银杏药用物质的开发利用现状及其发展设想

本文概述了银杏叶的药理作用及其开发利用现状。目前,银杏药用物质的获取仍然是通过提取这一途径,这同时存在地理环境,季节等诸多限制因则通过银杏组织,细胞培养获得其药用物质的技术刚刚起步,距离实际应用仍有相当的距离,但随着这项技术的不断发展。它不仅可用于生产银杏黄酮类和银杏内酯,而且有助于进一步研究银杏所含的特殊化学成分及其相关的代谢途径。     

银杏系列饮品的加工技术及质量控制

银杏系列饮品的加工技术及质量控制赵伯涛，王玉成（内贸部南京野生植物研究所）（扬州市银杏保健食品厂）银杏果仁营养丰富，具许多生理活性物质，有重要的药用和保健价值。我国银杏资源量大，果实产量约占世界的四分之三，但各产区大部分以原料销售或出口为主，其商品价...     

NO对银杏悬浮细胞生长及黄酮类物质合成的影响

以硝普钠(sodium nitroprusside,SNP)为一氧化氮(NO)的供体,向银杏悬浮细胞培养液中加入不同浓度的SNP,研究外源NO对银杏悬浮细胞生长状况、过氧化氢酶(CAT)活性、苯丙氨酸解氨酶(PAL)活性和黄酮类物质生物合成的影响.结果表明,低浓度SNP有利于银杏悬浮细胞生长,而高浓度SNP可以促进黄酮类物质的合成.银杏悬浮细胞在添加0.5和10 mmol/L SNP的培养基中培养16 d时,细胞干重分别为对照组的134%和73%;在添加10 mmol/L SNP的培养基中培养20 d时,细胞中黄酮类物质的含量为对照组的136%.同时,10 mmol/L SNP促进银杏悬浮细胞PAL和CAT活性显著升高.NO专一性淬灭剂c-PITO(carboxyl phenyltetramethylimidazoleoxide)抑制SNP对银杏悬浮细胞生长、CAT活性、PAL活性和黄酮类物质含量的促进作用,说明SNP是通过其分解产物NO影响细胞生长和黄酮类物质的合成.根据这些结果推测,NO可能通过触发银杏悬浮细胞的防卫反应,激活了细胞中黄酮类物质的生物合成途径.     

银杏的药用价值及开发前景

银杏的药用价值及开发前景王兆东（江苏省新沂市炮车中学２２１４３２）银杏全身都是宝,食用和药用价值很高。银杏的种仁、种壳、树叶、树皮、树根均有很高的药用价值。１银杏果的药用和食用价值银杏种子俗称白果,种仁营养丰富,药食俱佳。明朝李时珍的《本草纲目》对白...     

银杏细胞悬浮培养及其银杏内酯产生的研究

对银杏细胞悬浮培养及其次生代谢产物银杏内酯的产生进行了研究。考察了各种理化因子对细胞生长及银杏内酯产生的影响;对培养物中银杏内酯进行了定性及定量测定。HPLC测定结果显示,银杏悬浮细胞培养物中银杏内酯的含量可达0.0099%。     

银杏内酯研究概况

银杏内酯研究概况钱骅,赵伯涛（内贸部南京野生植物综合利用研究所）银杏（ＧｉｎｋｇｏｂｉｌｏｂａＬ．）做为药用在我国已有悠久的历史,但对其化学成份和药理作用的研究则开始于６０年代,现在药理实验已经表明,银杏叶中具生理活性的主要化学成分为黄酮忒、茁内酯、...     

银杏叶的药用价值与开发利用前景

银杏叶的药用价值与开发利用前景李淑娟（哈尔滨医药集团进出口公司,哈尔滨）银杏叶为银杏科植物银杏ＧｉｎｋｇｏＢｉｌ。ｂａＬ．的叶,它作为药用已有６００多年的历史,然而对它进行药理和其它方面的研究始于七十年代,尤其近十年来国内外的研究进展更为迅速。近年来...     

