| Inhibition of anticancer drug efflux transporter P-glycoprotein by rosemary phytochemicals. | |
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MedLine Citation:
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PMID: 19944162 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The effects of dietary antioxidative and chemopreventive rosemary phytochemicals on the function of the human drug efflux transporter P-glycoprotein (MDR1, ABCB1) and multidrug resistance protein 1 (MRP1, ABCC1) were investigated using P-glycoprotein-overexpressing human carcinoma KB-C2 cells and human MRP1 gene-transfected KB/MRP cells. The effects of natural phytochemicals found in rosemary such as carnosic acid, carnosol, rosmarinic acid, and ursolic acid were investigated. The accumulation of daunorubicin or rhodamine 123, fluorescent substrates of P-glycoprotein, in KB-C2 cells increased in the presence of carnosic acid, carnosol, and ursolic acid in a concentration-dependent manner. In contrast, carnosic acid, carnosol, rosmarinic acid, and ursolic acid had no effects on the accumulation of calcein, a fluorescent substrate of MRP1, in KB/MRP cells. The ATPase activities of P-glycoprotein were stimulated by carnosic acid, carnosol, and ursolic acid. KB-C2 cells were sensitized to vinblastine cytotoxicity by carnosic acid, showing that carnosic acid reverses multidrug resistance. These results suggest that rosemary phytochemicals, such as carnosic acid, have inhibitory effects on anticancer drug efflux transporter P-glycoprotein and may become useful to enhance the efficacy of cancer chemotherapy. |
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Authors:
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Tomohiro Nabekura; Takeshi Yamaki; Takashi Hiroi; Kazuyuki Ueno; Shuji Kitagawa |
Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't Date: 2009-11-26 |
Journal Detail:
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Title: Pharmacological research : the official journal of the Italian Pharmacological Society Volume: 61 ISSN: 1096-1186 ISO Abbreviation: Pharmacol. Res. Publication Date: 2010 Mar |
Date Detail:
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Created Date: 2010-03-15 Completed Date: 2010-10-28 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8907422 Medline TA: Pharmacol Res Country: England |
Other Details:
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Languages: eng Pagination: 259-63 Citation Subset: IM |
Copyright Information:
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2009 Elsevier Ltd. All rights reserved. |
Affiliation:
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Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Higashi-jima, Akiha-ku, Niigata 956-8603, Japan. nabe@nupals.ac.jp |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents, Phytogenic
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isolation & purification,
pharmacology* Daunorubicin / metabolism Humans KB Cells Multidrug Resistance-Associated Proteins P-Glycoprotein / antagonists & inhibitors*, physiology Phytotherapy Plant Extracts / isolation & purification, pharmacology* Plant Leaves / chemistry, physiology Rosmarinus / chemistry*, physiology |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents, Phytogenic; 0/Multidrug Resistance-Associated Proteins; 0/P-Glycoprotein; 0/Plant Extracts; 0/multidrug resistance-associated protein 1; 20830-81-3/Daunorubicin |
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