Chlorhexidine inhibits the activity of dental cysteine cathepsins

P. M.C. Scaffa, C. M.P. Vidal, N. Barros, T. F. Gesteira, A. K. Carmona, L. Breschi, David Henry Pashley, L. Tjäderhane, I. L.S. Tersariol, F. D. Nascimento, M. R. Carrilho

Research output: Contribution to journalArticle

117 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)420-425
Number of pages6
JournalJournal of Dental Research
Volume91
Issue number4
DOIs
StatePublished - Apr 1 2012

Fingerprint

Cathepsins
Chlorhexidine
Cysteine
Tooth
Dentin
Cathepsin K
Cathepsin L
Cathepsin B
Molecular Docking Simulation
Matrix Metalloproteinase Inhibitors
Matrix Metalloproteinases
Fluorescent Dyes
Human Activities
Hydrolysis
Peptide Hydrolases
Enzymes

Keywords

  • chlorhexidine
  • collagen
  • cysteine cathepsins
  • degradation
  • dentin
  • proteolytic activity

ASJC Scopus subject areas

  • Dentistry(all)

Cite this

Scaffa, P. M. C., Vidal, C. M. P., Barros, N., Gesteira, T. F., Carmona, A. K., Breschi, L., ... Carrilho, M. R. (2012). Chlorhexidine inhibits the activity of dental cysteine cathepsins. Journal of Dental Research, 91(4), 420-425. https://doi.org/10.1177/0022034511435329

Chlorhexidine inhibits the activity of dental cysteine cathepsins. / Scaffa, P. M.C.; Vidal, C. M.P.; Barros, N.; Gesteira, T. F.; Carmona, A. K.; Breschi, L.; Pashley, David Henry; Tjäderhane, L.; Tersariol, I. L.S.; Nascimento, F. D.; Carrilho, M. R.

In: Journal of Dental Research, Vol. 91, No. 4, 01.04.2012, p. 420-425.

Research output: Contribution to journalArticle

Scaffa, PMC, Vidal, CMP, Barros, N, Gesteira, TF, Carmona, AK, Breschi, L, Pashley, DH, Tjäderhane, L, Tersariol, ILS, Nascimento, FD & Carrilho, MR 2012, 'Chlorhexidine inhibits the activity of dental cysteine cathepsins', Journal of Dental Research, vol. 91, no. 4, pp. 420-425. https://doi.org/10.1177/0022034511435329
Scaffa PMC, Vidal CMP, Barros N, Gesteira TF, Carmona AK, Breschi L et al. Chlorhexidine inhibits the activity of dental cysteine cathepsins. Journal of Dental Research. 2012 Apr 1;91(4):420-425. https://doi.org/10.1177/0022034511435329
Scaffa, P. M.C. ; Vidal, C. M.P. ; Barros, N. ; Gesteira, T. F. ; Carmona, A. K. ; Breschi, L. ; Pashley, David Henry ; Tjäderhane, L. ; Tersariol, I. L.S. ; Nascimento, F. D. ; Carrilho, M. R. / Chlorhexidine inhibits the activity of dental cysteine cathepsins. In: Journal of Dental Research. 2012 ; Vol. 91, No. 4. pp. 420-425.
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