Inhibitory effects of natural products on Aldo-keto reductase family 1 B10

Inhibitory effects of natural products on Aldo-keto reductase family 1 B10
AKR1B10; aldo-keto reductase family 1 B10; natural product; cancer therapy; seaweed
Issue Date
The13th international symposium on the efficient application and preservation of marine biological resources
AKR1B10 has been considered as a potential cancer therapeutic target. We examined ethanol extracts prepared from 111 plants and 33 seaweeds for their inhibitory effects on recombinant human AKR1B10 (rhAKR1B10). To do this, rhAKR1B10 was first expressed in E. coli as an active form and purified by using Ni-affinity chromatography followed by gel permeation chromatography. Then, rhAKR1B10 was used for screening out 144 extracts. Among them, 25 extracts showed more than 50% inhibition of rhAKR1B10 activity at 10μg/ml of concentration. Especially, the extracts of Ligularia fischeri var. spiciformis Nakai and Rhus trichocarpa Miq. were the most potent because their IC50 values were 2.94 and 2.00 μg/ml, respectively. Fractions from Gymnaster koraiensis, Artemisia dubia and Rhus verniciflua were tested for rhAKR1B10 inhibition, and then active compounds were isolated from the most potent fraction of each plant. 3,5-O-Dicaffeoylquinic acid (3,5-DCQA) was isolated from ethyl acetate fraction of Gymnaster koraiensis as an AKR1B10 inhibitor and showed IC50 value of 1.2 μM. 3,4-DCQA, 3,5-DCQA, 4,5-DCQA, 3,5-DCQA methyl ester and 4,5-DCQA methyl ester were isolated from ethyl acetate fraction of Artemisia dubia and their IC50 values were 2.3, 1.5, 1.2, 1.7, 2.0 μM, respectively. Butein was isolated from ethyl acetate fraction of Rhus verniciflua and its IC50 value was 1.5 μM. According to enzyme kinetic analysis, all active compounds inhibited rhAKR1B10 uncompetitively.
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