C20型二萜生物碱的构效关系研究进展

C20型二萜生物碱是一类结构复杂、活性多样的化合物,它们的结构和活性之间有着密切的关系.本文综述了C20型二萜生物碱的结构特征与活性间的构效关系,为结构修饰提供依据以更快得到高效低毒的化合物.     

内酯型去甲二萜生物碱的合成

目的合成内酯型去甲二萜生物碱。方法塔拉萨敏经Jone’s氧化和Baeyer-V illiger氧化反应,合成了两种内酯型去甲二萜生物碱。单乙酰塔拉萨敏裂解C7-C17键后,经水解、Jone’s氧化、Baeyer-V illiger氧化及还原等共5步反应,合成了7,17-次裂的内酯型去甲二萜生物碱。结果和讨论所得产物的结构经MS1、HNMR和13CNMR确证。     

宣威乌头中生物碱成分的研究

目的 研究宣威乌头Aconitum nagarumvar lasiandrum中的生物碱成分.方法 采用酸提碱沉法提取总碱、硅胶层析法分离,用波谱法鉴定结构.结果和结论 从宣威乌头中分得10个单体化合物,应用光谱法鉴定了其结构为:光翠雀碱(denudatine)、宋果灵(songorine)、delnuttaline等3个C20-二萜生物碱和尼奥灵(neoline)、3-去氧乌头碱(3-deoxyaconitine)、8-methoxy-14-benzoylaconine、伏乌碱(flavaconitine)、异塔拉萨敏(isotalatizidine)、乌头碱(aconitine)和nevadensine等7个C19-二萜生物碱.     

高乌头的化学成分及药理作用研究进展

目的总结高乌头的化学成分和药理作用,为高乌头的进一步开发和利用提供参考。方法通过查阅国内外相关文献并进行归纳、分析,对高乌头的化学成分和药理作用等进行综述。结果高乌头的主要成分为生物碱类,包括C_(18)-型二萜生物碱、C_(19)-型二萜生物碱和C_(20)-型二萜生物碱等。现代药理研究表明,高乌头具有镇痛、局部麻醉、抗心律失常、抗炎及抗肿瘤等多种生物活性。结论高乌头的现代研究取得了一定的进展,但研究深度仍不够,需要进一步探讨。     

印度乌头中两个新的二萜生物碱成分

乌头Aconitum palmatum Don. 恨在印度作为一种民间草药已经使用许多年了。据报道,早自1965年印度人就从该植物中分离出5个二萜生物碱:vakognavine, palmasine,vakatisine, vakatisinine和vakatidine。作者多年来一直从事乌头二萜生物碱成分的研究,曾从印度乌头中分离出8种二萜生物碱。本文报道了2个新的二萜生物碱vakhmatine(1)和vaknmadine(2)以及2个已知生物碱阿替新atisine和hetisine。这2个新的生物碱均在C_(19)与C_(20)之间有一种胺桥,并且由C_8、C_9、C_(11)、C_(12)、C_(13)和C_(14)形成船式构型,C_(11)和C_(13)上的羟基均为α-型,这些与早期报道的结构有所不同。乌头乙醇提取物经常规pH梯度萃取分     

C20型二萜生物碱的药理活性研究进展

c20型二萜生物碱是一类结构复杂、活性多样的化合物,一直以来为化学家和药理学家所重视,近十年来,有关发现其新药理活性的报道不断涌现。综述c20型二萜生物碱药理活性的研究情况。     

圆滑番荔枝的化学成分研究

目的从番荔枝科植物圆滑番荔枝(annona glabra linn)树皮中分离其化学成分并进行成分分析.方法采用柱层析和红外、核磁共振、质谱仪等进行结构分析.结果分离到6个化合物,其中5个为贝壳杉烷型二萜,1个为生物碱.根据理化性质和波谱特征鉴定其为萜Ⅰ、Ⅱ分别为ent-19-carbomethoxykauran-17-oic acid、19-hydroxy-16α-(-)-kauran-17-oic acid,生物碱Ⅰ、Ⅱ分别为liriodenine、oxoglaucine.结论其中萜Ⅰ ent-19-carbomethoxykauran-17-oic acid、萜Ⅱ19-hydroxy-16α-(一)-kauran-17-oic acid和生物碱Ⅱoxoglaucine为首次从该植物中分得.     

紫乌头生物碱的化学研究

从紫乌头根中分出四种新二萜生物碱,分别命名为紫乌生、紫乌生宁、紫乌亭和紫乌定。根据红外光谱、紫外光谱、质谱、氢谱和碳谱以及制备衍生物,证明了前三个生物碱的结构(3,4,5),对紫乌定的结构曾初步推定为(8)⁽¹⁾;后来,经单晶X射线衍射结构分析修正为(9)。此外,作者认为,根据化学结构特点应从C₁₉二萜生物碱中划分出C-4失甲基的一类生物碱,称C₁₈二萜生物碱。     

草乌花及其煎煮液中二萜生物碱的电喷雾串联质谱研究

目的对草乌花及其煎煮液中的二萜生物碱进行定性分析,说明煎煮前后化学成分发生的变化. 方法用注射泵自动进样,电喷雾离子阱串联质谱直接分析草乌花及其煎煮液中生物碱混合物.结果在生草乌花中发现3个新生物碱,草乌花煎煮后其中的双酯型生物碱和三酯型生物碱都发生水解,前者水解为苯甲酰乌头原碱和乌头原碱类生物碱,后者水解为3-乙酰-乌头原碱类生物碱.结论该法简便、快速、灵敏、特异性强,为乌头属植物煎煮液中的生物碱分析提供了新途径.     

中药附子的研究进展

目的探讨附子的药效物质基础,为附子的进一步开发和利用提供参考。方法通过查阅国内外相关文献,进行归纳、分析,对附子的化学成分、生物活性及质量控制进行综述。结果附子的主要成分为生物碱类,其中以乌头碱骨架的C-19型二萜生物碱为主,其次为C-20型二萜生物碱,以海替生碱型、维替碱型、纳哌啉型、光翠雀碱型骨架类型为主;除生物碱外,还含有黄酮、皂苷、神经酰胺类等成分。附子的生物活性主要包括强心、抗肿瘤、抗炎镇痛、增强免疫、抗衰老等作用。附子药材质量控制方法包括高效液相色谱(HPLC)指纹图谱研究及主要成分的含量测定研究。结论附子的现代研究取得了一定进展,但在阐明其传统药效作用及机制方面仍存在一些问题,需要进一步深入探讨。     

直缘乌头根中生物碱成分的研究

目的：研究直缘乌头（Aconitum transsectum Diels.）根中的生物碱成分。方法：采用pH梯度、中压柱层析、常压硅胶柱层析及离心薄层层析法。结果：分得11个已知二萜生物碱，由光谱法分别鉴定为：滇乌碱（yunaconitine）、印乌碱（indaconitine）、黄草乌碱甲（vilmorrianine A）、黄草乌碱丙（vilmorrianine C）、草乌甲素(crassialine A)、膝乌碱（geniconitine）、查斯曼宁（chasmanine）、８－去乙酰滇乌碱（8-deacetylyunaconitine）、塔拉萨敏（talatisamine）、14-乙酰塔拉萨敏（14-acetyltalatisamine）和chasmaconitine。结论：黄草乌碱甲和chasmaconitine是首次从该植物中分离得到。     

Diterpenoid alkaloids from the aerial parts of Aconitum anthora L

Isolation and identification of six diterpenoid alkaloids, from Aconitum anthora L. are described. All proton detected 2D NMR techniques have been used for unambiguous 1H and 13C chemical shift assignments of guan-fu-base-Y (6). This is the first investigation of the diterpenoid alkaloids of this plant species.     

Diterpenoid alkaloids from the roots of Aconitum cochleare

From the roots of Aconitum cochleare Woroschin, collected in Turkey, a new diterpenoid alkaloid named acochlearine has been isolated along with the known diterpenoid alkaloids talatisamine, 14-O-acetyltalatisamine, senbusine C and condelphine. The structure for acochlearine was established on the basis of 1H, 13C, DEPT, homonuclear 1H COSY, NOESY, HSQC and HMBC NMR studies.     

