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, 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.

Highlights

  • Tuberculosis (TB) is caused by Mycobacterium tuberculosis and constitutes a major health problem exacerbated by the global human immunodeficiency virus (HIV) pandemic and the emergence

  • Five hundred microliters of the diluted culture were inoculated into each MGIT 960 tube and incubated until the growth reached about 10,000 growth units (G.U.), when the bacterial growth was in the late log phase, which usually took 8–9 days

  • The minimal inhibition concentrations (MICs) of ACA purified from A. galanga (S-ACA) against standard M. tuberculosis H37Ra and

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Summary

Introduction

Tuberculosis (TB) is caused by Mycobacterium tuberculosis and constitutes a major health problem exacerbated by the global human immunodeficiency virus (HIV) pandemic and the emergence. The activity of 10 -S-acetoxychavicol acetate (S-ACA), a major secondary metabolite of a popular Thai herb, Alpinia galanga (Linn) Swartz The crude rhizome extract of A. galanga has been shown to inhibit the in vitro growth. The crude rhizome extract of A. galanga has been shown to inhibit the in vitro growth of the avirulent of the avirulent M. tuberculosis H37Ra strain [3], streptomycin-resistant M. tuberculosis, M. avium and. Broad spectrum activities of of A. galanga rhizome extracts toward other pathogens have been described since 1976. ACA exhibited blocking coagulation in Staphylococcus aureus, leading to cell death [11]. The present study aimed to determine and compare the inhibitory activities against drug-sensitive and -resistant M. tuberculosis clinical isolates of the purified ACA (enantiopure S-form, S-ACA), as well as the synthetic form (racemic, R,S form, rac-ACA)

Bacterial Strains and Culture Condition
Extraction and Purification of ACA
Results
Discussion
Conclusions

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