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山竹黄酮及其衍生物的药理学特性。

Pharmacological profile of mangostin and its derivatives.

作者信息

Shankaranarayan D, Gopalakrishnan C, Kameswaran L

出版信息

Arch Int Pharmacodyn Ther. 1979 Jun;239(2):257-69.

PMID:314790
Abstract

Mangostin (M), a naturally occurring xanthone in the rinds of the fruits of Garcinia mangostana Linn. (Guttiferae) and its derivatives such as 3-0-methyl mangostin (MM), 3,6-di-O-methyl mangostin (DM), 1-isomangostin (IM), mangostin triacetate (MT), mangostin 3,6-di-O-(tetra acetyl) glucoside (MTG) and mangostin-6,6-di-O-glucoside (MOG) were screened for various pharmacological effects in experimental animals. With the exception of DM all the test compounds produced CNS depression characterised by ptosis, sedation, decreased motor activity, potentiation of pentobarbital sleeping time and ether anaesthesia in mice and rats. None of the compounds exhibited analgesic, antipyretic and anticonvulsant effects. With the exception of MOG, none of the test compounds produced significant effects on the cardiovascular system of frogs and dogs. MOG produced myocardial stimulation and a rise in blood pressure which was partially blocked by propranolol. M, IM and MT produced pronounced antiinflammatory activity both by intraperitoneal and oral routes in rats as tested by carrageenininduced hind paw oedema, cotton pellet implantation and granuloma pouch techniques. Antiinflammatory activity for M, IM and MT was observed even in bilaterally adrenalectomised rats. M, IM and MT did not produce any mast cell membrane stabilising effect and the degranulation effect of polymyxin B, diazoxide and Triton X-100 on rat peritoneal mast cells in vitro was not prevented. M, IM and MT did not alter the prothrombin time of albino rats. M alone produced significant antiulcer activity in rats.

摘要

山竹黄酮(M)是藤黄科植物山竹(Garcinia mangostana Linn.)果皮中天然存在的一种氧杂蒽酮,对其衍生物如3-O-甲基山竹黄酮(MM)、3,6-二-O-甲基山竹黄酮(DM)、1-异山竹黄酮(IM)、山竹黄酮三乙酸酯(MT)、山竹黄酮3,6-二-O-(四乙酰)葡萄糖苷(MTG)和山竹黄酮-6,6-二-O-葡萄糖苷(MOG)在实验动物中进行了多种药理作用的筛选。除DM外,所有受试化合物均产生中枢神经系统抑制作用,表现为小鼠和大鼠眼睑下垂、镇静、运动活性降低、戊巴比妥睡眠时间延长和乙醚麻醉增强。这些化合物均未表现出镇痛、解热和抗惊厥作用。除MOG外,受试化合物对青蛙和狗的心血管系统均未产生显著影响。MOG产生心肌兴奋和血压升高,普萘洛尔可部分阻断这种作用。通过角叉菜胶诱导的后爪水肿、棉球植入和肉芽肿袋技术检测,M、IM和MT经腹腔和口服途径在大鼠中均产生显著的抗炎活性。即使在双侧肾上腺切除的大鼠中也观察到M、IM和MT的抗炎活性。M、IM和MT未产生任何肥大细胞膜稳定作用,体外多粘菌素B、二氮嗪和 Triton X-100对大鼠腹膜肥大细胞的脱颗粒作用也未被阻止。M、IM和MT未改变白化大鼠的凝血酶原时间。仅M在大鼠中产生显著的抗溃疡活性。

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