干旱胁迫下外源一氧化氮促进银杏可溶性糖、脯氨酸和次生代谢产物合成

以硝普钠（sodium nitroprusside,SNP）为一氧化氮（NO）供体,研究其在干旱胁迫下对银杏叶片物质代谢的影响。结果表明,在土壤相对含水量为35％的干旱胁迫下,250μmol／LSNP显著提高可漆性糖含量、脯氨酸含量、苯丙氨酸解氨酶（phenyl Manineammonia lyase．PAL）活性、黄酮类化合物和银杏内酯含量。NO清除剂血红蛋白（hemoglobin）抑制了SNP对银杏叶片可溶性糖、脯氨酸、PAL酶活性、黄酮和银杏内酯合成的促进作用,说明SNP是通过其分解产物NO影响这些物质的合成。推测在干旱胁迫下次生代谢产物黄酮类物质和银杏内酯的作用类似脯氨酸和可溶性糖,NO通过促进这些物质的合成,来缓解干旱胁迫的不良影响。     

不同银杏无性系叶药用成分差异及聚类分析

运用HPLC技术分析了54个银杏(Ginkgo biloba)无性系叶总黄酮和萜内酯及其组分含量的差异,并进行了聚类。结果表明,银杏无性系间叶中总黄酮、萜内酯及其组分含量存在遗传变异,且萜内酯及其组分含量的变异系数明显高于总黄酮及其组分。总黄酮含量较高的无性系有18、42、32和50号,其槲皮素、异鼠李素、山奈酚含量均较高。萜内酯含量较高的无性系为13、42、33、51和65号,其银杏内酯A(GA)、银杏内酯B(GB)、银杏内酯C(GC)及白果内酯(BB)含量均较高。通过对总黄酮-萜内酯进行联合复选,显示叶中总黄酮和萜内酯含量均较高的无性系为13、65、33、51、18、32和42号。这些无性系可通过嫁接、扦插直接在银杏采叶园进行推广种植,或作为叶用银杏新品种的育种材料。     

银杏细胞固定化培养及银杏内酯的产生

探讨利用银杏 (GinkgobilobaL .)细胞固定化培养方法 ,大规模生产药用成分银杏内酯类化合物的可能性。考察了植物生长调节剂对银杏固定化培养细胞生长及发酵液中银杏内酯类成分产生的影响。结果显示 ,最优培养基生长调节剂配比为 2 ,4 D 8 0mg L KT 0 0 4mg L NAA 0 4mg L。优化培养后 ,固定化细胞最高生物量出现在第 1 2d ,为 0 4gDW 瓶。发酵液中银杏内酯含量 :GKA在 2 2d时最高 (2 0 0 μg L) ,GKB在 1 8d时最高 (1 2 2 μg L) ,GKC在 1 8d时最高 (5 0 9μg L)。     

Isolation of ginkgolides A, B, C, J and bilobalide from G. biloba extracts

Ginkgolides A, B, C and J, together with bilobalide, are unique terpenoid components of the Ginkgo biloba tree. Due to similar chemical properties, their separation is quite tedious. We have developed an efficient and rapid protocol for separation of individual ginkgolides and bilobalide from G. biloba extracts. The procedure takes advantage of enhanced susceptibility of ginkgolides B and C to benzylation and the ease of separation of these products from ginkgolides A and J which do not react. The protocol is applicable to the previously reported enriched extracts prepared from G. biloba leaves. A single chromatographic step prior to benzylation provides bilobalide and mixture of ginkgolides A, B, C, and J. After benzylation, the individual ginkgolides are separated by chromatography.     

Effect of supplementing terpenoid biosynthetic precursors on the accumulation of bilobalide and ginkgolides in Ginkgo biloba cell cultures

The effect of precursor feeding on the production of bilobalide and ginkgolides was studied with suspension cell cultures of Ginkgo biloba. The precursors greatly influenced the productivity of bilobalide and ginkgolides. Precursor supplementation increased the accumulation of both bilobalide and ginkgolides, and with positive effect on cell growth. The GA accumulation by cell cultures was influenced by precursors upstream in the metabolism, whereas the BB accumulation was under the influence of downstream precursors of the terpenoid biosynthetic pathway. Furthermore, precursor feeding modified the ratios of the BB, GA and GB in cells and cell cultures of G. biloba. The studies also aid in understanding effect of precursor feeding on the bilobalide and ginkgolides biosynthetic pathway.     

