THE INSULINOTROPIC EFFECT OF THIAZOLIDINEDIONE DERIVATIVES IN TYPE II DIABETIC MODEL, RIN-5F CELLS, AND ITS ACTION ON CULTURED HUMAN LUNG FIBROBLAST SHOWS OXYGEN FREE-RADICAL SCAVENGING ACTIVITY

REKHA S; KALPANA DIVEKAR; CHANDRASHEKHARA S

doi:10.22159/ajpcr.2021.v14i7.40792

Authors

REKHA S Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru, Karnataka, India.
KALPANA DIVEKAR Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru, Karnataka, India.
CHANDRASHEKHARA S Department of Pharmaceutics, Dr. Ravi Patil College of Pharmacy, Belgaum, Karnataka, India.

DOI:

https://doi.org/10.22159/ajpcr.2021.v14i7.40792

Keywords:

Diabetes, Free-radical scavenging activity, RIN-5F cells, Diseased human lung fibroblast

Abstract

Objective: Diabetes mellitus is a persistent disorder caused by deficiency in insulin production. Oxidative stress plays an important role in physiopathology of diabetes. The present research determined the antidiabetic and antioxidant effects of 5-naphthalidin thiazolidinediones derivatives.

Methods: Both in vitro and in vivo experiments were carried out on diabetes induced male Swiss albino rats by single intramuscular injection of alloxan (0.15 mg/kg i.m) and IDDM-rats received 4b, 4c, or 4d (36 mg/kg, p.o). The derivatives were further subjected to insulin secretion by RIN-5F cells confirmed insulinotropic effect. In vitro antioxidant activity was evaluated using enzymatic activities on cell lines In addition, all the synthesized derivatives showed non-toxic effects against a diseased human lung fibroblast (COPD), HCC7231 (TACC CCL-96).

Results: The results revealed that 4b, 4c, and 4d showed promising results by substantially lowering the blood glucose levels on 21st day of post-administration. Serum insulin levels substantially rose, suggesting that derivatives exert insulinotropic effects through different pathways. 4c showed oxygen free-radical scavenging activity.

Conclusion: Our study proves that oral administration of 5-naphthalidin-TZD twice a day is a valuable treatment for type II diabetes. It seems to be a good drug moiety endowed significant oxygen free-radical scavenging activity.

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