A β-Secretase (BACE1) Inhibitor Hispidin from the Mycelial Cultures of Phellinus linteus

 

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Abstract

In the course of screening for anti-dementia agents from natural products, a β-secretase (BACE1) inhibitor was isolated from the culture broth of Phellinus linteus and identified as hispidin. It showed an IC₅₀ value of 4.9 × 10^-6 M and a Ki value of 8.4 × 10^-6 M. The compound was a non-competitive inhibitor. Hispidin also inhibited a prolyl endopeptidase (IC₅₀ = 1.6 × 10^-5 M, Ki = 2.4 × 10^-5 M), but it was less inhibitory to α-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase.

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Prof. Kyung-Sik Song

Division of Applied Biology and Chemistry

College of Agriculture and Life Sciences

Kyungpook National University

1370 Sankyuk-Dong

Daegu 702-701

Korea

Fax: +82-53-956-5715

Email: kssong@knu.ac.kr