Cardiovascular effects of Tabernaemontana pandacaqui

Intravenous injection of ethanolic extracts of the stem, leaf and flower of Tabernaemontana pandacaqui caused hypotension in pentobarbital anesthetized rats. At high doses (100-300 mg/kg), the flower extract showed a transient hypertensive effect preceeding hypotensive activity. The effects of the extracts on the heart rate of anesthetized rats correlated well with the negative chronotropic and inotropic activity observed with isolated atrium. The hypotensive activity was not inhibited by antihistaminic and antimuscarinic agents. The extracts had no effect on the pressor effects induced by norepinephrine or dual carotid occlusion. These results suggest that the hypotensive action of the extracts is not mediated through histaminic and muscarinic receptors stimulation, alpha-adrenoceptor blockade or interference of sympathetic transmission.     

Pharmacological characterization of different fractions of Calotropis procera (Asclepiadaceae) in streptozotocin induced experimental model of diabetic neuropathy

Ethnopharmacological relevance

Calotropis procera (Ait.) R.Br. is one of an ancient traditional shrub, which has been used for the treatment of diabetes, pain and inflammation for thousands of years in India. The root extract of Calotropis procera has been widely used by the tribal?s of district Udaipur, Rajasthan (India) for treatment of diabetes mellitus and its associated complications like diabetic neuropathy. The present study was performed to explore the protective effect of root, stem and leaf extracts of Calotropis procera in diabetes and diabetic neuropathy against tactile allodynia, mechanical hyperalgesia and thermal hyperalgesia in streptozotocin induced diabetic rats.

Materials and methods

Diabetes and peripheral neuropathy were induced in Wistar rats by injection of streptozotocin (45 mg/kg/intraperitoneally). The roots, stem and leaves of Calotropis procera were sequentially extracted with petroleum ether, chloroform, ethyl acetate and methanol. All the extracts were assessed by oral administration at 100 and 250 mg/kg in streptozotocin diabetic rats. The following compounds were used as positive controls: insulin NPH (1 IU/kg/day), metformin (500 mg/kg/day), glibenclamide (2.5 mg/kg/day) and a combination of acarbose (20 mg/kg/day) with methylcobalamine (500 µg/kg/day). In contrast, the streptozotocin induced untreated diabetic rats termed as negative control. Thermal hyperalgesia, mechanical hyperalgesia and tactile allodynia were evaluated in all groups of streptozotocin diabetic rats to assess the extent of neuropathy by Eddy?s hot plate, tail immersion, Randall–Selitto and Von Frey hair tests. The basal nociceptive thresholds were assessed in week 4 of post streptozotocin injection. All groups received their treatment on a regular basis from 28 to 42 days following a confirmation of diabetic neuropathy. The nociceptive thresholds were assessed in all groups in week 5 and 6. The histopathology of pancreas and biochemical estimations of plasma insulin and glycosylated haemoglobin (HbA₁C%) levels were also performed in week 6 of post streptozotocin injection.

Results

The negative control rats developed diabetes and diabetic neuropathy after 6 week of streptozotocin administration distinguished by significant (p<0.01) hyperalgesia and tactile allodynia with enhanced HbA₁C% level compared to normoglycemic rats. Chronic administration of root methanol, stem methanol and leaf ethyl-acetate extracts of Calotropis procera for 2 weeks at 100 and 250 mg/kg doses significantly (p<0.01) attenuated the diabetes induced mechanical hyperalgesia, thermal hyperalgesia, tactile allodynia and HbA₁C% level in streptozotocin diabetic rats as compared to negative control rats. Further, the root methanol extract of Calotropis procera in 100 mg/kg dose showed the regeneration capability of β cells in the histology of pancreas with significant (p<0.01) improvement in plasma insulin level in streptozotocin diabetic rats compared to negative control rats.

Conclusion

Root methanol extract of Calotropis procera (100 mg/kg) has shown ameliorative effect in diabetic neuropathy which may be attributed by its multiple actions including potent hypoglycemic and antioxidant.     

