Antimycobacterial coumarins from the sardinian giant fennel (Ferula communis)

The structure of a new prenylated coumarin (E-omega-benzoyloxyferulenol, 1b) from the Sardinian giant fennel (Ferula communis) has been confirmed by synthesis. The parent compound ferulenol (1a) showed sub-micromolar antimycobacterial activity, which was partly retained in 1b and in the simplified synthetic analogue 3, but diminished in its omega-hydroxy and omega-acetoxy derivatives (1c and 1d, respectively). The outstanding activity of 1a, its low toxicity, and the evidence for definite structure-activity relationships make this prenylated 4-hydroxycoumarin an interesting antibacterial chemotype worth further investigation.     

Antifungal activity of some coumarins obtained from species of Pterocaulon (Asteraceae)

Fractionation of antifungal hexane extracts of the aerial parts of three Pterocaulon spp., Pterocaulon alopecuroides, Pterocaulon balansae and Pterocaulon polystachyum (Asteraceae) from South Brazil traditionally used to treat animal mycoses, afforded the coumarins 5-methoxy-6,7-methylenedioxycoumarin, 7-(2',3'-epoxy-3'-methylbutyloxy)-6-methoxycoumarin, 6,7-methylenedioxycoumarin (ayapin), along with a mixture of 6-hydroxy-7-(3'-methylbutyl-2'-en-oxy)-coumarin (prenyletin) and 6-methoxy-7-(3'-methylbutyl-2'-en-oxy)-coumarin (prenyletin-methyl-ether). Among the different components of the active extracts, only the mixture of prenyletin and prenyletin-methyl-ether isolated from Pterocaulon polystachyum showed activity against Cryptococcus neoformans, Microsporum gypseum, Trichophyton rubrum and Trichophyton mentagrophytes. Nevertheless their MIC values were higher than the MIC of the original extracts, suggesting that the mixture but not only one compound would be the responsible for the activity detected in these Pterocaulon species.     

Cytotoxic coumarins and lignans from extracts of the northern prickly ash (Zanthoxylum americanum)

Four pyranocoumarins; dipetaline, alloxanthoxyletin, xanthoxyletin and xanthyletin; and two lignans; sesamin and asarinin were isolated from the northern prickly ash, Zanthoxylum americanum. To varying degrees, all inhibited the incorporation of tritiated thymidine into human leukaemia (HL-60) cells. Dipetaline was the most active with an IC(50) of 0.68 ppm, followed by alloxanthoxyletin (1.31 ppm), sesamin (2.71 ppm), asarinin (4.12 ppm), xanthoxyletin (3.48 ppm) and xanthylletin (3.84 ppm).     

Antiinflammatory activity of coumarins from Ligusticum lucidum Mill. subsp. cuneifolium (Guss.) Tammaro (Apiaceae)

Four coumarin derivatives [selidinin 1, (+)-praeruptorin A 2, visnadin 3 and (R)-(+)-7-(2',3'-epoxy-3'-methylbutoxy)-coumarin 4] were isolated from the aerial parts of Ligusticum lucidum Mill. subsp. cuneifolium (Guss.) Tammaro (Apiaceae). This is the first report on the identification of these compounds in the Ligusticum genus. Their topical antiinflammatory activity was evaluated as the inhibition of croton oil-induced ear dermatitis in mice. Each compound (0.3 μmol/cm(2) ) induced a significant oedema reduction and compound 4 exerted an effect similar to that of the equimolar dose of the reference drug indomethacin.     

Vasodilator effect of the extracts and some coumarins from the stem bark of Mammea africana (Guttiferae)

CH(2)Cl(2) fraction obtained from the stem bark of Mammea africana inhibited noradrenaline (NA) or KCl-induced contraction in isolated guinea pig and rat aorta. The vasorelaxant potency of the CH(2)Cl(2) fraction of Mammea africana was diminished by a pre-treatment with Nitro-L-arginine methyl ester (L-NAME), an inhibitor of NO synthase, which was however not affected by indomethacin pre-treatment. These findings indicated that the vasorelaxant effect of Mammea africana may be partially endothelium dependent, mediated by nitric oxide and that vasoactive prostanoids might not be contributing to the vasorelaxation effect. Three bioactive compounds were isolated from this CH(2)Cl(2) fraction and identified as 4-n-propylcoumarins (1) (mammea B/BB), 4-phenylcoumarins (2) (mammea A/AA or mammeisin) and (B/BA) (3) and might involved in the vasorelaxant effect of the extract. The mechanisms of the vasorelaxant effect might therefore be multiple, including endothelium dependence and the mechanisms, which interfere with the liberation of Ca(2+) into the muscle cell.     

香豆素类化合物生物学活性研究进展

综述了近10年来香豆素类化合物有效成分及生物学活性的研究进展。香豆素是自然界很重要的一大类天然有机化合物,实验研究发现香豆素类化合物具有抗HIV、抗癌、降压、抗心律失常、抗骨质疏松、镇痛、平喘及抗菌等多方面生物学活性。因此,完善香豆素类化合物提取分离工艺,寻找有效的先导化合物,合成并筛选出高效低毒的香豆素类衍生物已成为药物研发工作的重要方向之一。     

小剂量~(131)I治疗甲亢215例疗效观察

目的:评价小剂量131I治疗甲状腺功能亢进症(甲亢)的疗效。方法:计算甲状腺吸收剂量,并计算给131I的放射性活度(mC i)。结果:患者在各治疗阶段甲状腺功能得到明显改善,治疗后甲状腺重量有所减少。结论:小剂量131I治疗甲亢的疗效明确。     

晶状体抗氧化能力指数的测定

目的:建立晶状体抗氧化能力指数的测定方法。方法:以D-半乳糖诱导小鼠高血糖模型,采用ORAC法测定小鼠晶状体的抗氧化能力指数,HPLC法测定晶状体内谷胱甘肽及维生素C含量。结果:与正常组相比,D-半乳糖诱导高血糖模型组小鼠晶状体的抗氧化能力指数、谷胱甘肽及维生素C含量均显著性下降。结论:ORAC方法可用于测定晶状体的抗氧化能力指数,其活性与晶状体中谷胱甘肽及维生素C含量相关。     

Insulin sensitizing property of Indigofera mysorensis extract

Indigofera mysorens is a shrub used for its antidiabetic activity in rural India. Here, we elucidate the antidiabetic potential of Indigofera mysorensis extract. Ethanolic extract of the whole shrub of Indigofera (EEI) at 300 mg/kg for 10 days, produced a 63% reduction in plasma glucose, 41% reduction in plasma triglyceride and 77% reduction in plasma insulin levels in insulin resistant db/db mice, which is better than insulin sensitizer, troglitazone (400 mg/kg). EEI unlike sulphonylureas failed to show any acute hypoglycemic effect in normoglycemic Swiss albino mice (SAM). Even in a chronic study (10 days) in SAM, EEI (300 mg/kg) like insulin sensitizers showed no effect on plasma glucose, but an 81% reduction in plasma insulin levels. When challenged with 3 gm/kg sucrose, SAM treated with EEI (300 mg/kg, 7 days) failed to show any effect on the absorption of sugar, whereas standard drug, acarbose (10 mg/kg) showed 52% reduction in the area under the plasma glucose curve. EEI failed to show any significant transactivation of PPARgamma, a proposed target of synthetic insulin sensitizers. Taken together, our data indicate that the antidiabetic effect of the ethanolic extract of Indigofera is due to its insulin sensitizing property and is clearly different from that of sulfonylurea or acarbose.     

