In silico analysis of selected nutrition rich fruit of Bunch berry (Lantana camara) constituents as human acetylcholinesterase (hAchE), carbonic anhydrase II (hCA-II) and carboxylesterase 1 (hCES-1) inhibitory agents.

Background: Bunch berry (Lantana camara) is primarily composed of flavonoids and vitamin C; therefore, it has been shown to possess various medical characteristics, including the ability to relieve fever, inflammation, and urinary tract infections. Objective: In this study, we intended to assess twenty chosen constituents of Bunch berry as potent inhibitory agents of human acetylcholinesterase (hAchE), carbonic anhydrase II (hCA-II) and carboxylesterase 1 (hCES-1) employing in silico techniques. Methods: The twenty chosen Bunch berry components were examined about docking behaviour of hAchE, hCA-II and hCES-I by using the Swissdock method. Apart from to docking, Molecular physico-chemical, drug-likeness, ADME (ingesting, dispersing, metabolising, and excreting), and toxicity assessments were also performed utilising the Molinspiration, Swiss ADME, pkCSM, and STITCH web sites, correspondingly. Results: Eight ligands (40 %) have exhibited strict adherence to Lipinski's rule of five (Ro5), according to molecular physico-chemical study. Drug-likeness property analysis has shown that five ligands (25 %) of Bunch berry predicted to exhibit moderate bioactivity score against all the descriptors. ADME analysis has shown that five ligands (25 %) of Bunch berry are predicted to possess high gastrointestinal absorption property Toxicity analysis has shown that six ligands (30 %) of Bunch berry are predicted to have hERG II (Human ether-a-go-go-related gene) inhibition activity. According to the docking analysis, lantic acid has the lowest atomic binding energy for all three target enzymes, hAchE (-6.23 kcal/mol), hCA-II (-4.46 kcal/mol), and hCES-I (-5.99 kcal/mol), respectively. Conclusions: Thus the current find provides an advanced understanding the twenty selected ligands of Bunch berry as potent inhibitory agents of human acetylcholinesterase (hAchE), carbonic anhydrase II (hCA-II) and carboxylesterase 1 (hCES-1).

Pouteria caimito fruit derived nanoparticles inhibited the apple ring rot disease as well as extended the shelf-life of sliced apples.

Background: Apple disease, exaggerated by Botryosphaeria dothidea, is a foremost intimidating problem for extending the apple fruit shelf-life and producing substantial economic losses for cultivators and distributors. Alternate sources are urgently needed to prevent or inhibit the ring rot infection of apple fruit instigated by Botryosphaeria dothidea. Objective: In this current study, we premeditated to make novel organic nanoparticles as of Pouteria caimito fruit extract and calcium chloride (PCNP), which were used to evaluate the preventive outcome of Botryosphaeria dothidea-caused apple disease on postharvest apple fruits. Results: Our findings corroborated that the fruit derived nanoparticle had been confirmed for quality and size by altered estimations such as fourier transform infrared (FTIR), UV-vis spectroscopic analysis, scanning electron microscope and energy dispersive X-ray (SEM and EDX) estimation, and dynamic light scattering (DLS) analysis. In addition, we have investigated the excellent inhibitory action of the pathogen infection in apples initiated by Botryosphaeria dothidea. The protective enzymes function was pointedly improved in nanoparticle-treated apple fruits once equated with those of control apple fruits. The catalase (CAT) and superoxide dismutase (SOD) activities were pointedly improved in nanoparticle-treated fruits when compared to those of control fruits. The shelf-life extension studies were conducted for 7 days with a fresh-cut apple. The total soluble solid, pH, weight loss, and sensory studies were analyzed, and they proved the extension of sliced apple shelf life up to 7 days. Conclusions: The discoveries of this study provided a well-organized, harmless, and environment-friendly substitute to control the apple disease as well as the durability postponement of sliced apples 7 days or may longer.

Vitamin A- and C-rich Pouteria camito fruit derived superparamagnetic nanoparticles synthesis, characterization, and their cytotoxicity.

