MyMedR

Displaying all 5 publications

Abstract:

Sort:

Triphenyltin(IV) benzoates with diazenyl/imino scaffold exhibiting remarkable apoptosis mediated by reactive oxygen species

Basu Baul TS, Dutta D, Duthie A, Prasad R, Rana NK, Koch B, et al.

J Inorg Biochem, 2017 08;173:79-92.
PMID: 28505480 DOI: 10.1016/j.jinorgbio.2017.04.020

The cytotoxic potency of a series of triphenyltin(IV) compounds of general composition [Ph3Sn(Ln)] (1-6) has been probed in vitro employing MDA-MB-231 (human breast cancer) and HeLa (human cervical cancer) cell lines, where Ln=L1-3; isomeric 2/3/4-{(E)-2-[4-(dimethylamino)phenyl]diazenyl}benzoates and L4-6are their corresponding isoelectronic imino analogues 2/3/4-[(E)-{[4-(dimethylamino)phenyl]methylidene}amino]benzoates. Compounds 1-6 have been characterized by elemental analysis and their spectroscopic properties were studied using IR and NMR (1H,13C,119Sn) techniques. The molecular structures of a pro-ligand 2-[(E)-{[4-(dimethylamino)phenyl]methylidene}amino]benzoic acid (HL4) and two representative molecules, Ph3Sn(L2) 2 and Ph3Sn(L5) 5, have been determined by X-ray crystallography. Structural analyses of 2 and 5 revealed distorted tetrahedral geometries within C3O donor sets owing to monodentate modes of coordination of the respective carboxylate ligands, close intramolecular Sn…O(carbonyl) interactions notwithstanding. Cytotoxic studies in vitro in MDA-MB-231 and HeLa cell lines revealed high activity, in sub-micromolar range, for all investigated compounds. Among these, 1 and 3 exhibited potent cytotoxicity most effectively towards MDA-MB-231 cells with a IC50value of 1.19 and 1.44μM, respectively, whereas 5 showed remarkable activity towards HeLa cells with a IC50value of 0.88μM, yet the series of compounds had minimal cytotoxic effect on normal HEK 293 (human embryonic kidney) cell line. The underlying investigation suggested that the compounds exert potent antitumor effect by elevating intracellular reactive oxygen species generation and cause delay in cell cycle by inhibiting cells at G2/M phase. The results presented herein suggest further development of this class of triphenyltin(IV) compounds-based drugs as potential anti-cancer therapies should be pursued.
Polyvinylpyrrolidone oral films of enrofloxacin: film characterization and drug release

Kumar GP, Phani AR, Prasad RG, Sanganal JS, Manali N, Gupta R, et al.

Int J Pharm, 2014 Aug 25;471(1-2):146-52.
PMID: 24858388 DOI: 10.1016/j.ijpharm.2014.05.033

Enrofloxacin is a fluoroquinolone derivative used for treating urinary tract, respiratory and skin infections in animals. However, low solubility and low bioavailability prevented it from using on humans. Polyvinylpyrrolidone (PVP) is an inert, non toxic polymer with excellent hydrophilic properties, besides it can enhance bioavailability by forming drug polymer conjugates. With the aim of increasing solubility and bioavailability, enrofloxacin thin films were prepared using PVP as a polymer matrix. The obtained oral thin films exhibited excellent uniformity and mechanical properties. Swelling properties of the oral thin films revealed that the water uptake was enhanced by 21%. The surface pH has been found to be 6.8±0.1 indicating that these films will not cause any irritation to oral mucosa. FTIR data of the oral thin films indicated physical interaction between drug and polymer. SEM analysis revealed uniform distribution of drug in polymer matrix. In vitro drug release profiles showed enhanced release profiles (which are also pH dependant) for thin films compared to pure drug. Antibacterial activity was found to be dose dependent and maximum susceptibility was found on Klebsiella pneumonia making this preparation more suitable for respiratory infections.
Clinical Spectrum of Esophageal Motility Disorders in Nonobstructive Dysphagia: A Multicenter, Multiethnic Study

Lim JX, Prasad R, Izham N, Chan WL, Ramasami N, Wong WJ, et al.

