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Mesima, Sanghwang · 2004 · Research Support, Non U.S. Gov'T

Medium relevance

A beta-secretase (BACE1) inhibitor hispidin from the mycelial cultures of Phellinus linteus.

Phellinus linteus

Oncology
SpeciesMesima, Sanghwang
JournalPlanta medica
Year2004

Key points

  • In the course of screening for anti-dementia agents from natural products, a beta-secretase (BACE1) inhibitor was isolated from the culture broth of Phellinus linteus and identified as hispidin
  • It showed an IC (50) value of 4.9 x 10 (-6) M and a Ki value of 8.4 x 10 (-6) M. The compound was a non-competitive inhibitor
  • Hispidin also inhibited a prolyl endopeptidase (IC (50) = 1.6 x 10 (-5) M, Ki = 2.4 x 10 (-5) M), but it was less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase

Metadata-grounded summary

Citation abstract

In the course of screening for anti-dementia agents from natural products, a beta-secretase (BACE1) inhibitor was isolated from the culture broth of Phellinus linteus and identified as hispidin. It showed an IC (50) value of 4.9 x 10 (-6) M and a Ki value of 8.4 x 10 (-6) M. The compound was a non-competitive inhibitor. Hispidin also inhibited a prolyl endopeptidase (IC (50) = 1.6 x 10 (-5) M, Ki = 2.4 x 10 (-5) M), but it was less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase.

Citation

Park IH, Jeon SY, Lee HJ, Kim SI, Song KS (2004). A beta-secretase (BACE1) inhibitor hispidin from the mycelial cultures of Phellinus linteus. Planta medica https://doi.org/10.1055/s-2004-815491 PMID: 14994192

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