Injection Of Triton WR-1339 Research Articles

Exploring Therapeutic Potential of Pleurotus ostreatus and Agaricus bisporus Mushrooms against Hyperlipidemia and Oxidative Stress Using Animal Model.

The mushrooms oyster (Pleurotus ostreatus) and white button (Agaricus bisporus) contain bioactive compounds that have potential beneficial effects on hypercholesterolemia and cardiovascular diseases. In this study, hypolipidemic and antioxidative potential of these mushrooms' extract were explored using hypercholesterolemic (HC) rats as animal model. For the study, 56 adult rats were divided into seven groups, i.e., G1 (negative control), G2 (positive control group), G3 (HC rats with statin drug orally), G4 and G5 (HC rats @ 100 and 200 mg/kg body weight (BW) dose of oyster mushroom extracts), and G6 and G7 (HC rats @ 100 and 200 mg/kg BW dose of white button mushroom extracts). The hypercholesterolemia was induced experimentally in fasted rats through a high-fat diet along with injection of triton WR-1339. After 48 h, the treatment groups were given extract for 28 days along with standard diet. At the trial termination, we analyzed the blood sugar levels, antioxidant parameters, lipid profile, and renal function, as well as conducting liver function tests of the rats. The results indicated that positive control group rats exhibited increased levels of total cholesterol (TC), triglycerides (TG), low-density level (LDL), and very-low-density level (vLDL) by 19%, 37%, 52%, and 32%, respectively, and 53% decrease in HDL, whereas treatment groups that received 200 mg oyster and white button mushroom extracts reported 15%, 34%, 22% reduction in TC, TG, vLDL, respectively, and 22% improvement in HDL level. The enzyme profiles of different groups showed non-significant differences, although both mushroom extracts provision reduced glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) levels. Overall, the results indicated that mushroom extracts were helpful in maintaining oxidative stress and have the potential to improve dyslipidemia in the tested rat animal model.

Antihyperlipidemic Bioactivity Guided Isolation and Structural Elucidation of Isolated Phytoconstituents from Convolvulus pluricaulis Choisy

Background: Atherosclerosis is a crucial element in the origination of coronary heart disease (CHD). Lipid aggregation inside the coronary arteries walls lead to the occurrence of hyperlipidemia. Aim: The research was conducted for assessing the lipid lowering effect of ethanol extract and chloroform fraction from Convolvulus pluricaulis Choisy. aerial parts in Triton induced hyperlipidemic rat model. Methodology: The active fraction was obtained from antihyperlipidemic bioactivity. The phytocomponents were separated from the active fraction using flash chromatography technique resulting in the isolation of n-hexatriacontane; 9-octadecenoic acid- octyl ester; 12, 14-heptacosanedione; dodecyl-octadeca-9,12-dienoate; tetracosanyl 9-hexadecenoate; heptacosan-14-ol; stigmasta- 5, 22- dien-3 beta-ol and stigmast-5-en-3 beta-ol. The phytocomponent structures were established by spectral data analysis. Intraperitoneal (i.p.) injection of Triton WR- 1339 at a dose of 400 mg/kg body weight (b.w.) was given to the animals. The ethanol extract at a dose of 200 mg/kg b.w. and chloroform fraction at a dose of 400 mg/kg b.w. were administered orally in rats after 24 hours of the Triton administration. Results: The study resulted in dose dependent inhibition of triglycerides (p <0.01), total cholesterol (p <0.05), Low density lipoprotein level (p <0.05) while significant increased HDL (p <0.01) level. Alteration in lipid profile in Triton treated rats was restored and found more effective in the chloroform fraction probably due to the presence of phytocomponents. The study elucidated different phytocomponents isolated from the active chloroform fraction of C. pluricaulis. Conclusion: Treatment with extract and fraction manifested significant decrease in triglyceride level. HDL exerts an inhibitory action in the etiology of atherosclerosis. It is considered as a beneficial lipoprotein and its lower level leads to the greater risk of CHD. It may be concluded that the isolated components were responsible for the lipid lowering level of active fraction. GRAPHICAL ABSTRACT

