Factors Influencing Rifampicin Autoinduction in Adult Pulmonary Tuberculosis Patients

Saranya,; Parthasarathy,; Hariprasad, B; H, Shobha Rani

doi:10.5958/0974-360x.2016.00233.x

Cited by 8 publications

(2 citation statements)

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“…However, this research still needs further confirmation by using molecular dynamics simulation, in vitro and in vivo test 42,43 . Moreover, in the wet laboratory experiment, designing drug delivery system for rifampicin with nanoparticles should be considered as well 10,44,46 . Considering herbal medicine for leprosy could be explored as well 47,48 .…”

Section: Resultsmentioning

confidence: 99%

“…Rifampicin has been standardized and formulized for leprosy, thus could be combined with another treatments [6][7][8][9] . Rifampicin also utilized in tuberculosis and hepatic damage patients as well, so this is considered semi-broad spectrum antibiotic 10,11 . The number of leprosy patients tested for resistance globally is too small to allow for accurate estimates of drug resistance.…”

Section: Introductionmentioning

confidence: 99%

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Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Maladan¹,

Krismawati²,

Wahyuni³

et al. 2021

RJPT

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Leprosy persists to be a health problem in Indonesia, especially in the provinces of North Maluku, West Papua and Papua. Early diagnosis and complete treatment with multidrug therapy (MDT) remain the key strategy for reducing the disease burden. One of the major components of MDT is rifampicin which in certain cases in several countries, M. leprae resistance to this drug issue has been reported albeit only a few. This research aimed to detect and analyze polymorphism in M. leprae rpoB gene that was isolated from leprosy patients in three provinces: North Maluku Province, West Papua Province and Papua Province, Indonesia. The identification of mutations in the M. leprae rpoB gene was carried out by aligning the results of DNA sequencing with the reference strain. The 3D structure of rpoB was derived using the Swiss Model. The T450A, S456L, and H451Y variants of RNA Polymerase B subunits were constructed using FoldX based on the wild-type structure. The structures were repaired, and protein stability was evaluated using foldX under the Yasara viewer. The QC of the rpoB M. leprae homology models was conducted with Ramachandran Plot modeling using PROCHECK. The difference in binding affinity between native protein and T450A, S456L, and H45I variants were analyzed using molecular docking. rpoB gene of M. leprae contains a mutation found in nucleotide of 1348 bp. The mutation triggered the conversion of the amino acid Threonine to Alanine in the amino acid to 450 rpoB subunit B. The structure of 3D RNA Polymerase Subunit B was constructed using rpoB Mycobacterium tuberculosis with PDB code 5UH5 as template. According to Ramachandran Plot, the percentage of residues in the most favored regions are 91.9%, and there was no significant number of residues in the disallowed regions. The results of molecular docking showed that the T450A variant had the same binding affinity with the native protein which was -8.9 kcal. Binding affinity on the S456L and H451Y variants increased by -7.3 kcal and -8.2 kcal, respectively. According to Molecular Docking analysis, T450A variant did not affect the energy binding between RNA polymerase and rifampicin.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Maladan¹,

Krismawati²,

Wahyuni³

et al. 2021

RJPT

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N-(Chlorobenzyl) Formamide as an Antituberculosis Agent from Multicomponent Reaction Synthesis

Permatasari

Ritmaleni

Nuryastuti

2021

RJPT

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Tuberculosis (TB) is an infectious disease caused by M. tuberculosis. A new series of four benzylformamide with chloro substitution were synthesized by multicomponent reaction method and screened for antituberculosis activity against Mycobacterium tuberculosis H37Rv strain. This study was based on amidoalkylation reaction of aromatic-aldehyde, formamide and formic acid at 150oC to give a good yield of benzylformamide. Target compound were isolated, purificated, identified and characterized by GC-MS, FTIR, 1H-NMR, and 13C-NMR then the antituberculosis activity was examined by Microplate Alamar Blue Assay (MABA) and Middlebrook 7H9-7H11 medium in concentration series of 1000 – 1,954 μg/mL, and isoniazid as a positive control. Among the three derivative, N-(2,4-dichlorobenzyl) formamide has the most potential antituberculosis activity up to 500.0 L/mL.

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Revisiting CYP2C9-Mediated drug-drug Interactions: A Review

Mutalib

Rafi

Latip

2021

RJPT

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Drug-drug interactions (DDI) are the most common cases that occur in our healthcare in which are very alarming as it may lead to severe complications. Consumption of natural products concomitantly with conventional drugs or treatment using polypharmacy have become the norm that promoting the potential of pharmacokinetic or pharmacodynamic drug interactions as the combination may mimic, increase or reduce the effects of the drug or the herb which could result in clinically significant interactions. CYP2C9 is the second major isoform from CYP450 family of enzyme, which responsible in phase 1 metabolism of 15-20% clinical drugs. Up to date, many substrates of CYP2C9 have been discovered and these discoveries may open more doors for potential drug-drug interactions in patients. Many studies have been done to evaluate the effect of drugs on the activity of CYP2C9 and how it influenced the effectiveness of therapy in patients. Various data regarding CYP2C9 related DDI from in vitro, in vivo and clinical studies were critically discussed in this review to provide insights on how these drugs and natural products may exhibit drug interactions clinically. This review could be beneficial reference material for health practitioners and researchers.

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Factors Influencing Rifampicin Autoinduction in Adult Pulmonary Tuberculosis Patients

Cited by 8 publications

References 0 publications

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

N-(Chlorobenzyl) Formamide as an Antituberculosis Agent from Multicomponent Reaction Synthesis

Revisiting CYP2C9-Mediated drug-drug Interactions: A Review

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