In vitro Antitubercular Activity of 3‐Deoxysappanchalcone Isolated From the Heartwood of Caesalpinia sappan Linn.

Abstract

Responsible for nearly 1.5 million deaths every year, the infectious disease tuberculosis remains one of the most serious challenges to global health. The emergence of multidrug-resistant tuberculosis and, more recently, extensively drug-resistant tuberculosis poses a significant threat in our effort to control this epidemic. New drugs are urgently needed to combat the growing threat of antimicrobial resistance. To achieve this goal, we screened approximately 500 species of medicinal plant methanol extracts and their solvent partitioned fractions for potential inhibitors of Mycobacterium tuberculosis growth. Using microdilution screening, the ethyl acetate solvent partitioned fraction from the heartwood of Caesalpinia sappan exhibited strong antitubercular activity. We isolated the active compound and identified it as 3-deoxysappanchalcone. The extracted 3-deoxysappanchalcone possessed activity against both drug-susceptible and drug-resistant strains of M. tuberculosis at MIC s of 3.125-12.5 μg/mL in culture broth and MIC s of 6.25-12.5 μg/mL inside macrophages and pneumocytes. 3-Deoxysappanchalcone was also found to act in partial synergy with streptomycin/ethambutol against M. tuberculosis H37Rv. 3-Deoxysappanchalcone had no cytotoxicity against the A549 cell line up to a concentration of 100 μg/mL (selectivity index > 8-32). Further studies are warranted to establish the in vivo effect and therapeutic potential of 3-deoxysappanchalcone. Copyright © 2017 John Wiley & Sons, Ltd.

Anti-Mycobacterium Tuberculosis Strain H37rv and Iron Chelation Activity of Sappan Wood Extract (Caesalpinia Sappan L.) in Vitro

“…Seo et al reported that the 3-deoxysappanchalcone isolated from the heartwood of C. sappan Linn. possessed the antitubercular activity of both drug susceptible and drug resistant of MTB strain H 37 Rv [12]. Based on these facts, this study was conducted to determine anti-MTB strain H 37 Rv and iron chelation activities of SWE.…”

Anti-tubercular substances produced by plants

“…The main active substance isolated from the heartwood of that plant is 3-deoxysappanchalcone, which displays activity not only against M. tuberculosis, but also against multidrugresistance and extensively drug-resistance tuberculosis strains. The MIC is within the range 3.125-12.5 µg/ml, which is much higher than rifampicin in most cases [13]. Diterpenoids, as the researchers have discovered, possess some anti-mycobacterial properties.…”

Development of Eco-friendly Dyeing Process Based on Caesalpinia sappan L. Bark, Cocos nucifera Fiber and Leucaena leucocephala Leaves

“…The extract has been used extensively as a natural dye, especially in the textile industry due to its low toxicity and low cost [37]- [39]. Sappanwood extracts in addition to functioning as a natural red dye, also show great benefits as antibacterial agents [38], [40]- [42], antioxidants [38], [43]- [45], and pharmacological activity [46]. Also, braziline is easily oxidized by light to form a very red brazilein [35], [38].…”