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Effects of alkyl gallates on P-glycoprotein function.

Authors
  • Kitagawa, Shuji
  • Nabekura, Tomohiro
  • Kamiyama, Shizu
  • Takahashi, Tomoharu
  • Nakamura, Yutaka
  • Kashiwada, Yoshiki
  • Ikeshiro, Yasumasa
Type
Published Article
Journal
Biochemical Pharmacology
Publisher
Elsevier
Publication Date
Oct 15, 2005
Volume
70
Issue
8
Pages
1262–1266
Identifiers
PMID: 16139251
Source
Medline
License
Unknown

Abstract

In this study, we examined the effects of the food antioxidants, alkyl gallates, on the function of P-glycoprotein (P-gp) and elucidated the importance of alkyl chains and gallic acid moieties on the activity of P-gp. We examined the effects of three alkyl (n-butyl, n-octyl and n-dodecyl) gallates and their related compounds on the cellular accumulation and efflux of rhodamine 123 and daunorubicin in P-gp overexpressing KB-C2 cells. Alkyl gallates increased the cellular accumulation of these P-gp substrates dependent on their alkyl chain lengths by inhibiting the efflux of the substrates. n-Dodecylresorcinol also increased the accumulation, but its effect was less than that of n-dodecyl gallate. However, either lauric acid or n-dodecyl-beta-d-maltoside, which does not have a phenol group, did not increase the accumulation. The results indicated that both the gallic acid moiety and a long alkyl chain play important roles in the modification of P-gp function. The cytotoxicity of daunorubicin was recovered in the presence of alkyl gallates possibly due to their inhibition of P-gp function.

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