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Expert Opin Drug Discov 2022 May 16. Epub 2022 May 16.

Department of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.

Introduction: Several decades of antitubercular drug discovery efforts have focused on novel antitubercular chemotherapies. However, recent efforts have greatly shifted towards countering extremely/multi/total drug-resistant species. Targeting the conditionally essential elements inside Mycobacterium is a relatively new approach against tuberculosis and has received lackluster attention. Read More

J Mol Biol 2022 Apr 28:167610. Epub 2022 Apr 28.

Research Unit in Bioinformatics (RUBi), Department of Biochemistry and Microbiology, Rhodes University, Makhanda 6140, South Africa. Electronic address:

Drug research and development is a multidisciplinary field with its own successes. Yet, given the complexity of the process, it also faces challenges over the long development stages and even includes those that develop once a drug is marketed, i.e. Read More

J Antimicrob Chemother 2022 Apr 25. Epub 2022 Apr 25.

Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Cape Town, South Africa.

Objectives: Ethambutol protects against the development of resistance to co-administered drugs in the intensive phase of first-line anti-TB treatment in children. It is especially relevant in settings with a high prevalence of HIV or isoniazid resistance. We describe the population pharmacokinetics of ethambutol in children with TB to guide dosing in this population. Read More

Int J Nanomedicine 2022 10;17:1005-1014. Epub 2022 Mar 10.

Department of General Surgery & Guangdong Provincial Key Laboratory of Precision Medicine for Gastrointestinal Tumor, Nanfang Hospital, The First School of Clinical Medicine, Southern Medical University, Guangzhou, Guangdong, 510515, People's Republic of China.

Introduction: Radiotherapy is a conventional treatment for gastrointestinal tumors. However, its therapeutic effect might not be satisfactory because of factors such as radio-resistance of tumor cells and dose reduction applied to avoid damage to normal tissues. We developed a novel combination therapy involving the use of isoniazid (INH) and core-shell magnetic nanospheres (NPs) to enhance the efficacy of radiotherapy. Read More

J Biomol Struct Dyn 2022 Mar 16:1-12. Epub 2022 Mar 16.

Rumsey, Berkshire, England, United Kingdom.

The present study examines cellular targeted drug delivery (CTDD) pattern of two novel Hyaluronic acid (HA) Tuberculosis Drug (TB) conjugates and its efficacy and strong binding affinity towards TB molecular protein targets. Two TB drugs ethambutol (EB) and isoniazid (IN) and their Hyaluronic acid conjugates (HA-EB & HA-IN) were tested for its metabolism, toxicity and excretion prediction through tools they revealed hyaluronic acid conjugate of two TB drugs exhibited good drug profile over their free form of TB drugs. Further these four molecules subjected to molecular docking study with four potential target proteins (3PD8, 4Y0L, 5DZK and 6GAU). Read More

Int J Retina Vitreous 2022 Mar 7;8(1):16. Epub 2022 Mar 7.

Departament of Ophthalmology, Federal University of São Paulo, UNIFESP, São Paulo, SP, Botucatu, 822, Vila Clementino, Brazil.

Background: Tuberculosis (TB) caused by Mycobacterium tuberculosis has a high prevalence in Brazil (Global tuberculosis report 2020. Geneva: World Health Organization; 2020). The ethambutol-induced optic neuropathy damage is partly reversible, making its early diagnosis essential to reduce permanent visual damage. Read More

Braz J Biol 2022 7;84:e254552. Epub 2022 Feb 7.

COMSATS University Islamabad, Department of Pharmacy, Lahore, Pakistan.

Anti-tuberculosis drugs are reported to cause hepatotoxicity, which varies from asymptomatic rise of the hepatic enzymes. Hepatoprotective plants plays important role to protect liver. This study investigated the hepatoprotective potential of the Solanum lycopersicum in rats intoxicated with Isoniazid and Rifampicin (INH+RIF) to induce hepatotoxicity. Read More

Evid Based Complement Alternat Med 2022 22;2022:7148511. Epub 2022 Jan 22.

Centre of Traditional Medicine and Drug Research, Kenya Medical Research Institute, P.O. Box 54840-00200, Nairobi, Kenya.

