Bio Screening Industry News

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

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 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

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

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:

• 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 (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

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.

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