白喉乌头的化学成分研究

目的:研究白喉乌头的化学成分。方法:采用硅胶、Sephadex LH-20等色谱技术分离纯化白喉乌头中的化学成分,根据波谱数据和理化性质进行结构鉴定。结果与结论:共鉴定出了5个化合物,分别为Delvestidine(1)、高乌甲素(2)、N-去乙酰高乌甲素(3)、氨茴酰牛扁碱(4)、冉乌碱(5)。其中,化合物1、5为首次从白喉乌头中获得。     

不同产地哈萨克药材白喉乌头中总生物碱含量的分析

目的 测定不同产地白喉乌头所含总生物碱的含量。 方法 采用索式提取法对药材进行提取,结合酸溶碱沉和萃取的方法从药材中提取白喉乌头总生物碱;利用紫外光谱对经过酸性染料络合的生物碱进行分析,检测其中总生物碱的含量。 结果 新源县、巩留县和昭苏县所产白喉乌头原药材中含有总生物碱分别为2.246,4.682和3.597 mg·g^-1;回归方程为Y=11.5X + 0.121,r=0.999 6,乌头碱浓度在6～36 μg·mL^-1内呈良好的线性关系。 结论 采用紫外-可见分光光度法测定不同产地白喉乌头中总生物碱的含量,具有操作简便、结果准确的特点;其结果可为该药材的活性和毒性物质基础研究提供依据。     

彭州岩乌头根中生物碱成分的研究

目的：研究彭州岩叶乌头根中的生物碱成分。方法：ｐＨ梯度洗脱及硅胶柱层析。结果;从中分得七个已知去甲二萜生物碱,通过光谱法鉴定为塔拉萨敏（ｔａｌａｔｉｓａｍｉｎｅ）１,异塔拉萨定（ｉｓｏｔａｌａｔｉｚｉｄｉｎｅ）２,ｓａｃｈａｃｏｎｉｔｉｎｅ３,ｎｅｖａｄｅｎｉｎ４,伪乌头宁（ｐｓｅｕｄａｃｏｌｌｉｎｅ）５,ｖｉｒｅｓｅｎｉｎ６和牛扁碱（ｌｙｃｏｃｔｏｎｉｎｅ）７。结论：以上化合物均是首次从该植物中     

高效液相色谱法分离测定康复新胶囊中乌头类生物碱含量

目的:建立一种用高效液相色谱法分离测定康复新胶囊中新乌头碱、次乌头碱和乌头碱含量的方法。方法:应用氨水碱化后,乙醚提取,提取液通过Oasis　MCX固相萃取柱对样品进行纯化,以ZORBAX SB-C8柱（250mm×4.6mm,5μm）为分析柱,0.04mol·L-1三乙胺（磷酸调pH=3）-甲醇（50:50）为流动相,检测波长235nm,柱温40℃。结果:新乌头碱、次乌人碱和乌头碱约在0.002～1μg范围内线性关系良好,其回收率>90％,RSD<2％。结论:该方法准确、专属,分离效果好,灵敏度高。     

乌头属药用植物中生物碱的研究进展

目的 综述乌头属药用植物中生物碱的国内研究进展。方法 对近十几年来国内发表的具有代表性的相关文章进行分析、整理和归纳。结果 乌头属药用植物主要成分为生物碱,现已从多种乌头属药用植物中分离鉴定出各种生物碱单体。综述了生物碱的各种含量测定方法。结论 应加强对乌头属植物中有效成分和毒性成分的分析,以加大这类植物的开发利用,确保临床用药的安全性和有效性。     

HPLC法测定两种乌头药材中生物碱的含量

高效液相色谱法测定湖北两种乌头药材中乌头碱、次乌头碱、中乌头碱的含量。采用SpherisorbODS柱，以甲醇-水-氯仿-三乙胺（60：40：2：0．1）为流动相，联苯为内标。     

二萜生物碱

本文主要综述了１９８９年至１９９２年初所发表的毛莨科乌头属和翠雀属植物二萜生物碱的化学及其药理方面的研究文献。     

乌头属植物二萜生物碱研究进展

乌头属植物中含有的特征成份二萜生物碱具有较强的毒性和广泛生物活性,多年以来一直是药物学家寻找新药和先导化合物的一个重要来源．也是植物化学分类学家研究的热点。本文从乌头属植物中二萜生物碱的来源,结构及其特点等方面,综述了1998-2008年从乌头属植物中分得的新的二萜生物碱的研究情况。     

