小半夏加茯苓汤复方及拆方的总生物碱含量测定

目的:建立小半夏加茯苓汤中总生物碱的含量测定方法。方法:用紫外分光光度法测定小半夏加茯苓汤中总生物碱的含量。以溴百里香草酚蓝为显色剂,λmax=414 nm,测得生物碱在2.2～7.7mg.L-1具有良好线性关系,平均回收率为97.38%,r=0.9998。结果:复方煎剂中总生物碱含量为0.05722%、拆方煎剂中总生物碱含量为0.02325%、单方煎剂中总生物碱含量为0.00847%。结论:该方法操作简便、准确、灵敏、重现性好,可用于小半夏加茯苓汤的质量控制。     

附片质量标准研究

目的:研究提高附片的质量标准。方法:按照2010年版《中国药典》方法测定附片中总灰分和酸不溶性灰分;采用RP-HPLC法测定附片中双酯型生物碱和单酯型生物碱的含量。色谱条件为Eclipse XDB-C18色谱柱(4.6 mm×250 mm,5μm),流动相0.1 mol.L-1醋酸铵溶液(每1 000 mL加0.5 mL冰醋酸)为A相,乙腈-四氢呋喃(25∶15)为B相,梯度洗脱,检测波长235 nm。结果:附片中总灰分、酸不溶性灰分含量差异很大;单酯型生物碱总量较为稳定,而双酯型生物碱总量相差较大,提示应制定附片中双酯型生物碱的含量幅度范围。结论:本法操作简便、可行,结果稳定,为附片质量控制提供参考方法。     

尖山橙和龙州山橙中的抗肿瘤吲哚生物碱(英文)

目的:研究尖山橙和龙州山橙中的抗肿瘤生物碱成分方法:采用层析柱和制备高效液相进行化合物分离,运用1D、2D-NMR及MS等波谱分析技术鉴定化合物结构。采用MTT法进行人体肿瘤细胞毒体外活性实验。结果:分离得到两个新的双吲哚生物碱melofusine I (1)和melomorsine I (2),以及22个已知吲哚生物碱,测试了24个化合物对5种(SW480,SMMC-7721,HL-60,MCF-7,A-549)人体肿瘤细胞的细胞毒活性。结论:化合物1-2是新的双吲哚生物碱,化合物tabersonine(3) and 19S-vindolinine(14)具有抑制5种人体肿瘤细胞株的活性。     

Haematological and immunological effects of repeated dose exposure of rats to integerrimine N-oxide from Senecio brasiliensis

This study is the first in the literature to focus attention on the possible immunotoxic effect of integerrimine N-oxide content in the butanolic residue (BR) of Senecio brasiliensis, a poisonous hepatotoxic plant that contains pyrrolizidine alkaloids (PAs). PAs have been reported as a pasture and food contaminant and as herbal medicine used worldwide and are responsible for poisoning events in livestock and human beings. After the plant extraction, BR extracted from Senecio brasiliensis was found to contain approximately 70% integerrimine N-oxide by elemental and spectral analyses (¹H and ¹³C NMR), which was administered to adult male Wistar Hannover rats at doses of 3, 6 and 9 mg/kg for 28 days. Body weight gain, food consumption, lymphoid organs, neutrophil analysis, humoural immune response, cellular immune response and lymphocyte analysis were evaluated. Our study showed that integerrimine N-oxide could promote an impairment in the body weight gain, interference with blood cell counts and a reducing T cell proliferative activity in rats; however, no differences in the neutrophil activities, lymphocytes phenotyping and humoural and cellular immune responses were observed. It is concluded that doses of integerrimine N-oxide here employed did not produce marked immunotoxic effects.     

一叶萩生物碱的合成和生物活性(英文)

一叶萩生物碱是从大戟科植物一叶萩,叶下珠属以及白饭树属中提取的一类化合物。它们中大部分呈现出广泛的生物活性,例如GABA受体拮抗活性,抗疟和抗菌活性。由于它的结构的特殊性,合成不同骨架的一叶萩生物碱对于有机化学和药物化学家来说是具有挑战性的工作。在本文中我们对几种一叶萩碱的全合成以及生物活性进行了概述。     

Developmental patterns of phenylpropylamino alkaloids accumulation in khat (Catha edulis, Forsk.)