Background: Recently, green nanoparticles are gaining importance in drug development because of their lower toxicity, sustainability, cost effectiveness, simplicity, and ecofriendly nature compared with toxic chemicals. Objective: In this study, we developed a nontoxic method for synthesizing iron oxide nanoparticles by using the fruit of Pouteria caimito that is rich in vitamin A and C and evaluated their cytotoxicity. Methods: Pouteria caimito fruit¬-derived superparamagnetic nanoparticles (PCSNs) were characterized using physical and chemical methods, and their cytotoxicity was examined using the 3-(4, 5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide (MTT) assay. Results: Ultraviolet-visible spectroscopy (UV-Vis spectro) analysis of PSNs showed a peak at 277 nm. Transmission electron microscopy (TEM) findings showed that PSNs exhibited a nanorod shape with their sizes ranging from 9.41 nm to 16.96 nm (average size: 13.08 nm). The findings of dynamic light scattering (DLS) indicated that the particle size was 186. 6-847.3 d.nm with an average of 367.5 d.nm. The Zeta potential analysis indicated that PSNs exhibited uniform surface charge distribution, and their surface charge was equal to -13.7 mV. Fourier-transform infrared spectroscopy (FTIR) analysis showed that PSNs exhibited bands at 3412, 1629, 1384, 1075, 818, 697, and 471 cm-1. Energy-dispersive X-ray spectroscopy (EDX) results showed that iron was the major element present in PCSNs, followed by other biomolecules such as C, O, and Cl, indicating the production of iron oxide nanoparticles. Conclusion: The Pouteria caimito fruit that possesses strong oxidizing and nontoxic properties can be a potentially attractive source for the production of iron oxide nanoparticles. Moreover, the cytotoxicity assay results revealed that iron oxide nanoparticles synthesized using the Pouteria caimito fruit extract derived can be used for targeting cancer cells and treating other diseases because of their nontoxic nature. These nanoparticles can be used for the treatment of cancer and other diseases in the future.

Cassia fistula nutrition rich flower tea derived biotic nanoparticles synthesis, characterization and their antioxidant and anti-hyperglycaemic properties.

Background: Cassia fistula (CF) is a nutrient-rich flowering plant and it has been used to cure numerous human health problems including cardiac diseases, bacterial infection, and inflammation. Objective: The purpose of this study was to investigate the production and characterisation of biomimetic iron oxide nanoparticles (ICF) derived from CF flower tea as well as evaluate their antioxidant and anti-hyperglycemic properties. Methodology: CF tea derived ICF synthesis and characterized by established physical-chemical methods. Moreover, this synthesized ICF were checked for their antioxidant and anti-hyperglycemic properties such as alpha-amylase, glucose intake, total antioxidant (TAA), ferrous reducing (FA), and radical scavenging (DPPH) properties. Results: The synthesized ICF characterization and size were confirmed primarily by described physical and chemical methods. Our findings revealed that ICF have a powerful antihyperglycemic mechanism by involving alpha-amylase inhibition and enhanced glucose absorption. Meanwhile, this ICF exhibited distinguished antioxidant competence by improving TAA and free radical scavenging (TAA, DPPH) properties. Finally, this ICF has proven anti-hyperglycemic and antioxidant mechanisms due to their presence of nano-sized biomolecules. Conclusion: In this study, it might be concluded that the CF is the best source for iron oxide nanoparticles production with clarity, small size and high solidity. Moreover, this nanoparticle has proven in vitro anti-hyperglycemic and antioxidant mechanisms.

Galangin ameliorates changes of membrane-bound enzymes in rats with streptozotocin-induced hyperglycemia

Objective: To assess the protective effect of galangin on membrane bound enzymes in rats with streptozotocin-induced diabetes. Methods: A single low dose of streptozotocin was injected to adult male albino rats to induce hyperglycemia. Galangin (8 mg/kg) or glibenclamide 600 μg/kg as a standard drug was given orally once daily for 45 days by gavage. Membrane-bound adenosine triphosphatases were determined including total ATPase, sodium-potassium-ATPase, calcium-ATPase and magnesium-ATPase in erythrocytes and tissues (kidney, liver, and heart). Results: The levels of total ATPases, sodium-potassium-ATPase, calcium-ATPase and magnesium-ATPase in erythrocytes and tissues were significantly altered in diabetic rats as compared to that in normal rats. After 45 days of treatment with galangin or glibenclamide, the levels of these enzymes were similar to that of normal control rats. Conclusions: Oral administration of galangin or glibenclamide can improve activities of these membrane-bound ATPases towards normal levels. Mechanism of galangin needs to be further explored in future.

