Browsing by Author "Kapil Dev"

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A proposed methodology for in vitro evaluation of bitterness in drug solutions and in vitro drug release samples
(Springer New York LLC, 2014) Kapil Dev; Vandana Kharb; Anupama Singh; Vikas Anand Saharan; Hemant Jadhav; Suresh Purohit
Purpose: Ethical and safety concerns, paediatric taste panels and predictivity in early drug development for strategic decisions are some of the reasons for seeking in vitro methods of bitterness evaluation for drugs and drug products. In this study, taste panel studies and in vitro drug release studies have been performed, correlated to each other and proposed as an analytical tool for evaluation of bitterness. Methods: Bitterness threshold and bitterness scores for different solutions of ondansetron hydrochloride (ONS) were estimated by taste panel studies. In vitro drug release studies on taste-masked drug product in pharmacopoeial apparatus and an in-house-developed apparatus were performed and correlated to drug release studies in oral cavity. Results: Concentration of 22 μg/ml and below was perceived bitterless by all the volunteers of taste panel. A second-order polynomial equation (y = 0.6206x 2 - 0.2011x - 0.7796; correlation coefficient R 2 = 0.991) was derived as a relationship between bitterness score and log ONS concentration. Drug release in in-house-assembled apparatus and oral cavity were not statistically different (α = 0.05) at both 60 and 120 s. Conclusions: Bitterness threshold and bitterness scores are helpful in evaluation of bitterness in drug solutions and samples obtained from drug release studies. © 2014 Springer Science+Business Media.
Anti-ulcer constituents of Annona squamosa twigs
(2011) Dinesh K. Yadav; Neetu Singh; Kapil Dev; Rolee Sharma; Mahendra Sahai; Gautam Palit; Rakesh Maurya
Phytochemical investigation of Annona squamosa twigs, resulted in isolation and identification of twelve known (1-12) compounds among them one 1-(4-β-D-glucopyranosyloxyphenyl)-2-(β-D-glucopyranosyloxy)-ethane (11) is synthetically known but first time isolated from natural sources. Their structures were elucidated using 1D and 2D NMR spectroscopic analysis. The isolated compounds (2-8, 11) were evaluated for H+ K +-ATPase activity. Three of these compounds (+)-O-methylarmepavine (2), N-methylcorydaldine (3), isocorydine (6) showed promising anti-secretory activity. Activity of these compounds, comparable to the standard drug omeprazole is novel to our finding. Moreover, there is no information accessible regarding the pharmacological effect of A. squamosa on the gastrointestinal system. This study is the first of its kind to show the significant anti-ulcer effect of A. squamosa. The present study aimed to evaluate the gastroprotective effect of A. squamosa (AS) and to identify its active constituents. Anti-ulcer activity was evaluated against cold restraint (CRU), pyloric ligation (PL), aspirin (ASP), alcohol (AL) induced gastric ulcer and histamine (HA) induced duodenal ulcer model and further confirmed through in vitro assay of H + K+-ATPase activity and plasma gastrin level. AS and its chloroform and hexane fraction attenuated ulcer formation in CRU, PL, HA model and displayed anti-secretory activity in vivo through reduced free, total acidity and pepsin in PL, confirmed by in vitro inhibition of H+ K+-ATPase activity with corresponding decrease in plasma gastrin level. Cytoprotection of AS was apparent with protection in AL, ASP models and enhanced mucin level in PL. © 2011 Elsevier B.V. All rights reserved.
