瓜馥木枝叶中生物碱类化学成分研究

采用硅胶柱色谱、ODS柱色谱、Sephadex LH-20柱色谱及半制备HPLC等色谱方法对番荔枝科瓜馥木属植物瓜馥木Fissistigma oldhamii中生物碱类化学成分进行了系统的分离与纯化,运用理化分析及NMR、MS等现代波谱学方法对其结构进行鉴定。从瓜馥木枝叶的总生物碱提取物中共分离得到14个生物碱类化合物,分别鉴定为:去甲头花千金藤二酮(1)、巴婆碱(2)、毛叶含笑碱(3)、六驳碱(4)、异紫堇定碱(5)、番荔枝叶碱(6)、甲氧番荔枝碱(7)、N-methylbuxifoline(8)、aristolactam AIIIa(9)、piperumbellactam A(10)、goniopedaline(11)、aristolactam BIII(12)、鹅掌揪碱(13)和salutaridine(14)。其中化合物3~5,8,10,11和14为首次从瓜馥木属植物中分离得到。     

陵水暗罗枝、叶中的阿朴菲生物碱

目的:对陵水暗罗Polyalthia nemoralis枝、叶中的阿朴菲生物碱进行分离和鉴定,并测细胞毒活性.方法:采用硅胶和凝胶柱色谱方法进行分离纯化,利用波谱数据和理化常数鉴定化合物的结构;MTT法测试细胞毒活性.结果:从乙醇提取物中分离鉴定了5个阿朴菲生物碱,分别为bidebiline A(1),annobrajne(2),lanuginosine(3),鹅掌楸碱(liriodenine,4),oxostephanosine(5).结论:化合物2,5为首次从该属中分到,1,3,4为首次从该植物中分离得到;化合物3～5对多种癌细胞生长有抑制作用.     

陵水暗罗枝、叶中的阿朴菲生物碱

目的：对陵水暗罗Polyalthia nemoralis枝、叶中的阿朴菲生物碱进行分离和鉴定,并测细胞毒活性。方法：采用硅胶和凝胶柱色谱方法进行分离纯化,利用波谱数据和理化常数鉴定化合物的结构;MTT法测试细胞毒活性。结果：从乙醇提取物中分离鉴定了5个阿朴菲生物碱,分别为是bidebiline A(1),annobraine(2),lanuginosine(3),鹅掌楸碱(liriodenine,4),oxostephanosine(5)。结论：化合物2,5为首次从该属中分到,1,3,4首次从该植物中分离得到;化合物3～5对多种癌细胞生长有抑制作用。     

瓜馥木化学成分的研究（Ⅲ）

目的:研究瓜馥木的化学成分。方法:采用硅胶柱色谱技术进行分离纯化,运用波谱法进行了结构解析,并进行了体外细胞毒活性评价。结果:从瓜馥木根的乙醇提取物中分离得到5个化合物,经理化常数和波谱(EI-MS、1H-NMR、13C-NMR)分析,鉴定为马兜铃内酰胺AⅡ(Ⅰ)、马兜铃内酰胺BⅡ(Ⅱ)、大黄素甲醚(Ⅲ)、β-谷甾醇(Ⅳ)及豆甾烷-7-酮(Ⅴ);化合物Ⅰ对肺腺癌GLC-82及HL60白血病细胞株均具有细胞毒作用。结论:化合物Ⅲ～Ⅴ为首次从瓜馥木植物中分离得到,化合物Ⅰ对肺腺癌GLC-82、白血病细胞株HL60的细胞株的IC50分别为:234.45、101.17μM。     

华南木姜子的阿朴菲型生物碱成分

通过MCI树脂、Sephadex LH-20和反相HPLC等多种色谱分离方法相结合,从华南木姜子乙醇提取中的水溶性部位中分离得到6个阿朴菲型生物碱,经MS和NMR等波谱技术分别鉴定为2,9-二羟基-1,10-二甲氧基-4,5-二氢-7酮-阿朴菲碱(1),樟苍碱(2),N-甲基樟苍碱(3),异南天竹种碱(4),异紫堇定碱(5),去甲异紫堇定碱(6)。化合物 1 为一新化合物。化合物2~6均为首次从该植物中分离得到。     

