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。     

葛根化学成分研究

摘要：目的:研究葛根化学成分。方法:通过大孔树脂、MCI柱以及制备型HPLC进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果:分离纯化得到23个化合物,分别为美佛辛-4’-O-葡萄糖苷(1)、3’-羟基葛根素芹菜糖苷(2)、大豆苷元-4’-葡萄糖苷(3)、葛根素芹菜糖苷(4)、大豆苷元-4’,7-二葡萄糖苷(5)、葛根素-6’’-O-木糖苷(6)、3’-羟基葛根素(7)、3’-甲氧基葛根素(8)、tuberosin(9)、毛蕊异黄酮苷(10)、葛根苷B(11)、葛根苷A(12)、3’-甲氧基大豆苷(13)、染料木素-7-O-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷(14)、染料木苷(15)、刺芒柄花素(16)、formononetin-8-C-β-D-apiofuranosyl-(1→6)-O-β-Dglucopyranoside(17)、(+)-puerol B-2"-O-glucoside (18)、印度黄檀苷(19)、3’-甲氧基大豆苷元(20)、puerol B(21)、染料木素(22)、hydroxytuberosone(23)。结论:其中化合物10为首次从葛根中分离得到,研究结果丰富了葛根的化学成分。     

共晶分离技术在染料木素-葛根素-大豆苷元三元体系分离纯化中的应用

共晶分离技术是一种利用配体选择性与目标化合物形成共晶后从混合体系中分离的技术。葛根素、染料木素及大豆苷元是葛根中的主要成分,这3种结构相似的成分的分离精制多采用常规柱色谱、重结晶等技术,具有分离周期长、溶剂消耗量大、制备效率低等问题。本团队利用前期新发现的共晶分离现象设计并实现了染料木素-葛根素-大豆苷元三元混合物的分步提取分离实验,在混合体系中依次加入咖啡因和脯氨酸作为共晶配体,通过混悬液法形成了染料木素-咖啡因共晶和葛根素-脯氨酸共晶,并从溶液中分别分离析出,最终得到染料木素纯度为93%的染料木素-咖啡因共晶和葛根素纯度为99%的葛根素-脯氨酸共晶,且大豆苷元的纯度也提高了6.76倍。本研究提出了一种不同于传统分离方法、操作简单、成本低、适用范围广的分离方法,实现了中药中结构相近化学组分的分离,为共晶技术应用于中药的分离与精制奠定基础。     

粉葛资源产业化过程废弃物中的黄酮类化学成分分析

目的:研究粉葛采收及加工过程废弃物中黄酮类化学成分的组成和含量,为该品种资源的综合开发与合理利用提供依据。方法:以江西产粉葛品种"赣葛2号"为对象,采用超高效液相色谱-四极杆-飞行时间质谱和高效液相色谱技术分别检测葛根(带皮或去皮)、葛根皮、葛花、葛须根、葛茎、葛根头、葛根渣(带皮或去皮)以及沉淀葛粉后的工业废水(带皮或去皮)干物质中的黄酮类化学成分组成和含量。结果:所建立的7种黄酮类成分(葛根素、大豆苷、鸢尾黄素-7-O-木糖葡萄糖苷、染料木苷、鸢尾苷、大豆苷元、葛花苷)的含量测定方法的线性、精密度、重复性、稳定性、加样回收率均符合要求。共鉴定出12个黄酮类化学成分,其中葛根、葛根皮、葛茎、葛须根、葛根头、葛根渣和工业废水干物质中的黄酮类成分种类基本一致,主要为葛根素、大豆苷、染料木苷、大豆苷元、丙二酰基黄豆苷元;葛花中主要含有鸢尾黄素-7-O-木糖葡萄糖苷、染料木苷、鸢尾苷、葛花苷、6″-O-木糖基黄豆黄苷,但未检出葛根素、大豆苷及苷元等成分。葛根素含量以葛根头中最高,达5.765%;葛根、葛根渣及废水干物质各带皮样品中葛根素含量均较相应的去皮样品更高。结论:粉葛资源产业化过程的废...     

