In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis

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, 1′-acetoxychavicol acetate (ACA), exhibited marked anti-tuberculosis activity....

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Main Authors: Saradee Warit, Kamolchanok Rukseree, Therdsak Prammananan, Poonpilas Hongmanee, Pamaree Billamas, Sarinya Jaitrong, Angkana Chaiprasert, Birgit U. Jaki, Guido F. Pauli, Scott G. Franzblau, Prasit Palittapongarnpim
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语言:English
出版: MDPI AG 2017-09-01
丛编:Scientia Pharmaceutica
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在线阅读:https://www.mdpi.com/2218-0532/85/3/32
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author Saradee Warit
Kamolchanok Rukseree
Therdsak Prammananan
Poonpilas Hongmanee
Pamaree Billamas
Sarinya Jaitrong
Angkana Chaiprasert
Birgit U. Jaki
Guido F. Pauli
Scott G. Franzblau
Prasit Palittapongarnpim
author_facet Saradee Warit
Kamolchanok Rukseree
Therdsak Prammananan
Poonpilas Hongmanee
Pamaree Billamas
Sarinya Jaitrong
Angkana Chaiprasert
Birgit U. Jaki
Guido F. Pauli
Scott G. Franzblau
Prasit Palittapongarnpim
author_sort Saradee Warit
collection DOAJ
description 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, 1′-acetoxychavicol acetate (ACA), exhibited marked anti-tuberculosis activity. The minimal inhibition concentrations (MICs) of the S-enantiomer of ACA (S-ACA) against M. tuberculosis H37Ra 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.
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spelling doaj.art-db2dd85e51ff423b83c44c9b81e5c00d2022-12-22T04:25:15ZengMDPI AGScientia Pharmaceutica2218-05322017-09-018533210.3390/scipharm85030032scipharm85030032In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosisSaradee Warit0Kamolchanok Rukseree1Therdsak Prammananan2Poonpilas Hongmanee3Pamaree Billamas4Sarinya Jaitrong5Angkana Chaiprasert6Birgit U. Jaki7Guido F. Pauli8Scott G. Franzblau9Prasit Palittapongarnpim10Tuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani 12120, ThailandScience and Liberal Art, Amnatcharoen Campus, Mahidol University, Bangkok 73170, ThailandTuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani 12120, ThailandDepartment of Pathology, Faculty of Medicine Ramathibodi Hospital, Mahidol University, Bangkok 73170, ThailandTuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani 12120, ThailandTuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani 12120, ThailandDepartment of Microbiology, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok 73170, ThailandInstitute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60607, USAInstitute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60607, USAInstitute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60607, USATuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani 12120, ThailandIn 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, 1′-acetoxychavicol acetate (ACA), exhibited marked anti-tuberculosis activity. The minimal inhibition concentrations (MICs) of the S-enantiomer of ACA (S-ACA) against M. tuberculosis H37Ra 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.https://www.mdpi.com/2218-0532/85/3/32Alpinia galanga1’-S-acetoxychavicol acetateanti-tuberculosisdrug resistance
spellingShingle Saradee Warit
Kamolchanok Rukseree
Therdsak Prammananan
Poonpilas Hongmanee
Pamaree Billamas
Sarinya Jaitrong
Angkana Chaiprasert
Birgit U. Jaki
Guido F. Pauli
Scott G. Franzblau
Prasit Palittapongarnpim
In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis
Scientia Pharmaceutica
Alpinia galanga
1’-S-acetoxychavicol acetate
anti-tuberculosis
drug resistance
title In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis
title_full In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis
title_fullStr In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis
title_full_unstemmed In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis
title_short In Vitro Activities of Enantiopure and Racemic 1′-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis
title_sort in vitro activities of enantiopure and racemic 1 acetoxychavicol acetate against clinical isolates of mycobacterium tuberculosis
topic Alpinia galanga
1’-S-acetoxychavicol acetate
anti-tuberculosis
drug resistance
url https://www.mdpi.com/2218-0532/85/3/32
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