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Antimicrobial Agents and Chemotherapy, January 2009, p. 216-222, Vol. 53, No. 1
0066-4804/09/$08.00+0     doi:10.1128/AAC.00045-08
Copyright © 2009, American Society for Microbiology. All Rights Reserved.

Evaluation of the Antimicrobial, Antioxidant, and Anti-Inflammatory Activities of Hydroxychavicol for Its Potential Use as an Oral Care Agent{triangledown}

Sandeep Sharma,1 Inshad Ali Khan,1* Intzar Ali,1 Furqan Ali,1 Manoj Kumar,1 Ashwani Kumar,1 Rakesh Kamal Johri,2 Sheikh Tasduq Abdullah,2 Sarang Bani,2 Anjali Pandey,2 Krishan Avtar Suri,3 Bishan Datt Gupta,3 Naresh Kumar Satti,3 Prabhu Dutt,3 and Ghulam Nabi Qazi1

Biotechnology Division,1 Pharmacology Division,2 Natural Product Chemistry Division, Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India3

Received 13 January 2008/ Returned for modification 5 March 2008/ Accepted 13 June 2008

Hydroxychavicol isolated from the chloroform extraction of aqueous extract of Piper betle leaves showed inhibitory activity against oral cavity pathogens. It exhibited an inhibitory effect on all of the oral cavity pathogens tested (MICs of 62.5 to 500 µg/ml) with a minimal bactericidal concentration that was twofold greater than the inhibitory concentration. Hydroxychavicol exhibited concentration-dependent killing of Streptococcus mutans ATCC 25175 up to 4x MIC and also prevented the formation of water-insoluble glucan. Interestingly, hydroxychavicol exhibited an extended postantibiotic effect of 6 to 7 h and prevented the emergence of mutants of S. mutans ATCC 25175 and Actinomyces viscosus ATCC 15987 at 2x MIC. Furthermore, it also inhibited the growth of biofilms generated by S. mutans and A. viscosus and reduced the preformed biofilms by these bacteria. Increased uptake of propidium iodide by hydroxychavicol-treated cells of S. mutans and A. viscosus indicated that hydroxychavicol probably works through the disruption of the permeability barrier of microbial membrane structures. Hydroxychavicol also exhibited potent antioxidant and anti-inflammatory activities. This was evident from its concentration-dependent inhibition of lipid peroxidation and significant suppression of tumor necrosis factor alpha expression in human neutrophils. Its efficacy against adherent cells of S. mutans in water-insoluble glucan in the presence of sucrose suggests that hydroxychavicol would be a useful compound for the development of antibacterial agents against oral pathogens and that it has great potential for use in mouthwash for preventing and treating oral infections.


* Corresponding author. Mailing address: Biotechnology Division, Indian Institute of Integrative Medicine, Canal Road, Jammu Tawi 180001, India. Phone: 91 191 2569001. Fax: 91 191 2569333. E-mail: iakhan{at}iiim.res.in

{triangledown} Published ahead of print on 23 June 2008.


Antimicrobial Agents and Chemotherapy, January 2009, p. 216-222, Vol. 53, No. 1
0066-4804/09/$08.00+0     doi:10.1128/AAC.00045-08
Copyright © 2009, American Society for Microbiology. All Rights Reserved.