Antidermatophytic and Protease-inhibiting Activities of Zerumbone: A Natural Sesquiterpene from the Rhizome of (L.) Roscoe ex J.E; Smith.

CONTEXT

Due to increase in the number of patients with impaired immunity, incidence of dermatophytoses has increased considerably. Antidermatophytic agents with anti-inflammatory and protease-inhibiting activities will help in restricting inflammatory response associated with dermatophytoses.

AIMS

The present study aims to evaluate antidermatophytic and protease-inhibiting activities of zerumbone. Cytotoxicity was tested using Chang liver cell line as a preliminary step in toxicity study.

METHODS AND MATERIALS

Minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of zerumbone purified from the rhizome of were determined against var. nigricans, , , and . MIC was determined according to Clinical and Laboratory Standards Institute (CLSI) method M38-A2. Protease-inhibiting property was tested using trypsin as the enzyme. cytotoxic effect was studied using the MTT assay.

RESULTS

MIC of zerumbone was 8 mg/L against and and 16 mg/L for and . MFC of zerumbone was 64 mg/L against and and 128 mg/L for and . Zerumbone exhibited remarkable protease-inhibiting activity. In the MTT assay, IC values were 150 and 0.31 µg, respectively, for zerumbone and reference drug.

STATISTICAL ANALYSIS USED

For protease inhibition, assay and cytotoxicity assay control and tests were done in triplicate and the results are expressed as mean ± SD, where = 3.

CONCLUSIONS

Zerumbone is a novel candidate for use in dermatophytoses therapy because of the combined antifungal, anti-inflammatory (unpublished results), and protease-inhibiting properties. Cytotoxicity of zerumbone was found to be very low compared with the reference drug.

KEY MESSAGES

Zerumbone possesses antidermatophytic, anti-inflammatory, and protease-inhibiting activities. Hence, it is a novel candidate for the development of new antidermatophytic drug.Cytotoxicity of zerumbone against Chang liver cell line was found to be very low compared with the reference drug doxorubicin.

SUMMARY

Zerumbone isolated from the rhizome of exhibited antidermatophytic activity against and (MIC 8 mg/L) and and (MIC 16 mg/L).Zerumbone exhibited remarkable protease-inhibiting activity.Zerumbone is a novel candidate for the development of new antidermatophytic drug.Cytotoxicity of zerumbone against Chang liver cell line was found to be very low compared with the reference drug doxorubicin. CFU: colony forming unit, CLSI: Clinical and Laboratory Standards Institute, COX: cyclooxygenase, DMSO: dimethyl sulphoxide, EDTA: ethylene diamine tetra acetic acid, FT-IR: Fourier transform-infra red spectroscopy, HPLC: high-performance liquid chromatography, LOX: lipoxygenase, IMTECH: Institute of Microbial Technology, LCMS: liquid chromatography mass spectrometry, MTT: 3-(4,5 dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide, MTCC: microbial type culture collection, MFC: minimum fungicidal concentration, MIC: minimum inhibitory concentration, MPO: myeloperoxidase, NMR: nuclear magnetic resonance spectroscopy, PAR: proteinase-activated receptor, PBS: phosphate-buffered saline, TCA: trichloro acetic acid.