Chlorhexidine Inhibits the Activity of Dental Cysteine Cathepsins

Chlorhexidine Inhibits the Activity of Dental Cysteine Cathepsins

Author Scaffa, Polliana Mendes Candia Google Scholar
Vidal, Cristina de Mattos Pimenta Google Scholar
Barros, Nilana Meza Tenório de Autor UNIFESP Google Scholar
Gesteira, Tarsis Ferreira Autor UNIFESP Google Scholar
Carmona, Adriana Karaoglanovic Autor UNIFESP Google Scholar
Breschi, Lorenzo Google Scholar
Pashley, David H. Google Scholar
Tjaderhane, Leo Google Scholar
Tersariol, Ivarne Luis dos Santos Autor UNIFESP Google Scholar
Nascimento, Fábio Dupart Google Scholar
Carrilho, Marcela Rocha de Oliveira Google Scholar
Institution Univ Bandeirante São Paulo
Universidade Estadual de Campinas (UNICAMP)
Universidade Federal de São Paulo (UNIFESP)
Univ Trieste
Georgia Hlth Sci Univ
Univ Oulu
Oulu Univ Hosp
Univ Mogi das Cruzes
Abstract The co-expression of MMPs and cysteine cathepsins in the human dentin-pulp complex indicates that both classes of enzymes can contribute to the endogenous proteolytic activity of dentin. Chlorhexidine (CHX) is an efficient inhibitor of MMP activity. This study investigated whether CHX could also inhibit cysteine cathepsins present in dentin. the inhibitory profile of CHX on the activity of dentin-extracted and recombinant cysteine cathepsins (B, K, and L) was monitored in fluorogenic substrates. the rate of substrate hydrolysis was spectrofluorimetrically measured, and inhibitory constants were calculated. Molecular docking was performed to predict the binding affinity between CHX and cysteine cathepsins. the results showed that CHX inhibited the proteolytic activity of dentin-extracted cysteine cathepsins in a dose-dependent manner. the proteolytic activity of human recombinant cathepsins was also inhibited by CHX. Molecular docking analysis suggested that CHX strongly interacts with the subsites S2 to S2' of cysteine cathepsins B, K, and L in a very similar manner. Taken together, these results clearly showed that CHX is a potent inhibitor of the cysteine cathepsins-proteolytic enzymes present in the dentin-pulp complex.
Keywords Cysteine cathepsins
Proteolytic activity
Language English
Sponsor Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Grant number FAPESP: 2007/54618-4
FAPESP: 2011/12226-8
FAPESP: 2009/14005-9
CNPq: 306100/2010-0
Date 2012-04-01
Published in Journal of Dental Research. Thousand Oaks: Sage Publications Inc, v. 91, n. 4, p. 420-425, 2012.
ISSN 0022-0345 (Sherpa/Romeo, impact factor)
Publisher Sage Publications Inc
Extent 420-425
Access rights Closed access
Type Article
Web of Science ID WOS:000301874200015

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