Inhibitory effects of polyphenols isolated from Rhus verniciflua on Aldo-keto reductase family 1 B10
- Inhibitory effects of polyphenols isolated from Rhus verniciflua on Aldo-keto reductase family 1 B10
- 송대근; 이주영; 이은하; 정상훈; 노주원; 차광현; 구송이; 판철호
- AKR1B10; Aldo-keto reductase; Aldose reductase-like; anticancer; butein; polyphenol; Rhus verniciflua
- Issue Date
- BMB REPORTS
- VOL 43, NO 4, 268-272
- 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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