Phytochemical analysis and bioactivity evaluation of Moroccan Thymus atlanticus (Ball) fractions

This study aims to evaluate the effect of polar and less polar fractions of Thymus atlanticus (T. atlanticus) on inflammation and hyperlipidemia in animal models, and on coagulation and lipid peroxidation in vitro. Polar and less polar fractions of T. atlanticus were analyzed by HPLC and their antioxidant activities were evaluated using different in vitro methods. The anti-inflammatory effect was tested using arachidonic acid and xylene-induced inflammation tests in animal models. Acute hyperlipidemia was induced in mice by an intraperitoneal injection of Triton WR-1339. After 24h, plasma was collected to analyze lipid profile. The effect of the fractions and heparin on coagulation of the rabbit blood was explored in vitro by partial thromboplastin time, prothrombin time and thrombin time tests. The results indicated that rosmarinic acid was the main phenolic acid. All fractions significantly protected plasma lipids against oxidation. The ethyl acetate fraction significantly inhibited inflammation induced by arachidonic and xylene in mice and rat, respectively. The administration of fractions at a dose of 2 g/kg body weight markedly decreased plasma total cholesterol, triglycerides and LDL-C but only the aqueous fraction increased the level of HDL-C in hyperlipidemic mice. The blood coagulation was completely inhibited even at very low concentration of fractions (280 µg/mL of plasma). T. atlanticus could be a source of potential lipid-lowering and anti-inflammatory compounds.

Effect of polyphenol, flavonoid, and saponin fractions from Thymus atlanticus on acute and chronic hyperlipidemia in mice

BackgroundThymus atlanticus is an endemic plant of the Mediterranean region, which has been used in the Moroccan mountain area to treat several diseases. This study aimed to investigate the effect of polyphenol, flavonoid, and saponin fractions derived from this plant on acute and chronic hyperlipidemia in male albino mice.ResultsThe results indicated that the injection of Triton WR-1339 (20 mg/100 g body weight (B.wt.)) and 6-week administration of a high-fat diet (which is an 81.8% standard diet supplemented with 2% cholesterol, 16% lard, and 0.2% cholic acid) significantly increased plasma total cholesterol, triglycerides and low-density lipoprotein cholesterol (LDL-C), but did not affect high-density lipoprotein cholesterol (HDL-C) levels in mice. Administration of a single dose (2 mg/kg B.wt.) of polyphenol, flavonoid, or saponin fractions significantly suppressed the effect of Triton injection on plasma total cholesterol, triglycerides, and LDL-C. In addition, the supplementation of the high-fat diet with polyphenol fraction (2 mg/kg B.wt./day) prevented the increase of total cholesterol, triglycerides, and LDL-C, and effectively increased HDL-C level when compared to mice feeding only the high-fat diet.ConclusionIn conclusion, phenolic compounds from Thymus atlanticus possess a significant hypocholesterolemic and hypotriglyceridemic effects and, therefore, could have an important role in the management of dyslipidemia.

Perinatal Taurine Supplementation Prevents the Adverse Effects of Maternal Dyslipidemia on Growth and Cardiovascular Control in Adult Rat Offspring.

Maternal dyslipidemia induces metabolic and cardiovascular disorders in adult offspring. This study tests the hypothesis that perinatal taurine supplementation prevents the adverse effects of maternal dyslipidemia on growth and cardiovascular function in adult rat offspring. Female Wistar rats were fed normal rat chow and water with (Dyslipidemia) or without dyslipidemia induction (Control) by intraperitoneal Triton WR-1339 injection, three times a week for 4weeks. The female Control and Dyslipidemia rats were supplemented with (Control+T, Dyslipidemia+T) or without 3% taurine in water from conception to weaning. After weaning, male and female offspring were fed normal rat chow and water throughout the experiment. At 16weeks of age, body weights significantly increased in male but not female Dyslipidemia compared to other groups, while visceral fat content significantly increased in both male and female Dyslipidemia groups. Further, both sexes displayed similar high fasting blood sugar and normal plasma leptin levels among the groups. While plasma total cholesterol and triglycerides significantly increased only in female Dyslipidemia, low-density lipoprotein cholesterol increased in both male and female Dyslipidemia groups. Mean arterial pressures and heart rates significantly increased, while baroreflex sensitivity decreased in male and female Dyslipidemia compared to all other groups. High-density lipoprotein cholesterol did not significantly different among male or female groups. These changes of the male and female Dyslipidemia group were ameliorated by perinatal taurine supplementation. The present study indicates that perinatal taurine supplementation prevents the adverse effects of maternal dyslipidemia on growth and cardiovascular function in both male and female, adult offspring.