Lavatera critica controls systemic insulin resistance by ameliorating adipose tissue inflammation and oxidative stress using bioactive compounds identified by GC-MS.

BACKGROUND: Lavatera critica, a leafy green herb, is reported to have many pharmacological activities; but, the improvement of insulin sensitivity against the high gram-fat diet (HGFD)-caused insulin resistance (IR) has not yet been studied. OBJECTIVE: This study evaluated the role of Lavatera critica leaf extract (LCE) in systemic insulin resistance through the alleviation of adipose tissue inflammation and oxidative damage in HGFD fed mice. METHODS: The mice were fed with HGFD for 10 weeks and the diet was supplemented with LCE each day for the next five weeks. Body weight, food intake, leptin, blood glucose, insulin, insulin resistance, and pro- and anti-inflammatory genes expression were assessed on day 106. RESULTS: The HGFD control mice displayed markedly elevated adipose tissue inflammation, oxidative stress, insulin inactivity, and hyperglycemia. Administration of LCE in the HGFD mice, especially a dose of 100 mg/kg, lowered the body weight, food intake, plasma leptin, plasma glucose, plasma insulin, insulin resistance, and increased the food efficacy ratio when compared with the HGFD control mice. The oral glucose tolerance test (OGTT) revealed that LCE prevented further increase in the circulating levels after the glucose load. LCE-treated mice demonstrated a marked suppression of pro-inflammatory cytokines mRNA expression. On the other hand, the mice showed a higher anti-inflammatory genes mRNA expression in the adipose tissue. In addition, LCE treatment improved the oxidative damage as evidenced by the reduced levels of lipid hydroperoxides and thiobarbituric acid reactive substances coupled with the increased antioxidants (superoxide dismutase, total glutathione, glutathione/glutathione disulfide ratio and glutathione peroxidase) in the adipose tissue, plasma and erythrocytes. Gas chromatography-mass spectrometry analysis of the bioactive compounds revealed the presence of 9, 12, 15-octadecatrienoic acid, vitamin E, phytol, hexadecanoic acid, benzenepropanoic acid, and stigmasterol. CONCLUSIONS: These findings prove that LCE improves the insulin-sensitizing activity in the mouse model of HGFD-caused IR, probably due to the amelioration of adipose tissue inflammation and oxidative damage. Hence, the LCE could serve as a useful anti-diabetic agent.

Herbacetin, a flaxseed flavonoid, ameliorates high percent dietary fat induced insulin resistance and lipid accumulation through the regulation of hepatic lipid metabolizing and lipid-regulating enzymes.

Healthy plants and their constituents have been considered as a safe remedy for the treatment of obesity and obesity associated diseases. Herbacetin is a dietary flavonoid that has been explored for many pharmacological activities; but, the anti-hyperglycaemic and anti-hyperlipidemic properties of herbacetin have not yet been explored. The present study was performed to evaluate the ameliorative effect of herbacetin on high-fat diet-induced hyperglycaemia and hyperlipidemia in 57BL/6 J mice. Obesity associated insulin resistance was induced by continuously feeding the mice with high-fat diet for 10 weeks. Afterwards, mice were subjected to intragastric administration of herbacetin (different doses) daily along with high-fat diet for the next 5 weeks. At the end of 106th day, changes in body weight, blood glucose, insulin, HOMA-IR, and lipids profiles and lipid-regulating enzymes were evaluated. Herbacetin significantly reduced the body weight, plasma glucose, plasma insulin, and HOMA-IR activity in obesity associated insulin resistant mice (OIR). In addition, herbacetin administration significantly reduced the plasma and hepatic total cholesterol, triglycerides, and free fatty acids in OIR mice. Moreover, herbacetin significantly improved the altered hepatic lipid metabolizing and lipid-regulating enzymes such as SREBP-1c, and 2, fatty acid synthase (FAS), fatty acid ß-oxidation (ß-oxidation), malic enzyme, glucose 6-phosphate dehydrogenase (G6PD), and carnitine palmitoyltransferase (CPT) when compared to OIR control mice. Histopathological examination clearly showed that herbacetin decreases lipid droplets in the liver tissue. Thus, observed results strongly indicate that herbacetin provides remarkable protection against the harmful effects of chronic high-fat diet consumption because of its anti-hyperglycaemic and anti-hyperlipidemic properties through the regulation of hepatic lipid metabolizing and lipid-regulating enzymes.

