Evaluation of the diuretic potentials of naringenin in hypercholesterolemic rats

Purpose: To investigate the diuretic potentials of naringenin (NGN) in obesity induced in rats by high fat diet (HFD).Methods: To prepare HFD, normal pellet diet was crushed and thoroughly mixed with cholesterol powder (1 % w/w). The mixture was mixed with some water and made into pellets which were then oven-baked to dry. Four groups of male Wistar albino rats (n = 6) were used for the study. Normal control (group I) received normal pellet diet. Group 2 (HFD-only) was fed HFD for 28 days, while Groups 3 and 4 were co-administered HFD and NGN at doses of 50 and 100 mg/kg, respectively. All treatments were given orally, and lasted for 28 days. Twenty-four hours after the last dose of NGN, blood was collected from all rats and total cholesterol levels determined to confirm obesity. Thereafter, the rats were placed in metabolic cages and urine samples were collected at two time-points (5 and 24 h) for measurement of urine volume, urinary pH, conductivity and electrolyte levels (Na, K and Cl).Results: Treatment with HFD resulted in significantly (p < 0.05) increased serum cholesterol level (178.83 ± 5.43 mg/dL) when compared to normal control rats (88.17 ± 4.04 mg/dL). It also led to decrease in urinary volume (~50 %) at both time points (5 and 24 h) and in excretion of urinary electrolytes (sodium, potassium and chloride ions). However, the changes in these parameters were significantly reversed by NGN administration (p < 0.05).Conclusion: These results demonstrate the diuretic activity of NGN in HFD-induced obese rats. Thus, NGN can be further explored for use in combination with hypolipidemic agents to tackle obesity.Keywords: High-fat diet, Hypercholesterolemia, Naringenin, Obesit

Moringa oleifera Lam. (family Moringaceae) leaf extract attenuates high-fat diet-induced dyslipidemia and vascular endothelium dysfunction in Wistar albino rats

Purpose: To investigate the protective effect of methanol extract of Moringa oleifera leaves (MEMO) in high-fat diet (HFD)-induced dyslipidemia and vascular endothelium dysfunction. Methods: Dose-dependent attenuating effect of MEMO was tested at doses of 200 and 400 mg/kg/day in an in vivo model of HFD-induced dyslipidemia using rats whereas vascular endothelial reactivity was assessed in isolated rat aorta using ex vivo organ bath setup. Results: MEMO administration in HFD-induced dyslipidemic rats for 3 consecutive weeks, resulted in significant decrease in rat body weight, LW/BW and RFPW/BW ratio when compared to rats treated with HFD only where an increase in body weight was observed. Decrease in the average daily feed intake and significant reductions in waist, Lee index and BMI was also observed after MEMO treatment in HFD-induced dyslipidemic rats. Lipid profile data indicate that HFD group showed significant increase in total cholesterol, triglyceride, LDL and VLDL levels while HDL levels decreased significantly. On the other hand, MEMO treatment improved lipid profile compared to HFD group. Ex-vivo isolated aorta results revealed that MEMO treatment reversed HFD-induced endothelium dysfunction when compared to SD group. Conclusion: MEMO treatment produces dose-dependent improvement in lipid profile and vascular endothelium protection, thereby rationalizing its traditional medicine use in the treatment of dyslipidemia and cardiovascular related endothelial disorders

Target Based Designing of Anthracenone Derivatives as Tubulin Polymerization Inhibiting Agents: 3D QSAR and Docking Approach

Novel anthracenone derivatives were designed through in silico studies including 3D QSAR, pharmacophore mapping, and molecular docking approaches. Tubulin protein was explored for the residues imperative for activity by analyzing the binding pattern of colchicine and selected compounds of anthracenone derivatives in the active domain. The docking methodology applied in the study was first validated by comparative evaluation of the predicted and experimental inhibitory activity. Furthermore, the essential features responsible for the activity were established by carrying out pharmacophore mapping studies. 3D QSAR studies were carried out for a series of 1,5- and 1,8-disubstituted10-benzylidene-10H-anthracen-9-ones and 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-one derivatives for their antiproliferation activity. Based on the pattern recognition studies obtained from QSAR results, ten novel compounds were designed and docked in the active domain of tubulin protein. One of the novel designed compounds “N1” exhibited binding energy −9.69 kcal/mol and predicted Ki 78.32 nM which was found to be better than colchicine

Role of Oxidative Stress and Inflammatory Cytokines (TNF-α and IL-6) in Acetic Acid-Induced Ulcerative Colitis in Rats: Ameliorated by Otostegia fruticosa

Ulcerative colitis (UC) is an inflammatory bowel disease (IBD) that causes irritation, inflammation, and ulceration in the linings of the colon and rectum. Otostegia fruticosa is traditionally used to treat various disorders in different parts of the Middle East and sub-Saharan Africa. In the present study, we evaluated the ameliorative effects of crude leaves extract of O. fruticosa (OF.Cr) on acetic acid (AA)-induced UC model in Wistar albino rats. Wistar rats were administered orally with either vehicle (10 mL/kg), OF.Cr (200 and 400 mg/kg), or prednisolone (2 mg/kg) once a day for 6 days. On day 6, UC was induced in rats by intrarectal administration of a single dose of 5% AA (1.0 mL). Disease activity index (DAI) was recorded after one day of colitis induction by assessing the symptoms of colitis and then the rats were euthanized by cervical dislocation, and colon tissues were isolated for the histopathological examination and biochemical analysis of oxidative stress parameters and cytokines (Interleukin-6 and Tumor Necrosis Factor-α). OF.Cr pretreatment exhibits significant prevention against UC, as confirmed by a significant decrease of DAI, colonic ulceration, and reduced inflammatory score as compared to the AA-induced colitis rats. Depletion of total glutathione (GSH) levels and catalase (CAT) activities in the colitis group was significantly restored in the OF.Cr treated groups, while increased lipid peroxidation in the colon tissues was significantly reduced. OF.Cr prevented the activation of the IL-6 and TNF-α pathways in the colonic tissues, which were clearly observed by the decreased levels of IL-6 and TNF-α in the OF.Cr treated animals. Hence, OF.Cr could be developed in the future for the treatment of UC

