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Evaluation of the Immuno-modulating Activity of Some Active Principles Isolated from the Fruiting Bodies of Antrodia camphorata 樟树子实体中部分活性成分的免疫调节活性评价
Pub Date : 2003-10-01 DOI: 10.7019/CPJ.200310.0313
Yuh-Chiang Shen, Chieh‐fu Chen, Yea-Hwey Wang, T. Chang, C. Chou
We have previously isolated some lanostane- and ergostane-type compounds from the fruiting bodies of Antrodia camphorata and Antrodia sp. in our laboratory. In this study, an ergostane-type chemical, named antcin C (Ant C), and three lanostane-type chemicals including sulphurenic acid (SA), eburicoic acid (EA), and dehydroeburicoic acid (DeEA), were examined for their immunomodulating effect against reactive oxygen species (ROS) production induced by N-formyl-meth-ionyl-leucyl-phenylalanine (fMLP) or phorbol-1 2-myristate-1 3-acetate (PMA) in peripheral human neutrophils (PMN) or mononuclear cells (MNC). ROS production by activated-leukocytes is an important inflammatory mediator and also signals immuno-responses. Pretreatment with these four compounds concentration-dependently diminished fMLP- and PMA-induced ROS production in PMN, as measured by lucigenin-amplified chemiluminescence, with IC50 values (jiM) of 16.9±4.2, 43.9±14 and 144.8±13 for Ant C, EA and DeEA, respectively. These compounds were relatively less effective in the inhibition of ROS production by MNC with IC50 values around 200 jiM. The anti-oxidative actions of these drugs were not due to cytotoxic effects because no significant difference in cell viability was observed as compared to the vehicle control group. In summary, our data suggests that inhibition of ROS production in leukocytes by these active principles could be responsible for the immuno-modulating effects of A. camphorata.
我们已经在实验室中从樟树和樟树的子实体中分离出了一些羊毛甾烷和麦角甾烷类化合物。在本研究中,我们研究了一种名为antcin C(蚂蚁C)的麦角甾类化学物质,以及三种麦角甾类化学物质,包括硫酸(SA)、eburicoic酸(EA)和脱氢eburicoic酸(DeEA),它们对人类外周中性粒细胞(PMN)或单核细胞(MNC)中n -甲酰基-甲基-ionyl-leucyl-苯丙氨酸(fMLP)或phorol - 2-肉豆酸酯-1 - 3-乙酸(PMA)诱导的活性氧(ROS)产生的免疫调节作用。激活的白细胞产生ROS是一种重要的炎症介质,也是免疫反应的信号。通过荧光素放大的化学发光测量,这四种化合物的预处理可以减少fMLP-和pma诱导的PMN中ROS的产生,对Ant C、EA和DeEA的IC50值(jiM)分别为16.9±4.2、43.9±14和144.8±13。这些化合物对MNC产生ROS的抑制作用相对较弱,IC50值约为200 jiM。这些药物的抗氧化作用不是由于细胞毒性作用,因为与对照组相比,细胞活力没有显著差异。总之,我们的数据表明,通过这些活性原理抑制白细胞中ROS的产生可能是樟树免疫调节作用的原因。
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引用次数: 18
Synthesis of antioxidative moscatilin and its bibenzyl derivatives 抗氧化莫斯卡汀及其联苯衍生物的合成
Pub Date : 2003-10-01 DOI: 10.7019/CPJ.200310.0381
Chien‐Chih Chen, Yu-Ling Huang, Y. Shiao, Ray-Ling Huang, Tai-Ti Fu, Chien-Chang Shen
Moscatilin and a series of bib enzyl derivatives were synthesized from appropriate aromatic a1dehydes and phosphonium salts through the Wittig reaction. The antioxidative and cytotoxic activities of these bibenzyl derivatives were evaluated.
