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2018-10-11 - Colloque/Présentation - communication orale - Anglais - 1 page(s)

Duez Pierre , "Pharmacology and chemistry of phytomedicines:a clue for the rational design of innovative drugs?" in Journée Scientifique de la Société Royale de Chimie, Mons, Belgique, 2018

  • Codes CREF : Chimie analytique (DI1314), Pharmacognosie (DI3410), Sciences pharmaceutiques (DI3400), Pharmacologie (DI3420), Toxicologie pharmaceutique (DI3440)
  • Unités de recherche UMONS : Chimie thérapeutique et Pharmacognosie (M136)
  • Instituts UMONS : Institut des Sciences et Technologies de la Santé (Santé)

Abstract(s) :

(Anglais) Herbal medicines are an acknowledged source for original, complex and biologically active molecules; their traditional use is also an indication that some biological activities are possible, yielding clues to pharmacological models that move on drug discovery to new avenues of research. Indeed, medicinal plants have been and are still a major source of drug discovery, including many of the drugs used today in virtually all therapeutic areas (morphine derivatives, local anesthetics, muscle relaxants, anticholinergics, anticancer agents, antimalarials,…). Between 1981 and 2014, natural sources still accounted, directly or indirectly, for 51 % of the new chemical entities registered in the USA (Newman et Cragg, 2016). For the last 20 years however, drug discovery has become a time-consuming (~ 10 - 15 years), difficult (9/10 drug candidates fail at an advanced development stage) and expensive ($2.56 Bn/drug; DiMasi et al, 2016) activity. Indeed, the modern discovery process for new small molecules encounters drastic conditions: drugability, easiness of production, metabolic stability, a low probability for multi-targets interaction, a low probability for drug transporters and metabolizing enzymes interactions, the existence or probability of a market, a proven advantage over existing drugs and a competition in priorities with high-profit biological drugs. Also, many late-stage withdrawals of molecules depend on unexpected or difficult-to-predict toxicities. As a consequence, many companies tend to concentrate on proven chemistries and to withdraw from more adventurous studies. Taking into account this difficult landscape, we'll try to present less obvious aspects of the research on herbal medicines, with some methodologies, initiatives, advances or drawbacks, and their link with the discovery of tomorrow's drugs: bioguided isolation, dereplication, hit expansion, antifibrotic strategies, indirect antimicrobial schemes, holistic approaches and WHO strategies for neglected populations. Newman D.J. and Cragg G.M. (2016) "Natural Products as Sources of New Drugs from 1981 to 2014", Journal of Natural Products 79, 629-661 DiMasi J.A., Grabowski H.G., Hansen R.A. (2016) "Innovation in the pharmaceutical industry: new estimates of R&D costs", Journal of Health Economics, 47, 20-33