Galangin, a natural flavonoid reduces mitochondrial oxidative damage in streptozotocin-induced diabetic rats.

OBJECTIVE: We designed this study to observe the effect of galangin on damaged mitochondria in the liver of diabetic rats. METHODS: Male albino Wistar rats were made diabetic by injecting streptozotocin (STZ) intraperitoneally (40 mg kg-1 body weight (BW)). Galangin (8 mg kg-1 BW) or glibenclamide (600 µg kg-1 BW) was given orally daily once for 45 days to both healthy and diabetic rats. RESULTS: Diabetic rats showed significant (P < 0.05) increase in liver mitochondrial oxidant [Thiobarbituric acid reactive substance (TBARS)] level and a significant decrease in enzymatic [superoxide dismutase (SOD), glutathione peroxidase (GPx)] and non-enzymatic (reduced glutathione (GSH)) antioxidant levels when compared with healthy rats. The mitochondrial enzymes isocitrate dehydrogenase (ICDH), alpha-ketoglutarate dehydrogenase (α-KGDH), succinate dehydrogenase (SDH) and malate dehydrogenase (MDH) and mitochondrial respiratory chain enzymes NADH-dehydrogenase and Cytochrome c-oxidase were decreased significantly (P < 0.05) in diabetic rats when compared with healthy rats. A natural flavonoid galangin administered to hyperglycemia-induced rats resulted in the following findings as compared to hyperglycemia-induced control rats: the oxidant levels decreased significantly (P < 0.05); the enzymatic and non-enzymatic antioxidant levels increased significantly (P < 0.05) and the function of mitochondrial enzymes and the mitochondrial respiratory chain enzymes increased significantly (P < 0.05). CONCLUSION: From the results, we conclude that galangin could maintain liver mitochondrial function in diabetic rats.

Lavatera critica, a green leafy vegetable, controls high fat diet induced hepatic lipid accumulation and oxidative stress through the regulation of lipogenesis and lipolysis genes.

BACKGROUND: Lipid accumulation is the most vital risk factor for inducing nonalcoholic fatty liver disease (NAFLD) and metabolic syndrome. Thus, the development of novel drugs is urgently needed to control obesity related diseases. OBJECTIVE: Here, we investigated the protective role of Lavatera critica (LC), a green vegetable, in male C57BL/6J mice fed with high fat (HF) diet for 10 weeks to induce hepatic lipid accumulation and oxidative cellular damage. RESULTS: After oral administration of chloroform (CFLC), ethyl acetate (EFLC), or methanol (MFLC) fractions of Lavatera critica to the HF group, EALC alone significantly reduced the activities of hepatic markers such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST); moreover, the results showed that 50 mg/kg dose has the maximum activity. Thus, this active dose of EFLC was used for further analysis. Moreover, EFLC reduced the level of hepatic triglycerides (TG), total cholesterol (TC), free fatty acids (FFA), and prevented further increase in the body weight. Intriguingly, EFLC treatment also reversed the mRNA expression of fatty acid oxidative genes, such as peroxisome proliferator activated receptor-α (PPAR-α), carnitine palmitoyltransferase-1 (CPT-1), and acetyl-CoA carboxylase (ACO), and fatty acid synthesis genes such as fatty acid synthase (FAS), sterol-regulatory-element-binding protein-1c (SREBP-1c), and acetyl-CoA carboxylase (ACC). Furthermore, EFLC treatment also decreased the production of oxidative stress biomarkers, such as conjugated diene (CD), thiobarbituric acid reactive substances (TBARS), and lipid hydroperoxide (LOOH), and significantly enhanced the level of enzymatic antioxidants, such as glutathione peroxidase (GPx), superoxide dismutase (SOD), and catalase (CAT), as well as non-enzymatic antioxidants, such as reduced glutathione (GSH), vitamin C, and vitamin E in the liver. CONCLUSION: Taken together, we conclude that EFLC has a protective effect against HF diet induced hepatic lipid accumulation and oxidative cellular damage through the regulation of lipogenesis and lipolysis genes.