Bitterness Score and its Correlation to Drug Concentration: An Approach for Estimating Bitterness Suppression in a Marketed Product of Ofloxacin
(Taylor and Francis Ltd., 2014) Vikas Anand Saharan; Kapil Dev; Vandana Kharb; Anupama Singh; Hemant Jadhav; Suresh Purohit
Abstract: In vitro approaches for assessing taste characteristics of taste masked drug and drug products are useful in reducing reliance on human panel tests. In this study, taste panel studies were used to determine bitterness threshold and bitterness score of various solutions of ofloxacin followed by correlation and the application of this approach in estimating bitterness suppression. Bitterness scores for different solutions of ofloxacin were estimated by trained human volunteers of a taste panel. Bitterness scores were correlated to ofloxacin concentration followed by determination of bitterness scores for various dissolution samples obtained from in vitro drug release study of ofloxacin taste masked drug product. Concentration of 80 µg/ml and below was perceived bitterless by all the volunteers of taste panel. A third order polynomial equation (y=13.51x3-91.08x2+206.7x-156.6; R2 = 0.973) was derived as a relationship between bitterness score (y) and log ofloxacin concentration (x). Marketed taste masked product achieved concentrations below bitterness threshold in in vitro drug release studies performed in pharmacopoeial apparatus at initial time points (0-5 min). Bitterness threshold and bitterness scores are helpful in estimating bitterness of ofloxacin solutions provided suitable correlation has been found between them. The suggested approach, which is applicable to any bitter or objectionable tasting drug, has potential to be used as analytical tool in formulation development and quality control. © 2014, Har Krishan Bhalla & Sons.
Developmental validation of the Ingenomics™ AutoProfiler STR system: a 6-dye STR multiplex kit for forensic DNA applications
(Springer, 2025) Shivkant Sharma; Rajendra V.E. Chilukuri; Rhea Shetkar; Ramkishan K. Kumawat; Vivek Sahajpal; Shivani Dixit; Braja Kishore Mohapatra; Dhirendra Singh Yadav; Kapil Dev; Rubina Mohammed; Umema Ahmad; Krishna Mani Yadav; Anita Pundir; Jaison Jeevan Sequeira; G. Chaubey
The Ingenomics™ AutoProfiler system utilises a 6-dye, multiplex genotyping technology that is optimised for the simultaneous amplification of 20 Combined DNA Index System (CODIS) short tandem repeat (STR) markers, along with D6S1043, Penta D, Penta E, DYS391, SE33, and two Y-Indels (Rs2032678, Rs771783753), as well as the Amelogenin loci. This kit includes specialised internal quality control (IQC) markers, both small and large, to evaluate the quality parameters for each sample. Designed for a diverse range of applications—such as forensic DNA casework, identity establishment, database management, kinship testing, scientific research, and other analyses related to human genetic identification—this multiplex system is particularly effective for analysing low-copy number (LCN) DNA from severely compromised forensic samples, as it also evaluates two SNP markers. The multidimensional validation study aligned with the guidelines set forth by the Scientific Working Group on DNA Analysis Methods (SWGDAM) examined crucial parameters, including PCR conditions, reproducibility, analytical threshold calculation, sensitivity, species specificity, stability, mixture analysis, casework sample analysis, direct amplification, and concordance. The optimal DNA concentration range was between 60 and 500 pg/µL, with an analytical threshold established at 50 relative fluorescence units (RFUs). Overall, the findings indicate that the Ingenomics™ AutoProfiler kit is a reliable, robust, and suitable assay for human identification in casework DNA analysis and database construction. © The Author(s) under exclusive licence to Archana Sharma Foundation of Calcutta 2025.
