Antihyperlipidemic effect of Garlip, a polyherbal formulation in streptozotocin induced diabetic rats

This study was undertaken to investigate the effect of Garlip, a polyherbal drug composed of aqueous extract of six medicinal plants on blood glucose, plasma insulin, tissue lipid profile, and lipidperoxidation in streptozotocin induced diabetic rats. Aqueous extract of Garlip a, polyherbal drug was administered orally (200 mg/kg body weight) for 30 days. The different doses of Garlip on blood glucose and plasma insulin in diabetic rats were studied and the levels of lipid peroxides (TBARS and Hydroperoxide) and tissue lipids (cholesterol, triglyceride, phospholipids and free fatty acids) were also estimated in streptozotocin induced diabetic rats. The effects were compared with tolbutamide. Treatment with Garlip and tolbutamide resulted in a significant reduction of blood glucose and increase in plasma insulin. Garlip also resulted in a significant decrease in tissue lipids and lipid peroxide formation. The effect produced by Garlip was comparable with that of tolbutamide. The decreased lipid peroxides and tissue lipids clearly showed the antihyperlipidemic and antiperoxidative effect of Garlip apart from its antidiabetic effect.     

Nootropic,anxiolytic and CNS-depressant studies on different plant sources of shankhpushpi

Context: Shankhpushpi, a well-known drug in Ayurveda, is extensively used for different central nervous system (CNS) effects especially memory enhancement. Different plants are used under the name shankhpushpi in different regions of India, leading to an uncertainty regarding its true source. Plants commonly used under the name shankhpushpi are: Convolvulus pluricaulis Chois., Evolvulus alsinoides Linn., both from Convolvulaceae, and Clitoria ternatea Linn. (Leguminosae).

Objective: To find out the true source of shankhpushpi by evaluating and comparing memory-enhancing activity of the three above mentioned plants. Anxiolytic, antidepressant and CNS-depressant activities of these three plants were also compared and evaluated.

Materials and methods: The nootropic activity of the aqueous methanol extract of each plant was tested using elevated plus-maze (EPM) and step-down models. Anxiolytic, antidepressant and CNS-depressant studies were evaluated using EPM, Porsolt’s swim despair and actophotometer models, respectively.

Results: C. pluricaulis extract (CPE) at a dose of 100?mg/kg, p.o. showed maximum nootropic and anxiolytic activity (p < 0.001). E. alsinoides extract (EAE) and C. ternatea extract (CTE) showed maximum memory-enhancing and anxiolytic activity (p < 0.001) at 200 and 100?mg/kg, respectively. Amongst the three plants, EAE and CTE showed significant (p < 0.05), while CPE did not exhibit any antidepressant activity. All the three plants showed CNS-depressant action at higher dose levels.

Discussion and conclusions: The above results showed all the three plants possess nootropic, anxiolytic and CNS-depressant activity. The results of memory-enhancing activity suggest C. pluricaulis to be used as true source of shankhpushpi.     

The pharmacokinetics of dronedarone in normolipidemic and hyperlipidemic rats

The objectives of the current study were to characterize the pharmacokinetic profile of dronedarone in the rat, and to examine the effect of hyperlipidemia on its pharmacokinetics. Single doses of dronedarone were administered to rats intravenously (4 mg/kg), orally (55 mg/kg) and intraperitoneally (65 mg/kg). To induce hyperlipidemia, some of the rats were administered intraperitoneal doses of poloxamer 407 before giving an oral dose of dronedarone. After intravenous doses of 4 mg/kg dronedarone, plasma clearance and volume of distribution at steady‐state were 25.1 ± 8.09 mL/min/kg and 10.8 ± 4.77 L/kg, respectively. After oral doses the maximum plasma concentrations (Cmax) and their median time of attainment (tmax) were 1.87 ± 1.65 mg/mL and 3.5 h, respectively. Intraperitoneal administration of 65 mg/kg dronedarone base yielded plasma Cmax and median tmax of 0.816 ± 0.611 mg/mL and 3 h, respectively. Protein binding was high in NL and HL plasma. Dronedarone is extensively distributed with high volume of distribution in the rat. The drug showed poor bioavailability (<20%) after oral and intraperitoneal administration. The increased plasma concentrations after oral dosing to hyperlipidemic rats appears to be attributable to a direct effect on metabolizing enzymes or transport proteins. Copyright © 2016 John Wiley & Sons, Ltd.     

Antihyperlipidemic effect of aqueous extract of Plumbago zeylanica roots in diet-induced hyperlipidemic rat

This study examined the antihyperlipidemic effect of the aqueous extract of Plumbago zeylanica Linn. (Plumbaginaceae) roots in diet-induced hyperlipidemic rats. The oral administration of the aqueous extract at the dose of 20, 40, and 80?mg kg^?1 were found to ameliorate the hyperlipidemic condition as evidenced by a reduction of cholesterol and triglyceride levels. The standards fenofibrate (20?mg kg^?1) and atorvastatin (8?mg kg^?1) were also found to exhibit significant (p?<?0.05) cholesterol and triglyceride lowering effect. Further, the aqueous extract at all doses demonstrated a significant (p?<?0.05) increase in fecal cholesterol excretion indicating a reduction in intestinal cholesterol absorption. Additionally, the activity of lipogenic enzymes like HMGCoA reductase in the liver remained significantly (p?<?0.05) low on treatment of aqueous extract (80?mg kg^?1), thus decreasing the cholesterogenesis. The aqueous extract (20, 40 and 80?mg kg^?1) also significantly (p?<?0.05) reduced the total lipid content in the liver. Moreover, the aqueous extract demonstrated a potential antioxidant capacity in DPPH and TBARS in vitro antioxidant assay. Thus the results suggest a beneficial role of aqueous extract of Plumbago zeylanica roots in ameliorating the hyperlipidemic condition leading to atherosclerosis.     

武汉地区2000～2002年降脂药用药情况分析

目的：探讨武汉地区降脂药的应用状况及市场趋势。方法：分类统计武汉地区2000～2002年降脂药数据资料。结果：他汀类作为降脂药中的一线药物，占有58．22％的份额，具有很大优势。结论：合理选择疗效确切的降脂药意义重大。     

Clitoria ternatea ameliorated the intracerebroventricularly injected streptozotocin induced cognitive impairment in rats: behavioral and biochemical evidence

Rationale

Clitoria ternatea, commonly known as Aparajita, is used as Medhya rasayana in Ayurveda. The role of C. ternatea in experimental models of cognitive impairment is yet to be explored.

Objectives

The present study was designed to study the effect of aqueous and hydroalcoholic extracts of C. ternatea on biochemical and behavioral parameters related to cognitive impairment in in vitro and in vivo studies.

Methods

In vitro free radical scavenging and enzyme-inhibitory (cholinesterase, glycogen synthase kinase-3-β, rho kinase, prolyl endopeptidase, catechol-O-methyl transferase, and lipoxygenase) activities of aqueous and hydroalcoholic extracts of C. ternatea plant were evaluated. Based on in vitro results, hydroalcoholic extract of C. ternatea (100, 300, and 500 mg/kg, p.o.) was selected for evaluation in intracerebroventricularly injected streptozotocin (STZ)-induced cognitive impairment in male Wistar rats. Behavioral assessment was performed at baseline and on the 14th, 21st, and 28th days after STZ injection using elevated plus maze, passive avoidance, Morris water maze, and photoactometer. Oxidative stress parameters (malondialdehyde, reduced glutathione, nitric oxide levels, and superoxide dismutase activity), cholinesterase activity, and rho kinase (ROCK II) expression were studied in cerebral cortex and hippocampus of rats' brain at the end of the study.

Results

The hydroalcoholic extract possessed significantly more in vitro antioxidant and enzyme-inhibitory activities as compared to aqueous extract. The hydroalcoholic extract of C. ternatea prevented STZ-induced cognitive impairment dose dependently by reducing oxidative stress, cholinesterase activity, and ROCK II expression.

Conclusion

In vitro and in vivo results suggest the potential of hydroalcoholic extract of C. ternatea for treatment of cognitive deficit in neurological disorders.     

Evaluation of antinociceptive effect of methanolic leaf and root extracts of Clitoria ternatea Linn. in rats

Aim:

Clitoria ternatea Linn. (C. ternatea) is an Ayurvedic herb traditionally used as medicine to relieve inflammatory, rheumatism, ear diseases, fever, arthritis, eye ailments, sore throat and body ache. This study aims to evaluate and elucidate the possible mechanism underlying the antinociceptive action of methanolic extracts of C. ternatea leaf and root using several antinociception models.

Materials and Methods:

The different antinociception models such as hot plate, tail-flick and formalin tests were used along with naloxone (a non-selective opioid antagonist) to establish the antinociceptive activity of both leaf and root extracts.

Results:

Both C. ternatea leaf and root extracts markedly demonstrated antinociceptive action in experimental animals. Results of formalin test showed that the antinociceptive activity of the extracts may be mediated at both central and peripheral level. Moreover, the results of hot plate and tail-flick tests further implies that C. ternatea root extract mediates antinociceptive activity centrally at supraspinal and spinal levels whereas, the C. ternatea leaf extract''s antinociceptive activity is mediated centrally at supraspinal level only. It is believed that the opioid receptors are probably involved in antinociceptive activity of both C. ternatea root extract.

Conclusions:

Our studies support the traditional use of C. ternatea leaf and root against pain. The extracts can also be utilised as a new source of central analgesics in treatment of pain.KEY WORDS: Anti-inflammatory, antinociceptive, C. ternatea, opioid receptors     

喃氟啶从Poloxamer407凝胶基质中的体外释放

目的:观察Poloxamer 407凝胶的形成及液体/凝胶互相转化的条件和喃氟啶在该凝胶中的体外释放.方法:以磷酸盐缓冲液[pH(7.40±0.01)作为Poloxamer 407的稀释剂,以喃氟啶作为实验药物做体外溶出.结果:Poloxmer 407的浓度在15%～40%之内时,随着温度从0℃上升到37℃,其混合物从液体迅速转化成凝胶.相变温度随着Poloxamer407的浓度升高而降低.喃氟啶在该凝胶中的体外释放为零级释放,且随Poloxamer 407浓度的增加,释放速度变慢.8h时.含Poloxamer 407分别为20%,25%,30%,35%(m/m)的凝胶中时喃氟啶的累积释放率分别是(98.22±0.12)%,(86.20±0.20)%,(68.25±0.14)%,(50.02±0.08)%.结论:鉴于Poloxamr 407所具有的特殊的逆温相变性质,作为血管外注射型缓释植入剂的载体是有前途的.     

Clitoria ternatea (Linn) root extract treatment during growth spurt period enhances learning and memory in rats

Neonatal rat pups (7 days old) were intubated with either 50 mg/kg body weight or 100 mg/kg body weight of aqueous root extract of Clitoria ternatea (CTR) for 30 days. These rats were then subjected to open field, two compartment passive avoidance and spatial learning (T-Maze) tests (i) immediately after the treatment and (ii) 30 days after the treatment, along with age matched normal and saline control rats. Results showed no change in open field behaviour, but showed improved retention and spatial learning performance at both time points of behavioural tests, indicating the memory enhancing property of CTR which implicates a permanent change in the brain of CTR treated rats.     

Evaluation of anti-osteoarthritic activity of Vigna mungo in papain induced osteoarthritis model

Aim:This study was carried out to evaluate the effect of Vigna mungo hydroalcoholic extract (VMHA) by papain induced osteoarthritis (OA) in the rat model.Results:VMHA improved inflammatory condition with all the doses, but significant (P < 0.05) attenuation of inflammation was present only with 400 mg/kg dose. The grip strength, locomotion activity and hanging time were also significantly (P < 0.05) improved at dose level of 100 mg/kg however other two doses (200 mg/kg and 400 mg/kg) were not found to be effective. VMHA did not show any mortality or any toxic clinical signs after oral administration of 2 g/kg dose.Conclusion:VMHA improved arthritic condition by significantly reducing pain and inflammation.KEY WORDS: Grip strength, inflammation, osteoarthritis, papain     

Hypolipidemic effects of Solidago chilensis hydroalcoholic extract and its major isolated constituent quercetrin in cholesterol-fed rats

Abstract

Context: Despite several studies on the effects of Solidago chilensis Meyen (Asteraceae), the phytochemical and hypolipidemic properties remain underappreciated.

Objective: This study evaluates the hypolipidemic and antioxidant effects of hydroalcoholic extract (HE) and quercetrin from S. chilensis aerial parts in cholesterol-fed rats.

Materials and methods: The HE was analyzed by high-performance liquid chromatography, followed by quercetrin isolation. Hypercholesterolemic rats (1% cholesterol and 0.5% cholic acid for 15?d) were treated with HE (150, 300, and 600?mg/kg p.o.; n?=?6), simvastatin (4?mg/kg p.o.; n?=?6), or quercetrin (10?mg/kg p.o.; n?=?6) once a day for 30?d. During this period, a high-cholesterol diet was maintained until the 30th day of treatment.

Results: Rats treated with HE (150, 300, and 600?mg/kg) and quercetrin showed decreased serum levels of total cholesterol (?19.9, ?27.5, ?31.0, and ?39.4%), lipoprotein-cholesterol (?36.0, ?37.5, ?43.3, and ?59.4%), and triacylglycerides (?15.6, ?23.5, ?29.8, and ?27.2%) when compared with the control group similar to simvastatin. Moreover, treatment with HE and quercetrin decreased hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase activity (35.1% on average) and increased fecal cholesterol levels (38.2% on average).

