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anti tuberculosis drugs

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https://www.readbyqxmd.com/read/28647191/pyrrolidine-dithiocarbamate-alleviates-the-anti-tuberculosis-drug-induced-liver-injury-through-jak2-stat3-signaling-pathway-an-experimental-study
#1
Hong Zhang, Yang Liu, Li-Kun Wang, Na Wei
OBJECTIVE: To study the effect of pyrrolidine dithiocarbamate (PDTC) on the anti-tuberculosis drug-induced liver injury and the molecular mechanism. METHODS: Clean male SD rats were selected as experimental animals and randomly divided into normal group, model group, PDTC group and AG490 group. Animal model of anti-tuberculosis drug-induced liver injury was established by intragastric administration isoniazid + rifampicin. PDTC group received intraperitoneal injection of PDTC, and AG490 group received intraperitoneal injection of AG490...
May 2017: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/28646434/performance-of-quantiferon-%C3%A2-tb-gold-in-tube-assay-in-children-receiving-disease-modifying-anti-rheumatic-drugs
#2
Francesca Gabriele, Maria Trachana, Maria Simitsopoulou, Polixeni Pratsidou-Gertsi, Elias Iosifidis, Zoi Dorothea Pana, Emmanuel Roilides
BACKGROUND: To evaluate the performance of the Quantiferon(®)-TB Gold In-Tube (QFT-IT) interferon (IFN)-γ assay for the detection of latent tuberculosis infection (LTBI) in children receiving anti-rheumatic treatment in a tertiary referral hospital of Northern Greece. METHODS: A total of 79 consecutive children receiving anti-rheumatic treatment [of which 18 screened prior to antitumor necrosis factor (TNF)-α treatment] were tested using Mantoux tuberculin skin test (TST) and QFT-IT...
June 22, 2017: World Journal of Pediatrics: WJP
https://www.readbyqxmd.com/read/28642632/mcl-plays-an-anti-inflammatory-role-in-mycobacterium-tuberculosis-induced-immune-response-by-inhibiting-nf-%C3%AE%C2%BAb-and-nlrp3-inflammasome-activation
#3
Qingwen Zhang, Xinru Jiang, Weigang He, Kailin Wei, Jinxia Sun, Xiangyang Qin, Yuejuan Zheng, Xin Jiang
Mycobacterium tuberculosis (Mtb) remains a significant menace to global health as it induces granulomatous lung lesions and systemic inflammatory responses during active tuberculosis (TB). Micheliolide (MCL), a sesquiterpene lactone, was recently reported to have a function of relieving LPS-induced inflammatory response, but the regulative role of MCL on the immunopathology of TB still remains unknown. In this experiment, we examined the inhibitory effect of MCL on Mtb-induced inflammatory response in mouse macrophage-like cell line Raw264...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28636418/dxs-as-a-target-for-structure-based-drug-design
#4
Robin Matthias Gierse, Eswar Redeem, Eleonora Diamanti, Carsten Wrenger, Matthew R Groves, Anna Kh Hirsch
In this review, we analyze the enzyme DXS, the first and rate-limiting protein in the methylerythritol 4-phosphate pathway. This pathway was discovered in 1996 and is one of two known metabolic pathways for the biosynthesis of the universal building blocks for isoprenoids. It promises to offer new targets for the development of anti-infectives against the human pathogens, malaria or tuberculosis. We mapped the sequence conservation of 1-deoxy-xylulose-5-phosphate synthase on the protein structure and analyzed it in comparison with previously identified druggable pockets...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28635627/molecular-quantum-similarity-chemical-reactivity-and-database-screening-of-3d-pharmacophores-of-the-protein-kinases-a-b-and-g-from-mycobacterium-tuberculosis
#5
Alejandro Morales-Bayuelo
Mycobacterium tuberculosis remains one of the world's most devastating pathogens. For this reason, we developed a study involving 3D pharmacophore searching, selectivity analysis and database screening for a series of anti-tuberculosis compounds, associated with the protein kinases A, B, and G. This theoretical study is expected to shed some light onto some molecular aspects that could contribute to the knowledge of the molecular mechanics behind interactions of these compounds, with anti-tuberculosis activity...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28633700/trends-in-drug-resistant-tuberculosis-after-the-implementation-of-the-dots-strategy-in-shenzhen-china-2000-2013
#6
L Zhu, Y-Z Yang, H-Y Guan, S-M Cheng, Y-Y Jin, W-G Tan, Q-F Wu, X-L Liu, M-G Zhao, Z-H Lu, Z-W Jia
SETTING: The DOTS strategy has been regarded as the most cost-effective way to stop the spread of tuberculosis (TB) since its launch by the World Health Organization. OBJECTIVE: To estimate the effects of DOTS by tracking long-term trends in multidrug-resistant TB (MDR-TB). DESIGN: A retrospective cohort study was conducted from 2000 to 2013 to analyse trends in resistance to anti-tuberculosis drugs and the effect of DOTS-based treatment in Shenzhen, China, using the χ2 test...