葛根异黄酮类化合物抗动脉粥样硬化药理研究进展

动脉粥样硬化(Atherosclerosis,AS)是当今导致心脑血管疾病高发的主要因素,越来越多的报道说明中药葛根具有抗动脉粥样硬化的药理作用,其主要有效成分为异黄酮类化合物,以葛根素(puerarin)、大豆苷元(daidzein)和大豆苷(daidzin)研究最多,药理作用也最明显。文中对近年来葛根及其有效成分在动脉粥样硬化方面的研究进行综述。     

葛根素在2型糖尿病及合并症的临床应用

中医认为葛根素具有活血化瘀的功效。近年来葛根的研究与开发逐渐受到关注。在临床上应用葛根素治疗 2型糖尿病及合并症病人 ,发现其对血糖、胰岛素敏感性及血流变学及并发症症状有明显改善。在糖尿病中已得广泛应用 ,现综述如下。葛根 ,为豆科葛属植物野葛或甘葛藤的干燥根。该药始载于《神农本草经》 ,列为中品 ,历代本草均有记载 ,为常用中药之一。通过对葛根主要成分的提取、分离和鉴定 ,发现葛根的主要成分为如下几类[1] :①异黄酮类 ,主要包括大豆苷元 (大豆素、大豆黄素、黄豆苷元 )、大豆苷、葛根素等 ;②葛根苷类 ,主要包括葛根苷…     

葛根的化学成分、药理作用和临床应用研究

现代药理研究证明,葛根中葛根素、大豆苷元和大豆苷等异黄酮类化合物为有效成分,对心血管系统、免疫系统的疾病有较好的治疗作用,其制剂用于治疗头晕头痛、高血压病、心绞痛和突发性耳聋等疾患疗效显著,临床应用广泛。本文对葛根的化学成分、药理作用和临床应用等方面作一综述。     

HPLC法同时测定保健食品中6种大豆异黄酮类成分的含量

目的:建立同时测定大豆类保健食品中大豆苷、黄豆黄苷、染料木苷、大豆苷元、黄豆黄素、染料木素6种成分含量的高效液相色谱法。方法:色谱柱为 Agilent Zorbax SB-C_(18)(4.6 mm×150 mm,5 μm),采用流动相乙腈-0.2%甲酸进行梯度洗脱,流速为1 mL·min~(-1),检测波长为255 nm。结果:大豆苷、黄豆黄苷、染料木苷、大豆苷元、黄豆黄素、染料木素的线性范围分别为0.42～3.15,0.20～2.25,0.41～3.06,0.15～1.14,0.051～0.38,0.21～1.55 μg;加样回收率(n=5)分别为95.86%,96.87%,96.85%,96.63%,96.48%,96.67%。结论:本方法简便、灵敏、准确,可用于含大豆异黄酮类保健食品中以上6种成分的含量测定和产品质量控制。     

葛根正丁醇部位的化学成分研究

目的 研究葛根正丁醇萃取物的化学成分.方法 采用聚酰胺柱色谱、反相ODS柱色谱、凝胶柱色谱、制备液相色谱等方法进行分离纯化,根据化合物的理化性质及波谱数据鉴定其结构.结果 分离鉴定了12个化合物,分别为葛酚苷元A(1)、葛酚苷元B(2)、染料木素(3)、3′-甲氧基葛根素(4)、3′-羟基葛根素(5)、葛根素芹糖苷(6)、葛根素木糖苷(7)、大豆苷元(8)、大豆素7,4′-二葡萄糖苷(9)、大豆苷(10)、葛根素(11)、胡萝卜苷(12).结论 其中化合物1、2为首次从葛属植物中分离得到.     

HPLC法同时测定中国、泰国葛根中异黄酮的含量

目的:建立HPLC法同时测定中国、泰国葛根中异黄酮大豆苷、大豆苷元和染料木素的含量,为其质量控制提供方法学参考.方法:色谱柱为AT.LICHROM ODS-C18柱(250 mm ×4.6 mm,5μm);流动相为甲醇和水,梯度洗脱;流速:0.8 ml·min-1;检测波长250 nm;柱温为25℃.结果:大豆苷、大豆苷元和染料木素分别在0.15 ～0.88 μg,0.10 ～0.63 μg,0.15 ～0.89 μg范围内呈良好线性关系,r分别为0.9997,0.9995,0.9996.其平均回收率在99.5％～100.4％范围内,RSD均小于3％.结论:建立的方法简单、准确,分离效果好,首次用于中国、泰国葛根的定量分析和比较分析,为葛根的资源研究提供参考.     

麦冬提取物及其有效成分的药理作用研究进展

麦冬来源于百合科植物麦冬Ophiopogon japonicus的干燥块根,有养阴生津,润肺清心的功效。麦冬的化学成分丰富,主要成分有甾体皂苷类、高异黄酮类、多糖类等,具有保护心血管、保护消化系统、抗肿瘤、保护神经系统、改善肝、肺损伤、抗炎抗氧化、降糖、抗衰老、免疫调节等药理作用。主要对麦冬皂苷B、麦冬皂苷D、麦冬多糖、麦冬水提物及醇提物的药理作用进行全面综述,以期为麦冬的深度开发以及新药研发提供参考。     