Hippocratic screening of ethanolic extracts from two Tabernaemontana species

Ethanolic extracts of roots, stems, leaves and flowers of Tabernaemontana divaricata and T. pandacaqui were studied by an observational (hippocratic) screening method in rats. Extracts of all plant parts caused sedation, decreased respiration and decreased skeletal muscle tone. Except for the leaf extract of T. pandacaqui, the extracts caused vasodilatation of ear vasculature. Analgesic activity was found for all extracts of both Tabernaemontana species, except for the flower extract of T. divaricata. Lethal doses of the extracts caused the animals to die from respiratory paralysis. Intensity of pharmacological activities was greater with the root and stem extracts. The extracts of T. pandacaqui were more potent than those of T. divaricata.     

Anti-diabetic activity of methanol/methylene chloride stem bark extracts of Terminalia superba and Canarium schweinfurthii on streptozotocin-induced diabetic rats

Stem bark extracts of Terminalia superba Engl. and Diels and Canarium schweinfurthii Engl. are used in Africa for the treatment of various ailments, including diabetes mellitus. The anti-diabetic effects of the methanol/methylene chloride extracts of the stem barks on streptozotocin (STZ)-induced diabetes were evaluated on male rats. Through the subcutaneous route, diabetes was induced using 60 mg/mL of streptozotocin. After 2 days, the rats received, by gavage, 150 mg/kg and 300 mg/kg of extract daily for 14 days. At 300 mg/kg, the two extracts (Terminalia superba and Canarium schweinfurthii), significantly showed at least 67.1% and 69.9% reduction in blood glucose level, respectively, while insulin (three units) given subcutaneously and once daily, had 76.8% reduction compared to diabetic untreated control rats. Similarly, the weight gains were 6.6% and 4.9%, respectively, and were comparable to the normal rats, whereas, diabetic untreated rats lost 14.1% body weight. Still with the same dose, there was 68.5% and 58.5% (p < 0.001) significant decrease in food consumption and 79.7% and 64.0% (p < 0.001) in fluid intake by diabetic rats treated with the respective plant extracts. The insulin-treated rats showed 56.4% and 75.8% decrease in food and fluid intake compared to an augmentation for diabetic control rats, 43.0% and 383.8%, respectively, at the end of the second week of experimentation. These results showed that the plant extracts can reverse hyperglycemia, polyphagia and polydipsia provoked by streptozotocin, and thus, they have anti-diabetic properties.     

Effects of Lythrum salicaria in normoglycemic rats

Several extracts from stem and flower of Lythrum salicaria were evaluated for their hypoglycemic activity in rats. Results indicate that ether extracts from stem or flowers at a dose equivalent to 10 g/kg of crude plant material caused a significant reduction in blood glucose 4 h after oral administration and that this effect was associated with an increase of circulating insulin. The effects of extracts on lipid and carbohydrate metabolism were also studied.     

Antioxidant and hepatoprotective activity of ethanolic and aqueous extracts of Momordica dioica Roxb. leaves

In present study, the hepatoprotective activity of ethanolic and aqueous extracts of Momordica dioica Roxb. leaves were evaluated against carbon tetrachloride (CCl4) induced hepatic damage in rats. The extracts at dose of 200mg/kg were administered orally once daily. The substantially elevated serum enzymatic levels of serum glutamate oxaloacetate transaminase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (SALP) and total bilirubin were restored towards normalization significantly by the extracts. Silymarin was used as standard reference and exhibited significant hepatoprotective activity against carbon tetrachloride induced haptotoxicity in rats. The biochemical observations were supplemented with histopathological examination of rat liver sections. The results of this study strongly indicate that Momordica dioica Roxb. leaves have potent hepatoprotective action against carbon tetrachloride induced hepatic damage in rats. Ethanolic extract was found more potent hepatoprotective. Meanwhile, in vivo antioxidant and free radical scavenging activities were also screened which were positive for both ethanolic and aqueous extracts. This study suggests that possible mechanism of this activity may be due to free radical-scavenging and antioxidant activities which may be due to the presence of flavonoids in the extracts.     

