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1.
小檗碱的药理研究及临床应用   总被引:6,自引:0,他引:6  
小檗碱通过竞争性阻断α-肾上腺能受体增强心房收缩力,起到抗心律失常和降血压的作用;通过促进胰岛β细胞修复和增生,使胰岛素释放增加,同时抑制糖元异生,和(或)促进糖酵解,产生降血糖的作用,通过抗胃肠道粘膜细菌感染治疗溃疡性胃肠道炎。因此,小檗碱临床应用前景广泛。  相似文献   

2.
二甲双胍(Metformin)是一种双胍类口服降血糖药。为胰岛素增敏剂,可以降低II型糖尿病患者空腹及餐后血糖。具有多种作用机制,包括延缓葡萄糖由胃肠道的摄取,通过提高胰岛素的敏感性而增加外周葡萄糖的利用,以及抑制肝、肾过度的糖原异生,不降低非糖尿病患者的血糖水平。二甲双胍可单独用药,也可与磺脲类,胰岛素或其它抗糖尿  相似文献   

3.
黄连素的降血糖药效学试验与临床观察   总被引:11,自引:0,他引:11  
目的探讨中药小檗碱(黄连素)的降血糖作用。方法用四氧嘧啶建立糖尿病小鼠模型,以小檗碱不同剂量和西药降糖灵对照治疗观察糖尿病小鼠,采用葡萄糖氧化酶法测定血糖和糖耐量,用放射免疫法测定血清胰岛素;并采用黄连素与对照组达美康随机分配73例糖尿病患者进行临床对比观察。结果小檗碱对糖尿病小鼠有降血糖作用,有提高其糖耐量和提高血清胰岛素作用,且有量效关系。黄连素治疗糖尿病43例,临床有效率为81.39%,对照组达美康治疗同症30例,临床有效率为80.00%,两组疗效明显,但无明显差异(P<0.05)。结论小檗碱对糖尿病小鼠和糖尿病患者有降血糖作用。  相似文献   

4.
小檗碱是黄连的主要成分,属于异喹啉类生物碱,具有调血脂、抗血栓形成、降血糖、抗氧化、抗炎、抑制血管平滑肌细胞增殖、保护血管内皮细胞和促血管内皮舒张因子释放等多种作用,且能从多个环节抑制动脉粥样硬化的形成与发展。综述研究近年来有关小檗碱对动脉粥样硬化作用机制的相关文献,发现其作用机制主要包括调控炎症因子相关基因的表达、抗氧化应激、减少脂质合成、改善血管内膜细胞等几方面,从而为小檗碱临床应用及研发新的天然药物提供理论基础。  相似文献   

5.
周迎生 《药品评价》2012,9(10):12-15
二甲双胍为双胍类口服降糖药,具有多种作用机制。其降糖机制与磺脲类药物不同,它不刺激胰岛素分泌,主要是增加周围组织糖无氧酵解,促进周围组织细胞(如肌肉等)利用葡萄糖;抑制肝糖原异生,从而降低肝糖输出;增加周围组织对胰岛素的敏感性,通过增加胰岛素与胰岛素受体的结合,增加胰岛素介导的葡萄糖利用,动物实  相似文献   

6.
小檗碱又名黄连素.是从黄连等植物中提取的异喹啉类生物碱,具有广泛的药理作用。近年来,随着对小檗碱及其衍生物的深入研究发现。小檗碱具有改善胰岛素抵抗作用。现综合国内外对小檗碱的研究,对小檗碱改善胰岛素抵抗及作用机制进行综述。  相似文献   

7.
CS-045系日本三共公司开发的降血糖药,与磺酸豚类药物不同,不是通过胰脏分泌胰岛素,而是通过增强胰岛素在外周的作用、抑制肝脏过度的糖原异生未达到降血糖作用。动物实验表明,它还具有降低血中甘油三酯的作用。非胰岛素依赖性糖尿病患者口服本品,每日200~800mg,连续给药52周,57例单用本品者给药开始时空腹血糖值为184mg/di,第乃周为141mg/di,以后至52周血糖值在137一15Omg/dl范围内变化。HbA1c给药开始时为8.7%,第16周为7.9%,以后至立2周在7.0~7.3%范围内变动。主治医师对血糖控制的综合评定,在“良”以上的有71…  相似文献   

