Synthesis and Evaluation of Novel Quinazolin-4-(3h)-one Analogues for their Anti-Inflammatory Activity RS Kulkarni, NK Sathish, AA Kempwade, SA Kavatagimath International Journal of Pharmaceutical Quality Assurance, 2023 New 2, 3-disubstituted quinazolin-4-(3H)ones was conceived and synthesized through the substitution of various primary amines at the 3-position and a range of aldehydes at the 2-position. These compounds were characterized using elemental analysis, IR spectroscopy, 1H NMR spectroscopy and MS. Subsequently, the anti-inflammatory activity of these newly developed quinazoline derivatives was investigated by in-vitro protein denaturation method. In-vitro studies revealed that compounds QB1, QB2, QB4, QB8, QB9, QF1, QF3, QF4, QF8 and QF10 have significant anti-inflammatory potential. In-vivo anti-inflammatory properties of QB2 and QF8 were tested in carrageenan-induced paw edema. Research findings demonstrated that compounds QB2 and QF8 have significant anti-inflammatory properties.
Bioinformatics and Next-Generation Data Analysis for Identification of Genes and Molecular Pathways Involved in Subjects with Diabetes and Obesity Prashanth Ganekal, Basavaraj Vastrad, Satish Kavatagimath, Chanabasayya Vastrad, Shivakumar Kotrashetti Medicina Lithuania, 2023 Background and Objectives: A subject with diabetes and obesity is a class of the metabolic disorder. The current investigation aimed to elucidate the potential biomarker and prognostic targets in subjects with diabetes and obesity. Materials and Methods: The next-generation sequencing (NGS) data of GSE132831 was downloaded from Gene Expression Omnibus (GEO) database. Functional enrichment analysis of DEGs was conducted with ToppGene. The protein–protein interactions network, module analysis, target gene–miRNA regulatory network and target gene–TF regulatory network were constructed and analyzed. Furthermore, hub genes were validated by receiver operating characteristic (ROC) analysis. A total of 872 DEGs, including 439 up-regulated genes and 433 down-regulated genes were observed. Results: Second, functional enrichment analysis showed that these DEGs are mainly involved in the axon guidance, neutrophil degranulation, plasma membrane bounded cell projection organization and cell activation. The top ten hub genes (MYH9, FLNA, DCTN1, CLTC, ERBB2, TCF4, VIM, LRRK2, IFI16 and CAV1) could be utilized as potential diagnostic indicators for subjects with diabetes and obesity. The hub genes were validated in subjects with diabetes and obesity. Conclusion: This investigation found effective and reliable molecular biomarkers for diagnosis and prognosis by integrated bioinformatics analysis, suggesting new and key therapeutic targets for subjects with diabetes and obesity.
Bioinformatics Analysis of Next Generation Sequencing Data Identifies Molecular Biomarkers Associated With Type 2 Diabetes Mellitus Varun Alur, Varshita Raju, Basavaraj Vastrad, Chanabasayya Vastrad, Satish Kavatagimath, Shivakumar Kotturshetti Clinical Medicine Insights Endocrinology and Diabetes, 2023 Background: Type 2 diabetes mellitus (T2DM) is the most common metabolic disorder. The aim of the present investigation was to identify gene signature specific to T2DM. Methods: The next generation sequencing (NGS) dataset GSE81608 was retrieved from the gene expression omnibus (GEO) database and analyzed to identify the differentially expressed genes (DEGs) between T2DM and normal controls. Then, Gene Ontology (GO) and pathway enrichment analysis, protein-protein interaction (PPI) network, modules, miRNA (micro RNA)-hub gene regulatory network construction and TF (transcription factor)-hub gene regulatory network construction, and topological analysis were performed. Receiver operating characteristic curve (ROC) analysis was also performed to verify the prognostic value of hub genes. Results: A total of 927 DEGs (461 were up regulated and 466 down regulated genes) were identified in T2DM. GO and REACTOME results showed that DEGs mainly enriched in protein metabolic process, establishment of localization, metabolism of proteins, and metabolism. The top centrality hub genes APP, MYH9, TCTN2, USP7, SYNPO, GRB2, HSP90AB1, UBC, HSPA5, and SQSTM1 were screened out as the critical genes. ROC analysis provides prognostic value of hub genes. Conclusion: The potential crucial genes, especially APP, MYH9, TCTN2, USP7, SYNPO, GRB2, HSP90AB1, UBC, HSPA5, and SQSTM1, might be linked with risk of T2DM. Our study provided novel insights of T2DM into genetics, molecular pathogenesis, and novel therapeutic targets.
