博落回茎中抗玉米大斑病的生物碱类成分研究

为了解博落回茎中具有抗玉米大斑病的活性成分,采用天然产物分离和活性追踪的方法分离鉴定了8个生物碱类化合物。这8个化合物分别为6-(2-羟基乙基)-5,6-二氢血根碱(1)、6-(2-甲氧基-2-氧代乙基)-5,6-二氢血根碱(2)、6-丙酮基二氢血根碱(3)、6-丙酮基白屈菜红碱(4)、isointegriamide(5)、arnottianamide(6)、二氢血根碱(7)和白屈菜红碱(8)。其中化合物1、2、5、6首次从博落回茎中分离得到。以上生物碱类化合物(1～8)通过滤纸片琼脂糖扩散法对玉米大斑病进行抗菌测试,确定了化合物8具有显著的抗玉米大斑病的生物活性,然后用48孔板测定了化合物8对玉米大斑病孢子萌发实验,其IC_(50)值为12.0μg/mL,以上研究为防治玉米大斑病提供了一种潜在的新型生物农药原料。     

HPLC指纹图谱结合化学计量法对比研究博落回不同器官化学组分CSCD

本研究采用HPLC法分别建立博落回根、叶、果、茎化学指纹图谱,并测定其原阿片碱、别隐品碱、血根碱、白屈菜红碱4种生物碱含量;采用正交偏最小二乘法-判别分析(OPLS-DA)对博落回根、叶、果进行质量评价。指纹图谱结果表明,17批根样品共标定10个共有峰,14批叶样品共标定9个共有峰,14批果样品共标定9个共有峰,10批茎样品共标定6个共有峰。博落回不同器官4种生物碱总含量高低顺序依次为:果>根>叶>茎;果中以上4种生物碱含量均较高,根和叶中原阿片碱、别隐品碱含量高,茎中以上4种生物碱含量均低;博落回根资源量大且原阿片碱、别隐品碱含量高于果和叶,可同博落回果、叶作为以上生物碱提取原料进行开发利用。OPLS-DA结果以VIP>1计,别隐品碱及白屈菜红碱可作为博落回根潜在质量标志物;血根碱、白屈菜红碱可作为博落回叶潜在质量标志物;原阿片碱、别隐品碱、血根碱可作为博落回果的潜在质量标志物。本研究结果为博落回根、叶、果、茎的鉴别评价及博落回根的开发利用提供了研究依据。     

延胡索的化学成分研究(英文)

采用现代分离技术和方法,从延胡索根茎中分离得到17个化合物,通过波谱分析鉴定其结构。包括11个生物碱类化合物,二氢白屈菜红碱(1)、去氢紫堇碱(2)、四氢非洲防己胺(3)、异紫堇球碱(4)、紫堇碱(5)、四氢黄连碱(6)、药根碱(7)、黄连碱(8)、小檗碱(12)、巴马汀(13)和延胡索乙素(14);2个蒽醌类化合物,大黄素(9)和大黄素甲醚(10);1个三萜类化合物,即3β-羟基-齐墩果烷-111,3(18)-二烯-28-酸(11)和3个甾醇类化合物,豆甾醇(15)、β-谷甾醇(16)和胡萝卜苷(17)。其中,化合物9～11首次从该属植物中分离得到,1首次从该种中分离得到。     

小果博落回中2种杀虫活性成分的分离及鉴定

以粘虫(Mythimna separata)3龄幼虫为试虫,采用生物活性示踪法从小果博落回(Macleaya microcarpa)乙醇提取物中分离纯化出2种活性成分,经MS1、H-NMR1、3C-NMR分析鉴定为二氢血根碱和二氢白屈菜红碱。采用小叶碟添加法测试了2种化合物对粘虫3龄幼虫的拒食及毒杀活性。结果表明,2种化合物对粘虫3龄幼虫均具有较高的拒食活性,48 h的拒食AFC50分别为0.168和0.231 mg.mL-1,同时,二氢血根碱对粘虫3龄幼虫具有一定的毒杀活性,96 h的LC50为0.085 mg.mL-1。分析认为二氢血根碱可能是小果博落回的主要杀虫活性成分之一。     