Synthesis and in Vivo Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats.

A new series of imidazole-5-carboxamide derivatives were prepared and tested for their anti-hyperlipidemic activity in Triton-WR-1339-induced hyperlipidemic Wistar rats. The purpose of this research was to improve benzophenone carboxamides water solubility maintaining at the same time the antihyperlipidemic activity. Compounds 4, 6, 10, and 11 were synthesized through a coupling reaction between imidazoles-5-carbonyl chloride and amino benzophenones. The tested animals (n=48) were divided into six groups: the first group (hyperlipidemic control group; HCG) received an intraperitoneal injection (i.p.) of (300 mg/kg) Triton WR-1339. The second group received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of bezafibrate (100 mg/kg) (bezafibrate; BF). The third, fourth, fifth, and sixth groups received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of (30 mg/kg) of compounds 4, 6, 10, and 11, respectively. At a dose of 30 mg/kg body weight compounds 4, 6, 10, and 11 significantly (p<0.0001) decreased the plasma level of triglyceride (TG), low-density lipoprotein (LDL) and total cholesterol (TC) levels after 18 h of treatment. Additionally, compounds 4, 6, 11 and bezafibrate (100 mg/kg) significantly (p<0.0001) increased the plasma level of high-density lipoprotein (HDL) levels, which is known for its preventive role against atherogenesis. These results demonstrate the possibility of pharmacokinetic properties improvement maintaining the biological and pharmacological profile of these compounds.

Assessment of Antihyperlipidemic and Antitumor Effect of Isolated Active Phytoconstituents from Apium graveolens L. through Bioassay-Guided Procedures

ABSTRACTThe seeds of A. graveolens yielded coumarin derivatives such as seselin, methoxsalen, and 3H-isobenzofuran-1-one through chromatographic separation techniques. The structure of the components has been established on the basis of spectral data analysis. The present study was undertaken to explore the antihyperlipidemic and antitumor effects of ethanolic extract and phytoconstituents of A. graveolens in rodents. Albino rats were administered intraperitoneal (i.p.) injection of Triton WR 1339 for the induction of hyperlipidemia at a dose of 400 mg/kg body weight. After 24 h of Triton administration, the test drugs were administered orally at dose of 50 mg/kg body weight in rats. The extract and isolated components were further investigated for the tumor take inhibitory activity in hybrid mice (of C57BL strain + Swiss albino strain). Preventive group animals were injected daily with the extract and isolated components at a dose of 50 mg/kg body weight i.p. for 10 consecutive days. The animals were observed for the growth of tumor after injection of B16F10 melanoma cells into the dorsal skin of mice. The study showed significant reduction in total cholesterol (p < .001), triglycerides (p < .001) and low-density lipoprotein (LDL) level (bp < .01) and significantly increased high density lipoprotein (HDL) level (p < .01) after the treatment. Pretreatment showed delay in tumor growth by increasing the volume-doubling time (p < .01), growth delay (p < .01), and mean survival time (p < .001). Acute treatment caused stimulatory effect on HDL level and inhibition in total cholesterol (TC) and triglyceride (TG) elevation induced by Triton. Tumor regression studies showed a regression response for tumor growth in vivo of murine mouse melanoma tumor cell lines.

