Document Detail


The HMG-CoA reductase inhibitor pravastatin stimulates insulin secretion through organic anion transporter polypeptides.
MedLine Citation:
PMID:  20610886     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor pravastatin has been reported to have a beneficial effect on reducing the new onset of diabetes as well as lowering plasma lipids. Because pravastatin is a water-soluble organic anion, it cannot easily penetrate the lipid bilayer of the cell membrane. As the precise mechanisms of the effect of pravastatin on glucose metabolism and diabetes have not been clarified, we examined the roles of the organic anion transporter family on pravastatin-treated islet and adipocyte functions. Rat oatp1/slco1a1, oatp2/slco1a4 and oatp3/slco1a5 were expressed in the pancreas, and rat oatp3/slco1a5 was also detected in rat insulinoma cell line INS-1e. Pravastatin was transported not only by oatp1/slco1a1 and oatp2/slco1a4, but also by rat oatp3/slco1a5. Pravastatin uptake into INS-1e cells was detected and this transport was inhibited by sulfobromophthalein and rifampicin, both of which are known to inhibit oatp family-mediated uptake. In addition, pravastatin enhanced the glucose-stimulated insulin secretion from INS-1e cells. When fat-loaded db/db mice were treated with pravastatin, glucose intolerance and insulin resistance were prevented. In addition, insulin secretion from isolated islets was enhanced by pravastatin. These data suggest that pravastatin has pleiotropic effects on islets through membrane transport under high fat/glucose conditions.
Authors:
Michiaki Abe; Takafumi Toyohara; Akiko Ishii; Takehiro Suzuki; Naoya Noguchi; Yasutoshi Akiyama; Hiromi O Shiwaku; Rie Nakagomi-Hagihara; Guodong Zheng; Eisuke Shibata; Tomokazu Souma; Tomohiko Shindo; Hirohito Shima; Yoichi Takeuchi; Eikan Mishima; Masayuki Tanemoto; Tetsuya Terasaki; Tohru Onogawa; Michiaki Unno; Sadayoshi Ito; Shin Takasawa; Takaaki Abe
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Drug metabolism and pharmacokinetics     Volume:  25     ISSN:  1880-0920     ISO Abbreviation:  Drug Metab. Pharmacokinet.     Publication Date:  2010  
Date Detail:
Created Date:  2010-07-08     Completed Date:  2010-10-12     Revised Date:  2012-04-09    
Medline Journal Info:
Nlm Unique ID:  101164773     Medline TA:  Drug Metab Pharmacokinet     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  274-82     Citation Subset:  IM    
Affiliation:
Division of Nephrology, Endocrinology, and Vascular Medicine, Tohoku University Graduate School of Medicine, 1-1 Seiryo-cho, Aoba-ku, Sendai, Japan.
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MeSH Terms
Descriptor/Qualifier:
Adiponectin / blood
Animals
Biological Transport / drug effects
Cell Line, Tumor
Diabetes Mellitus / drug therapy
Hydroxymethylglutaryl CoA Reductases
Immunohistochemistry
Insulin / agonists,  secretion*
Islets of Langerhans / cytology*,  drug effects
Male
Mice
Mice, Inbred Strains
Models, Animal
Organic Anion Transporters, Sodium-Independent / analysis,  metabolism*
Pancreas / cytology,  drug effects
Pravastatin / pharmacokinetics*,  pharmacology*
Rats
Rifampin / pharmacology
Sulfobromophthalein / pharmacology
Chemical
Reg. No./Substance:
0/Adiponectin; 0/Adipoq protein, mouse; 0/Insulin; 0/Organic Anion Transporters, Sodium-Independent; 13292-46-1/Rifampin; 297-83-6/Sulfobromophthalein; 81093-37-0/Pravastatin; EC 1.1.1.-/Hydroxymethylglutaryl CoA Reductases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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