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。     

不同煎煮时间对熟附子生物碱的影响

目的通过测定熟附子不同煎煮时间的生物碱含量,确定最佳的煎煮时间,为规范化的煎煮工艺提供参考。方法采用HPLC和UV方法分别测定熟附子煎煮液中6种生物碱和总生物碱的含量,并以此含量为指标综合评价其煎煮工艺。结果熟附子主要含有单酯型生物碱和微量的双酯型生物碱,煎煮0.5 h后,3种双酯型生物碱完全消失,而煎煮1 h后,总单酯型生物碱和总生物碱均达到了峰值,分别为:2.900 1 mg/g和4.832 0 mg/g,随着煎煮时间的延长,单酯型生物碱和总生物碱的含量均逐渐下降。结论熟附子的最佳煎煮时间为1 h。     

不同煎煮时间对熟附子生物碱的影响

目的 通过测定熟附子不同煎煮时间的生物碱含量,确定最佳的煎煮时间,为规范化的煎煮工艺提供参考.方法 采用HPLC和UV方法分别测定熟附子煎煮液中6种生物碱和总生物碱的含量,并以此含量为指标综合评价其煎煮工艺.结果 熟附子主要含有单酯型生物碱和微量的双酯型生物碱,煎煮0.5h后,3种双酯型生物碱完全消失,而煎煮1h...     

配伍前后四逆汤中酯型生物碱的变化规律

目的 研究四逆汤中附子配伍不同药味前后,汤液中酯型生物碱的变化规律.方法 采用HPLC法测定附子单煎液、附子干姜合煎液、附子甘草合煎液和四逆汤中单酯型生物碱及双酯型生物碱成分的含量.结果 附子配伍不同药味之后,苯甲酰乌头原碱等3种单酯型生物碱的含量均升高,依次为四逆汤＞附子甘草合煎液＞附子干姜合煎液＞附子单煎液;仅在附子单煎液中检出次乌头碱,其浓度为0.11 mg·g-1,而在附子干姜合煎液、附子甘草合煎液、四逆汤中均未检测到双酯型生物碱成分.结论 附子在配伍其他药味后,单酯型生物碱成分的含量升高、双酯型生物碱成分的含量减低,为“附子无干姜不热、干姜缓附子之毒”与附子-甘草“相畏/相杀”减毒配伍“毒减而效不减”提供了依据;四逆汤组单酯型生物碱成分的含量上升幅度最大,体现了全方药简力专、大辛大热,使阳复厥回通,共奏回阳救逆之功.     

附子不同部位及其炮制品生物碱的含量比较△

目的:比较附子不同部位及其炮制品生物碱含量变化。方法:采用HPLC法同时测定附子不同部位及其炮制品中6种单、双酯型生物碱的含量,采用滴定法测定其总生物碱含量,分析其不同部位及其炮制品生物碱含量的变化。结果:单酯型生物碱大小依次为:制附子皮>黑顺片>白附片>附子皮>生附子,双酯型生物碱大小为:附子皮>生附子>制附子皮>黑顺片>白附片,总生物碱大小为:附子皮>生附子>制附子皮>黑顺片>白附片。结论:附子皮中生物碱的含量高,毒性大,为了保证其临床有效性与安全性,黑顺片与白附片临床应用应有所区分。     

传统药对附子-炮姜的配伍研究

目的:以附子、炮姜为对象,研究温热药对配伍前后关键组分的变化,探讨传统药对附子-炮姜配伍的科学意义。方法:采用紫外分光光度法测定附子总生物碱、酯型生物碱含量在配伍前后的变化,结合高效液相色谱指纹图谱研究附子与炮姜配伍前后附子总体成分的变化。结果:附子与炮姜配伍后,附子总生物碱与酯型生物碱含量均大幅减少;从指纹图谱分析可知,附子与炮姜配伍后,附子各成分总加权变化率为81.00%,即总体上附子成分有所减少,为配伍前的81.00%。结论:附子与炮姜配伍后抑制了附子的热性,增强了炮姜的温性,主要用于温经止血。     

不同炮制方法对川乌双酯型生物碱含量的影响

目的 研究炮制方法对川乌双酯型生物碱含量的影响。方法将生川乌分别通过药典法、黑豆法和米醋法进行炮制,以RP—HPLC结合梯度洗脱的色谱方法为检测手段,比较分析不同川乌炮制方法对双酯型生物碱（主要为乌头碱、次乌头碱）含量的影响。结果3种炮制方法均可显著降低生川乌中乌头碱、次乌头碱的含量。所建立的色谱方法可定量分析炮制品中双酯型生物碱。结论不同炮制方法对生川乌均能起到减毒作用。     