Galangin, a dietary flavonoid, improves antioxidant status and reduces hyperglycemia-mediated oxidative stress in streptozotocin-induced diabetic rats.

OBJECTIVE: To examine the effect of galangin on hyperglycemia-mediated oxidative stress in streptozotocin (STZ)-induced diabetic rats. METHODS: Diabetes was induced by intraperitoneal administration of low-dose STZ (40 mg/kg body weight (BW)) into male albino Wistar rats. Galangin (8 mg/kg BW) or glibenclamide (600 µg/kg BW) was given orally, once daily for 45 days to normal and STZ-induced diabetic rats. RESULTS: Diabetic rats showed significantly increased levels of plasma glucose, thiobarbituric acid reactive substances, lipid hydroperoxides, and conjugated dienes. The levels of insulin and non-enzymatic antioxidants (vitamin C, vitamin E, reduced glutathione) and the activity of enzymatic antioxidants (superoxide dismutase, catalase, glutathione peroxidase, and glutathione-S-transferase (GST)) were decreased significantly in diabetic control rats. These altered plasma glucose, insulin, lipid peroxidation products, enzymatic and non-enzymatic antioxidants ions were reverted to near-normal level after the administration of galangin and glibenclamide. CONCLUSION: The present study shows that galangin decreased oxidative stress and increased antioxidant status in diabetic rats, which may be due to its antidiabetic and antioxidant potential.

Influence of kaempferol, a flavonoid compound, on membrane-bound ATPases in streptozotocin-induced diabetic rats.

CONTEXT: Kaempferol is a flavonoid found in many edible plants (e.g. tea, cabbage, beans, tomato, strawberries, and grapes) and in plants or botanical products commonly used in traditional medicine. Numerous preclinical studies have shown that kaempferol have a wide range of pharmacological activities, including antioxidant, anti-inflammatory, anticancer, cardioprotective, neuroprotective, and antidiabetic activities. OBJECTIVE: The present study investigates the effect of kaempferol on membrane-bound ATPases in erythrocytes and in liver, kidney, and heart of streptozotocin (STZ)-induced diabetic rats. MATERIALS AND METHODS: Diabetes was induced into adult male albino rats of the Wistar strain, by intraperitoneal administration of STZ (40 mg/kg body weight (BW)). Kaempferol (100 mg/kg BW) or glibenclamide (600 µg/kg BW) was administered orally once daily for 45 d to normal and STZ-induced diabetic rats. The effects of kaempferol on membrane-bound ATPases (total ATPase, Na(+)/K(+)-ATPase, Ca(2+)-ATPase, and Mg(2+)-ATPase) activity in erythrocytes and in liver, kidney, and heart were determined. RESULTS: In our study, diabetic rats had significantly (p < 0.05) decreased activities of total ATPases, Na(+)/K(+)-ATPase, Ca(2+)-ATPase, and Mg(2+)-ATPase in erythrocytes and tissues. Oral administration of kaempferol (100 mg/kg BW) or glibenclamide (600 µg/kg BW) for a period of 45 d resulted in significant (p < 0.05) reversal of these enzymes' activities to near normal in erythrocytes and tissues when compared with diabetic control rats. DISCUSSION AND CONCLUSION: Thus, obtained results indicate that administration of kaempferol has the potential to restore deranged activity of membrane-bound ATPases in STZ-induced diabetic rats. Further detailed investigation is necessary to discover kaempferol's action mechanism.

