Inhibition of Human Kallikrein 5 Protease by Triterpenoids from Natural Sources.

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Yosuke MatsubaraKenshi Yamasaki

Abstract

Stratum corneum tryptic enzyme kallikrein 5 (KLK5) is a serine protease that is involved in the cell renewal and maintenance of the skin barrier function. The excessive activation of KLK5 causes an exacerbation of dermatoses, such as rosacea and atopic dermatitis. Some triterpenoids are reported to suppress the serine proteases. We aimed to investigate whether bioactive triterpenoids modulate the KLK5 protease. Nineteen triterpenoids occurring in medicinal crude drugs were evaluated using an enzymatic assay to measure the anti-KLK5 activity. The KLK5-dependent cathelicidin peptide LL-37 production in human keratinocytes was examined using immunoprecipitation and Western blotting. Screening assays for evaluating the anti-KLK5 activity revealed that ursolic acid, oleanolic acid, saikosaponin b₁, tumulosic acid and pachymic acid suppressed the KLK5 protease activity, although critical molecular moieties contributing to anti-KLK5 activity were unclarified. Ursolic acid and tumulosic acid suppressed the proteolytic processing of LL-37 in keratinocytes at ≤10 μM; no cytotoxicity was observed. Both triterpenoids were detected in the plasma of rats administered orally with triterpenoid-rich crude drug Jumihaidokuto. Our study reveals t...Continue Reading

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Citations

May 3, 2019·Acta Crystallographica. Section F, Structural Biology Communications·James H ThorpeAlain Hovnanian
Jun 23, 2020·Critical Reviews in Clinical Laboratory Sciences·Caitlin T Di PaoloIoannis Prassas
May 28, 2019·Clinical Chemistry and Laboratory Medicine : CCLM·Caitlin T Di PaoloIoannis Prassas
Dec 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Kyung-Baeg RohEunsun Jung
Feb 6, 2021·Experimental Dermatology·Georgia SotiropoulouGeorgios Pampalakis
Jun 25, 2021·Journal of Inflammation Research·Susanne SchiffmannMichael J Parnham

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Methods Mentioned

BETA
immunoprecipitation
glycosylation
protein assay

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