| A bitter melon extract inhibits the P-glycoprotein activity in intestinal Caco-2 cells: monoglyceride as an active compound. | |
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MedLine Citation:
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PMID: 15630255 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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P-glycoprotein (P-gp) is a 170 kDa membrane protein that belongs to the ATP-binding cassette (ABC) transporter superfamily. In normal tissues, P-gp functions as an ATP-dependent efflux pump that excretes highly hydrophobic xenobiotic compounds, playing an important role in protecting the cells/tissues from xenobiotics. In the present study, chemical substances that could directly modulate the intestinal P-gp activity were searched in vegetables and fruits. By using human intestinal epithelial Caco-2 cells as a model of the small intestinal cells, we observed that a bitter melon fraction extracted from 40% methanol showed the greatest increase of the rhodamine-123 accumulation by Caco-2 cells. Inhibitory compounds in the bitter melon fraction were then isolated by HPLC using Pegasil C4 and Pegasil ODS columns. The HPLC fraction having the highest activity was analyzed by (1)H-NMR and FAB-MS, and the active compound was identified as 1-monopalmitin. It is interesting that certain types of monoglyceride might be involved in the drug bioavailability by specifically inhibiting the efflux mediated by P-gp. |
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Authors:
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Tomoko Konishi; Hideo Satsu; Yasuo Hatsugai; Koichi Aizawa; Takahiro Inakuma; Shinji Nagata; Sho-hei Sakuda; Hiromichi Nagasawa; Makoto Shimizu |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: BioFactors (Oxford, England) Volume: 22 ISSN: 0951-6433 ISO Abbreviation: Biofactors Publication Date: 2004 |
Date Detail:
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Created Date: 2005-01-04 Completed Date: 2005-04-14 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8807441 Medline TA: Biofactors Country: Netherlands |
Other Details:
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Languages: eng Pagination: 71-4 Citation Subset: IM |
Affiliation:
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Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Cell Line, Tumor Chromatography, High Pressure Liquid Colonic Neoplasms Cucurbitaceae* Daunorubicin / pharmacokinetics Glycerides / pharmacology* Humans P-Glycoprotein / antagonists & inhibitors*, drug effects Palmitic Acid / pharmacology Phytotherapy Plant Extracts / isolation & purification, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Glycerides; 0/P-Glycoprotein; 0/Plant Extracts; 20830-81-3/Daunorubicin; 57-10-3/Palmitic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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