荷叶的化学成分研究

从荷叶(Folium Nelumbinis)的乙醇提取物中分离鉴定出13个化合物,分别为荷叶碱(nuciferine,1),鹅掌楸碱(liriodenine,2),2-羟基-1-甲氧基阿朴啡(2-hydfoxy-1-methoxyaporphine,3),原荷叶碱(pronuciferine,4),去氢莲碱(dehydroroemerine,5),去氢荷叶碱(dehydronuciferine,6),莲碱(roemerine,7),胡萝卜苷(daucosterol,8),β-谷甾醇(β-sitosterol,9),1-二十烷醇(1-icosanol,10),1-十一烷醇(1-undecanol,11),(2R,4S,4aS,8aS)-4,4a-环氧-4,4a-二氢食用西番莲素[(2R,4S,4aS,8aS)-4,4a-epoxy-4,4a-dihydroedulan,12]和邻二羟基苯酚(benzene-1,2-did,13).其中化合物10～13为首次从荷叶中分离得到.     

小果十大功劳化学成分的研究

从小果十大功劳的石油醚层、氯仿层、正丁醇层中分离出9个化合物,利用UV、IR、NMR和MS等现代波谱分析方法,鉴定这9个化合物的结构为:二十九烷-10-醇(1)、亚麻酸甲酯(2)、β-谷甾醇(3)、小檗碱(4)、异汉防已碱甲素(5)、四氢小檗碱(6)、白蓬皱褶碱(7),药根碱(8),1-棕榈酸单甘油酯(9)。所有化合物均为首次从该植物中分离得到。     

藏波罗花化学成分的研究

从藏波罗花95％乙醇提取物分离得到11个化合物,通过理化性质及波谱方法分别鉴定为β-咔啉(1),6,7-二甲氧基-2-萘乙醇(2),6,7-二甲氧基-2-萘乙酸(3),9-hydroxy-δ-skytanthine (4),异角蒿素(5),二丁醇对苯二酯(6),(+)-连翘环乙酮(7),对羟基苯乙(8),cleroindicin D(9),4-甲氧基肉桂酸(10)和β-谷甾醇(11).以上化合物均首次从该植物中分离得到.     

香鳞毛蕨的化学成分研究

本文对香鳞毛蕨水提液进行大孔树脂柱色谱,用水、30%、60%、95%乙醇依次洗脱,从香鳞毛蕨30%乙醇组分中分离得到10个化合物,通过波普数据和理化性质分别鉴定为:5,7二羟基-2-羟甲基色原酮(1)、咖啡酸甲酯(2)、2S-圣草素-7-O-β-D-葡萄糖苷(3)、二氢松柏醇(4)、1,3-二羟基-5-丙基苯(5)、3β-羟基-5α,6α-环氧-7-大柱香波龙烯-9-酮(6)、2-羟基苯甲酸(7)、咖啡酸(8)、对羟基苯乙酮(9)、圣草素(10),以上化合物中4~10为首次从鳞毛蕨属植物中分离得到。     

爆杖花的黄酮类成分研究

爆杖花(Rhododendron spinuliferum)茎叶75%丙酮水提取物采用硅胶柱色谱、Sephadex LH-20色谱、高效液相色谱等技术分离纯化,从其乙酸乙酯部分中共分离和鉴定了6个黄酮类化合物,槲皮素-3-O-[3″,4″-O-(异丙叉基)-β-D-木吡喃糖苷] (1),二氢槲皮素(2),二氢槲皮素-3-O-β-D-木吡喃糖苷(3),5,7,4′-三羟基-二氢黄酮醇-3-O-α-L-鼠李吡喃糖苷(4),二氢槲皮素-3-O-α-L-鼠李吡喃糖苷(5),花青素A-2(6).其中化合物1为新化合物,爆杖花的化学成分为首次报道.     

催吐萝芙木中生物碱的研究

从催吐萝芙木根的乙醇提取物中分离得到15个吲哚生物碱,利用波谱(ESI-MS,1H NMR,13C NMR)等技术分别鉴定为利血平(1),四氢鸭脚木碱(2),异山德维辛碱(3),利血平酸甲酯(4),萝芙木碱(5),山德维辛碱(6),异育亨宾(7),霹雳萝芙木碱(8),α-育亨宾(9),育亨宾(10),催吐萝芙木定(11),四叶萝芙新碱(12),harman(13),mauiensine(14),12-hydroxymauiensine(15)。其中化合物13 ~15是首次从该植物中分离到。     

The Chemical Studies on Corydalis hendersonii Hemsl（ =C. nepalensis Kitamura——

Five alkaloids were isolated from the whole plants of Corydalis hendersonii Hemsl (= C. nepalensis Kitamura) by means of centrifugal TLC method. Alkaloids Cn-20(I) was assigned as a new alkaloid named henderine. Alkaloids Cn-1, Cn-2, Ch-16 and Cn- 19 were identified as β-allocryptopine, protopine, stylopine and Cheilanthifoline, respectively, based on mp. UV. IR. MS and 1H-NMR spectra.     

峨眉翠雀花中生物碱成分的研究

从峨眉翠雀花(Delphinium omeiense)块根中分得12个已知生物碱氨茴酰基牛扁碱(anthranoyllycoctonine)1、牛扁碱(lycoctonine)2、甲基牛扁碱(methyllycaconitine)3、德尔塔生(deltatsine)4、德尔色明甲(delsemine A)5、德尔色明乙(delsemine B)6、delsoline 7、potanine 8、delectine 9、delectinine 10、isodelectine11、kusnesoline 12,除1、2和3外,其余化合物均系首次自该植物中分得.应用光谱学和化学方法鉴定了报告的所有化合物的结构.     

(+)-12alpha-Hydroxysophocarpine, a new quinolizidine alkaloid and related anti-HBV alkaloids from Sophora flavescens

(+)-12alpha-Hydroxysophocarpine (8), a new quinolizidine alkaloid was isolated from the roots of Sophora flavescens, together with 10 known quinolizidine alkaloids, (+)-oxymatrine (1), (+)-matrine (2), (+)-9alpha-hydroxymatrine (3), (+)-allomatrine (4), (+)-oxysophocarpine (5), (-)-sophocarpine (6), (-)-9alpha-hydroxysophocarpine (7), (+)-lehmannine (9), (-)-13,14-dehydrosophoridine (10), and (-)-anagyrine (11). Their structures were elucidated by spectroscopic methods, and the stereochemistry of 8 was confirmed by X-ray analysis. These alkaloids were tested for anti-hepatitis B virus (HBV) activity in vitro, compounds 5, 6, 9, and 10 showed significant anti-HBV activity with inhibitory potency against HBsAg secretion at 48.3-79.3% and that against HBeAg secretion at 24.6-34.6%.     

Indole alkaloids from the leaves of Philippine Alstonia scholaris

The first seco-uleine alkaloids, manilamine (1) (18-hydroxy-19,20-dehydro-7,21-seco-uleine) and N4-methyl angustilobine B (2), were isolated from the (pH 5) alkaloid extract of Philippine Alstonia scholaris leaves together with the known indole alkaloids 19,20-(E)-vallesamine (3), angustilobine B N4-oxide (4), 20(S)-tubotaiwine (5), and 6,7-seco-angustilobine B (6). The structure of the alkaloids was established from MS and NMR experiments.     

Alkaloids from Sri Lankan curry-leaf (Murraya koenigii) display melanogenesis inhibitory activity: Structures of karapinchamines A and B

A methanolic extract and its ethyl acetate-soluble fraction from Sri Lankan curry-leaf, the leaves of Murraya koenigii, inhibited melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. Two new carbazole alkaloids, karapinchamines A and B, were isolated from the ethyl acetate-soluble fraction together with 12 known carbazole alkaloids. The structures of karapinchamines A and B were determined by physicochemical analyses. The principal alkaloid constituents were found to display potent melanogenesis inhibitory activity. The structural requirements of the carbazole alkaloids for melanogenesis inhibitory activity were discussed.     

单面针的生物碱研究

自芸香科(Rutaceae)花椒属植物单面针(Zanthoxylum nitidum var. fastuosum How ex Huang)的根皮中分得五种已知生物碱:乙氧基白屈菜红碱(ethoxychelerythrine)(Ⅰ);氯化光花椒碱(nitidine chloride)(Ⅱ);去甲基白屈菜红碱(des-N-methychelerythrine)(Ⅲ);α—别隐品碱(α-allocryptopine)(Ⅳ);鹅掌揪宁(liriodenine)(Ⅴ).     

Induction of apoptosis by carbazole alkaloids isolated from Murraya koenigii.

In the current study, we isolated 10 carbazole alkaloids from the plant species Murraya koenigii (Rutaceae), and examined their effects on the growth of the human leukemia cell line HL-60. Three carbazole alkaloids, mahanine (6), pyrayafoline-D (7) and murrafoline-I (9), showed significant cytotoxicity against HL-60 cells. Fluorescence microscopy with Hoechst 33342 staining revealed that the percentage of apoptotic cells with fragmented nuclei and condensed chromatin was increased in a time-dependent manner after treatment with each alkaloid. Interestingly, each carbazole alkaloid induced the loss of mitochondrial membrane potential. In addition, both caspase-9 and caspase-3 were also time-dependently activated upon treatment with the alkaloids. Caspase-9 and caspase-3 inhibitors suppressed apoptosis induced by these alkaloids. The results suggest that these three alkaloids induced apoptosis in HL-60 cells through activation of the caspase-9/caspase-3 pathway, through mitochondrial dysfunction.     