乌头碱类成分中药制剂质量控制探讨

目的:探讨乌头碱类成分制剂的质量控制.方法:比较2005年版,2010年版中国药典对乌头类生物碱的质量控制要求,分析乌头碱类生物碱的毒性及其化学结构特征.结果与结论:2010年版药典与2005年版药典比较.2010年版药典对乌头类药材质量控制要求有利于药材使用的安全有效:2010年版药典对含乌头类生物碱成分的中药制剂的质量控制有待进一步加强.建议对含乌头类生物碱成分的中药制剂,在质量标准中研究建立双酯型生物碱的限量检查方法,以及双酯型生物碱水解产物苯甲酰新乌头原碱、苯甲酰乌头原碱和苯甲酰次乌头原碱等单酯型生物碱的总量测定,制定合理的含量范围,以保证用药的安全有效.     

附子不同配伍药对中生物碱成分的电喷雾质谱分析

以传统中医用药附子的配伍药对为研究对象，考察附子与不同中药配伍对附子中生物碱的影响规律，揭示配伍减毒的科学内涵。利用电喷雾质谱技术和内标法，分别对生附子，生附子加炙甘草、白芍、干姜、大黄共煎液和药渣中乌头类生物碱进行系统考察。与生附子相比，双酯型生物碱在附子加炙甘草、大黄、白芍、干姜共煎液中的含量降低；附子加炙甘草、白芍、干姜共煎液中的脂型生物碱含量增高。附子与炙甘草、白芍、干姜配伍的解毒机制是使毒性较大的双酯型生物碱转化为毒性小的脂型生物碱；与大黄配伍的解毒机制是药物所含成分与附子中的双酯型生物碱络合生成难溶于水的复合物，使双酯型生物碱的含量降低。本法对深入研究乌头属植物的配伍作用机制具有借鉴作用。     

UPLC-MS/MS法测定市售附子中的13种生物碱

目的 采用UPLC-MS/MS法测定附子中13种生物碱的含量,分析市售附子中毒、效成分的差异.方法 采用Agilent SB-C18色谱柱(50mm×2.1 mm,1.8 μm),流动相为2 mmol·L-1乙酸铵-乙腈,梯度洗脱;质谱采用ESI+离子源,多反应监测模式(MRM)检测13种生物碱及内标的定量离子和定性离子.结果 测定了附子中13种生物碱的含量,13种生物碱成分在选定的浓度范围内线性关系良好(r均＞0.996),平均回收率为86.4％～101.1％,RSD≤4.4％(n=6);市售附子中主要毒、效成分的差异较大.结论 文中方法能更全面、准确地表征市售附子成分的差异,可为附子的加工炮制、质量控制和临床应用提供参考.     

Pyrrole alkaloids from Bolbostemma Paniculatum

Three pyrrole alkaloids were isolated from Bolbostemma paniculatum. Their structures were elucidated as 4-(2-formyl-5-methoxymethylpyrrol-1-yl)butyric acid methyl ester (1), 2-(2-formyl-5-methoxymethylpyrrol-1-yl)-3-phenylpropionic acid methyl ester (2) and α-methyl pyrrole ketone (3) by spectroscopic techniques. Among them, 1 and 2 are new compounds.     

Effect of 3‐Alkylpyridine Marine Alkaloid Analogues in Leishmania Species Related to American Cutaneous Leishmaniasis

A series of oxygenated analogues of marine 3‐alkylpyridine alkaloids were synthesized, and their leishmanicidal activity was assayed. All compounds were prepared from 3‐pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a classic Williamson etherification under phase‐transfer conditions. Besides toxicity in peritoneal macrophages, the compounds exhibited a significant leishmanicidal activity. Of twelve compounds tested, five showed a strong leishmanicidal activity against promastigote forms of Leishmania amazonensis and L. braziliensis with IC₅₀ below 10 μm . Compounds 11 , 14 , 15, and 16 showed a strong leishmanicidal activity on intracellular amastigotes (IC₅₀ values of 2.78; 0.27; 1.03, and 1.33 μm , respectively), which is unlikely to be owing to the activation of nitric oxide production by macrophages.     