8.
小檗碱抗肿瘤作用与Wnt/-βcaten in信号转导关系   总被引:1,自引:2,他引:1  
目的证明小檗碱抗肿瘤作用机制可能与信号转导过程的调控有关。方法采用细胞增殖抑制和Hoechst 33258染色凋亡实验比较小檗碱和黄连总碱对人结肠癌HCT116和SW 480细胞的作用。利用Tcf-4报告基因研究小檗碱对肿瘤细胞的信号转导影响。结果小檗碱在5~40 mg.L-1浓度范围内呈浓度依赖性和时间依赖性抑制人结肠癌HCT116和SW 480细胞的增殖;小檗碱(20 mg.L-1)处理72 h后的HCT116和SW 480细胞出现明显凋亡;相当于小檗碱浓度的黄连总碱有类似于小檗碱的作用。20~40 mg.L-1小檗碱和黄连总碱均能明显抑制-βcaten in/Tcf介导的转录活性。结论黄连总碱的抗肿瘤作用可能与其主要成分小檗碱有关;其抗肿瘤作用机制至少与抑制W nt/-βcaten in信号通路有关。  相似文献   

9.
小檗碱降血糖作用的药效学试验与临床疗效观察   总被引:1,自引:0,他引:1  
郭彬  赵恒侠 《中国药业》2006,15(21):30-31
目的研究小檗碱(黄连素)的降血糖作用及临床疗效。方法用四氧嘧啶建立糖尿病小鼠模型,进行药效学试验,并以格列齐特为对照进行临床疗效观察。结果小檗碱对糖尿病小鼠有降血糖作用且有量效关系,可提高其糖耐量和血清胰岛素水平;临床有效率治疗组为80.00%,对照组为76.67%,两组疗效明显但无显著性差异(P〉0.05)。结论小檗碱对糖尿病小鼠和2型糖尿病患者均有降血糖作用。  相似文献   

10.
糖尿病是一种代谢紊乱型疾病,恢复胰岛素敏感性和改善代谢稳态对治疗糖尿病及其并发症至关重要。小檗碱可缓解胰岛素抵抗,降低血糖。总结了小檗碱通过依赖性蛋白激酶(MAPK)信号通路、胰岛素信号通路、核因子-κB(NF-κB)信号通路以及其他信号通路改善胰岛素抵抗来说明小檗碱降血糖的作用机制。  相似文献   

11.
Our preliminary study demonstrated that 70% ethanol Cortidis Rhizoma extracts (CR) had a hypoglycemic action in diabetic animal models. We determined whether CR fractions acted as anti-diabetic agent, and a subsequent investigation of the action mechanism of the major compound, berberine ([C(20)H(18)NO(4)](+)), was carried out in vitro. The 20, 40 and 60% methanol fractions from the XAD-4 column contained the most insulin sensitizing activities in 3T3-L1 adipocytes. The common major peak in these fractions was berberine. Treatment with 50 microM berberine plus differentiation inducers significantly reduced triglyceride accumulation by decreased differentiation of 3T3-L1 fibroblasts to adipocytes and triglyceride synthesis. Significant insulin sensitizing activity was observed in 3T3-L1 adipocytes which were given 50 microM berberine plus 0.2 nM insulin to reach a glucose uptake level increased by 10 nM of insulin alone. This was associated with increased glucose transporter-4 translocation into the plasma membrane via enhancing insulin signaling pathways and the insulin receptor substrate-1-phosphoinositide 3 Kinase-Akt. Berberine also increased glucose-stimulated insulin secretion and proliferation in Min6 cells via an enhanced insulin/insulin-like growth factor-1 signaling cascade. Data suggested that berberine can act as an effective insulin sensitizing and insulinotropic agent. Therefore, berberine can be used as anti-diabetic agent for obese diabetic patients.  相似文献   

