摘要
芒果苷是一种药理活性广泛的双苯吡酮类黄酮类化合物,具有抗糖尿病,抗肿瘤,抗炎,抗氧化,免疫调节,解热,抗菌,改善记忆,防止紫外线所致皮肤老化等多种药理作用。查阅近年来国内外芒果苷的药理作用与结构修饰的文献,可知芒果苷溶解性及跨膜通透性均很小,导致其生物利用度低,严重制约了芒果苷制剂的开发。从改善其脂溶性与水溶性入手,对芒果苷进行有效的结构修饰、优化,改善了芒果苷的理化性质,提高了芒果苷的生物活性及生物利用度,扩大了其临床应用的范围,旨在研发出比芒果苷更易吸收且药理活性更强的衍生物。本文综述了近几年来国际上芒果苷的体内外药理作用,从化学修饰与生物转化等方面论述芒果苷结构修饰的研究进展,通过酰基化、成盐反应、合成磷脂复合物等化学方法及生物转化法可显著改善其水溶性或者脂溶性,有利于其在胃肠道的吸收,提高生物活性及生物利用度。为使芒果苷尽快投入到临床应用,今后还应加强芒果苷及其衍生物的药代动力学及体内代谢方面的研究,从而为开发芒果苷的高效新剂型提供理论支持。
Mangiferin, a natural polyphenol compound, which is so frequently occurring in plants and have conspicuous pharmacological activities, such as anti-inflammatory, antidiabetic, antitumour. From searching the recent years domestic and foreign literature on mangiferin about its pharmacological effects and structural modifications, we can know that the mangiferin has a low level of solubleness, mucosal permeability and bioavailability , which seriously restrict the development of its development and utilization. By modifying the structure of mangiferin, the physical and chemical properties are improved, the biological activity and the bioavailability are enhanced, the clinical application range is expanded. This article summarized the progress on pharmacological activities and structural modifications through the analysis of literature of mangiferin, in order to provide some references for the further study and development of mangiferin. The research of pharmacokinetic and metabolic should be strengthened in the future, with the purpose of putting mangiferin into clinic use.
出处
《中国实验方剂学杂志》
CAS
北大核心
2014年第12期248-252,共5页
Chinese Journal of Experimental Traditional Medical Formulae
基金
上海市科技创新行动计划项目(12431900805)
关键词
芒果苷
药理作用
结构修饰
mangiferin
pharmacological activities
structural modifications