Effect of Hibiscus rosa sinensis Linn. ethanol flower extract on blood glucose and lipid profile in streptozotocin induced diabetes in rats

Blood glucose and total lipid levels were determined in streptozotocin induced diabetic rats after oral administration of an ethanol flower extract of Hibiscus rosa sinensis. A comparable hypoglycemic effect was evidenced from the data obtained after 7 and 21 days of oral administration of the extract and glibenclamide. Maximal diminution in blood glucose (41-46%) and insulin level (14%) was noticed after 21 days. The extract lowered the total cholesterol and serum triglycerides by 22 and 30%, respectively. The increase in HDL-cholesterol was much higher (12%) under the influence of the extract as compared to that of glibenclamide (1%). The hypoglycemic activity of this extract is comparable to that of glibenclamide but is not mediated through insulin release. Other possible mechanisms are discussed.     

Antioxidant activity of Siamese neem tree (VP1209)

Leaves, fruits, flowers and stem bark extracts from the Siamese neem tree (Azadirachta indica A. Juss var. siamensis Valeton, Meliaceae) were assessed for antioxidant activity in vitro using the 1,1-diphenyl-2-picryl hydrazyl (DPPH) scavenging assay, total antioxidant activity and inhibition of lipid peroxidation in Chago K1 cancer cell culture by the thiobarbituric acid reactive substances (TBARS) method. The results showed that leaf aqueous extract, flower and stem bark ethanol extracts exhibited higher free radical scavenging effect on the DPPH assay with 50% scavenging activity at 26.5, 27.9 and 30.6 microg/ml, respectively. The total antioxidant activity of these extracts was found to be 0.959, 0.988 and 1.064 mM of standard trolox, respectively. At 100 microg/ml, the flower ethanol and leaf aqueous extracts significantly decreased malondialdehyde (MDA) levels (46.0 and 50.6%, respectively) by the TBARS method. The results suggest that extracts from leaf, flower and stem bark of the Siamese neem tree have strong antioxidant potential. This report supports the ethnomedical use of young leaves and flowers of this plant as a vegetable bitter tonic to promote good health.     

Hepatoprotective activity of Emblica officinalis and Chyavanaprash

Hepatoprotective activity of Emblica officinalis (EO) and Chyavanaprash (CHY) extracts were studied using carbon tetrachloride (CCl(4)) induced liver injury model in rats. EO and CHY extracts were found to inhibit the hepatotoxicity produced by acute and chronic CCl(4) administration as seen from the decreased levels of serum and liver lipid peroxides (LPO), glutamate-pyruvate transaminase (GPT), and alkaline phosphatase (ALP). Chronic CCl(4) administration was also found to produce liver fibrosis as seen from the increased levels of collagen-hydroxyproline and pathological analysis. EO and CHY extracts were found to reduce these elevated levels significantly, indicating that the extract could inhibit the induction of fibrosis in rats.     

Hypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic rats.

The hypoglycemic effects of water and butanolic extracts prepared from leaves of Cecropia obtusifolia (Cecropiaceae) were examined in streptozotocin induced diabetic rats. A single oral administration of a water extract at doses of 90 and 150 mg/kg and of a butanol extract at doses of 9 and 15 mg/kg significantly (P<0.05) lowered the plasma glucose levels in diabetic rats after 3 h administration. Glibenclamide was used as reference and showed similar hypoglycemic effect to the tested extracts at a dose of 3 mg/kg. The flavone, isoorientin and 3-caffeoylquinic acid (chlorogenic acid), were isolated as the important constituents of the plant and were identified as the main constituents in both extracts, too.     