12.
知母聚糖降糖作用及其机理研究   总被引:6,自引:1,他引:6  
目的研究知母聚糖的降血糖作用和作用机理。方法利用葡萄糖氧化酶法测血糖 ,用蒽酮法测定肝糖原含量 ,用放射免疫法测定血浆胰岛素水平和骨骼肌对3H 2 脱氧葡萄糖摄取能力 ,并在光镜下做胰岛组织的形态学观察。结果知母聚糖能降低正常小鼠和对四氧嘧啶诱发的高血糖大鼠的血糖、增高肝糖原含量、增加骨骼肌对3H 2 脱氧葡萄糖摄取能力。结论知母聚糖具有降血糖作用 ,其降血糖作用与其增加肝糖原合成、减少肝糖原分解 ,增加骨骼肌对葡萄糖摄取等因素有关  相似文献   

13.
乌拉坦诱导的高血糖反应(英文)   总被引:4,自引:0,他引:4  
目的:观察麻醉剂量的乌拉坦对空腹大鼠、葡萄糖负荷大鼠,肾上腺素或四氧嘧啶诱发高血糖大鼠血糖水平的影响,并探讨其对外源性胰岛素降血糖作用的影响。方法:葡萄糖氧化酶法测定血糖含量。结果:麻醉剂量1.5g·kg~(-1)乌拉坦(sc,ip各半)显著升高空腹大鼠和葡萄糖负荷大鼠的血糖水平,但对肾上腺素(胰岛功能正常)或四氧嘧啶(胰岛功能受损)诱发的高血糖大鼠的血糖水平无明显影响。在四氧嘧啶诱发的高血糖大鼠,乌拉坦显著对抗外源性胰岛素的降血糖作用。结论:乌拉坦升高血糖的作用除与已知的释放肾上腺素有关外,抑制胰岛素的降血糖作用也是其升高血糖的机制之一。  相似文献   

14.
The antidiabetic effects of 2-piperazinyl-4-methylamino-5-methylthieno [2,3-d]pyrimidine dihydrochloride hydrate (Compound-(I] were investigated in various animals and in various conditions. Compound-(I) is a new hypoglycemic agent structurally unrelated to sulfonylurea and biguanide. It produced dose dependent hypoglycemic effects (10-100 mg/kg) in rats and mice under fed, fasted and glucose tolerated states. However, it was ineffective in fasted guinea pigs even when given at 100 mg/kg. In normal fed rats and mice, hypoglycemic effects of Compound-(I) were estimated to be 3-19 times and 12-70 times more potent than tolbutamide and phenformin, respectively. Compound-(I) also produced hypoglycemic action in streptozocin diabetic rats and genetically diabetic KK mice. Especially, its hypoglycemic effect was observed at the dose as low as 3 mg/kg p.o. in KK mice. However, elevation of blood lactate was accompanied by lowering of blood glucose after oral administration of Compound-(I) in normal rats and mice and in streptozocin diabetic rats, while these effects were not observed in guinea pigs. In addition, plasma insulin significantly increased after administration of Compound-(I) in both normal and KK mice, while this increase in plasma insulin was not so prominent in fed rats. This elevation in plasma insulin might be produced by alpha 2-adrenergic antagonism at pancreatic B cell as Compound-(I) suppressed epinephrine induced hyperglycemia by elevating plasma insulin. In conclusion, Compound-(I) seems mainly to produce hypoglycemic action through extrapancreatic mechanism which increases blood lactate associated with anaerobic glycolysis or inhibition of gluconeogenesis. In addition, elevation of plasma insulin also might be responsible for hypoglycemic effects.  相似文献   

15.
Hypoglycemic action of brazilin was found to be based on the improvement of peripheral glucose utility, and this action might be correlated with the insulin action pathway. In the present study we investigated the effect of brazilin on the insulin receptor autophosphorylation, protein kinase C (PKC), protein phosphatase and insulin receptor serine kinase in order to confirm whether the hypoglycemic mechanism is concerned with insulin action pathway. Brazilin was found to inhibit PKC and insulin receptor serine kinase, which are involved in the regulation of insulin signal pathway. But any significant effect was not shown on insulin receptor tyrosine kinase activity, autophosphorylation and phosphatase activity. These findings suggest that brazilin might enhance insulin receptor function by decreasing serine phosphorylation, which might mediate hypoglycemic effect of brazilin  相似文献   

