your doctor if your health problem is not on the list or if the dose is not given for a product you want to use.

* Cancer (adrenal), tablet: 40 to 60 milligrams daily, by mouth (1)
* Cancer (glioma), tablet: Racemic Gossypol 10 milligrams twice daily, by mouth (2)
* Female birth control, gel: put application of a Gossypol acetic acid gel 0.5 milligram/milliliter into vagina before having sex (3)
* Male birth control, tablet: 10 to 20 milligrams (mg) daily for 75 to 180 days or until adequate reduction in sperm count is reached, followed by 35 to 65 mg weekly, by mouth (4-8)

To store this medicine: Keep all medicine locked up and away from children. Store medicine away from heat and direct light. Do not store your medicine in the bathroom, near the kitchen sink, or in other damp places. Heat or moisture may cause the medicine to break down and not work the way it should work. Throw away medicine that is out of date or that you do not need. Never share your medicine with others.

Drug and Food Interactions: Do not take Gossypol without talking to your doctor if you are taking:

* Chloroquine (9)
* Digoxin (1,7,10-12)
* Diuretic (1,7,11)
* Ethanol (13-15)
* Iron (16)
* Isoproterenol (10,17,18)
* Nonsteroidal anti-inflammatory medicine (1,19,20)
* Potassium (7,11,12)

Warnings:

* Do not take Gossypol if you are pregnant or breastfeeding

Side Effects: Stop taking your medicine right away and talk to your doctor if you have any of the following side effects. Your medicine may be causing these symptoms which may mean you are allergic to it.

* Breathing problems or tightness in your throat or chest
* Chest pain
* Skin hives, rash, or itchy or swollen skin
* Severe tiredness (21)
* Muscle weakness or paralysis (21)
* Dry mouth or skin, nausea (upset stomach), vomiting (throwing up), hair loss, bowel problems (1)

References:
1. Flack MR, Pyle RG, Sullen NM et al: Oral gossypol in the treatment of metastatic adrenal cancer. J Clin Endocrinol Metab 1993; 76:1019-1024.
2. Bushunow P, Reidenberg NM, Wasenko J et al: Gossypol treatment of recurrent adult malignant gliomas. J Neuro-Oncology 1999; 43(1):79-86.
3. Ratsula K, Haukkamaa M, Wichmann K et al: Vaginal contraception with gossypol: a clinical study. Contraception 1983; 27(6):571-576.
4. Coutinho EM, Athayde C, Atta G et al: Gossypol blood levels and inhibition of spermatogenesis in men taking gossypol as a contraceptive. A multicenter, international, dose-finding study. Contraception 2000; 61(1): 61-67.
5. Gu ZP, Mao BY, Wang YX et al: Low dose gossypol for male contraception. Asian J Androl 2000; 2(4):283-287.
6. Coutinho EM & Melo JF: Clinical experience with gossypol in non-Chinese men: a follow-up. Contraception 1988; 37(2):137-151.
7. Liu GZ, Lyle KC & Cao J: Clinical trial of gossypol as a male contraceptive drug. Part I. Efficacy study. Fertil Steril 1987; 48(3):459-461.
8. Liu GZ, Lyle K & Cao J: Experiences with gossypol as a male pill. Am J Obstet Gynecol 1987a; 157(4 pt 2):1079-1082.
9. Nwoha PU & Aire TA: The effects of gossypol and chloroquine interaction on serum electrolytes of protein-malnourished rats. Contraception 1995a; 52(4):255-259.
10. Ye YX, Akera T & Ng YC: Modification of the positive inotropic effects of catecholamines, cardiac glycosides and Ca2+ by the orally active male contraceptive, gossypol, in isolated guinea pig heart. Life Sci 1989; 45(20): 1853-1861.
11. Liu GZ, Ch’iu-Hinton K, Cao J et al: Effects of potassium salt or a potassium blocker on gossypol-related hypokalemia. Contraception 1988; 37(2):111-117.
12. Shaozhen A, Guangwei J, Xiaoyun W et al: Gossypol related hypokalemia: clinicopharmacologic studies. Chin Med J 1980; 93:477-482.
13. Akingbemi BT, Rao PV & Aire TA: Chronic ethanol intake may delay the onset of gossypol-induced infertility in the male rat. Andrologia 1997; 29(4):201-207.
14. Messiha FS: Effect of gossypol on kinetics of mouse liver alcohol and aldehyde dehydrogenase. Gen Pharmac 1991; 22(4):573-576.
15. Messiha FS: Behavioral and metabolic interaction between gossypol and ethanol. Toxicol Lett 1991a; 57(2):175-181.
16. Herman DL & Smith FH: Effect of bound gossypol on the absorption of iron by rats. J Nutr 1973; 103(6):882-889.
17. Wu DF, Yu YW, Tang ZM et al: Pharmacokinetics of (+/-)-,(+)-, and (-)-gossypol in humans and dogs. Clin Pharmacol Ther 1986; 39(6):613-618.
18. Ye YX, Akera T & Ng YC: Direct actions of gossypol on cardiac muscle. Eur J Pharmacol 1987; 136(1):55-62.
19.Wagner H, Hikino H & Farnsworth NR (eds): Economic and Medicinal Plant Research. Academic Press, London, England; 1985.
20. DeSmet PAGM, Keller K, Hansel R et al (eds): Adverse Effects of Herbal Drugs 2. Springer-Verlag, Berlin, Germany; 1993:195-208.
21. Wooley RJ: Contraception-a look forward, part II: Mifepristone and gossypol. Contraception 1991; 4:103-113.

