Exploring the potential of N-benzylidenebenzohydrazide derivatives as antidiabetic and antioxidant agents : design, synthesis, spectroscopic, crystal structure, DFT and molecular docking study

SUPPLEMENTARY MATERIALS SUMMARY : Supplementary crystallographic data for the compounds mentioned in the article can be obtained from the Cambridge Crystallographic Data Centre (CCDC) free of charge. The CCDC numbers for the supplementary crystallographic data are as follows: CCDC no: 2325385 (BB2), CCDC no: 232586 (BB4), and CCDC no: 232587 (BB6). To access the supplementary crystallographic data, please visit the Cambridge Crystallographic Data Centre's website at http://www.ccdc.cam.ac.uk/data request/cif.Please read abstract in the article.URC; South African National Research Foundation (NRF); Department of Chemical Science, University of Johannesburg; Center for High Performance Computing (CHPC).https://chemistry-europe.onlinelibrary.wiley.com/journal/23656549hj2024ChemistrySDG-03:Good heatlh and well-bein

Comparative effects of xylitol and erythritol on modulating blood glucose; inducing insulin secretion; reducing dyslipidemia and redox imbalance in a type 2 diabetes rat model

Xylitol and erythritol have been reported in numerous previous and recent studies as potential antidiabetic sweeteners, however, it is not certain which one is most effective in this regard. In the present study, the effects of xylitol and erythritol were comparatively investigated on blood glucose, insulin level, dyslipidemia, pancreatic islet morphology and β-cell function, and redox imbalance in a type 2 diabetes (T2D) model of rats. Seven-week-old male Sprague-Dawley rats were randomly divided into 8 groups: Normal Control (NC), Diabetic Control (DC), Diabetic Xylitol 5 % (DX5), Diabetic Xylitol 10 % (DX10), Diabetic Xylitol 20 % (DX20), Diabetic Erythritol 5 % (DE5), Diabetic Erythritol 10 % (DE10), and Diabetic Erythritol 20 % (DE20). T2D was induced in the diabetic groups initially by feeding 10 % fructose solution to induce insulin resistance followed by an intraperitoneal injection of streptozotocin (40 mg/kg body weight) dissolved in citrate buffer (pH 4.5) to induce partial pancreatic β-cells dysfunctions. The animals in NC group were fed with normal drinking water and injected with citrate buffer only. After the confirmation of diabetes, the xylitol and erythritol with above-mentioned concentrations were supplied to the respective animal groups when the animals in NC and DC groups were supplied with normal drinking water. After 8 weeks intervention period, the body weight, fluid and water intake, blood glucose, serum alanine aminotransferase, aspartate aminotransferase, CK-MB and creatinine were significantly decreased, while the serum insulin level, serum lipids, glucose tolerance ability, pancreatic islet morphology and β-cell function, pancreatic and serum redox imbalance were improved in the most xylitol and erythritol fed groups compared to the DC group, when effects were better for xylitol compared to erythritol. The data of this study suggest that xylitol has better antioxidant and antidiabetic effects compared to erythritol. Therefore, xylitol can be used as a preferrable dietary anti-diabetic sweetener or supplement over erythritol for the management of diabetes and its associated complications

<i>Croton gratissimus</i> Burch Herbal Tea Exhibits Anti-Hyperglycemic and Anti-Lipidemic Properties via Inhibition of Glycation and Digestive Enzyme Activities

Over the years, the world has continued to be plagued by type 2 diabetes (T2D). As a lifestyle disease, obese individuals are at higher risk of developing the disease. Medicinal plants have increasingly been utilized as remedial agents for managing metabolic syndrome. The aim of the present study was to investigate the in vitro anti-hyperglycemic and anti-lipidemic potential of Croton gratissimus herbal tea infusion. The inhibitory activities of C. gratissimus on carbohydrate (α-glucosidase and α-amylase) and lipid (pancreatic lipase) hydrolyzing enzymes were determined, and the mode of inhibition of the carbohydrate digestive enzymes was analyzed and calculated via Lineweaver–Burk plots and Michaelis Menten’s equation. Its effect on Advanced Glycation End Product (AGE) formation, glucose adsorption, and yeast glucose utilization were also determined. High-performance liquid chromatography (HPLC) was used to quantify the possible phenolic compounds present in the herbal tea infusion, and the compounds were docked with the digestive enzymes. C. gratissimus significantly (p 50 = 60.56 ± 2.78 μg/mL), α-amylase (IC50 = 35.67 ± 0.07 μg/mL), as well as pancreatic lipase (IC50 = 50.27 ± 1.51 μg/mL) in a dose-dependent (15–240 µg/mL) trend. The infusion also inhibited the non-enzymatic glycation process, adsorbed glucose effectively, and enhanced glucose uptake in yeast cell solutions at increasing concentrations. Molecular docking analysis showed strong binding affinity between HPLC-quantified compounds (quercetin, caffeic acid, gallic acid, and catechin) of C. gratissimus herbal tea and the studied digestive enzymes. Moreover, the herbal tea product did not present cytotoxicity on 3T3-L1 cell lines. Results from this study suggest that C. gratissimus herbal tea could improve glucose homeostasis and support its local usage as a potential anti-hyperglycemic and anti-obesogenic agent. Further in vivo and molecular studies are required to bolster the results from this study

