葛根素的药理研究

葛根素是葛根的主要有效成分,药理作用有抗心律失常、舒张血管、改善缺血心肌代谢、降血脂、抗凝血、改善肾功能、解酒、降血糖、抗氧化、增强耐缺氧能力、对抗结核药物性肝炎、抗肿瘤及对突发性耳聋的作用等。为利于临床进一步的开发使用,本文对其药理作用进行综述。     

复方葛参胶囊的安全毒理学评价

正葛根为豆科植物野葛或甘葛藤的干燥根,它既是我国传统中药材,也是食物,始载于《神农本草经》,具有解肌退热、生津止渴及生阳止泻的功效[1]。葛根含有多种有效成分,如黄酮、内酯、萜类、多糖和氨基酸等[2]。其主要活性成分是异黄酮类物质,如葛根素、大豆苷及其苷元等[3-4]。研究表明,葛根异黄酮类物质能扩张冠状动脉,抗心肌缺血,抗动脉粥样硬化,降血压、降血糖、降血脂,清除自由基、抗氧化、抗衰老作用[5-8]。人参是我国滋补类名贵中药材,已有数千     

葛根醋降糖软胶囊中总黄酮含量测定

<正>葛根醋软胶囊是由葛根、苦荞麦、山西老陈醋等为原料,采用现代提取分离技术研制成的一种软胶囊保健食品,具有辅助降血脂、降血压、降血糖等保健功效。据现代科学研究:葛根的有效成分为葛根素、异黄酮类化合物,具有抗心律失常、扩张冠状动脉、抗心肌缺血、抗血小板聚集、降血压、保护血管等作用[1]。苦荞又名黑苦荞、三角麦,其种植起源于中国,现主产于山西和四川凉山地区,研究表明:苦荞主要活性成分为黄酮类化合物,具有降脂     

葛根素的药理作用及临床应用新进展

目的对葛根素的药理作用．一临床应用、不良反应等研究进展进行综述。方法通过机检和手检,查阅文献,进行分析、归纳和总结。结果与结论葛根素对心血管、脑血管系统有明显的药理作用,且可改善外周循环,具β-受体阻断作用．抑制血小板聚集,降血脂,降血糖作用。临床应用广泛,毒性低,安全范围广。     

葛根素的临床应用进展

葛根是常见的中药材之一,中医认为葛根素具有胃经、活血、归脾、通络、升阳的作用。葛根素具有很高的药学价值,被广泛的应用于临床治疗。现代医学证明,豆科植物野葛中提取物葛根素。葛根素有降血糖、血脂、抗氧化、改善血液流变学特性、扩张冠状动脉和脑血管等作用,而广泛用于临床高血压、冠心病、急性脑梗死、糖尿病等病症的治疗具有显著的疗效。     

葛根总黄酮及葛根素对神经系统保护作用的研究进展

葛根的主要活性成分为异黄酮类化合物,包括葛根素、大豆素、大豆苷等。研究发现葛根总黄酮及葛根素具有抗氧化、抑制动脉硬化斑块进展、抑制血管平滑肌凋亡、预防脑缺血及再灌注损伤、保护继发性脊髓损伤等作用,因此被广泛用于缺血性脑血管病、痴呆、胶质瘤等神经系统疾病的临床辅助治疗中,本文对葛根总黄酮及葛根素对神经系统的保护作用的研究进展和可能机制做一概述,为临床应用该药提供参考。     

复方葛根胶囊对实验性糖尿病、高脂血症模型血糖和血脂作用的实验研究

目的：研究由中药葛根提取物葛根素和酵母生物提取物葡萄糖耐量因子组成的复方葛根胶囊对实验性糖尿病小鼠和高脂血症大鼠的降糖、降脂作用。方法：采用四氧嘧啶复制糖尿病小鼠模型和高脂饲料复制高血脂大鼠模型，分别观察复方葛根胶囊对其空腹血糖、糖耐量和高脂血症大鼠血脂水平的影响。结果：复方葛根胶囊能显著降低四氧嘧啶所致的小鼠高血糖水平和改善四氧嘧啶性糖尿病小鼠的糖耐量，同时该药有显著降低TG、TC，提高HDL-C、HDL／TC的作用。结论：复方葛根胶囊有明显的降糖和降脂作用，可为临床应用和开发研究提供药理学依据。     

葛根素药理研究进展

葛根用作解表药已有悠久的历史 ,现代药理研究表明葛根具有改善脑循环及外周循环的作用。我国和日本等国学者相继从葛根中分离出 2 0多种成分 ,葛根素是其中的主要有效成分之一 ,其化学名 :4 ,7-二羟基 - 8- β -Ｄ -葡萄糖基异黄酮。近年来对葛根素的研究取得了许多进展 ,现综述如下 :一、主要药效学研究1 β -肾上腺素能受体拮抗作用 :放射性配体结合分析表明 ,葛根素明显降低大鼠心肌膜制备中 β受体的最大结合容量。结合竞争试验显示葛根素能与标记配体竞争与受体的结合 ,并且可完全抑制肾上腺素对腺苷酸环化酶的激活作用 ,表明葛根素为…     