Biochemical and Histological effects of Aqueous extract of &lt;i&gt;Cyperus Esculentus&lt;/i&gt; in Triton Wr-1339 Induced Hyperglycemic Rats.

Researchers and physicians look forward to effective therapeutic agents possibly from medicinal plants following the ineffectiveness of modern drugs used in the treatment of fatty liver and its related diseases. To this ends, we evaluated the effect of Cyperus esculentus on the liver in experimentally induced hyperlipidemia in rats. Aqueous extract of the plant was administered orally to rats at the doses of 300,400 and 600mg/kg body weight(b.wt) for a period of twenty nine days. Fatty liver was induced by twice intraperitoneal injection of TritonWR-1339 at a dose of 300mg/kg b.wt. to wistar rats . The result shows that administration of triton led to significant (P˂0.05) serum increase in the activities of alanine and aspartate aminotransferases (ALT and AST) of the rats.There was no significant (p˃0.05) change in the activities of serum alkaline phosphatase following the administration of triton.The study also shows that there were significant( p˂0.05) reduction in the serum level of total protein , albumin and globulin and increase in serum level of total and conjugated bilirubin though not statistically significant (p˃0.05) following the administration of triton to rats.The observed effects are suggestive of mild toxicity of the liver by triton and this is further supported by several histopathological manifestations such as hepatocellular degeneration, macrovesicular vacuolation,periportal necrosis, congestion ,severe intimal ulceration and stenosis in the blood vessels . Treatment with the aqueous extract of Cyperus esculentus attenuated both the biochemical effects and histopathological manifestations.In conclusion, the results from the serum liver enzymes biochemical parameters and histopathological analyses suggested the toxicity of triton and also showed the effectiveness of the aqueous extract of Cyperus esculentus in attenuating the liver toxicity Key Words : Cyperus esculentus ,Triton,macrovesicular vacuolation,periportal necrosis.

Hypolipidemic Activity of of Madhuca longifolia in Triton Induced Hyperlipidemic Rats

Objective: In the present study, an aqueous extract from Madhuca longifolia bark was evaluated for its hypocholesterolaemic and hypotriglyceridaemic activities using Triton WR-1339 induced hyperlipemic rats as experimental model. Material and Method: Hyperlipidemia was induced by a single injection of Triton WR 1339 (400 mg/kg i.p.) in sprauge dawley rats. Aqueous extract of Madhuca longifolia bark (ML) (250, 500 and 750 mg/kg/day) was administered to hyperlipidemic rats for one week. Harvested serum was analyzed for lipid profile such as cholesterol, triglyceride, and lipoproteins. Oxidative stress parameters like Superoxide dismutase (SOD), Catalase (CAT), Glutathione peroxidase (GPx) and Glutathione reductase (GRh) and activity of lipolytic enzyme such as lecithincholesterol-acyltransferase (LCAT) & post-heparin lipolytic activity (PHLA) were estimated in the liver tissues of hyperlipidemic rats. Results: Result of the study suggested that treatment with ML 750mg/kg/day significantly (p?0.01) lowered the level of serum cholesterol, triglyceride phospholipids and increased in lecithincholesterol-acyltransferase activity & post-heparin lipolytic activity compared to Triton-treated rats. In addition, ML 750mg/kg/day significantly (p?0.01) reduced oxidative stress and normalizes the activities of SOD, CAT, GPx and GRh compared to Triton-treated rats. Conclusion: The current study provides strong evidence that intragastric administration of ML 750mg/kg/day has a beneficial effect in treating dyslipidemia with decrease in oxidative stress.

