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Applicatory study of natural compounds with receptor blocking effect to vasodilator

具有受体阻断作用的天然化合物在血管扩张剂中的应用研究

基本信息

批准号：
10557228
负责人：
OHIZUMI Yasushi
金额：
$ 8.64万
依托单位：
TOHOKU UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B)
财政年份：
1998
资助国家：
日本
起止时间：
1998 至 1999
项目状态：
已结题

项目摘要

Hypertension triggers various vascular diseases such as arteriosclerosis, angina or myocardial infarction. Since in general, it is necessary to administer vasodilator chronically to patients in hypertension, it is socially important to develop good medicine with less side effects. Human beings have been utilize vegetoanimal products as medicine for thousands of years. Furthermore, there are huge amount of synthesized medicines which are originated from natural products. Our aim of this study is to seak lead compound from natural resources such as traditional medicinal plants or marine organisms, synthesize derivatives and develop good vasodilator with small side effects. We have discovered physiologically active isolated from natural resources which act on α-adrenergic receptor, serotonergic receptor or muscle contractile proteins. In isolated rat fundus, guinea pig trachea or rabbit aorta, nantenine, isolated from methanol extract of nanten fruit, moved concentration-contraction curve of serotonin toward right in parallel manner. Nantenine also moved concentration-contraction curve of phenylephrine toward right. Therefore, it is suggested that nantenine possessing both α-adrenergic- and serotonergic-blocking effects. We have also successfully isolated new types of anti-serotonergic and anti-histaminergic contents from Thai medicinal plant Garcinia mangostana, traditionally used as anti-inflammatory. γ-Mangostin, content showing anti-serotonergic effect, showed not only inhibited contraction in aorta, but also showed anti-serotonergic effect in central nerve system. We also studied the central effect of compound which affect on CaィイD12+ィエD1 release sarcoplasmic reticulum, the key of excitation-contraction coupling in muscle.

高血压会引发各种血管疾病，如动脉硬化、心绞痛或心肌梗死。一般来说，高血压患者长期服用血管扩张剂是必要的，因此开发副作用较少的好药具有重要的社会意义。几千年来，人类一直使用动植物产品作为药物。此外，还有大量来自天然产物的合成药物。本研究的目的是从传统的药用植物或海洋生物等自然资源中提取先导化合物，合成衍生物，开发副作用小的良好的血管扩张剂。我们已经发现从自然资源中分离出来的作用于α-肾上腺素能受体、5-羟色胺能受体或肌肉收缩蛋白的生理活性物质。在大鼠眼底、豚鼠气管和兔主动脉上，从南藤果甲醇提取物中分离得到的南藤碱使5-羟色胺的浓度-收缩曲线平行右移。南替宁还使去氧肾上腺素的浓度-收缩曲线右移。因此，我们认为南藤碱同时具有α-肾上腺素能和5-羟色胺能阻断作用。我们还成功地从泰国药用植物山竹中分离出了新型的抗5-羟色胺能和抗组胺能成分，传统上用于抗炎。γ-芒果苷具有抗5-羟色胺作用，不仅对主动脉收缩有抑制作用，对中枢神经系统也有抗5-羟色胺作用。我们还研究了影响钙ィイD12+ィエD1释放肌浆网的中枢作用，肌浆网是肌肉兴奋-收缩偶联的关键。