Relations between Structure and Antituberculotic Activity of 4-Alkoxybenzoic Acids

1993 ◽  
Vol 58 (1) ◽  
pp. 191-196 ◽  
Author(s):  
Karel Waisser ◽  
Jiří Kuneš ◽  
Jiří Klimeš ◽  
Miroslav Polášek ◽  
Želmíra Odlerová
Keyword(s):  
Active Compound ◽  
Antimycobacterial Activity ◽  
Methoxybenzoic Acid

Antimycobacterial activity of a series of alkoxybenzoic acids including 4-methoxybenzoic acid (II), 4-ethoxybenzoic acid (III), 4-propoxybenzoic acid (IV), 4-butoxybenzoic acid (V), 4-pentoxybenzoic acid (VI), 4-allyloxybenzoic acid (IX), 4-isopropoxybenzoic acid (VII), 4-isobutoxybenzoic acid (VIII) and 4-benzyloxybenzoic acid (X) has been determined and found to increase with the lipophilicity of the compounds expressed by the corresponding HPLC capacity factors. Also determined were the pKa values of the compounds mentioned. The most active compound, 4-pentoxybenzoic acid (VI), is comparable with commercial antituberculotics when tested in vitro.

scholarly journals ChCl: Gly (DESs) Promote Environmentally Benign Synthesis of Xanthene Derivatives and Their Antitubercular Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3667
Author(s):  
Mashooq A. Bhat ◽  
Ahmed M. Naglah ◽  
Siddique Akber Ansari ◽  
Hanaa M. Al-Tuwajiria ◽  
Abdullah Al-Dhfyan
Keyword(s):  
Reaction Times ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
Environmentally Benign ◽  
Reaction Yield ◽  
Benign Synthesis ◽  
Xanthene Derivatives ◽  
Wide Range ◽  
Major Application

A ChCl: Gly (DESs) promoted environmentally benign method was developed for the first time using the reaction of aryl aldehydes and dimedone to give excellent yields of xanthene analogues. The major application of this present protocol is the use of green solvent, a wide range of substrate, short reaction times, ease of recovery, the recyclability of the catalyst, high reaction yield, and ChCl: Gly as an alternative catalyst and solvent. In addition to this, all the synthesized compounds were evaluated for their in vitro antimycobacterial activity against M. tuberculosis H37Ra (MTB) and M. bovis BCG strains. The compounds 3d, 3e, 3f, and 3j showed significant antitubercular activity against MTB and M. bovis strains with minimum inhibitory concentration (MIC) values of 2.5−15.10 µg/mL and 0.26–14.92 µg/mL, respectively. The compounds 3e, 3f, and 3j were found to be nontoxic against MCF-7, A549, HCT 116, and THP-1 cell lines. All the prepared compounds were confirmed by 1H NMR and 13C NMR analysis.

scholarly journals Biofilm formation in the lung contributes to virulence and drug tolerance of Mycobacterium tuberculosis

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Poushali Chakraborty ◽  
Sapna Bajeli ◽  
Deepak Kaushal ◽  
Bishan Dass Radotra ◽  
Ashwani Kumar
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Immune System ◽  
Biofilm Formation ◽  
Antimycobacterial Activity ◽  
Drug Tolerance ◽  
Host Immune System ◽  
Tissue Sections ◽  
Slow Growing

AbstractTuberculosis is a chronic disease that displays several features commonly associated with biofilm-associated infections: immune system evasion, antibiotic treatment failures, and recurrence of infection. However, although Mycobacterium tuberculosis (Mtb) can form cellulose-containing biofilms in vitro, it remains unclear whether biofilms are formed during infection in vivo. Here, we demonstrate the formation of Mtb biofilms in animal models of infection and in patients, and that biofilm formation can contribute to drug tolerance. First, we show that cellulose is also a structural component of the extracellular matrix of in vitro biofilms of fast and slow-growing nontuberculous mycobacteria. Then, we use cellulose as a biomarker to detect Mtb biofilms in the lungs of experimentally infected mice and non-human primates, as well as in lung tissue sections obtained from patients with tuberculosis. Mtb strains defective in biofilm formation are attenuated for survival in mice, suggesting that biofilms protect bacilli from the host immune system. Furthermore, the administration of nebulized cellulase enhances the antimycobacterial activity of isoniazid and rifampicin in infected mice, supporting a role for biofilms in phenotypic drug tolerance. Our findings thus indicate that Mtb biofilms are relevant to human tuberculosis.