沉香的化学成分研究(Ⅰ)

目的研究沉香中2-(2-苯乙基)色酮类成分。方法沉香乙醇提取物的乙醚部位,用硅胶柱色谱,以石油醚、醋酸乙酯不同比例梯度洗脱,分得2个成分,通过理化常数和光谱分析鉴定化合物的结构。结果从沉香乙醇提取物中分得2个色酮类成分,分别鉴定为6,8-二羟基-2-[2-(3′-甲氧基-4′-羟基苯乙基)]色原酮{6,8-dihydroxy-2-[2-(3′-methoxy-4′-hydroxylphenylethyl)]chromone,}和6-甲氧基-2-[2-(3′-甲氧基-4′-羟基苯乙基)]色原酮{6-methoxy-2-[2-(3′-methoxy-4′-hydroxylphenylethyl)]-chromone,}。结论化合物为新化合物,化合物为已知化合物。     

三棱的化学成分研究(Ⅰ)

目的研究黑三棱Sparganium stoloniferum的化学成分。方法用硅胶、Sephadex LH-20柱色谱等方法进行分离纯化,通过理化性质及光谱数据结合化学反应确定化合物的结构。结果分离得到9个化合物,分别鉴定为胡萝卜苷棕榈酸酯(Ⅰ)、β-谷甾醇棕榈酸酯(Ⅱ)、24-亚甲基环阿尔廷醇(Ⅲ)、6,7,10-三羟基-8-十八烯酸(Ⅳ)、香草酸(Ⅴ)、对羟基苯甲醛(Ⅵ)、α-棕榈酸单甘油酯(Ⅶ)、5-羟甲基糠醛(Ⅷ)、β-谷甾醇(Ⅸ)。结论化合物～和～均为首次从该属植物中分离得到。     

香豆素的药理研究进展

香豆素具有抗高血压、抗凝血、抗微生物、抗病毒、抗癌、抗氧化等多种药理活性,备受国内外学者的关注.本文对近十年来国内外有关香豆素的药理作用作一综述.     

通塞脉微丸血清药物化学的初步研究(Ⅰ)

目的 研究通塞脉微丸复方大鼠给药后血清中移行成分的归属.方法 建立通塞脉微丸及大鼠ig通塞脉微丸后血清的HPLC色谱分析方法;比较全方制剂、金银花、当归、甘草、玄参、黄芪和石斛各单方制剂分别给药后所得的血清样品,分析口服通塞脉微丸后大鼠血中移行成分、来源生药及其代谢产物.结果 大鼠ig通塞脉微丸后从血清中发现了15种入血成分,其中10种成分为复方所含成分的原型,其中绿原酸、阿魏酸、甘草素和肉桂酸为已知确定结构的化合物,另外5种成分分别来源于金银花、当归、甘草、玄参和石斛,其具体结构还有待进一步检测分析;1种为复方给药后新产生的代谢物质;3种为给药后产生的未知化合物.结论 血中移行成分及其代谢产物是通塞脉微丸的体内直接作用物质,对其深入研究将有助于阐明复方效应的物质基础.     

秦艽细胞悬浮培养研究(Ⅰ)

目的建立秦艽细胞悬浮培养体系。方法通过小细胞团法优选细胞系并考察不同培养基、细胞种龄、初始pH值、培养温度、摇床转速对秦艽悬浮细胞生长及龙胆苦苷积累的影响。结果适于秦艽细胞悬浮培养条件为:MS培养基为基本培养基,用15d种龄的细胞接种,初始pH7、25℃,110r/min,摇瓶培养。结论通过摇瓶培养建立了良好的秦艽细胞悬浮培养体系。不同培养基对细胞生长及龙胆苦苷积累的显著影响提示某些无机离子有重要的调控作用。     

疏刺茄化学成分研究(Ⅰ)

目的研究疏刺茄Solanum nienkui的化学成分。方法应用硅胶柱色谱、Sephadex LH-20柱色谱、反相柱色谱及重结晶等方法分离纯化,根据理化性质和光谱数据鉴定化合物结构。结果从疏刺茄的三氯甲烷部位分离得到11个化合物,分别鉴定为7,2′,4′-三羟基-5-甲氧基异黄酮(1)、香叶木素(2)、柚皮素(3)、山柰酚(4)、槲皮素(5)、咖啡酸乙酯(6)、原儿茶醛(7)、邻羟基苯甲酸(8)、香草醛(9)、水杨酸甲酯(10)、N-p-香豆酰酪胺(11)。结论所有化合物均为首次从该植物中分离得到,化合物1为首次从茄科植物中分离得到。     

