IN VITRO STUDY OF URSOLIC ACID COMBINATION FIRST-LINE ANTITUBERCULOSIS DRUGS AGAINST DRUG-SENSITIVE AND  DRUG-RESISTANT STRAINS OF Mycobacterium tuberculosis

Pitaloka, Dian Ayu Eka; Sukandar, Elin Yulinah

doi:10.22159/ajpcr.2017.v10i4.16582

Cited by 12 publications

(15 citation statements)

References 13 publications

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“…It reported having a wide range of activities including anti mycobacteria and can inhibit the growth of MTB in both sensitive and resistant strains. It also is shown that UA has a synergistic effect when it combined with INH, rifampicin, ethambutol, or pyrazinamide [13]. In this research, UA acts as a ligand and docked on the site of drug action of the selected receptor of MTB which is responsible for the pharmaceutical effect.…”

Section: ■ Results and Discussionmentioning

confidence: 78%

“…In vitro study of UA found that it has activity as anti-TB with Minimum Inhibitory Concentration (MIC) in sensitive and resistant strains of MTB. UA has also displayed a synergistic interaction when combined with isoniazid (INH), rifampicin, ethambutol, and streptomycin [13]. The in vivo study was also found that UA showed a significant reduction of activity in rats induced by MTB H37Rv sensitive strain and MDR strains [14].…”

Section: ■ Introductionmentioning

confidence: 94%

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Molecular Docking, Dynamics Simulation, and Scanning Electron Microscopy (SEM) Examination of Clinically Isolated <i>Mycobacterium tuberculosis</i> by Ursolic Acid: A Pentacyclic Triterpenes

et al. 2019

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The purpose of this study was to analyze the inhibitory action of ursolic acid (UA) as an antitubercular agent by computational docking studies and molecular dynamics simulations. The effect of UA on the cell wall of Mycobacterium tuberculosis (MTB) was evaluated by using Scanning Electron Microscopy (SEM). UA was used as a ligand for molecular interaction and investigate its binding activities to a group of proteins involved in the growth of MTB and the biosynthesis of the cell wall. Computational docking analysis was performed by using autodock 4.2.6 based on scoring functions. UA binding was confirmed by 30 ns molecular dynamics simulation using gromacs 5.1.1. H37Rv sensitive strain and isoniazid-resistant strain were used in the SEM study. UA showed to have the optimum binding affinity to inhA (Two-trans-enoyl-ACP reductase enzyme involved in elongation of fatty acid) with the binding energy of -9.2 kcal/mol. The dynamic simulation showed that the UA-inhA complex relatively stable and found to establish hydrogen bond with Thr196 and Ile194. SEM analysis confirms that UA treatment in both sensitive strain and resistant strain affected the morphology cell wall of MTB. This result indicated that UA could be one of the potential ligands for the development of new antituberculosis drugs.

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Section: ■ Results and Discussionmentioning

confidence: 78%

Section: ■ Introductionmentioning

confidence: 94%

Molecular Docking, Dynamics Simulation, and Scanning Electron Microscopy (SEM) Examination of Clinically Isolated <i>Mycobacterium tuberculosis</i> by Ursolic Acid: A Pentacyclic Triterpenes

et al. 2019

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“…In 2017, 87% of new TB cases occurred in 30 countries and >95% cases of TB-infected individuals in developing countries such as India, China, Indonesia, the Philippines, Pakistan, Nigeria, Bangladesh, and South Africa [2]. Indonesia, with 842,000 cases, is the third country with the highest number of cases of TB worldwide after India and China [2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

“…The compliance with medication intake in patients infected with TB and with other diseases is challenging, leading to multidrug-or rifampicin-resistant (RR) TB (Multidrug resistance [MDR]/RR-TB) [4,5]. Some reasons for this include failure in dose use, indiscipline, and drug interaction with other medicines [6].…”

Section: Introductionmentioning

confidence: 99%

Identification of Drug-Related Problems in Adults With Tuberculosis at the Tebet Subdistrict Health Center From July to December 2018