Synthesis and in vitro antimycobacterial activity of 3-substituted 5-hydroxy-5-trifluoro[chloro]methyl-4,5-dihydro-1H-1-(isonicotinoyl) pyrazoles

2008 ◽  
Vol 32 (2) ◽  
pp. 139-144 ◽  
Author(s):  
Pedro E. Almeida da Silva ◽  
Daniela F. Ramos ◽  
Helio G. Bonacorso ◽  
Agustina I. de la Iglesia ◽  
Marli R. Oliveira ◽  
...  
Keyword(s):  
Antimycobacterial Activity

scholarly journals In Vitro Activities of DC-159a, a Novel Fluoroquinolone, against Mycobacterium Species

2010 ◽  
Vol 54 (6) ◽  
pp. 2684-2686 ◽  
Author(s):  
Areeya Disratthakit ◽  
Norio Doi
Keyword(s):  
Active Compound ◽  
Nontuberculous Mycobacteria ◽  
Multidrug Resistant ◽  
Mycobacterium Species

ABSTRACT The in vitro activities of DC-159a against seven species of Mycobacterium were compared with moxifloxacin, gatifloxacin, levofloxacin, and rifampin. DC-159a was the most active compound against quinolone-resistant multidrug-resistant M. tuberculosis (MIC90, 0.5 μg/ml) as well as drug-susceptible isolates (MIC90, 0.06 μg/ml). The anti-tubercle bacilli activity of DC-159a was 4- to 32-fold more potent than those of currently available quinolones. DC-159a also demonstrated the highest activities against clinically important nontuberculous mycobacteria.

In vitro evaluation of the anti-mycobacterial properties of the extracts of Momordica Charantia

2021 ◽  
Vol 16 (7) ◽  
pp. 15-22
Author(s):  
Paul Giftson ◽  
Jerrine Joseph ◽  
Revathy Kalyanasundaram ◽  
V. Ramesh Kumar ◽  
Wilson Aruni
Keyword(s):  
Medicinal Plants ◽  
Fungal Pathogens ◽  
Communicable Disease ◽  
Antimycobacterial Activity ◽  
Bitter Gourd ◽  
World Population ◽  
Methanol Extracts ◽  
Crude Extracts ◽  
The World

Tuberculosis (TB) is a communicable disease and remains one of the top 10 causes of death worldwide. One fourth of the world population is infected with TB at a risk of developing disease. The increase in the incidence of drug resistant TB around the world urges the need to develop a new candidate to fight against the disease. Plants were considered as the rich source of bioactive components to be used as potential drugs. Medicinal plants are used in pure as well as crude materials for their medicinal properties. Our research aims in identifying the phyto-molecules which have anti- tuberculosis property. Four medicinal plants namely, Acalyphaciliata (Kuppaimeni), Solanumtrilobatum (Thuthuvalai), Momordicacharantia (Bitter Gourd) and Sennaauriculata (Avaram) were chosen to evaluate their antimicrobial activity focusing on anti-tubercular activity. The methanol extracts of the medicinal plants showed significant inhibitory activity against bacterial and fungal pathogens. Sennaauriculata methanol extracts showed activity against S. aureus, E. coli, P. aeruginosa and C. albicans. In the screening of antimycobacterial activity done by LRP assay, among the plant extracts tested, the hexane crude extracts of Momordicacharantia (Bitter Gourd) showed 82.2% and 81.03% of inhibition against M. tuberculosis H37Rv at 500µg/ml and 250µg/ml concentration respectively. Similarly, the methanol crude extracts of Momordicacharantia showed 87.14% and 63.55% of inhibition at 500µg/ml and 250µg/ml concentration respectively.

