scholarly journals Antimycobacterial Activity of the Extract and Isolated Compounds From the Stem Bark of Zanthoxylum leprieurii Guill. and Perr.

2021 ◽  
Vol 16 (8) ◽  
pp. 1934578X2110358
Author(s):  
Benson Oloya ◽  
Jane Namukobe ◽  
Matthias Heydenreich ◽  
Willy Ssengooba ◽  
Bernd Schmidt ◽  
...  
Keyword(s):  
Antimycobacterial Activity ◽  
Stem Bark ◽  
Multidrug Resistant ◽  
Moderate Activity ◽  
Spectroscopic Techniques ◽  
Minimum Inhibitory Concentrations ◽  
Mdr Tb ◽  
Weak Activity ◽  
First Time ◽  
Chloroform Methanol

Zanthoxylum leprieurii Guill. and Perr. (Rutaceae) stem bark is used locally in Uganda for treating tuberculosis (TB) and cough-related infections. Lupeol (1), sesamin (2), trans-fagaramide (3), arnottianamide (4), ( S)-marmesinin (5), and hesperidin (6) were isolated from the chloroform/methanol (1:1) extract of Z. leprieurii stem bark. Their structures were elucidated using spectroscopic techniques and by comparison with literature data. Furthermore, the extract and isolated compounds were subjected to antimycobacterial activity. The extract exhibited moderate activity against the susceptible (H37Rv) TB strain, but weak activity against the multidrug resistant (MDR)-TB strain with minimum inhibitory concentrations (MICs) of 586.0 and 1172.0 μg/mL, respectively. Compound 3 (trans-fagaramide) showed significant antimycobacterial activity against the susceptible (H37Rv) TB strain (MIC 6 μg/mL), but moderate activity against the MDR-TB strain (MIC 12.2 μg/mL). Compounds 2, 5, 6, and 1 showed moderate activities against the susceptible (H37Rv) strain (MIC 12.2-98.0 μg/mL) and moderate to weak activities against the MDR-TB strain (MIC 24.4-195.0 μg/mL). This study reports for the first time the isolation of compounds 1 to 6 from the stem bark of Z leprieurii. trans-Fagaramide (3) may present a vital template in pursuit of novel and highly effective TB drugs.

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.

scholarly journals Bedaquiline for multidrug-resistant TB in paediatric patients

2021 ◽  
Vol 25 (9) ◽  
pp. 716-724
Author(s):  
R. Moodliar ◽  
V. Aksenova ◽  
M. V. G. Frias ◽  
J. van de Logt ◽  
S. Rossenu ◽  
...  
Keyword(s):  
Geometric Mean ◽  
Area Under The Curve ◽  
Antimycobacterial Activity ◽  
Multidrug Resistant ◽  
Dose Selection ◽  
Primary Analysis ◽  
Open Label ◽  
Target Values ◽  
Mdr Tb ◽  
Age Appropriate

BACKGROUND: TMC207-C211 (NCT02354014) is a Phase 2, open-label, multicentre, single-arm study to evaluate pharmacokinetics, safety/tolerability, antimycobacterial activity and dose selection of bedaquiline (BDQ) in children (birth to <18 years) with multidrug-resistant-TB (MDR-TB).METHODS: Patients received 24 weeks’ BDQ with an anti-MDR-TB background regimen (BR), followed by 96 weeks of safety follow-up. Results of the primary analysis are presented based on data up to 24 weeks for Cohort 1 (≥12–<18 years; approved adult tablet at the adult dosage) and Cohort 2 (≥5–<12 years; age-appropriate 20 mg tablet at half the adult dosage).RESULTS: Both cohorts had 15 patients, of whom respectively 53% and 40% of Cohort 1 and Cohort 2 children had confirmed/probable pulmonary MDR-TB. Most patients completed 24 weeks´ BDQ/BR treatment (Cohort 1: 93%; Cohort 2: 67%). Geometric mean BDQ area under the curve 168h values of 119,000 ng.h/mL (Cohort 1) and 118,000 ng.h/mL (Cohort 2) at Week 12 were within 60–140% (86,200–201,000 ng.h/mL) of adult target values. Few adverse event (AE) related discontinuations or serious AEs, and no QTcF >460 ms during BDQ/BR treatment or deaths occurred. Of MGIT-evaluable patients, 6/8 (75%) Cohort 1 and 3/3 (100%) Cohort 2 culture converted.CONCLUSION: In children and adolescents aged ≥5–<18 years with MDR-TB, including pre-extensively drug-resistant-TB (pre-XDR-TB) or XDR-TB, 24 weeks of BDQ provided a comparable pharmacokinetic and safety profile to adults.