Identification of candidate biomarkers and pathways associated with type 1 diabetes mellitus using bioinformatics analysis Madhu Pujar, Basavaraj Vastrad, Satish Kavatagimath, Chanabasayya Vastrad, Shivakumar Kotturshetti Scientific Reports, 2022 Type 1 diabetes mellitus (T1DM) is a metabolic disorder for which the underlying molecular mechanisms remain largely unclear. This investigation aimed to elucidate essential candidate genes and pathways in T1DM by integrated bioinformatics analysis. In this study, differentially expressed genes (DEGs) were analyzed using DESeq2 of R package from GSE162689 of the Gene Expression Omnibus (GEO). Gene ontology (GO) enrichment analysis, REACTOME pathway enrichment analysis, and construction and analysis of protein–protein interaction (PPI) network, modules, miRNA-hub gene regulatory network and TF-hub gene regulatory network, and validation of hub genes were performed. A total of 952 DEGs (477 up regulated and 475 down regulated genes) were identified in T1DM. GO and REACTOME enrichment result results showed that DEGs mainly enriched in multicellular organism development, detection of stimulus, diseases of signal transduction by growth factor receptors and second messengers, and olfactory signaling pathway. The top hub genes such as MYC, EGFR, LNX1, YBX1, HSP90AA1, ESR1, FN1, TK1, ANLN and SMAD9 were screened out as the critical genes among the DEGs from the PPI network, modules, miRNA-hub gene regulatory network and TF-hub gene regulatory network. Receiver operating characteristic curve (ROC) analysis confirmed that these genes were significantly associated with T1DM. In conclusion, the identified DEGs, particularly the hub genes, strengthen the understanding of the advancement and progression of T1DM, and certain genes might be used as candidate target molecules to diagnose, monitor and treat T1DM.
Central Composite Design for the Development and Evaluation of Liquisolid Compacts of Glyburide Archana Patil, Bhakti Kauthankar, Satish Kavatagimath, Rajashree Masareddy, Panchaxari Dandagi Indian Journal of Pharmaceutical Education and Research, 2022 Background: Glyburide is an oral antidiabetic agent with a shorter half-life and is practically insoluble in water. As a result, there is a need to enhance the drug solubility with a aim to improve drug absorption via the oral route. The goal of this study was to formulate, optimize and evaluate the liquisolid tablets of Glyburide using a suitable liquid vehicle in order to enhance the solubility, and bioavailability of the Glyburide. Materials and Methods: The liquisolid compacts of Glyburide were prepared by direct compression method using approved excipients. Using central composite design, the amount of Transcutol HP and carrier: coating ratio to be added in the formulations of Glyburide liquisolid compact has been theoretically generated by the software. The liquisolid tablets were evaluated for thickness and diameter, hardness, weight variation, friability, content uniformity, disintegration time, in-vitro dissolution study and compared with marketed product. Results: The prepared liquisolid system exhibited good flow-properties. The allpost compression parameters were well within the specified limits. The release profile of optimal formulation revealed higher drug release compared to marketed formulation. Increases in the concentration of liquid vehicle and carrier: coating material ratio resulted in an increase in the dissolution rate. Conclusion: The liquisolid compact method was discovered to be a potential method to enhance the dissolution profile, thereby enhancing the solubility of the Glyburide.
Pharmacological evaluation of caesalpinia pulcherrima leaf extract for anticancer activity against ehrlich ascites carcinoma bearing mice Shamanand Mallapur, Prakash Rajshekhar Biradar, Satish Annayya Kavatagimath, Priyanka Patil, Vishal Patil, Namit Kudatarkar Indian Journal of Pharmaceutical Education and Research, 2021 Objectives: The aim of the study is to assess the anticancer activity of Caesalpinia pulcherrima leaf extract against Erlich Ascites Carcinoma (EAC) in mice. Materials and Methods: BALB/c mice with Erlich Ascites Carcinoma were used for the present study. Ethanolic extract of C. pulcherrima (EECP) was administered p.o. in three different doses i.e. 200, 400 and 800 mg/kg body weight, after 24 hr of tumor inoculation in mice for 14 days. Effect of EECP on haematological parameters, liver enzymes marker, biochemical parameters/ antioxidants was evaluated after 14 days treatment. Results: Effect of EECP on Haematological parameters were evaluated and Hb, Lymphocytes, RBC and Monocytes showed significant increase in their count when compared to Disease. WBC and neutrophil count was decreased in EECP group compared to disease. Effect of EECP on Serum parameters were evaluated and showed significant decrease in ALP, TC, AST, ALT and TG compared to disease. TP was significantly increased in EECP groups compared to DISEASE group. Effect of EECP on Antioxidant activity showed significant increase in CAT, SOD, GSH and GPx counts compared to Disease. LPO level was significantly reduced in all the treated groups compared to Disease group. Conclusion: Ethanolic extract of C. pulcherrima leaf exhibited significant antioxidant and anticancer activity against Erlich Ascites Carcinoma.