Protective Effect of Carvacrol on Oxidative Stress and Cellular DNA Damage Induced by UVB Irradiation in Human Peripheral Lymphocytes.

Exposure to ultraviolet B (UVB; 280-320 nm) radiation induces the formation of reactive oxygen species (ROS) in the biological system. In this study, we examined the protective effect of carvacrol on UVB-induced lipid peroxidation and oxidative DNA damage with reference to alterations in cellular an-tioxidant status in human lymphocytes. A series of in vitro assays (hydroxyl radical, superoxide, nitric oxide, DPPH (2,2-Diphenyl-1-picryl hydrazyl), and ABTS (2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging assays) demonstrate antioxidant property of carvacrol in our study. UVB exposure significantly increased thiobarbituric acid reactive substances (TBARS), lipid hydroperoxides (LHPs), % tail DNA and tail moment; decreased % cell viability and antioxidant status in UVB-irradiated lymphocytes. Treatment with carvacrol 30 min prior to UVB-exposure resulted in a significant decline of TBARS, LHP, % tail DNA, and tail moment and increased % cell viability as carvacrol concentration increased. UVB irradiated lymphocytes with carvacrol alone (at 10 µg/mL) gave no significant change in cell viability, TBARS, LHP, % tail DNA, and tail moment when compared with normal lymphocytes. On the basis of our results, we conclude that carvacrol, a dietary antioxidant, mediates its protective effect through modulation of UVB-induced ROS.

Ameliorative effect of kaempferol, a flavonoid, on oxidative stress in streptozotocin-induced diabetic rats.

OBJECTIVE: The aim of the present study was to evaluate the protective effect of kaempferol against oxidative stress in streptozotocin (STZ)-induced diabetic rats. METHODS: Diabetes was induced in male, adult albino rats of the Wistar strain, by intraperitoneal administration of STZ (40 mg/kg body weight (BW)). Kaempferol (100 mg/kg BW) or glibenclamide (600 µg/kg BW) was administered orally once daily for 45 days to normal and STZ-induced diabetic rats. RESULTS: The STZ-induced diabetic rats showed significantly increased levels of plasma glucose, thiobarbituric acid reactive substances, lipid hydroperoxides, and conjugated dienes in plasma, liver, kidney, and heart whereas they showed significantly decreased level of plasma insulin. The levels of non-enzymic antioxidants (vitamin C, vitamin E, reduced glutathione) in plasma, liver, kidney, and heart and the activities of enzymatic antioxidants (superoxide dismutase, catalase, glutathione peroxidase, and glutathione-S-transferase) in liver, kidney, and heart were significantly decreased in diabetic rats. Administration of kaempferol to diabetic rats was showed brought back in plasma glucose, insulin, lipid peroxidation products, enzymatic, and non-enzymatic antioxidants to near normal. CONCLUSION: The present study indicates that kaempferol has a good antioxidant property, as evidenced by its increase of antioxidant status and decrease of lipid peroxidation markers, thus providing protection from the risks of diabetic complications.

Morin, a flavonoid, on lipid peroxidation and antioxidant status in experimental myocardial ischemic rats.

BACKGROUND: Myocardial infarction affects a large population in the world. Lipid peroxide metabolism plays an important role in the pathology of myocardial infarction. OBJECTIVE: The present study was designed to investigate the antioxidant potential of morin, a flavonoid in isoproterenol (ISO)-induced myocardial infarction (MI), in rats. MATERIALS AND METHODS: Male albino Wistar rats were pre-treated with morin (40 mg/kg), daily for a period of 30 days. After the treatment period, ISO (85 mg/kg), was subcutaneously injected in rats at an interval of 24 h for 2 days. RESULTS: ISO-administered rats showed elevated levels of thiobarbituric acid reactive substances (TBARS), and lipid hydro-peroxide (LOOH), in plasma and heart. Pretreatment with morin, the above changes were significantly reduced to near normal level. ISO-administered rats showed decrease in the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and glutathione-S-transferase (GST) in heart. In addition, decrease the levels non enzymatic antioxidants such as reduced glutathione (GSH), vitamin C and vitamin E in plasma and heart while ceruloplasmin in plasma. CONCLUSION: Pretreatment with morin, reversed these above biochemical changes towards normalcy. These findings revealed that, the morin possess antioxidant activity in experimentally induced cardiac toxicity.