Khat (Catha edulis Forsk., Celastraceae) is a perennial shrub that was introduced to Israel by Yemenite immigrants. Khat young leaves are chewed as a stimulant. The main stimulating active principles in this plant are the phenylpropylamino alkaloids (-)-cathinone [(S)-alpha-aminopropiophenone], (+)-cathine [(+)-norpseudoephedrine] and (-)-norephedrine. A novel GC-MS analysis method for the quantitative determination of phenylpropylamino alkaloids and their putative precursor 1-phenyl-1,2-propanedione in khat leaves was developed. We found a marked diversity in the phenylpropylamino alkaloids content and composition in 9 different accessions originated in seedlings and in the commercial cultivar "Mahanaim". The highest 1-phenyl-1,2-propanedione and (-)-cathinone levels occur in young leaves, the part traditionally chewed for its psycho-stimulating properties. Older leaves lack (-)-cathinone but contain the less active (+)-cathine and (-)-norephedrine. Young stems and flowers also contain 1-phenyl-1,2-propanedione, (-)-cathinone, (+)-cathine and (-)-norephedrine. We report the presence of a (-)-cathinone reductase in khat leaves capable of reducing (-)-cathinone to (+)-cathine in the presence of NADPH. We propose that (-)-cathinone is a biosynthetic precursor of (+)-cathine and (-)-norephedrine in khat leaves.     

Evaluation of the cholinergic and adrenergic effects of two tropane alkaloids from Erythroxylum pervillei

Pervilleine A is an aromatic ester tropane alkaloid from Erythroxylum pervillei that has shown promising activity as a multidrug resistance inhibitor. Due to its structural similarity with the well known (-)-hyoscyamine and (-)-cocaine, the cholinergic and adrenergic activities of pervilleine A were evaluated. At 30 microm (+/-)-pervilleine A hydrochloride exhibited non-competitive inhibition of the cholinergic response in the guinea-pig ileum and did not affect the carbachol-induced contraction of the rat anococcygeus smooth muscle. (+/-)-Pervilleine A hydrochloride blocked nonspecifically the vascular response of (-)-norepinephrine in the rat aorta ring, while the contractile response of rat vas deferens to (-)-norepinephrine was not affected significantly at a 100 microm concentration. An analogue of pervilleine A, (+/-)-pervilleine H, without a 6-O-trans-3,4,5-trimethoxycinnamoyl ester substituent required for anti-multidrug resistance activity, did not exhibit any effects in these experiments. The data suggest that (+/-)-pervilleine A hydrochloride has weak nonspecific anticholinergic and vascular antiadrenergic activities. The lack of significant cholinergic and adrenergic receptor-mediated activities may be considered advantageous for the further development of pervilleine A as a new adjuvant in cancer chemotherapy.     

Isolation and Characterization of Antineoplastic Alkaloids from Catharanthus Roseus L. Don. Cultivated in Egypt

Vinblastine and vincristine (the antileukemic agents) were isolated, in a pure form, from Catharanthus roseus L. Don., cultivated in Egypt, by several chromatographic techniques. Five modified methods for the preparation of total alkaloids were carried out. All the isolated mixtures were evaluated by HPLC and HPTLC analyses. The antineoplastic alkaloids; vinblastine and vincristine, were isolated by the use of vacuum liquid chromatographic column on silica gel : aluminium oxide (1:1) mixed bed vacuum liquid chromatography (VLC), Charcoal column, and finally purified by centrifugally accelerated radial chromatography (Chromatotrone).     

罐组逆流提取荷叶生物碱的研究

目的 采用罐组逆流提取技术提取荷叶中的荷叶生物碱并优化其工艺条件。方法 采用分光光度法测定荷叶生物碱。按L16 (44)正交设计表设计试验,分别考察提取时间、提取温度、固液比和乙醇体积分数4个因素的影响。结果 通过极差分析得出罐组逆流提取荷叶生物碱的最佳工艺条件为：提取时间25 min,提取温度80 ℃,固液比1∶50,乙醇体积分数为70%。结论 可以将罐组逆流提取技术应用于荷叶提取工程。     

黄连中生物碱有效部位纯化工艺研究

目的：用大孔吸附树脂对黄连总生物碱有效部位进行纯化工艺研究。方法：以总生物碱吸附量、含量和解吸率为考察指标,采用高效液相色谱法检测黄连中总生物碱的含量。结果：HPD722型大孔吸附树脂对黄连总生物碱有良好吸附分离性能,适宜的工艺条件为：黄连药材上样液质量浓度为100mg·ml^-1（相当于原生药）,上样体积为3BV湿树脂体积,洗脱方法为先以5BV湿树脂体积蒸馏水除去杂质,再以7BV湿树脂体积50％乙醇洗脱,收集50％乙醇洗脱部分。结论：该法简单可行,适合工业生产。