不同采收期银杏叶总内酯及黄酮甙的含量测定

采用ＨＰＬＣ法对不同采收期银杏叶总内酯及黄酮甙含量进行测定,结果表明,八至九月采收的银杏叶总内酯及黄酮甙含量均较高。     

Gingkolides and bilobalide: structure, pharmacology, and synthesis]

The review summarizes data on the structure, pharmacology properties and synthetic investigations of ginkgolides and bilobalide occurring in the ginkgo tree (Ginkgo biloba L.). Ginkgolide B is a powerful antagonist of platelet activating factor.     

Effect of Ginkgo biloba extract on rat hepatic microsomal CYP1A activity: role of ginkgolides, bilobalide, and flavonols

The present study investigated the in vitro effect of Ginkgo biloba extracts and some of the individual constituents (ginkgolides, bilobalide, and flavonols such as kaempferol, quercetin, isorhamnetin, and their glycosides) on CYP1A-mediated 7-ethoxyresorufin O-dealkylation in hepatic microsomes isolated from rats induced with beta-naphthoflavone. G. biloba extract competitively inhibited CYP1A activity, with an apparent Ki value of 1.6 +/- 0.4 microg/mL (mean +/- SE). At the concentrations present in the G. biloba extracts, ginkgolides A, B, C, and J and bilobalide did not affect CYP1A activity, whereas kaempferol (IC50 = 0.006 +/- 0.001 microg/mL, mean +/- SE), isorhamnetin (0.007 +/- 0.001 microg/mL), and quercetin (0.050 +/- 0.003 microg/mL) decreased this activity. The monoglycosides (1 and 10 microg/mL) and diglycosides (10 microg/mL) of kaempferol and quercetin but not those of isorhamnetin also inhibited CYP1A activity. The order of inhibitory potency was kaempferol approximately equal to isorhamnetin > quercetin, and for each of these flavonols the order of potency was aglycone > monoglycoside > diglycoside. In summary, G. biloba extract competitively inhibited rat hepatic microsomal CYP1A activity, but the effect was not due to ginkgolides A, B, C, or J, bilobalide, kaempferol, quercetin, isorhamnetin, or the respective flavonol monoglycosides or diglycosides.     

Terpene trilactones from Ginkgo biloba are antagonists of cortical glycine and GABA(A) receptors

Glycine and gamma-aminobutyric acid, type A (GABA(A)) receptors are members of the ligand-gated ion channel superfamily that mediate inhibitory synaptic transmission in the adult central nervous system. During development, the activation of these receptors leads to membrane depolarization. Ligands for the two receptors have important implications both in disease therapy and as pharmacological tools. Terpene trilactones (ginkgolides and bilobalide) are unique constituents of Ginkgo biloba extracts that have various effects on the central nervous system. We have investigated the relative potency of these compounds on glycine and GABA(A) receptors. We find that most of the ginkgolides are selective and potent antagonists of the glycine receptor. Bilobalide, the single major component in G. biloba extracts, also reduces glycine-induced currents, although to a lesser extent. Both ginkgolides and bilobalide inhibit GABA(A) receptors, with bilobalide demonstrating a more potent effect. Additionally, we provide evidence that open channels are required for glycine receptor inhibition by ginkgolides. Finally, we employ molecular modeling to elucidate the similarities and differences in the structure of the terpene trilactones to account for the pharmacological properties of these compounds and demonstrate a striking similarity between ginkgolides and picrotoxinin, a GABA(A) and recombinant glycine alpha-homomeric receptor antagonist.     

