重楼总皂苷的现代研究进展与展望  

Total Saponins in Paridis Rhizoma:A Review

作　　者：张艺博 张慧中 付京 阮意丹 姚爱娜 张萍芝 尹兴斌[1] 曲昌海[1] 倪健[1] 董晓旭[1] ZHANG Yibo;ZHANG Huizhong;FU Jing;RUAN Yidan;YAO Aina;ZHANG Pingzhi;YIN Xingbin;QU Changhai;NI Jian;DONG Xiaoxu(School of Chinese Material Medica,Beijing University of Chinese Medicine,Beijing 102488,China;Beijing Institute of Chinese Medicine,Beijing Hospital of Traditional Chinese Medicine,Capital Medical University,Beijing 100010,China)

机构地区：[1]北京中医药大学中药学院,北京102488 [2]首都医科大学附属北京中医医院北京市中医药研究所,北京100010

出　　处：《中国实验方剂学杂志》2024年第1期232-243,共12页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81973492);中央高校基本科研业务费专项(2022-JYB-XJSJJ015)。

摘　　要：重楼具有清热解毒、消肿止痛、凉肝定惊的作用,重楼皂苷是重楼的主要活性成分。研究表明,重楼总皂苷抗肿瘤作用显著,对乳腺癌、肺癌、胃癌、肝癌等实体瘤和白血病等非实体瘤有明显的抑制作用,其机制与抑制肿瘤细胞增殖、迁移和侵袭,调控细胞周期,诱导凋亡和非凋亡的死亡途径,调节机体代谢与肿瘤微环境等密切相关。此外,重楼总皂苷在抗炎、抗氧化、抑菌、止血、缩宫等方面也表现出很好的药理活性。与此同时,重楼总皂苷可能诱导正常细胞凋亡、诱发炎症反应与氧化应激、导致机体代谢紊乱,近年来其肝损伤、生殖损伤、胃肠损伤、溶血等不良反应报道逐渐增多。药代动力学研究显示,不同给药方式的重楼总皂苷在机体内代谢存在着较大的差异,注射给药清除速度较快,口服则可能存在肝肠循环,同时由于溶解度低、并能激活P-糖蛋白(P-gp),导致其原型吸收差、在肠道渗透率和回收率低,影响重楼总皂苷的生物利用度,借助现代技术制备新剂型或新型载药系统一定程度上可提高其生物利用度。基于上述研究,该文将“重楼总皂苷”“Rhizoma Paridis Total Saponins”作为关键词,通过检索中国知网、维普、Web of Science等国内外中英文数据库,对重楼总皂苷的药理作用、药代动力学及不良反应展开综述,以期能为重楼总皂苷的研究开发及临床应用提供参考。Paridis Rhizoma possesses the functions of clearing heat and detoxifying,alleviating swelling and relieving pain,cooling the liver and calming the convulsion.Saponins are the main active components of Paridis Rhizoma.Studies have shown that total saponins in Paridis Rhizoma have obvious inhibitory effect on solid tumors such as breast cancer,lung cancer,gastric cancer,and liver cancer and non-solid tumors such as leukemia.The saponins may exert the anti-tumor effects by inhibiting the proliferation,migration,and invasion of tumor cells,regulating cell cycle,inducing apoptotic and non-apoptotic death pathways,and regulating metabolism and tumor microenvironment.Furthermore,total saponins in Paridis Rhizoma showed anti-inflammatory,antioxidant,antimicrobial,hemostatic,and uterus-contracting activities.At the same time,they may induce apoptosis of normal cells,inflammation and oxidative stress,and metabolic disorders.In recent years,the reports of liver injury,reproductive injury,gastrointestinal injury,hemolysis,and other adverse reactions caused by total saponins in Paridis Rhizoma have been increasing.Pharmacokinetic studies have shown that there are significant differences in the metabolism of total saponins in Paridis Rhizoma administrated in different ways.Injection has a fast clearance rate,while oral administration may have hepatoenteric circulation.Meanwhile,due to the low solubility and activation of P-glycoprotein(P-gp)molecular pump,the prototype absorption,intestinal permeability,and recovery rate of total saponins in Paridis Rhizoma are poor,which affects the bioavailability.The bioavailability can be improved to some extent by preparing new dosage forms or new drug delivery systems with advanced technology.This paper reviews the pharmacological effect,pharmacokinetics,and adverse reactions of Rhizoma Paridis total saponins by searching the China National Knowledge Infrastructure(CNKI),VIP,and Web of Science with''Rhizoma Paridis total saponins''as the keywords,hoping to provide references for the rese

关 键 词：重楼总皂苷 抗肿瘤 药理作用 药代动力学 不良反应 

分 类 号：R2-0[医药卫生—中医学] R22R242R285.5R287