新疆乌头属植物中双酯型生物碱的含量测定

目的:采用高效液相色谱法测定新疆乌头属植物中双酯型生物碱(乌头碱、新乌头碱、次乌头碱)的含量。方法:采用X Bridge C18色谱柱(250 mm×4.6 mm,5μm),以甲醇-水-三氯甲烷(浓氨水调节pH为10.62)(70∶30∶2)为流动相,流速为1.0mL·min-1,进样量10μL,检测波长为235 nm。结果:(1)HPLC法测定乌头碱在0.020 1～2.012 0 mg·mL-1范围内线性关系良好(r=0.999 9);平均加样回收率为100.06%,RSD为0.60%;新乌头碱在0.002 2～0.086 4 mg·mL-1范围内线性关系良好(r=0.999 9);平均加样回收率为99.69%,RSD为1.04%;次乌头碱在0.002 1～0.084 0 mg·mL-1范围内线性关系良好(r=0.999 9);平均加样回收率为99.68%,RSD为1.08%。样品含量测定结果表明新疆乌头属植物含有双酯型生物碱,但不同种之间含量和成分有一定的差异。(2)新疆乌头属植物中含有乌头碱、新乌头碱和次乌头碱,但不同种植物之间,成分和含量有一定差异,准噶尔乌头、白喉乌头中双酯型生物碱含量较高。结论:本实验建立了新疆乌头属植物中双酯型生物碱的HPLC含量测定方法,本法方便、准确,为进一步研究和利用新疆乌头属植物奠定了基础。新疆乌头属植物中准噶尔乌头和白喉乌头双酯型含量较高,具有潜在药用价值,值得进一步深入研究。     

拟康定乌头中二萜生物碱成分的研究

目的 研究毛茛科乌头属拟康定乌头中的二萜生物碱成分.方法 采用硅胶柱色谱法进行分离,再根据HR-ESI-MS和NMR等多种方法鉴定化合物的结构.结果 从拟康定乌头95％乙醇提取物中分离并鉴定了 17个单体化合物,分别鉴定为 talatisamine、14-O-acetyltalatisamine、dolichotine...     

Mode of antinociceptive and toxic action of alkaloids of Aconitum spec.

Extracts of the plant Aconitum spec. are used in traditional Chinese medicine predominantly as anti-inflammatory and analgesic agents, the latter allegedly equally potent as morphine but without any habit-forming potential. As the only pharmacologically active compounds, the C₁₉ diterpenoid alkaloid aconitine, and some of its derivatives, have been proven to be antinociceptive in different analgesic assays, but the mode of action is unknown. To elucidate the mode of action, ten aconitine-like derivatives were investigated with respect to their affinity for voltage-dependent Na⁺ channels, the action on synaptosomal Na⁺ and Ca²⁺ homoeostasis and their antinociceptive, arrhythmogenic and acute toxic properties. Since aconitine is known to bind to site II of Na⁺ channels, we determined the affinity of the aconitine-like derivatives in vitro to synaptosomal membranes by the [³H]-batrachotoxinin-binding assay and their properties on intrasynaptosomal concentrations of free Na⁺ and Ca²⁺ ([Na⁺]_i and [Ca²⁺]_i), both the latter determined fluorometrically with SBFI and Fura-2 respectively. Furthermore, the alkaloids’ arrhythmogenic potential was investigated in guinea-pig isolated atria and the antinociceptive action on formalin-induced hyperalgesia and the acute toxic action estimated in mice. The results show that the alkaloids could be divided into at least three groups. The first is characterized by a high affinity to the site II of Na⁺ channels (K _i about 1.2 μM), the ability to enhance [Na⁺]_i and [Ca²⁺]_i (EC₅₀ about 3 μM), a strong arrhythmogenic action that starts at about 30 nM, an antinociceptive effect (ED₅₀ about 0.06 mg/kg) and high acute toxicity (LD₅₀ values about 0.15 mg/kg). To this group belong aconitine, 3-acetylaconitine and hypaconitine. The second group, with lappaconitine as the only member, has an affinity to Na⁺ channels an order of magnitude lower (K _i = 11.5 μM), less acute toxicity (LD₅₀ about 5 mg/kg), and a two orders of magnitude lower antinociceptive action (ED₅₀ about 2.8 mg/kg) and lower cardiotoxicity (bradycardia observed at 3 μM). Additionally, lappaconitine suppresses the increase in [Ca²⁺]_i of aconitine-stimulated synaptosomes and increases the excitation threshold of left atria, indicating an inhibition of Na⁺ channels. The other derivatives, i.e. delcorine, desoxydelcorine, karakoline, lappaconidine, lappaconine and lycoctonine, belong to the third group, which has hardly any effects. They have a low affinity to Na⁺ channels with K _i values in the millimolar range, show no effect on synaptosomal [Na⁺]_i and [Ca²⁺]_i, no arrhythmogenic potential up to 100 μM, no antinociceptive activity and low toxicity with LD₅₀ values greater than 50 mg/kg. For the investigated alkaloids we suggest two different antinociceptive-like modes of action. Aconitine, hypaconitine and 3-acetylaconitine may induce a block of neuronal conduction by a permanent cell depolarisation, whereas lappaconitine might act like local anaesthetics. However, because of the low LD₅₀/ED₃₀ quotients of 2–6, the antinociceptive-like action of the Aconitum alkaloids seems to reflect severe intoxication rather than a specific antinociceptive action. The structure/activity relationship shows that alkaloids that activate or block Na⁺ channels have a benzoyl ester side chain in the C-14 or C-4 positions respectively, whereas the other compounds lack this group. Received: 24 June 1997 / Accepted: 8 September 1997     