Discussion and conclusions: Our results suggest that hypolipidemic effects of HE are associated with it modulating the activity of HMG-CoA reductase and its interference in the reabsorption and/or excretion of intestinal lipids. Solidago chilensis and its main constituent, quercetrin, may thus be effective as cholesterol-lowering agents and in preventing atherosclerosis.     

不同因素对去甲斑蝥素—泊洛沙姆407缓释制剂体外释放度的影响

目的：了解溶出介质温度、转盘速度及泊洛沙姆407浓度对去甲斑蝥素／泊洛沙姆407缓释制剂释放动力学的影响。方法：采用紫外分光光度法,对去甲斑蝥素在不同情况下的体外释放度进行考察。结果：去甲斑蝥素随泊洛沙姆407凝胶的溶解而逐步释放,随着介质温度升高、转盘速度加快及辅料浓度的降低,去甲斑蝥素释放度相应增加。结论：去甲斑蝥素从泊洛沙姆407中的释放速度与介质温度、转蓝速度呈线性正相关,而与泊洛沙姆407的浓度呈线性负相关。     

新目安眼用即型凝胶与普通凝胶兔眼内药动学特性比较研究

目的 探索新目安眼用即型凝胶相变过程对兔眼内房水中药物药动学特性的影响，并与普通凝胶比较，评价该即型凝胶的剂型特征。方法 以新西兰家兔为试验对象，采用眼部给予新目安眼用即型凝胶（存在相变过程）和普通凝胶后，按时间点取房水，测定更昔洛韦含量，建立药物在房水中的药动学方程，计算体内药动学参数，比较两者的差别。结果 新目安眼用即型凝胶房水中更昔洛韦药动学方程为C=18.94×e^{-0.015 4 t}-18.94×e^{-0.079 85 t}，普通凝胶房水中更昔洛韦药动学方程为C=15.42×e^{-0.015 3 t}-15.42×e^{-0.048 8 t}，说明两者在兔眼内的药动学机制相同。从各药动学参数比较分析，新目安眼用即型凝胶由于相变过程使达峰时间仅为25.51 min，达峰浓度高达10.31 μg·mL^-1，吸收半衰期缩短为8.679 min，AUC提高到992.4 μg·mL^-1·min，而普通凝胶达峰时间为34.63 min，达峰浓度仅为6.232 μg·mL^-1，吸收半衰期为14.20 min，AUC仅为691.4 μg·mL^-1·min。结论 即型凝胶相转变过程能将相变潜能（△H）转变成药物角膜渗透的动能，可最大限度发挥药效。     

雌二醇阴道用生物黏附性温敏型凝胶的处方筛选及流变学考察

目的:研制雌二醇阴道用生物黏附性温敏型凝胶(E₂-VTISG),并进行热力学和流变学考察。方法:采用冷法工艺制备E₂-VTISG。采用倒试管法测定胶凝温度(T_gel),以T_gel为考察指标,泊洛沙姆P407,泊洛沙姆P188为主要影响因素,用星点设计-效应面法进行处方筛选。采用黏度计测定表观粘度,采用动态流变学实验测定温敏凝胶在相变过程中的流变参数。结果:雌二醇阴道用生物黏附性温敏型凝胶的最优处方的基质配比为P407:P188:甘油:PCP:尼泊金乙酯=18:2.96:5:0.2:0.2,实测胶凝温度为33.4℃。结论:星点设计-效应面法筛选E₂-VTISG处方预测性良好,流变学结果显示优化后的雌二醇温敏凝胶符合阴道局部用药要求。     

Influence of clitoria ternatea extracts on memory and central cholinergic activity in rats

Clitoria ternatea , commonly known as Shankpushpi, is widely used in the traditional Indian system of medicine as a brain tonic and is believed to promote memory and intelligence. We examined the effectiveness of alcoholic extracts of aerial and root parts of C. ternatea at 300 and 500 mg/kg doses orally in rats in attenuating electroshock-induced amnesia. Extracts at 300 mg/kg dose produced significant memory retention, and the root parts were found to be more effective. In order to delineate the possible mechanism through which C. ternatea elicits the anti-amnesic effects, we studied its influence on central cholinergic activity by estimating the acetylcholine content of the whole brain and acetylcholinesterase activity at different regions of the rat brain, viz., cerebral cortex, midbrain, medulla oblongata and cerebellum. Our results suggest that C. ternatea extracts increase rat brain acetylcholine content and acetyl cholinesterase a ctivity in a similar fashion to the standard cerebro protective drug Pyritinol.     

