- Translational predictions of phase 2a first-in-patient efficacy studies for antituberculosis drugs. [Preprint]bioRxiv. 2023 Jan 20B
- CONCLUSIONS: This platform provides an innovative solution to inform or even replace phase 2a EBA trials, to bridge the gap between mouse efficacy studies and phase 2b and phase 3 trials, and to substantially accelerate drug development.
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- One-pot green synthesis of chitosan biguanidine nanoparticles for targeting M. tuberculosis. [Journal Article]Int J Biol Macromol. 2023 Jan 23 [Online ahead of print]IJ
- Tuberculosis (TB) is considered as one of the most fatal infectious diseases nowadays. Several traditional anti-tuberculosis drugs like isoniazid have been largely applied; however, they are associated with toxicity and poor anti-TB treatment. So, the fabrication of new alternative anti-TB drugs containing natural biopolymers for TB treatment has attracted great attention in recent years because …
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- Biocompatible and biodegradable copper-protocatechuic metal-organic frameworks as rifampicin carrier. [Journal Article]Biomater Adv. 2022 Dec 22; 146:213269.BA
- Tuberculosis (TB) is a disease caused by the M. tuberculosis bacteria infection and is listed as one of the deadliest diseases to date. Despite the development of antituberculosis drugs, the need for long-term drug consumption and low patient commitment are obstacles to the success of TB treatment. A continuous drug delivery system that has a long-term effect is needed to reduce routine drug cons…
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- State of the Art on Developments of (Bio)Sensors and Analytical Methods for Rifamycin Antibiotics Determination. [Review]
- This review summarizes the literature data reported from 2000 up to the present on the development of various electrochemical (voltammetric, amperometric, potentiometric and photoelectrochemical), optical (UV-Vis and IR) and luminescence (chemiluminescence and fluorescence) methods and the corresponding sensors for rifamycin antibiotics analysis. The discussion is focused mainly on the foremost c…
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- In Vivo Toxicity, Redox-Modulating Capacity and Intestinal Permeability of Novel Aroylhydrazone Derivatives as Anti-Tuberculosis Agents. [Journal Article]
- The emergence and spread of Mycobacterium tuberculosis strains resistant to many or all anti-tuberculosis (TB) drugs require the development of new compounds both efficient and with minimal side effects. Structure-activity-toxicity relationships of such novel, structurally diverse compounds must be thoroughly elucidated before further development. Here, we present the aroylhydrazone compounds (3a…
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- Imidazole: Synthesis, Functionalization and Physicochemical Properties of a Privileged Structure in Medicinal Chemistry. [Review]
- Imidazole was first synthesized by Heinrich Debus in 1858 and was obtained by the reaction of glyoxal and formaldehyde in ammonia, initially called glyoxaline. The current literature provides much information about the synthesis, functionalization, physicochemical characteristics and biological role of imidazole. Imidazole is a structure that, despite being small, has a unique chemical complexity…
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- First and Second-Line Anti-Tuberculosis Drug-Resistance Patterns in Pulmonary Tuberculosis Patients in Zambia. [Journal Article]
- CONCLUSIONS: This study has established a high rate of multidrug-resistant TB and has further identified both pre-XDR- and XDR-TB. There is a need to intensify surveillance of MDR- and XDR-TB to inform future guidelines for effective treatment and monitoring.
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- QSAR Studies, Molecular Docking, Molecular Dynamics, Synthesis, and Biological Evaluation of Novel Quinolinone-Based Thiosemicarbazones against Mycobacterium tuberculosis. [Journal Article]
- In this study, a series of novel quinolinone-based thiosemicarbazones were designed in silico and their activities tested in vitro against Mycobacterium tuberculosis (M. tuberculosis). Quantitative structure-activity relationship (QSAR) studies were performed using quinolinone and thiosemicarbazide as pharmacophoric nuclei; the best model showed statistical parameters of R2 = 0.83; F = 47.96; s =…
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- A multidisciplinary approach to verify and de-label of drug allergic histories in a university hospital in Thailand: a retrospective descriptive study. [Journal Article]
- CONCLUSIONS: More than half of drug allergic histories were successfully confirmed or de-labeled by the multidisciplinary ADR team. The collaborative activities of various healthcare professionals, consisting of physicians, nurse, and pharmacists as presented in the study were effective in VD services and should be implemented in other healthcare settings.
