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引用本文:阮清锋,卢淇平,陈小晶,赵敏,崔辉,赵钟祥.山胡椒内生真菌Trichoderma sp. SHJN1和Perenniporia sp. SHJG1的抗肿瘤活性成分研究[J].中国现代应用药学,2023,40(18):2535-2542.
RUAN Qingfeng,LU Qiping,CHEN Xiaojing,ZHAO Min,CUI Hui,ZHAO Zhongxiang.Chemical Constituents of Endophytic Fungi Trichoderma sp. SHJN1 and Perenniporia sp. SHJG1 from Lindera glauca and Their Anti-tumor Activities[J].Chin J Mod Appl Pharm(中国现代应用药学),2023,40(18):2535-2542.
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山胡椒内生真菌Trichoderma sp. SHJN1和Perenniporia sp. SHJG1的抗肿瘤活性成分研究
阮清锋1,2, 卢淇平2, 陈小晶2, 赵敏2, 崔辉2, 赵钟祥2
1.武汉市第一医院药学部, 武汉 430022;2.广州中医药大学中药学院, 广州 510006
摘要:
目的 从民族药山胡椒内生真菌Trichoderma sp.SHJN1和Perenniporia sp.SHJG1的代谢物中寻找活性先导化合物。方法 采用正相硅胶、反相硅胶、Sephadex LH-20凝胶及制备型HPLC等对Trichoderma sp.SHJN1和Perenniporia sp.SHJG1发酵物进行分离纯化,再通过NMR、ESI-MS等鉴定化合物结构,同时采用人乳腺癌细胞(MCF-7)和人肺癌细胞(A549)对这些化合物的抗肿瘤活性进行初步评价。结果 从2株内生真菌次级代谢产物中共分离鉴定了12个化合物:alantrypinone (1)、oryzalactam (2)、phomoindene A (3)、cis-gregatin B (4)、huaspenone B (5)、stigmasta-7,22-dien-3β,5α,6α-triol (6)、ergosterol (7)、1-deoxy-2-demethylviridiol (8)、viridiol (9)、trichodermamides A (10)、chromone (11)、对-羟基苯乙酸(12)。抗肿瘤活性评价结果显示,化合物3 抑制MCF-7细胞增殖活性IC50为(62.9±1.02)μmol·L-1[顺铂(cisplatin,DDP) IC50为(30.1±1.67)μmol·L-1];化合物89 抑制A549细胞增殖活性的IC50分别为(34.6±1.57)μmol·L-1和(44.9±1.74)μmol·L-1[DDP IC50为(20.6±1.42)μmol·L-1]。结论 化合物389 具有潜在抗肿瘤活性。
关键词:  山胡椒  内生真菌  木霉属真菌  多年卧孔菌属真菌  次级代谢产物
DOI:10.13748/j.cnki.issn1007-7693.20230437
分类号:R965.1
基金项目:湖北省自然科学基金资助项目(2022CFB976);武汉市科技局知识创新专项项目(2023020201020533)
Chemical Constituents of Endophytic Fungi Trichoderma sp. SHJN1 and Perenniporia sp. SHJG1 from Lindera glauca and Their Anti-tumor Activities
RUAN Qingfeng1,2, LU Qiping2, CHEN Xiaojing2, ZHAO Min2, CUI Hui2, ZHAO Zhongxiang2
1.Department of Pharmacy, Wuhan No. 1 Hospital, Wuhan 430022, China;2.School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
Abstract:
OBJECTIVE To find lead compounds with potent bioactivities from endophytic fungi Trichoderma sp. SHJN1 and Perenniporia sp. SHJG1 from the traditional Chinese medicine Lindera glauca. METHODS The fermentation of Trichoderma sp. SHJN1 and Perenniporia sp. SHJG1 were isolated and purificated by repeated silica gel, ODS, Sephadex LH-20, and semi-preparation HPLC. The structures of compounds were performed by NMR and ESI-MS. The preliminary evaluation of anti-tumor activity of these compounds was performed by human breast cancer cells(MCF-7) and human lung cancer cells(A549). RESULTS A total of 12 compounds were purified from the above two endophytic fungi and identified as alantrypinone(1), oryzalactam(2), phomoindene A(3), cis-gregatin B(4), huaspenone B(5), stigmasta-7,22-dien-3β,5α,6α-triol(6) and ergosterol(7), 1-deoxy-2-demethylviridiol (8), viridiol(9), trichodermamides A(10), chromone(11) and 4-hydroxyphenylacetic acid(12). The evaluation of antitumor activity showed that, compound 3 showed inhibitory activity on MCF-7 cell line with an IC50 value of (62.9±1.02)μmol·L-1[cisplatin(DDP) IC50=(30.1±1.67)μmol·L-1], while compound 8 and 9 showed inhibitory activities on A549 cell line with IC50 values of (34.6±1.57)μmol·L-1 and (44.9±1.74)μmol·L-1, respectively[DDP IC50=(20.6±1.42)μmol·L-1]. CONCLUSION Compounds 3, 8 and 9 show potent anti-tumor effects.
Key words:  Lindera glauca  endophytic fungi  Trichoderma sp.  Perenniporia sp.  secondary metabolites
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