木香烃内酯抗肿瘤活性研究进展  

Research progress on the antitumor activity of costunolide

作　　者：刘丹[1] 刘明 金良友[3] 潘娟 辛昊儒 刘梦圆 李鑫 郑坤 冯晓灵[1] LIU Dan;LIU Ming;JIN Liangyou;PAN Juan;XIN Haoru;LIU Mengyuan;LI Xin;ZHENG Kun;FENG Xiaoling(Chongqing Three Gorges Medical College Chongqing Key Laboratory of Development and Utilization of Genuine Medicinal Materials in Three Gorges Reservoir Area,Wanzhou 404120,Chongqing,China;Chongqing College of Mobile Communication,Qijiang 404120,Chongqing,China;Chongqing Three Gorges University,Wanzhou 404120,Chongqing,China)

机构地区：[1]重庆三峡医药高等专科学校,三峡库区道地药材开发利用重庆市重点实验室,重庆万州404120 [2]重庆移通学院,重庆綦江401520 [3]重庆三峡学院,重庆万州404120

出　　处：《中国临床药理学与治疗学》2023年第10期1168-1176,共9页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：重庆市教育委员会科学技术研究项目(KJQN201902710);重庆市教育委员会科学技术研究项目(KJQN202202704);重庆三峡医药高等专科学校重点实验室项目(Sys20210009);重庆三峡医药高等专科学校自然科学重大项目(XJ2022003103)。

摘　　要：近年来,中药抗肿瘤作用的研究呈现逐年增加的趋势,无论是中药有效提取成分或是复方制剂在肿瘤治疗方面都具有显著的疗效及优势。中药木香中的活性成分木香烃内酯是一种天然倍半萜内酯,具有多种药理作用,如抗氧化、抗炎、降血糖、抗微生物等。近年来,越来越多的体内外实验研究表明,该成分具有抗肿瘤活性,可抑制乳腺癌、胃癌、黑色素瘤、前列腺癌、白血病、肝癌、肺癌、卵巢癌、食管癌、结直肠癌、骨肉瘤等多种肿瘤的生长。其抗肿瘤的机制主要是通过调控PI3K/AKT/mTOR、AKT-MDM2-p53、ROS-AKT/GSK3β、Bcr/Abl和Stat5等信号通路,影响活性氧、细胞凋亡相关蛋白和自噬相关蛋白、细胞周期蛋白等方面,从而诱导细胞凋亡、介导自噬及导致细胞周期阻滞在G2/M期、G1期、S期。此外,木香烃内酯与伊马替尼、阿霉素联用可以起到减毒增效、增强抗肿瘤作用,并且还能逆转肿瘤耐药。笔者通过查阅和整理国内外相关研究文献,对木香烃内酯抗肿瘤作用及机制、联合用药、逆转肿瘤耐药的研究进展进行综述,以期为该成分新药开发与利用提供理论依据。In recent years,the research on the anti-tumor effect of traditional Chinese medicine has been increasing year by year.Both the effective extracted ingredients of Chinese medicine and its compound preparations have significant efficacy and advantages in tumor treatment.Costunolide,the active ingredient of Aucklandia lappa(a traditional Chinese medicine),is a natural sesquiterpene lactone,which has a variety of pharmacological effects,such as anti-oxidation,anti-inflammation,hypoglycemic effect,anti-microbial effect etc.In recent years,more and more experimental studies in vivo and in vitro have shown that this component has anti-tumor activity,which can inhibit the growth of breast cancer,gastric cancer,melanoma cancer,prostate cancer,leukemia,liver cancer,lung cancer,ovarian cancer,esophageal cancer,colorectal cancer,osteosarcoma and other tumors.Its antitumor mechanism mainly lies in the regulation of PI3K/AKT/mTOR,AKT-MDM 2-p53,ROS-AKT/GSK-3β,Bcr/Abl,Stat5 and other signaling pathways,which affects reactive oxygen species,apoptosis-related proteins,autophagy-related proteins,and cyclin,and thus induces apoptosis,causes autophagy and arrests cell cycle in G2/M phase,G1 phase,and S phase.In addition,the combination of costunolide with imatinib and doxorubicin can attenuate toxicity and enhance anti-tumor effect,and also reverse tumor drug resistance.By consulting and sorting out the relevant research literature at home and abroad,the author summarized the research progress of costunolide on the antitumor effect and mechanism,the combined drug use and the reversal of tumor drug resistance in order to provide theoretical basis for the development and utilization of new drugs of this ingredient.

关 键 词：木香烃内酯 肿瘤 机制 研究进展 联合用药 

分 类 号：R285.5[医药卫生—中药学] R73[医药卫生—中医学]