Background Polycystic ovary syndrome (PCOS) is a chronic endocrine disorder prevalent in premenopausal women and is characterized by a range of physiological and biochemical abnormalities which may include reproductive, endocrine, and metabolic alterations such as insulin resistance. Insulin resistance is the hallmark of PCOS as it predisposes the affected subjects to a higher risk of impaired glucose tolerance and type 2 diabetes mellitus (T2DM). In this study, the inhibitory activities of phytosterols and saccharides from aqueous extract of Costus spicatus rhizome were investigated against phosphoenolpyruvate carboxykinase (PEPCK), α-amylase, β-glucosidase, and fructose 1,6-biphosphatase (FBPase) in silico as potential novel therapeutic targets for T2DM-associated-PCOS. Phytochemical constituents of the plant were determined using gas chromatography-mass spectrophotometry (GC-MS), while molecular docking of the compounds with PEPCK, α-amylase, β-glucosidase, and FBPase was conducted using Vina. Thereafter, the binding modes were determined using Discovery Studio Visualizer, 2020. Results GCMS analysis of an aqueous extract of Costus spicatus rhizome revealed the presence of three compounds with a higher binding affinity for all enzymes studied compared to metformin. The compounds also interacted with key amino acid residues crucial to the enzyme’s activities. This study identified Lyxo-d-manno-nononic-1,4-lactone as potential multi-target inhibitors of PEPCK, α-amylase, β-glucosidase, and FBPase with reasonable pharmacokinetic properties and no significant toxicity. Conclusion These compounds can be explored as potential therapeutic agents for the management of insulin resistance in PCOS, subject to further experimental validation.
The biochemical and toxicological effects of aqueous extract of Parquetina nigrescens leaves (AEPNL) at the doses of 50, 100, and 200 mg/kg body weight on mifepristone-induced in Polycystic Ovarian Syndrome (PCOS) was investigated in female Wistar rats. Sixty female Wistar rats (190.00 ± 13.00 g) were assigned into 6 groups (A - F) of ten each: animals in group A received 0.5 ml of distilled water orally on daily basis for 30 days while the mifepristonized rats in groups B, C, D and E also received orally 0.5 ml of distilled water, 7.14mg/kg of metformin (reference drug) and same volume of the extract corresponding to 50, 100, and 200 mg/kg body weight of AEPNL respectively after which levels of some biochemical and toxicological indices were determined. AEPNL aggravated mifepristone-treatment related increases in albumin, total protein and liver aspartate aminotransferase activity and mitigated the increases in globulin, total bilirubin, urea, creatinine, liver and serum alkaline phosphatase and alanine aminotransferase activities, and no treatment-related histoarchitectural changes occurred in the liver, kidney and uterus of the female rats. Therefore, the aqueous extract of Parquetina nigrescens leaves attenuated and also aggravated some biochemical parameters in the serum, liver and kidney but with no histological changes in the liver, kidney and uterus of the mifepristonized female Wistar rats. Keywords: Mifepristone, toxicology, Parquetina nigrescens, Polycystic Ovarian Syndrome, histology
The biochemical and toxicological effects of aqueous extract of Parquetina nigrescens leaves (AEPNL) at the doses of 50, 100, and 200 mg/kg body weight on mifepristone‐induced in Polycystic Ovarian Syndrome (PCOS) was investigated in female Wistar rats. Fifty female Wistar rats (190.00 ± 13.00 g) were assigned into 5 groups (A – E) of ten each: animals in group A received 0.5 ml of distilled water orally on daily basis for 30 days while the mifepristonized rats in groups B, C, D and E also received orally 0.5 ml of distilled water and same volume of the extract corresponding to 50, 100, and 200 mg/kg body weight of AEPNL respectively after which levels of some biochemical and toxicological indices were determined. AEPNL aggravated mifepristone‐treatment related increases in albumin, total protein and liver aspartate aminotransferase activity and mitigated the increases in globulin, total bilirubin, urea, creatinine, liver and serum alkaline phosphatase and alanine aminotransferase activities, and no treatment‐related histoarchitectural changes occurred in the liver, kidney and uterus of the female rats. Therefore, the aqueous extract of Parquetina nigrescens leaves attenuated and also aggravated some biochemical parameters in the serum, liver and kidney but with no histological changes in the liver, kidney and uterus of the mifepristonized female Wistar rats.
Though cypermethrin (Cyp) has contributed considerably to human welfare, their adverse effects on non‐target organisms are significant. The lipophilic nature of this pyrethroid exacerbates its toxicity by facilitating rapid access to the various tissues which in turn increase its interaction with the central nervous system, for which pesticides have high affinity. This study was designed to investigate the anticlastogenic and antidyslipidemic effects of Jatropha gossypifolia (JG), alpha‐lipoic acid (αLA) and vitamin C (VC) on plasma lipoprotein fractions in female rats. Eighty female rats were divided into ten groups of eight animals each and treated orally for 30 days. Groups 1 and 2 were given corn oil and cypermetrhin respectively, groups 3,4,5 and 6 were co‐administered with Cyp+JG50 mg/kg, Cyp+JG100 mg/kg, Cyp+αLA50 mg/kg and Cyp+VC50 mg/kg respectively. Groups 7, 8, 9 and 10 were given only JG50 mg/kg, JG100 mg/kg, αLA50 mg/kg and VC50 mg/kg respectively. From this study, cypermethrin administration resulted in an array of dyslipidemia as evidenced by significant increase in the level of cholesterol in plasma (64.05%), vLDL+LDL (571.88%), ovary (313.97%), uterus (147.49%); and triglyceride in plasma (88.69%), vLDL+LDL (71.51%), uterus (27.27%); however, a significant decrease was observed in ovary triglyceride (70.24%). Also, a significant increase was observed in the mean polychromatic erythrocyte (429.00%) compared to the control. Co‐administration with the methanolic leaf extract of JG, αLA and VC was able to attenuate the observed cypermethrin‐induced dyslipidemia and clastogenicity. Toxicological study from this study revealed that the plant extract is therapeutically safe for consumption at the doses under investigation. It can thus be concluded that the methanolic extract of Jatropha gossypifolia leaf could help regulate the dyslipidemic effect of cypermethrin on lipid parameters in organs and plasma lipoprotein fractions. The anticlastogenic effect of the plant could also be linked to the various phytoconstituents embedded in the plant.
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