Antihyperglycemic and antihyperlipidemic activity of ethyl acetate fraction of Rhododendron arboreum Smith flowers in streptozotocin induced diabetic rats and its role in regulating carbohydrate metabolism

Objective:To explore and identify the most potent antihyperglycemic fraction from the ethanol extract of Rhododendron arboreum(R.arboreum)flowers.Methods:Normal and streptozotocin induced diabetic rats were treated with all four fractions of R.arboreum flowers for short term and with fraction 3 for long term study.On completion of the treatment,a range of indicators were tested including fasting blood glucose,plasma protein,haemoglobin A1C,insulin secretion,body weight,blood lipid profile and carbohydrate metabolism regulating enzymes of liver.Results:In short term study,the fraction 3(Active fraction)produced a significant(P<0.0001)reduction(73.6%)in blood glucose level at a dose of 200 mg/kg after the treatment in the diabetic rats.Administration of active fraction(200 and 400 mg/kg)once daily for 30 d in streptozotocin diabetic rats resulted in a significant(P<0.001 to P<0.0001)fall in blood glucose level,hemoglobin A1C,serum urea and creatinine with significant but a increase in insulin level similar to standard drug glybenclamide.Further,the active fraction showed antihyperlipidemic activity as evidenced by significant(P<0.001 to P<0.0001)decreases in serum serum total cholesterol,triglycerides,low density lipoprotein cholesterol and very low density cholesterol levels coupled together with elevation of high density lipoprotein cholesterol in the diabetic rats.Conclusions:The active fraction of R.arboreum flowers decreases streptozotocin induced hyperglycemia by promoting insulin secretion and glycolysis and by decreasing gluconeogenesis.

In vivo hypoglycemic investigation, antihyperglycemic and antihyperlipidemic potentials of Pereskia bleo Kunth. in normal and streptozotocin-induced diabetic rats

Objective: To elucidate the in vivo hypoglycemic capability, antihyperglycemic and antihyperlipidemic activities of Pereskia bleo(Kunth) leaves extracts and bioactive fraction. Methods: The various solvent extracts of Pereskia bleo were investigated for the hypoglycemic and antihyperglycemic activities using a relevant in vivo normal rat model and streptozotocininduced diabetic rat model with glibenclamide and metformin utilized as positive controls. The effects of the most potent extract and its bioactive fraction on the insulin level, lipid profile and body weight of the diabetic rats were also analyzed. Results: All the extracts showed no hypoglycemic effect while petroleum ether, chloroform and aqueous extracts demonstrated significant(P<0.05) reduction in blood sugar level in the intraperitoneal glucose tolerance test. Aqueous extract and aqueous fraction significantly(P<0.05) reduced the blood glucose level in streptozotocin-induced diabetic rats as early as day 6 compared to the diabetic control as well as significantly restored the serum insulin of diabetic rats. Moreover, the aqueous extract and aqueous fraction disclosed a significant(P<0.05) reduction in total cholesterol, triglycerides, and low-density lipoprotein levels. An elevation in high-density lipoprotein as well as improved body weight loss of the diabetic rats were also observed. Conclusions: In summary, Pereskia bleo appears effective in the management of diabetes and correlated impairments arising from high blood sugar level. Further studies will possibly bring about the discovery of effective and secure plant derived antidiabetic drugs.

Synchronized separation of atorvastatin——an antihyperlipidemic drug with antihypertensive, antidiabetic, antithrombotic drugs by RP-LC for determination in combined formulations

A new rapid and sensitive high performance liquid chromatography (HPLC) method has been developed for the simultaneous determination of atorvastatin—an antihyperlipidemic drug along with most commonly prescribed drugs (antihyperlipidemic, antihypertensive, antidiabetic, antithrombotic) in bulk and marketed combined formulations. The chromatographic separation was carried out by gradient elution mode with acetonitrile as organic modifier and 0.1% triethylamine acetate (TEAA) buffer pH 5 at a flow rate of 1 mL/min and a diode array detector at wavelength 230 nm was employed for detection of the analytes. Calibration curves were linear in the range of 5-150 mg/mL for all the drugs with correlation coefficients of determination (r 2 values)Z0.999. Limits of detection (LODs) and Limits of quantification (LOQs) ranged from 0.1 to 0.27 mg/mL and 0.3 to 0.89 mg/mL respectively. Intra-day and inter-day precision was studied at three concentration levels (20, 60 and 100 mg/mL). The intra-day and inter-day RSD for all compounds was less than 2.0%. The accuracy for all compounds was found to be between 98% and 102%. Thus, the performance of the method described allows its use in quantification of atorvastatin along with 9 most commonly prescribed drugs available in market as atorvastatin combined dosage forms.

