摘要
藁本内酯(LIG)是中药当归和川芎含有的一种苯酞类化合物,具有广泛的药理活性,主要有抗炎、抗氧化、镇痛、抗肿瘤、神经保护和血管保护作用等,然而LIG稳定性差,容易受温度、光照和氧气、溶媒pH值、溶媒种类等因素的影响发生变构;此外,LIG水溶性低,生物利用度小,限制了LIG在新药成药方面的开发应用.笔者综述近年来国内外有关LIG天然来源、结构特点及结构改造、降解及转化机制、影响降解的主要因素、稳定化方法、生物活性等方面的研究进展,以期为LIG的进一步开发应用提供参考.
Abstract
Ligustilide(LIG)is a phthalide compound found in Angelica sinensis(Oliv.)Diels and Ligusticum chuanxiong Hort,which has a wide range of pharmacological activities in clinical practice,including anti-inflammatory,antioxidant,analgesic,anti-tumor,neuroprotective,and vascular protective effects.However,LIG has poor stability and is easily affected by factors such as temper-ature,light,oxygen,pH value,and solvent type,leading to conformational changes.In addition,the low water solubility and low bio-availability of LIG limit its development and application in new drugs.The article reviews the research progress on natural sources,struc-tural characteristics and structural modifications,degradation and transformation mechanisms,main degradation influencing factors,stabi-lization methods and bioactivity of LIG in recent years,in order to provide reference for the further development and applications of LIG.
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