Protective effect of Cardiospermum halicacabum leaf extract on glycoprotein components on STZ-induced hyperglycemic rats.

OBJECTIVE: To investigate the protective role of Cardiospermum halicacabum (C. halicacabum) leaf extract on glycoprotein metabolism in streptozotocin (STZ)-induced diabetic rats. METHODS: Diabetes was induced in male albino Wistar rats by intraperitonial administration of STZ. The C. halicacabum leaf extract (CHE) was administered orally to normal and STZ-diabetic rats for 45 days. The effects of C. halicacabum leaf extract (CHE) on plasma and tissue glycoproteins (hexose, hexosamine, fucose and sialic acid) were determined. RESULTS: The levels of plasma and tissues glycoproteins containing hexose, hexosamine and fucose were significantly increased in STZ-induced diabetic rats. In addition, the level of sialic acid significantly increased in plasma and liver while decreased in kidney of STZ-induced diabetic rats. After administration of CHE to diabetic rats, the metabolic alteration of glycoprotein reverted towards normal levels. CONCLUSIONS: The present study indicates that the CHE possesses a protective effect on abnormal glycoprotein metabolism in addition to its antihyperglycemic activity.

Antihyperlipidemic effect of Melothria maderaspatana leaf extracts on DOCA-salt induced hypertensive rats.

OBJECTIVE: To investigate the antihyperlipidemic effect of crude ethanolic extract of Melothria maderaspatana (M. maderaspatana) leaf (CEEM) on deoxycorticosterone acetate (DOCA)-salt hypertensive rats. METHODS: A midscapular incision was made on each rat and the left kidney was excised after ligation of the renal artery. The surgical wound was closed using an absorbable suture. After one week recovery period, hypertension was induced by subcutaneous injection of DOCA-salt solution, twice a week, and the rats received a 1% sodium chloride solution as drinking water throughout the experimental period. CEEM or nifedipine was administered orally once a day for 6 weeks. RESULTS: In DOCA-salt hypertensive rats, the level of plasma and tissues of total cholesterol (TC), triglycerides (TG), free fatty acids (FFA) and phospholipids (PL) significantly increased and administration of CEEM significantly reduced these parameters towards normality. Further, the levels of low density lipoprotein-cholesterol (LDL-C) and very low density lipoprotein-cholesterol (VLDL-C) significantly increased while high density lipoprotein-cholesterol (HDL-C) decreased in hypertensive rats and administration of CEEM brought these parameters to normality which proved their antihyperlipidemic action. Histopathology of liver, kidney and heart on DOCA-salt induced rats treated with CEEM showed reduced the damages towards normal histology. CONCLUSIONS: These findings provided evidence that CEEM was found to be protecting the liver, kidney and heart against DOCA-salt administration and the protective effect could attribute to its antihyperlipidemic activities.

Protective effect of Melothria maderaspatana leaf fraction on electrolytes, catecholamines, endothelial nitric oxide synthase and endothelin-1 peptide in uninephrectomized deoxycorticosterone acetate-salt hypertensive rats.

This study was designed to investigate the protective effect of ethyl acetate fraction of Melothria maderaspatana (EAFM) leaf on electrolytes, catecholamines, endothelial nitric oxide synthase (eNOS) and endothelin-1 (ET-1) peptide in uninephrectomized deoxycorticosterone acetate (DOCA)-salt hypertensive rats. Administration of DOCA-salt significantly increased the systolic and diastolic blood pressure and treatment with EAFM significantly lowered the blood pressure. In DOCA-salt rats, the levels of sodium and chloride increased significantly while potassium level decreased and administration of EAFM brought these parameters to normality. The levels of epinephrine and norepinephrine increased significantly in DOCA-salt rats and administration of EAFM significantly decreased these parameters to normality. DOCA-salt hypertensive rats exhibited significantly decreased L: -arginine and nitrite + nitrate levels and administration of EAFM brought these parameters to normality. DOA-salt hypertensive rats showed down-regulation of eNOS and up-regulation of ET-1 protein expressions in heart and kidney, and treatment with EAFM prevented down-regulation of eNOS and significantly down-regulated the ET-1 protein expressions. In conclusion, EAFM provides good blood pressure control by enhancing potassium and decreasing sodium levels, decreasing levels of epinephrine and norepinephrine, and preventing down-regulation of eNOS and significantly down-regulating ET-1 protein expression.

