Abstract
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.
Keywords: Berberine, Bile acids, Synthesis, Anticancer, Antimicrobial, Oral bioavailability
Letters in Drug Design & Discovery
Title:Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues
Volume: 9 Issue: 6
Author(s): Qingyong Li, Wuna He, Li Zhang, Yuangang Zu, Qiaochu Zhu, Xiaoqiu Deng, Tengfei Zhao, Wenqing Gao and Baoyou Zhang
Affiliation:
Keywords: Berberine, Bile acids, Synthesis, Anticancer, Antimicrobial, Oral bioavailability
Abstract: 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.
Export Options
About this article
Cite this article as:
Li Qingyong, He Wuna, Zhang Li, Zu Yuangang, Zhu Qiaochu, Deng Xiaoqiu, Zhao Tengfei, Gao Wenqing and Zhang Baoyou, Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues, Letters in Drug Design & Discovery 2012; 9 (6) . https://dx.doi.org/10.2174/157018012800673010
DOI https://dx.doi.org/10.2174/157018012800673010 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Novel Molecular Targets and Mechanisms Involved in the Invasion and Metastasis of Pancreatic Cancer
Clinical Cancer Drugs Targeting ErbB Receptors in High-Grade Glioma
Current Pharmaceutical Design Kisspeptin: Paving the Way to a New Therapeutic Avenue in Reproduction
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Selectively Replicating Adenoviruses for Oncolytic Therapy
Current Cancer Drug Targets Design, Synthesis and in vitro Cytotoxicity Evaluation of New 3',4'-bis (3,4,5-trisubstituted)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one Derivatives as Promising Anticancer Agents
Letters in Drug Design & Discovery Peptide Self-Assembly for Therapeutic Applications
Current Organic Chemistry MiR-92a-3p Promotes the Malignant Progression of Hepatocellular Carcinoma by Mediating the PI3K/AKT/mTOR Signaling Pathway
Current Pharmaceutical Design Editorial: [Hot Topic: Bio-Pharmaceutics and Materials in Oral Cavity]
Current Pharmaceutical Design Approaches for Imaging the Diabetic Pancreas: First Results
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Exosomes: The Messengers of Health and Disease
Current Neuropharmacology How to Target Activated Ras Proteins: Direct Inhibition vs. Induced Mislocalization
Mini-Reviews in Medicinal Chemistry Histone Deacetylase Inhibitors: Recent Insights from Basic to Clinical Knowledge & Patenting of Anti-Cancer Actions
Recent Patents on Anti-Cancer Drug Discovery Improving Brain Drug Targeting Through Exploitation of The Nose-to- Brain Route: A Physiological and Pharmacokinetic Perspective
Current Drug Delivery The Transcription Factor ETS-1: Its Role in Tumour Development and Strategies for its Inhibition
Mini-Reviews in Medicinal Chemistry Benzofuran Small Molecules as Potential Inhibitors of Human Protein Kinases. A Review
Current Pharmaceutical Design Immunoregulatory and Effector Activities of Nitric Oxide and Reactive Nitrogen Species in Cancer
Current Medicinal Chemistry Pulmonary and Nasal Anti-Inflammatory and Anti-Allergy Inhalation Aerosol Delivery Systems
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Molecular Basis of Notch Signaling Regulation: A Complex Simplicity
Current Molecular Medicine Patent Selections
Recent Patents on Anti-Cancer Drug Discovery Therapeutic Transfer of DNA Encoding Adenoviral E1A
Recent Patents on Anti-Cancer Drug Discovery