Antifungal activity of biflavones from Taxus baccata and Ginkgo biloba

Bilobetin and 4'-O-methylamentoflavone were isolated and identified in the needles of Taxus baccata, for the first time in this species. The antifungal activity of biflavones from T. baccata and Ginkgo biloba, namely amentoflavone, 7-O-methylamentoflavone, bilobetin, ginkgetin, sciadopitysin and 2,3-dihydrosciadopitysin towards the fungi Alternaria alternata, Fusarium culmorum, Cladosporium oxysporum was determined employing computer-aided image analysis couplet to a microscope. Bilobetin exhibited a significant antifungal activity with values of ED50 14, 11 and 17 microM respectively. This compound completely inhibited the growth of germinating tubes of Cladosporium oxysporum and Fusarium culmorum at a concentration 100 microM. Activity of ginkgetin and 7-O-methylamentoflavone towards Alternaria alternata was stronger than that of bilobetin. Moreover, slight structural changes in the cell wall of Alternaria alternata exposed to ginkgetin at concentration of 200 microM were observed.     

银杏叶单组分双黄酮分离制备及抗氧化活性研究

从银杏叶中分离制备高纯度双黄酮对照品,探讨其抗氧化活性强弱。以60%乙醇-水提取的银杏叶浸膏为原料,反溶剂沉淀得到含量80.40%的双黄酮粗品,再以甲醇-水为流动相,半制备色谱梯度洗脱。结果得到了4种符合中药化学对照品要求的高纯度双黄酮,在最佳制备条件下,4种双黄酮纯度:阿曼托黄素(98.45%)、白果素(98.66%)、银杏黄素异构体(98.87%)、金松双黄酮(99.29%),其产率(mg/kg)分别为:22.5、23.8、192.5、71.8,考察了它们的抗氧化活性,并采用60%乙腈和有机酸水溶液对银杏黄素异构体进行了完全分离。建立的制备方法快速简便,所得单组分双黄酮纯度、产量高。本工作为单组分银杏双黄酮新药的研究与开发提供重要的技术支持。     

Assay and inhibition of diacylglycerol lipase activity

A series of N-formyl-α-amino acid esters of β-lactone derivatives structurally related to tetrahydrolipstatin (THL) and O-3841 were synthesized that inhibit human and murine diacylglycerol lipase (DAGL) activities. New ether lipid reporter compounds were developed for an in vitro assay to efficiently screen inhibitors of 1,2-diacyl-sn-glycerol hydrolysis and related lipase activities using fluorescence resonance energy transfer (FRET). A standardized thin layer chromatography (TLC) radioassay of diacylglycerol lipase activity utilizing the labeled endogenous substrate [1″-(14)C]1-stearoyl-2-arachidonoyl-sn-glycerol with phosphorimaging detection was used to quantify inhibition by following formation of the initial product [1″-(14)C]2-arachidonoylglycerol and further hydrolysis under the assay conditions to [1-(14)C]arachidonic acid.     

银杏内生菌的分离及其抑菌活性筛选

从健康的银杏（Ginkgo biloba）茎和叶片中分离内生菌,结果从银杏叶和茎上共分离到内生真菌20株,其中9株来自银杏茎部,11株来自银杏叶部;内生放线菌23株,其中15株来自于银杏茎部,8株来自于银杏叶部;内生细菌15株,其中8株来自于银杏茎部,7株来自于银杏叶部。以金黄色葡萄球菌（Staphylococcus aureus）、枯草芽胞杆菌（Bacillus subtilis）、大肠埃希菌（Escherichia coli）、黑曲霉（Aspergillus niger）、酿酒酵母（Saccharomyces cerevisiae）作为指示菌,采用双层平板法对内生菌进行抑菌活性筛选,结果表明：20株内生真菌中有12株出现了抑菌活性,有抑菌活性菌株的比例为60.0%;23株内生放线菌中,仅3株出现了抑菌活性,有抑菌活性菌株的比例为13.0%;15株内生细菌中,有4株出现了抑菌活性,有抑菌活性菌株的比例为26.7%。     

Characteristics and antifungal activity of a chitin binding protein from Ginkgo biloba

An antifungal peptide from leaves of Ginkgo biloba, designated GAFP, has been isolated. Its molecular mass of 4244.0 Da was determined by mass spectrometry. The complete amino acid sequence was obtained from automated Edman degradation. GAFP exhibited antifungal activity towards Pellicularia sasakii Ito, Alternaria alternata (Fries) Keissler, Fusarium graminearum Schw. and Fusarium moniliforme. Its activities differed among various fungi. GAFP could also cause increased hyphal membrane permeabilization and a rapid alkalization of the medium when applied at 100 microgram/ml to Pellicularia sasakii Ito hyphae. The amino acid sequence of GAFP shows characteristics of the cysteine/glycine-rich chitin binding domain of many chitin binding proteins. The cysteine residues are well conserved.     