Background: Welw ex. Oliver (Fabaceae) is one of the plants used by herbalists in the East Africa community to prepare herbal remedies for the management of symptoms of TB. Despite its widespread use, the antimycobacterial activity of this plant was uninvestigated and there was contradicting information regarding its cytotoxicity. Read More

J Appl Toxicol 2022 Jan 31. Epub 2022 Jan 31.

School of Pharmacy, Changzhou University, Changzhou, China.

To investigate the neurotoxicity of pyrazinamide (PZA) to larval zebrafish, the PZA effects were assessed followed by its mechanism being explored. Same as isoniazid (INH), this compound is a first-line anti-tuberculosis drug and is suggested to be a risk that inducing nerve injury with long-term intoxication. Our findings indicated that zebrafish larvae obtained severe nerve damage secondary to constant immersion in various concentrations of PZA (i. Read More

Langmuir 2022 02 31;38(5):1877-1887. Epub 2022 Jan 31.

Amity Center for Nanobiotechnology and Nanomedicine (ACNN), Amity Institute of Biotechnology, Amity University Rajasthan, Jaipur 303002, Rajasthan, India.

The smart design of nanoparticles with varying surfaces may open a new avenue for potential biomedical applications. Consequently, several approaches have been established for controlled synthesis to develop the unique physicochemical properties of nanoparticles. However, many of the synthesis and functionalization methods are chemical-based and might be toxic to limit the full potential of nanoparticles. Read More

Tuberc Respir Dis (Seoul) 2022 Apr 20;85(2):111-121. Epub 2022 Jan 20.

Division of Pharmacology, Department of Biomedical Science, Padjadjaran University/Dr. Hasan Sadikin General Hospital, Bandung, Indonesia.

Multidrug-resistant tuberculosis (MDR-TB) is caused by an organism that is resistant to both rifampicin and isoniazid. Extensively drug-resistant TB, a rare type of MDR-TB, is caused by an organism that is resistant to quinolone and one of group A TB drugs (i.e. Read More

Acta Pharm Sin B 2021 Dec 7;11(12):3857-3868. Epub 2021 Jun 7.

University of Rhode Island, College of Pharmacy, Kingston, RI 02881, USA.

Drug-induced liver injury (DILI) is a leading reason for preclinical safety attrition and post-market drug withdrawals. Drug-induced mitochondrial toxicity has been shown to play an essential role in various forms of DILI, especially in idiosyncratic liver injury. This study examined liver injury reports submitted to the Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS) for drugs associated with hepatotoxicity mitochondrial mechanisms compared with non-mitochondrial mechanisms of toxicity. Read More

Heliyon 2021 Dec 29;7(12):e08482. Epub 2021 Nov 29.

Department of Microbiology, Faculty of Sciences, University of Maiduguri, P.M.B. 1069, Maiduguri, Nigeria.

ATP synthase subunit c (AtpE) is an enzyme that catalyzes the production of ATP from ADP in the presence of sodium or proton gradient from (MTB). This enzyme considered an essential target for drug design and shares the same pathway with the target of Isoniazid. Thus, this enzyme would serve as an alternative target of the Isoniazid. Read More

Front Mol Biosci 2021 23;8:752072. Epub 2021 Nov 23.

School of Public Health, Qingdao University, Qingdao, China.

Isoniazid (INH), an effective first-line drug for tuberculosis treatment, has been reported to be associated with hepatotoxicity for decades, but the underlying mechanisms are poorly understood. -acetyltransferase 2 (NAT2) is a Phase II enzyme that specifically catalyzes the acetylation of INH, and NAT2 expression/activity play pivotal roles in INH metabolism, drug efficacy, and toxicity. In this study, we systematically investigated the regulatory roles of microRNA (miRNA) in expression and INH-induced liver injury via a series of , , and analyses. Read More

Antimicrob Agents Chemother 2022 02 6;66(2):e0168421. Epub 2021 Dec 6.

Department of Pulmonary and Critical Care Medicine, Asan Medical Center, University of Ulsan College of Medicine, Seoul, South Korea.

Delpazolid, an oxazolidinone, has been studied in non-clinical studies of efficacy and toxicity and Phase 1 clinical studies. Delpazolid has activity against Gram-positive bacteria, including Mycobacterium tuberculosis. This study evaluated the bactericidal activity, safety, and pharmacokinetics of delpazolid in patients with pulmonary tuberculosis (TB). Read More

Molecules 2021 Oct 23;26(21). Epub 2021 Oct 23.