紫花毕岱提取物对肥胖大鼠血脂及瘦素水平的影响

目的通过紫花毕岱提取物对肥胖大鼠的干预,观察大鼠体重、血脂、血浆瘦素水平的变化及血浆中肝酯酶和脂蛋白酯酶活性的变化,探讨紫花毕岱提取物对肥胖大鼠的减肥作用及机制。方法用高能量饲料造成雄性大鼠肥胖模型,按体重将其随机分为4组,各组均继续给予高能量饲料。肥胖对照组灌胃生理盐水;阳性西药组灌胃盐酸西布曲明;另外2组灌胃紫花毕岱提取物,剂量分别为6、12g／kg。给药6周后,观察紫花毕岱提取物治疗前后大鼠体重、肥胖指数、内脏脂肪重量、血脂、血浆中肝酯酶和脂蛋白酯酶、血浆中瘦素水平的变化。结果给予紫花毕岱提取物治疗后,营养性肥胖大鼠体重、肥胖指数、内脏脂肪重量均明显低于肥胖对照组（P〈0．05）;血浆瘦素水平明显降低（P〈0．01）;紫花毕岱提取物高、低剂量组血三酰甘油、总胆固醇明显降低（P〈0．05）,血浆中肝酯酶和脂蛋白酯酶活性明显升高。结论紫花毕岱提取物灌服6周后对营养性肥胖大鼠有明显减肥作用,该作用未显示与促进血浆瘦素分泌有关,机制可能与紫花毕岱提取物降血脂作用有关。     

Effect of coriander seed (Coriandrum sativum L.) ethanol extract on insulin release from pancreatic beta cells in streptozotocin‐induced diabetic rats

Coriander (Coriandrum sativum L.) is grown as a spice crop all over the world. The seeds have been used to treat indigestion, diabetes, rheumatism and pain in the joints. In the present study, an ethanol extract of the seeds was investigated for effects on insulin release from the pancreatic beta cells in streptozotocin‐induced diabetic rats. Blood samples were drawn from the retro‐orbital sinus before and 1.5, 3 and 5 h after administration of the seed extract. Serum glucose levels were determined by the glucose oxidase method. To determine the insulin releasing activity, after extract treatment the animals were anaesthetized by diethyl ether, the pancreas was excised, fixed in 10% formaldehyde and embedded in paraffin for sectioning. Pancreatic sections of 5 µm were processed for examination of insulin‐releasing activity using an immunocytochemistry kit. The results showed that administration of the ethanol extract (200 and 250 mg/kg, i.p.) exhibited a significant reduction in serum glucose. Administration of streptozotocin decreased the number of beta cells with insulin secretory activity in comparison with intact rats, but treatment with the coriander seed extract (200 mg/kg) increased significantly the activity of the beta cells in comparison with the diabetic control rats. The extract decreased serum glucose in streptozotocin‐induced diabetic rats and increased insulin release from the beta cells of the pancreas. Copyright © 2008 John Wiley & Sons, Ltd.     

Pharmacological activities of extracts of Daniellia oliveri (Rolfe) Hutch. and Dalz. (Leguminosae)

Extracts of the stem bark of Daniellia oliveri using hexane, ethyl acetate and methanol were tested for analgesic, antipyretic and antiinflammatory activities. The hexane extract exhibited a dose related analgesic activity whilst the methanolic extract was active in the induced inflammatory condition. The ethyl acetate extract was relatively inactive and none of the extracts showed any antipyretic activity. Metabolic cage studies showed that a 70% ethanolic extract of the bark caused significant decreases in body weight, food intake, urine and stool output of rats. This extract also exhibited a competitive antagonism on histamine-induced contractions of the guinea-pig ileum and a non-competitive inhibition of acetyl choline-induced contraction of the frog rectus abdominis muscle.     

Antiplasmodial, analgesic, and anti-inflammatory activities of the aqueous extract of the stem bark of Erythrina senegalensis

The in vivo antiplasmodial, analgesic and anti-inflammatory properties of Erythrina senegalensis, an ornamental plant commonly used in Northern Nigeria for the treatment of fevers, was evaluated. Aqueous extracts of the stem bark of the plant was used for the study. The in vivo antiplasmodial activity of the aqueous extract against Plasmodium berghei was assessed using the suppressive and curative test procedures. Analgesic activity was assessed using the acetic acid (0.75%v/v) induced abdominal constriction, while the anti-inflammatory activity was evaluated on egg-albumin induced paw oedema in rats as a model of acute inflammation. The stem bark extract of E. senegalensis exhibited only slight antiplasmodial activity while significant (P<0.05) analgesic and anti-inflammatory effects were observed. Preliminary phytochemical analysis of the extract indicates the presence of alkaloids and glycosides.     