Weight losing, antihyperlipidemic and cardioprotective effects of the alkaloid fraction of Hunteria umbellata seed extract on normal and triton-induced hyperlipidemic rats

Objective: To investigate the weight losing, antihyperlipidemic and cardioprotective effects of the alkaloid fraction of Hunteria umbellata(H. umbellata) seed.Methods: Adult female Wistar rats(weight range: 120-150 g) were randomly divided into 4 and 5 treatment groups in the normal and triton-induced hyperlipidemic models, respectively. and were daily treated for 14 d before they were humanely sacrificed under inhaled diethyl ether anesthesia. About 5 mL of whole blood was obtained by cardiac puncture from each treated rat, from which serum for lipids assay was subsequently separated. Tissue samples of livers of treated rats were harvested and processed for histopathological analysis.Results: Repeated daily oral treatments of normal rats with 25 and 50 mg/kg/day of alkaloid fraction of H. umbellata resulted in significant(P<0.05 and P<0.001) and dose-dependent weight loss, and decreases in the serum triglyceride, total cholesterol and low density lipoprotein cholesterol, while significantly(P<0.001) increased the serum levels of high density lipoprotein cholesterol fraction. Similarly, oral pre-treatments with 25 and 50 mg/kg/day of alkaloid fraction of H. umbellata for 14 d before induction of hyperlipidemia with triton WR-1339 significantly(P<0.01, P<0.001) and dose-dependently attenuated increases in the average body weights, serum levels of triglyceride, total cholesterol and low density lipoprotein cholesterol while also significantly(P<0.01, P<0.001) and dose-dependently attenuated significant(P<0.001) decrease in the serum high-density lipoproteincholesterol levels when compared to the untreated control values. However, the results obtained for 50 mg/kg of alkaloid fraction of H. umbellata in both normal and triton WR-1339-induced hyperlipidemic rats were comparable to that recorded for 20 mg/kg of simvastatin. Similarly, oral pretreatments with 25 and 50 mg/kg/day of alkaloid fraction of H. umbellata significantly improved the histological lesions of fatty hepatic degeneration induced by triton WR-1339 treatment.Conclusions: Overall, results of this study showed that repeated oral treatments with 25 and 50 mg/kg/day of alkaloid fraction of H. umbellata elicited weight losing, antihyperlipidemic and cardioprotective effects in triton WR-1339 induced hyperlipidemic rats that were mediated via de novo cholesterol biosynthesis inhibition.

Estimation of the novel antipyretic, anti-inflammatory, antinociceptive and antihyperlipidemic effects of silymarin in Albino rats and mice

Objective: To evaluate the other pharmacological actions of silymarin in Albino rats and mice such as antipyretic, anti-inflammatory, antinociceptive and antihyperlipidemic effects. Methods: Rats were injected intramuscularly with pyrogenic dose of brewer's yeast for the antipyretic test of silymarin. Another group of rats injected with 0.1 mL of 1% carrageenan solution in saline at the subplanter area of the right hind paw for the anti-inflammatory test of silymarin. Another group of mice tested by hot plate method for determination of antinociceptive effect of silymarin. Hyperlipidemia was induced using high fat diet for 2 months to estimate the antihyperlipidemic activity of silymarin. Results: Silymarin showed a significant antipyretic effect of both doses(50 and 100 mg/kg) compared with control untreated group. Moreover, silymarin elucidated a significant anti-inflammatory effect of both doses reflected on the decrease of the rat paw edema every hour interval for 4 h after administration in comparison with control positive group. By the same taken, both doses of silymarine revealed a significant antinociceptive action in hot plate method at 30 and 60 min post administration. Besides, it lowered significantly the serum levels of prostaglandin E2, tumor necrosis factor alpha and interleukin 1 beta after 2 h of silymarin administration in carrageenan induced rat paw edema besides the significant decrease of total cholesterol, triglycerides, low density lipoprotein and significantly elevated high density lipoprotein after 2 weeks of silymarin administration. Conclusions: These outcomes delivered a new vision into the possible pharmacological mechanisms by which silymarin advances antipyretic, anti-inflammatory, antinociceptive and antihyperlipidemic effects.

