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从藏胡黄连种子中提取和纯化的三种化合物的抗乙肝病毒活性

Anti-HBV Activities of Three Compounds Extracted and Purified from Herpetospermum Seeds.

作者信息

Gong Pu-Yang, Yuan Zhi-Xiang, Gu Jian, Tan Rui, Li Jia-Chuan, Ren Yan, Hu Sha

机构信息

College of Pharmacy, Southwest University for Nationalities, Chengdu 610041, Sichuan, China.

Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, Sichuan, China.

出版信息

Molecules. 2016 Dec 27;22(1):14. doi: 10.3390/molecules22010014.

Abstract

The goal of this research was to evaluate the anti-hepatitis B virus (HBV) activities of three compounds extracted and purified from seeds (HS) on HepG2.2.15 cells. Herpetin (HPT), herpetone (HPO), and herpetfluorenone (HPF) were isolated from HS and identified using HR-ESI-MS and NMR. Different concentrations of the drugs were added to the HepG2.2.15 cells. Cell toxicity was observed with an MTT assay, cell culture supernatants were collected, and HBsAg and HBeAg were detected by ELISA. The content of HBV DNA was determined via quantitative polymerase chain reaction (PCR) with fluorescent probes. The 50% toxicity concentration (TC) of HPF was 531.48 μg/mL, suggesting that this species is less toxic than HPT and HPO. HPT and HPF showed more potent antiviral activities than HPO. The 50% inhibition concentration (IC) values of HPF on HBsAg and HBeAg were 176.99 and 134.53 μg/mL, respectively, and the corresponding therapeutic index (TI) values were 2.66 and 3.49, respectively. HPT and HPF were shown to significantly reduce the level of HBV DNA in the HepG2.2.15 culture medium compared to the negative control. This initial investigation of the anti-HBV constituents of HS yielded three compounds that revealed a synergistic effect of multiple components in the ethnopharmacological use of HS.

摘要

本研究的目的是评估从种子中提取和纯化得到的三种化合物对HepG2.2.15细胞的抗乙型肝炎病毒(HBV)活性。从种子中分离出了蛇床亭(HPT)、蛇床酮(HPO)和蛇床芴酮(HPF),并通过高分辨电喷雾电离质谱(HR-ESI-MS)和核磁共振(NMR)进行了鉴定。将不同浓度的药物加入到HepG2.2.15细胞中。采用MTT法观察细胞毒性,收集细胞培养上清液,通过酶联免疫吸附测定(ELISA)检测HBsAg和HBeAg。通过荧光探针定量聚合酶链反应(PCR)测定HBV DNA的含量。HPF的50%毒性浓度(TC)为531.48μg/mL,表明该化合物的毒性低于HPT和HPO。HPT和HPF显示出比HPO更强的抗病毒活性。HPF对HBsAg和HBeAg的50%抑制浓度(IC)值分别为176.99和134.53μg/mL,相应的治疗指数(TI)值分别为2.66和3.49。与阴性对照相比,HPT和HPF能显著降低HepG2.2.15培养基中HBV DNA的水平。对种子抗HBV成分的初步研究得到了三种化合物,揭示了种子在民族药理学应用中多种成分的协同作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/37f9/6155818/bd40e89fd6dc/molecules-22-00014-g001.jpg

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