Hypolipidemic Effect of EthanolicExtract of Cyperus esculentumis in TritonWR-1339-Induced Hyperlipidemic Rats

Currently, there has been an observed interest in phytochemicals as a new hypolipidemic agents to replace synthetic toxic hypolipidemic drugs. The investigation was carried out to evaluate the hypolipidemic effects of ethanolicextract of Cyperus esculentumis in triton-induced hyperlipidemic rats. The ethanolic extract of the plant was administered orally to rats at the doses of 300,400 and 600mg/kg body weight for a period of twenty nine days in accordance with the Ethical committee on experimental animals. Hyperlipidemia was developed by interaperitoneal injection of Triton at a dose 250mg/kg b.wt. to wistar rats . Intraperitoneal injection of Triton WR-1339 at a dose of 250mg/kg to rats resulted in the increase in serum triglyceride, total cholesterol , low density and very low density lipoproteins cholesterol accompanied by reduction in the high density lipoprotein cholesterol .The histopathological examination also revealed that there were remarkable histopathological changes in the aorta and artery of rats induced with Triton WR-1339 . The damages were manifested as ulceration and stenosis .Pretreatment with the ethanolic tuber extract of Cyperus esculentumis led to significant reduction of TC, TG, LDL and VLDL cholesterol in triton-induced hyperlipidemic rats as compared to the control. There was also an increased in HDL-cholesterol and attenuation of histopathological damages. Among the different doses administered, only 600 mg/kg exhited statistical significant effects. Other doses 300 and 400mg/kg showed mild toxicity. This finding suggests that the cholesterol-lowering effect of Cyperus esculentumis may be due to the enhancement of LDL-C metabolism which might be attributed to the presence of the valuable phytochemicals in the extract.

Hepatocyte-Specific Depletion of UBXD8 Induces Periportal Steatosis in Mice Fed a High-Fat Diet.

We showed previously that UBXD8 plays a key role in proteasomal degradation of lipidated ApoB in hepatocarcinoma cell lines. In the present study, we aimed to investigate the functions of UBXD8 in liver in vivo. For this purpose, hepatocyte-specific UBXD8 knockout (UBXD8-LKO) mice were generated. They were fed with a normal or high-fat diet, and the phenotypes were compared with those of littermate control mice. Hepatocytes obtained from UBXD8-LKO and control mice were analyzed in culture. After 26 wk of a high-fat diet, UBXD8-LKO mice exhibited macrovesicular steatosis in the periportal area and microvesicular steatosis in the perivenular area, whereas control mice exhibited steatosis only in the perivenular area. Furthermore, UBXD8-LKO mice on a high-fat diet had significantly lower concentrations of serum triglyceride and VLDL than control mice. A Triton WR-1339 injection study revealed that VLDL secretion from hepatocytes was reduced in UBXD8-LKO mice. The decrease of ApoB secretion upon UBXD8 depletion was recapitulated in cultured primary hepatocytes. Accumulation of lipidated ApoB in lipid droplets was observed only in UBXD8-null hepatocytes. The results showed that depletion of UBXD8 in hepatocytes suppresses VLDL secretion, and could lead to periportal steatosis when mice are fed a high-fat diet. This is the first demonstration that an abnormality in the intracellular ApoB degradation mechanism can cause steatosis, and provides a useful model for periportal steatosis, which occurs in several human diseases.

Hypolipidemic Activity of Aqueous Extract of Turnip (Brassica rapa) Root in Hyperlipidemic Rats

Aims: Turnip is one of the most consumed medicinal plants that seem to have advantageous efficacy on hyperlipidemia. The present work was undertaken to evaluate the hypolipidemic activity of aqueous extract of Brassica rapa root on hyperlipidemic rats. Materials & Methods: In this experimental study 40 male Wistar rats were divided into 5 equal groups; normal control, hyperlipidemic control (1ml normal saline once a day), Atorvastatin (10mg/kg of body weight per day) and aqueous extract of Brassica rapa root groups (200 and 400mg/kg of body weight per day) were treated for 10 days. After 18h fasting in 11th day, hyperlipidemia was induced by a single intraperitoneal (IP) injection of triton WR1339 (300mg/kg of body weight) in all groups except normal control. 24 hours after injection, blood collection was done and plasma analyzed for lipid profiles. Data was compared between group s by ANOVA and Tukey tests in SPSS 18 software. Findings: Aqueous extract of Brassica rapa root inhibited the elevation of plasma total cholesterol level at the dose of 200mg/kg of body weight. The extract also decreased LDL cholesterol and triglyceride levels in hyperlipidemic rats significantly but in compare to normal control group these levels were significantly high (p<0.05). Conclusion: The consumption of turnip may act as a potent antihyperlipidemic nutrient for patients with dyslipidemia, cardiovascular and diabetes diseases.