HPLC-ELSD法测定贝母中异甾类生物碱及糖苷类成分的含量

目的建立同时测定贝母中5种异甾类生物碱——peimissine, imperialine, sinpeinine A, imperialine-3β-glucoside和yibeinoside A含量的HPLC分析方法。方法C₁₈柱;流动相:乙腈-水(含0.1%二乙胺);梯度洗脱,流速1.0 mL·min^-1;检测器:Alltech 500蒸发光散射检测器(ELSD)。结果线性范围为peimissine 13.1～288.2 mg·L^-1(r²=0.997 5), imperialine-3β-glucoside 7.7～169.4 mg·L^-1 (r²=0.999 3), yibeinoside A 7.3～160.6 mg·L^-1 (r²=0.999 7), imperialine 16.5～363.0 mg·L^-1 (r²=0.999 2), sinpeinine A 8.7～191.4 mg·L^-1 (r²=0.994 2)。 5个化合物的精密度和重现性RSD均<5%。结论本方法简便、有效、可行,可用于贝母中5种异甾类生物碱的含量测定。     

天然产物研究中的人工产物

植物中的萜类、生物碱等类成分由于提取分离过程中溶剂或外界光热等作用反应而生成植物本身并不含有的成分,称为人工产物。对分离所得的纯物质需进行仔细分析,确定是人工产物还是植物本身含有的成分。例如,早在５０年代,傅丰永等［１］从秦艽根中提取出３个生物碱［１～３］：秦艽碱甲（２,ｇｅｎｔｉａｎｉｎｅ）、秦艽碱乙（２′,ｇｅｎｔｉａｎｉｄｉｎｅ）和秦艽丙素（３,ｇｅｎｔｉａｎａｌ）。但随后的研究［４～５］表明,秦艽的乙醇提取液中没有秦艽碱甲等３个生物碱,而含有龙胆苦苷（１）,龙胆苦苷在氨水中转化生成秦艽碱…     

Synthetic study toward the total synthesis of fumigaclavines A–D

In the present study, we developed a novel approach for the synthesis of the tetracyclic core of fumigaclavines A–D. A palladium-catalyzed intramolecular Larock indole synthesis was utilized to assemble the B/C rings of the tetracyclic core in one step. Although all attempts to convert compound 18 to fumigaclavine B failed, this study provided useful information for the total synthesis of fumigaclavines A–D.     

Pharmacology of nootropics and metabolically active compounds in relation to their use in dementia

The development of effective drugs for the treatment of dementia is an important therapeutic target. Drugs which stop the progression of dementia have not been developed; however, nootropics and metabolically active compounds such as the vinca alkaloids and the ergot alkaloids as well as alkylxanthines are widely used to alleviate the symptoms. This review summarises animal studies investigating the mechanism of action of these compounds and highlights gaps in our knowledge of their pharmacology. Nootropics, such as piracetam, facilitate learning and retrieval of information and protect the brain from physical and chemical intoxication. Nootropics may produce these effects via an enhancement of acetylcholine or dopamine release; however, this postulate requires further evaluation. The pharmacology of vinca alkaloids is reviewed with particular reference to vinpocetine. This compound attenuates cognitive deficits, reduces ischaemia-induced hippocampal cell loss and increases cerebral blood flow and glucose utilisation. These effects may be induced by modulation of cyclic nucleotide levels and adenosine re-uptake inhibition. An extensively examined ergot alkaloid is co-dergocrine; this compound increases both the oxygen tension and the electrical activity of the ischaemic cerebral cortex. Alkylxanthines have a wide range of pharmacological activities, and in this review the pharmacology of pentoxifylline, propentofylline and denbufylline is contrasted with that of theophylline and caffeine. In particular, the pharmacology of propentofylline and the selective lowK _m cyclic AMP phosphodiesterase inhibitor denbufylline is summarised. Although more carefully controlled clinical trials in well defined patient collectives are required, present evidence suggests some therapeutic efficacy for nootropics and metabolically active compounds. Further studies to more closely evaluate their mechanism of action may lead to the development of more effective agents for the therapy of dementia.     

