毒理性
识别和使用:蝙蝠毒素是一种神经毒性的甾体生物碱,最初从哥伦比亚的毒箭蛙中分离出来,后来在巴布亚新几内亚的某些鸣禽中发现。人们认为这两类脊椎动物群体并非从头开始产生毒素,而是很可能从饮食来源中储存这些毒素。人体研究:蝙蝠毒素是电压门控钠通道的强效调节剂,导致神经和肌肉不可逆的去极化,纤维颤动,心律不齐,最终导致心脏衰竭。自从被发现以来,田野研究者还报告说,当他们的皮肤接触到这种毒素后,会出现麻木感。动物研究:当P. terribilis在笼养中时,蝙蝠毒素的水平往往会降低,但即使在笼养6年后,这些青蛙的毒性仍然至少是本地人用于毒害吹管箭的其他叶蛙属物种的五倍。在笼养中成熟的第一代后代中检测不到蝙蝠毒素。从野外捕获的青蛙和无毒的第一代青蛙的神经和肌肉制剂都对蝙蝠毒素不敏感。控制钠通道激活和渗透性的调节位点似乎已经被最小程度地改变,以防止与蝙蝠毒素的相互作用,但对青蛙不会自然接触的其他钠传导激活剂(如藜芦碱、灰毛毒素)仍然敏感。
IDENTIFICATION AND USE: Batrachotoxins are neurotoxic steroidal alkaloids first isolated from a Colombian poison-dart frog and later found in certain passerine birds of New Guinea. Neither vertebrate group is thought to produce the toxins de novo, but instead they likely sequester them from dietary sources. HUMAN STUDIES: Batrachotoxin is a potent modulator of voltage-gated sodium channels, leading to irreversible depolarization of nerves and muscles, fibrillation, arrhythmias and eventually cardiac failure. Since its discovery, field researchers also reported numbness after their skin came into contact with this toxin. ANIMAL STUDIES: Levels of batrachotoxin tend to be reduced when P. terribilis is maintained in captivity, but even after being confined for up to 6 years, these frogs were still at least five times more toxic than other Phyllobates species used by natives for poisoning blowgun darts. Batrachotoxin was not detectable in F1 progeny reared to maturity in captivity. Nerve and muscle preparations from wild-caught frogs and from the nontoxic F1 frogs were both insensitive to batrachotoxin. The regulatory site controlling sodium-channel activation and permeability appears to have been minimally altered to prevent interaction with batrachotoxin, but is still sensitive to other sodium conductance activators (veratridine, grayanotoxin) to which the frogs are not exposed naturally.
来源:Hazardous Substances Data Bank (HSDB)