Antiestrogenic activities of Ginkgo biloba extracts

Most climacteric and postmenopausal women appear to have vasomotor symptoms as well as a high risk of osteoporosis and cardiovascular disease. Although exogenous estrogens can reduce these symptoms, women are reluctant to use hormone replacement therapy (HRT) due to its undesirable side effects, such as irregular bleeding and an increased risk of breast cancer. A previous study suggested that Ginkgo biloba extracts (GBE) have estrogenic activity and might be suitable as an alternative to HRT. However, there are no reports of the preventive effect of GBE on breast cancer, which is the side effect of classical HRT. In this study, it was confirmed that GBE exhibits estrogenic and antiestrogenic activity depending on the E₂ and GBE concentration, via estrogen receptor (ER)-dependent and ER-independent pathways. In addition, GBE reduced the E₂ levels by stimulating the E₂ metabolism and inhibiting E₂ synthesis, which indicates that GBE can induce antiestrogenic activity via the depletion of E₂. Furthermore, GBE might have similar action to selective arylhydrocarbon receptor modulators (SAhRMs), which induce antiestrogenic activity through cross-talk between the arylhydrocarbon receptor (AhR) and ER. In conclusion, GBE has a biphasic effect on estrogen, and can be considered as a potential alternative to HRT with chemopreventive effects on breast cancer. However, further studies on animals and humans will be required.     

Quercetin coumaroyl glucorhamnoside from Ginkgo biloba

A new flavonoid glycoside was isolated from the leaves of Ginkgo biloba (Ginkgoaceae) and its structure elucidated as quercetin-3-O-α-(6‴-p-coumaroylglucosyl-β-1,4-rhamnoside).     

银杏叶片形态研究

通过对银杏不同枝类、不同叶序的叶片形态进行调查,结果表明:银杏不同枝类的叶片形态差异较大,叶宽、叶柄长、叶基角:多年生鳞枝＞一年生鳞枝＞一年生长枝;叶长、叶形指数:一年生长枝＞一年生鳞枝＞多年生鳞枝;叶面积:一年生和多年生鳞枝＞一年生长枝;有缺刻叶比例:一年生长枝＞多年生鳞枝＞一年生鳞枝.一年生长枝叶片的叶宽、叶长、叶面积、叶柄长、叶基角均随叶序的增加逐渐减小,叶形指数和有缺刻叶的比例则增加.一年生和多年生鳞枝1～5叶的叶长、叶宽和叶面积随叶序增加而逐渐增加,第5～6叶达最大,以后随叶序增加而逐渐减小,叶形指数和叶柄长度随叶序增加而增加,叶基角随叶序增加而减小.一年生长枝的第2叶、一年和多年生鳞枝的第4叶可作为品种描述的标准叶.     

银杏内生真菌的生态分布

2004—2005年春夏秋3季,在江西省九江地区4个地点分别采集健康的银杏(Ginkgo biloba)植株,分离得到内生真菌198株,经形态学分类鉴定为6目、7科、22属。研究结果表明,银杏内生真菌的分布存在季节差异、组织部位差异、年龄差异;优势菌群的组成与数量随采样地点、分离组织部位、不同生长时期内生真菌的不同而变化。与中国其他地区的银杏植株内生真菌进行比较,结果表明,植物内生真菌的分布与地域具有一定的相关性,体现了内生真菌生态分布的多样性。     

银杏叶多酚的机械力辅助提取及其体外抗氧化活性研究

为优化银杏叶多酚提取工艺,通过单因素试验考察填充率、球磨转速、球磨时间、乙醇浓度、料液比、提取温度、提取时间七个因素对机械力辅助提取银杏叶多酚得率的影响,以银杏叶多酚得率为响应值,采用Box-Benhnken三因素三水平响应面设计优化工艺,同时比较了4种提取方法对银杏叶多酚提取得率和抗氧化活性的差异。结果表明,机械力辅助提取银杏叶多酚的最佳工艺条件为:填充率26%、球磨转速为400rpm、球磨时间为15min。在此条件下,银杏叶多酚的得率为7.33%。机械力辅助乙醇提取银杏叶多酚得率低于碱水提取法,但是抗氧化活性高于碱水法提取的银杏叶多酚;抗氧化活性与乙醇回流法提取的银杏叶多酚相当,但是提取得率高于乙醇回流法。此提取工艺高效可行,具有一定的参考价值。