瓜馥木的化学成分研究(Ⅱ)

瓜馥木F issistigm a oldham ii(H em sl.)M err.为番荔枝科瓜馥木属植物,根入药,性温味辛,具有祛风除湿、镇痛消肿、活血化瘀等功效,主要用于跌打损伤、关节炎及坐骨神经痛的治疗[1]。为寻找反映瓜馥木中抗炎、镇痛活性特征成分,笔者对瓜馥木化学成分进行了系统研究。前文[2]已报道N-甲基-2,3,6-三甲氧基吗啡烷二烯酮(N-m ethy l-trim ethoxym orph inand ien-7-one),本研究从其根的乙醇提取物中分得4个化合物,经理化常数和波谱分析,鉴定为O-甲基芒籽碱(O-m ethy l-m oschtao line,Ⅰ)、酸花木碱(毛叶含笑碱,oxy lop-ine,Ⅱ)、氧代克斑…     

瓜馥木化学成分的研究(简报)

<正> 瓜馥木Fissistigma oldhamii(番荔枝科)为治疗关节炎的一种民间草药,具有驱风祛湿、镇痛消肿、活血化瘀等功效。江西中医学院进行了瓜馥木抗关节炎的研究,动物实验发现瓜馥木有心血管生物活性和抑瘤作用。本文简介从瓜馥木酒精提取物中分离得到六种化合物,即A-Ⅰ和A-Ⅱ两个有机酸,以及B-Ⅰ、B-Ⅱ、B-Ⅲ和B-Ⅳ4个生物碱,其中3个生物碱为新生物碱。A-Ⅰ为白色针状结晶,熔点206～     

假鹰爪枝中新的氧化阿朴菲生物碱

目的：研究假鹰爪枝的化学成分。方法：采用硅胶柱层析及Sephadex LH-20等色谱技术分离和纯化化合物，根据理化性质及近代波谱学方法法鉴定结构。结果：从假鹰爪枝的氯仿萃取部分分离得到5个化合物，其中两个氧化阿朴菲生物碱为3，9，11-三甲氧基-1，2-亚甲二氧基氧化阿朴菲(3，9，11-trinethoxy-1，2-methylenedioxyl oxoaporphine，1)，oxoanolobin(2)，两个黄酮类化合物分别为荠芋黄酮(mosloflavone，3)，黄芩素-7-甲醚(negletein，4)，一个甾醇为β-谷甾醇(β-sitosterol，5)。结论：化合物1为新化合物，化合物2在该属植物中首次发现。     

德钦乌头中的二萜生物碱

目的 研究乌头属植物德钦乌头Aconitum ouvrardianum根的二萜生物碱类化学成分.方法 采用反复硅胶柱色谱进行分离纯化,根据谱学数据和对照TLC分析鉴定化合物的结构.结果 从德钦乌头根的醋酸乙酯提取物中分离得到12个化合物,分别鉴定为塔拉乌头胺(1)、彭乌碱乙(2)、卡马考宁(3)、黄草乌碱亭(4)、粗茎乌头碱甲(5)、贡乌生(6)、14-乙酰黄草乌碱亭(7)、展花乌头碱(8)、黄乌宁(9)、膝乌亭丁(10)、异塔拉乌头定(11)、翠雀它灵(12).结论 12个化合物均为C-3位或C-6位无含氧取代的C19-二萜生物碱,且均为首次从该植物中分离得到.乌头碱型C19-二萜生物碱为德钦乌头药材的主要药用化学成分.     

延胡索中的生物碱成分

目的:研究延胡索Corydalis yanhusuo块茎60%乙醇提取物的生物碱成分.方法:采用多种色谱学方法进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构.结果:从延胡索块茎60%乙醇提取物的氯仿可溶部分分离得到9个生物碱,分别鉴定为7-醛基脱氢海罂粟碱(1),O-甲基南天竹碱(2),(+)-O-甲基球紫堇碱(3),d-紫堇碱(4),四氢黄连碱(5),8-氧黄连碱(6),巴马亭(7),四氢巴马亭(8)和去氢紫堇碱(9).结论:化合物1为首次从生物样品中获得,首次报道了其核磁数据,化合物3为首次从罂粟科植物中分离得到,化合物6为首次从该植物中分离得到.     

