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柴胡根中的抗氧化和细胞毒性木脂素。

Antioxidant and cytotoxic lignans from the roots of Bupleurum chinense.

作者信息

Li Dan-Qi, Wang Di, Zhou Le, Li Ling-Zhi, Liu Qing-Bo, Wu Ying-Ying, Yang Jing-Yu, Song Shao-Jiang, Wu Chun-Fu

机构信息

a School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University , Shenyang 110016 , China.

b Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education , Shenyang Pharmaceutical University , Shenyang 110016 , China.

出版信息

J Asian Nat Prod Res. 2017 May;19(5):519-527. doi: 10.1080/10286020.2016.1234456. Epub 2016 Sep 21.

Abstract

In the search for biologically active compounds from the roots of Bupleurum chinense D C., phytochemical investigation of its ethanol extract led to the isolation and identification of a new 8-O-4' neolignan glucoside, saikolignanoside A (1), along with eight known lignans (2-9). Their structures were determined on the basis of IR, UV, HRESIMS, and NMR spectroscopic analyses. The antioxidant and cytotoxic effects of isolated compounds were evaluated in vitro. The isolated compounds (IC > 200 μM) did not display 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity. Whereas compounds 1-2, 5, 7, and 9 exhibited potent 2, 2'-azinobis(3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) free radical scavenging properties with IC values ranging from 8.34 to 15.24 μM, while compounds 3-4, 6, 8 showed moderate properties. In addition, all compounds were evaluated for cytotoxicities against A549, HepG2, U251, Bcap-37, and MCF-7 cell lines. Compounds 5 and 9 (IC< 51.62 μM) possessed stronger cytotoxic activities against all the tested tumor cell lines, compared with the positive control 5-Fluorouracil.

摘要

在从柴胡根中寻找生物活性化合物的过程中,对其乙醇提取物进行植物化学研究,分离并鉴定出一种新的8-O-4'新木脂素糖苷,柴胡木脂素苷A(1),以及8种已知木脂素(2-9)。它们的结构通过红外光谱、紫外光谱、高分辨电喷雾电离质谱和核磁共振光谱分析确定。对分离得到的化合物的抗氧化和细胞毒性作用进行了体外评价。分离得到的化合物(IC>200μM)未表现出对2,2-二苯基-1-苦基肼(DPPH)自由基的清除活性。而化合物1-2、5、7和9表现出较强的对2,2'-偶氮双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)自由基的清除性能,IC值范围为8.34至15.24μM,而化合物3-4、6、8表现出中等性能。此外,对所有化合物针对A549、HepG2、U251、Bcap-37和MCF-7细胞系的细胞毒性进行了评价。与阳性对照5-氟尿嘧啶相比,化合物5和9(IC<51.62μM)对所有测试的肿瘤细胞系具有更强的细胞毒性活性。

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