Evaluation of antihyperlipidemic effect of Polygonum minus,a South East Asian salad plant in poloxamer 407-induced acute hyperlipidemic rats

OBJECTIVE To investigate the antihyperlipidemic effect of methanol and aqueous extracts of the leaves of Polygonum minus in acute hyperlipidemic rat model.METHODS Acute hyperlipidemia was chemically induced in Sprague Dawley rats by using poloxamer 407(500mg·kg-1 of body weight;intraperitoneal).Increase in total cholesterol was confirmed after six hours of induction.The normal and hyperlipidemic control groups were administered with 1mL carboxymethylcellulose(CMC),the two test groups received aqueous and methanol extract of leaves of P.minus respectively(1000mg·kg-1;orally;suspended in 1% CMC)whereas reference standard treated group received atorvastatin(60mg·kg-1;orally;suspended in 1% CMC)once daily for 3consecutive days.Blood samples were collected at 10 th and 24 th hour of the study for total cholesterol and triglycerides determination,while terminal blood samples were collected at58 th hour for full lipids profile analysis.RESULTS In the present study,both methanol and aqueous extracts lowered the serum total cholesterol and triglycerides significantly(P<0.001 and P<0.05,respectively)when compared with the hyperlipidemic control,similar to the standard drug atorvastatin.Varying effects were observed for both extracts on the other lipid parameter studied.Methanol extract showed significant reduction in LDL(P<0.05),VLDL(P<0.01)and atherogenic index(AI;P<0.001)and it showed a significant elevation in HDL levels(P<0.05).On the other hand,the aqueous extract showed significant reduction only in VLDL and AI(P<0.05)but no increase in HDL levels.CONCLUSION Present study confirmed the antihyperlipidemic effect of leaves of P.minus in acute hyperlipidemic rat model.The study also suggested that the methanol extract possess higher antihyperlipidemic effect than aqueous extract.Currently a study is ongoing to evaluate the antihyperlipidemic effect of the methanol extract in high-fat diet-induced chronic hyperlipidemic rat model.

Antihyperglycemic,antihyperlipidemic and antioxidant effects of standard ethanol extract of Bombax ceiba leaves in high-fat-diet-and streptozotocin-induced Type 2 diabetic rats

The present study aimed at exploring the therapeutic potential of standard extract of Bombax ceiba L.leaves(BCE) in type 2 diabetic mellitus(T2DM).Oral administration of BCE at doses of 70,140,and 280 mg·kg^(-1),to the normal rats and the high-fat-diet-and streptozotocin-induced T2 DM rats were carried out.Effects of BCE on blood glucose,body weight,and a range of serum biochemical parameters were tested,and histopathological observation of pancreatic tissues was also performed.HPLC-ESI-Q/TOF-MS/MS analysis indicated that the chemical composition of BCE mainly contained mangiferin,isoorientin,vitexin,isomangiferin,isovitexin,quercetin hexoside,2'-trans-O-cumaroyl mangiferin,and nigricanside.BCE caused a significant decrease in the concentrations of fasting blood glucose,glycosylated hemoglobin,total cholesterol,triglyceride,low density lipoprotein-cholesterol,serum insulin,and malondialdehyde,and increases in oral glucose tolerance,high density lipoprotein-cholesterol,and superoxide dismutase in the T2 DM model rats.Moreover,considerable pancreatic β-cells protection effect and stimulation of insulin secretion from the remaining pancreatic β-cells could be observed after BCE treatment.The results indicated that BCE exhibited an excellent hypoglycemic activity,and alleviated dyslipidemia which is associated with T2 DM.Antioxidant activity and protecting pancreatic β-cells are the possible mechanisms involved in anti-diabetic activity of BCE.

