Evaluation and comparison of anti-cancer activity of dapagliflozin and canagliflozin in oral cancer cell line: an in vitro study

Background: Cancer is rapidly evolving life-threatening ailment in the mankind due to changes in daily food intake and lifestyle changes. Oral carcinoma is 6th major cause of cancer death in the world and it is third major reason of cancer mortality in India. Every cell in the human body requires glucose for its metabolic energy. Besides normal cell, cancer cells also require the glucose for its endurance and multiplication. SGLT2 inhibitors which are aimed at diabetes therapy exhibited anticancer properties also in colon and pancreatic cancer lines. Present study aim is to evaluate the anticancer activity of SGLT2 inhibitors against oral cancer cell by MTT Assay.Methods: To evaluate the anticancer activity of SGLT2 inhibitors MTT Cytotoxic assay is performed as per standard protocols. Cancer cells were plated in 24-well plates and incubated at 370C with 5% CO2 condition. After convergence, samples are added to the plates in various concentrations and allowed to incubate then they are detached from the plates and cleansed with the reagents. The wells are coated with the dye and incubated. Later samples are analysed in UV-spectrophotometer.Results: Cytotoxic assay showed decrease in cell viability with increasing dose of SGLT2 inhibitors. IC50 values were determined graphically. The IC50 value of dapagliflozin is 400µg/ml and canagliflozin is 250µg/ml respectively after 24 hours of Assessment.Conclusions: The results of the current study give us an evidence that SGLT2 inhibitors dapagliflozin and canagliflozin exhibits anticancer property in Oral Cancer cell line

Comparative study of the efficacy and safety of topical sertaconazole versus topical terbinafine in the treatment of dermatophytoses in a tertiary care centre

Background: Dermatophytes are superficial fungal infection termed dermatophytosis, diagnosed by direct microscopy and confirmed with culture and treated with antifungal agents by both topical and systemic therapy. The objective of this study was to compare the efficacy of topical sertaconazole with topical terbinafine applied twice daily in reducing the size and severity of the lesions.Methods: Two groups of patients, the topical sertaconazole nitrate 2% cream (group 1) and the topical terbinafine hydrochloride 1% cream (group 2) were treated twice daily for 2 weeks and followed after 4 weeks. Skin scrapings were taken to confirm the diagnosis, to assess the efficacy and potency of the study drugs. The statistical analysis was performed using statistical package for Social Sciences. Assessment of the groups was analysed using Chi-square test. Baseline demographic data was analysed using ANOVA.Results: At the end of first week, sertaconazole group showed significant changes in pruritis (p value 0.045) as compared to terbinafine group (p value <0.05) and no severe symptoms of erythema in both grups. After 2 weeks, resolution of vesicle was seen higher in terbinafine group. But after ‘follow-up phase’, all patients showed absence of vesicles and negative mycological assessment.Conclusions: Topical sertaconazole nitrate was better in reducing the severity of pruritis and achieving faster mycological cure compared to terbinafine and found to possess additional anti-pruritic and anti-inflammatory action

Evaluation of neuroprotective effect of flupirtine in brain of albino rats

Background: Flupirtine (FP) is found to antagonize both glutamate and N methyl, D aspartate (NMDA) and the current study was undertaken to elucidate a possible neuroprotective role of flupirtine against NMDA induced neurotoxicity in experimental rat model.Methods: Excitotoxicty was produced in rat and it is counteracted by flupirtine. The animals were grouped as Group 1 (vehicle treated), Group 2 (received NMDA+vehicle), Group 3 (received FP+NMDA only), and Group 4 (received FP+vehicle) and were observed of animal behavior and oxidative stress biomarkers and also mRNA expression using reverse transcriptase-polymerase chain reaction (PCR PCR) was performed to determine the level of mRNA expression of acetyl cholinesterase (AChE) and muscarinic cholinergic receptor (MChR) in brain samples (hippocampus) of experimental animals.Results: Depression effect induced by NMDA was reversed by flupirtine. Decrease in oxidative stress bio-markers associated with increase in the antioxidant enzyme activities in group 3 and 4 compared to group 1 and 2. Gene expression were up-regulated in group 2 compared to 1, 3 and 4. Flupritine treatment reversed these alterations.Conclusions: This study represents the neuroprotective characteristics of flupiritne against the excitotoxicity induced by NMDA in an in vivo rat models