Synthesis of tritium‐labeled puerarin—a potential antidipsotropic agent

Puerarin 1 (8‐β‐D ‐Glucopyranosyl‐4′‐7‐dihydroxyisoflavone, NPI‐031G) is the major isoflavone C‐glycoside isolated from Pueraria lobata, a traditional Chinese medicine widely used for the treatment of alcohol intoxication. In order to understand the mode of action of puerarin in the reward pathway of the central nervous system and to study its bioavailability and pharmacokinetics, we developed a synthetic route for the preparation of tritium‐labeled puerarin. The key intermediate 4 was obtained by trimethylsilyl protection of all hydroxyl groups followed by selective deprotection. The corresponding aldehyde 5 was obtained through the subsequent oxidation of the primary alcohol. Standard NaB[³H]₄ reduction and hydrolysis produced the tritium‐labeled puerarin 6 . Copyright © 2007 John Wiley & Sons, Ltd.     

败酱草及其有效成分抗结直肠癌药理作用机制研究进展

败酱草来源于败酱科草本植物黄花败酱Patrinia scabiosaefolia和白花败酱P.villosa的带根全草,其乙醇提取物在动物体内外实验中均表现出明显的抗结直肠癌作用,抗肿瘤的主要活性成分为黄酮类和皂苷类。败酱草抗结直肠癌药理作用机制主要是抑制结直肠癌细胞增殖并诱导其凋亡,抑制肿瘤血管生成,调控相关蛋白表达,调节信号传导通路,逆转结直肠癌细胞耐药及调节机体免疫功能。对败酱草及其有效成分抗结直肠癌的药理作用机制进行综述,以期为抗结直肠癌新药研发提供参考。     

The effects of Puerarin on CYP2D6 and CYP1A2 activities <Emphasis Type="Italic">In vivo</Emphasis>

Ge-gen (Radix Puerariae) is used in traditional oriental medicine for various medicinal purposes. The drug is the root of a wild leguminous creeper, Pueraria lobata (Willd) Ohwi. It possesses a high content of avonoid derivatives, the most abundant of which is puerarin. Our goal was to find the effect of puerarin on cytochrome P450 enzymes in vivo. The study was conducted in 18 male volunteers of different genotypes (CYP2D6 *1/*1, *1/*10, *10/*10). Plasma was obtained at 6 h after oral administration and urine was collected from 0 to 8 h after probe drug administration. The logarithm value of metabolic rate decrease from −0.0055 ± 0.1887 to −0.1754 ± 0.2411 implied puerarin inhibited activity of CYP2D6. There was no significant relationship between the inhibition with the CYP2D6 genotypes. The paraxanthin/caffeine ratio in the plasma sample at 6th hour was increased by 30 ± 47% (p = 0.003), implied puerarin induced the activity of CYP1A2. While puerarin used together with the substrates of both enzymes, drug interaction worth the attention and at sometimes precautions are needed.     

Simultaneous analysis of isoflavones and saponins in <Emphasis Type="Italic">Pueraria</Emphasis> flowers using HPLC coupled to an evaporative light scattering detector and isolation of a new isoflavone diglucoside

The Pueraria flowers, Puerariae Flos [Puerariae Lobatae Flos (the flowers of P. lobata) and Puerariae Thomsonii Flos (the flowers of P. thomsonii)], have been used as crude drugs to counteract the overconsumption of alcohol in Japan and China. Both types of Puerariae Flos contain a large amount of isoflavones and saponins. Simultaneous analysis of the total saponin and isoflavone fraction within the flowers has proven difficult thus far; however, profile analysis of saponin and isoflavone levels was attempted in this study by using HPLC coupled to an evaporative light scattering detector (ELSD). A characteristic peak of kakkalide was common in the chromatograms of extracts originating from the flowers of P. lobata, though original habitats were different. Tiny peaks of saponins were also observed in chromatograms of all specimens derived from P. lobata. In the chromatograms of six out of eight extracts of Puerariae Thomsonii Flos originating from Guangdong, China, characteristic twin peaks corresponding to tectorigenin 7-O-xylosylglucoside and tectoridin were observed. The distinctive twin peaks were not found in the chromatograms of the extracts produced in Hunan and Sichuan. Although the amounts of total saponins and isoflavones obtained from Puerariae Lobatae Flos were almost the same, those of Puerariae Thomsonii Flos varied remarkably and were not related to habitat. A good yield of a new isoflavone glycoside was obtained from some specimens of Puerariae Thomsonii Flos; the structure was determined to be 6-hydroxygenistein 6,7-di-O-glucoside.     

Effects of glycyrrhizin on the pharmacokinetics of puerarin in rats

1. Puerarin has been reported to possess a wide range of pharmacological activities. This study investigated the effects of glycyrrhizin on the pharmacokinetics of puerarin in rats.

