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Effets inhibiteurs de l'acide ascorbique sur la métalloprotéinase de venin de serpent (SVMP) provenant du venin d'Indian Echis carinatus: informations tirées de la modélisation moléculaire et d'études de liaison.

Le traitement antivenin classique n’est pas en mesure de protéger les complications de la morsure de vipère et présente des limitations telles que l’anaphylaxie et la maladie sérique. Les métalloprotéinases de venin de serpent sont responsables de lésions tissulaires locales et d'hémorragies au site piqué lors de l'envenimation par la vipère, ce qui a conduit à une recherche persistante d'inhibiteurs de la métalloprotéinase. Nous rapportons ici les effets inhibiteurs de l'acide ascorbique sur la métalloprotéinase du venin d'Echis carinatus, à la fois in silico et in vitro. L'acide ascorbique a efficacement inhibé l'activité protéolytique du venin d'E. Carinatus d'une manière dépendante de la dose. Des études d'interaction de l'acide ascorbique avec de l'ecarine purifiée à l'aide de la calorimétrie par titrage isotherme ont montré une énergie de liaison et une énergie favorables. La fixation moléculaire de l’acide ascorbique avec l’écarine a révélé des interactions importantes avec les résidus au niveau de la poche du site actif de l’écarine. Il a été observé que le ligand se comporte comme un inhibiteur chélatant. Ainsi, l’échafaudage structural de l’acide ascorbique de l’épine dorsale peut être utilisé comme un élément de base dans la conception de molécules analogues à des médicaments pour la gestion des morsures de vipère.


Source: https://www.ncbi.nlm.nih.gov/pubmed/30276921


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