16.
二精丸多糖对糖尿病大鼠降血糖作用的研究   总被引:1,自引:0,他引:1  
目的研究二精丸多糖对糖尿病大鼠的降血糖作用,并初步探讨其作用机制。方法采用高脂高糖饲料结合小剂量链脲佐菌素(STZ)建立2型糖尿病大鼠模型,并分为模型对照组,二精丸多糖低、中、高剂量组,同时设立正常对照及吡咯列酮组。研究二精丸多糖对糖尿病大鼠的空腹血糖(FBG)、糖化血红蛋白(HbA1c)、血清胰岛素(Ins)、总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白(HDL)、低密度脂蛋白(LDL)等指标的影响。结果二精丸多糖3个剂量组糖尿病大鼠FBG、HbAlc、TC、TG、LDL降低,Ins、HDL升高,与模型组相比有统计学意义(P〈0.05)。结论 二精丸多糖对糖尿病大鼠有降血糖作用,其作用可能与增加Ins水平有关。  相似文献   

17.
Berberine from Rhizoma Coptidis is an oral hypoglycemic agent with anti-dyslipidemia and anti-obesity activities. Its metabolic activity of regulating blood glucose and lipids has been widely studied and evidenced in patients and various animal models. Berberine is known as an AMP-activated protein kinase (AMPK) activator. Its insulin-independent hypoglycemic effect is related to inhibition of mitochondrial function, stimulation of glycolysis and activation of AMPK pathway. Additionally, berberine may also act as an α-glucosidase inhibitor. In the newly-diagnosed type 2 diabetic patients, berberine is able to lower blood insulin level via enhancing insulin sensitivity. However, in patients with poor β-cell function, berberine may improve insulin secretion via resuscitating exhausted islets. Furthermore, berberine may have extra beneficial effects on diabetic cardiovascular complications due to its cholesterol-lowering, anti-arrhythmias and nitric oxide (NO) inducing properties. The antioxidant and aldose reductase inhibitory activities of berberine may be useful in alleviating diabetic nephropathy. Although evidence from animal and human studies consistently supports the therapeutic activities of berberine, large-scale multicenter trials are still necessary to evaluate the efficacy of berberine on diabetes and its related complications.  相似文献   

18.
小檗碱对NIT-1细胞胰岛素分泌和葡萄糖激酶活性的影响   总被引:4,自引:0,他引:4  
王增四  陆付耳  陈广  徐丽君  王开富  邹欣 《药学学报》2007,42(10):1045-1049
本文探讨小檗碱对NIT-1细胞胰岛素分泌的影响及其分子机制。采用不同浓度小檗碱干预NIT-1细胞后,以放射免疫法、液体闪烁计数法、酶法分析及Western blotting分别检测其胰岛素水平、葡萄糖利用、葡萄糖激酶(GK)活性、GK和葡萄糖激酶调节蛋白(GKRP)的表达。结果表明,在高浓度葡萄糖刺激下,与空白对照组相比,小檗碱组的NIT-1细胞胰岛素分泌增加、葡萄糖利用活跃,且GK酶活性增强、GK表达增加,而GKRP表达降低(P<0.05)。结果表明,小檗碱促进NIT-1细胞高浓度葡萄糖诱导的胰岛素分泌,可能与其作为GK激活剂,使NIT-1细胞葡萄糖利用增加、GK酶活性及表达增强有关。  相似文献   

19.
The administration of L-isoleucine (isoleucine) has been shown to induce hypoglycemia in normal rats. However, it remains to be elucidated whether isoleucine can improve the blood glucose level in glucose-intolerant or diabetic animals. In the present study, oral isoleucine significantly reduced the blood glucose level after an oral glucose challenge in normal mice, as well as in glucose-intolerant mice fed a high-fat diet (HFD) and db/db mice, a model of severe type 2 diabetes. Isoleucine treatment significantly augmented the blood insulin level after an oral glucose load in HFD mice, but not in normal or db/db mice, suggesting that its hypoglycemic activity was attributable to both insulinotropic and non-insulinotropic mechanisms. Chronic supplementation of isoleucine in mice on a high-fat/high-sucrose diet significantly reduced insulin release after an oral glucose challenge without any change in glucose tolerance curve, suggesting that isoleucine might have an insulin-sensitizing effect along with its acute hypoglycemic effect. These results indicate that both acute and chronic treatment with isoleucine is beneficial for glucose metabolism in glucose-intolerant and diabetic animals.  相似文献   

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