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

Scientia Pharmaceutica

Angkana Chaiprasert¹  Poonpilas Hongmanee²  Scott G. Franzblau³  Birgit U. Jaki³  Guido F. Pauli³  Kamolchanok Rukseree⁴  Sarinya Jaitrong⁵  Pamaree Billamas⁵  Saradee Warit⁵  Therdsak Prammananan⁵  Prasit Palittapongarnpim⁵ 

[1] Department of Microbiology, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok 73170, Thailand;Department of Pathology, Faculty of Medicine Ramathibodi Hospital, Mahidol University, Bangkok 73170, Thailand;Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60607, USA;Science and Liberal Art, Amnatcharoen Campus, Mahidol University, Bangkok 73170, Thailand;Tuberculosis Research Laboratory, Medical Molecular Biology Research Unit, BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani 12120, Thailand;

关键词: Alpinia galanga;    1’-S-acetoxychavicol acetate;    anti-tuberculosis;    drug resistance;   

DOI  :  10.3390/scipharm85030032

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown