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Contemporary Development In NPYY5 Receptor Antagonist NPYY5受体拮抗剂的研究进展
Pub Date : 2008-12-31 DOI: 10.5580/793
Daxesh P. Patel, N. Patel
The prevalence of obesity continues to increase throughout the world and the burden of obesity and related co morbidities is large. Contemporary consideration has focused on physiology of neuropeptide Y and its role in the regulation of energy homeostasis. The data obtained to date with these newly developed tools suggests that neuropeptide Y receptor antagonists, particularly neuropeptide YY5 receptor antagonist, have potentiality to bless the obesity patients worldwide. However, the redundancy of the neurochemical systems regulating energy homeostasis may limit the effect of ablating a single pathway. New leads are under research by major pharmaceutical companies to limit the side effects and explore the area to meet clinical requirement.
肥胖的患病率在世界范围内持续增加,肥胖和相关并发症的负担很大。目前的研究主要集中在神经肽Y的生理作用及其在能量稳态调节中的作用。迄今为止,这些新开发的工具所获得的数据表明,神经肽Y受体拮抗剂,特别是神经肽YY5受体拮抗剂,有可能为全世界的肥胖患者带来福音。然而,调节能量稳态的神经化学系统的冗余可能会限制单个通路的消融效果。大型制药公司正在研究新的先导药物,以限制副作用并探索满足临床需求的领域。
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引用次数: 0
Pharmacological Basis For Antianaphylactic, Antihistaminic And Mast Cell Stabilization Activity Of Ocimum Sanctum 天竺葵抗过敏、抗组胺和肥大细胞稳定活性的药理学基础
Pub Date : 2008-12-31 DOI: 10.5580/bc4
G. Sridevi, P. Gopkumar, S. Ashok, C. Shastry
Purpose: The present paper reports the antianaphylactic, antihistaminic and mast cell stabilization activity of Ocimum sanctum leaf extract on various experimental models. Methods: After optimizing the dose the extract was tested for its therapeutic activity using Wistar rats and Duncan Hartley guinea pigs. The antianaphylactic activity was investigated in rats using the active anaphylaxis model. The effect on mast cell stabilization was performed by ex vivo challenge of antigen in sensitized rat intestinal mesenteries. Antihistaminic activity was studied in guinea pigs using histamine-induced bronchospasm where preconvulsive dyspnea was used as an end point following exposure to histamine aerosol. Results: The findings from various studies reveal that the antihistaminic and antianaphylactic activity of extract which is mainly due to its mast cell stabilizing potential, suppression of IgE, and inhibition of release of inflammatory mediators Conclusion: Thus use of Ocimum sanctum leaves proved the strong rationale behind the mentioned therapeutic activities.
目的:在不同的实验模型上报道了麝香叶提取物的抗过敏、抗组胺和肥大细胞稳定活性。方法:优化剂量后,采用Wistar大鼠和Duncan Hartley豚鼠对提取物进行治疗作用试验。采用大鼠活动性过敏反应模型研究其抗过敏活性。在致敏的大鼠肠系膜中,通过体外激发抗原对肥大细胞的稳定作用。使用组胺诱导支气管痉挛的豚鼠研究了抗组胺活性,其中惊厥前呼吸困难被用作暴露于组胺气溶胶后的终点。结果:各种研究结果表明,提取物的抗组胺和抗过敏活性主要是由于其具有稳定肥大细胞的潜力,抑制IgE,抑制炎症介质的释放。结论:因此,使用茴香叶证明了上述治疗活性背后的强大原理。
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引用次数: 14
Cyclooxygenase isoforms in health and disease 环加氧酶在健康和疾病中的异构体
Pub Date : 2008-12-31 DOI: 10.5580/21fc
Asma Saqib, C. Karigar
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) have long been used for the treatment of pain and inflammation owing to their inhibitory effects on cyclooxygenase (COX). Ever since NSAIDs have been in use, multiple adverse effects have been noted. Assessment of many of these effects has been complicated due to the discovery of multiple splice variants of the COX gene, greater array of COX and specific COX-2 inhibitor availability. The effect of these drugs on COX cannot be readily explained. This has sparked a new field of investigation on splice variants of COX and effects of COX inhibitors. This review summarizes our current understanding of the role of cyclooxygenase in health and disease.
非甾体抗炎药(NSAIDs)由于其抑制环氧化酶(COX)的作用,长期以来被用于治疗疼痛和炎症。自从使用非甾体抗炎药以来,已经注意到多种不良反应。由于COX基因的多剪接变异体的发现,更多的COX阵列和特异性COX-2抑制剂的可用性,许多这些影响的评估变得复杂。这些药物对COX的影响还不能轻易解释。这为研究COX的剪接变异体和COX抑制剂的作用开辟了新的领域。本文综述了目前对环加氧酶在健康和疾病中的作用的认识。
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引用次数: 6
Anxiolytic activity of root extracts of Cardiospermum halicacabum in mice 心芹根提取物对小鼠抗焦虑活性的影响
Pub Date : 2008-12-31 DOI: 10.5580/1e23
Shailesh Malaviya, K. Nandakumar, J. Vaghasiya, Ys Bhalodiya, N. Jivani, N. Sheth, Ravi A. Manek, SP Chauhan
The present study was designed to investigate anti anxiety effects of alcoholic and aqueous root extracts of Cardiospermum halicacabum in mice. Mice were treated with the alcoholic or aqueous extract (100 or 300 mg/kg p.o.) 1 hr before subjecting the animals to various anxiety models. Anti anxiety activity was evaluated using elevated plus maze (EPM), light-dark model (LDM) and open field test (OFT). In EPM, treatment with alcoholic and aqueous extracts increased the time spent in open arm and total locomotion time. In light dark model treatment with these extracts showed increase in time spent in light compartment and in Open field test treatment with these extracts increased the time spent in central compartment. These results suggest that alcoholic and aqueous extracts of Cardiospermum halicacabum possess anti anxiety activity.
本研究旨在探讨心芹醇提物和水提物对小鼠的抗焦虑作用。小鼠在建立各种焦虑模型前1小时用酒精或水提取物(100或300 mg/kg)治疗。采用升高+迷宫(EPM)、光暗模型(LDM)和开阔场试验(OFT)评价抗焦虑活性。在EPM中,酒精和水提取物处理增加了张开臂的时间和总运动时间。在光暗模型中,用这些提取物处理的小鼠在光室的时间增加,而在空地试验中,用这些提取物处理的小鼠在中央室的时间增加。结果表明,心芹醇提液和水提液具有抗焦虑作用。
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引用次数: 9
Paliperidone ER - A novel antipsychotic 帕利哌酮ER -一种新型抗精神病药
Pub Date : 2008-12-31 DOI: 10.5580/1ed0
S. Deshmukh, T. Bhat, N. Bachewar, Anil Joshi, Harshal Rathod
Paliperidone ER is metabolite of risperidone (9-hydroxy-risperidone) formulated as OROS extended release system, which facilitates its once daily use and improves treatment compliance. It is indicated not only in schizophrenia but also in schizoaffective disorder and bipolar mania. Due to lack of interactions of CYP enzymes, minimal or no pharmacological interactions are evident. Due to favorable pharmacodynamic profile i.e. antagonism of 5HT 2A , �± 1 and D2; it has improved positive and negative symptoms (reduction in PANSS score), reduced extra pyramidal side effects and efficacy. Only renal failure patients demand dose reduction. In various therapeutic trials, paliperidone ER has shown better efficacy than placebo and olanzapine, also delays symptoms recurrence of schizophrenia. Paliperidone ER has caused various adverse effects like akathisia, headache, increase serum prolactin level and weight gain but serum lipid, glucose and insulin level remained unaffected. Paliperidone ER has increased the number of annual stable days and more cost effective than other atypical antipsychotics.
帕利培酮ER是利培酮(9-羟基利培酮)的代谢物,配制成OROS缓释体系,方便每日一次使用,提高治疗依从性。它不仅适用于精神分裂症,也适用于分裂情感性障碍和双相躁狂症。由于缺乏相互作用的CYP酶,很少或没有药理相互作用是明显的。由于良好的药效学特征,即5HT 2A,±1和D2的拮抗;它改善了阳性和阴性症状(减少了PANSS评分),减少了额外的锥体副作用和疗效。只有肾衰竭患者需要减量。在各种治疗试验中,帕利哌酮ER已显示出优于安慰剂和奥氮平的疗效,并可延缓精神分裂症的症状复发。帕利潘酮ER引起了各种不良反应,如静息症、头痛、血清催乳素水平升高和体重增加,但血脂、血糖和胰岛素水平未受影响。与其他非典型抗精神病药物相比,帕利哌酮ER增加了年稳定天数,更具成本效益。
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引用次数: 2
Prescription pattern study in type 2 diabetes mellitus in an Indian referral hospital 印度一家转诊医院治疗2型糖尿病的处方模式研究
Pub Date : 2008-12-31 DOI: 10.5580/1ffe
A. Hasamnis, S. Patil
Diabetes is a disease of the millions and it is projected that a quarter billion people across the globe would be suffering from diabetes mellitus by the year 2025.A major burden of this disease would be shared by developing countries like India and will be having approximately 57 million people suffering from the disease in the near future. Medications for diabetes mellitus need to be taken for the entire life and factors like efficacy, side effects, drug interactions and cost of therapy need to be taken into consideration [1].
糖尿病是一种数百万人的疾病,据预测,到2025年,全球将有2.5亿人患有糖尿病。这种疾病的主要负担将由印度等发展中国家分担,在不久的将来将有大约5700万人患有这种疾病。糖尿病药物治疗需要终生服用,需要综合考虑疗效、副作用、药物相互作用、治疗费用等因素[1]。
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引用次数: 15
Hepatoprotective Activity of Cassia fistula Linn. Bark Extracts against Carbon Tetra Chloride Induced Liver Toxicity in Rats 决明子瘘的保肝作用。树皮提取物对四氯化碳诱导大鼠肝毒性的影响
Pub Date : 2008-12-31 DOI: 10.5580/28f1
G. Parthasarathy, V. Prasanth
In the present study cassia fistula (Caesalpinaceae) bark was extracted with water. The extracts were vacuum dried to yield Aqueous Extract (AQET). The extracts were evaluated for hepatoprotective activity against Carbon tetrachloride (CCl4) induced liver damage at 250 mg/kg and 500 mg/kg dose level. The biochemical parameters observed in serum were total bilirubin, Alkaline phosphatase (ALP), Serum glutamate oxaloacetate transaminase (SGOT), Serum glutamate pyruvate transaminase (SGPT) levels and total protein. Aspartate transaminase (AST), Alanine Transaminase (ALT) and total protein levels in liver were also evaluated. Histopathological study on the liver tissue was also performed. The extracts exhibited dose dependant reduction in total bilirubin, ALP, SGOT, SGPT, AST, ALT and increase in total protein (serum and liver) levels. The extract treated groups shows mild hepatatocytic damage compared to the CCl4 treated group. CONCLUSION: Cassia fistulal attenuates the hepatotoxic effect of CCl4.
本研究采用水提法提取决明子(Caesalpinaceae)树皮。抽提液经真空干燥得到水提液(AQET)。在250 mg/kg和500 mg/kg剂量水平下,对四氯化碳(CCl4)诱导的肝损伤进行肝保护活性评价。血清生化指标为总胆红素、碱性磷酸酶(ALP)、谷草酰乙酸转氨酶(SGOT)、谷氨酸丙酮酸转氨酶(SGPT)水平和总蛋白。同时测定肝脏中谷草转氨酶(AST)、丙氨酸转氨酶(ALT)和总蛋白水平。同时对肝组织进行组织病理学检查。总胆红素、ALP、SGOT、SGPT、AST、ALT呈剂量依赖性降低,总蛋白(血清和肝脏)水平升高。与CCl4处理组相比,提取物处理组表现出轻微的肝细胞损伤。结论:决明子可减弱CCl4的肝毒性作用。
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引用次数: 14
Comparison of Antivenom potential of chicken Egg yolk Antibodies Generated against Bentonite and Adjuvant coated Echis carinatus venom 鸡卵黄抗膨润土和佐剂包被胭脂鱼毒抗体抗蛇毒潜能的比较
Pub Date : 2008-12-31 DOI: 10.5580/1244
S. Meenatchisundaram, R. Selvakumaran, G. Parameswari, A. Michael
The Chicken egg yolk antibodies generated against Bentonite and Adjuvant (FCA) coated Echis carinatus venom was evaluated for their anti-venom potential. Antibodies are extracted from immunized chicken egg yolk by the method described by Polson et al.(1980) and further purified by DEAE cellulose ion exchange column chromatography, which gave pure (180 - 200KDa) specific antibodies against venom. Inhibition of lethal, edema, procoagulant, and phospholipase A2 activities of Echis carinatus venom was determined. We found that 1.27mg of IgY (generated against FCA coated venom) and 1.33mg of IgY (generated against Bentonite coated venom) was able to completely neutralize the lethal activity (2LD 50) of Echis carinatus venom. Both chicken egg yolk antibodies effectively inhibited procoagulant activity and partially inhibited the Edema forming activity. IgY generated using Adjuvant (FCA) coated venoms showed very high anti-phospholipase A2 activity. In general, the results demonstrated the effectiveness of chicken egg yolk antibodies raised against adjuvant and bentonite coated venoms in neutralizing various pharamacological effects of Echis carinatusvenom.Keywords: Venoms, FCA, Bentonite, Chicken antibodies (IgY), PLA 2