The effect of poloxamer 407 on the functional properties of HDL in mice

Objectives There is an inverse relationship between high‐density lipoprotein (HDL) and heart disease. HDL possesses not only both antioxidant and anti‐inflammatory properties, but also anti‐thrombotic and endothelial function‐promoting qualities. However, it is not only the serum concentration of HDL that is important, but also the ‘functional’ quality of the HDL. The objective was to determine the functional status of HDL in a well‐established mouse model of dyslipidaemia and atherosclerosis induced by the administration of a block copolymer (poloxamer 407; P‐407). Methods C57BL/6 mice were administered a single intraperitoneal dose of P‐407 (0.5 g/kg) and blood was collected at 24 h post‐dosing. HDL was isolated from controls (control HDL) and P‐407‐treated (P‐407 HDL) mice and used to test its anti‐inflammatory properties in vitro. Additionally, antioxidant enzymes associated with HDL, namely, platelet activating factor‐acetylhydrolase (PAF‐AH) and paraoxonase (PON), were evaluated for any potential reduction in their biological activity. Key findings A single injection of P‐407 in C57BL/6 mice resulted in a marked decrease in the levels of HDL‐cholesterol and phospholipids. HDL particle size significantly increased, primarily due to remodelling of HDL with triglyceride. It was demonstrated that (i) long‐chain saturated fatty acids were higher and the n‐3/n‐6 fatty acid ratio was significantly lower for P‐407 HDL compared with control HDL, and (ii) P‐407 HDL lost its capacity to inhibit tumour necrosis factor‐α (TNF‐α)‐induced vascular cell adhesion molecule‐1 (VCAM‐1) expression compared with control HDL. Additionally, P‐407 HDL was not able to neutralize lipopolysaccharide and inhibit subsequent TNF‐α production compared with control HDL. The biological activity of platelet‐activating factor acetylhydrolase (PAF‐AH) and paraoxonase (PON) decreased in direct proportion to the circulating levels of both HDL‐cholesterol and apolipoprotein (apoA‐1). Conclusions Combination of previously reported findings in P‐407‐treated mice, such as (i) production of both oxidized LDL and malondialdehyde, and (ii) profound elevations in the soluble forms of intercellular adhesion molecule‐1 (ICAM‐1), VCAM‐1, and E‐selectin, with the present results, would strongly suggest that HDL in P‐407‐treated mice is rendered dysfunctional. Thus, these findings help to explain why P‐407‐treated mice begin to form aortic atherosclerotic lesions about one month after initiating P‐407 treatment.     

Antihyperlipidemic activity of Salacia chinensis root extracts in triton-induced and atherogenic diet-induced hyperlipidemic rats

Objectives:

The aim of this study has been to investigate the possible antihyperlipidemic effect of Salacia chinensis root extract in triton (400mg/kg b.w.)-induced and atherogenic diet-induced hyperlipidemic rats.

Materials and Methods:

Petroleum ether (60-80°C), chloroform, ethanol and aqueous extracts of Salacia chinensis roots were evaluated for antihyperlipidemic activity in triton- and atherogenic diet-induced hyperlipidemic rats. A comparison was also made between the action of Salacia chinensis root extract and a known antihyperlipidemic drug simvastatin (10 mg/kg body wt.). The results of the study were expressed as mean± S.E. and data was analyzed by using one way analysis of variance test (ANOVA) followed by Dunnett''s t-test for multiple comparisons. Values with P < 0.05 were considered as significant.

Results:

Oral administration of 500 mg/kg body wt. of the chloroform extract and alcoholic extract of Salacia chinensis root exhibited a significant reduction (P<0.01) in serum lipid parameters like total cholesterol, triglycerides, low density lipoprotein (LDL), very low density lipopreotein (VLDL) and increase in high density lipoprotein (HDL) in hyperlipidemic rats of both models as compared to hyperlipidemic control statistically. These extracts were found to possess better antihyperlipidemic potential as compared to pet ether and aqueous extract.

Conclusions:

Our results demonstrated that chloroform and alcoholic extract of Salacia chinensis roots possessed significant antihyperlipidemic activity and hence it could be a potential herbal medicine as adjuvant with existing therapy for the treatment of hyperlipidemia.KEY WORDS: Hyperlipidemia, Salacia chinensis, simvastatin, triton