scholarly journals Composition of Three Essential Oils, and their Mammalian Cell Toxicity and Antimycobacterial Activity against Drug Resistant-Tuberculosis and Nontuberculous Mycobacteria Strains

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Juan Bueno ◽  
Patricia Escobar ◽  
Jairo René Martínez ◽  
Sandra Milena Leal ◽  
Elena E. Stashenko
Keyword(s):  
Essential Oils ◽  
Mammalian Cells ◽  
Antimycobacterial Activity ◽  
Multidrug Resistant ◽  
Beijing Genotype ◽  
Cell Toxicity ◽  
Epidemic Disease ◽  
Opportunistic Disease ◽  
Turnera Diffusa ◽  
Mdr Tb

Tuberculosis (TB) is the most ancient epidemic disease in the world and a serious opportunistic disease in HIV/AIDS patients. The increase in multidrug resistant Mycobacterium tuberculosis (MDR-TB, XDR-TB) demands the search for novel antimycobacterial drugs. Essential oils (EOs) have been widely used in medicine and some EOs and their major components have been shown to be active against M. tuberculosis. The aim of this work was to evaluate the antimycobacterial and cell toxicity activities of three EOs derived from Salvia aratocensis, Turnera diffusa and Lippia americana, aromatics plants collected in Colombia. The EOs were isolated by hydrodistillation and analyzed by GC/MS techniques. The EOs were tested against 15 Mycobacterium spp using a colorimetric macrodilution method and against mammalian Vero and THP-1 cells by MTT. The activity was expressed as minimal concentration in μg/mL that inhibits growth, and the concentration that is cytotoxic for 50 or 90% of the cells (CC50 and CC90). The major components were epi-α-cadinol (20.1%) and 1,10-di- epi-cubenol (14.2%) for Salvia aratocensis; drima-7,9(11)-diene (22.9%) and viridiflorene (6.6%) for Turnera diffusa; and germacrene D (15.4%) and trans-β- caryophyllene (11.3%) for Lippia americana. The most active EO was obtained from S. aratocensis, with MIC values below 125 μg mL−1 for M. tuberculosis Beijing genotype strains, and 200 to 500 μg mL−1 for nontuberculous mycobacterial strains. The EOs were either partially or non toxic to Vero and THP-1 mammalian cells with CC50 values from 30 to >100 μg mL−1, and a CC90 >100 μg mL−1. The EOs obtained from the three aromatic Colombian plants are an important source of potential compounds against TB. Future studies using the major EO components are recommended.

scholarly journals Cytotoxic Prenyl and Geranyl Coumarins from the Stem Bark of Casimiroa edulis

2020 ◽  
Vol 17 (9) ◽  
pp. 680-687
Author(s):  
Khun Nay Win Tun ◽  
Nanik Siti Aminah ◽  
Alfinda Novi Kristanti ◽  
Rico Ramadhan ◽  
Yoshiaki Takaya
Keyword(s):  
Methanolic Extract ◽  
T47d Cell ◽  
Stem Bark ◽  
Moderate Activity ◽  
Compound K ◽  
Pure Compound ◽  
Phytochemical Investigation ◽  
Ic50 Value ◽  
Casimiroa Edulis ◽  
First Time

