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In vitro activities of enantiopure and racemic 1′-acetoxychavicol acetate against clinical isolates of Mycobacterium tuberculosis
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Metadata
Document Title
In vitro activities of enantiopure and racemic 1'-acetoxychavicol acetate against clinical isolates of Mycobacterium tuberculosis
Author
Warit S.,Rukseree K.,Prammananan T.,Hongmanee P.,Billamas P.,Jaitrong S.,Chaiprasert A.,Jaki B.U.,Pauli G.F.,Franzblau S.G.,Palittapongarnpim P.
Name from Authors Collection
Scopus Author ID
8974555500
Scopus Author ID
55544000600
Affiliations
Tuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani, 12120, Thailand; Science and Liberal Art, Mahidol University, Amnatcharoen Campus, Bangkok, 73170, Thailand; Department of Pathology, Faculty of Medicine Ramathibodi Hospital, Mahidol University, Bangkok, 73170, Thailand; Department of Microbiology, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok, 73170, Thailand; Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60607, United States; Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60607, United States; Department of Microbiology, Faculty of Science, Mahidol University, Bangkok, 73170, Thailand
Type
Article
Source Title
Scientia Pharmaceutica
ISSN
00368709
Year
2017
Volume
85
Issue
3
Open Access
All Open Access, Gold, Green
Publisher
MDPI AG
DOI
10.3390/scipharm85030032
Abstract
In the process of evaluating the effect of several plant extracts against Mycobacterium tuberculosis using the Microplate Alamar Blue Assay (MABA), an extract of Thai herb Alpinia galanga rhizome and its major component, l'-acetoxychavicol acetate (ACA), exhibited marked anti-tuberculosis activity. The minimal inhibition concentrations (MICs) of the S-enantiomer of ACA (S-ACA) against M. tuberculosis H37R/7 ATCC 25177 and H37Rv ATCC 27294 strains were 0.2 μg/mL and 0.7 μg/mL, respectively. More than 95% of 100 drug-sensitive and 50 drug-resistant mycobacterial clinical isolates were inhibited by extracted S-ACA at 1.0 μg/mL. All of the remaining isolates were inhibited at 2.0 μg/mL. In contrast to the S-enantiomer, synthetic racemic 1'-R,S-ACA (rac-ACA) showed MICs of 0.5 μg/mL and 2.7 μg/mL for M. tuberculosis H37Ra ATCC 25177 and H37Rv ATCC 27294, respectively, suggesting that the anti-tuberculosis effect might be primarily due to the S-form. These observations were in line with the MICs of rac-ACA against 98% of 93 drug-resistant clinical isolates, which showed the effective inhibitory dose at 2.0 μg/mL. After exposure to 2.7 μg/mL of rac-ACA for at least 3 h, the tubercle bacilli were completely killed. These demonstrated that ACA had potent anti-TB activity. © 2017 by the authors.
Industrial Classification
Knowledge Taxonomy Level 1
Knowledge Taxonomy Level 2
Knowledge Taxonomy Level 3
Funding Sponsor
National Science and Technology Development Agency; National Center for Genetic Engineering and Biotechnology
License
CC BY
Rights
Author
Publication Source
Scopus