scholarly journals In Vitro Interactions of Costus speciosus (J. Koenig) Sm., Cymbopogon citratus (Dc. Ex Nees) Stapf. and Tabernaemontana coronaria (L.) Willd. with First-Line Anti-Tuberculosis Drugs Against Mycobacterium tuberculosis H37rv

2021 ◽  
Vol 19 (2) ◽  
pp. 171-178
Author(s):  
Suriyati Mohamad ◽  
◽  
Nur Najihah Ismail ◽  
Hasnah Osman ◽  
Habibah A Wahab ◽  
...  

Global tuberculosis (TB) burden underscores the importance of developing new effective anti-TB drugs. This study was concerned with prospecting for potential anti-TB agents from Malaysian medicinal plants. In our previous study, we have reported that n-hexane fractions of Costus speciosus (C. speciosus) (J. Koening) Sm., Cymbopogon citratus (C. citratus ) (DC.) Stapf. and Tabernaemontana coronaria (T. coronaria) (Jacq.) posses promising anti-TB activity against Mycobacterium tuberculosis (M. tuberculosis) H37Rv with minimum inhibitory concentrations (MICs) of 200–100 µg/mL. This study aimed to investigate the interactions of these active fractions with first-line anti-TB drugs (isoniazid, rifampicin, ethambutol and streptomycin) against M. tuberculosis H37Rv using the microdilution checkerboard method. C. citratus (stem-rhizome) n-hexane fraction exhibited synergism with all drugs except ethambutol which showed additive interaction. Synergistic was also observed when C. speciosus (stem-flower) n-hexane and T. coronaria (leaf) n-hexane fractions in combination with rifampicin. C. speciosus (stem-flower) n-hexane and T. coronaria (leaf) n-hexane exhibited additive interaction with isoniazid, ethambutol and streptomycin. Hence, these active plants are worthy of further investigations for the discovery of anti-TB drug leads.

2010 ◽  
Vol 14 (1) ◽  
pp. 47-52 ◽  
Author(s):  
L. Ouattara ◽  
J. Koudou ◽  
D.S. Karou ◽  
L. Giaco ◽  
G. Capelli ◽  
...  

2010 ◽  
Vol 434 (1) ◽  
pp. 371-374 ◽  
Author(s):  
S. N. Andreevskaya ◽  
T. G. Smirnova ◽  
Yu. A. Zhogina ◽  
D. I. Smirnova ◽  
Yu. L. Mikulovich ◽  
...  

2019 ◽  
Vol 2 (1) ◽  
pp. 37-48
Author(s):  
Ruswanto Ruswanto

Isoniazid merupakan obat antituberkulosis yang memiliki aktivitas antimikobakterial yang baik yang bekerja secara aktif dengan menghambat biosintesis asam mikolat. Telah dilakukan pengujian In Vitro pada senyawa N’-(4-Methylbenzoyl) Isonicotinohydrazide N’-(4-Chlorobenzoyl) Isonicotinohydrazide dan N’-(3,5-Dinitrobenzoyl) Isonicotinohydrazide terhadap Mycobacterium tuberculosis H37Rv, bakteri gram positif serta bakteri gram negatif dengan menggunakan metode sumuran dan pada pengujian Mycobacterium tuberculosis H37Rv menggunakan metode REMA (Resazurin Microtiter Assay). Didapat nilai MIC terbaik pada senyawa N’-(3,5-Dinitrobenzoyl) Isonicotinohydrazide memiliki potensi tinggi sebagai antibakteri dengan nilai MIC 0,169 ppm terhadap bakteri e.colli. Ketiga senyawa yang diujikan pada  Mycobacterium tuberculosis H37Rv memiliki kemampuan sebagai anti tuberkulosis tetapi isoniazid lebih baik dari senyawa uji. Senyawa N’-(3,5-Dinitrobenzoyl) Isonicotinohydrazide di dockingkan pada reseptor 1KZN memiliki binding affinity yang lebih kecil dibandingkan senyawa pembanding yaitu isoniazid sebesar -6,89 kkal/mol.


2020 ◽  
Vol 19 (1) ◽  
pp. 163-168
Author(s):  
Lin Ling ◽  
Chen Ling ◽  
Hua Wu

Purpose: To investigate the anti-tuberculosis potential of twelve commercially available pyridone analogues against Mycobacterium tuberculosis H37Rv strain.Methods: Twelve commercially available pyridone-based compounds were screened against M. tuberculosis H37Rv using different susceptibility tests. The most active or lead compound was further evaluated in detail for its anti-tuberculosis (anti-TB) potential. Kill kinetics was used to determine the dynamics of its anti-TB activity in vitro.Results: Compounds d, j and k were potent against M. tuberculosis H37Rv, with minimum inhibitory concentrations (MICs) of 10, 5 and 10 μg/mL, respectively. The standard anti-TB drugs used in this study (positive control drugs) demonstrated MIC of 2.5 μg/mL. The anti-TB effect of compound j was comparable with those of the standard drugs (RIF, LVX, AMK, EMB and INH). The minimum bactericidal concentration (MBC) of compound j was 10 μg/mL. It produced an MIC of 5 μg/mL in agar proportion method (APM). However, its MIC in Middlebrook 7H9 broth supplemented with 10 % fetal bovine serum (FBS) and 4 % bovine serum albumin (BSA) increased 4- and 8-fold, respectively. The bactericidal effect of compound j was time- and concentration-dependent at dilutions above 2x MIC. Combination of compound j with RIF, LVX or AMK exhibited fractional inhibitory concentration index (ΣFIC) of 1, indicative of additive drug-drug interactions. However, combination with INH or EMB produced a ΣFIC of 2. None of the tested drug combinations was antagonistic.Conclusion: Compound j exhibits potent time- and concentration-dependent antimicrobial effect against M. tuberculosis H37Rv. Thus, it may be suitable as an adjunct to current treatment of drug sensitive and drug-resistant TB. Keywords: Tuberculosis, Mycobacterium tuberculosis, Pyridone analogs, Antimicrobial activity, Antibiotics


2004 ◽  
Vol 72 (1) ◽  
pp. 35-41 ◽  
Author(s):  
D. Sriram ◽  
K. Jyothi Mallika ◽  
P. Yogeeswari

3-Substituted-5-(4-pyridylcarboxamide)tetrahydro-2H-[1,3,5]thiadizine-2-thione derivatives (1-9) were synthesized as derivatives of isoniazid (INH) to overcome the resistance developed with its therapeutic use. The structures were confirmed by their spectral and elemental analyses data. These derivatives revealed higher lipophilicity compared with INH. The antimycobacterial activity of the synthesized compounds and INH was evaluated in vitro against Mycobacterium tuberculosis H37Rv at 6.25 µg/ml in BACTEC 12B medium using the BACTEC 460 radiometric system. The derivatives exhibited antitubercular activity.


INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 41-47
Author(s):  
R. R Somani ◽  
◽  
G. K Shinde ◽  
P.Y. Shirodkar ◽  
G. J. Sanap

A series of 5-(N-substituted carboxamidoethylthio)-3-(3’pyridyl)-4-amino-1,2,4-triazole derivatives (6a-j) were synthesized and evaluated for anti-tubercular activity. The derivatives were purified and structures were elucidated by spectral and elemental analyses. They were screened in-vitro at 10µg/mL concentration against Mycobacterium tuberculosis H37RV (ATCC 27294). Compounds 6e and 6h were found active as they exhibited IC50 and IC90 values at < 100µg/mL.


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