薄层扫描法测定复方伤风胶囊中葛根素的含量

薄层扫描法测定复方伤风胶囊中葛根素的含量深圳市药检所５１８０２６傅先珏，熊英，邬晓鸥复方伤风胶囊由葛根、菊花、黄芩、柴胡等药物经提取，喷雾干燥制成。具有解表清热的功效。葛根为其主药，葛根素是葛根中的有效成分之一。测定单味葛根制剂中葛根素含量的方法已有...     

中药葛根改善胰岛素抵抗作用的实验研究

葛根是中医临床常用药物,其单味药及复方在消渴病的治疗中应用广泛.现代研究表明:葛根煎剂及葛根素具有降低血糖的作用,但关于葛根治疗糖尿病的机制研究甚少.     

黄连总生物碱对糖尿病大鼠降血糖作用研究

目的：探讨黄连总生物碱对糖尿病大鼠的降血糖作用。方法：采用链脲佐菌素50 mg/kg诱导SD大鼠形成糖尿病模型,筛选糖尿病大鼠空腹血糖的禁食时间,考察黄连总生物碱给药68d对糖尿病大鼠血糖、糖化血清蛋白、肌酐、尿素氮的影响,并测定其肝、胃、肾脏器指数,评价黄连总生物碱对糖尿病大鼠的降血糖作用。结果：（1）选择白天禁食6 h为糖尿病大鼠的禁食时间。（2）与模型组比较,黄连总生物碱高剂量组（含黄连总生物碱578.7 mg/kg）可明显降低糖尿病大鼠空腹6 h血糖及糖化血清蛋白（P〈0.05）;黄连总生物碱低剂量组（含黄连总生物碱192.9 mg/kg）可显著降低谷胱甘肽-过氧化物酶（P〈0.01）。黄连总生物碱对糖尿病大鼠肌酐、超氧化物歧化酶、总胆固醇、甘油三酯及脏器指数总体上影响不明显（P〉0.05）。结论：黄连总生物碱对糖尿病大鼠有降血糖的作用。     

葛根素对小鼠实验性微循环障碍的改善作用

本文报告了葛根素对肾上腺素(Adr)引起的小鼠肠系膜微循环障碍的影响,并与罂粟碱作比较。结果表明,预先局部滴注0.5%葛根素能够拮抗Adr所致微动脉收缩、流速减慢和流量减少;而局部先滴注Adr造成微循环障碍后,再局部滴注1%葛根素,获得与上类似结果。给小鼠ⅳ葛根素(52 mg/kg)后再局部滴注Adr,可减轻Adr引起的微动脉收缩、流速减慢和流量减少,其作用优于罂粟碱。因此葛根素可改善实验性微循环障碍。     

Puerarin Attenuates Carbon Tetrachloride‐Induced Liver Oxidative Stress and Hyperlipidaemia in Mouse by JNK/c‐Jun/CYP7A1 Pathway

Puerarin (PU), a natural flavonoid, has been reported to have many benefits and medicinal properties. The aim of this study was to investigate the effects of puerarin on hepatic oxidative stress and hyperlipidaemia in mice exposed to carbon tetrachloride (CCl₄). Male ICR mice were injected with CCl₄ with or without puerarin co‐administration (200 and 400 mg/kg intragastrically once‐daily) for 8 weeks. Our data showed that puerarin significantly prevented CCl₄‐induced hepatotoxicity, indicated by both diagnostic indicators of the liver damage (serum aminotransferase levels) and histopathological analysis. Puerarin decreased the thiobarbituric acid reactive substances (TBARS) and the protein carbonyl content (PCO) in the liver of CCl₄‐treated mice. Puerarin also restored the levels of reduced glutathione (GSH) and total antioxidant capacity (TAC) in the liver. Furthermore, the increase in serum cholesterol, triglycerides and low‐density lipoproteins (LDL) induced by CCl₄ was effectively suppressed by puerarin. The high‐density lipoprotein (HDL) level in the CCl₄ treatment mice was also increased by puerarin. Western blot analysis showed that puerarin remarkably inhibited hyperlipidaemia by regulating the expression of phosphorylated Jun N‐terminal kinases (JNK), phosphorylated c‐Jun protein and cholesterol 7a‐hydroxylase (CYP7A1) in the liver of CCl₄‐treated mice. Altogether, these results suggest that puerarin could protect the CCl₄‐induced liver injury and hyperlipidaemia by reducing reactive oxygen species S production, renewing the total antioxidant capacity and influencing expression of hepatic lipid biosynthesis and metabolism genes.     

