PHARMACOLOGICALLY ACTIVE COMPOUNDS FROM AMPHIBIANS AND OTHER NATURAL SOURCES

天然产品提供了广泛的生物活性剂，许多 其具有独特的药理活性和治疗作用 潜力 在提取物中已鉴定出300多种生物碱 从两栖动物的皮肤。 其中包括Batrachotoxins， 钠通道激活剂，Histrionicotoxins，非竞争性 烟碱受体通道复合物和钾的阻断剂 通道和短小毒素，具有肌强直和强心活性 这是由于对钠通道关闭的抑制作用。 进一步 生物碱包括2，5-二取代十氢喹啉，5，8- 二取代的吲嗪，1，4-二取代的喹嗪，3，5- 二取代的吡咯烷类、pumiliotoxins、homopumiliotoxins和 别普米毒素和三环生物碱，包括吡咯里西啶 肟，环戊[B]喹嗪，cocinellines，和有效的 非阿片类药物地棘蛙素。 同倍体肉毒毒素是在 新几内亚鸟的羽毛、皮肤和肌肉。 表征 生物碱在非dendrobatid两栖动物表明，生物合成 某些石斛生物碱的途径分别在一个 蟾蜍科、肌蟾科两栖动物的一个谱系（属） 和蛙科，并在一个谱系中导致四个属的家庭 树蛙科 人工饲养的老鼠体内缺乏生物碱 树蛙仍然是个谜 地棘蛙素的合成路线和 已经开发了吡咯里西啶肟。 无相关性 抑制蛙毒素结合和抗惊厥活性之间的关系 对于一系列的carbetapentane类似物。 疾病也在进行中。

Natural products provide a wide range of biologically active agents, many of which have unique profiles of pharmacological activity and therapeutic potential. Over three hundred alkaloids have been identified in extracts from amphibian skins. These included batrachotoxins, which are potent activators of sodium channels, histrionicotoxins, which are noncompetitive blockers of nicotinic receptor channel complexes and of potassium channels, and pumiliotoxins, which have myotonic and cardiotonic activity due to inhibitory effects on closing of sodium channels. Further alkaloids included 2,5-disubstituted decahydroquinolines, 5,8- disubstituted indolizidines, 1,4-disubstituted quinolizidines, 3,5- disubstituted pyrrolizidines, pumiliotoxins, homopumiliotoxins and allopumiliotoxins, and tricyclic alkaloids, including pyrrolizidine oximes, cyclopenta[b]quinolizidines, cocinellines, and the potent nonopioid analgetic epibatidine. Homobatrachotoxin has been discovered in feathers, skin and muscle of a New Guinean bird. Characterization of alkaloids in non-dendrobatid amphibians indicated that the biosynthetic pathways to certain dendrobatid alkaloids have evolved separately in one lineage (genus) of amphibians from the families Bufonidae, Myobatrachidae and Ranidae and in a lineage leading to four genera in the family Dendrobatidae. The lack of alkaloid production in captive-raised dendrobatid frogs remains an enigma. Synthetic routes to epibatidine and to the pyrrolizidine oximes have been developed. There was no correlation between inhibition of batrachotoxin binding and anticonvulsant activity for a series of analogs of carbetapentane.individuals devoid of renal disease was also undertaken.