瓜馥木化学成分的研究

从中药瓜馥木Fissistigma oldhamii (Hemsl.)Merr.根茎甲醇提取物的碱性部分分得一种非酚性生物碱,命名为瓜馥木甲素,经理化常数及UV、IR、MS、^1HNMR、^13CNMR和^13C-^1HCOSY波谱分析鉴定为N－甲基－2,3,6－三甲氧基吗啡烷二烯酮。吗啡烷二烯酮（Morphinandienone)类型的生物碱多具有较强的生理活性。该生物碱系首次从中国大陆产瓜馥木属植物中分得。     

Anti-inflammatory effects of Z23 on LPS-induced inflammatory responses in RAW264.7 macrophages

Aim of the study

Fissistigma oldhamii (Hemsl.) Merr, a traditional Chinese herb medicine, is used for treating rheumatoid arthritis in China. In our previous study, an effective compound, 7′-(3′,4′-dihydroxyphenyl)-N-[(4-methoxyphenyl) ethyl] propenamide (Z23), from this herb has showed potent immunosuppressive effects both in vitro and in vivo. However, its anti-inflammatory effect and mechanism is still need to explore.

Materials and methods

We examined the in vitro effects of Z23 on the production of nitric oxide (NO), prostaglandin E2 (PGE2) and cytokines by lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages.

Results

Z23 significantly decreased the production of PGE2, NO, tumour necrosis factor alpha (TNFalpha) and IL6 production. Inducible nitric oxide synthase (iNOS) and cyclooxygenase2 (COX2) gene expression were also significantly reduced.

Conclusions

These results demonstrated that Z23 exerted an anti-inflammatory effect through modulating the synthesis of several mediators and cytokines involved in the inflammatory process. This study provided evidence to understand the therapeutic effects of Fissistigma oldhamii (Hemsl.) Merr and indicated that Z23 has the potential for treatment of various inflammatory diseases where the overproduction of NO, PGE2 and inflammatory cytokines has been shown to play a role, e.g. rheumatoid arthritis.     

Aristolactams and dioxoaporphines from Fissistigma balansae and Fissistigma oldhamii

Investigation of extracts of Fissistigma balansae and Fissistigma oldhamii resulted in the isolation of 11 aristolactams-stigmalactam (1), piperolactam A (2), piperolactam C (3), aristolactam AII (4), aristolactam AIIIa (5), aristolactam BII (6), aristolactam BIII (7), aristolactam FII (8), goniothalactam (9), enterocarpam I (10), and velutinam (11)-as well as two dioxoaporphines, noraristolodione (12) and norcepharadione B (13). The new compound 1 was identified by spectral data interpretation. Compounds 1-13 were subjected to antiplatelet aggregation testing.     

Antinociceptive and free radical scavenging activities of alkaloids isolated from Lindera angustifolia Chen

Lindera angustifolia Chen is a folk medicine used for the treatment of contusions-induced swelling, rheumatic pains and bellyache in south and the middle part of China. Phytochemical studies showed that aporphine and benzyltetrahydroisoquinoline alkaloids are the characteristic constituents of this plant. In this study, we evaluated the antinociceptive and free radical scavenging properties of six aporphine and two benzyltetrahydroisoquinoline alkaloids isolated from the root of Lindera angustifolia. All alkaloids except magnocurarine exhibited remarkable radical scavenging effects (36-90% scavenging at 25-100microg/ml) in DPPH radical scavenging test, among them norisocorydine showed the hightest activity (SC(50): 14.1microg/ml). Antinociceptive activities were tested by using acetic acid-induced writhing and formalin test at dose of 20mg/kg. Norisocorydine exhibited the highest antinociceptive ability with 83.5% writhing inhibition. Boldine, norboldine showed significant antinociceptive activity with 76.3% and 74.6% writhing inhibition respectively. Indomethacin was used as positive control, which showed 67.8% writhing inhibition at dose of 10mg/kg. Most of the compounds, except N-ethoxycarbonyllaurotetanine and magnocurarine, could significantly inhibit the phase I reaction (P<0.01), and all of them inhibited the phase II reaction (P<0.001) in the formalin tests (indomethacin and morphine were used as positive drugs). The antinociceptive effects exhibited a structure-activity relationship similar to that of the free radical scavenging activities. Above results suggested that the alkaloids from the root of Lindera angustifolia possess both free radical scavenging and antinociceptive activities, and the antinociceptive activity seems to be related to the free radical scavenging effect.     