Impact of Chicory-Supplemented Diet on HMG-CoA Reductase, Acetyl-CoA Carboxylase, Visfatin and Anti-Oxidant Status in Triton WR-1339-Induced Hyperlipidemia

Hyperlipidemia is a major risk factor for cardiovascular diseases. The present study was conducted to evaluate the potential role of chicory (Cichorium intybus Linn.) against hyperlipidemia and its subsequent effect in rats. Sixty male albino rats were randomly and equally divided into four groups. Hyperlipidemia was induced via intraperitoneal injection of Triton WR-1339 at a dose of 250 mg/kg body weight three times a week for 2 weeks. Chicory-supplemented diet (10 g/100 g diet) was given for 4 weeks to group II and group IV. Chicory caused significant improvement in lipid profile and decreased the liver and heart acetyl-CoA carboxylase activity, atherogenic indices, hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA level and visfatin level. Meanwhile, significant increase in paraoxonase-1, superoxide dismutase and catalase activity was recorded. In conclusion, chicory has the potential role of being hypolipidemic, anti-lipotoxic, anti-oxidant and anti-atherogenic factor. Practical Applications Herbal treatments for hyperlipidemia are relatively cheap and locally available. The results showed that chicory (Cichorium intybus) has the potential of being hypolipidemic, anti-oxidant, anti-inflammatory, and decreased the atherogenic risk indices and anti-steatotic. Thus, it may represent a new source of natural food supplement aimed at preventing dyslipidemic risk for atherosclerosis, cardiac and hepatic steatosis.

Efficacy of β-sitosterol isolated from Evolvulus alsinoides L. as anti-hyperlipidemic and anti-tumor agent: Evidence from animal studies.

To explore the anti-hyperlipidemic and anti-tumor effect of ethanolic extract of Evolvulus alsinoides, its chloroform fraction and isolated components in Triton-induced hyperlipidemic rats. Animals were administered with intraperitoneal (i.p.) injection of Triton WR 1339 at a dose of 400 mg/kg body weight. After 24 h of Triton administration the test drugs were administered orally at a dose of 200 mg/kg body weight in rats. The ethanolic extract and stigmast-5-en-3β-ol from Evolvulus alsinoides were further investigated for the tumor take inhibitory activity in hybrid mice (of C57BL strain + Swiss albino strain). Preventive group animals were injected daily with the extract and stigmast-5-en-3β-ol at dose of 50 mg/kg body weight i.p. for 10 consecutive days. The animals were observed for the growth of tumor after injection of B16F10 melanoma cells into the dorsal skin of mice. Stigmast-5-en-3β-ol showed a marked antihyperlipidemic potential by reducing the total cholesterol, triglycerides, low density lipoproteins level, and significantly increased high density lipoprotein level compared with other isolated component. Pretreatment with the drug showed delay tumor growth by increasing the volume doubling time and growth delay. The stigmast-5-en-3β-ol showed better mean survival time. The supplementation of antioxidants and phytosterols rich food Evolvulus alsinoides has significant tumor take inhibitory activity.

Synthesis of novel N-(4-benzoylphenyl)-2-furamide derivatives and their pharmacological evaluation as potent antihyperlipidemic agents in rats.

