Phlorofucofuroeckol-A, a Potent Inhibitor of Aldo-keto Reductase Family 1 Member B10, from the Edible Brown Alga Eisenia bicyclis
- Phlorofucofuroeckol-A, a Potent Inhibitor of Aldo-keto Reductase Family 1 Member B10, from the Edible Brown Alga Eisenia bicyclis
- 이주영; 김상민; 정우석; 송대근; 엄병헌; 손진기; 판철호
- aldo-keto reductase; aldo-keto reductase family 1
member B10; Eisenia bicyclis; phlorofucofuroeckol-A; phlorotannins
- Issue Date
- 한국응용생명화학회지; JOURNAL OF THE KOREAN SOCIETY FOR APPLIED BIOLOGICAL CHEMISTRY
- VOL 55, NO 6, 721-727
- Aldo-keto reductase family 1 member B10 (AKR1B10)
belongs to a superfamily of NADPH-dependent aldo-keto reductases
and is considered a biomarker of several cancers. Inhibition of
recombinant human AKR1B10 (rhAKR1B10) was assayed using
31 seaweed extracts, among which, an Eisenia bicyclis extract
was selected for further study. To identify the compounds in E.
bicyclis responsible for inhibitory effects on rhAKR1B10, five
compounds were isolated by bioactivity-guided fractionation and
isolation. Among them, phlorofucofuroeckol-A (PFF-A), isolated
from an ethyl acetate fraction, exhibited the greatest inhibition of
rhAKR1B10. The inhibitory rate of PFF-A against rhAKR1B10
was 61.41% at 10 μM, with an IC50 of 6.22 μM. Enzyme kinetic
analyses revealed non-competitive inhibition with a KD of 2.76
μM. These results indicate that PFF-A from E. bicyclis may be a
promising anticancer agent.
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