Phytochemical investigation of the methanolic extract of the stem bark of Casimiroa edulis afforded four coumarins. Various spectroscopic experiments were used to characterize the isolated coumarins. The structures were identified as auraptene (K-1), suberosin (K-2), 5-geranyloxypsoralen (bergamottin) (K-3), and 8-geranyloxypsoralen (K-4), based on the chemical and spectral analysis. Among these compounds, suberosin (K-2) and 5-geranyloxypsoralen (bergamottin) (K-3) were isolated for the first time from this genus, and auraptene (K-1) was isolated from this plant for the first time. Cytotoxicity of pure compound K-4 and sub-fraction MD-3 was evaluated against HeLa and T47D cell lines and moderate activity was found with an IC50 value in the range 17.4 to 72.33 μg/mL.

Synthesis, Spectroscopic, In-vitro and Computational Analysis of Hydrazones as Potential Antituberculosis Agents: (Part-I)

2020 ◽  
Vol 23 (5) ◽  
pp. 392-401 ◽  
Author(s):  
Bapu R. Thorat ◽  
Deepa Rani ◽  
Ramesh S. Yamgar ◽  
Suraj N. Mali
Keyword(s):  
Electronic Excitation ◽  
Condensation Reaction ◽  
Multidrug Resistant ◽  
Healthcare Sector ◽  
Spectroscopic Techniques ◽  
Resistant Tuberculosis ◽  
Extensively Drug Resistant ◽  
In Silico Admet ◽  
Mdr Tb

Background: Since the last few decades, the healthcare sector is facing the problem of the development of multidrug-resistant (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) infections all over the world. Regardless of the current healthcare progress for the treatment of mycobacterial infections, we are still unable to control addition of every year 9 million new cases of tuberculosis (TB). Objective: We had an objective to synthesize some novel hydrazones, which were further subjected to characterization, Photoluminescence study, in vitro anti-mycobacterium testing and in silico ADMET predictions. Methods: Some new hydrazone derivatives have been successfully prepared by the condensation reaction in the present study. All the compounds were characterized by using FTIR, NMR, UV, Fluorescence spectroscopic techniques. Results: All our newly synthesized compounds showed strong electronic excitation at 292.6 – 319.0 nm and displayed more intense emissions in the 348 – 365 nm regions except compound 3i. The newly synthesized hydrazones 3a, 3b, 3f and 3g were found to be the most active compounds and showed MIC (Minimum inhibitory concentrations) values of 12.5 μg/mL. Conclusion: In the realm of development of more potent, effective, safer and less toxic antituberculosis agents; our current study would definitely help the medicinal chemists to develop potent analogues containing hydrazine motifs in them.

scholarly journals Plasma concentrations of second-line antituberculosis drugs in relation to minimum inhibitory concentrations in multidrug-resistant tuberculosis patients in China: a study protocol of a prospective observational cohort study

BMJ Open ◽  
2018 ◽  
Vol 8 (9) ◽  
pp. e023899 ◽  
Author(s):  
Lina Davies Forsman ◽  
Katarina Niward ◽  
Yi Hu ◽  
Rongrong Zheng ◽  
Xubin Zheng ◽  
...  
Keyword(s):  
Drug Exposure ◽  
Plasma Concentrations ◽  
Multidrug Resistant ◽  
Ethical Review ◽  
Therapeutic Drug ◽  
Minimum Inhibitory Concentrations ◽  
Drug Concentrations ◽  
Study Results ◽  
Custom Made ◽  
Mdr Tb