Biochemical studies on some hypoglycemic agents (II) effect ofCalligonum comosum extract

People in some tropical countries used to use some plant extracts in folklore medicine as treatment of diabetes mellitus. Of these plants isCalligonum comsum (“orta”). The present work deals with the biochemical effects of the whole plant water extract given orally to the albino rats, normals and alloxan diabetics, as to fulfil its hypoglycemic effects on rats. The results showed that “orta” extract produced a hypoglycemic effect indicated by the decrease in blood sugar level. It was observed that the diabetic state in rats treated with 300 mg/kg body weight of “orta” extract, was alleviated, showing normal levels of blood glucose, liver fat and cholesterol contents. Liver proteins were still below the normal level in the rats. Gibenclamide, a hypoglycemic drug, was used for comparison with “orta” extract. Although it did alleviate the diabetic state, yet the liver fat and cholesterol contents were still higher than those of normal. Also the liver proteins were lower than the control levels.     

实验性肥胖及糖尿病大鼠模型

本文报告用小剂量链脲霉素(25 mg/kg)给雌性大鼠静脉注射,使大鼠糖耐量异常,然后加喂高热量食物,引起动物肥胖,饲养8或18周,可形成类似Ⅱ型糖尿病的肥胖大鼠模型。     

葛根素抑制钠-葡萄糖协同转运蛋白2活性发挥促尿糖作用研究

目的 研究葛根素通过抑制钠-葡萄糖协同转运蛋白2（SGLT2）发挥促尿糖、降血糖作用。方法 同源模建获得SGLT2蛋白虚拟结构,以达格列净为阳性药,与葛根素进行分子对接,考察其分子结合强弱;采用能稳定表达人SGLT2（hSGLT2）蛋白的中国仓鼠卵巢（CHO）细胞、以^14C-甲基葡萄糖苷（[^14C]-AMG）为底物,评价葛根素体外抑制SGLT2的活性;以达格列净为阳性药,采用大鼠体内口服糖耐量试验（OGTT）和尿排泄糖试验（UGE）观察葛根素直接降血糖和促尿糖活性。结果 分子对接得分显示,葛根素是SGLT2的底物,总体作用强度不及达格列净;体外实验显示,葛根素可较强抑制hSGLT2,最大效应为84%左右,半数抑制浓度（IC₅₀）为0.40 μmol/L;OGTT结果显示,葛根素10、30、60和120 mg/kg剂量的抑糖率分别为5.1%、6.5%、16%和22%,呈剂量相关性;在UGE实验中,随着葛根素剂量的增大,尿糖量增加,与模型组比较,30、60和120 mg/kg剂量组差异显著（P<0.05、0.01）。结论 葛根素具有抑制hSGLT2、促尿糖降低血糖的药理活性,有可能作为一类新型结构的SGLT2抑制剂的先导化合物。     

Hypoglycemic effect of Hypoxis hemerocallidea corm (African potato) aqueous extract in rats

Diabetes mellitus has been recognized as a clinical syndrome since ancient times, and remains a crippling global health problem today. It is a group of heterogeneous, autoimmune, hormonal and metabolic disorders, often accompanied by hypertension, hyperlipidemia and obesity. Current estimates suggest that approximately 150 million people worldwide suffer from diabetes mellitus. The present study was undertaken to examine the hypoglycemic effect of aqueous extract of Hypoxis hemerocallidea (family: Hypoxidaceae) corm (locally known as "African Potato") in normal (normoglycemic) and in streptozotocin (STZ)-treated, diabetic rats. Young adult, male Wistar rats weighing 250-300 g were used. Diabetes mellitus was induced in the group of diabetic test rats by intraperitoneal injections of STZ (90 mg/kg). In one set of experiments, graded doses of the aqueous extract of African Potato (100-800 mg/kg p.o.) were administered to 12-h fasted normal and diabetic rats. In another set of experiments, 800 mg/kg of African potato extract, a dose of the plant extract that produced maximal hypoglycemic effects in fasted normal and diabetic rats in our pilot experiments, was used. The hypoglycemic effect of this single dose was compared with those of insulin (5 micro U/kg s.c.) and glibenclamide (5 mg/kg p.o.) in 12-h fasted normal and diabetic rats. Following acute treatment, relatively moderate to high doses of African potato extract (100-800 mg/kg p.o.) produced dose-dependent, significant reductions (p < 0.05-0.001) in the blood glucose concentrations of fasted normal and diabetic rats. Similarly, insulin (5 micro U/kg s. c.) and glibenclamide (5 mg/kg p.o.) produced significant reductions (p < 0.01-0.001) in the blood glucose concentrations of the fasted normal and diabetic rats. At a dose of 800 mg/kg, the plant extract caused 30.20% and 48.54% reductions in the blood glucose concentrations of fasted normal and STZ-treated diabetic rats, respectively. While it is likely that the hypoglycemic effect of the plant extract is largely due to its phytosterols and/or sterolin content, the exact mechanism of its hypoglycemic action is still obscure and will have to await further studies. However, the results of this experimental animal study indicate that African potato possesses hypoglycemic activity; and thus lends credence to the suggested folkloric use of the herb in the control and/or management of adult-onset, type 2 diabetes mellitus in some communities of South Africa.     

