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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2010.1
- 수록면
- 268 - 272 (5page)
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Aldo-keto reductase family 1 B10 (AKR1B10) is a member of the NADPH-dependent aldo-keto reductase (AKR) superfamily,and has been considered to be a potential cancer therapeutic target. Total extract from the bark of Rhus verniciflua (Toxicodendron vernicifluum (Stokes)) showed AKR1B10 inhibitory activity. To identify the active compounds from R. verniciflua responsible for AKR1B10 inhibition, nine compounds were isolated via bioactivity-guided isolation and tested for their effects against recombinant human AKR1B10 (rhAKR1B10).
Results showed that butein, isolated from the ethyl acetate fraction, was most able to inhibit rhAKR1B10. The inhibitory rate of butein against rhAKR1B10 was 42.86% at 1 μM with an IC50 value of 1.47 μM, and enzyme kinetic analysis revealed its inhibition mode to be uncompetitive.
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참고문헌 (21)
참고문헌 신청
Cao, D. / 1998 / Identification and characterization of a novel human aldose reductase-like gene / J. Biol. Chem. 273 : 11429 ~ 11435
Crosas, B. / 2003 / Human aldose reductase and human small intestine aldose reductase are efficient retinal reductases: consequences for retinoid metabolism / Biochem J. 373
Dunlop, M. / 2000 / Aldose reductase and the role of the polyol pathway in diabetic nephropathy / Kidney Int. 77 : S3 ~ S12
Endo, S. / 2009 / Kinetic studies of AKR1B10, human aldose reductase-like protein: endogenous substrates and inhibition by steroids / Arch. Biochem. Biophys. 487 : 1 ~ 9
Frank, R. N. / 1983 / Galactose-induced retinal capillary basement membrane thickening: prevention by Sorbinil / Invest. Ophthalmol. Vis. Sci. 24 : 1519 ~ 1524
Crosas, B. / 2003 / Human aldose reductase and human small intestine aldose reductase are efficient retinal reductases: consequences for retinoid metabolism / Biochem J. 373
Dunlop, M. / 2000 / Aldose reductase and the role of the polyol pathway in diabetic nephropathy / Kidney Int. 77 : S3 ~ S12
Endo, S. / 2009 / Kinetic studies of AKR1B10, human aldose reductase-like protein: endogenous substrates and inhibition by steroids / Arch. Biochem. Biophys. 487 : 1 ~ 9
Frank, R. N. / 1983 / Galactose-induced retinal capillary basement membrane thickening: prevention by Sorbinil / Invest. Ophthalmol. Vis. Sci. 24 : 1519 ~ 1524
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