Formulation, evaluation and 32 full factorial design-based optimization of Ondansetron hydrochloride incorporated taste masked microspheres
(Informa Healthcare, 2014) Vandana Kharb; Vikas Anand Saharan; Kapil Dev; Hemant Jadhav; Suresh Purohit
Context: Masking the bitter taste of Ondansetron hydrochloride (ONS) may improve palatability, acceptance and compliance of ONS products. Objective: ONS-loaded, taste-masked microspheres were prepared with a polycationic pHsensitive polymer and 32 full factorial design (FFD) was applied to optimize microsphere batches. Materials and methods: Solvent evaporation, in acetone-methanol/liquid paraffin system, was used to prepare taste-masked ONS microspheres. The effect of varying drug/polymer (D/P) ratios on microspheres characteristics were studied by 32 FFD. Desirability function was used to search the optimum formulation. Microspheres were evaluated by FTIR, XRD and DSC to examine interaction and effect of microencapsulation process. In vitro taste assessment approach based on bitterness threshold and drug release was used to assess bitterness scores. Results: Prepared ONS microspheres were spherical and surface was wrinkled. ONS was molecularly dispersed in microspheres without any incompatibility with EE100. In hydrochloric acid buffer pH 1.2, ONS released completely from microsphere in just 10 min. Contrary to this, ONS release at initial 5 min from taste-masked microspheres was less than the bitterness threshold. Conclusion: Full factorial design and in vitro taste assessment approach, coupled together, was successfully applied to develop and optimize batches of ONS incorporated taste-masked microspheres. © 2014 Informa Healthcare USA, Inc.
Molecular characterization of 23 Y chromosomal STR markers in the Gurjar population of National Capital Region (NCR), India
(Springer Science and Business Media Deutschland GmbH, 2022) Kapil Dev; Lav Kesharwani; Pushpesh Kushwaha; Akshay Kumar; Kunwar Veer Vikram Srivastav; Varsha Bhasney; R.K. Kumawat; Shivani Dixit; Ankit Srivastava; Gyaneshwer Chaubey; Pankaj Shrivastava
In the present study, DNA samples of 202 unrelated male individuals of Gurjar population were evaluated for the molecular diversity at 23 Y chromosomal Y-STR markers. Out of selected individuals, results showed 143 unique haplotypes. Highest degree of gene diversity (GD), polymorphic information content (PIC), and power of discrimination (PD) was observed as 0.7941, 0.7590, and 0.7902, respectively, for the locus DYS385a/b. Haplotype diversity (HD), gene diversity (GD), polymorphic information content (PIC), and power of discrimination (PD) was found to be 0.7079, 0.999999999989, 0.9999999996, and 0.999999999986, respectively, for the studied 23 Y-STR markers. Allele 11 of locus DYS392 was found to be the most frequent allele with the frequency of 0.762. In inter-population relationship, studied population showed genetic relatedness with the population of Jammu and Kashmir, India, and Ladakh, India. The haplotype data of the present study will not only enrich the existing Indian Y-STR data but will also be useful for forensic DNA application. © 2021, The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.
New lignan glycosides from Cissus quadrangularis stems
(Taylor and Francis Ltd., 2019) Padam Kumar; Kapil Dev; Khushbu Sharma; Mahendra Sahai; Rakesh Maurya
Phytochemical investigation of Cissus quadrangularis stems led to the isolation of one new phenolic glycoside (1) and two new lignan glycosides (7 & 8) along with twelve known compounds (2–6 & 9–15). Their chemical structures were determined on the basis of extensive spectroscopic analysis using 1D, 2D NMR, and mass spectrometric analysis. Among the known compounds, 4–6, 9 and 12 were isolated for the first time from the genus Cissus whereas compounds 10, 11 and 13 for the first time from this plant. © 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.
Revealing genomic history and forensic features of Gurjars from western Uttar Pradesh and National Capital Region Delhi using 23 autosomal STRs
(Elsevier B.V., 2021) Kapil Dev; Lav Kesharwani; Pushpesh Kushwaha; Akshay Kumar; Kunwar Veer Vikram Srivastav; Manisha Rana; Shivani Dixit; R.K. Kumawat; Ankit Srivastava; Munish Mishra; Gyaneshwer Chaubey; Pankaj Shrivastava
Here we report the genomic history of Gurjars and framed the useful set of autosomal STRs for Gujjar population. We designed this study with a total number of 215 Gurjars from district Saharanpur (previously known as Gujarat due to presence of many Gujjar zamindars), Moradabad, Bulandshahr, Ghaziabad, Meerut, Noida and NCR Delhi. Locus SE33 was found the most polymorphic and discriminating marker for Gujjar population while locus TPOX is the least. Ancestral information of Gurjars was revealed by comparing the Gujjar's population data with 19 neighbouring populations. In Neighbor Joining (NJ) tree Gurjars were found closer to Gujjars of Jammu region, population of Rajasthan and Uttarkhand, due to the same stock of gene pool. © 2021 Elsevier B.V.