In vitro activity of C20-diterpenoid alkaloid derivatives in promastigotes and intracellular amastigotes of Leishmania infantum

The in vitro anti-proliferative effects are described of several atisine-type diterpenoid alkaloids against the protozoan parasite Leishmania infantum, which causes human visceral leishmaniasis and canine leishmaniasis in the Mediterranean basin, as well as human cutaneous leishmaniasis throughout the Mediterranean region. From a total of 43 compounds tested, including C19- and C20-diterpene alkaloids from several chemical classes, only 15,22-O-diacetyl-19-oxo-dihydroatisine, azitine and isoazitine were highly active against cultures of the parasite (promastigote form) with IC50 values within the range of the reference drug pentamidine-isothionate (7.39-12.80 mg/L for the test compounds, 11.32 mg/L for the positive control). These compounds were not toxic to the host cell. When treated with a dosage of 5 microg/mL of the active compounds (half of their IC50), the promastigote forms lost 80% of their infection capacity and the multiplication of extracellular forms of L. infantum was severely affected. The study showed that atisine-type C20-diterpenoid alkaloids exhibited promising anti-leishmanial properties with strong molecular selectivity. These might have implications for other intracellular pathogens- or phylogenetically related parasites, such as Trypanosoma spp.     

不同品种附子生物碱和多糖含量的比较

目的:比较不同品种附子生物碱和多糖的含量。方法:采用酸性染料比色法测定附子总生物碱含量,反相高效液相色谱法测定双酯型生物碱含量,蒽酮-硫酸法测定多糖含量。结果:不同品种附子总生物碱和双酯型生物碱含量差异较大,附子多糖含量差异不显著。附子炮制后,黑附片中总生物碱、双酯型生物碱含量显著下降,附子多糖含量稍有增加。结论:本试验结果可为附子品种选育提供一定的科学依据。     

Two new diterpenoid alkaloids, beiwusines A and B, from Aconitum kusnezoffii

Two new atisine-type diterpenoid alkaloids, beiwusine A (1) and B (2), have been isolated from the roots of Aconitum kusnezoffii Reichb. Their structures were established on the basis of spectroscopic data. Beiwusines A and B are the first examples of atisine-type diterpenoid alkaloids having a hydroxyl group at C-1. In addition, one known diterpenoid alkaloid spiramine H (3) has been isolated.     

Diterpenoid alkaloid derivatives as potential chemotherapeutic agents in American trypanosomiasis

The use of natural products for the treatment of protozoal infections (Leishmania and Trypanosoma spp.) is well known and has been documented since ancient times. We have already established an in vitro culture system using mammalian host cells (Vero) infected with Trypanosoma cruzi in which the time course of parasite growth is determined quantitatively. This system was used to screen anti-T. cruzi agents using two experimental models: simultaneous cell infection and compound addition or preincubation of the parasite with the test compound prior to cell infection. Among 64 diterpenoid alkaloids tested, including C19 and C20 skeletons, five C20 compounds were active on T. cruzi epimastigotes: azitine, isoazitine and 15,22-O-diacetyl-19-oxodihydroatisine had moderate effects on the parasite, while atisinium chloride and 13-oxocardiopetamine were potent T. cruzi epimastigote growth inhibitors with activity levels similar to that of benznidazole, used as the reference drug. Additionally, these compounds decreased the ability of metacyclic forms to invade mammalian cells, their intracellular replications and their transformation into trypomastigotes, with no toxicity to the host cell. These results suggest that these alkaloids are structural leads of clinically active compounds against T. cruzi and probably other members of the Trypanosomatidae.     

Willipelletierine,a new diterpenoid alkaloid from Consolida scleroclada (Boiss.) Schrod

From the aerial parts of Consolida scleroclada (Boiss.) Schrod. collected in Turkey, a new diterpenoid alkaloid named willipelletierine has been isolated along with the known diterpenoid alkaloids aconitine, lapaconidine, and delcosine. The structure for willipelletierine was established on the basis 1H, 13C, DEPT, homonuclear 1H COSY, HETCOR and NOESY NMR studies.