以合适的芳醛和磷盐为原料,通过Wittig反应合成了mosscatilin和一系列bib酶衍生物。对这些联苯衍生物的抗氧化活性和细胞毒活性进行了评价。
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引用次数: 1
Quantitatively Evaluation of Bioactive Components of Evodia Rutaecarpa (Tetradium Ruticarpum) in Different Harvesting Times 不同采收期吴茱萸生物活性成分的定量评价
Pub Date : 2003-10-01 DOI: 10.7019/CPJ.200310.0305
H. Ko, K. Chen, C. Chou, Yi-Ju Chang, Guei‐Jane Wang, Chieh‐fu Chen
In this study, a high performance liquid chromatographic method was developed for simultaneous determination of four bioactive components in T ruticarpum collecting from various flowering seasons. Our results demonstrate that the component synephrine (IV) was only found in flower bud and flower. During the season of flower and unripe fruit, the contents of dehydroevodiamine (I), evodiamine (II), and rutaecarpine (III) were found to increase with the development time of flower and fruit, upon ripening of the fruit, the amount of these three components were found to be decreasing with time. Therefore, the time of harvesting is an important factor to control the quality of herbal drugs.
本研究建立了高效液相色谱法同时测定不同花期紫穗槐中4种生物活性成分的方法。结果表明,辛弗林(IV)只存在于花蕾和花中。在花季和未熟果期,脱氢evolodiamine (I)、evolodiamine (II)和rutaecarpine (III)的含量随着花和果实发育时间的延长而增加,果实成熟后,这三种成分的含量随着时间的延长而减少。因此,采收时间是控制药材质量的重要因素。
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引用次数: 5
Characterization of the Water Soluble Fraction from the Root Extract of Eurycoma Longifolia 长叶Eurycoma Longifolia根提取物水溶性组分的表征
Pub Date : 2003-08-01 DOI: 10.7019/CPJ.200308.0257
P. Kuo, A. G. Damu, Tian-Shung Wu
Investigation of the chemical composition of the water soluble fraction of the methanolic extract of the roots of Eurycoma longifolia, a medicinal plant popularly known as ”Tongkat Ali”, afforded three quassinoid diterpenoids, sugar and amino acid fractions. The sugar fraction was analyzed for its qualitative and quantitative carbohydrate con tent and glucose and fructose were identified. Quantification of these natural free sugars was achieved by HPLC using refractive index detection. The total amino acid concentration and the amino acid pattern, i.e., the relative proportion of each amino acid to the total amino acids, in the amino acid fraction were analyzed using an amino acid analyzer. Twenty five amino acids were identified. The predominant amino acids were alanine, proline, arginine, and serine summing up to 53.39% of the total. The isolated quassinoid diterpenes exhibited potent cytotoxicity and antimalarial activity.
对药用植物“东革阿里”长叶Eurycoma longifolia根甲醇提取物水溶性组分的化学成分进行了研究,得到了3个准萜类化合物、糖和氨基酸组分。对其糖组分进行了定性和定量分析,并对葡萄糖和果糖进行了鉴定。利用高效液相色谱法测定这些天然游离糖的含量。用氨基酸分析仪分析氨基酸组分中总氨基酸浓度和氨基酸格局,即每种氨基酸占总氨基酸的相对比例。鉴定出25种氨基酸。主要氨基酸为丙氨酸、脯氨酸、精氨酸和丝氨酸,占总氨基酸的53.39%。分离得到的准番石榴二萜具有较强的细胞毒性和抗疟活性。
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引用次数: 2
Alkyl Phenols from the Leaves of Formosan Ardisia Virens 台湾紫荆叶中的烷基酚
Pub Date : 2003-08-01 DOI: 10.7019/CPJ.200308.0273
A. Dixit, Jih-Jung Chen, T. Ishikawa, I. Tsai, I. Chen
Five new alkyl phenols, virenols A~E (1~5), were isolated from the leaves of Ardisia virens. The structures of these compounds were determined by spectral analysis.
从紫荆叶中分离到5个新的烷基酚,分别为毒酚A~E(1~5)。通过光谱分析确定了这些化合物的结构。
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引用次数: 4
Modern research routes to new medicines from Chinese Materia Medica 从中药到新药的现代研究路线
Pub Date : 2003-08-01 DOI: 10.7019/CPJ.200308.0221
K. Lee
Chinese Materia Medica (CMM), in eluding herbal and traditional medicines, has been used for centuries by Asian peoples to treat disease and main tam health. CMM has also played an important role as the basis of numerous new leads for modern ”single-component” drug discovery and development. How ever, modern scientific technology should be applied not only to the discovery of single bioactive lead com pounds, but also to the development of active fractions and effective and safe herbal prescriptions as new medicines and high quality dietary supplements. This review will discuss modern research routes to wards the discovery and development of bioactive natural products and their analogs as new medicines, with emphasis on those single pure com pounds developed in the author's laboratory as anticancer and anti-AIDS clinical trials candidates. In addition, this brief re view will also discuss the quality control methods for the production of standardized new medicines, as well as the introduction of modern research technologies, such as proteomics, for the generation of new medicines from CMM in the post genomic era.
