| Design, synthesis, and cholesterol-lowering efficacy for prodrugs of berberrubine. | |
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MedLine Citation:
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PMID: 20673726 Owner: NLM Status: In-Process |
Abstract/OtherAbstract:
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In order to enhance oral bioavailability of berberine (BBR) for its cholesterol-lowering efficacy in vivo, a series of ester or ether prodrugs of berberrubine (M1), which is an active metabolite of BBR after first-pass metabolism, were designed, semi-synthesized, and evaluated. Among these M1 prodrugs, compound 5g possessing palmitate at the 9-position showed a moderate LogP value and esterase hydrolysis rate for releasing M1 in blood. Its cholesterol-lowering efficacy in vivo was evaluated in hyperlipidemic SD rats. Compound 5g (100mg/kg/d) reduced blood CHO and LDL-c by 35.8% and 45.5%, respectively, similar to that by BBR. It also exhibited a good safety in rats with no side-effect on liver and kidney function. Therefore, the design of M1 prodrug appears to be an effective strategy to improve pharmacokinetic feature of BBR for its lipid-lowering efficacy in vivo. |
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Authors:
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Ying-Hong Li; Yi Li; Peng Yang; Wei-Jia Kong; Xue-Fu You; Gang Ren; Hong-Bin Deng; Yue-Ming Wang; Yan-Xiang Wang; Jian-Dong Jiang; Dan-Qing Song |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-07-30 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-08-20 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 6422-8 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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