Discovery of imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents in streptozotocin-induced diabetes in Wistar rats <i>via</i> inhibition of DPP-4

Gupta, Akanksha; Bhat, Hans Raj; Singh, Udaya Pratap

doi:10.1039/d3md00085k

Cited by 5 publications

(3 citation statements)

References 53 publications

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“…The rate of TNB production was directly proportional to the concentration of GSH (nm/mg protein) in the sample. 18,19…”

Section: Methodsmentioning

confidence: 99%

“…The calculation of each sample was done using the conversion formula. 18,19 Estimation of glutathione. GSH (Glutathione) was assessed according to the procedure of the GSH assay kit (cat.…”

Section: Preparation Of Tissue Homogenatementioning

confidence: 99%

“…The rate of TNB production was directly proportional to the concentration of GSH (nm/mg protein) in the sample. 18,19 Docking analysis. The docking of Eupatilin was performed with cyclooxygenase-2 (COX-2) (3ln1.pdb) using the default setting of the CB-Dock tool.…”

Section: Preparation Of Tissue Homogenatementioning

confidence: 99%

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Mechanistic Evaluation of Antiarthritic Effects of Eupatilin in CFA-Induced Arthritic Rats: An in Vivo and in Silico Study

Wang,

Liu,

Zhang

et al. 2024

Natural Product Communications

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Objectives In the present study, we explored the antiarthritic potential of Eupatilin on complete Freund's adjuvant (CFA)-induced arthritis rats. Materials and Methods In order to induce arthritis in the Sprague-Dawley rats, CFA vaccination was used, and Eupatilin was given to the rats at dose of 5, 10, and 20 mg/kg. Various biochemical and other parameters were studied to define the pharmacological benefit of Eupatilin. Results The study's findings revealed that Eupatilin increases rats’ body weight and significantly reduces hind paw volume. It also improves the antioxidant status of CFA rats by lowering malondialdehyde levels and increasing the concentration of endogenous antioxidants superoxide dismutase and GPx. Eupatilin also improved hematological markers, which were demonstrated to be altered in CFA rats as compared to the control. In the Eupatilin-treated group, the level of pro-inflammatory cytokines was found to be reduced as compared to CFA rats. In a molecular docking analysis, it showed favorable interaction with the active site of cyclooxygenase-2 (COX-2) by the formation of numerous nonbonded interactions by interacting with Cys32, Leu138, Pro 139, Val141, Ala142, and Cys145. It also showed a Vina score of −9.4 and interacts with the cavity volume of 4435 Å3. Conclusion Eupatilin showed favorable antiarthritic benefits in the CFA-induced arthritis model, as evidenced by reductions in paw volume, significant weight loss prevention, and maintenance of the healthy hematological and biochemical profile may be through inhibiting COX-2.

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“…The rate of TNB production was directly proportional to the concentration of GSH (nm/mg protein) in the sample. 18,19…”

Section: Methodsmentioning

confidence: 99%

“…The calculation of each sample was done using the conversion formula. 18,19 Estimation of glutathione. GSH (Glutathione) was assessed according to the procedure of the GSH assay kit (cat.…”

Section: Preparation Of Tissue Homogenatementioning

confidence: 99%

See 1 more Smart Citation

Mechanistic Evaluation of Antiarthritic Effects of Eupatilin in CFA-Induced Arthritic Rats: An in Vivo and in Silico Study

Wang,

Liu,

Zhang

et al. 2024

Natural Product Communications

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Synthesis and protective effect of 7-O-thiazole Oroxylin A derivative against diabetic nephropathy in streptozotocin-induced diabetes in Wistar rats

Dang,

2024

Chem. Pap.

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In Vivo Study to Explore the Antiarthritic Potential of Tiliroside on Complete Freund’s Adjuvant-Induced Rheumatoid Arthritis in Rats

Liu,

Wang

2024

Rev. Bras. Farmacogn.

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Discovery of imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents in streptozotocin-induced diabetes in Wistar rats via inhibition of DPP-4

Abstract: Novel 1,3,5-triazine derivatives bearing oxazine have been synthesized and tested for their ability to inhibit a panel of dipeptidyl peptidase (DPP)-4, 8, and 9 enzymes. In a comparative inhibitory assay,...

Cited by 5 publications

References 53 publications

Mechanistic Evaluation of Antiarthritic Effects of Eupatilin in CFA-Induced Arthritic Rats: An in Vivo and in Silico Study

Mechanistic Evaluation of Antiarthritic Effects of Eupatilin in CFA-Induced Arthritic Rats: An in Vivo and in Silico Study

Synthesis and protective effect of 7-O-thiazole Oroxylin A derivative against diabetic nephropathy in streptozotocin-induced diabetes in Wistar rats

In Vivo Study to Explore the Antiarthritic Potential of Tiliroside on Complete Freund’s Adjuvant-Induced Rheumatoid Arthritis in Rats

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