Nanobiofar Group, Department of Pharmacology, Pharmacy & Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Campus Vida, 15782 Santiago de Compostela, Galicia, Spain.

Tuberculosis (TB) is an infectious disease that causes a great number of deaths in the world (1.5 million people per year). This disease is currently treated by administering high doses of various oral anti-TB drugs for prolonged periods (up to 2 years). Read More

BMC Pharmacol Toxicol 2021 10 11;22(1):57. Epub 2021 Oct 11.

Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Federal University of Agriculture, P.M.B.2373, Makurdi, Benue State, Nigeria.

Background: Pharmacokinetics (PK) is the process of absorption, distribution, metabolism and elimination (ADME) of drugs. Some drugs undergo zero-order kinetics (ethyl alcohol), first order kinetics (piroxicam) and mixed order kinetics (ascorbic acid). Drugs that undergo Michaelis-Menten metabolism are characterized by either increased or decreased metabolism constant (Km) and maximum velocity (Vmax) of enzyme reaction. Read More

Antimicrob Agents Chemother 2021 11 4;65(12):e0170521. Epub 2021 Oct 4.

University of California, San Franciscogrid.266102.1, Department of Bioengineering and Therapeutic Sciences, San Francisco, California, USA.

Rifapentine has facilitated treatment shortening for latent tuberculosis infection (LTBI) in combination with isoniazid once weekly for 3 months (3HP) or daily for 1 month (1HP). Our objective was to determine the optimal rifapentine dose for a 6-week monotherapy regimen (6wP) and predict clinical efficacy. Rifapentine and isoniazid pharmacokinetics were simulated in mice and humans. Read More

J Microbiol Biotechnol 2021 Dec;31(12):1632-1642

Department of Microbiology and Immunology, School of Medicine, Soonchunhyang University, Cheonan 31151, Republic of Korea.

Tuberculosis is a highly contagious disease caused by . It affects about 10 million people each year and is still one of the leading causes of death worldwide. About 2 to 3 billion people (equivalent to 1 in 3 people in the world) are infected with latent tuberculosis. Read More

Plants (Basel) 2021 Sep 18;10(9). Epub 2021 Sep 18.

Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Abbasia, Cairo 11566, Egypt.

In-depth botanical characterization was performed on Blanco (Lamiaceae) different organs for the first time. The leaves are opposite, hairy and green in color. Flowers possess fragrant aromatic odors and exist in inflorescences of 4-15 cm long corymbose cyme-type. Read More

J Clin Tuberc Other Mycobact Dis 2021 Dec 20;25:100276. Epub 2021 Sep 20.

Faculty of Sciences, Department of Pure and Applied Chemistry, Kaduna State University, Tafawa Balewa Way, Kaduna State, Nigeria.

Tuberculosis (TB) is one of the leading infectious diseases worldwide even with the ravaging COVID-19 pandemic in recent times. This mandated further search and exploration of more possible anti-TB drug candidates against strains. As an extension of our previous work on the homology modeled cytochrome subunit of the bc1 complex (QcrB) of Mycobacterium tuberculosis, an in-silico design was carried out in order to further explore more newly potential anti-TB compounds. Read More

Drug Chem Toxicol 2021 Sep 21:1-7. Epub 2021 Sep 21.

Research Unit n° 17/ES/12, Faculty of Medicine, University of Tunis El Manar, Tunis, Tunisia.

Isoniazid (INH), being the first-line drug used as an anti-tuberculosis drug, is known to be associated with physiological deteriorations including hepatic and neurologic disturbances. This study was aimed at biochemical and behavioral characterization of toxic manifestations of isoniazid treatment in rats. Experimental animals were divided into four groups. Read More

J Appl Toxicol 2022 03 7;42(3):516-528. Epub 2021 Sep 7.

Department of Pharmacy, The Second Xiangya Hospital of Central South University, Changsha, China.

Isoniazid (INH)-induced liver injury is a great challenge for tuberculosis treatment. Existing biomarkers cannot accurately determine the occurrence of this injury in the early stage. Therefore, developing early specific sensitive biomarkers of INH-induced liver injury is urgent. Read More

Colloids Surf B Biointerfaces 2021 Dec 21;208:112054. Epub 2021 Aug 21.