中药(CMM),包括草药和传统药物,几个世纪以来一直被亚洲人民用来治疗疾病和主要团队健康。CMM作为现代“单组分”药物发现和开发的许多新线索的基础也发挥了重要作用。然而,现代科学技术不仅应该应用于发现单一的生物活性铅化合物,还应该应用于开发有效成分和有效安全的草药处方,作为新药和高质量的膳食补充剂。本文将讨论生物活性天然产物及其类似物作为新药的发现和开发的现代研究路线,重点介绍作者实验室开发的单一纯化合物作为抗癌和抗艾滋病临床试验的候选药物。此外,这篇简短的综述还将讨论标准化新药生产的质量控制方法,以及引入现代研究技术,如蛋白质组学,在后基因组时代从CMM产生新药。
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引用次数: 0
Antitumor Agents 225. Acrofoliones A and B, Two Novel Cytotoxic Acetophenone Dimers from Acronychia Trifoliolata 抗肿瘤药物三叶草中两种新的细胞毒性苯乙酮二聚体Acrofoliones A和B
Pub Date : 2003-08-01 DOI: 10.7019/CPJ.200308.0239
M. Oyama, K. Bastow, Y. Tachibana, Y. Shirataki, S. Yamaguchi, G. Cragg, Tian-Shung Wu, K. Lee
Two novel prenylated acetophenone dimers, acrofoliones A (1) and B (2), were isolated from Acronychia trifoliolata (Rutaceae) to gether with a known cytotoxic principle, acrovestone (3). The new structures were determined from NMR and MS spectroscopic anal y sis. Com pounds 1 and 2 showed only moderate cytotoxicity against HCT-8 and KB cells with ED50 values of 4.3 and 4.8 μg/mL, respectively; how ever, both compounds demonstrated selectivity against MOLT-4 and RPMI-8225 leukemia cell lines.
从芦花科(rutacae)中分离到两个新的烯丙基化苯乙酮二聚体acrofoliones A(1)和B(2),并与已知的细胞毒性原理acrovestone(3)进行了核磁共振和质谱分析。Com磅1和2对HCT-8和KB细胞仅表现出中等的细胞毒性,ED50值分别为4.3和4.8 μg/mL;然而,两种化合物对MOLT-4和RPMI-8225白血病细胞系均表现出选择性。
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引用次数: 10
Chemical constituents from the roots of Cassia fistula L. 决明子根的化学成分。
Pub Date : 2003-08-01 DOI: 10.7019/CPJ.200308.0231
Ching-Kuo Lee, Y. Chung, F. Hsu, Y. Kuo
The chemical constituents in the roots of Cassia fistula L. were investigated with column chromatography. Nine teen compounds including seven anthraquinones, chrysophanol (1), physcion (2), emodin (3), aloe-emodin (4), 11-acetylaloe-emodin (5), rhein (6), citreorosein (7); four flavan-3-ols, (-)-epiafzelechin (8), (+)-afzelechin (9), (-)-epicatechin (10), (+)-catechin (11); three sterols, a mixture of β-sitosterol (12) and stigmasterol (13), β-sitosterol-3-O-β-glucopyanoside (14); one triterpene, lupeol (15); and four gly cer ides, a mixture of glycerol-1-tetraeicosanoate (16) and glycerol-1-pentaeicosanoate (17), trimyristin (18), and glyceryl trilinolate (19) were determined by spectroscopic analysis.
