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1.
Heliyon ; 6(8): e04787, 2020 Aug.
Article in English | MEDLINE | ID: mdl-32913908

ABSTRACT

The present study is aimed to investigate the anti-inflammatory, antioxidant and antidiabetic activities of three series of hydroxytriazenes based on sulfa drugs viz; Sulphathiazole (ST), Sulfisoxazole (SF) and Sulphamethoxazole (SM). Antidiabetic activities of the synthesized hydroxytriazenes were investigated by α-glucosidase and α-amylase inhibition method and IC50 values were recorded. The compounds presented significant α-glucosidase and α-amylase inhibition effect with IC50 values ranging from 122 to 341 µg/mL. Anti-inflammatory activity was also investigated by carrageenan-induced paw edema (CPE) method, where % inhibition was up to 89% after 4 h of treatment and antioxidant properties of the similar compounds were assessed by DPPH and ABTS radical scavenging assays. Antioxidant capacity of all the hydroxytriazenes detected by ABTS assay, was significantly higher as compared to DPPH assay. The hydroxytriazenes having highest antioxidant capacity presented IC50 values for compound ST-1 and ST-6 are 488 µg/mL for DPPH, 54.12 µg/mL for ABTS and 858.5 µg/mL for DPPH, 48.0 µg/mL for ABTS, respectively. These results suggested that ABTS assay may be more useful than DPPH assay for synthetic antioxidants. The findings from the molecular docking experiments may also expand the formation of new potent sulpha drugs based hydroxytriazenes targeting towards the subunit of C-terminal of human maltase-glucoamylase for the treatment of diabetes metabolic disorder. Overall, highlight the multifunctional role of hydroxytriazenes as antidiabetic, antioxidant and anti-inflammatory agents.

2.
Med Pharm Rep ; 93(3): 280-286, 2020 Jul.
Article in English | MEDLINE | ID: mdl-32832893

ABSTRACT

INTRODUCTION: The interocclusal registration materials record the occlusal relationship between the natural and /or artificial teeth for planning an occlusal rehabilitation in removable and fixed partial dentures. AIM AND OBJECTIVES: The aim of this in vitro study was to evaluate and compare the accuracy and the three dimensional stability offered by three different types of interocclusal recording materials at storage time intervals of 1 hour and 24 hours. METHODS: Three commercially available interocclusal recording materials were used: Group I-Polyether bite registration paste (Ramitec), Group II-Polyvinylsiloxane bite registration material (Imprint), Group III-Bite registration wax (Maarc). The test was carried out using an epoxy resin model. A total of 30 samples were made with each group consisting of ten samples. Three dimensional measurements were carried out by using 3D-Coordinate measuring machine (CMM) at time intervals of 0-1 hour and 0-24 hours in X, Y and Z-axis. RESULTS: Twelve readings were obtained for three axes (4 readings for each sample at 1 axis) and the averages of these four values were noted for a particular axis (X/Y/Z). Statistical analysis was performed using analysis of variance (ANOVA) for comparison among the groups and then Tukey's honestly significant difference (HSD) tests was performed for comparison among groups at the 0.05 level of significance. CONCLUSION: Polyvinylsiloxane was dimensionally the most stable material followed by polyether and finally bite registration wax. Dimensional accuracy and stability is influenced by both "material" and "time" factors.

