Chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb.

In the present study,we aimed to investigate the chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb. The isolation and purification of components were achieved by a series of chromatography, including silica gel, Sephadex LH-20 and HPLC. By using spectroscopic analysis, their structures were identified. Using PDE-4A as analgesic target, moleculardocking was conducted between isolated compounds by using Schrodinger software. Neoline is a typical non-ester diterpene alkaloid. It was studied by using the mouse torsion body method and hot plate method. A total of 12 diterpene alkaloids were obtainedand identified as Mesaconitine(1), Bewutine (2), Bewudine (3), Songoramine (4), Songorine (5), Neoline (6), Talasamine (7), isotalatizidine (8), Hokbusine A (9), Mesaconine (10), 8-OEt-14-benzoylmesaconine (11), 8-Methoxy-14-benzoyl-beiwutinine (12).Compounds 9 and 12 were isolated from Aconitum kusnezoffii Reichb. for the first time. Twelve diterpenealkaloids could act on the analgesic target. Neoline is a typical non-ester diterpene alkaloid. It had significant analgesic effect. Diterpene alkaloids were the main components of Aconitum kusnezoffiiReichb., and they had good analgesic activity.     

Diterpene Alkaloids of Aconitum kirinense Nakai I.Lepe-nine and Kirinine A

从毛茛科乌头属植物吉林乌头（ＡｃｏｎｉｔｕｍｋｉｒｉｎｉｎｅＮａｋａｉ）中分得两个Ｃ２０二萜生物碱ｌｅｐｅｎｉｎｅ（雷乌宁）和ｋｉｒｉｎｉｎｅＡ（吉乌碱甲），用化学和波谱方法鉴定了它们的结构，其中后者为新化合物。     

Three new diterpene alkaloids from the roots of Aconitum nagarum var. lasiandrum

Three new diterpene alkaloids, 16,17-dihydro-12 beta,16 beta-epoxynapelline (1), N-deethyl- N-methyl-12-epi-napelline (2) and 11- epi-16 alpha,17-dihydroxylepenine (3), along with twenty-six known alkaloids (4 - 29) were isolated from the roots of Aconitum nagarum var. lasiandrum. The chemical structures of the new compounds were established by HR-MS as well as 1D- and 2D-NMR spectroscopic analysis. The absolute stereochemistry of 1 was confirmed by X-ray crystallography.     

Alkaloidal constituents fromAconitum jaluense

Aconitum jaluense Komar. (Ranunculaceae) is one of the Aconitum plants growing in Korean peninsula. An investigation of the alkaloidal constituents of this species led to the isolation of seven C19-norditerpenoid and a C20-diterpenoid alkaloid. Three of them have been identified as neoline, mesaconitine, and hypaconitine, which were isolated from this plant collected from Mt. Bultasan in the north part. The other five alkaloids were determined as lipomesaconitine, lipohypaconitine, 15alpha-hydroxyneoline, hokbusine A, and napelline, which have not been found in this plant. Structures of those alkaloids were determined on the basis of their spectral data. It is of interest to note that a comparison of the present work and the previous report showed some differences in the alkaloidal contents.     

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。     

New diterpene polyesters isolated from Hungarian Euphorbia species

Sixteen new diterpene polyesters were isolated and identified from Hungarian Euphorbiaceae species. Two of them (21, 23) are based on formerly unknown diterpene core. The structures of three jatrophane type diterpene heptaester were elucidated (1, 3, 6), which are diterpenoids with the highest degree of esterification identified from this plant family. Some of the isolated compounds have pharmacological effects, others are under testing now.     

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.     