IntroductionIndividualised treatment through therapeutic drug monitoring (TDM) may improve tuberculosis (TB) treatment outcomes but is not routinely implemented. Prospective clinical studies of drug exposure and minimum inhibitory concentrations (MICs) in multidrug-resistant TB (MDR-TB) are scarce. This translational study aims to characterise the area under the concentration–time curve of individual MDR-TB drugs, divided by the MIC forMycobacterium tuberculosisisolates, to explore associations with markers of treatment progress and to develop useful strategies for clinical implementation of TDM in MDR-TB.Methods and analysisAdult patients with pulmonary MDR-TB treated in Xiamen, China, are included. Plasma samples for measure of drug exposure are obtained at 0, 1, 2, 4, 6, 8 and 10 hours after drug intake at week 2 and at 0, 4 and 6 hours during weeks 4 and 8. Sputum samples for evaluating time to culture positivity and MIC determination are collected at days 0, 2 and 7 and at weeks 2, 4, 8 and 12 after treatment initiation. Disease severity are assessed with a clinical scoring tool (TBscore II) and quality of life evaluated using EQ-5D-5L. Drug concentrations of pyrazinamide, ethambutol, levofloxacin, moxifloxacin, cycloserine, prothionamide and para-aminosalicylate are measured by liquid chromatography tandem-mass spectrometry and the levels of amikacin measured by immunoassay. Dried blood spot on filter paper, to facilitate blood sampling for analysis of drug concentrations, is also evaluated. The MICs of the drugs listed above are determined using custom-made broth microdilution plates and MYCOTB plates with Middlebrook 7H9 media. MIC determination of pyrazinamide is performed in BACTEC MGIT 960.Ethics and disseminationThis study has been approved by the ethical review boards of Karolinska Institutet, Sweden and Fudan University, China. Informed written consent is given by participants. The study results will be submitted to a peer-reviewed journal.Trial registration numberNCT02816931; Pre-results.

scholarly journals Chemical and Antioxidant Studies of Citrus macroptera

1970 ◽  
Vol 43 (4) ◽  
pp. 449-454 ◽  
Author(s):  
Sadia A Chowdhury ◽  
M Hossain Sohrab ◽  
Bidyut K Datta ◽  
Choudhury M Hasan
Keyword(s):  
Antioxidant Activity ◽  
Methanol Extract ◽  
Radical Scavenging ◽  
Stem Bark ◽  
Free Radical Scavenging ◽  
Moderate Activity ◽  
Free Radical Scavenging Assay ◽  
First Time ◽  
Radical Scavenging Assay

Lupeol (1) and Stigmasterol (2) were isolated from the crude extracts of the stem bark of Citrus macroptera (Family: Rutaceae) for the first time. The n-hexane, dichloromethane and methanol extracts were screened in vitro for antioxidant activity using the 1, 1-diphenyl-2-picrylhydrazyl-hydrate (DPPH) free radical scavenging assay. The hot methanol extract showed potential antioxidant activity (IC50: 178.96 μg/ml) whereas the cold methanol and dichloromethane extracts showed moderate activity (IC50: 242.78 μg/ml and 255.78 μg/ml respectively). Mild antioxidant activity was observed with the n-hexane extract of the stem bark of Citrus macroptera (IC50: 422.94 μg/ml). Key words: Citrus macroptera, Rutaceae, Lupeol, Stigmasterol, Antioxidant.   doi: 10.3329/bjsir.v43i4.2235 Bangladesh J. Sci. Ind. Res. 43(4), 449-454, 2008

scholarly journals Constituents of Erythrina lysistemon: Their Brine Shrimp Lethality, Antimicrobial and Radical Scavenging Activities

2006 ◽  
Vol 1 (2) ◽  
pp. 1934578X0600100 ◽  
Author(s):  
Benard F. Juma ◽  
Runner R. T. Majinda
Keyword(s):  
Radical Scavenging ◽  
Dienoic Acid ◽  
Stem Bark ◽  
Artemia Salina ◽  
Moderate Activity ◽  
Stem Wood ◽  
Brine Shrimps ◽  
Weak Activity ◽  
Radical Scavenging Ability ◽  
New Compounds