Source: Health Library
The information contained in this health library is for reference purposes only. Some services or procedures listed here may not be provided by Genesis Health System entities. Please consult your medical professional for further information.

New Attractiveness of Plant-Derived Natural Products

BioPlanta GmbH and AnalytiCon Discovery GmbH announce their cooperation in the plant-based search for active ingredients.

Leipzig, 09/06/2005 – The aim of the cooperation between BioPlanta and AnalytiCon is to find and to develop new plant-derived active ingredients for use in medicinal therapy. The potential for continuous production of these plant-derived pure compounds – independent of seasonal variation – is of vital importance!

Cell and organ cultures of rare plant species featuring an interesting pattern of substances are produced in bioreactors under clean room conditions. The most promising species are identified by means of a meaningful analytical profiling program in combination with selected biotests and a database comparison of the results. Potential drug candidates contained in these species are efficiently purified and identified. The main focus of interest in this cooperation is on substances with antitumoral properties.

First tests have already shown that in vitro cultures can produce more active agents than plants from wild collections or greenhouse cultures and frequently also yield new ones. The two cooperation partners have combined their technologies, to create an exceptionally effective in vitro production and screening platform.

BioPlanta has gained reputation within the scientific community for the development of its worldwide unique bioreactor technology for the production of plants under clean room conditions and their commercial exploitation. In collaboration with AnalytiCon, this technology is now being used to produce entirely novel groups of natural active ingredients in premium quality and with reliable availability. Innovative active agents can now be rapidly identified and provided in amounts needed for preclinical studies.

For AnalytiCon, the cooperation with BioPlanta represents another significant step towards strengthening the company´s position as leading provider of natural product-based pure compound libraries and collections. From AnalytiCon´s point of view, the reliable resupply which is independent of seasonal variation is a crucial requirement which will considerably boost the attractiveness of herbal ingredients as starting points in the search for active agents.

About AnalytiCon.
AnalytiCon a brand and at the same time successful company is world’s first address for all needs in connection with natural product drug discovery. From prospecting for biosources, via fermentation, extraction and isolation to high throughput structure elucidation, the company provides a vast portfolio of first class services. Beyond that, AnalytiCon produces pure natural compound collections and libraries of synthetic, natural product based molecules carrying relevant bioactive structure elements. The natural product drug discovery platform is complemented by a portfolio of medicinal chemistry services.
For further information see www.ac-discovery.com.

About BioPlanta.
BioPlanta is one of the leading companies in applying bioengineered approaches for discovery, development, and commercialisation of fine chemicals and pharmaceutical compounds using it’s proprietary platform technology. This technology – the BioPlant-System – is particularly suitable for manipulating plant metabolism to generate active compounds with higher value than field plants. The control and variation of cultivation conditions enables customized content and spectra of the specific compounds. This innovative platform technology was installed to manufacture plant derived chemical compounds for pharmaceutical, flavour, and food related industries. It allows the production of high-quality drugs, cost-effective scale up, an efficient screening of new active compounds, and the design of novel drugs.
For further information see www.bioplanta-leipzig.de.