Studies on structural elucidation of Aconitum diterpenoid alkaloid by LC-APCI-MS and effects of Aconitum diterpenoid alkaloid on cutaneous blood flow

The chemical constituents of Aconitum yesoense var. macroyesoense and Aconitum japonicum were examined using high-resolution spectral analysis. Twelve novel alkaloids were isolated from A. yesoense var. macroyesoense together with 20 known alkaloids. Eight novel alkaloids were isolated from A. japonicum together with 15 known alkaloids. An HPLC-atmospheric pressure chemical ionization-mass spectrometry (HPLC-APCI-MS) method was useful for the simultaneous determination of 21 Aconitum alkaloids found in A. yesoense var. macroyesoense and A. japonicum. These compounds were fairly stable under the conditions used, and the protonated molecules or fragment ions characteristic of the molecule appeared as base peaks in the mass spectra and were used for selected ion monitoring. HPLC-APCI-MS is a very promising approach for structural investigations of positional isomers and stereoisomers. This method was applied successfully to stereoisomeric Aconitum alkaloids differing in configuration at C-1, -6, or -12. Comparison of the APCI spectra showed that the abundance of fragment ions was significantly higher for the C-1, -6, or -12 beta-form alkaloid than for C-1, -6, or -12 alpha-form alkaloid. The main alkaloid constituents in the root of A. yesoense var. macroyesoense, Aconitum alkaloids of the C20-diterpenoid type, kobusine and pseudokobusine, and their acyl derivatives were examined for their peripheral vasoactivities by measuring laser-flowmetrically the cutaneous blood flow in the hind foot of mice after intravenous administration. It is thought that the hydroxyl groups of alkaloids, especially a free OH group of pseudokobusine at C-6, were important for action on the peripheral vasculature leading to dilatation, and the results indicated that esterification of the hydroxyl group at C-15 with either anisoate, veratroate, or p-nitroben-zoate may contribute to enhancement of the activity of the parent alkaloids.     

Norditerpenoid and dianthramide glucoside alkaloids from cultivated<Emphasis Type="Italic">aconitum</Emphasis> species from Korea

A new norditerpene alkaloid named 8-O-methylhypaconine (1) was isolated along with twelve known alkaloids from the underground parts of an unknown species of Aconitum plant culti vated in Korea. Among the known alkaloids, two dianthramide glucosides, N-(2'-beta-glucopyra nosyl-5'-hydroxysalicyl)-5-hydroxyanthranilic acid methyl ester (2) and N-(2'-beta-glucopyranosyl-5'-hydroxysalicyl)-5-hydroxy-6-methoxyanthranilic acid methyl ester (3), were isolated from Aconitum plants for the first time. The structures were established on the basis of chemical and spectroscopic methods.     

太白乌头中一新的去甲二萜生物碱

为了研究太白乌头(Aconitum taipaicum)根的化学成分，采用硅胶柱色谱进行分离纯化，根据其理化性质和波谱数据确定化合物结构。从该植物的根中分离得到1个新的去甲二萜生物碱isodelelatine (1)和5个已知生物碱，分别为atisine (2)、 delfissinol (3)、 liangshanine (4)、 hypaconitine (5)和delelatine (6)。化合物2～6均为首次从该植物中分离得到。     

两个新的双去甲二萜生物碱高乌宁碱丁和高乌宁碱戊的结构研究

目的：研究高乌头Aconitum sinomontanum Nakai根的化学成分。方法：采用硅胶柱色谱及离心薄层色谱分离化学成分,IR, ¹HNMR, ¹³CNMR, ¹H-¹H COSY, HMBC, HMQC, MS等方法进行结构鉴定。结果：得到两个双去甲二萜生物碱高乌宁碱丁(sinomontanine D, 1)和高乌宁碱戊(sinomontanine E, 2)。结论：化合物1,2为新的双去甲二萜生物碱。     

Phytochemical and biological investigations of Amaryllidaceae alkaloids: a review

Amaryllidaceae is a family that includes 75 genera and about 1100 species, which have a long history of medicinal use. Many plants have been proven to possess efficacy for neurological injury and inflammatory conditions. This article summarizes 357 Amaryllidaceae alkaloids, and cites 166 174 references over the last three decades. These alkaloids are classified into 14 skeleton types, and their abundant sources are also included. Modern pharmacology studies demonstrate that alkaloids that exclusively occur in Amaryllidaceae plant possess wide-ranging pharmacological actions, especially effects on the central nervous system, as well as antitumor, antimicrobial, and anti-inflammatory activities. Effective monomeric compounds from Amaryllidaceae screened for pharmacological activity in vivo and in vitro are also summarized.     