J Gastroenterol Hepatol, 2026 Nov;41(11):3405-3412.
PMID: 42710884 DOI: 10.1111/jgh.70713

BACKGROUND AND AIMS: Nonobstructive dysphagia (NOD) is a frequently encountered condition. The spectrum of underlying esophageal motility disorders remains incompletely characterized in Asian populations. We aimed to define the manometric spectrum of NOD, identify predictors of achalasia, and evaluate the diagnostic value of provocative testing.
METHODS: This retrospective multicenter study included adults who underwent high-resolution manometry (HRM) for NOD at two tertiary hospitals in Malaysia from 2014 to 2023. Diagnoses were classified according to Chicago Classification v3.0. Clinical predictors of achalasia were evaluated. The discriminatory performance of rapid drink challenge (RDC)-integrated relaxation pressure (IRP) in differentiating achalasia from non-achalasia was explored.
RESULTS: Among 230 patients (mean age 53.3; 47.0% male), achalasia was identified in 23.9%, esophagogastric junction outflow obstruction (EGJOO) in 17.3%, and ineffective esophageal motility in 24.8%. Weight loss (adjusted OR 2.99, 95% CI 1.25-7.15, p = 0.014), absence of dyspepsia (adjusted OR 0.09, 95% CI 0.02-0.45, p = 0.004), and presence of nausea/vomiting (adjusted OR 3.35, 95% CI 1.34-8.40, p = 0.010) independently predicted achalasia. RDC-IRP demonstrated strong discrimination between achalasia and non-achalasia (AUC 0.894, 95% CI 0.794-0.993, p
Anti-cancerous efficacy and pharmacokinetics of 6-mercaptopurine loaded chitosan nanoparticles

Kumar GP, Sanganal JS, Phani AR, Manohara C, Tripathi SM, Raghavendra HL, et al.

Pharmacol Res, 2015 Oct;100:47-57.
PMID: 26232590 DOI: 10.1016/j.phrs.2015.07.025

6-Mercaptopurine is a cytotoxic and immunosuppressant drug. The use of this drug is limited due to its poor bioavailability and short plasma half-life. In order to nullify these drawbacks, 6-mercaptopurine-chitosan nanoparticles (6-MP-CNPs) were prepared and evaluated to study the influence of preparation conditions on the physicochemical properties by using DLS, SEM, XRD and FTIR. The in vitro drug release profile at pH 4.8 and 7.4 revealed sustained release patterns for a period of 2 days. The nanoformulations showed enhanced in vitro anti-cancer activities (MTT assay, apoptosis assay, cell cycle arrest and ROS indices) on HT-1080 and MCF-7 cells. In vivo pharmacokinetics profiles of 6-MP-CNPs showed improved bioavailability. Thus, the results of the present study revealed that, the prepared 6-MP-CNPs have a significant role in increasing anti-cancer efficacy, bioavailability and in vivo pharmacokinetics profiles.
Fulltext Predicting attitudinal and behavioral responses to COVID-19 pandemic using machine learning

Pavlović T, Azevedo F, De K, Riaño-Moreno JC, Maglić M, Gkinopoulos T, et al.

PNAS Nexus, 2022 Jul;1(3):pgac093.
PMID: 35990802 DOI: 10.1093/pnasnexus/pgac093

At the beginning of 2020, COVID-19 became a global problem. Despite all the efforts to emphasize the relevance of preventive measures, not everyone adhered to them. Thus, learning more about the characteristics determining attitudinal and behavioral responses to the pandemic is crucial to improving future interventions. In this study, we applied machine learning on the multinational data collected by the International Collaboration on the Social and Moral Psychology of COVID-19 (N = 51,404) to test the predictive efficacy of constructs from social, moral, cognitive, and personality psychology, as well as socio-demographic factors, in the attitudinal and behavioral responses to the pandemic. The results point to several valuable insights. Internalized moral identity provided the most consistent predictive contribution-individuals perceiving moral traits as central to their self-concept reported higher adherence to preventive measures. Similar results were found for morality as cooperation, symbolized moral identity, self-control, open-mindedness, and collective narcissism, while the inverse relationship was evident for the endorsement of conspiracy theories. However, we also found a non-neglible variability in the explained variance and predictive contributions with respect to macro-level factors such as the pandemic stage or cultural region. Overall, the results underscore the importance of morality-related and contextual factors in understanding adherence to public health recommendations during the pandemic.