In the search for new potential antihyperlipidemic agents, the present study focuses on the synthesis and pharmacological activity of a series of novel N-(4-benzoylphenyl)-2-furamides (3a-3e). Hyperlipidemia was induced in rats by single intraperitoneal injection of Triton WR-1339 (300 mg/kg body weight). At a dose of 15 mg/kg body weight, compounds 3b, 3d and bezafibrate (100 mg/kg) significantly (p<0.0001) reduced elevated plasma triglyceride levels after 18 h compared to the hyperlipidemic control group. However, only groups treated with compounds 3b, and 3d obviously showed a significant (p<0.0001) reduction in plasma total cholesterol levels. Moreover, high density lipoprotein-cholesterol levels were significantly (p<0.0001) increased in animals treated with compounds 3b, 3d and bezafibrate. It is therefore reasonable to assume that compounds 3b and 3d may have promising potential in the treatment of hyperlipidemia. This beneficial activity may contribute to their cardioprotective and antiatherosclerotic role.

Mouse liver lysosomes contain enzymatically active processed forms of Hyal-1

It has long been known that liver lysosomes contain an endoglycosidase activity able to degrade the high molecular mass glycosaminoglycan hyaluronic acid (HA). The identification and cloning of a hyaluronidase with an acidic pH optimum, Hyal-1, suggested it might be responsible for this activity. However, we previously reported that this hydrolase could only be detected in pre-lysosomal compartments of the mouse liver using a zymography technique that allows the detection of Hyal-1 activity after SDS–PAGE (“renatured protein zymography”). Present work reveals that the activity highlighted by this technique belongs to a precursor form of Hyal-1 and that the lysosomal HA endoglycosidase activity of the mouse liver is accounted for by a proteolytically processed form of Hyal-1 that can only be detected using “native protein zymography”. Indeed, the distribution of this form follows the distribution of β-galactosidase, a well-established lysosomal marker, after fractionation of the mouse liver in a linear sucrose density gradient. In addition, both activities shift toward the lower density region of the gradient when a specific decrease of the lysosomal density is induced by Triton WR-1339 injection. The fact that only native protein zymography but not renatured protein zymography is able to detect Hyal-1 activity in lysosomes points to a non-covalent association of Hyal-1 proteolytic fragments or the existence of closely linked partners supporting Hyal-1 enzymatic activity. The knockdown of Hyal-1 results in an 80% decrease of total acid hyaluronidase activity in the mouse liver, confirming that Hyal-1 is a key actor of HA catabolism in this organ.

Hypolipidemic action of chrysin on Triton WR-1339-induced hyperlipidemia in female C57BL/6 mice

Chrysin (5,7-dihydroxyflavone) is a flavonoid, natural component of traditional medicinal herbs, present in honey, propolis and many plant extracts. The objective of this study was to investigate the hypolipidemic properties of chrysin on Triton WR-1339-induced hyperlipidemia in female C57BL/6 mice. Triton WR-1339 was administered intraperitoneally (400 mg/kg) to overnight-fasted mice to develop acute hyperlipidemia. Chrysin was administered orally (10 mg/kg) 30 min before Triton WR-1339. At 24 h after Triton WR-1339 injection, blood samples were collected to measure plasma lipid levels. The hepatic thiobarbituric acid reactive substances (TBARS), carbonyl content, non-protein sulfhydryl (NPSH) and ascorbic acid (AA) levels, as well as catalase (CAT) and superoxide dismutase (SOD) activity were recorded. Chrysin administration significantly decreased total cholesterol levels. In addition, it partially decreased non-high density lipoprotein-cholesterol and triglycerides levels in plasma of hyperlipidaemic mice. In addition chrysin administration prevented the increase on TBARS levels and prevented the decrease in SOD activity induced by Triton WR-1339. These findings indicated that chrysin was able to decrease plasma lipids concentration and that its antioxidant properties was, at least in part, involved in the hypolipidaemic action of chrysin.

Antihypercholesterolemic and Antioxidative Potential of an Extract of the Plant, Piper betle, and Its Active Constituent, Eugenol, in Triton WR-1339-Induced Hypercholesterolemia in Experimental Rats.