Screening Withania somnifera as biostimulant for crop plants and chemical profiling of its active fractions
(Elsevier B.V., 2025) Sarika Sharma; Arti Shukla; Kapil Dev; Shachi Singh
Studies have highlighted that Withania somnifera contain endogenous molecules, with varying biological activities. In light of this, the current experiment aimed the plant growth-promoting potential of Withania somnifera leaf extract (WsLE) through seed priming. Twenty crop plants were tested to assess the bio-stimulatory effects of WsLE. The selected morphological features for evaluation included germination percentage, plant length and fresh biomass while the biochemical parameters assessed were total polyphenolic, protein, and flavonoid content, enzymatic activities: peroxidase, phenylalanine ammonia lyase and antioxidant activities. The results demonstrated that WsLE enhanced the evaluated parameters though the bio-stimulant effects varied across the crop species. Certain crop plants, such as, T. foenum-graceum, V. radiata and S.bicolor showed particularly strong responses, exhibiting marked improvements in plant growth and biochemical traits. To better understand the variability in response, Principal component analysis was conducted to categorize the crop plants according to the influence of different WsLE dilutions. Chromatographic profiling and identification of bioactive compounds in WsLE were performed using HPLC and UHPLC/HRMS. The analytical characterization revealed that the presence of 26 withanolides, 5 phytohormones and 26 other bioactive phytoconstituents. Quantitative analysis demonstrated that 27- hydroxywithanone and withaferin A exhibited the highest abundance among all identified compounds, suggesting potential role as the primary bioactive constituent. The comprehensive chemical characterization indicated that these major bioactive compounds likely serve as key modulators of physiological and biochemical pathways. © 2025
Tinosporaside from Tinospora cordifolia Encourages Skeletal Muscle Glucose Transport through Both PI-3-Kinase- and AMPK-Dependent Mechanisms
(MDPI, 2023) Akansha Mishra; Khushbu Sharma; Jyotsana Pandey; Kapil Dev; Sleman Kadan; Mahendra Sahai; Ishbal Ahmad; Arvind K. Srivastava; Akhilesh K. Tamrakar; Hilal Zaid; Rakesh Maurya
The stem of Tinospora cordifolia has been traditionally used in traditional Indian systems of medicine for blood sugar control, without the knowledge of the underlying mechanism and chemical constitution responsible for the observed anti-diabetic effect. In the present study, Tinosporaside, a diterpenoid isolated from the stem of T. cordifolia, was investigated for its effects on glucose utilization in skeletal muscle cells, which was followed by determining the anti-hyperglycemic efficacy in our diabetic db/db mice model. We found that tinosporaside augmented glucose uptake by increasing the translocation of GLUT4 to the plasma membrane in L6 myotubes, upon prolonged exposure for 16 h. Moreover, tinosporaside treatment significantly increased the phosphorylation of protein kinase B/AKT (Ser-473) and 5′ AMP-activated protein kinase (AMPK, Thr-172). These effects were abolished in the presence of the wortmannin and compound C. Administration of tinosporaside to db/db mice improved glucose tolerance and peripheral insulin sensitivity associated with increased gene expression and phosphorylation of the markers of phosphoinositide 3-kinases (PI3Ks) and AMPK signaling in skeletal muscle tissue. The findings revealed that tinosporaside exerted its antidiabetic efficacy by enhancing the rate of glucose utilization in skeletal muscle, mediated by PI3K- and AMPK-dependent signaling mechanisms. © 2023 by the authors.