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.     

新疆天山地区林地乌头的性状与显微鉴别

目的对林地乌头的生药特征进行分析和探讨。方法采用性状鉴别、组织横切面及粉末显微鉴别方法对林地乌头的根、茎和叶分别进行研究。结果林地乌头根呈棕褐色,6～10个小瘤状侧根成链状相连;根木质部导管4～5束,呈放射状;具多角形金黄色的石细胞和螺纹导管;淀粉粒较小,直径2～8μm;根中木质部占大部分。结论林地乌头与新疆地产其他乌头相比,具有明显的生药学差异,可作为其鉴别的依据。     

茯苓皮中三萜酸类成分的研究

目的 研究茯苓皮中的三萜酸类化合物.方法 采用柱色谱法和制备液相色谱法,从茯苓皮的二氯甲烷及乙酸乙酯提取物中分离纯化单体化合物,并通过光谱方法鉴定其结构.结果 从茯苓皮的提取物中分离并鉴定了11个三萜酸,分别为茯苓酸A(Ⅰ)、茯苓酸B(Ⅱ)、茯苓酸AM(Ⅲ)、茯苓酸(Ⅳ)、dehydroeburiconic acid(Ⅴ)、dehydrotrametenonic acid(Ⅵ)、dehydrotrametenolic acid(Ⅶ)、eburicoic acid(Ⅷ)、3-O-acetyl-16α-hydroxytrametenolic acid(Ⅸ)、3-O-formyl-dehydrotrametenolic acid(X)、3-O-formyl-eburicoic acid(Ⅺ),其中化合物Ⅹ、Ⅺ为新化合物.结论 通过验证实验证明:化合物Ⅹ、Ⅺ为分离过程中产生的人工产物.     

新疆乌头属(毛茛科)一新变种

目的描述毛茛科乌头属药材一新变种那拉提乌头(Aconitum leucostomum var.nalatiensis F.Zhang et D.M.Cai)。方法采用性状鉴别、组织横切面及粉末显微鉴定等方法。结果该变种茎、花梗和小苞片均为绿色;花的上萼片、侧萼片和下萼片为乳白色,末端略呈淡黄白色,上萼片为狭圆筒形;花瓣的瓣片上部为白色、下部为紫色,唇为白色,距直立拳卷。结论该物种与白喉乌头和空茎乌头相比有显著差异,为一新变种。     

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.     

长柱十大功劳的化学成分研究(Ⅰ)

目的研究长柱十大功劳Mahonia duclouxiana Gagnep.的化学成分。方法利用硅胶柱层析分离纯化长柱十大功劳的乙醇提取物,并通过理化性质和TLC、UV、IR、1HNMR、13CNMR、MS等分析鉴定化合物结构。结果分离得到5个化合物,分别鉴定为小檗碱(Ⅰ)、巴马汀(Ⅱ)、药根碱(Ⅲ)、异粉防己碱(Ⅳ)和β-谷甾醇(Ⅴ)。结论5个化合物均为首次从该植物中分离鉴定。