Chemical Constituents with Antihyperlipidemic Activities from Desmodium triquetrum

Objective To study the chemical constituents from Desmodium triquetrum and their antihyperlipidemic activities. Methods The constituents of D. triquetrumwere isolated and purified using various column chromatographies. Their chemical structures were elucidated using extensive spectroscopic methods. The lipid-lowering effects of the isolates were evaluated in HepG2 cells. Results Nine compounds were obtained from the ethanol extract of D. triquetrum and determined to be 6＇-O-cis-p-coumaroyl- 3,5-dihydroxyphenyl-β-D-glucopyranoside （1）, tadehaginoside （2）, rutin （3）, quercetin-3-O-β-D-glucopyranoside （4）, quercetin-3-O-β-D-galactopyranoside （5）, 6-O-（E）-p-hydroxy-cinnamoyl-β-glucose （6）, 6-O-（E）-p-hydroxy-cinnamoyl-α-glucose （7）, kaempferol-3-O-β-D-rutinoside （8）, and 3-O-β-D-galacopyranosyl （6-1）-α-L- rhamnosyl quercetin （9）. Compounds 1 and 2 significantly reduced the intracellular content of total cholesterols and triglycerides. Conclusion Compound 1 is a new phenolic compound and exhibits potent anti-hyperlipidemic activity. Additionally, compounds 6 and 7 are isolated from D. triquetrum for the first time.

Clinical Observation on Hyperlipemia Treated with Antihyperlipidemic Decoction

Objective： To observe the therapeutic effect of antihyperlipidemic decoction on hyperlipemia. Methods： 77 hyperlipemia patients are selected and randomly divided into two groups. 37 cases in the treatment group received the treatment of antihyperlipidemic decoction, and 40 cases in the control group received western medicine, zhinbiticose. The course of treatment for both groups was 8 weeks. Results： The difference in total effective rate between the two groups was significant （P〈0.05）. Conclusion： Antihyperlipidemic decoction has a better therapeutic effect for hvoerlioemia, with a lower recurrence rate and less side effect.

Antihyperglycemic activity,antihyperlipedemic activity,haematological effects and histopathological analysis of Sapindus mukorossi Gaerten fruits in streptozotocin induced diabetic rats

Objective:To investigate the antihyperglycemic and antihyperlipidemie properties of hydroalcoholic extract of fruits of Sapindus mukorossi Caerlen and its beneficial effect on haeniatological parameters with histopathological analysis in streptpzotocin induced diabetic rats.Methods:Sapindus mukorossi fruits extract(250 and 500 mg/kg body weight) and standard drug glybenclamide(0.5 mg/kg body weight) were administered to diabetic rats.Effect of extract on hyperglycemia,hyperlipidemia and hematological parameters was studied in diabetic rats.Histopathological changes in diabetic rat pancreas were also observed after extract and glybenclamide treatment.Results:Daily oral administration of Sapindus mukorossi fruits extract(250 and 500 mg/kg body weight) and glybenclamide for 20 days showed beneficial effects on blood glucose level(P【0.01) and lipid level.The extract has a favorable effect on the histopathological changes of the pancreas in streptozotocin induced diabetes.Conclusions: These findings reveal that the hydroalcoholic extract of Sapindus mukorossi fruits extract possesses antihyperglycemic and antihyperlipidemie properties.In addition.the extract can prevent various complications of diabetes and improve some haeniatological parameters.

Antidiabetic activity of aqueous root extract of Merremia tridentata(L.) Hall,f.in streptozotocin-induced—diabetic rats

Objective:To investigate the antidiabetic effect of aqueous extract of Merremia Iridentala (M.tridentala) root(MTRAE) in normal,glucose-loaded hyperglycemic and streptozotoein(STZ)induced diabetic rats.Methods:Oral administration of MTRAE at the doses of 50,100 and 150 nig/kg was studied in normal,glucose-loaded and STZ-diabetie rats.The three doses caused significant reduction in blood glucose levels in all the models.Results:The effect was more pronounced in 100 and 150 mg/kg than 50 mg/kg.MTRAK also showed significaut increase in serum insulin,body weight and glycogen content in liver and skeletal muscle of STZ-induced dialietie rats while there was significant reduction in the levels of serum triglyceride and total cholesterol.MTRAE also showed significant antilipidperoxidative effect in the pancreas of STZinduced diabetic rats.The antidiabetic effect of M.tridentata was compared with glibenclamide. a well known hypoglycemic drug.Conclusions:The results indicate that aqueous extract of M. tridentata root possesses significant antidiabetic activity.