CNR-ISC Sede Sapienza, Piazzale A. Moro 2, I-00185 Rome, Italy; Dipartimento di Fisica, La Sapienza Università di Roma, Piazzale A. Moro 2, I-00185 Rome, Italy. Electronic address:

Isoniazid (INH) is one of the primary drugs used in tuberculosis treatment and its encapsulation in liposomal vesicles can both improve its therapeutic index and minimize toxicity. Here we consider mixtures of hydrogenated soy phosphatidylcholine-phosphatidylglycerol (HSPC-DPPG) to get novel biocompatible liposomes for INH delivery. We determined INH encapsulation efficiency by coupling for the first time UV and Laser Transmission Spectroscopy and we showed that HSPC-DPPG liposomes can load more INH than expected from simple geometrical arguments, thus suggesting the presence of drug-lipid association. Read More

In Vivo 2021 Sep-Oct;35(5):2675-2685

Department of Medical Microbiology, Faculty of Medicine, Universiti Malaya, Kuala Lumpur, Malaysia;

Background/aim: Isoniazid is an antibiotic used for the treatment of tuberculosis. Previously, we found that the isoniazid derivative (E)-N'-(2,3,4-trihydroxybenzylidene) isonicotinohydrazide (ITHB4) could be developed as novel antimycobacterial agent by lead optimization. We further explored the ability of this compound compared to zerumbone in inhibiting the growth of MCF-7 breast cancer cells. Read More

Methods Mol Biol 2021 ;2342:781-808

Translational Medicine, Novartis Institutes for BioMedical Research, Inc., Cambridge, MA, USA.

Major routes of metabolism for marketed drugs are predominately driven by enzyme families such as cytochromes P450 and UDP-glucuronosyltransferases. Less studied conjugative enzymes, like N-acetyltransferases (NATs), are commonly associated with detoxification pathways. However, in the clinic, the high occurrence of NAT polymorphism that leads to slow and fast acetylator phenotypes in patient populations has been linked to toxicity for a multitude of drugs. Read More

Neural Plast 2021 26;2021:5566890. Epub 2021 Jun 26.

School of Pharmacy and Pharmaceutical Sciences, College of Health and Allied Sciences, University of Cape Coast, Cape Coast, Ghana.

A number of currently used drugs have been obtained from medicinal plants which are a major source of drugs. These drugs are either used in their pure form or modified to a semisynthetic drug. Drug discovery through natural product research has been fruitful over the years. Read More

Onderstepoort J Vet Res 2021 Jun 11;88(1):e1-e8. Epub 2021 Jun 11.

National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Obihiro.

Toxoplasma gondii, an obligate intracellular parasite, is the aetiological agent of toxoplasmosis, a disease that affects approximately 25% - 30% of the world's population. At present, no safe and effective vaccine exists for the prevention of toxoplasmosis. Current treatment options for toxoplasmosis are active only against tachyzoites and may also cause bone marrow toxicity. Read More

Environ Sci Pollut Res Int 2021 Nov 24;28(43):60833-60841. Epub 2021 Jun 24.

National Institute of Oceanography & Fisheries, Alexandria, Egypt.

In more than two-thirds of the diabetic foot ulcer (DFUs) cases, lower limb amputation of foot ulceration is caused by the infection. The role of transition a metal complex as a therapeutic compound is becoming increasingly important. In vitro, four groups of antibiotics and one sulfa drug were tested against diabetic foot resistant bacteria. Read More

J Clin Pharmacol 2021 12 26;61(12):1567-1578. Epub 2021 Jul 26.

Center for Personalized Precision Medicine of Tuberculosis (cPMTb), Inje University College of Medicine, Busan, Republic of Korea.

The wide variability of isoniazid (INH) pharmacokinetics is mainly attributed to the trimodal N-acetyltransferase 2 (NAT2) acetylator phenotype, that is, rapid, intermediate, and slow. Consequently, a uniform INH dose in current clinical practice may lead to treatment failure and emergence of drug resistance. There is a lack of studies on specific doses of INH for different NAT2 acetylator phenotypes among tuberculosis (TB) patients. Read More