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目的研究薯蓣皂苷元及其衍生物的制备及对豚鼠离体气管平滑肌的作用。方法采用酰化和还原的方法合成衍生物;药理学实验在豚鼠离体气管模型上进行。结果合成了11个薯蓣皂苷元衍生物(化合物Ⅰ~Ⅺ);薯蓣皂苷元及其衍生物对豚鼠离体气管平滑肌都有不同程度的舒张作用。结论经1HNMR、13CNMR鉴定了所合成衍生物的结构;首次发现薯蓣皂苷元对离体豚鼠气管条有舒张作用,其3位的结构修饰可以提高其活性。
Objective To study the preparation of diosgenin and its derivatives and its effect on isolated tracheal smooth muscle of guinea pigs. Methods The derivatives were synthesized by acylation and reduction methods. Pharmacological experiments were performed on guinea pig tracheal models. Results Eleven diosgenin derivatives (compounds Ⅰ ~ XI) were synthesized. Diosgenin and its derivatives exerted a relaxing effect on isolated tracheal smooth muscle of guinea pigs. Conclusions The structure of the synthesized derivatives was identified by 1HNMR and 13CNMR. Diosgenin was found to relax diaphragms of guinea pig trachea strips for the first time, and its structural modification at position 3 could enhance its activity.