Hypoglycemic effects and mechanisms of action of Cortex Lycii Radicis on alloxan-induced diabetic mice

Cortex Lycii Radicis (CLR) has been used as a traditional Oriental medicine as an antipyretic and to treat pneumonia, night-sweats, cough, hematemesis, inflammation, and diabetes mellitus for centuries. This study aimed to determine the effects of CLR on alloxan-induced diabetic mice and its mechanisms. Based on thin-layer chromatography (TLC) assay, the main compounds of CLR include an organic acid, flavone, alkaloid, polysaccharide, anthraquinone, and saponin. The mice were divided into four groups: normal control (NC), diabetes control (DC), diabetes+high-dose CLR (200 mg kg(-1)), and diabetes+low-dose CLR (100 mg kg(-1)). The diabetic mice were administered CLR daily for 28 days. The CLR treatment resulted in significant decreases in fasting blood glucose, total cholesterol, and triglycerides. CLR also showed a tendency to improve body weight gain in diabetic mice. Furthermore, the serum insulin level of each group was assayed, and the DC group had a lower serum insulin level than the NC group. Insulin levels were dose dependently raised in the CLR-treated groups compared with the DC group. According to single-cell gel electrophoresis and LD(50) analysis, CLR was nontoxic to the animals. The results indicate that CLR alleviates the blood glucose and lipid increases associated with diabetes and improves the abnormal glucose metabolism and increases insulin secretion by restoring impaired pancrease beta-cells in alloxan-induced diabetic mice. The results suggest that CLR has hypoglycemic potential and could be useful in diabetes therapy.     

本草消渴丹对2型糖尿病大鼠血糖和血清胰岛素含量的影响

目的:研究本草消渴丹对2型糖尿病大鼠血糖和血清胰岛素含量的影响。方法:选择高脂、高糖饲料加小剂量链脲佐素(STZ,25mg·kg-1腹腔注射)复制大鼠2型糖尿病模型,分别以本草消渴丹和二甲双胍进行干预,检测空腹血糖。治疗4周后测大鼠空腹血糖、血清胰岛素含量以及大鼠体质量变化。结果:本草消渴丹能显著降低2型糖尿病大鼠血糖含量和胰岛素含量且具有显著缓解体质量增长缓慢的作用。结论:本草消渴丹治疗糖尿病的机制之一是缓解血清胰岛素抵抗。     

Pharmacologic profile and insulin secretagogue effect of linogliride (McN-3935), a new,orally effective hypoglycemic agent

Linogliride (McN-3935) [N-(1-methyl-2-pyrrolidinylidene)-N'-phenyl-4-morpholinecarboximidamide] was selected for clinical evaluation as a potential orally effective hypoglycemic agent for treatment of noninsulin-dependent diabetes mellitus. Linogliride is structurally unrelated to sulfonylureas and biguanides. It produced a dose-dependent hypoglycemic effect in nondiabetic rats, mice, and dogs. The minimum effective oral doses that lowered fasting blood glucose levels and improved glucose tolerance were 1–5 mg/kg. Comparison of the dose-response curves from fasting rat studies showed linogliride to be approximately two times more potent than the related compound pirogliride and approximately eight times more potent than tolbutamide. Tolerance to its hypoglycemic effect did not develop in rat and dog 3-day repeat dose studies. Linogliride did not alter plasma lactic acid levels in normal and streptozotocin-induced diabetic rats, and it improved glucose tolerance whether the glucose was administered orally or parenterally. In nondiabetic rats and dogs, decreases in fasting blood glucose levels following linogliride administration were associated with elevated (two- to fourfold) plasma insulin concentrations. Linogliride was inactive in depancreatized diabetic dogs. In genetically diabetic (db/db) mice and streptozotocin-induced diabetic rats, linogliride (25–100 mg/kg p.o.) produced variable, nondose-dependent reductions of blood glucose levels, unlike the sulfonylureas, which were consistently ineffective in these diabetic rodent models. In conclusion, although the observed activity in diabetic rodent models is suggestive of a potential nonpancreatic mechanism, the experimental evidence to date indicates that the acute effectiveness of linogliride as a hypoglycemic agent is due primarily to stimulation of insulin release.