July 1, 2017: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/28630193/pyrazinamide-susceptibility-and-pnca-mutation-profile-of-mycobacterium-tuberculosis-among-multi-drug-resistant-tuberculosis-patients-in-bangladesh
#7
Arfatur Rahman, Sara Sabrina Ferdous, Shahriar Ahmed, S M Mazidur Rahman, Mohammad Khaja Mafij Uddin, Suporn Pholwat, Jean Gratz, Eric Houpt, Sayera Banu
Pyrazinamide (PZA) is a front line anti-tuberculosis (anti-TB) drug used in both first and second line treatment regimen. However, due to complex laboratory requirements, the PZA susceptibility test is rarely performed leading to the scarcity of data. Bangladesh is both a high TB and multi-drug resistant (MDR-TB) burden country but to our knowledge the published data on PZA susceptibility is limited, especially among MDR-TB patients. We aimed to analyze the PZA susceptibility pattern of Mycobacterium tuberculosis (MTB) isolates from MDR-TB patients and to correlate pncA mutation with PZA resistance in Bangladesh...
June 19, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28629306/%C3%AE-ca-specific-inhibitor-dithiocarbamate-fc14-584b-a-novel-antimycobacterial-agent-with-potential-to-treat-drug-resistant-tuberculosis
#8
Ashok Aspatwar, Milka Hammarén, Sanni Koskinen, Bruno Luukinen, Harlan Barker, Fabrizio Carta, Claudiu T Supuran, Mataleena Parikka, Seppo Parkkila
Inhibition of novel biological pathways in Mycobacterium tuberculosis (Mtb) creates the potential for alternative approaches for treating drug-resistant tuberculosis. In vitro studies have shown that dithiocarbamate-derived β-carbonic anhydrase (β-CA) inhibitors Fc14-594 A and Fc14-584B effectively inhibit the activity of Mtb β-CA enzymes. We screened the dithiocarbamates for toxicity, and studied the in vivo inhibitory effect of the least toxic inhibitor on M. marinum in a zebrafish model. In our toxicity screening, Fc14-584B emerged as the least toxic and showed minimal toxicity in 5-day-old larvae at 300 µM concentration...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28628823/drug-development-against-tuberculosis-impact-of-alkaloids
#9
REVIEW
Shardendu K Mishra, Garima Tripathi, Navneet Kishore, Rakesh K Singh, Archana Singh, Vinod K Tiwari
Despite of the advances made in the treatment and management, tuberculosis (TB) still remains one of main public health problem. The contrary effects of first and second-line anti-tuberculosis drugs have generated extended research interest in natural products in the hope of devising new antitubercular leads. Interestingly, plethoras of natural products have been discovered to exhibit activity towards various resistant strains of M. tuberculosis. Extensive applications of alkaloids in the field of therapeutics is well-established and nowday's researches being pursued to develop new potent drugs from natural sources for tuberculosis...
June 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28627738/systematic-review-on-the-proteomic-profile-of-mycobacterium-tuberculosis-exposed-to-drugs
#10
REVIEW
Paula Aline Zanetti Campanerut-Sá, Luciana Dias Ghiraldi-Lopes, Jean Eduardo Meneguello, Jorge Juarez Vieira Teixeira, Regiane Bertin de Lima Scodro, Vera Lucia Dias Siqueira, Terezinha Inez Estivalet Svidzinski, Fernando Rogério Pavan, Rosilene Fressatti Cardoso
We present an over view about proteomics studies in Mycobacterium tuberculosis exposed to some anti-tuberculosis drugs and new candidates, using two-dimensional gel electrophoresis and mass spectrometry. To date, that we have knowledge, this is the first studies that was performed specifically in M. tuberculosis using systematic review on electronic literature conducted in three databases using the following search terms: tuberculosis OR mycobacterium tuberculosis, proteome OR proteomics, and mass spectrometry electrospray ionization OR matrix assisted laser desorption ionization OR two dimensional gel electrophoresis...
June 19, 2017: Proteomics. Clinical Applications
https://www.readbyqxmd.com/read/28627431/evaluation-of-the-quantamatrix-multiplexed-assay-platform-system-for-simultaneous-detection-of-mycobacteirum-tuberculosis-and-rifampicin-resistance-gene-using-culture-positive-mycobacteria
#11
Hye-Young Wang, Young Uh, Seoyong Kim, Tae-Sun Shim, Hyeyoung Lee
BACKGROUND: The differentiation of Mycobacterium tuberculosis complex (MTBC) from nontuberculous mycobacteria (NTM) is of primary importance for infection control and choice of anti-tuberculosis drugs. Prevailing data on rifampicin (RIF)-resistant TB is essential for early management of multidrug resistant-TB. The aim of this study was to evaluate the usefulness of a newly developed multiplexed, bead-based bioassay (Quantamatrix Multiplexed Assay Platform; QMAP) for the rapid differentiation of 23 Mycobacterium species including MTBC and RIF-resistant strains...
