CHEMISTRY AND PHARMACOLOGY OF SKIN TOXINS FROM FROG ATELOPUS-ZETEKI (ATELOPIDTOXIN-ZETEKITOXIN)

CHEMISTRY AND PHARMACOLOGY OF SKIN TOXINS FROM FROG ATELOPUS-ZETEKI (ATELOPIDTOXIN-ZETEKITOXIN)
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DOI:
10.1016/0041-0101(77)90030-7
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发表时间:
1977-01-01
期刊:
影响因子:
2.8
通讯作者:
FUHRMAN, FA
FUHRMAN, FA
中科院分区:
医学4区
文献类型:
--
作者:
BROWN, GB;KIM, YH;FUHRMAN, FA

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通过一系列步骤从巴拿马青蛙A.zeteki的皮肤中获得纯化的Zetekitoxin,最后阶段使用制备自由流动电泳法。毒性较小的成分(Zetekitoxin C)的LD_(50)为80微克/公斤(小鼠),而毒性较大的成分(Zetekitoxin AB)的LD_(50)为11微克/公斤。这些毒素具有水溶性、低分子量、非多肽、非类固醇和非碳水化合物等性质。哲客毒素明显不同于河豚毒素和奇立曲霉毒素。泽特基对从自己皮肤中获取的毒素具有抵抗力。Zetekitoxin AB(1.5-3微克/公斤)使麻醉的猫和狗持续低血压,在此期间,对肾上腺素和去甲肾上腺素的升压反应不变,但对颈动脉阻断的升压反应减弱。该毒素在0.5微克/升时可阻断电刺激兔耳动脉灌流引起的血管收缩,这种作用可被右旋苯丙胺所拮抗。它不能减少主动膜的收缩,也不能阻断α-雄激素能受体(输精管)。只有在10微克/升以上的高浓度时,它才能部分阻断β-肾上腺素能受体(豚鼠心房)。
Zetekitoxins were obtained in purified form from skins of the Panamanian frog A. zeteki by a series of steps which used preparative free-flowing electrophoresis in the last stages. The minor, less toxic component (zetekitoxin C) had an LD50 of 80 .mu.g/kg (i.p., mouse), and the major, more toxic compont (zetekitoxin AB) had an LD50 of 11 .mu.g/kg. These toxins are water-soluble, low MW, non-polypeptide, non-steroid and non-carbohydrate in nature. The zetekitoxins are clearly different from tetrodotoxin and chiriquitoxin. A. zeteki were resistant to toxin obtained from their own skins. Zetekitoxin AB (1.5-3 .mu.g/kg) produced sustained hypotension in anesthetized dogs and cats, during which time the pressor response to epinephrine and norepinephrine was unchanged, but that to carotid occlusion was reduced. The toxin at a concentration of 0.5 .mu.g/1 blocked vasoconstriction caused by electrical stimulation of perfused rabbit ear arteries, and this effect was antagonized by dextroamphetamine. It did not reduce contraction of the nicitating membrane or block .alpha.-andrenergic receptors (vas deferns). It partially blocked .beta.-adrenergic receptors (guinea pig atria) only in high concentrations above 10 .mu.g/1.