Puspitasari¹,

Yunaz

Nadhilah³

2020

Int J App Pharm

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Objective: Tuberculosis (TB) is a highly prevalent infectious disease caused by Mycobacterium tuberculosis. The recommended TB treatment is acombination of various antibiotics in the form of a fixed-dose combination tablet or kombipak; however, this increases the prevalence of drug-relatedproblems. Therefore, this study aimed to identify drug-related problems of patients receiving TB therapy at the Tebet Subdistrict Health Center fromJuly 2018 to December 2018.Methods: The study was designed as a cross-sectional study using the retrospective data retrieval method from prescriptions of patients withTB from July 2018 to December 2018. The classification system prepared by Cipolle, Strand, and Morley was used for the classification of drugrelatedproblems; this system includes unnecessary drug therapy, required additional drug therapy, ineffective drug, dosage error, and druginteraction.Results: The percentage of unnecessary drug therapy, required additional drug therapy, ineffective drug, dosage error, and drug interaction was2.85%, 6.89%, 1.54%, 12.46%, and 66.18%, respectively, with the occurrence of drug-related problems being the highest.Conclusion: The administration of anti-TB drugs can potentially cause drug-related problems. Therefore, the assessment needs to be optimizedbefore the administration of medications to patients and medications should be prescribed and monitored regularly to achieve rational drug use

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“…Angiogenesis was highly needed by tumor cells to spread to another organ or metastatic [12]. Ursolic acid was able to inhibit the regulation of pro-inflammatory cytokines expression through the inhibition of NF-κB activation and antitumor [13]. In the other hand, TCa contains diterpenoid compounds that exhibit cytotoxic activities in human prostate cancer [14].…”

Section: Introductionmentioning

confidence: 99%

Combination of Hedyotis Corymbosa L. And Tinospora Crispa Ethanolic Extract Increase Cisplatin Cytotoxicity on T47d Breast Cancer Cells

Rollando

2018

Asian J Pharm Clin Res

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Objective: Ursolic acid was a compound found in Hedyotis corymbosa L., (HCoL) while berberine found in Tinospora crispa (TCa) which are proven to have cytotoxic effect to cancer cells. This research aims to review the effect of cisplatin, ethanolic extract of HCoL and TCa to the sensitivity increase on breast cancer cells, which will be confirmed through apoptosis induction and cell cycle modulation.Methods: The cytotoxic effect was tested using 3-(4,5-dimethylthiazol-2-il)-2,5-diphenyltetrazolium bromide assay on T47D cell using the IC50 parameter. The combination was tested by determining their combination index (CI) and cell viability. The combination effect of apoptosis induction and cell cycle modulation was observed using flow cytometry method.Results: The cytotoxic test result of the combination shows CI value of below 1 at the concentration of HCoL ethanolic extract as much as 1 μg/mL, TCa ethanolic extract as much as 6 μg/mL, and cisplatin as much as 2,5 μM. The combination of HCoL ethanolic extract, TCa ethanolic extract, and cisplatin results in phase S cell accumulation (29.98%) on breast cancer cell T47D and was able to induce apoptosis.Conclusion: The result proves that ethanolic extract of HCoL and TCa can be developed as a cochemotherapeutic agent with cisplatin to increase the effectivity of breast cancer treatment.

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IN VITRO STUDY OF URSOLIC ACID COMBINATION FIRST-LINE ANTITUBERCULOSIS DRUGS AGAINST DRUG-SENSITIVE AND DRUG-RESISTANT STRAINS OF Mycobacterium tuberculosis

Cited by 12 publications

References 13 publications

Molecular Docking, Dynamics Simulation, and Scanning Electron Microscopy (SEM) Examination of Clinically Isolated <i>Mycobacterium tuberculosis</i> by Ursolic Acid: A Pentacyclic Triterpenes

Molecular Docking, Dynamics Simulation, and Scanning Electron Microscopy (SEM) Examination of Clinically Isolated <i>Mycobacterium tuberculosis</i> by Ursolic Acid: A Pentacyclic Triterpenes

Identification of Drug-Related Problems in Adults With Tuberculosis at the Tebet Subdistrict Health Center From July to December 2018

Combination of Hedyotis Corymbosa L. And Tinospora Crispa Ethanolic Extract Increase Cisplatin Cytotoxicity on T47d Breast Cancer Cells

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