Hypoglycemic effect of Equisetum myriochaetum aerial parts on streptozotocin diabetic rats

The hypoglycemic effect of water as well as butanolic extracts prepared from aerial parts of Equisetum myriochaetum (Equisetaceae) was examined in streptozotocin induced diabetic rats. A single oral administration of the water extract (WE) at doses of 7 and 13 mg/kg and of the butanol extract (BE) at doses of 8 and 16 mg/kg significantly (P<0.001) lowered the plasma glucose levels in diabetic rats after three hours of the administration. As a reference drug glibenclamide was used and showed, at a dose of 3 mg/kg, similar hypoglycemic effect like the tested extracts. Three kaempferol glucosides and one caffeoyl glucoside were isolated from the drug and were shown to be the main constituents in both extracts.     

Preliminary studies on antihepatotoxic effect of Physalis peruviana Linn. (Solanaceae) against carbon tetrachloride induced acute liver injury in rats

Physalis peruviana is a medicinal herb used by Muthuvan tribes and Tamilian native who reside in the shola forest regions of Kerala, India against jaundice. It was evaluated for its antihepatotoxic, phytochemical analysis and the acute toxicity of the most promising extract in rats. Water, ethanol and hexane extracts of Physalis peruviana (500mg/kg body weight) showed antihepatotoxic activities against CCl(4) induced hepatotoxicity. The ethanol and hexane extracts showed moderate activity compared to water extract, which showed activity at a low dose of 125mg/kg. The results were judged from the serum marker enzymes. Histopathological changes induced by CCl(4) were also significantly reduced by the extract. Further, the extract administration to rats resulted in an increase in hepatic GSH and decrease in MDA. Preliminary phytochemical analysis revealed the presence of various components in the crude aqueous extract. The extract was found to be devoid of any conspicuous acute toxicity in rats.     

Hypoglycemic effect of aqueous extract of seabuckthorn (Hippophae rhamnoides L.) seed residues in streptozotocin‐induced diabetic rats

An extract of seabuckthorn (Hippophae rhamnoides L.) seed residues has been shown to possess hypoglycemic and hypolipidemic properties in normal mice. The present study investigated the effects of an aqueous extract of seabuckthorn seed residues (ASSR) on serum glucose, lipid profiles and antioxidant parameters in streptozotocin‐induced diabetic rats. Male Sprague‐Dawley rats were divided into four groups: a normal control group; diabetic control group; diabetic groups supplemented with 5 mg/kg body weight glibenclamide (reference drug) and 400 mg/kg body weight ASSR. Diabetes in rats was induced by intraperitoneal injection of streptozotocin (45 mg/kg body weight). Vehicle (distilled water), glibenclamide and ASSR were administered orally to normal and diabetic rats once a day lasting for 4 weeks. The data showed that administration of ASSR significantly lowered the serum glucose, triglyceride and nitric oxide levels in diabetic rats. Moreover, ASSR treatment also increased serum superoxide dismutase activity and glutathione level markedly. These results show that ASSR has hypoglycemic, hypotriglyceridemic and antioxidant effects in streptozotocin‐induced diabetic rats, suggesting that ASSR supplementation can be useful in preventing diabetic complications associated with hyperlipidemia and oxidative stress. Copyright © 2009 John Wiley & Sons, Ltd.     