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- Essential oil of Gallesia integrifolia is active against mycobacteria. [Journal Article]Future Microbiol. 2023 Jan 20 [Online ahead of print]FM
- Background: There is critical need for new therapeutic options for treatment of diseases caused by mycobacteria. Materials & methods: Gallesia integrifolia essential oils (EOs) and crude extracts (CEs) were tested for their anti-Mycobacterium tuberculosis and anti-nontuberculous mycobacteria activity. Results: Minimum inhibitory concentration (MIC) of EOs ranged from 15.63 to 62.5 μg/ml against M…
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- 3D Printed Housing Devices for Segregated Compartmental Delivery of Oral Fixed-Dose Anti-Tubercular Drugs Adopting Print and Fill Strategy. [Journal Article]
- World Health Organization (WHO) recommends the use of first-line anti-tuberculosis drugs, that is, rifampicin (RIF) and isoniazid (INH) fixed-dose combination (FDC) therapies in tuberculosis (TB) disease. The absorption of RIF from an FDC incorporates INH, and it is significantly compromised due to its reaction with INH, resulting in a severe loss of RIF under gastric stomach pH condition. Such r…
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- Need for anti-tuberculosis treatment in patients with latent tuberculosis infection who undergo arthroplasty: a case report. [Case Reports]
- CONCLUSIONS: Patients with LTBI who undergo artificial arthroplasty require anti-TB treatment to reduce the risk of TB recurrence.
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- Molecular Characterization of Resistance to Second-Line Anti-Mycobacterial Drugs among Clinical Isolates of Multidrug-Resistant Mycobacterium tuberculosis. [Journal Article]Clin Lab. 2023 Jan 01; 69(1)CL
- CONCLUSIONS: The frequency of CIP/OFL and AMK/CAP/KAN-resistant TB is considerable among Iranian tuberculosis cases. HRM assay is a rapid and inexpensive test and can detect important mutation-based drug resistance in MDR-TB and XDR-TB isolates.
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- Dual antituberculosis drugs-loaded gelatin hydrogel bioimplant for treating spinal tuberculosis. [Journal Article]Int J Pharm. 2023 Jan 13; 633:122609.IJ
- Spinal tuberculosis (TB) represents around 1% of the recorded TB with a high mortality rate due to neurological complications and kyphosis. The current work aimed to develop a bioimplant scaffold to treat spinal TB disease. The scaffold is composed of a biocompatible semi-interpenetrating (semi-IPN) gelatin-based hydrogel incorporating mesoporous silica nanoparticles (MPS-NPs) loaded with rifampi…
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- Analysis of serum microRNA-122 in a randomized controlled trial of N-acetylcysteine for treatment of antituberculosis drug-induced liver injury. [Journal Article]Br J Clin Pharmacol. 2023 Jan 13 [Online ahead of print]BJ
- CONCLUSIONS: miR-122 concentrations in our participants with AT-DILI were considerably higher than previously reported in healthy volunteers and in patients on antituberculosis therapy without liver injury. We did not detect an effect of NAC on miR-122 concentrations. Further research is needed to determine the utility of miR-122 in the diagnosis and management of AT-DILI.