June 13, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28625141/bedaquiline-a-new-hope-for-shorter-and-better-anti-tuberculosis-regimens
#12
Niccolò Riccardi, Filippo Del Puente, Federica Magnè, Lucia Taramasso, Antonio Di Biagio
In 2014, an estimated 1.8 million people died from Mycobacterium tuberculosis (MTB); moreover, 680,000 people developed multidrug-resistant TB (MDR-TB). Currently available anti-MDR and XDR regimens are long-lasting and expensive, need high adherence and are undermined by a high frequency of adverse drug events, thus leading to a low success rate; moreover, in the last 50 years only two new molecules, bedaquiline (BDQ) and delamanid, have been approved and released for treatment of MDR-TB. BDQ is a diarylquinoline anti-mycobacterial drug, active regardless the state of MTB; in fact, its efficacy is conserved against replicating and non-replicating bacilli, despite extracellular or intracellular location...
June 19, 2017: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/28624659/surface-engineering-of-solid-lipid-nanoparticle-assemblies-by-methyl-%C3%AE-d-mannopyranoside-for-the-active-targeting-to-macrophages-in-anti-tuberculosis-inhalation-therapy
#13
Eleonora Maretti, Luca Costantino, Cecilia Rustichelli, Eliana Leo, Maria Antonietta Croce, Francesca Buttini, Eleonora Truzzi, Valentina Iannuccelli
This study describes the development of new mannosylated Solid Lipid Nanoparticle assemblies (SLNas) delivering rifampicin for an inhaled treatment of tuberculosis. SLNas were surface engineered with mannose residues to recognize mannose receptors located on infected alveolar macrophages and facilitate cell internalization. Two sets of SLNas were produced by the melt emulsifying technique using biocompatible lipid components, i.e. cholesteryl myristate combined with palmitic acid (PA set) or tripalmitin (TP set), in the presence of the targeting moiety, methyl α-d-mannopyranoside...
June 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28621733/discovery-of-indeno-1-2-c-quinoline-derivatives-as-potent-dual-antituberculosis-and-anti-inflammatory-agents
#14
Chih-Hua Tseng, Chun-Wei Tung, Chen-Hsin Wu, Cherng-Chyi Tzeng, Yen-Hsu Chen, Tsong-Long Hwang, Yeh-Long Chen
A series of indeno[1,2-c]quinoline derivatives were designed, synthesized and evaluated for their anti-tuberculosis (anti-TB) and anti-inflammatory activities. The minimum inhibitory concentration (MIC) of the newly synthesized compound was tested against Mycobacterium tuberculosis H37RV. Among the tested compounds, (E)-N'-[6-(4-hydroxypiperidin-1-yl)-11H-indeno[1,2-c]quinolin-11-ylidene]isonicotino-hydrazide (12), exhibited significant activities against the growth of M. tuberculosis (MIC values of 0.96 μg/mL) with a potency approximately equal to that of isoniazid (INH), an anti-TB drug...
June 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28620844/comparison-of-the-characteristics-of-mycobacterium-tuberculosis-isolates-from-sputum-and-lung-lesions-in-chronic-tuberculosis-patients
#15
M-S Hong, Y Kim, E-J Cho, J-S Lee, H-K Kwak, J-H Kim, C-T Kim, J-S Cho, S-K Park, D Jeon, Y-I Choi, H Lee, S-Y Eum
Mycobacterium tuberculosis (Mtb) in sputum originates from lung cavities in tuberculosis (TB) patients. But drug susceptibility testing (DST) of sputum Mtb can not be conducted the same as in the lung because mutagenesis of bacilli may be happening in the lung during treatment and result in the possibility of the presence of heterogeneous drug-resistant subpopulations in the different lung lesions. This could be one of the reasons for low cure rates for multi-drug resistant (MDR)-TB. We studied the resected lungs of nine surgery patients with chronic TB...
June 15, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28619387/evaluation-of-ameliorative-ability-of-silibinin-against-zidovudine-and-isoniazid-induced-hepatotoxicity-and-hyperlipidaemia-in-rats-role-of-silibinin-in-phase-i-and-ii-drug-metabolism
#16
Raghu Ramanathan, Karthikeyan Sivanesan
HIV/AIDS patients have suppressed immune system, making them vulnerable to many opportunistic infections including tuberculosis (TB). The patients who are co-infected with TB undergo combined regimens with anti-retroviral drugs such as zidovudine (AZT) and anti-tubercular drug such as isoniazid (INH) for therapy leading to hepatotoxicty. Silibinin (SBN), extracted from Silybum marianum commonly called as "Milk thistle" is used against several drugs-induced hepatotoxicity. The present study evaluates the ameliorative effect of SBN against AZT alone, INH alone, and INH + AZT-induced toxic insults to liver of rats...
