Background: Diabetes mellitus is a class of metabolic disorder which results high level of sugar due to inadequacy in insulin secretion. High Sugar level in diabetes is linked with the impairment and dysfunction of eyes, kidneys, blood vessels, nerves and heart. In current research there is extended interest in herbal medicines because of the side effects noticed with oral hypoglycemic for therapy of hyperglycemia. Herbal medicines could play a dominant role in the control of diabetes mellitus. Methods: Methanolic extracts of seeds of Psoralea corylifolia L & Psoralea esculenta L has been screened for both in-vitro and in-vivo antihyperglycemic role using streptozotocin induced diabetic rats. The methanolic extract of both plants were evaluated for pancreatic tissue studies. Results: According to the outcomes, a stunning blood glucose level decrement was observed in the diabetic groups treated by methanolic extracts of Psoralea corylifolia L. seeds. Conclusion: In this study, the methanolic extract of Psoralea corylifolia L. seeds used to evaluate antihyperglycemic potential showed appreciably notable and astonishing results, when compared with the Glibenclamide. Methanolic extract of Psoralea corylifolia L. seeds have potential to regulate hyperglycemia in the In-vivo model. Hence Psoralea corylifolia L. methanolic seeds extract may be selected for its antihyperglycemic activity.
Background: Operculina turpethum (Linn.) Silva Manso, family- convolvulaceae, is an important plant in Indian conventional system of medicine which is extensively employed by different tribes in many countries to cure edema and painful conditions like arthritis, back pain; hyperlipidemia, diabetes mellitus, liver disorders, skin disorders and to regulate bowel functions. Objective: The roots of O. turpethum (Linn.) was subjected to physicochemical, phytochemical standardization, the chromatographic separation which was accomplished by column chromatography, TLC, and HPTLC, further, the acute toxicity, cytotoxic and anti-inflammatory activities of Operculina turpethum roots were estimated by in vivo and in vitro models. Materials and Methods: This study includes percentage yield of extraction, organoleptic evaluation along with the analysis of its physicochemical investigations & preliminary phytochemical estimation. The isolation of active phytoconstituents was done by column chromatography, and the isolated compound was then exposed to TLC and HPTLC analysis. Cytotoxic activity was tested by WST-1 based cell viability assay on HepG2 cells. Anti-inflammatory activity of methanol extract (ME) was evaluated against inflammation occur by both in vitro and in vivo method. Results: The methanolic extract exhibited the presence of most of the phytoconstituents out of all the extracts, the phytoconstituent phytosterol, i.e., β-sitosterol was isolated by column chromatography, identified and quantified by TLC and HPTLC, which is liable for anti-inflammatory activity. The amount of β-sitosterol was estimated to be 14.09 µg in 10.00 mg fraction of MEOT. MEOT is devoid of toxicity up to 2000 mg/kg in Wistar albino rats. It was analysed that in vitro anti-inflammatory activity of MEOT by egg albumin denaturation method exhibited a incredible decrement in turbidity and increasing the percentage inhibition of albumin denaturation (60.52%) in MEOT treated group as compared with control group. In egg albumin-induced edema in rats, MEOT at the dose of 400 mg/kg reduced the edema formation (3.03 ± 0.02) induced by egg albumin at 4th h. In cotton pellet-induced granuloma in rats, MEOT at the dose of 400 mg/kg displayed maximum granuloma inhibition (51.06%) which is similar to that of indomethacin. Conclusion: From the obtained findings it is confirmed that O. turpethum contains β-sitosterol which is responsible for potent anti-inflammatory activity without causing cytotoxicity to the plant. The results suggested that ME of O. turpethum roots had high potential for application as an anti-inflammatory agent. The recognization and confirmation of the plant can be obtaineded from the study and will present data which is aidful in determining the quality and purity of a crude drug which further helps in preventing its adulteration.
Background: Thiazolidine-2, 4-diones and their derivatives are well-established chemical class of compounds that express their pharmacological actions through insulin sensitization and enhanced glucose utilization in peripheral tissues. In the current research different approaches have been employed to synthesize thiazolidine-2, 4-dione derivatives and these synthesized compounds were chemically characterized for the establishment of their chemical structures. Method: A series of thiazolidine-2, 4-dione (TZD) derivatives, scheme I (3A-3V) 22 compounds were synthesized and characterized by FT-IR, 1H NMR and mass spectral analysis. The title compounds were screened for their in vitro and in vivo anti-diabetic, antioxidant, and cytotoxicity studies. In vivo antihyperglycemic effect was assessed by measuring plasma glucose (PG) levels in alloxan-induced type II diabetic rat models. The synthesized TZD derivatives were evaluated for hepatotoxicity and pancreatic tissue integrity. Antioxidant activity was evaluated by the DPPH method and H2O2 method. Thiazolidinedione derivatives were subjected to predict free energy of binding towards target PPARγ, using rosiglitazone as the reference compound for molecular docking visualization through FlexX docking program. Molecular docking studies are also performed for understanding the binding of ligand to receptor. Results: The compound 3V 4-(5-(naphthalen-1-ylmethylene)-2, 4-dioxothiazolidin-3-yl) benzoic acid exhibited better blood glucose lowering activity than that of the standard drug rosiglitazone. Compound 3T and 3U exhibited potent antioxidant activity. Among the tested compounds for cytotoxicity using an MTT assay, compound 3H 5-(4-chlorobenzylidene)-2, 4-dioxothiazolidin-3-yl) benzoic acid exhibited better viability and cytotoxicity activity. From selected anti-diabetic targets, the proposed derivatives exhibited better interaction with PPARγ receptor, for example while rosiglitazone showed docking score of -19.891 kJ/mol, compound 3V exhibited highest docking score of -31.6617 kJ/mol. Conclusion: Computational molecular docking study demonstrated the selectivity and provided a binding model for the further refinement of this chemotype. Therefore, this series of thiazolidine-2, 4-diones derivatives (3A–3V) have considerable promise for development as potential antihyperglycemic and hypolipidemic agents.
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