Antihypertensive effect of Melothria maderaspatana leaf fractions on DOCA-salt-induced hypertensive rats and identification of compounds by GC-MS analysis.

The present study was designed to investigate the antihypertensive effect of Melothria maderaspatana leaf fractions on deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats and to identify compounds from the active fraction by GC-MS analysis. Administration of DOCA salt significantly increased the systolic and diastolic blood pressure compared to sham-operated control rats. When treated with chloroform (CFM), ethyl acetate (EAFM) or methanol fractions of M. maderaspatana (MFM), EAFM alone significantly lowered the systolic and diastolic blood pressure. The levels of magnesium and copper significantly increased in plasma and decreased in tissues while the zinc level significantly increased in plasma and tissues, and administration of EAFM brought these parameters back to sham-operated control levels. By GC-MS analysis, phytochemicals such as coumarin, vallinic acid, p-coumaric acid, gallic acid, caffeic acid, and ferulic acid were identified in EAFM. In conclusion, the EAFM controls blood pressure in DOCA-salt hypertensive rats and reverts the metabolic alterations in magnesium, copper and zinc.

Effects of Melothria maderaspatana leaf extract on antioxidant status in sham-operated and uninephrectomized DOCA-salt hypertensive rats.

The present study was designed to investigate the antihypertensive and antioxidant effect of Melothria maderaspatana leaf extract (MME) on sham-operated and DOCA-salt (deoxycorticosterone acetate) induced hypertensive rats. Administration of DOCA-salt significantly increased the systolic (from 127 to 212 mm Hg) and diastolic (from 91 to 174 mm Hg) blood pressure compared to sham-operated control rats, while treatment with MME significantly reduced the systolic (from 212 to 135 mm Hg) and diastolic (from 174 to 96 mm Hg) blood pressure compared to hypertensive control. In DOCA-salt rats, the plasma and tissue concentration of thiobarbituric acid reactive substances (TBARS) and lipid hydroperoxide (LOOH) significantly increased and administration of MME significantly reduced these parameters towards the levels in sham-operated control. In hypertensive rats, activities of the enzymatic antioxidants such as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) and levels of non-enzymatic antioxidants such as vitamin C, vitamin E and reduced glutathione (GSH) decreased significantly in the plasma and tissues. Administration of MME returned the enzymatic and non-enzymatic antioxidants towards sham-operated control. MME shows both antihypertensive and antioxidant properties in DOCA-salt hypertensive rats and, among the three different doses tested, 200 mg/kg caused the maximum effect.

Antihypertensive efficacy of Melothria maderaspatana leaf extract on sham-operated and uninephrectomized DOCA-salt hypertensive rats.

The plant Melothria maderaspatana (MME) has been used traditionally as antihypertensive and has been proven scientifically to possess high antioxidant and hepatoprotective activity. The present study has been designed to investigate the antihypertensive effect of ethanolic extract of MME leaves on sham-operated and uninephrectomized DOCA-salt-induced hypertensive male albino Wistar rats. A midscapular incision was made on each rat and the left kidney was excised after ligation of the renal artery. The surgical wound was closed using a suture. After one week recovery period, hypertension was induced by subcutaneous injection of DOCA-salt solution, twice a week, and the rats received a 1% sodium chloride solution as drinking water throughout the experimental period. After 6 weeks injection of DOCA-salt, systolic, diastolic and mean arterial blood pressure was significantly elevated as compared with sham-operated control. Treatment with MME significantly decreased theblood pressure. Thus, the results show that MME possesses antihypertensive activity in DOCA-salt hypertensive rats.