scholarly journals IN VITRO STUDY OF URSOLIC ACID COMBINATION FIRST-LINE ANTITUBERCULOSIS DRUGS AGAINST DRUG-SENSITIVE AND DRUG-RESISTANT STRAINS OF Mycobacterium tuberculosis

2017 ◽  
Vol 10 (4) ◽  
pp. 216 ◽  
Author(s):  
Dian Ayu Eka Pitaloka ◽  
Elin Yulinah Sukandar
Keyword(s):  
Ursolic Acid ◽  
Drug Combination ◽  
Resistant Strain ◽  
Inhibitory Concentration ◽  
In Vitro Study ◽  
Antimycobacterial Activity ◽  
Multidrug Resistant ◽  
Minimum Concentration ◽  
Different Strains

Objective: The resurgence of tuberculosis (TB) caused by Mycobacterium TB (MTB) is associated with the rapid spread of multidrug-resistant,therefore, the development of new antimycobacterial agents is necessary. The aim of this study was to evaluate the antimycobacterial activity ofursolic acid (UA) when it using alone and combination with TB drugs.Methods: MTB H37Rv strain, streptomycin-rifampicin resistant strain, and isoniazid-ethambutol resistant strain were evaluated by susceptibility testusing a serial number of UA (25-150 µg/mL). Minimum inhibitory concentration (MIC) was read as minimum concentration of drugs that completelyinhibit visible growth of organism. Activities of drug combination of UA with TB drug were determined in Lowenstein-Jensen media by calculatingthe fractional inhibitory concentration index.Results: The results showed that MIC of UA was 50 µg/mL against three different strains of MTB. The combination of UA and TB drugs displayedsynergistic interaction, and no antagonism result from the combination was observed for strains of MTB.Conclusion: These results indicate that UA may serve as a promising lead compound for future antimycobacterial drug development.Keywords: Ursolic acid, Tuberculosis, Drug combination, Susceptibility test

Selectivity of auxin for induction and growth of callus from excised embryo of spring and winter wheat

1984 ◽  
Vol 62 (7) ◽  
pp. 1393-1397 ◽  
Author(s):  
M. D. Zhou ◽  
T. T. Lee
Keyword(s):  
Winter Wheat ◽  
Chinese Spring ◽  
Shoot Growth ◽  
Callus Formation ◽  
Triticum Aestivum L ◽  
Dichlorophenoxyacetic Acid ◽  
Naphthaleneacetic Acid ◽  
2,4 Dichlorophenoxyacetic Acid ◽  
Methoxybenzoic Acid

The callus-promoting activity of most commonly known as well as some rarely tested auxins was compared with that of 2,4-dichlorophenoxyacetic acid (2,4-D) for in vitro culture of the excised embryo of spring and winter wheat (Triticum aestivum L.), cv. Chinese Spring and cv. Fredrick. Different auxins in a concentration range from 1 to 50 μM showed widely different activities. Also the two wheat cultivars responded differently to the auxins. When rapid callus formation with limited root growth was used as the basis for comparison, 2-(2-methyl-4-chlorophenoxy)propionic acid (2-MCPP), α-naphthaleneacetic acid, 3,6-dichloro-2-methoxybenzoic acid (dicamba), 4-amino-3,5,6,trichloropicolinic acid (picloram), γ-(2,4-dichlorophenoxy)butyric acid, 2,4,5-trichlorophenoxyacetic acid, and 2,4,5-trichlorophenoxypropionic acid, in the order of effectiveness, were superior to 2,4,-D for callus induction from the embryo of 'Chinese Spring,' although the concentration required was higher than that of 2,4-D. For the winter wheat 'Fredrick,' however, only picloram, dicamba, and 2-MCPP performed as well as 2,4-D. All auxins tested promoted shoot growth; 2-methyl-4-chlorophenoxypropionic acid was most effective for 'Chinese Spring,' whereas picloram was most effective for 'Fredrick.'

scholarly journals In Vitro Antimycobacterial Activity of Pakistani Beri Honey Using BACTEC MGIT 960

