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- Shuji Kitagawa
- Niigata University of Pharmacy and Applied Life Sciences, Kamishin'ei-cho 5-13-2, Niigata 950-2081, Japan
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- Tomohiro Nabekura
- Niigata University of Pharmacy and Applied Life Sciences, Kamishin'ei-cho 5-13-2, Niigata 950-2081, Japan
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- Shizu Kamiyama
- Niigata University of Pharmacy and Applied Life Sciences, Kamishin'ei-cho 5-13-2, Niigata 950-2081, Japan
抄録
<jats:title>Abstract</jats:title> <jats:p>We studied the effects of tea catechins, (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epicatechin gallate (ECG), and (-)-epigallocatechin gallate (EGCG) on the P-glycoprotein (P-gp) function in multidrug-resistant P-gp over-expressing KB-C2 cells. EC did not have any effects on cellular accumulation of P-gp substrates, rhodamine-123 and daunorubicin, but the other catechins increased the accumulation in the order of EGC<ECG<EGCG. The effects of EGCG were larger than those of verapamil and quercetin. Since these catechins inhibited the efflux of P-gp substrates, the elevation of substrate accumulation seemed to be induced by the inhibition of the efflux transporter. The results showed that the inhibitory effects of the catechins did not depend on their total hydrophobicity, but significantly depended on their chemical structure. The presence of the galloyl moiety on the C-ring markedly increased the n-octanol/PBS partition coefficients of the catechins and their activity on P-gp. On the other hand, the presence of the trihydric pyrogallol group as the B-ring decreased the partition coefficients but increased the activity on P-gp, compared with the action of the corresponding catechins with a dihydric catechol B-ring.</jats:p>
収録刊行物
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- Journal of Pharmacy and Pharmacology
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Journal of Pharmacy and Pharmacology 56 (8), 1001-1005, 2004-08
Oxford University Press (OUP)
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詳細情報 詳細情報について
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- CRID
- 1360574094640402176
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- NII論文ID
- 30023106230
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- ISSN
- 20427158
- 00223573
- http://id.crossref.org/issn/00223573
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