Applicatory study of natural compounds with receptor blocking effect to vasodilator

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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.