Pancreatic lipase inhibition activity of trilactone terpenes of Ginkgo biloba

The prevalence of obesity is increasing at an alarming rate, but, unfortunately, only a few drugs are currently available on the market. In the present study, the methanolic extract of Ginkgo biloba L. (Ginkgoaceae) was investigated as an inhibitor of pancreatic lipase (PL) in an attempt to explain its hypolipidaemic activity. In vitro assay of G. biloba leaves extract revealed a substantial PL inhibition activity (IC(50)?=?16.5 μg/mL). Further investigation was performed by employing theoretical docking simulations and experimental testing to uncover the active constituents responsible for G. biloba anti-lipase activity. Virtually, terpene trilactones, including ginkgolides and bilobalide, were found to fit within the binding pocket of PL via several attractive interactions with key amino acids. Experimentally, ginkgolides A, B, and bilobalide were found to inhibit PL significantly (IC(50)?=?22.9, 90.0, and 60.1 μg/mL, respectively). Our findings demonstrated that the hypolipidaemic effects of G. biloba extract can be attributed to the inhibition of PL by, at least in part, terpene trilactones. In conclusion, this work can be considered a new step towards the discovery of new natural safe hypolipidaemic PL inhibitors.     

Effects of extract of Ginkgo biloba leaves and its constituents on carcinogen-metabolizing enzyme activities and glutathione levels in mouse liver

The effects of a standardized extract of Ginkgo biloba L. leaves (EGb) and its terpene constituents, bilobalide and ginkgolides, on the activities of detoxification enzymes, i.e., glutathione S-transferases (GSTs) and DT-diaphorase, and glutathione contents, were investigated in the mouse liver. Oral treatment with EGb (100-1,000 mg/kg) and bilobalide (10-30 mg/kg) once a day for 4 days caused a dose-dependent elevation in GST activity. Ginkgolide A (30 mg/kg, for 4 days) also significantly elevated GST activity, whereas ginkgolide B and ginkgolide C at the same dose had no effects. EGb significantly increased the protein level of GST pi, and bilobalide significantly increased those of GST alpha and GST mu Moreover, EGb-treatment and bilobalide-treatment caused significant elevations in DT-diaphorase activity and in hepatic glutathione contents.     

Effect of biotic elicitors on the accumulation of bilobalide and ginkgolides in Ginkgo biloba cell cultures

The effect of biotic elicitors on the production of bilobalide and ginkgolides in Ginkgo biloba cell suspension cultures was studied. The treatment of cell cultures with Candida albicans and Staphylococcus aureus as elicitors increased the amounts of bilobalide (BB), ginkgolide A (GA) and ginkgolide B (GB), with slight growth inhibition. The native bacterial elicitor was more effective for secondary metabolite accumulations both in cells and culture medium than autoclaved. However, exposure times of the cells to the elicitors strongly influenced the production of BB, GA and GB. This study suggests that biotic elicitors can regulate the production of BB, GA and GB either directly or indirectly. These results also describe the establishment of optimum conditions that determine the effects of biotic elicitors on secondary metabolism of bilobalides.     

Variation of ginkgolides and bilobalide contents in leaves and cell cultures of<Emphasis Type="Italic">Ginkgo biloba</Emphasis> L.

Ginkgolides (GK) and bilobalide are valuable compounds that belong to the lactone terpene. The contents of these metabolites were determined by HPLC from female and male tree ofGinkgo biloba L. The productivity ofG. biloba cells was also compared with the corresponding individual trees. High variations in the ginkgolides and bilobalide were observed from different individuals, plant parts, and cultured cells. The ginkgolides and bilobalide contents were different depending on the plant parts. Callus was obtained from various plant tissues, and NAA was better at callogenesis than 2,4-D in both the female and male trees. The plants and their corresponding cells showed considerable variation in their ginkgolides and bilobalide concentrations. The ginkgolides and bilobalide contents were not correlated with the production between dominant trees and their corresponding cells. Light irradiation enhanced the production of GK-A and GK-B, however, the concentration of bilobalide decreased under dark conditions.