Lipid-lowering effect of Oroxylum indicum(L.)Kurz extract in hyperlipidemic mice

Objective:To investigate the effect of Oroxylum indicum fruit extract on high-fat diet-induced hyperlipidemic mice.Methods:The phytochemical composition of Oroxylum indicum fruit extract was determined by liquid chromatographymass spectrometry/mass spectrometry(LC-MS/MS)and gas chromatography-mass spectrometry.Forty-two male mice were used.The mice were divided into six groups:normal control,high-fat diet control,simvastatin treatment(20 mg/kg BW/day),and Oroxylum indicum fruit extract(100,200,300 mg/kg BW/day)treatment groups.Food intake,body weight,serum parameters,lipid profile,and histopathological lesions of the kidney,liver,and epididymal fat were observed.Results:LC-MS/MS results revealed four major components of Oroxylum indicum fruit extract:luteolin,apigenin,baicalein,and oroxylin A.Twenty-seven volatile oils were identified from Oroxylum indicum fruit extract.Daily oral administration of Oroxylum indicum fruit extract at 100 to 300 mg/kg BW/day significantly reduced the body weight,total cholesterol,triglyceride,and low-density lipoprotein cholesterol level(P<0.05),whereas high-density lipoprotein cholesterol was higher than the high-fat diet control group.Treatment with 300 mg/kg BW/day Oroxylum indicum fruit extract reduced the pathological lesion and prevented fat accumulation in the kidney and liver.Conclusions:Oroxylum indicum fruit extract has hypolipidemic effect in hyperlipidemic mice,and the active ingredients of Oroxylum indicum fruit extract,both flavonoids and volatile oils,should be further explored as an antihyperlipidemic agent.

Effects of soy hull polysaccharide on dyslipidemia and pathoglycemia in rats induced by a high-fat-high-sucrose diet

The present work aimed at investigating the effects of soy hull polysaccharide(SHP)in alleviating adverse effects in rats fed a high-fat-high-sucrose diet.After SHP feeding for 4 weeks,the fasting blood glucose(FBG),serum triglyceride(TG),serum high-density lipoprotein cholesterol(HDL-C),short chain fatty acids(SCFAs),and 16S rDNA gene sequence were determined.Administration of SHP significantly decreased body fat content and TG levels,and increased water intake and HDL-C levels after 4 weeks of treatment.The antihyperglycemic effect of SHP at a dose of 400 mg/kg mb had the most significant effects among the three dosage groups.SHP notably restored the FBG in rats fed a high-fat-high-sucrose diet(P<0.05).Furthermore,SHP at 400 mg/kg mb increased the abundance of Bacteroidetes and decreased that of Firmicutes and Actinobacteria at the phylum level.The polysaccharide treated groups had significantly higher content of total SCFAs,and the main fermentation products were acetic,propionic,n-valeric and i-valeric acids.Thus,SHP restores blood lipid levels in rats fed a high-fat-high sucrose diet through regulation of the gut microbiota.

Supplements of an aqueous combination of Justicia adhatoda and Ocimum tenuiflorum boost antioxidative effects and impede hyperlipidemia