Contact Details:
BioPlanta GmbH
Contact Person: Dr. Dirk Wilken
Deutscher Platz 5
D-04103 Leipzig
Tel.: +49 341 224 58 30
Fax: +49 341 224 58 31
info@bioplanta-leipzig.de
www.bioplanta-leipzig.de

AnalytiCon Discovery GmbH
Contact Person: Dr. Lutz Müller-Kuhrt
Hermannswerder Haus 17
D-14473 Potsdam
Tel.: +49 331 2300 300
Fax: +49 331 2300 333
info@ac-discovery.com
www.ac-discovery.com

In Search Of Bioactive Shapes

Metal complexes that mimic the shapes of natural products show unique properties

Natural products are classic inspirations for, and indeed sources of, therapeutic agents, but they are scarce and often painstaking to make by synthetic means. At the American Chemical Society national meeting this week in Washington, D.C., Eric Meggers of the University of Pennsylvania demonstrated that simple metal complexes could replicate the unique activities of natural products.

more…

SA, India, Brazil in resource deal

Cape Biotech is investigating a possible bio-prospecting partnership which would enable South Africa, Brazil and India to share each other’s resources in order to capitalize on their rich biodiversity.

Bio-prospecting is the search for valuable compounds in nature – plants, animals or micro-organisms – that can assist in the development of new drugs or industrial products.

Dr Mark Fyvie, Managing Director of Cape Biotech recently attended an India-Brazil-South Africa (IBSA) trade delegation where he met with his counterparts in New Delhi, and where a bio-prospecting memorandum of understanding was signed. Fyvie believes the three countries have “huge tracts of biodiversity” that can benefit each other, particularly sharing and collaborating on information platforms.

Biotechnology is one of the core focus areas of the IBSA agreement and representatives from government and industry met to discuss, among other issues, setting up tangible collaborations in the areas of functional genomics and high throughput biology.

“We are starting off very pragmatically and see this as a process that will gradually align the biodiversity objectives of the three countries,” he said.

Fyvie adds that they would like to create the ability for a powerful screening presence for the three countries, thereby enabling access to samples that are being poorly managed.

“This partnership is an agreement to work together going forward and is one of a number of areas of co-operation, where we could optimally exploit value from biodiversity and potentially embark on a joint bio-diversity project,” he says.

“The rollout is envisaged in three stages: sharing and learning, exchanging technologies and technology transfer, and eventually shared facilities among the three countries, but this will only be potentially possible once the alignment of national policies has begun.”

Fyvie was very impressed with India’s investment in skills development.

“There are many highly skilled people in India, which has contributed enormously to the country’s success in the biotech industry. The message is that you cannot over-invest in skills. This coupled with the strong IT industry, as biotech is becoming more information rich, will sustain the future expansion of the biotech sector of the Indian economy.”

Where South Africa is at an “advantage” says Fyvie, is that our infrastructure is better developed, our business culture is more westernised and the language barrier is less of an issue for foreign investors.

“What we don’t have is as big a local market to justify working on and developing expensive products like India, and this is probably why they are the 12th largest biotechnology entity in the world.” he said.

Fyvie hopes that this cooperative effort will allow all three countries to maximize their biodiversity by capitalising on each country’s areas of strength and experience.

Cape Biotech is the Western Cape-based Biotechnology Regional Innovation Centre (Bric) an initiative of the Department of Science and Technology.

I-Net Bridge

AnalytiCon Discovery To Identify New Natural Compounds For Johnson & Johnson Pharmaceutical Research & Development

AnalytiCon to provide a highly purified, fully elucidated natural product compound library

Potsdam, Germany (July 12, 2005) – AnalytiCon Discovery GmbH (AnalytiCon), a specialist in all aspects of natural product drug discovery, announced it has signed an agreement that will provide Johnson & Johnson Pharmaceutical Research & Development, Division of Janssen Pharmaceutica N.V. (J&JPRD), with full access to the unique chemical diversity contained within AnalytiCon’s extensive natural products biological collection. Financial terms of the agreement were not disclosed.

According to the agreement, AnalytiCon will apply its proprietary MEGAbolite® technology to isolate and characterize small molecule compounds from a variety of biosources to find novel and pharmaceutically active compounds on behalf of J&JPRD. AnalytiCon will profile both its own extensive proprietary biological collections and biomaterials provided by Tibotec Pharmaceuticals Ltd. (Tibotec) that are described in ethno-botany for active compounds. In addition, AnalytiCon will carry out all tasks beginning with the acquisition of plant and microbial material, and the isolation and fractionation of the contained natural product compounds up to their analytical characterization. AnalytiCon expects to deliver more than 500 highly purified compounds with fully elucidated structures to J&JPRD and Tibotec for drug discovery screening activities. AnalytiCon also expects to establish the resupply protocol in order to guarantee compound supply for J&JPRD’s follow-up discovery work on an as-needed basis.

