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目的设计合成具有心肌保护作用的葡萄糖硫苷化合物。方法以四乙酰基-α-溴代葡萄糖为原料合成四乙酰基-β-硫代葡萄糖,再与取代溴苄反应制得葡萄糖硫苷,最后脱去乙酰基得到目标化合物。通过体外心肌细胞的缺氧/复氧损伤模型评价其心肌保护活性。结果与结论合成了14个苄基葡萄糖硫苷新化合物。初步药理评价表明,该类化合物对缺氧/复氧损伤心肌具有一定的保护作用,其中3个化合物的活性强于红景天苷,并呈剂量依赖关系。
Objective To design and synthesize glucosinolate compounds with myocardial protection. Methods Tetraacetyl-β-thioglucose was synthesized from tetraacetyl-α-bromoglucose as raw material, and glucopyranoside was prepared by reaction with substituted benzyl bromide. Finally, the acetyl group was removed to obtain the target compound. Myocardial protective activity was evaluated by hypoxia / reoxygenation injury model of cardiomyocytes in vitro. RESULTS AND CONCLUSIONS A total of 14 novel compounds of benzyl glucosinolate were synthesized. Preliminary pharmacological evaluation showed that these compounds have a protective effect on myocardial injury caused by hypoxia / reoxygenation, of which three compounds are more active than salidroside in a dose-dependent manner.