Background: Justicia adhatoda and Ocimum tenuiflorum, locally known as bashok and tulsi, are two ethnomedicinally important herbs that have been using as dietary supplements for several therapeutic applications. This study evaluated the combined effect of both the herbs as an antioxidative and antihyperlipidemic agent.Methods: Antihyperlipidemic effect was assessed in a high-fat diet-induced hyperlipidemic model in Wistar albino rats. The rats were treated orally with extracts of bashok(J adhatoda, 200 mg/kg bw), tulshi(O tenuiflorum, 200 mg/kg bw), and a combination of bashok and tulshi(50:50), as well as with a reference drug, atorvastatin(10 mg/kg/day), with or without high-fat diet for 14 days. The antioxidative effect was studied using established in vitro models. The studies were supported by experimentally testing the effects of the extracts on membrane stabilization and inhibition of protein denaturation.Results: The results showed that the serum lipid profile was significantly decreased in the different treatment groups, with bashok having the greatest effect. Body weights, total serum protein, LDH, and relative liver and adipose tissue weights were markedly restored towards baseline values, the lowest atherogenic index being achieved with the combined extract. The combination treatment significantly enhanced total phenolic content and antioxidative capacity and greatly potentiated membrane stabilization, but inhibition of protein denaturation was not significantly affected.Conclusion: The data demonstrate that a combination of Justicia adhatoda and Ocimum tenuiflorum could be developed as a food supplement with antioxidative and antihyperlipidemic benefits.

“Diabegon”, a safe and effective polyherbal therapy for type 2 diabetes mellitus

AIM: To investigate the antihyperglycemic, antihyperlipidemic and antioxidant functions of a polyherbal formulation, "Diabegon", in human subjects with type 2 diabetes mellitus.METHODS: A total of 33 human subjects with type 2 diabetes mellitus were recruited for the study and all anthropological and biochemical parameters were recorded at the time of registration. The subjects were given hot water extract obtained from 10 gm of "Diabegon" powder, "Diabegon kwath", on an empty stomach everyday in the morning under personal supervision for 6 mo. The therapeutic functions of the "Diabegon kwath" was assessed by monitoring the blood glucoselevels at monthly intervals and glycosylated hemoglobin, lipid profile and biomarkers of oxidative stress, liver and kidney function markers at three monthly intervals in the study subjects. RESULTS: Daily administration of hot water extract of "Diabegon" regularly for 6 mo resulted in significant reductions of blood glucose and glycosylated hemoglobin levels. There was also a significant increase in high density lipoprotein cholesterol levels with concomitant decreases in total cholesterol, triglycerides, low density lipoprotein cholesterol and very low density lipoprotein. A significant improvement in glycosuria and proteinuria was also observed. Also, the subjects exhibited a significant improvement in enzymatic and nonenzymatic biochemical markers of oxidative stress. The kidney and liver functions remained normal and in fact improved in many subjects.CONCLUSION: The study which is first of its kind, advocates "Diabegon kwath" as a safe and effective Ayurvedic therapy for the treatment of human type 2 diabetes mellitus and further placebo controlled trial may substantiate the therapeutic efficacy of the formulation.

In vivo activities of the structured lipids-1,3-dioleic acid 2-palmitic acid triglyceride(OPO)in high-fat diet mice

High-energy diets and lipid metabolism can lead to high levels of total cholesterol,a decrease in antioxidant,enzyme activity,and an increase in oxidative stress and dyslipidemia biomarker.In this study,the in vivo antihyperlipidemic and antioxidant effects of 1,3-dioleoyl-2-palmitoyl triglyceride(OPO)using a high fat-diet model were investigated.The mice were divided into groups including high-fat model group(HF),auxiliary group(AG),positive Control group(PC),low OPO dose group(LO),medium OPO dose group(MO)and high OPO.OPO was administrated to 60 hyperlipidemia induced male Kunming mice at the dosage of 200,400 and 800 mg/kg•d body weight,for 35 days.The results showed that the administration of OPO decreased the body weight from 43.92 g in HF to 37.74 g in HO group,liver index from 3.94%in HF to 3.43 in HO group and kidney index from 1.38 in HF%to 1.17%in HO group.The administration of OPO significantly decreased hyperlipidemia mice's serum triglyceride,total cholesterol,and low-density lipoprotein cholesterol levels at P<0.05.High-density lipoprotein cholesterol levels were increased with reductions of visceral hypertrophy and fat accumulation in model mice.Furthermore,in the HO group,superoxide dismutase,catalase and glutathione peroxidase levels increased significantly by 27.39,38.33 and 22.90%at(P<0.05),respectively.OPO also significantly reduced the enzyme activity of aspartate aminotransferase and alanine aminotransferase in serum at P<0.05.These findings suggested that OPO has potential use in hyperlipidemia treatment and other health-related complications.