Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues

被引：7

作者：

Li, Qingyong ^{[1
]}

He, Wuna ^{[1
]}

Zhang, Li ^{[1
]}

Zu, Yuangang ^{[1
]}

Zhu, Qiaochu ^{[1
]}

Deng, Xiaoqiu ^{[1
]}

Zhao, Tengfei ^{[1
]}

Gao, Wenqing ^{[1
]}

Zhang, Baoyou ^{[1
]}

机构：

[1] NE Forestry Univ, Minist Educ, Key Lab Forest Plant Ecol, Harbin 150040, Heilongjiang Pr, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 06期

关键词：

Berberine; Bile acids; Synthesis; Anticancer; Antimicrobial; Oral bioavailability; SUBSTRATE-SPECIFICITY; COTRANSPORTERS; TRANSPORT; RABBIT; ILEAL;

D O I：

10.2174/157018012800673010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Fifteen berberine-bile acid analogues were synthesized. Anticancer activities of these analogues compared with berberine (BBR) were evaluated in vitro; among the analogues, A4, B4, and B5 had higher cytotoxicity than that of BBR. Most of the analogues showed higher antimicrobial activity against Staphylococcus aureus ATCC 25923 and Staphylococcus albus ATCC 8799 than that of BBR, but Bacillus subtilis AS 1.398 and Escherichia coli ATCC 31343 were not sensitive to all of the analogues. A4 and B4 were stable in the serum stability assay. B4 showed promising oral bioavailability in mice.

引用

页码：573 / 580

页数：8

共 35 条

[1]

Atiq-ur-Rehman, 1999, TETRAHEDRON LETT, V40, P1865

[2] Apical sodium dependent bile acid transporter (ASBT, SLC10A2): A potential prodrug target [J].

Balakrishnan, Anand ;

Polli, James E. .

MOLECULAR PHARMACEUTICS, 2006, 3 (03) :223-230

[3]

Baringhaus KH, 1999, J LIPID RES, V40, P2158

[4] Synthesis of 9-substituted derivatives of berberine as anti-HIV agents [J].

Bodiwala, Hardik S. ;

Sabde, Sudeep ;

Mitra, Debashis ;

Bhutani, Kamlesh Kumar ;

Singh, Inder Pal .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (04) :1045-1049

[5] Synthesis of bile acid derivatives and in vitro cytotoxic activity with pro-apoptotic process on multiple myeloma (KMS-11), glioblastoma multiforme (GBM), and colonic carcinoma (HCT-116) human cell lines [J].

Brossard, Dominique ;

El Kihel, Laila ;

Clement, Monique ;

Sebbahi, Walae ;

Khalid, Mohamed ;

Roussakis, Christos ;

Rault, Sylvain .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (07) :2912-2918

[6]

Chili K., 2004, CANC LETT, V203, P127

[7]

Cho E., 1990, PHARMACOPOEIA PEOPLE

[8]

Criado JJ, 1997, J LIPID RES, V38, P1022

[9] New organotropic compounds -: Synthesis, characterization and reactivity of Pt(II) and Au(III) complexes with bile acids:: DNA interactions and 'in vitro' anticancer activity [J].

Criado, JJ ;

Manzano, JL ;

Rodríguez-Fernández, E .

JOURNAL OF INORGANIC BIOCHEMISTRY, 2003, 96 (2-3) :311-320

[10] New lithocholic and chenodeoxycholic piperazinylcarboxamides with antiproliferative and pro-apoptotic effects on human cancer cell lines [J].

El Kihel, Laila ;

Clement, Monique ;

Bazin, Marc-Antoine ;

Descamps, Geraldine ;

Khalid, Mohamed ;

Rault, Sylvain .

BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (18) :8737-8744

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