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- Tuberculous Pleurisy Diagnosed From Massive Pleural Effusion in an Older Patient With No History of Tuberculosis. [Case Reports]
- Tuberculous pleurisy is an infectious disease with a poor prognosis needing early diagnosis. The use of appropriate antituberculosis drugs can improve prognosis. However, the diagnosis of tuberculous pleurisy is often challenging in older patients. Decreased activities of daily living (ADLs) may lead to difficulty in performing invasive procedures to make a definite diagnosis of pleural effusion.…
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- Anti-tuberculosis drug development via targeting the cell envelope of Mycobacterium tuberculosis. [Review]
- Mycobacterium tuberculosis possesses a dynamic cell envelope, which consists of a peptidoglycan layer, a mycolic acid layer, and an arabinogalactan polysaccharide. This envelope possesses a highly complex and unique structure representing a barrier that protects and assists the growth of M. tuberculosis and allows its adaptation to the host. It regulates the immune response of the host cells, cau…
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- [Annual progress of chemotherapy of multidrug/rifampicin-resistant tuberculosis in 2022]. [Review]Zhonghua Jie He He Hu Xi Za Zhi. 2023 Jan 12; 46(1):62-66.ZJ
- At present, the number of cases with multidrug/rifampicin-resistant tuberculosis (MDR/RR-TB) in China ranks fourth in the world, and the prevention and control situation is still serious. Chemotherapy, as the most important treatment for MDR/RR-TB, was studied and explored by domestic and foreign researchers in 2022. New chemotherapeutic drugs such as delpazolid, sutezolid, telacebec and independ…
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- Synthesis and Structure-Activity Relationship of 2,6-Disubstituted Thiosemicarbazone Derivatives of Pyridine as Potential Antituberculosis Agents. [Journal Article]
- In this study, six new 2,6-disubstituted thiosemicarbazone derivatives of pyridine were synthesized (4-9), and their tuberculostatic activity was evaluated. All of them showed two- to eightfold higher activity (minimum inhibitory concentration (MIC) 0.5-4 µg/mL) against the resistant strain compared with the reference drug. Compounds 5 and 7, which contained the most basic substituents-pyrrolidin…
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- Epidemiology of tuberculosis and susceptibility to antituberculosis drugs in Reunion Island. [Journal Article]
- CONCLUSIONS: This is the first exhaustive epidemiological study of tuberculosis in Reunion Island. The incidence there is relatively low but increased for people with links to neighboring islands, particularly Madagascar. The prevalence of multidrug resistance is low, with no associated increased risk for patients from the Indian Ocean area.
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- Ardisia gigantifolia stapf (Primulaceae): A review of ethnobotany, phytochemistry, pharmacology, clinical application, and toxicity. [Review]J Ethnopharmacol. 2023 Apr 06; 305:116079.JE
- CONCLUSIONS: To date, most bioactive compounds are identified from the rhizomes of A. gigantifolia, which pharmacological activity and clinical observational studies have validated the plant's traditional use as a treatment for rheumatoid arthritis. It would be helpful to verify the mechanism of some components in vivo, such as gigantifolinol. Moreover, the plant's triterpenoid saponins demonstrated valid anti-tumor effects, especially the AG4 and AG36 compounds, which were shown to have anti-breast cancer effects both in vitro and in vivo. Further research on these components, including molecular mechanisms and in vivo metabolic regulation, needs to be confirmed.
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- The first-line antituberculosis drugs, and their fixed-dose combination induced abnormal sperm morphology and histological lesions in the testicular cells of male mice. [Journal Article]
- Rifampicin (RIF), Isoniazid (INH), Ethambutol (EMB), Pyrazinamide (PZA), and/or their fixed-dose combination (FDC) are extensively prescribed in the cure of Tuberculosis (TB) globally. In spite of the beneficial effect, these drugs are capable of inducing cellular toxicity. Existing information on the genotoxic effects of the first-line anti-TB drugs is limited and contentious. Herein, we evaluat…
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- Synthesis, Characterization, 'ADMET-SAR' Prediction, DPPH Assay, and Anti-Mycobacterium Study of 4-[(substituted benzyl) amino]benzohydrazides and its Hydrazones as the Acyl-CoA Carboxylase, AccD5 Inhibitors. [Journal Article]Curr Comput Aided Drug Des. 2022 12 27 [Online ahead of print]CC
- CONCLUSIONS: Our results signify hydrazones/hydrazines as potential hit candidates against the future developments of potent and safer anti-TB agents.
