连翘脂素药理作用、制备工艺及应用研究进展  

Review on pharmacology,preparation and application of phillygenin

作　　者：孟冰冰 梁春花 徐国伟 毛鹏年 杨泽 李成 古雪艳 王磊[1] 冯海鹏 郭志廷[1] 路晓荣 李建喜[1] 张景艳[1] MENG Bingbing;LIANG Chunhua;XU Guowei;MAO Pengnian;YANG Ze;LI Cheng;GU Xueyan;WANG Lei;FENG Haipeng;GUO Zhiting;LU Xiaorong;LI Jianxi;ZHANG Jingyan(Chinese-Thai Traditional Chinese Veterinary Medicine and Techniques Cooperation Laboratory,Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS,Lanzhou Gansu 730050,China;Minle County Agriculture and Rural Bureau in Gansu Province,Minle Gansu 734500,China)

机构地区：[1]中国农业科学院兰州畜牧与兽药研究所,中泰中兽医药学技术联合实验室,甘肃兰州730050 [2]甘肃省民乐县农业农村局,甘肃民乐734500

出　　处：《中兽医医药杂志》2025年第2期37-42,共6页Journal of Traditional Chinese Veterinary Medicine

基　　金：国家重点研发计划(2023YFD1800804-02);中国农业科学院科技创新工程(CAAS-ASTIP-2015-LIHPS)。

摘　　要：连翘脂素是一种双四氢呋喃型天然小分子化合物,是连翘苷脱糖后的活性成分,主要存在于连翘、桂花、牛蒡叶、猫爪草等植物中。连翘脂素具有抗炎、抗氧化、保肝、抗肿瘤、抗菌、抗病毒、免疫调节、镇痛、降压和扩张血管等多种药理活性。连翘脂素制备工艺包括化学提取、微生物转化和化学合成等方法。然而,由于提取效率低等因素的影响,天然产物的提取制备成本相对较高,未来可以聚焦人工合成等方法来制备连翘脂素。连翘脂素具有水溶性低、吸收不完全和渗透性有限的特点,导致其口服生物利用度较低。为了提高其溶解度和生物利用度,研究者已开发了连翘脂素纳米混悬液、微丸、微乳等制剂。本文从连翘脂素的理化特性、药理作用、制备工艺和制剂开发等方面进行综述,旨在为连翘脂素的药理研究、药物研发、临床应用提供参考。Phillygenin is a naturally occurring small molecule compound of the dihydrofuran class,which is the active component derived from the deglycosylation of phillyin,predominantly found in plants such as Fructus Forsythiae,Osmanthus Fragrans,Arctium lappa leaves and Radix Ranunculi Ternati.It exhibits a range of pharmacological activities,including anti-inflammatory,antioxidant,hepatoprotective,antitumor,antibacterial,antiviral,immunomodulatory,analgesic,hypotensive,and vasodilatory effects.Preparation methods for phillygenin encompass chemical extraction,microbial biotransformation,and chemical synthesis.However,the extraction and preparation of this natural product are relatively costly due to factors such as low extraction efficiency,thereby advocating for a future research trajectory that prioritizes synthetic methodologies for the generation of phillygenin.Phillygenin is characterized by low water solubility,incomplete absorption,and limited permeability,which contribute to its low oral bioavailability.To enhance its solubility and bioavailability,formulations such as phillygenin nanosuspensions,microspheres,and microemulsions have been developed.This review summarized the physicochemical properties,pharmacological effects,preparation methods,and formulation development of phillygenin,aiming to provide a reference for in-depth research,drug development,and clinical application of phillygenin.

关 键 词：连翘 连翘脂素 药理作用 制备工艺 剂型 应用 

分 类 号：S853.7[农业科学—临床兽医学]