Recovery of oral glucose tolerance by wistar rats after treatment with Coreopsis tinctoria infusion

Infusions of Coreopsis tinctoria flowering tops have traditionally been used in Portugal to control hyperglycaemia but no pharmacological or toxicological studies have been reported until now. The chalcones marein and okanin were isolated from the aqueous extract, together with the 2S‐3′,4′,7,8‐tetrahydroxyflavanone. The content of marein in extracts was determined by HPLC‐UV and the radical scavenging capacity evaluated by the DPPH method (EC₅₀ = 21 µg/mL). Glucose intolerance was induced by a single intraperitoneal injection of streptozotocin in saline (40 mg/Kg). After three weeks of oral treatment with C. tinctoria extract (500 mg/Kg/day) the animals were no longer glucose‐intolerant (p > 0.05). Additionally, this oral treatment caused no hepatotoxicity in the rats, as determined by blood alanine and aspartate transaminases. A single administration of extract had no effect on oral glucose tolerance in normal Wistar rats. The extract also had no effect on insulin secretion by MIN6 cells. In conclusion, C. tinctoria infusion is able to abolish the streptozotocin‐induced glucose‐intolerance in rats after three weeks of oral treatment by a mechanism other than induction of insulin secretion. The recovery of β‐pancreatic function mediated by an antioxidant mechanism is a possibility that deserves further investigation. Copyright © 2009 John Wiley & Sons, Ltd.     

Antidiabetic activity of standardized extract of Quassia amara in nicotinamide-streptozotocin-induced diabetic rats

The aim of the present study was to evaluate the efficacy of a standardized methanol extract of Quassia amara L. (Family: Simaroubaceae) in nicotinamide–streptozotocin‐induced diabetic rats. Non insulin dependent diabetes mellitus was induced by streptozotocin in rats pre‐treated with nicotinamide. Diabetic rats were treated with oral doses of Quassia amara extract (QaE; 100 and 200 mg/kg) or glibenclamide (10 mg/kg; as standard). QaE and glibenclamide were administered as a suspension in 0.3% carboxy methyl cellulose for 14 days. Control animals received an equal volume of vehicle. Blood samples were collected by retro‐orbital puncture on day 14, 1 h after last treatment. Plasma glucose, insulin and lipid parameters (total cholesterol, LDL‐C, HDL‐C and triglycerides) were measured using commercially available biochemical kits. The oral glucose tolerance test was performed to evaluate the effect of the extract on peripheral glucose utilization in normal rats. Both doses of QaE significantly (p < 0.01) reduced elevated fasting blood glucose levels in diabetic rats. In the oral glucose tolerance test, QaE treatment significantly increased (p < 0.05) the glucose tolerance compared with the vehicle. QaE and glibenclamide, effectively normalized dyslipidemia associated with streptozotocin‐induced diabetes. The findings of the present study indicate that Quassia amara extract may be potentially valuable in the treatment of diabetes and associated dyslipidemia. Copyright © 2011 John Wiley & Sons, Ltd.     

Effect of Sclerocarya birrea (Anacardiaceae) stem bark methylene chloride/methanol extract on streptozotocin-diabetic rats

Sclerocarya birrea (Anacardiaceae) is used as a traditional treatment of diabetes in Cameroon. In this study, we investigated the possible antidiabetic effect of the stem bark extract in diabetic rats. Diabetes was induced by intravenous injection of streptozotocin (STZ, 55 mg/kg) to male Wistar rats. Experimental animals (six per group), were treated by oral administration of plant extract (150 and 300 mg/kg body weight) and metformin (500 mg/kg; reference drug) for comparison, during 21 days. The stem bark methanol/methylene chloride extract of Sclerocarya birrea exhibited at termination, a significant reduction in blood glucose and increased plasma insulin levels in diabetic rats. The extract also prevented body weight loss in diabetic rats. The effective dose of the plant extract (300 mg/kg) tended to reduce plasma cholesterol, triglyceride and urea levels toward the normal levels. Four days after diabetes induction, an oral glucose tolerance test (OGTT) was also performed in experimental diabetic rats. The results showed a significant improvement in glucose tolerance in rats treated with Sclerocarya birrea extract. Metformin, a known antidiabetic drug (500 mg/kg), significantly decreased the integrated area under the glucose curve. These data indicate that Sclerocarya birrea treatment may improve glucose homeostasis in STZ-induced diabetes which could be associated with stimulation of insulin secretion.