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海氏海桑和其生物活性的新贝壳杉烯和大根香叶烯衍生物。

New -kaurene and germacrene derivatives from Hemseley and their biological activity.

机构信息

Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Taipei, Taiwan.

Department of Biochemical Science and Technology, National Chiayi University, Chiayi, Taiwan.

出版信息

Nat Prod Res. 2023 Jul;37(13):2172-2180. doi: 10.1080/14786419.2022.2034811. Epub 2022 Feb 1.

Abstract

Hemseley is a well-known traditional herbal medicine used for heat-related ailments. In Taiwan, boiled extracts of are also used as desserts called grass jelly. In this study, the hexane extract from 75% EtOH of showed potent activities on inhibition of β-glucuronidase (eβG) and NO production and cytotoxicity against MCF-7 and HepG2 cancer cell lines. Furthermore, using various flash columns and HPLC chromatography on the bioactive layer led to the isolation of twelve compounds (-), including a new -kaurene, mesokaurol A (), and a new germacrene derivative, mesogermapene A (). Their structures were elucidated by extensive spectroscopic analyses, especially 2 D NMR and mass data. Biological assays showed that compound (linolenic acid) had specific activity on inhibition of eβG (68.27%) at 100 µg/mL but was non-inhibitory to human β-glucuronidase. Compound possessed significant cytotoxicity against MCF-7 (EC = 9.76 µM) and HepG2 (EC = 8.64 µM) cancer cell lines.

摘要

何氏凤仙花是一种著名的传统草药,用于治疗与热有关的疾病。在台湾,也将其 75%乙醇水煮提取物用作草果冻等甜点。在这项研究中, 75%乙醇提取物对β-葡萄糖醛酸酶(eβG)和一氧化氮(NO)的产生具有很强的抑制作用,对 MCF-7 和 HepG2 癌细胞系也具有细胞毒性。此外,在生物活性层上使用各种闪式柱和 HPLC 色谱法,分离出了 12 种化合物(-),包括一种新的贝壳杉烯,中孔卡醇 A()和一种新的倍半萜烯衍生物,中孔甾烯 A()。通过广泛的光谱分析,特别是 2D NMR 和质谱数据,阐明了它们的结构。生物测定表明,化合物 (亚油酸)在 100μg/mL 时对 eβG(68.27%)具有特异性抑制活性,但对人β-葡萄糖醛酸酶没有抑制作用。化合物 对 MCF-7(EC=9.76μM)和 HepG2(EC=8.64μM)癌细胞系具有显著的细胞毒性。

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