The chemistry and biochemistry of Spiraea japonica complex

The characteristic components of Spiraea japonica complex, which consists of seven varieties, are the hetisine- and atisine-type diterpene alkaloids, and the atisane-type diterpenes. From this complex, 20 hetisines, 37 atisines and 7 diterpenes were isolated during 1964-2001, including the observations of the isomerization of spiraea diterpene alkaloids having the oxazolidine ring and the interconversion of the oxazolidine rings, the configuration of the oxygen substitution at C-15 of the atisine-type alkaloids, and the interconversion relationship between the two main subtypes of the hetisine-type alkaloids. The chemotaxonomy based on structures of the reported diterpene alkaloids were suggested. The studies on the anti-inflammation, anti-platelet aggregation and neuroprotective bioactivities of the alkaloids from S. japonica var. acuta were reviewed as well.     

Quantitative determination of diterpenoid alkaloids in four species of Aconitum by HPLC

A high performance liquid chromatography (HPLC) method has been developed for the determination of five principal alkaloids (benzoylmesaconine, mesaconitine, aconitine, hypaconitine and deoxyaconitine) found in four species of genus Aconitum. The five alkaloids were analyzed simultaneously with an XTerraRP18 column by gradient elution using 0.03 M ammonium hydrogen carbonate-acetonitrile as mobile phase. The recovery of the method was 94.6-101.9%, and all the alkaloids showed good linearity (gamma = 0.9999) in a relatively wide concentration range. The results indicated that contents of alkaloids in Aconitum varied significantly from species to species; hence quality control of Aconitum drugs is very necessary.     

Jenamidines A to C: unusual alkaloids from Streptomyces sp. with specific antiproliferative properties obtained by chemical screening

Three new naturally occurring bicyclic alkaloids, jenamidines A (1), B (2) and C (3), were discovered and isolated from the culture broth of Streptomyces sp. (strain HKI0297) via the chemical screening approach. Fermentation, isolation, structure and biological activities of these three new secondary metabolites are reported. The jenamidines have an unusual octahydro-pyrido[1,2-a]pyrimidine skeleton. Jenamidine A (1) shows antiproliferative effects against the chronic myeloid leukaemic cell line K-562. In addition, the new tricyclic sesquiterpenoid, africantriol (4) was isolated from the same strain.     

露蕊乌头生物碱的研究(Ⅰ)

从藏药露蕊乌头(Aconitum gymnandrum Maxim)中分得四个生物碱,经化学和光谱鉴定,其中两个为已知生物碱atisine.Hcl(A)和talatisamine(B),另两个为新的二萜类生物碱,分别命名为露乌碱,(C)(gymnaconitine)和甲基露乌碱(D)(mgthyl gymnaconitine),这两种新的生物碱均联接有二甲基咖啡酸酯:在乌头生物碱中是首次发现。     

松潘乌头二萜生物碱的研究

甘肃省文县产的松潘乌头(Aconitum sungpanense Hand-Mazz),俗称缠绕乌头,民间用于治疗跌打损伤,风湿性关节痛等症。其化学成分尚未见报道。松潘乌头粗粉用0.5%的盐酸渗漉,通过阳离子树脂交换,经乙醚及二氯甲烷先后洗脱,乙醚部分用硅胶柱层析等     

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.     

白花瓜叶乌头中生物碱成份的研究

目的：研究白花瓜叶乌头（Aconitum hemsleyanum Pritz vor.laueanthus P.Guo et.M.R.Jia)根中生物碱成份。方法：pH与溶剂极性梯度萃取及硅胶层析。结果：从中分得7个已知去甲二萜生物碱,由光谱法分别鉴定为大渡乌碱1;13,15－dideoxyaconitine 2;indaconitine 3;crassicaudine4;塔拉萨敏5;查斯曼宁6;ezochasmanine 7。结论：这些化合物均首次从该植物中分离得到。