D'Suze G, Sevcik C, Ramos M
Laboratory of Cellular Neuropharmacology, Instituto Venezolano de Investigaciones Cientificas (IVIC), Caracas, Venezuela.
Toxicon. 1995 Mar;33(3):333-45. doi: 10.1016/0041-0101(94)00171-4.
Four toxic polypeptidic fractions (TdF-I-IV) were purified from the venom of the Venezuelan scorpion Tityus discrepans by means of gel filtration on Sephadex G'-50. The peptides have mol. wts of approx. 6000 and normalized elution volumes (Vn = Elution volume/Total column volume) of: TdF-I = 0.27 (0.26, 0.28), n = 13; TdF-II = 0.40 (0.39, 0.41), n = 15; TdF-III = 0.57 (0.56, 0.59), n = 14, and TdF-IV = 0.68 (0.67, 0.70), n = 13 (median and its 95% confidence interval, n = number of elutions used to calculate the median). Mice (white, male, 16-19 g, IVIC strain) were injected with these fractions and sacrificed 48 hr later. No toxicity was observed when fraction I (0.93 microgram/g mice) or IV (2.51 micrograms/g mice) was injected i.p. into mice. TdF-II (9 to 50 micrograms/g mice) produced sialorrhea, dyspnea and death 1 hr after i.p. injection. Light microscopy of the pancreas revealed that TdF-III (3.42 micrograms/g mice) produced structural modifications such as acinar cell vacuolization, degranulation and interstitial swelling; these changes are characteristic of acute pancreatitis. No effects on the islets of Langerhans or the pancreatic ducts were observed. TdF-III had no overt muscarinic effects when injected i.p. into mice. On the neuromuscular preparation of the frog (Hyla crepitans) TdF-I blocked neuromuscular transmission at the postsynaptic membrane; TdF-II depolarized the muscle membrane by opening sodium channels and TdF-IV prolonged action potentials, suggesting potassium channel blockage.
通过在葡聚糖凝胶G - 50上进行凝胶过滤,从委内瑞拉蝎子Tityus discrepans的毒液中纯化出四种有毒多肽组分(TdF - I - IV)。这些肽的分子量约为6000,归一化洗脱体积(Vn = 洗脱体积/总柱体积)分别为:TdF - I = 0.27(0.26,0.28),n = 13;TdF - II = 0.40(0.39,0.41),n = 15;TdF - III = 0.57(0.56,0.59),n = 14,以及TdF - IV = 0.68(0.67,0.70),n = 13(中位数及其95%置信区间,n = 用于计算中位数的洗脱次数)。将这些组分注射到小鼠(白色,雄性,16 - 19 g,IVIC品系)体内,48小时后处死。腹腔注射组分I(0.93微克/克小鼠)或组分IV(2.51微克/克小鼠)时,未观察到毒性。腹腔注射TdF - II(9至50微克/克小鼠)1小时后会导致流涎、呼吸困难和死亡。胰腺的光学显微镜检查显示,TdF - III(3.42微克/克小鼠)会引起结构改变,如腺泡细胞空泡化、脱颗粒和间质肿胀;这些变化是急性胰腺炎的特征。未观察到对胰岛或胰管有影响。腹腔注射TdF - III时,对小鼠没有明显的毒蕈碱样作用。在青蛙(雨蛙)的神经肌肉标本上,TdF - I在突触后膜阻断神经肌肉传递;TdF - II通过打开钠通道使肌膜去极化,而TdF - IV延长动作电位,提示钾通道阻滞。