研究了鸡卵黄抗体对膨润土和佐剂(FCA)包被胭脂鱼毒的抗毒能力。用Polson等人(1980)的方法从免疫后的蛋黄中提取抗体,再用DEAE纤维素离子交换柱层析纯化,得到纯的(180 - 200KDa)特异性抗蛇毒抗体。测定了鲫鱼毒液对致死性、水肿性、促凝性和磷脂酶A2活性的抑制作用。我们发现,1.27mg的IgY(对FCA包被毒液产生)和1.33mg的IgY(对膨润土包被毒液产生)能够完全中和Echis carinatus毒液的致死活性(2ld50)。两种鸡蛋黄抗体均能有效抑制促凝剂活性,部分抑制水肿形成活性。用佐剂(FCA)包被毒液生成的卵磷脂具有很高的抗磷脂酶A2活性。综上所述,针对佐剂和膨润土包被毒液制备的蛋黄抗体能有效中和蛇腹毒的多种药理作用。关键词:毒液,FCA,膨润土,鸡抗体,PLA 2
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引用次数: 2
Stimulation of Immune Function Activity of the Extract of Heliotropium Indicum Leaves 向日葵叶片提取物对免疫功能活性的刺激作用
Pub Date : 2008-12-31 DOI: 10.5580/3af
M. Shenoy, C. Shastry, K. Sridevi, P. Gopkumar
The objective of present study is to assess the immunostimulatory activity of H. indicum, using different in vitro and in vivo experimental models. The immunostimulatory potential of the test compound was investigated by in vitro phagocytic index and lymphocyte viability tests using interferon α-2b, a standard immunostimulant drug. Other tests such as carbon clearance, antibody titer and delayed type hypersensitivity were studied in mice using levimasole as the standard drug.The dried leaves extract (200mg/ml) significantly increased the in vitro phagocytic index and lymphocyte viability in all assays. They also showed a significant increase in antibody titer, carbon clearance and delayed type hypersensitivity in mice. To concludeH. indicum exhibited a dose-dependent immunostimulant effect, which could be attributed to the alkaloid content or due to the combination with other component(s).
本研究采用不同的体外和体内实验模型,对籼米的免疫刺激活性进行了评价。采用标准免疫刺激药物干扰素α-2b进行体外吞噬指数和淋巴细胞活力测定,考察化合物的免疫刺激潜能。其他测试,如碳清除率,抗体滴度和延迟型超敏反应研究小鼠使用左马索作为标准药物。干叶提取物(200mg/ml)显著提高了体外吞噬指数和淋巴细胞活力。他们还显示,小鼠的抗体滴度、碳清除率和延迟型超敏反应显著增加。concludeH。Indicum表现出剂量依赖性的免疫刺激作用,这可能归因于其生物碱含量或与其他成分的结合。
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引用次数: 11
Phosphodiesterase as a novel target in Cancer Chemotherapy 磷酸二酯酶作为肿瘤化疗的新靶点
Pub Date : 2008-12-31 DOI: 10.5580/2c8
G. Sandeep, S. Bhasker, Y. Ranganath
The Phosphodiesterase inhibitors have been used for the treatment of non-malignant conditions like asthma, pulmonary hypertension and erectile dysfunction etc, but the recent research suggests that they have great therapeutic value in the adjunctive therapy of Cancer. This article reviews the various substances elevating the intracellular cyclic AMP levels such as cAMP analogues and Phosphodiesterases inhibitors to induce apoptosis selectively in a variety of cancer cell lines with out affecting the normal cells. Their usefulness in the adjunctive therapy of cancer is explained.
磷酸二酯酶抑制剂已被用于治疗哮喘、肺动脉高压、勃起功能障碍等非恶性疾病,但近年来的研究表明,磷酸二酯酶抑制剂在癌症的辅助治疗中具有很大的治疗价值。本文综述了提高细胞内环AMP水平的各种物质,如cAMP类似物和磷酸二酯酶抑制剂,在不影响正常细胞的情况下选择性诱导多种癌细胞凋亡。说明了它们在癌症辅助治疗中的作用。
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引用次数: 3
期刊
The Internet Journal of Pharmacology
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