喙尾琵琶甲中抗肿瘤活性化合物的分离及鉴定

天然产物研究与开发 ›› 2020, Vol. 32 ›› Issue (增刊2): 41-45.

所属专题： No.4

喙尾琵琶甲中抗肿瘤活性化合物的分离及鉴定

史晓玲1，屈瑶1，唐会鹏1，王耀杰2，李蕾1*

1云南大学省部共建云南生物资源保护与利用国家重点实验室，昆明 650091；2河北医科大学第四医院，石家庄 050011

出版日期:2020-12-09 发布日期:2020-12-09
基金资助:
国家自然科学基金（31660538）

Isolation and identification of antitumor compounds from Blaps rynehopetera Fairmaire

SHI Xiao-ling1,QU Yao1,TANG Hui-peng1,WANG Yao-jie 2,LI Lei1*#br#

#br#

1State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan,Yunnan University,Kunming 650091,China; 2Fourth Hospital of Heibei Medical University,Shijiazhuang 050011,China

Online:2020-12-09 Published:2020-12-09

摘要/Abstract

摘要：

在抗肿瘤活性模型的指导下，采用萃取法、硅胶色谱、凝胶色谱等方法对喙尾琵琶甲全虫95%乙醇浸提液中具有抗肿瘤活性的馏分进行分离纯化，并综合运用HR-EMI-MS、¹H NMR、¹³C NMR等方法鉴定化合物的结构;采用MTT法测定化合物对乳腺癌MD-A-MB-23的细胞毒活性。喙尾琵琶甲的抗肿瘤活性集中在乙醇提取物的乙酸乙酯萃取部位，从中分离纯化得到6个化合物，分别鉴定为：hydroquinone（1）、2-methyl-1,4-benzenediol（2）、2-ethyl-1,4-benzenediol（3）、hydroxytyrosol（4）、1-(3,4-dihydroxyphenyl) isochroman-6,7-diol（5）和2,5-dihydroxyphenethyl 2-hydroxypropanoate（6）。这6个活性化合物均为苯酚类，化合物4是首次从喙尾琵琶甲中分离得到，首次报道化合物4、5和6对MD-A-MB-23细胞有中度的细胞毒活性。化合物1、2和3表现出较强的活性，化合物1苯环二位上的氢分别被甲基（化合物2）或乙基（化合物3）取代后，它们对MD-A-MB-23细胞的IC₅₀值从69.86 μg/mL分别下降到676、2.64 μg/mL。

关键词: 喙尾琵琶甲, 苯酚类化合物, 对苯二酚, 2-甲基对苯二酚, 2-乙基对苯二酚, 抗肿瘤活性

Abstract:

The separation procedure was guided by a bioassay using MD-A-MB-23 cells,and the column chromatography over silica gel,Sephadex LH-20 was employed for the purification of compounds from 95% ethyl alcohol extract of B. Rynehopetera.Their structures were fully determined based on spectroscopic analysis including HR-EMI-MS,¹H NMR and ¹³C NMR.The compound cytotoxicity was evaluated in vitro against MD-A-MB-23 cells by MTT method.After anti-tumor-guide purification,six active compounds with antitumor activity were isolated from ethyl acetate fraction of 95% ethyl alcohol extract of B. Rynehopetera.These compounds were identified as hydroquinone(1),2-methyl-1,4-benzenediol(2),2-ethyl-1,4-benzenediol(3),hydroxytyrosol(4),1-(3,4-dihydroxyphenyl) isochroman-6,7-diol(5)and 2,5-dihydroxyphenethyl 2-hydroxypropanoate(6).The six active compounds are all phenolic derivatives.It is for the first time that compound 4 was isolated from the B. Rynehopetera and compounds 4,5 and 6 showed the moderate cytotoxic activity against MD-A-MB-23 cells.Compounds 1,2 and 3 showed strong activities.The hydrogen at the di-position of the benzene ring of compound 1 was replaced respectively by methyl (2) or ethyl (3),and their IC₅₀of MD-A-MB-23 cells decreased from 69.86 μg/mL to 6.76 and 2.64 μg/mL.

Key words: Blaps rynehopetera Fairmaire, phenolic derivative, hydroquinone, 2-methyl-1,4-benzenediol, 2-ethyl-1,4-benzenediol, antitumor activity

中图分类号: R282.74

史晓玲, 屈瑶, 唐会鹏, 王耀杰, 李蕾. 喙尾琵琶甲中抗肿瘤活性化合物的分离及鉴定[J]. 天然产物研究与开发, 2020, 32(增刊2): 41-45.

SHI Xiao-ling, QU Yao, TANG Hui-peng, WANG Yao-jie , LI Lei. Isolation and identification of antitumor compounds from Blaps rynehopetera Fairmaire[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2020, 32(增刊2): 41-45.

喙尾琵琶甲中抗肿瘤活性化合物的分离及鉴定

Isolation and identification of antitumor compounds from Blaps rynehopetera Fairmaire

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