Novel 3α-methoxyserrat-14-en-21β-ol (PJ-1) and 3β-methoxyserrat-14-en-21β-ol (PJ-2)-curcumin, kojic acid, quercetin, and baicalein conjugates as HIV agents

被引：58

作者：

Tanaka, Reiko ^{[1
]}

Tsujii, Hiroko ^{[1
]}

Yamada, Takeshi ^{[1
]}

Kajimoto, Tetsuya ^{[1
]}

Amano, Fumio ^{[2
]}

Hasegawa, Junya ^{[3
]}

Hamashima, Yoshio ^{[3
]}

Node, Manabu ^{[3
]}

Katoh, Kayoko ^{[4
]}

Takebe, Yutaka ^{[4
]}

机构：

[1] Osaka Univ Pharmaceut Sci, Med Chem Lab, Osaka 5691094, Japan

[2] Osaka Univ Pharmaceut Sci, Lab Biodeferense & Regulat, Osaka 5691094, Japan

[3] Kyoto Pharmaceut Univ, Dept Pharmaceut Mfg Chem, Yamashina Ku, Kyoto 6078414, Japan

[4] Natl Inst Infect Dis, AIDS Res Ctr, Lab Mol Virol & Epidemiol, Shinjuku Ku, Tokyo 1628640, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 14期

关键词：

Conjugates; 3; alpha-Methoxyserrat-14-en-21; beta-ol; beta-Methoxyserrat-14-en-21; Curcumin; Kojic acid; Quercetin; Baicalein; HIV; C8166-CCR5; cells; ANTI-AIDS AGENTS; HUMAN-IMMUNODEFICIENCY-VIRUS; CANCER CHEMOPREVENTIVE ACTIVITY; SERRATANE-TYPE TRITERPENOIDS; MOUSE SKIN; SCHISANDRA-LANCIFOLIA; BETULINIC ACID; MORONIC ACID; STEM BARK; DERIVATIVES;

D O I：

10.1016/j.bmc.2009.05.049

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Sixteen novel compounds; 3 alpha-methoxyserrat-14-en-21 beta-ol (1) and 3 beta-methoxyserrat-14-en-21 beta-ol (2) and their curcumin, kojic acid, quercetin, and baicalein conjugates (3)-(18) were designed, synthesized, and evaluated for in vitro anti-HIV-1 reverse transcriptase (RT) activity in infected C8166-CCR5 cells, a human CD4(+) T-lymphocyte cell line. Among them, kojic acid derivatives, 9-12 showed significant biological activity. In particular, the compound 13, the conjugate of two molecules of 3 alpha-methoxyserrat-14-en-21 beta-ol (1) and one molecule of kojic acid, exerted significant anti-HIV activity with an EC50 value of 0.12 mu g/mL. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5238 / 5246

页数：9

共 5 条

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Tanaka, Reiko
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