Exploring the global animal biodiversity in the search for new drugs -Amphibians

D. Mans, J. Pawirodihardjo, M. Djotaroeno, P. Friperson
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引用次数: 2

Abstract

Many breakthrough drugs have been developed from plants with medicinal properties on the basis of ethnopharmacological information. In the search for structurally novel and mechanistically unique lead compounds, drug discovery and development progams are now also paying attention to the myriad of bioactive molecules provided by the animal biodiversity. A well-known example emerging from these efforts is the breakthrough angiotensin-converting enzyme inhibitor captopril used for the treatment of hypertension and congestive heart failure. Captopril has been developed as an analogue of bradykinin in the venom of the Brazilian pit viper Bothrops jararaca (Viperidae) following the observation that the latter agent lowered blood pressure by vasodilation. In the mean time, dozens of clinically useful and potentially therapaeutically applicable compounds from animal origin have been identified. The skin gland secretions of amphibians have been refined during millions of years of evolution to highly efficient defensive chemicals. These compounds have remarkable pharmacological activities and may also represent a treasure chest of potentially novel drugs against pathophysiological conditions. This paper addresses the importance of bioactive compounds in the skin secretions of frogs, toads, salamanders, newts, and caecilians, and elaborates on the therapeutic potential of some of them as anti-alzheimer, cardiotonic, antidiabetic, anti-HIV, analgesic, antimicrobial, and antiparasitic compounds.
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探索全球动物生物多样性,寻找新药——两栖类
基于民族药理学信息,从具有药用特性的植物中开发出了许多突破性药物。在寻找结构新颖和机制独特的先导化合物的过程中,药物发现和开发项目现在也开始关注动物生物多样性提供的无数生物活性分子。从这些努力中出现的一个著名的例子是突破性的血管紧张素转换酶抑制剂卡托普利用于治疗高血压和充血性心力衰竭。卡托普利是巴西蝮蛇Bothrops jararaca(蝮蛇科)毒液中缓动肽的类似物,在观察到后者通过血管扩张降低血压后被开发出来。与此同时,已经鉴定出数十种临床有用和潜在治疗应用的动物源性化合物。在数百万年的进化过程中,两栖动物的皮肤腺分泌物已经被提炼成高效的防御化学物质。这些化合物具有显著的药理活性,也可能代表了一个潜在的新型药物对抗病理生理条件的宝库。本文阐述了青蛙、蟾蜍、蝾螈、蝾螈和无尾螈皮肤分泌物中生物活性化合物的重要性,并详细阐述了其中一些生物活性化合物的治疗潜力,如抗阿尔茨海默病、强心剂、抗糖尿病、抗艾滋病毒、镇痛、抗菌和抗寄生虫化合物。
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