Three new compounds, 4′,7-dihydroxy-2″,2″-dimethylpyrano [5″,6″: 5,6]-isoflavone (1), (7 E) (8,2′)-3,7,9,5′,9′-pentahydroxy-4,4′-dimethoxyneolign-7-ene (2) and (9 E,11 Z) 14-hydroxyoctadecan-9,11-dienoic acid (3), along with other known flavonoids, benzenoids, alkaloids and phenylpropanoids were isolated from the twigs, leaves, stem bark, stem wood and flowers of Erythrina lysistemon. Their structures were established on the basis of spectroscopic evidence. Some of these compounds have shown high lethality against brine shrimps ( Artemia salina), moderate radical scavenging ability in the DPPH assay, moderate antifungal activity against Candida mycoderma, moderate activity against the Gram-positive ( Bacillus subtilis and Staphylococcus aureus) and weak activity against Gram-negative bacteria ( Escherichia coli).

scholarly journals Chemical Constituents of the Aerial Parts ofDaucus carotasubsp.hispidusGrowing in Tunisia

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1986351
Author(s):  
Saoussen Hammami ◽  
Abdelsamed I. Elshamy ◽  
Ridha El Mokni ◽  
Ali Snene ◽  
Kanako Iseki ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Squamous Carcinoma ◽  
2D Nmr ◽  
Spectroscopic Techniques ◽  
Aerial Parts ◽  
Weak Activity ◽  
Cervical Cells ◽  
Antimicrobial And Antioxidant Activity ◽  
First Time ◽  
High Resolution Mass Spectroscopy

Three known polyol menthane monoterpenoids, namely, (4 R)-1- p-menthen-6,8-diol (1), (4 R)-1- p-menthen-4,7-diol (2), and (1 R,2 R,4 R)- p-menthane-1,2,4-triol (3), and 6 known phenolics (4-9), in addition to β-sitosterol 3- O-glucoside (10), were isolated from the aerial parts of Daucus carota subsp. hispidus (Ball) Heywood (Family: Apiaceae) growing in Tunisia. The structures of the isolated compounds were established depending upon the spectroscopic techniques including one and two-dimensional nuclear magnetic resonance (1D, and 2D NMR) and high resolution mass spectroscopy (HRMS). The absolute configuration of the compounds 1 to 3 was determined using experimental circular dichroism (CD) for the first time. Compounds 1 to 3 were reported for the first time from this plant. Compounds 1 to 3 exhibited no antimicrobial and antioxidant activity using superoxide dismutase-like activities. Compounds 2 and 3 exhibited weak activity, while 1 showed negative cytotoxic activity against human mouth squamous carcinoma (HSC-2) and human cervical cells (HeLa) cancer cells.

scholarly journals Antiparasitic Indole Alkaloids from Aspidosperma desmanthum and A. spruceanum from the Peruvian Amazonia

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900
Author(s):  
Matías Reina ◽  
Lastenia Ruiz-Mesia ◽  
Wilfredo Ruiz-Mesia ◽  
Frida Enriqueta Sosa-Amay ◽  
Leonor Arevalo-Encinas ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Indole Alkaloids ◽  
2D Nmr ◽  
Stem Bark ◽  
Spectroscopic Techniques ◽  
Root Bark ◽  
Antiparasitic Activity ◽  
Specific Cytotoxicity ◽  
First Time ◽  
Selective Activity

Twenty-three indole alkaloids were isolated from Aspidosperma desmanthum and A. spruceanum. Alkaloids 1-4 were isolated from the leaves, 5-8 from the stem bark and 9-15 from the root bark of A. desmanthum. Alkaloids 5, 11, 16, 17 and 19 were isolated from the stem bark, 18 and 20-22 from the root bark and 23 from the flowers of A. spruceanum. Compounds 4, 14, and 15 have not been previously reported as natural products while 16 and 20 have been isolated for the first time from the genus Aspidosperma. Their structures were determined by spectroscopic techniques including 1D and 2D NMR experiments (COSY, NOESY, HSQC, HMBC). The antiparasitic activity of these compounds was tested against Trypanosoma cruzi and Leishmania infantum and their non-specific cytotoxicity on mammalian cells. The most active compounds were 10, 12, 13, and 14 from A. desmanthum, and 19, 21 and 22 from A. spruceanum. Aspidolimine (10) aspidocarpine (12) and tubotaiwine (21) showed selective activity against L. infantum.

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