2014 ◽  
Vol 2014 ◽  
pp. 1-4
Author(s):  
Abdul Hannan ◽  
Saira Munir ◽  
Muhammad Usman Arshad ◽  
Nabila Bashir
Keyword(s):  
Growth Control ◽  
Antimycobacterial Activity ◽  
Multidrug Resistant ◽  
Bacterial Disease ◽  
First Line ◽  
Development Of Resistance ◽  
Extensively Drug Resistant ◽  
Mdr Tb ◽  
Growth Controls

Background. Tuberculosis (TB) is a chronic bacterial disease. Mycobacterium tuberculosis, being the leading member of the MTB complex, is the main cause of tuberculosis worldwide. Tuberculosis is managed with combination of drugs: streptomycin, isoniazid, rifampicin, ethambutol, and pyrazinamide. Over the recent past years resistance against first line antituberculous drugs has emerged rapidly throughout the world resulting in MDR strains. The new threat in the management of MDR-TB is the development of resistance against second line drugs: aminoglycosides, polypeptides, fluoroquinolones, and thioamides. Multidrug resistant (MDR) and extensively drug resistant TB (XDR) strains have become a major concern to control TB particularly in the developing countries. The need of the hour is to look for new modalities having antimycobacterial activity. Honey has been well known for its antibacterial activity. We intended to explore its antimycobacterial activity against MDR-TB. Objective. The objective of this study was to determine whether Pakistani Beri honey has any antimycobacterial activity. Method. The study was conducted in the Department of Microbiology, University of Health Sciences, Lahore. Clinical isolates (n=21) of MDR-MTB were evaluated for their susceptibility to Beri honey. The isolates were provided, courtesy of Pakistan Medical Research Council. These isolates were identified by MTBc ID test (Becton & Dickinson) and further tested for their antimycobacterial activity using Beri honey. The honey was tested at the following concentrations (v/v): 1%, 2%, 3%, 4%, and 5% in MGIT 960. Growth controls were also inoculated with each isolate (growth control has no concentration of honey, only containing growth of isolate). Results. MDR-TB isolates (n=21) were tested; 3 (14%) isolates were susceptible at 1% v/v honey, while at 2% v/v of honey 18 (86%) isolates were found to be susceptible. All the 21 isolates (n=21) were susceptible at 3% v/v of honey. Conclusion. The present study clearly demonstrates that Pakistani Beri honey possesses significant antimycobacterial activity in vitro. The antimycobacterial activity of Pakistani Beri honey may, therefore, be exploited in an appropriate mouse model.

In vitro synergistic interactions of oleanolic acid in combination with isoniazid, rifampicin or ethambutol against Mycobacterium tuberculosis

2010 ◽  
Vol 59 (5) ◽  
pp. 567-572 ◽  
Author(s):  
Fa Ge ◽  
Fanli Zeng ◽  
Siguo Liu ◽  
Na Guo ◽  
Haiqing Ye ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Oleanolic Acid ◽  
Antimycobacterial Activity ◽  
Vero Cells ◽  
Drug Resistant ◽  
Synergistic Interactions ◽  
Combination Treatments ◽  
Low Cytotoxicity ◽  
Drug Resistant Strains

Reports have shown that oleanolic acid (OA), a triterpenoid, exists widely in food, medicinal herbs and other plants, and that it has antimycobacterial activity against the Mycobacterium tuberculosis strain H37Rv (ATCC 27294). In this study it was found that OA had antimycobacterial properties against eight clinical isolates of M. tuberculosis and that the MICs of OA against drug-sensitive and drug-resistant isolates were 50–100 and 100–200 μg ml−1, respectively. The combination of OA with isoniazid (INH), rifampicin (RMP) or ethambutol (EMB) showed favourable synergistic antimycobacterial effects against six drug-resistant strains, with fractional inhibitory concentration indices of 0.121–0.347, 0.113–0.168 and 0.093–0.266, respectively. The combination treatments of OA/INH, OA/RMP and OA/EMB displayed either a synergistic interaction or did not show any interaction against two drug-sensitive strains. No antagonism resulting from the OA/INH, OA/RMP or OA/EMB combination was observed for any of the strains tested. OA exhibited a relatively low cytotoxicity in Vero cells. These results indicate that OA may serve as a promising lead compound for future antimycobacterial drug development.

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