Hypercholesterolemia is a dominant risk factor for atherosclerosis and cardiovascular diseases. In the present study, the putative antihypercholesterolemic and antioxidative properties of an ethanolic extract of Piper betle and of its active constituent, eugenol, were evaluated in experimental hypercholesterolemia induced by a single intraperitoneal injection of Triton WR-1339 (300 mg/kg b.wt) in Wistar rats. Saline-treated hypercholesterolemic rats revealed significantly higher mean blood/serum levels of glucose, total cholesterol, triglycerides, low density and very low density lipoprotein cholesterol, and of serum hepatic marker enzymes; in addition, significantly lower mean serum levels of high density lipoprotein cholesterol and significantly lower mean activities of enzymatic antioxidants and nonenzymatic antioxidants were noted in hepatic tissue samples from saline-treated hypercholesterolemic rats, compared to controls. However, in hypercholesterolemic rats receiving the Piper betle extract (500 mg/kg b.wt) or eugenol (5 mg/kg b.wt) for seven days orally, all these parameters were significantly better than those in saline-treated hypercholesterolemic rats. The hypercholesterolemia-ameliorating effect was better defined in eugenol-treated than in Piper betle extract-treated rats, being as effective as that of the standard lipid-lowering drug, lovastatin (10 mg/kg b.wt). These results suggest that eugenol, an active constituent of the Piper betle extract, possesses antihypercholesterolemic and other activities in experimental hypercholesterolemic Wistar rats.

Isolation of Bioactive Phytoconstituent from Alpinia galanga L. with Anti-Hyperlipidemic Activity

ABSTRACTThe present study was undertaken to explore the antihyperlipidemic effect of ethanolic extract of rhizomes of Alpinia galanga L. and its chloroform fraction in Triton-induced hyperlipidemic rats. Bioactivity guided fractionation was followed by chromatographic studies. Flash chromatography was done for the most active fraction resulting in the isolation of 5-(hydroxymethyl) furfural. Animals were administered with i.p. injection of Triton WR 1339 at dose of 400 mg/kg body weight. After 24 hr of Triton administration, the ethanolic extract and its fraction were administered orally at doses of 200 and 400 mg/kg body weight in rats. The treatment was continued for 5 days with a view to see the effect on lipid profile. Serum samples were subjected to biochemical analysis. The study dose dependently inhibited the total cholesterol (TC), triglycerides (TG), low-density lipoprotein (LDL) level, and significantly increased high-density lipoprotein (HDL) level. Phytochemical screening revealed the presence of tannins, coumarins, flavanoids, sterols, and glycosides. Phytochemical investigation of the chloroform fraction of A. galanga L. resulted in the isolation of 5-(hydroxymethyl) furfural. UV λmax was found to be 276 nm for the isolated component. Acute treatment caused a stimulatory effect on the HDL level and inhibition in TC and TG elevation induced by triton.

English

The present study evaluates anti-hyperlipidaemic and anti-atherogenic activities in Triton WR-1339 and high cholesterol diet induced hyperlipidemia in rat models. Chloroform, ethyl acetate and ethanol extracts of whole plant of Blepharis maderaspatensis were evaluated for their anti-hyperlipidaemic and anti-atherogenic activities using Triton WR-1339 induced hyperlipidaemic rats (acute study) and high cholesterol diet induced (chronic study) experimental models. Hyperlipideamia was developed by intraperitonial injection of Triton WR-1339 (200 mg/kg body weight) in acute study and feeding with cholesterol rich diet in chronic study. The animals were divided into various groups and intragastric administration of various extracts of B. maderaspatensis (100 mg/kg) body weight was given in both models. After the completion of the treatment, they were evaluated for serum total cholesterol, triglycerides, high density lipoprotein (HDL), low density lipoprotein (LDL), very low density lipoprotein (VLDL), atherogenic index (AI), coronary risk index (CRI) and were compared with the rats treated with simvastatin (20 mg/kg) of the body weight. Pre-treatment of ethanol extracts of B. maderaspatensis significantly reduced the serum total cholesterol, triglycerides, LDL, VLDL, AI and CRI as comparable with simvastatin. Key words: Serum lipids, atherogenic index, cholesterol diet, coronary risk index, Triton WR-1339, Blepharis maderaspatensis, high cholesterol diet.