急尖绣线菊中一微量新二萜生物碱

从蔷薇科绣线菊属植物急尖绣线菊（Ｓｐｉｒａｅａ ｊａｐｏｎｉｃａ ｖａｒ．ａｃｕｔａ Ｙｕ）的根部分离得到６个二萜生物碱,经光谱分析,其中５个来ｓｐｉｒａｍｉｎｅｓ Ａ（１）,Ｂ（２）,Ｐ（３）和Ｕ（４）及ｓｐｉｒａｄｉｎｅ Ｆ（５）,另一微量成分被鉴定为一新的二萜生物碱,命名为ｓｐｉｒａｍｉｎｅ Ｗ（６）。     

Nuphar alkaloids with immediately apoptosis-inducing activity from Nuphar pumilum and their structural requirements for the activity

The methanolic extract and its alkaloid fraction from the rhizomes of Nuphar pumilum showed cytotoxic effects on human leukemia cell (U937), mouse melanoma cell (B16F10), and human fibroblast (HT1080). Dimeric sesquiterpene thioalkaloids with the 6-hydroxyl group (6-hydroxythiobinupharidine, 6,6'-dihydroxythiobinupharidine, 6-hydroxythionuphlutine B) showed substantial cytotoxic activity at a concentration of 10 microM, but dimeric sesquiterpene thioalkaloids lacking the 6-hydroxyl group (thiobinupharidine, thionuphlutine B, 6'-hydroxythionuphlutine B, neothiobinupharidine, thionuphlutine B beta-sulfoxide, and neothiobinupharidine beta-sulfoxide) and monomeric sesquiterpene alkaloids (nupharidine, 7-epideoxynupharidine, and nupharolutine) showed weak activity. Next, apoptosis-inducing activity of a principal active constituent, 6-hydroxythiobinupharidine, on U937 was examined using morphological observation and DNA fragmentation assay (TUNEL method). Apoptosis of U937 was immediately observed within 1 h after treatment of 6-hydroxythiobinupharidine at 2.5-10 microM.     

Insecticidal and antifeedant effects of two alkaloids from Cynanchum komarovii against larvae of Plutella xylostella L

A bioassay‐guided fractionation of Cynanchum komarovii crude alkaloid extract led to the isolation of two alkaloids. The isolated alkaloids were identified as 7‐demethoxytylophorine (1) and 6‐hydroxyl‐2,3‐dimethoxy phenanthroindolizidine (2) based on the comparison of their spectroscopic characteristics with the literature data. Insecticidal, antifeedant and growth inhibitory effects of these two alkaloids against the 3rd instar larvae of Plutella xylostella L. (Lepidoptera: Plutellidae) were examined. The results showed that alkaloid 1 was more toxic than alkaloid 2 against the 3rd instar larvae of Plutella xylostella L., but both alkaloids were less toxic than the total alkaloid fraction. For antifeedant activity, alkaloid 1 showed AFC₅₀ of 1.82 mg/ml at 24 h after treatment, alkaloid 2 showed 3.89 mg/ml, while total alkaloids showed 1.56 mg/ml. In dipping toxicity test, alkaloids 1 and 2 produced 93.3% and 63.3% mortality at 72 h after treatment, respectively, while total alkaloids produced 96.7% mortality. The LC₅₀ values for alkaloids 1, 2 and the total alkaloids were 3.54, 9.21 and 2.63 mg/ml, respectively. The development of larvae was also inhibited, and the growth inhibition rates at the concentration of 15.00 mg/ml were 92.8%, 78.2% and 98.6% for alkaloids 1, 2 and total alkaloids, respectively, at 72 h after treatment. Compared with antifeedant and dipping effect, the alkaloids 1, 2 and total alkaloid fraction revealed weak feeding toxicity, and their corrected mortality rates at the concentration of 15.00 mg/ml were 60.0%, 40.0% and 63.3% at 7 days after treatment. The LC₅₀ values for alkaloids 1, 2 and total alkaloids were 12.58, 32.37 and 8.88 mg/ml, respectively, at 7 days after treatment.