阿朴菲类生物碱研究进展

阿朴菲类生物碱是异喹啉类生物碱中的一类,具有广泛的生理学活性,目前这类天然产物及其衍生物是发现治疗多种疾病药物的先导化合物和研究热点。通过对国内外文献调研,从自然界植物资源分布、生源合成途径、天然有机合成方法、药理活性等方面的研究进展进行综述,为阿朴菲类生物碱的进一步研究和深层次开发提供参考依据。     

乌骨藤辨考

目的：弄清中药乌骨藤的基原。方法：查阅文献并整理考证。结果：乌骨藤存在严重的同名异物现象,文献记载作乌骨藤用的有通光散Marsdenia tenacissima及白叶瓜馥木Fissistigma glaucescens等多种,而药用记载最早见于《滇南本草》,历代诸家对乌骨藤的功效看法一致。结论：乌骨藤应为萝藦科植物通光散Marsdenia tenacissima。     

瓜馥木总黄酮提取纯化及其清除自由基活性研究

目的:研究瓜馥木总黄酮最佳提取工艺,并将总黄酮进行富集纯化,测试其清除自由基活性。方法:采用正交实验,考察乙醇浓度、提取温度、固液比及提取时间4个因素对该工艺的影响;利用AB-8大孔吸附树脂分离纯化总黄酮粗品;采用清除DPPH自由基初步评价瓜馥木提取物及总黄酮的抗氧化能力。结果:确立了瓜馥木总黄酮的最佳提取工艺为:提取时间3 h,乙醇浓度90%,固液比1∶10,提取温度为70℃。黄酮粗品经AB-8大孔树脂纯化以后,含量可达到55%以上。结论:优选出的最佳提取工艺条件及纯化总黄酮的方法对进一步的工艺开发有较好的参考价值,瓜馥木富集纯化的总黄酮部位具有较强的清除自由基能力,为开发成为中药保健品提供了一定的依据。     

Four dimeric aporphine-containing alkaloids from Thalictrum fauriei.

Four dimeric alkaloids (1-4) containing an aporphine unit and representing unique structural features were obtained from Thalictrum fauriei and were characterized by spectral and chemical methods. Fauripavine (1), with a munitagine pavine unit, is the first such dimer with an aporphine C-1 diphenyl ether connection; although fauridine (2), also the first of its class, has codamine, a benzyl tetrahydroisoquinoline, linked at the same position. Faurithaline (3) and its 3-methoxy analogue 4, both with reticuline, a benzyl tetrahydroisoquinoline as the second unit, are the first dimers with the diphenyl ether linkage at C-8 of an aporphine oxygenated at C-10 and C-11. Oconovine (8) was converted to 8-hydroxy-O-methyloconovine (12) to determine the effect of oxygenation at C-8 on the proton chemical shift of the C-7 hydrogens in a study to support the C-8 ether linkage of alkaloids 3 and 4. All the alkaloids have the S-configuration at their asymmetric centers as established from their CD spectra when compared with those of model compounds.     

乌骨藤常见混用品种辨析

目的　纠正中药乌骨藤的常见混用现象。方法　查阅文献并整理考证。结果　乌骨藤存在严重的同名异物现象 ,文献记载作乌骨藤用的有通光散及白叶瓜馥木等 10数种。结论　正品乌骨藤应为萝　艹摩 科植物通光散