Role of Oxidative Stress and Inflammatory Cytokines (TNF-α and IL-6) in Acetic Acid-Induced Ulcerative Colitis in Rats: Ameliorated by <i>Otostegia fruticosa</i>

Ulcerative colitis (UC) is an inflammatory bowel disease (IBD) that causes irritation, inflammation, and ulceration in the linings of the colon and rectum. Otostegia fruticosa is traditionally used to treat various disorders in different parts of the Middle East and sub-Saharan Africa. In the present study, we evaluated the ameliorative effects of crude leaves extract of O. fruticosa (OF.Cr) on acetic acid (AA)-induced UC model in Wistar albino rats. Wistar rats were administered orally with either vehicle (10 mL/kg), OF.Cr (200 and 400 mg/kg), or prednisolone (2 mg/kg) once a day for 6 days. On day 6, UC was induced in rats by intrarectal administration of a single dose of 5% AA (1.0 mL). Disease activity index (DAI) was recorded after one day of colitis induction by assessing the symptoms of colitis and then the rats were euthanized by cervical dislocation, and colon tissues were isolated for the histopathological examination and biochemical analysis of oxidative stress parameters and cytokines (Interleukin-6 and Tumor Necrosis Factor-α). OF.Cr pretreatment exhibits significant prevention against UC, as confirmed by a significant decrease of DAI, colonic ulceration, and reduced inflammatory score as compared to the AA-induced colitis rats. Depletion of total glutathione (GSH) levels and catalase (CAT) activities in the colitis group was significantly restored in the OF.Cr treated groups, while increased lipid peroxidation in the colon tissues was significantly reduced. OF.Cr prevented the activation of the IL-6 and TNF-α pathways in the colonic tissues, which were clearly observed by the decreased levels of IL-6 and TNF-α in the OF.Cr treated animals. Hence, OF.Cr could be developed in the future for the treatment of UC

Comparative study of subchronic toxicities of mosquito repellents (coils, mats and liquids) on vital organs in Swiss albino mice

The aim of the current study was to evaluate and compare the toxicities of different types of mosquito repellents i.e. coils, mats and liquid vapors in animal models. Different types of mosquito repellents including liquid vaporizers, coils and mats have been extensively used by the people to get protection from the mosquitoes and diseases associated with them. The active constituents of these repellents include; allethrins, pyrethrins, paraffin and various other derivatives, are well known for their toxicities. Exposure of albino mice to these repellents for 3 h per day over a period of 20 days produced significant toxicological effects on vital body organs including; liver, lungs, kidneys, brain and heart. The order of toxicity of different repellents on nervous and hepatic tissues was found to be: Coil > Liquid > Mat while in renal and cardiac tissues, the coil was again found to be the most toxic one, mat with medium toxicity whereas liquid as least toxic (Coil > Mat > liquid). Lungs tissues are almost equally affected by all the repellants. On the basis of current findings, it has been concluded that exposure to various types of mosquito repellents can be deleterious to health and can cause various health related issues by producing pathological changes in the vital organs. Keywords: Allethrin, Mosquito repellents, Subchronic toxicity, Vital organs, Mic

Antihyperglycemic and Antihyperlipidemic Effects of Ferula duranii in Experimental Type 2 Diabetic Rats

WOS: 000369214000002In the present study, DPPH radical scavenging assay and ferric-reducing antioxidant assay were used to evaluate in vitro antioxidant potential of the methanol extract of Ferula duranii (F. duranii). The antihyperglycemic and antihyperlipidemic activities of F. duranii extract were evaluated in streptozotocin (STZ)-induced diabetic rats. F. duranii showed considerable antioxidant potential in the DPPH radical scavenging assay and minimum reducing power in ferric-reducing antioxidant power assay. A meaningful reduction in the concentrations of Fasting Blood Glucose (FBG), glycosylated hemoglobin (Hb Alc), triglycerides (TG), Total Cholesterol (TC) and Low Density Lipoprotein (LDL-C) in plasma and an elevation in the activity of superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT) in hepatic and pancreas homogenates were observed in diabetic animals medicated with F. duranii extract in comparison with diabetic control rats. The level of insulin raised significantly in plasma of diabetic groups received F. duranii in respect to diabetic control one. Levels of alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), bilirubin, total protein and High Density Lipoprotein (HDL-C) in plasma and malondialdehyde (MDA) in liver and pancreas homogenates were recovered significantly in F. duranii-medicated diabetic rats in comparison with diabetic controls. The present data suggest that F. duranii has both antidiabetic and antihyperlipidemic effects.Deanship of Scientific Research, Prince Sattam Bin Abdulaziz University, Al-Kharj, KSA [2014/01/787]This project was supported by Support Research Projects with Global Partnership Program, Deanship of Scientific Research, Prince Sattam Bin Abdulaziz University, Al-Kharj, KSA. Grant No. 2014/01/787. The authors would like to express their gratitude to the Deanship of Scientific Research at Prince Sattam bin Abdulaziz University Al-Kharj, for their assistance