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[从冬眠地松鼠大脑中分离出的生物活性肽]

[Biologically active peptides isolated from the brain of hibernating ground squirrels].

作者信息

Ziganshin R Kh, Sviriaev V I, Vas'kovskiĭ B V, Mikhaleva I I, Ivanov V T, Kokoz Iu M, Alekseev A E, Korystova A F, Sukhova G S, Emel'ianova T G

出版信息

Bioorg Khim. 1994 Aug-Sep;20(8-9):899-918.

PMID:7826417
Abstract

More than 20 peptides have been isolated and sequenced from the brain of hibernating ground squirrel Citellus undulatus. Some of the isolated peptides were chemically synthesized and investigated for the spectrum of biological activity. One of the isolated peptides, neokyotorphin (Thr-Ser-Lys-Tyr-Arg), earlier known as a weak analgetic, is found to have a cardiotropic and thermoregulatory activity. Neokyotorphin activates in vitro voltage-dependent calcium and blocks ATP-dependent potassium currents in the frog atrial fibres. Intraperitoneal injection of this peptide in hibernating ground squirrels speeds up the arousal of animals increasing sharply the heart rate and oxygen consumption. Intraperitoneal and intranasal administrations of neokyotorphin in rats raises body temperature in thermoneutral conditions (26-28 degrees C) exerting no effects at low (4-6 degrees C) and high (31-32 degrees C) environmental temperatures. Another isolated peptide, Asp-Tyr, blocks the inward voltage-dependent calcium current in the frog atrial fibres and slightly increases the outward potassium current. Sulfated analogue of this dipeptide (aspartyl-O-sulfate-tyrosine) more effectively blocks the inward voltage-dependent calcium current in the frog atrial fibres and have no effects on the outward potassium current.

摘要

从冬眠地松鼠(Citellus undulatus)的大脑中已分离并测序出20多种肽。部分分离出的肽经化学合成,并对其生物活性谱进行了研究。其中一种分离出的肽,新酪酪肽(苏氨酸-丝氨酸-赖氨酸-酪氨酸-精氨酸),此前被认为是一种弱镇痛药,现已发现它具有心脏otropic和体温调节活性。新酪酪肽在体外可激活青蛙心房纤维中的电压依赖性钙通道,并阻断ATP依赖性钾电流。给冬眠的地松鼠腹腔注射这种肽可加速动物苏醒,显著提高心率和耗氧量。给大鼠腹腔和鼻内注射新酪酪肽,在热中性条件(26 - 28摄氏度)下可使体温升高,而在低温(4 - 6摄氏度)和高温(31 - 32摄氏度)环境温度下则无作用。另一种分离出的肽,天冬氨酸-酪氨酸,可阻断青蛙心房纤维中的内向电压依赖性钙电流,并略微增加外向钾电流。这种二肽的硫酸化类似物(天冬氨酰-O-硫酸-酪氨酸)能更有效地阻断青蛙心房纤维中的内向电压依赖性钙电流,且对外向钾电流无影响。

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