Isolation, synthesis and anti-hepatitis B virus evaluation of p-hydroxyacetophenone derivatives from Artemisia capillaris

Bioorganic & Medicinal Chemistry Letters
Yong ZhaoJi-Jun Chen

Abstract

p-Hydroxyacetophenone (p-HAP), as a main hepatoprotective and choleretic constituent of Artemisia capillaris, was revealed with anti-hepatitis B virus (HBV) effects in recent investigation. In addition to p-HAP, four derivatives of p-HAP were also isolated from A. capillaris by various chromatographic methods. Subsequent structural modification on p-HAP and its glycoside led to the synthesis of 28 additional derivatives, of which 13 compounds showed activity inhibiting hepatitis B surface antigen (HBsAg) secretion; and 18 compounds possessed inhibition on HBV DNA replication. The primary structure-activity relationships (SARs) suggested that the conjugated derivatives of p-HAP glycoside and substituted cinnamic acids (2a-2i) obviously enhanced the activity against HBV DNA replication with IC50 values ranged from 5.8 to 74.4 μM.

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Citations

Sep 15, 2015·Evidence-based Complementary and Alternative Medicine : ECAM·Eungyeong JangJang-Hoon Lee
Jan 13, 2016·World Journal of Gastroenterology : WJG·Yi-Hang Wu
Sep 29, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Si-Xin HuangCheng-Qin Liang
Jul 7, 2018·Natural Products and Bioprospecting·Chang-An Geng, Ji-Jun Chen
Nov 26, 2019·Food Science & Nutrition·Guo-Kai WangJai-Sing Yang
Dec 31, 2020·BioMed Research International·Xuqiang LiuWenyi Kang

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