Phytochemical Properties of <i>Croton gratissimus</i> Burch (Lavender Croton) Herbal Tea and Its Protective Effect against Iron-Induced Oxidative Hepatic Injury

Oxidative stress plays a vital role in the pathogenesis and progression of various liver diseases. Traditional medicinal herbs have been used worldwide for the treatment of chronic liver diseases due to their high phytochemical constituents. The present study investigated the phytochemical properties of Croton gratissimus (lavender croton) leaf herbal tea and its hepatoprotective effect on oxidative injury in Chang liver cells, using an in vitro and in silico approach. C. gratissimus herbal infusion was screened for total phenolic and total flavonoid contents as well as in vitro antioxidant capacity using ferric reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picryl-hydrazyl (DPPH) methods. Oxidative hepatic injury was induced by incubating 0.007 M FeSO4 with Chang liver cells which has been initially incubated with or without different concentrations (15–240 μg/mL) of C. gratissimus infusion or the standard antioxidants (Gallic acid and ascorbic acid). C. gratissimus displayed significantly high scavenging activity and ferric reducing capacity following DPPH and FRAP assays, respectively. It had no cytotoxic effect on Chang liver cells. C. gratissimus also significantly elevated the level of hepatic reduced glutathione (GSH), superoxide dismutase (SOD), and catalase activities as well as suppressed the malondialdehyde (MDA) level in oxidative hepatic injury. Liquid Chromatography–Mass Spectrometry (LC-MS) analysis of the herbal tea revealed the presence of 8-prenylnaringenin, flavonol 3-O-D-galactoside, caffeine, spirasine I, hypericin, pheophorbide-a, and 4-methylumbelliferone glucuronide. In silico oral toxicity prediction of the identified phytochemicals revealed no potential hepatotoxicity. Molecular docking revealed potent molecular interactions of the phytochemicals with SOD and catalase. The results suggest the hepatoprotective and antioxidative potentials of C. gratissimus herbal tea against oxidative hepatic injury

Quinoline Functionalized Schiff Base Silver (I) Complexes: Interactions with Biomolecules and In Vitro Cytotoxicity, Antioxidant and Antimicrobial Activities

A series of fifteen silver (I) quinoline complexes Q1–Q15 have been synthesized and studied for their biological activities. Q1–Q15 were synthesized from the reactions of quinolinyl Schiff base derivatives L1–L5 (obtained by condensing 2-quinolinecarboxaldehyde with various aniline derivatives) with AgNO3, AgClO4 and AgCF3SO3. Q1–Q15 were characterized by various spectroscopic techniques and the structures of [Ag(L1)2]NO3Q1, [Ag(L1)2]ClO4Q6, [Ag(L2)2]ClO4Q7, [Ag(L2)2]CF3SO3Q12 and [Ag(L4)2]CF3SO3Q14 were unequivocally determined by single crystal X-ray diffraction analysis. In vitro antimicrobial tests against Gram-positive and Gram-negative bacteria revealed the influence of structure and anion on the complexes′ moderate to excellent antibacterial activity. In vitro antioxidant activities of the complexes showed their good radical scavenging activity in ferric reducing antioxidant power (FRAP). Complexes with the fluorine substituent or the thiophene or benzothiazole moieties are more potent with IC50 between 0.95 and 2.22 mg/mL than the standard used, ascorbic acid (2.68 mg/mL). The compounds showed a strong binding affinity with calf thymus-DNA via an intercalation mode and protein through a static quenching mechanism. Cytotoxicity activity was examined against three carcinoma cell lines (HELA, MDA-MB231, and SHSY5Y). [Ag(L2)2]ClO4Q7 with a benzothiazole moiety and [Ag(L4)2]ClO4Q9 with a methyl substituent had excellent cytotoxicity against HELA cells