“We have had a long business relationship with J&JRPD and we are excited to continue this relationship,” said Dr. Lutz Müller-Kuhrt, CEO of AnalytiCon Discovery GmbH. “We expect to supply a number of novel compounds and we look forward to working with J&JPRD within their discovery process.”

The internationally operating AnalytiCon Discovery GmbH is a worldwide market-leader in the field of structurally fully elucidated natural product libraries. On the basis of its ready-to-screen technology in the field of natural products (MEGAbolite®) and natural product analogues (NatDiverseTM) the company enjoys an exceptional market positioning. AnalytiCon has direct access to roughly a quarter of all known natural compounds worldwide, i.e. in their pure and structurally fully elucidated form. The company is able to offer its clients a complete Supply-Chain-Management from the initial biomaterial to the final lead compound.

About AnalytiCon
AnalytiCon a brand and at the same time successful company, is world’s first address for all needs in connection with natural product drug discovery. >From prospecting for biosources, via fermentation, extraction and isolation to high throughput structure elucidation, the company provides a vast portfolio of first class services. Beyond that, AnalytiCon produces pure natural compound collections and libraries of synthetic, natural product based molecules carrying relevant bio-active structure elements. The natural product drug discovery platform is complemented by a portfolio of medicinal chemistry services. For further information see www.ac-discovery.com.

AnalytiCon Discovery To Identify New Natural Compounds For Johnson & Johnson Pharmaceutical Research & Development

AnalytiCon to provide a highly purified, fully elucidated natural product compound library

Potsdam, Germany (July 12, 2005) – AnalytiCon Discovery GmbH (AnalytiCon), a specialist in all aspects of natural product drug discovery, announced it has signed an agreement that will provide Johnson & Johnson Pharmaceutical Research & Development, Division of Janssen Pharmaceutica N.V. (J&JPRD), with full access to the unique chemical diversity contained within AnalytiCon’s extensive natural products biological collection. Financial terms of the agreement were not disclosed.

According to the agreement, AnalytiCon will apply its proprietary MEGAbolite® technology to isolate and characterize small molecule compounds from a variety of biosources to find novel and pharmaceutically active compounds on behalf of J&JPRD. AnalytiCon will profile both its own extensive proprietary biological collections and biomaterials provided by Tibotec Pharmaceuticals Ltd. (Tibotec) that are described in ethno-botany for active compounds. In addition, AnalytiCon will carry out all tasks beginning with the acquisition of plant and microbial material, and the isolation and fractionation of the contained natural product compounds up to their analytical characterization. AnalytiCon expects to deliver more than 500 highly purified compounds with fully elucidated structures to J&JPRD and Tibotec for drug discovery screening activities. AnalytiCon also expects to establish the resupply protocol in order to guarantee compound supply for J&JPRD’s follow-up discovery work on an as-needed basis.

“We have had a long business relationship with J&JRPD and we are excited to continue this relationship,” said Dr. Lutz Müller-Kuhrt, CEO of AnalytiCon Discovery GmbH. “We expect to supply a number of novel compounds and we look forward to working with J&JPRD within their discovery process.”

The internationally operating AnalytiCon Discovery GmbH is a worldwide market-leader in the field of structurally fully elucidated natural product libraries. On the basis of its ready-to-screen technology in the field of natural products (MEGAbolite®) and natural product analogues (NatDiverseTM) the company enjoys an exceptional market positioning. AnalytiCon has direct access to roughly a quarter of all known natural compounds worldwide, i.e. in their pure and structurally fully elucidated form. The company is able to offer its clients a complete Supply-Chain-Management from the initial biomaterial to the final lead compound.

About AnalytiCon
AnalytiCon a brand and at the same time successful company, is world’s first address for all needs in connection with natural product drug discovery. >From prospecting for biosources, via fermentation, extraction and isolation to high throughput structure elucidation, the company provides a vast portfolio of first class services. Beyond that, AnalytiCon produces pure natural compound collections and libraries of synthetic, natural product based molecules carrying relevant bio-active structure elements. The natural product drug discovery platform is complemented by a portfolio of medicinal chemistry services. For further information see www.ac-discovery.com.

Contact:
AnalytiCon Discovery GmbH
Matthias Hess, Head of Marketing & Sales
Email m.hess@ac-discovery.com
Phone +49 331 2300 300