Curare is a mixture of naturally occurring alkaloids found in various South American plants and used...

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Curare is a mixture of naturally occurring alkaloids found in various South American plants and used as arrow poisons by indians. The most important component is tubucurarine. It does not survive the stomach and that’s why indians could eat the meat of curare poisened animals. Antagonist of Acetylcholine receptor and very effective at neuromuscular junction En 1856, Claude Bernard a démontré que le curare bloque la jonction neuromusculaire, mais sans affecter le muscle lui même. Le mot Curare vient en fait d'un mot en langue indigène «ourari» qui signifie la mort qui tue tout bas. L’approche empirique

Transcript of Curare is a mixture of naturally occurring alkaloids found in various South American plants and used...

Page 1: Curare is a mixture of naturally occurring alkaloids found in various South American plants and used as arrow poisons by indians. The most important component.

Curare is a mixture of naturally occurring alkaloids found in various South American plants and used as arrow poisons by indians. The most important component is tubucurarine. It does not survive the stomach and that’s why indians could eat the meat of curare poisened animals. Antagonist of Acetylcholine receptor and very effective at neuromuscular junction

En 1856, Claude Bernard a démontré que le curare bloque la jonction neuromusculaire, mais sans affecter le muscle lui même.

Le mot Curare vient en fait d'un mot en langue indigène «ourari» qui signifie la mort qui tue tout bas.

L’approche empirique

Page 2: Curare is a mixture of naturally occurring alkaloids found in various South American plants and used as arrow poisons by indians. The most important component.

Atropa belladonna

Plant très toxique. include dilated pupils, tachycardia, hallucinations, blurred vision, loss of balance, a feeling of flight, staggering, a sense of suffocation, paleness followed by a red rash, flushing, husky voice, extremely dry throat, constipation, urinary retention, and confusion.

Utilisé en cosmétiqueInduit la dilatation des pupilles ce que rends les femmes plus attractives

Bella donna = belle femme

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SYDNEY RINGER, M.D.(around 1890)

Pitury

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QUITE recently a student of University College, London, whose, name we have unfortunately forgotten, gave us a small packet containing a few twigs and broken leaves of the powerful and interesting drug, Pituri. These we placed in Mr Gerard’s hands, and he kindly made first an extract from which he obtained a minute quantity of an alkaloid, and with this he made a solution containing one part of the alkaloid to twenty of water.

The use of pituri is confined to the men of a tribe called Mallutha.. Before any serious undertaking, they chew these dried leaves, using about a tea-spoonful. A few twigs are burnt and the ashes mixed with the leaves. After a slight mastication the bolus is placed behind the ear (to increase it is supposed its strength), to be again chewed from time to time, the whole being at last swallowed. The native after this process is in a sufficiently courageous state either to transact business or to fight. When indulged in to excess, it is said to induce a condition of infuriation. In persons not accustomed to its use pituri causes severe headache.

Page 5: Curare is a mixture of naturally occurring alkaloids found in various South American plants and used as arrow poisons by indians. The most important component.

Henry (Hallett) Dale

Extraits de Claviceps purpurea, l’ergot de seigle, un champion qui produit des alcoloides polycyclique dont le dérivate LSD (lysergic acid diethylamide ) est le mieux connu, ainsi que ergotamine dans le traitement de migraine)

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Alexander Fleming remarque un halo d’inhibition autour d’un moisissure bleu verte qui a contaminé une culture de Staphylococcus (bactérie). Il en conclut que la moisissure produit une substance qui inhibe la croissance bactérienne. Il cultive cette moisissure et découvre qu’il s’agit de Penicillium notatum.

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Alexander Fleming

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Vers une approche rationnelle

Prix Nobel de médecine et physiologie en 1988« For their discoveries of important principles for drug treatment »

J Black(Kings College London)

GB Elion(Wellcome)

GH Hitchings(Wellcome)

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propranolol

(adrenaline- receptor antagonist)

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Cimetidine (Histamine-2 receptor antagonist)

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Mercaptopurine (purine analogue)

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Acyclovir (purine analogue)

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EXPLOITABLE DIFFERENCEInfection d’une cellule épitheliale par le virusHerpesSimplex

Acyclovir est uniquement actif dans les cellules infectées car elles expriment la thymidine kinase virale, essentiel pour l’activation de l’acyclovir

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Zidovudine (AZT)

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Le groupe azoture augmente la nature lipophile de l'AZT, lui permettant de traverser les membranes cellulaires facilement par diffusion et de traverser de ce fait également la barrière barrière hémato-encéphalique. Les enzymes cellulaires (kinases) convertissent l'AZT en la forme active du 5'-triphosphate. Les études ont prouvé que l'arrêt des brins d'ADN ainsi formées est le facteur spécifique dans l'effet inhibiteur.

L’enzyme virale transcriptase inverse fabrique de l’ADN viral à partir de l’ARN du VIH en détournant des nucléotides normalement destinés à la cellule, cette synthèse de l’ADN viral lançant, en temps normal, alors la réplication du VIH dans la cellule

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Nouvelles cibles pour les interventions thérapeutiques contre le cancer

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Cellules cancéreuses (myoblastes)

Leucémie chronique myéloïde

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Médicament(inhibiteur de l’enzyme c-Abl)

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