天然产物中抗HIV生物碱类化合物的研究进展

近年来,从天然产物中寻找高效低毒的先导化合物已成筛选抗HIV药物的重要研究方向。生物碱类化合物作为一类重要的天然产物,数量众多,结构类型复杂,其中有多种抑制和阻断HIV感染的有效成分,通过实验室研究工作和临床用药观察,有望从中获得抗HIV的有效药物。以生物碱类化合物的化学结构为基础,将生物碱类化合物分为异喹啉类、喹啉类、大环类、哌啶类、莨菪烷类、吲哚类、咔唑类、海洋多环胍类、萜类、manzamine型生物碱等10类,对其抗HIV活性进行综述。     

莲心总碱及其甲基化物对牵张性心律失常的拮抗效应(英文)

目的　澄清莲心总碱 (TAL)与氨基糖苷类抗生素的共同化学结构带正电的氨基是否使之具有抗牵张性心律失常的共同效应。方法　通过膨胀心室腔内的球囊、夹闭升主动脉和牵拉乳头肌建立心律失常、动作电位时程的缩短和触发活动的模型。采用离体心电图、细胞内微电极和在体单相动作电位的标准技术进行记录。结果　①TAL和甲基莲心总碱 (TMAL) (2 .5 ,5和 10 μmol·L- 1)能剂量依赖性的缩短大鼠离体心脏牵张性心律失常的持续时间 ,从对照组的 (2 .16± 0 .38)s减少到 (1.5 3± 0 .14 ) ,(0 .93± 0 .2 1) ,(0 .5 2± 0 .35 )s (TAL )和(1.5 9± 0 .16 ) ,(0 .94± 0 .2 1) ,(0 .79± 0 .15 )s(TMAL)。②在麻醉豚鼠 ,TAL 2 .3mg·kg- 1iv和TMAL 2 .6mg·kg- 1iv能显著抑制夹闭主动脉引起的单相动作电位 5 0 %和 90 %复极时程的缩短及触发活动的发生率 ,分别从 (2 8.9± 8.1) %减少到(5 .4± 1.2 ) %和 (10 .8± 2 .3) %。③TAL和TMAL也能显著抑制牵拉豚鼠乳头肌所致的动作电位 5 0 %和 90 %复极时程的缩短。结论　TAL和TMAL能抑制牵张性心律失常和牵张引起的动作电位的改变 ,这种作用可能是通过阻断牵张活化的离子通道实现的。     

Variation of alkaloid contents and antimicrobial activities of Papaver rhoeas L. growing in Turkey and northern Cyprus

Context: Papaver rhoeas L. (Papaveraceae) corn poppy, widely distributed in Turkey, is used to make a cough syrup for children, as a tea for disturbed sleep, for pain relief and as a sedative in folk medicine.

Objective: Samples of P. rhoeas collected from eight different locations in Turkey and three from northern Cyprus were investigated for their alkaloid content and screened for their antimicrobial activities.

Materials and methods: From the aerial parts of P. rhoeas samples, alkaloids were isolated by column and preparative thin-layer chromatography. The alkaloids were identified by comparing their spectral data (UV, IR and ¹H-NMR) and TLC Rf values with those of authentic samples. The antimicrobial study was carried out by microbroth dilution technique against six strains of bacteria and three strains of fungi.

Results: Twelve different alkaloids belonging to proaporphine (mecambrine), aporphine (roemerine), promorphinan (salutaridine), protopine (coulteropine and protopine) and rhoeadine (epiglaucamine, glaucamine, glaudine, isorhoeadine, isorhoeagenine, rhoeadine and rhoeagenine) groups were isolated. The most significant activity was observed with the alkaloid extract of P8 against Staphylococcus aureus with a MIC value of 1.22?μg/mL and against Candida albicans with a MIC value of 2.4?μg/mL.

Discussion: The results indicate that P. rhoeas samples (P8 and P9), which contain roemerine as their major alkaloid, were the most active extracts.     

吡咯里西啶生物碱的细胞毒性及致毒机制研究进展

吡咯里西啶生物碱广泛分布于6000多种高等植物中,是一类肝毒性很强的天然产物。吡咯里西啶生物碱在肝脏代谢成活性代谢物吡咯后产生肝毒性。利用体外细胞毒性研究方法评价吡咯里西啶生物碱的毒性,对于阐明吡咯里西啶生物碱的致毒机制,研究开发拮抗其毒性的药物及保证临床用药安全具有重要意义。本文对吡咯里西啶生物碱的细胞毒性及致毒机制的研究进展进行综述。