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- Antimicrobial Peptides as Immunomodulators and Antimycobacterial Agents to Combat Mycobacterium tuberculosis: a Critical Review. [Journal Article]Probiotics Antimicrob Proteins. 2022 Dec 28 [Online ahead of print]PA
- Tuberculosis (TB) is a devastating disease foisting a significantly high morbidity, prepotent in low- and middle-income developing countries. Evolution of drug resistance among Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis, has made the TB treatment more complicated. The protracted nature of present TB treatment, persistent and tolerant Mtb populations, interaction with an…
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- Pharmacokinetics and pharmacodynamics of anti-tuberculosis drugs: An evaluation of in vitro, in vivo methodologies and human studies. [Review]
- There has been an increased interest in pharmacokinetics and pharmacodynamics (PKPD) of anti-tuberculosis drugs. A better understanding of the relationship between drug exposure, antimicrobial kill and acquired drug resistance is essential not only to optimize current treatment regimens but also to design appropriately dosed regimens with new anti-tuberculosis drugs. Although the interest in PKPD…
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- Morphology of Lymphoid Tissue in the Lungs of Guinea Pigs Infected with Mycobacterium bovis against the Background of Vaccine Immunity and the Action of Betulin and Its Derivatives. [Journal Article]
- Tuberculosis caused by Mycobacterium bovis is a serious problem for animal and human health worldwide. A promising concept for the design of anti-tuberculosis drugs is the conjugation of an immunogenic fraction isolated from bacterial vaccines with a stimulating component. Taking this principle as a basis, conjugates based on BCG antigens with betulin and its derivatives (betulonic and betulinic …
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- Ultrasensitive Detection of Multidrug-Resistant Mycobacterium tuberculosis Using SuperSelective Primer-Based Real-Time PCR Assays. [Journal Article]
- The emergence of drug-resistant tuberculosis is a significant global health issue. The presence of heteroresistant Mycobacterium tuberculosis is critical to developing fully drug-resistant tuberculosis cases. The currently available molecular techniques may detect one copy of mutant bacterial genomic DNA in the presence of about 1-1000 copies of wild-type M. tuberculosis DNA. To improve the limit…
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- The pathogenic mechanism of Mycobacterium tuberculosis: implication for new drug development. [Review]
- Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis (TB), is a tenacious pathogen that has latently infected one third of the world's population. However, conventional TB treatment regimens are no longer sufficient to tackle the growing threat of drug resistance, stimulating the development of innovative anti-tuberculosis agents, with special emphasis on new protein targets. The…
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- SigH stress response mediates killing of Mycobacterium tuberculosis by activating nitronaphthofuran prodrugs via induction of Mrx2 expression. [Journal Article]
- The emergence of drug-resistant Mycobacterium tuberculosis strains highlights the need to discover anti-tuberculosis drugs with novel mechanisms of action. Here we discovered a mycobactericidal strategy based on the prodrug activation of selected chemical derivatives classified as nitronaphthofurans (nNFs) mediated by the coordinated action of the sigH and mrx2 genes. The transcription factor Sig…
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- A case of prosthetic joint infection caused by Mycobacterium tuberculosis complicated secondary bacterial infection after knee joint replacement surgery. [Case Reports]J Infect Chemother. 2022 Dec 15 [Online ahead of print]JI
- Mycobacterium tuberculosis (M. tuberculosis) is a rare cause of prosthetic joint infection (PJI). Previous studies have reported that many cases of PJI caused by M. tuberculosis have no medical history of active tuberculosis (TB) or other localization, which contributes to diagnostic difficulties. Furthermore, owing to the limited number of studies on treatment, appropriate treatment strategies, …
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