采用柱层析法对决明子根中的化学成分进行了研究。9种化合物,包括7种蒽醌类化合物,大黄酚(1),物理(2),大黄素(3),芦荟大黄素(4),11-乙酰芦荟大黄素(5),大黄素(6),柠檬酸酪蛋白(7);四个flavan-3-ols, (-) -epiafzelechin (8), (+) -afzelechin(9)、(-)表儿茶素(10)、(+)儿茶素(11);三种甾醇,β-谷甾醇(12)和豆甾醇(13)的混合物,β-谷甾醇-3- 0 -β-葡萄糖苷(14);一种三萜,芦皮醇(15);并通过光谱分析确定了四种甘油三酯,即甘油-1-四二十酸酯(16)和甘油-1-五二十酸酯(17)的混合物,三嘧菌素(18)和甘油三酯(19)。
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引用次数: 3
The Cytotoxic Constitunets of Euphorbia Makinoi 大戟的细胞毒性成分
Pub Date : 2003-08-01 DOI: 10.7019/CPJ.200308.0267
J. Weng, H. Su, M. Yen, S. Won, Chun-nan Lin
One new triterpene, cycloart-24β-methoxy-3β-ol (1), and seven known com pounds, were isolated from the whole herb of Euphorbia makinoi. Their structures were established by spectral methods, and their cytotoxic activities were evaluated against three different cell lines. Com pound 1 showed marginal cytotoxic activity against the three human cancer cell lines while 3 showed marginal cytotoxic activity against Hep 3B and HT-29 cells in vitro.
从大戟(Euphorbia makinoi)全草中分离到1个新的三萜环亚酮-24β-甲氧基-3β-醇(1)和7个已知化合物。用光谱法确定了它们的结构,并对三种不同细胞系进行了细胞毒活性评价。compound 1对3种人类癌细胞系均表现出边缘性细胞毒活性,而3对Hep 3B和HT-29细胞均表现出边缘性细胞毒活性。
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引用次数: 1
Expression of the Kappa (K) Light Chain of Mouse Anticreatine Kinase-M (MAK33) Antibody in the Yeast Hansenula Polymorpha 小鼠抗尿酸激酶- m (MAK33)抗体Kappa (K)轻链在酵母多态羊肠菌中的表达
Pub Date : 2003-06-01 DOI: 10.7019/CPJ.200306.0197
H. Abdel-salam, G. Enan, F. Serry, M. Ghonaim, Hemmat K. Abdel-Latif, C. Hollenberg
An expression plasmid was constructed and transformed to the methylotrophic yeast Hansenulapolyinorpha to produce the kappa chain peptide of IgG antibody (MAK33). Hansenula polymorpha appears to be one of the most efficient host cells for the expression of genetically engineered antibody genes. Although the rate of transformation of this yeast by polyethylene glycol was low (3-5 cells/1.0μg plasmid DNA), yet the transformants showed high mitotic stability for more than 100 generations. The expression plasmid was integrated within the yeast genome at one or more integrations site(s) with low and multicopy-number plasmids via a non-homologous integration mechanism. An N-terminal glucoamylase gene fragment was linked to the light chain (kappa) gene of the Fab derivative of the MAK33 antibody. Prepro-alpha factor of the yeast Saceharomyces cerevisiae was inserted into the plasmid between the glucoamylase and light chain genes as a secretion signal sequence for the light chain peptide. The kappa chain was produced at 50mg/L free protein in the culture medium and 500mg/L entrapped within the cells, amounting to 550mg/L and representing about 10% of the total cell protein. The prepro-a factor was shown to be incompletely processed in Hansenulapolyinorpha and the pro-segment accompanied the light chain peptide.
构建表达质粒,转化到甲基营养酵母中,产生IgG抗体kappa链肽(MAK33)。多态汉氏菌似乎是表达基因工程抗体基因最有效的宿主细胞之一。虽然聚乙二醇对该酵母的转化率较低(3-5个细胞/1.0μg质粒DNA),但转化子在100代以上表现出较高的有丝分裂稳定性。通过非同源整合机制,将表达质粒与低拷贝数质粒和多拷贝数质粒整合在酵母基因组的一个或多个整合位点上。一个n端葡萄糖淀粉酶基因片段连接到MAK33抗体Fab衍生物的轻链(kappa)基因上。将酵母(Saceharomyces cerevisiae)的pre - α因子插入到糖淀粉酶与轻链基因之间的质粒中作为轻链肽的分泌信号序列。培养基中游离蛋白为50mg/L,细胞内包埋蛋白为500mg/L时产生kappa链,总量为550mg/L,约占细胞总蛋白的10%。结果表明,前a因子在汉参中加工不完全,前段伴随轻链肽。
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引用次数: 0
期刊
The Chinese Pharmaceutical Journal
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