3.
Bioorg Chem ; 96: 103642, 2020 03.
Article in English | MEDLINE | ID: mdl-32062065

ABSTRACT

Herein, we report synthesis, characterization, anti-diabetic, anti-inflammatory and anti-oxidant activities of hydroxytriazenes derived from sulpha drugs, namely sulphanilamide, sulphadiazine, sulphapyridine and sulphamethazine. Before biological screening of the compounds, theoretical prediction using PASS was done which indicates probable activities ranging from Pa (probable activity) values 65-98% for anti-inflammatory activity. As per the predication, experimental validation of some of the predicted activities particularly anti-diabetic, anti-inflammatory and anti-oxidant was done. Anti-diabetic activities have been screened using two methods namely α-amylase and α-glucosidase inhibition method and IC50 values were ranging from 66 to 260 and 148 to 401 µg/mL, while for standard drug acarbose the values were 12 µg/mL and 70 µg/mL, respectively. Docking studies have also been done for antidiabetic target pancreatic alpha amylase. The molecular docking studies in α-amylase enzyme reveal that the middle phenyl ring of all the compounds mainly occupies in the small hydrophobic pocket formed by the Ala198, Trp58, Leu162, Leu165 and Ile235 residues and sulphonamide moiety establish H-bond interaction by two water molecules. Further, anti-inflammatory activity has been evaluated using carrageenan induced paw-edema method and results indicate excellent anti-inflammatory activity by hydroxytriazenes (71 to 97%) and standard drug diclofenac 94% after 4 h of treatment. Moreover, antioxidant effect of the compounds was tested using DPPH and ABTS methods. All the compounds displayed good results (24-488 µg/mL) against ABTS radical and many compounds are more active than ascorbic acid (69 µg/mL) while all other compounds showed moderate activity against DPPH radical (292-774 µg/mL) and ascorbic acid (29 µg/mL). Thus, the studies reveal potential of sulfa drug based hydroxytriazenes as candidates for antidiabetic, anti-inflammatory and antioxidant activities which have been experimentally validated.


Subject(s)
Anti-Inflammatory Agents/chemistry , Antioxidants/chemistry , Hypoglycemic Agents/chemistry , Triazenes/chemistry , Animals , Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemical synthesis , Antioxidants/pharmacology , Chemistry Techniques, Synthetic , Female , Glycoside Hydrolase Inhibitors/chemical synthesis , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Humans , Hypoglycemic Agents/chemical synthesis , Hypoglycemic Agents/pharmacology , Male , Molecular Docking Simulation , Rats , Sulfadiazine/analogs & derivatives , Sulfadiazine/chemical synthesis , Sulfadiazine/pharmacology , Sulfanilamide/analogs & derivatives , Sulfanilamide/chemical synthesis , Sulfanilamide/pharmacology , Sulfapyridine/analogs & derivatives , Sulfapyridine/chemical synthesis , Sulfapyridine/pharmacology , Triazenes/chemical synthesis , Triazenes/pharmacology
4.
J Indian Prosthodont Soc ; 19(1): 79-82, 2019.
Article in English | MEDLINE | ID: mdl-30745758

ABSTRACT

Radiotherapy for carcinomas that involve the mouth and its related structures has been improved by the usage of different prostheses known as radiation carriers. These prostheses can accurately position radionuclide such as radium, iridium, cesium, and cobalt to allow adequate transfer of a concentrated radiation dose to a tumor region. At the same time, they minimize the exposure to radiation of nearby tissues due to rapid fall-off the radioactivity and thus minimizing the side effects of radiation. This study emphasizes the usage of a modified technique for the development of afterload mold brachytherapy appliance for squamous cell carcinoma patients of hard palate/soft palate.

5.
Contemp Clin Dent ; 9(Suppl 1): S127-S132, 2018 Jun.
Article in English | MEDLINE | ID: mdl-29962777

ABSTRACT

BACKGROUND: Majority of general dental practitioners provide fixed dental prosthesis in India. The aim of this study was to gather information on selection, usage, and materials and methods employed in interocclusal records and their communication with the dental laboratory for restorative procedures practised by dentists in Indore district to evaluate and to improve the quality of current practice. AIM AND OBJECTIVES: The purpose of this cross-sectional study was to understand and to evaluate dental practitioner's knowledge on interocclusal recording materials, its usage, their clinical implications, and their correlation with the laboratory in restorative procedures practiced by the dental practitioners in Indore district. MATERIALS AND METHODS: A questionnaire comprising 11 questions were framed and circulated among general dental practitioners except prosthodontists, and the results were statistically analyzed. RESULTS: Most of the practitioner's preferred wax (54.6%) as an interocclusal recording material over polyvinylsiloxane and polyether. Most of the dentists preferred full arch interocclusal record (27.8%). About 51.5% clinicians trimmed the interocclusal record before sending to the laboratory. CONCLUSION: From this survey, it has been concluded that the practitioner's attitude toward the use of interocclusal record materials is found to be deviated from well-acknowledged prosthodontic quality guidelines.

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