2. The pharmacokinetics of orally administered puerarin (50?mg/kg) with or without glycyrrhizin pretreatment (100?mg/kg/day for 7?days) were investigated. The plasma concentration of puerarin was determined using a sensitive and reliable LC-MS/MS method. The pharmacokinetics profiles were calculated and compared. Additionally, a Caco-2 cell transwell model was used to investigate the potential mechanism of glycyrrhizin’s effects on the pharmacokinetics of puerarin.

3. The results showed that when the rats were pretreated with glycyrrhizin, the maximum concentration (C_max) of puerarin decreased from 761.25?±?52.34 to 456.32?±?34.75?ng/mL, and the area under the concentration–time curve from zero to infinity (AUC_0–inf) also decreased from 4142.15?±?558.51 to 2503.74?±?447.57?μg·h/L. The oral clearance of puerarin increased significantly from 12.20?±?1.53 to 20.47?±?3.25?L/h/kg (p?4. In conclusion, these results indicated that glycyrrhizin could affect the pharmacokinetics of puerarin, possibly by decreasing the systemic exposure of puerarin by inducing the activity of P-gp.     

Dynamics of phytoestrogen,isoflavonoids, and its isolation from stems of Pueraria lobata (Willd.) Ohwi growing in Democratic People’s Republic of Korea

Four isoflavonoids were isolated from stems of Pueraria lobata (Willd.) Ohwi growing in Democratic People’s Republic of Korea and identified as daidzein (1), genistin (2), daidzin (3), and puerarin (4), structures, which were elucidated by means of spectroscopic analysis. Isoflavonoids were isolated using silica gel chromatography and purified with organic solvents. Isoflavonoid contents in P. lobata were determined using reliable high-performance liquid chromatography. The results indicated that the contents of puerarin and genistin in the roots are higher than those in the stems (6.19% and 0.04% vs. 1.15% and 0.02%), whereas the stems have higher contents of daidzin and daidzein than the roots (3.17% and 0.06% vs. 1.72% and 0.05%). Accordingly, the root part of the plant is useful for the isolation of puerarin and the stem part for daidzin. This study suggests that the stem of P. lobata is useful as an alternative source of puerarin, daidzin, genistin, and daidzein. In addition, collection of the stem will not sacrifice the plant and thus is beneficial to the natural ecosystems.     

芒柄花素药理作用的研究进展

芒柄花素属于异黄酮类化合物,是黄芪中异黄酮类化合物的代表成分,具有抗炎、抗氧化、抗肿瘤、雌激素样作用.对芒柄花素保护脑血管系统、保护心血管系统、抗肿瘤作用、对糖尿病心肌病的保护作用等进行了总结,以期为芒柄花素的基础研究和临床应用提供依据.     

Peroxyl radical scavenging capacity of extracts and isolated components from selected medicinal plants

We determined the ability of extracts and active components isolated from nine medicinal plants, Poncirus trifoliata, Astragalus membranaceus, Magnolia obovata, Salvia miltiorrhiza, Angelica dahurica, Cornus officinalis, Cnidium officinale, Pueraria lobata and Ostericum koreanum, to neutralize peroxyl radicals using the total oxyradical scavenging capacity (TOSC) assay. Peroxyl radicals were generated from thermal homolysis of 2,2′-azobis(2-methylpropionamidine) dihydrochloride, which oxidize α-keto-γ-methiolbutyric acid to yield ethylene, and the TOSC of the substances tested is quantified from their ability to inhibit ethylene formation. Extracts from S. miltiorrhiza, M. obovata and P. lobata were determined to be potent peroxyl radical scavenging agents with a specific TOSC (sTOSC) being at least threefold greater than that of glutathione. Major constituents of the three plants, tanshinone, cryptotanshinone, 15,16-dihydrotanshinone, syringin, honokiol, magnolol, daidzein, puerarin and genistein, were examined for the antioxidant potential toward peroxyl radical. Puerarin and genistein were shown to have μM sTOSCs at least ten-fold greater than sTOSC of glutathione. Daidzein, syringin and honokiol demonstrated the peroxyl radical scavenging capacity comparable to that of glutathione. The implication of peroxyl radical in lipid peroxidation and other cellular damage suggests a possible protective role for the extracts and isolated components in oxidative stress caused by this reactive oxygen species.     

葛根素治疗相关疾病的研究

葛根素是从中药葛根中提取分离出来的一种单体,属异黄酮类化合物,具有多种药理作用,药理活性强,药效明确,适用于冠心病、心绞痛、心肌梗死、视网膜动静脉阻塞、突发性耳聋等疾病。主要的药理作用：对脏器组织的保护、抗缺血再灌注损伤、改善血液流变学指标、抑制钙超载、保护神经细胞作用、改善胰岛素抵抗作用等。本文主要就葛根素的药理作用及近年来在临床治疗方面的进展进行综述。