糙苏的化学成分研究(I)

从糙苏Ｐｈｌｏｍｉｓ ｕｍｂｒｏｓａ全草的脂溶性部位共分得１６个化合物,分别鉴定为：１－Ｏ－ｂ－葡萄糖－２－Ｏ－顺－二十碳烯－９－酸－甘油酯（１）,甘油酸甘油三酯（Ⅱ）,齐墩果酸（Ⅲ）,马斯里酸（Ⅳ）,熊果酸（Ⅴ）,２α－羟基－熊果酸（Ⅵ）,３α－羟基０熊果酸（Ⅶ）,β－谷甾醇葡萄糖苷（Ⅷ）,２,６－二聚果糖（Ⅸ）,Ｄ－果糖（Ⅹ）,Ｄ－吡喃葡萄糖（Ⅺ）,豆甾醇（Ⅻ）,β－谷旮醇（Ⅻ）,油酸（０２８     

糙苏的化学成分研究(I)

从糙苏Ｐｈｌｏｍｉｓ ｕｍｂｒｏｓａ全草的脂溶性部位共分得１６个化合物,分别鉴定为： １－Ο－ｂ－葡萄 糖－２－Ｏ－顺－二十碳烯－９－酸－甘油酯（Ｉ）,甘油酸甘油三酯（Ⅱ）,齐墩果酸（Ⅲ）,马斯里酸（Ⅳ）,熊果 酸（Ｖ）,２ａ－羟基－熊果酸（Ⅵ）,３ａ－羟基－熊果酸（Ⅶ）,β－谷甾醇葡萄糖苷（Ⅷ）,２,６－二聚果糖（Ⅹ）,Ｄ－ 果糖（Ⅹ）,Ｄ－吡喃葡萄糖（ⅩⅠ）,豆甾醇（ⅩⅡ）,β－谷甾醇（ⅩⅢ）,油酸（ⅩⅣ）,亚油酸（ⅩⅤ）,月桂酸 （Ⅵ）。其中化合物 Ⅰ、Ⅱ、Ⅲ、Ⅳ、Ⅵ、Ⅶ、Ⅸ、ⅩⅡ系首次从该植物中分得。化合物Ⅰ为一新的天然产 物。它们的结构经波谱分析和化学转化等方法确定。     

Mammea coumarins from the flowers of Mammea siamensis

Four new mammea coumarins, mammea E/BA cyclo D (1), mammea E/BC cyclo D (2), mammea E/BD cyclo D (3), and mammea E/AC cyclo D (4), were isolated from the flowers of Mammea siamensis, along with six known coumarins. Extensive 1D and 2D NMR experiments and other spectroscopic studies, as well as chemical transformations, were employed to determine the structures of 1-4.     

黄花三宝木中香豆素类成分研究

目的对黄花三宝木Trigonostemon lutescens枝叶的95%乙醇提取物中的化学成分进行研究。方法利用硅胶柱色谱、MCI和Sephadex LH-20柱色谱及半制备型高效液相等色谱方法分离纯化,结合理化性质和MS、NMR等波谱学数据对化学结构进行解析。结果从黄花三宝木醋酸乙酯萃取物中发现并鉴定了11个化合物,分别为7个香豆素类:酸橙素烯醇(1)、水合橘皮内酯(2)、花椒毒素(3)、佛手柑内酯(4)、异茴芹内酯(5)、别异欧芹属素乙(6)、异去甲基呋喃羽叶芸香素(7);2个苯丙素糖苷:3,4-dihydroxyallylbenzene-4-O-β-D-glucopyranoside(8)、1-O-β-D-glucopyranosyl-4-allylbenzene(9);1个苯乙醇类:1-(2-ethylphenyl)-1,2-ethanediol(10);1个生物碱类:8-hydroxy-3-methoxy-5H-pyrido [2,1-c] pyrazin-5-one(11)。结论化合物1～11均为首次从三宝木属植物中分离得到。