COMPARATIVE ANALYSIS OF THE ANTICANCER ACTIVITY OF ANGIOTENSIN RECEPTOR BLOCKERS - IRBESARTAN AND TELMISARTAN

Objective: Angiotensin receptor blockers (ARBs) are effective hypertensive drugs. Reduction in risk of lung cancer with ARBs was proven in clinical studies. Telmisartan and irbesartan are the second-generation ARBs. This study screens the anticancer activity of these two drugs in a dose-dependent manner using A549 cell line.Methods: Different concentrations of irbesartan and telmisartan were treated on A549 cells and the anticancer activity was evaluated through methylthiazolyldiphenyl-tetrazolium [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] cytotoxicity assay. The dot plot of the cytotoxicity results was used to extrapolate the half maximal inhibitory concentration (IC50) values. Microscopic changes in the cells post-treatment with these drugs were also recorded at ideal concentrations.Results: A reduction in cell viability was noted in A549 cells with increasing concentration of the drug. The IC50 values for irbesartan and telmisartan were 31.1 μg and 15.6 μg, respectively. Microscopic observation of the cells shows more rounded and deformed dead cells on telmisartan- and irbesartan-treated cells when compared with the untreated control.Conclusion: The results confirm the anticancer activity of both the drugs with telmisartan being more efficient. The anticancer activity could probably be due to the role of irbesartan and telmisartan in inhibiting mitogen-activated protein kinase cell survival pathway and local angiogenesis

EVALUATION AND COMPARISON OF CYTOTOXIC EFFECT OF VILAZODONE HYDROCHLORIDE WITH 5-FLUOROURACIL IN HT-29 BOWEL CANCER CELL LINE

Objectives: Vilazodone hydrochloride is a novel selective serotonin reuptake inhibitor (SSRI) used to treat major depressive disorders. There are only sparse data available to know about the SSRI’s and its association with colon cancer. This study aims to evaluate and compare the in vitro cytotoxic effect of vilazodone with 5-fluorouracil (5-FU) in HT-29 cell line. Methods: Cell viability was tested by the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay (Mosmann, 1983). Test sample and standard drug in variable concentrations were added to the HT-29 cell lines for incubation over 24 h under ideal conditions. After washing the test and standard drug sample from the well with saline, MTT was added and incubated for 4 h. Dimethyl sulfoxide of 1 ml was added in all wells after incubation with MTT. The absorbance at 570 nm was measured with an ultraviolet - spectrophotometer. Results: The values were tabulated, and the graph was plotted to find the IC-50 value (inhibitory concentration at 50%) which was struck at 28.5 μg/ml and12. 8 μg/ml for vilazodone hydrochloride and 5-FU, respectively. Conclusion: The results show that vilazodone hydrochloride has good anticancer property comparable with 5-FU, which would probably play a role as a cytotoxic agent in tumor cells. The proposed mechanism of action could be by activation of caspase-3 enzyme, thereby increasing apoptosis and indicates its use in coexisting depression and colon carcinoma. Other mechanism includes suppression of oncogene p53, which can be confirmed by future studies

Isolation and characterization of a cytokinin-binding protein from cucumber cotyledons

A protein which binds specifically to [3H]-zeatin has been isolated from cucumber cotyledons by chromatographic techniques. Its binding to [3H]-zeatin was inhibited remarkably by the addition of non-radioactive cytokinins and the order of inhibition was zeatin > -zeatin riboside > N6-(Delta2-isopentenyl)adenine > N6-(Delta2-isopentenyl)adenosine > N6-benzyl-adenosine > kinetin riboside. This protein behaved as a soluble protein with an apparent molecular size of 43,000 daltons on gel filtration through calibrated Sephadex G-100 column. The dissociation constant, Kd, of the protein-zeatin complex was about 4 × 10–7 M

