Planta Med 2004; 70(2): 143-146
DOI: 10.1055/s-2004-815491
Original Paper
Biochemistry
© Georg Thieme Verlag Stuttgart · New York

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

In-Hye Park1 , So-Young Jeon1 , Hee-Ju Lee1 , Sang-In Kim1 , Kyung-Sik Song1
  • 1Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu, Korea
This work was supported by a grant from the Ministry of Health and Welfare, Korea (grant No. 02-PJ2-PG3 - 21 604 - 0002).
Further Information

Publication History

Received: June 2, 2003

Accepted: November 8, 2003

Publication Date:
02 March 2004 (online)

Preview

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.

References

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