In-vivo screening of ethanolic extract of antigonon leptopus flower for anti-diabetic and antioxidant potential Satish Annayya Kavatagimath, Sunil Satyapa Jalalpure, Ravindra Durdundayya Hiremath, Amolkumar Ashok Kempwade Indian Journal of Pharmaceutical Education and Research, 2020 Objectives: Medicinal plants have always been a consummate source for drugs and already provided us with lead compounds for numerous currently available drugs with no or less side effects. This supports the usage of herbal drugs for the treatment and management of various diseases. However, an assessment with available techniques has become an essential aspect to establish a valid scientific rationale for their usage in major healthcare problems. Methods: Ethanolic extract of Antigonon leptopus flower was screened for antioxidant activity by DPPH method and its effects on blood glucose levels (OGTT, acute and sub-acute study) in Alloxan induced diabetic rats, effects on serum lipid profiles and histopathological study of pancreas. Results: The extract showed potent in-vitro antioxidant activity. Treatment with ethanolic extract of Antigonon leptopus exhibits remarkable reduction in fasting blood glucose level (OGTT) at 2nd and 4th hr with a percentage of 26% and 11% respectively, whereas in acute study (at 6 hr) it was found to be 16 % and in sub acute study (15 days) it was reported to be 54%. Also, a significant lipid lowering activity was observed. Conclusion: This potent antioxidant, hypoglycemic and hypolipidemic efficacy may be attributed to the secondary metabolites (phenols, flavonoids, terpenoids, alkaloids, phytosterols and proteins) present.
Screening of ethanolic extract of diospyros malabarica desr. Bark for anti-diabetic and antioxidant potential Satish Annayya Kavatagimath, Sunil Satyappa Jalalpure Indian Journal of Pharmaceutical Education and Research, 2016 Objective: Evaluation of ethanolic extract of Diospyrous malabarica Desr. Bark for anti-diabetic and antioxidant potentials. Materials and Methods: Diospyros malabarica Desr. bark ethanol extract was studied for the OGTT study and acute and sub-acute effects on alloxan induced diabetic rats. Blood glucose levels, Serum lipid profiles and histopathological study of pancreas were performed. The Bark extract was also studied for DPPH radical scavenging potential. Results: Ethanolic extract of bark of Diospyros malabarica significantly improved the glucose tolerance test upto 4h., approximately, 17% and 29% reduction in blood glucose level was observed at 2 h and 4 h respectively. Blood glucose lowering potential percentage was 19% at 6 h in acute studyand after 15 days of treatment it was 39% in Sub acute study. The extract also showed better activity in quenching DPPH radical. Conclusion: Ethanolic extract (200 mg /kg) treated diabetic rats showed partial restoration of normal cellular population and size of islet cells.
Screening of ethanolic extract of Borassus flabellifer flowers for its antidiabetic and antioxidant potential Satish A. Kavatagimath, Sunil S. Jalalpure, Ravindra D. Hiremath Journal of Natural Remedies, 2016 <p>Diabetes mellitus is an age old metabolic disorder characterized by increased blood glucose levels. This may be due to deficiency of insulin (Type I Diabetes) or insulin resistance (Type II Diabetes). Traditional system of medicine provides with many plant sources for the effective management of diabetes mellitus preferable than any other system of medicine. The rationale behind use of such herbal medicines is to be supported by establishing the scientific basis for their traditional claims. In the present study ethanolic extract of <em>Borassus flabellifer </em>flowers was screened for its anti-diabetic potential against alloxan induced diabetic rats. Oral glucose tolerance test (OGTT), blood glucose level, serum lipid profile and histological study of pancreas were performed. The free radical scavenging effect was studied by using DPPH method. After administration of the ethanolic extract, there was a significant reduction in fasting blood glucose levels from 60 min (OGTT) acute study reveals blood glucose lowering potential of 20 % at 6 hr whereas sub-acute study after 15 days of treatment it was observed to be 35 %. The extract exerts a significant DPPH radical scavenging effect. From the data it can be inferred that ethanolic extract of <em>Borassus flabellifer </em>flowers are in confirmation with the claims made in traditional system of medicine. This marked antihyperglycemic effect and <em>in vitro</em> antioxidant potential may be attributed to the presence of active constituent’s like flavonoids and triterpenoids.</p><p> </p>
Synthesis and pharmacological screening of some 1,4-dihydropyridines for antiinflammatory activity Indian Drugs, 2008