Comparative study of the efficacy and safety of topical sertaconazole versus topical terbinafine in the treatment of dermatophytoses in a tertiary care centre

Background: Dermatophytes are superficial fungal infection termed dermatophytosis, diagnosed by direct microscopy and confirmed with culture and treated with antifungal agents by both topical and systemic therapy. The objective of this study was to compare the efficacy of topical sertaconazole with topical terbinafine applied twice daily in reducing the size and severity of the lesions. Methods: Two groups of patients, the topical sertaconazole nitrate 2% cream (group 1) and the topical terbinafine hydrochloride 1% cream (group 2) were treated twice daily for 2 weeks and followed after 4 weeks. Skin scrapings were taken to confirm the diagnosis, to assess the efficacy and potency of the study drugs. The statistical analysis was performed using statistical package for Social Sciences. Assessment of the groups was analysed using Chi-square test. Baseline demographic data was analysed using ANOVA. Results: At the end of first week, sertaconazole group showed significant changes in pruritis (p value 0.045) as compared to terbinafine group (p value <0.05) and no severe symptoms of erythema in both grups. After 2 weeks, resolution of vesicle was seen higher in terbinafine group. But after and lsquo;follow-up phase', all patients showed absence of vesicles and negative mycological assessment. Conclusions: Topical sertaconazole nitrate was better in reducing the severity of pruritis and achieving faster mycological cure compared to terbinafine and found to possess additional anti-pruritic and anti-inflammatory action. [Int J Basic Clin Pharmacol 2016; 5(3.000): 855-861

Evaluation of neuroprotective effect of flupirtine in brain of albino rats

Background: Flupirtine (FP) is found to antagonize both glutamate and N methyl, D aspartate (NMDA) and the current study was undertaken to elucidate a possible neuroprotective role of flupirtine against NMDA induced neurotoxicity in experimental rat model.Methods: Excitotoxicty was produced in rat and it is counteracted by flupirtine. The animals were grouped as Group 1 (vehicle treated), Group 2 (received NMDA+vehicle), Group 3 (received FP+NMDA only), and Group 4 (received FP+vehicle) and were observed of animal behavior and oxidative stress biomarkers and also mRNA expression using reverse transcriptase-polymerase chain reaction (PCR PCR) was performed to determine the level of mRNA expression of acetyl cholinesterase (AChE) and muscarinic cholinergic receptor (MChR) in brain samples (hippocampus) of experimental animals.Results: Depression effect induced by NMDA was reversed by flupirtine. Decrease in oxidative stress bio-markers associated with increase in the antioxidant enzyme activities in group 3 and 4 compared to group 1 and 2. Gene expression were up-regulated in group 2 compared to 1, 3 and 4. Flupritine treatment reversed these alterations.Conclusions: This study represents the neuroprotective characteristics of flupiritne against the excitotoxicity induced by NMDA in an in vivo rat models

Facile preparation and some applications of an affinity matrix with a cleavable connector arm containing a disulfide bond

A versatile affinity matrix in which the ligand of interest is linked to the matrix through a connector arm containing a disulfide bond is described. It can be synthesized from any amino-substituted matrix by successive reaction with 2-imino-thio-lane, 5, 5'-dithiobis(2-nitrobenzoic acid), and a thiol derivative of the ligand of choice. The repertoire of ligands can be significantly increased by the appropriate use of avidin-biotin bridges. After adsorption of the material to be fractionated, elution can be effected by reducing the disulfide bond in the connector arm with dithiothreitol. Examples of the preparation and use of various affinity matrices based on amino-substituted Sepharose 6MB are given. One involves the immobilization of the Fab' fragment of a monoclonal antibody against Aspergillus oryzae β-galactosidase and the specific binding of that enzyme to the resulting immunoaffinity matrix. Another involves the immobilization of N-biotinyl-2-thioethylamine followed by complex formation with avidin. The resulting avidin-substituted matrix was used for the selective adsorption and subsequent recovery of mouse hybridoma cells producing anti-avidin antibodies. By further complexing the avidin-substituted matrix with appropriate biotinylated antigens, it should be possible to fractionate cells producing antibodies against a variety of antigens