June 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28611374/efficacy-and-safety-of-mycobacterium-indicus-pranii-as-an-adjunct-therapy-in-category-ii-pulmonary-tuberculosis-in-a-randomized-trial
#17
Surendra K Sharma, Kiran Katoch, Rohit Sarin, Raman Balambal, Nirmal Kumar Jain, Naresh Patel, Kolluri J R Murthy, Neeta Singla, P K Saha, Ashwani Khanna, Urvashi Singh, Sanjiv Kumar, A Sengupta, J N Banavaliker, D S Chauhan, Shailendra Sachan, Mohammad Wasim, Sanjay Tripathi, Nilesh Dutt, Nitin Jain, Nalin Joshi, Sita Ram Raju Penmesta, Sumanlatha Gaddam, Sanjay Gupta, Bakulesh Khamar, Bindu Dey, Dipendra K Mitra, Sunil K Arora, Sangeeta Bhaskar, Rajni Rani
Prolonged treatment of tuberculosis (TB) often leads to poor compliance, default and relapse, converting primary TB patients into category II TB (Cat IITB) cases, many of whom may convert to multi-drug resistant TB (MDR-TB). We have evaluated the immunotherapeutic potential of Mycobacterium indicus pranii (MIP) as an adjunct to Anti-Tubercular Treatment (ATT) in Cat II pulmonary TB (PTB) patients in a prospective, randomized, double blind, placebo controlled, multicentric clinical trial. 890 sputum smear positive Cat II PTB patients were randomized to receive either six intra-dermal injections (2 + 4) of heat-killed MIP at a dose of 5 × 10(8) bacilli or placebo once in 2 weeks for 2 months...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28610794/molecular-mechanisms-of-action-resistance-detection-to-the-first-line-anti-tuberculosis-drugs-rifampicin-and-pyrazinamide-in-the-post-whole-genome-sequencing-era
#18
REVIEW
Ameeruddin Nusrath Unissa, Luke Elizabeth Hanna
Recent studies in addition to studies based on whole genome sequencing (WGS) of clinical isolates of Mycobacterium tuberculosis (MTB) from diverse geographical regions have provided useful insights into the mechanisms of drug resistance. Of importance, are some of the findings pertaining to mechanisms of resistance to two of the first-line anti-tuberculosis (TB) drugs, namely, rifampicin (RIF) and pyrazinamide (PZA). For example, the implication of mutations in rpoA and rpoC genes that act as compensatory mutations for those in the rpoB gene with respect to RIF resistance is noteworthy...
July 2017: Tuberculosis
https://www.readbyqxmd.com/read/28610791/the-role-of-the-time-kill-kinetics-assay-as-part-of-a-preclinical-modeling-framework-for-assessing-the-activity-of-anti-tuberculosis-drugs
#19
Hannelore I Bax, Irma A J M Bakker-Woudenberg, Corné P de Vogel, Aart van der Meijden, Annelies Verbon, Jurriaan E M de Steenwinkel
Novel treatment strategies for tuberculosis are urgently needed. Many different preclinical models assessing anti-tuberculosis drug activity are available, but it is yet unclear which combination of models is most predictive of clinical treatment efficacy. The aim of this study was to determine the role of our in vitro time kill-kinetics assay as an asset to a predictive preclinical modeling framework assessing anti-tuberculosis drug activity. The concentration- and time-dependent mycobacterial killing capacities of six anti-tuberculosis drugs were determined during exposure as single drugs or in dual, triple and quadruple combinations towards a Mycobacterium tuberculosis Beijing genotype strain and drug resistance was assessed...
July 2017: Tuberculosis
https://www.readbyqxmd.com/read/28606115/peripheral-neuropathy-in-a-diabetic-child-treated-with-linezolid-for-multidrug-resistant-tuberculosis-a-case-report-and-review-of-the-literature
#20
Aravind Swaminathan, Philipp du Cros, James A Seddon, Shamsiya Mirgayosieva, Rajabov Asladdin, Zulfiya Dusmatova
BACKGROUND: Extensively drug-resistant (XDR) tuberculosis (TB) and multidrug resistant (MDR)-TB with additional resistance to injectable agents or fluoroquinolones are challenging to treat due to lack of available, effective drugs. Linezolid is one of the few drugs that has shown promise in treating these conditions. Long-term linezolid use is associated with toxicities such as peripheral and optic neuropathies. Diabetes mellitus (DM), especially when uncontrolled, can also result in peripheral neuropathy...
June 12, 2017: BMC Infectious Diseases
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