Inhibitory effects of phlorofucofuroeckol-A isolated from Eisenia bicyclis on aldo-keto reductase family 1 B1 and 1 B10
- Inhibitory effects of phlorofucofuroeckol-A isolated from Eisenia bicyclis on aldo-keto reductase family 1 B1 and 1 B10
- 이주영; 김상민; 송대근; 정우석; 차광현; 엄병헌; 손진기; 판철호
- phlorofucofuroeckol-A; Eisenia bicyclis; aldo-keto reductase; AKR1B1; AKR1B10
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- 한국응용생명화학회 춘계학술대회
- Aldo-keto reductase family 1 B1 (AKR1B1) and 1 B10 (AKR1B10) are members of the NADPH-dependent aldo-keto reductase (AKR) superfamily. AKR1B1 catalyzes the NADPH-dependent conversion of glucose to sorbitol, the first step in polyol pathway of glucose metabolism. AKR1B10 was identified as a biomarker of lung cancer showing high sequence identity with human AKR1B1. During the screening of inhibition ativity against AKR1B1 and AKR1B10 from seaweed extracts, Eisenia bicyclis extract showed dual inhibition activities. To identify the active compounds from Eisenia bicyclis responsible for both inhibition activities, five compounds were isolated via bioactivity-guided fractionation and isolation. Among them, phlorofucofuroeckol-A (PFF-A) isolated from ethyl acetate fraction was most able to inhibit both enzymes. The inhibitory rate of PFF-A against AKR1B1 was 61.24% at 10 μM with an IC50 of 6.54 μM, and enzyme kinetic analysis revealed its inhibition mode to be uncompetitive. For AKR1B10, the inhibitory rate of PFF-A was 61.41% at 10 μM with an IC50 of 6.22 μM, and its inhibition mode was noncompetitive.(SRAA)
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