剑麻提取物的细胞毒活性研究

用溶剂萃取法对剑麻的95%乙醇提取物进行分段处理,利用MTT法测定各提取部位的体外细胞毒活性。正丁醇提取物对肿瘤细胞株K-562、SMMC-7721和SGC-7901显示有生长抑制活性,IC50值分别为5.6、23.8和26.8μg/mL,而石油醚、乙酸乙酯和水溶性部位则没有活性。     

入侵植物猫爪藤体外细胞毒活性成分的筛选分离

为了筛选分离入侵植物猫爪藤的细胞毒活性成分,采用MTT法以75%乙醇提取物的不同组分分别处理人肝癌细胞SMMC7721、Bel7402和正常肝细胞Chang Liver,对他们的体外增殖抑制率进行了研究。结果表明,总醇提物的氯仿组分对肝癌细胞表现出明显的体外增殖抑制作用,其次是石油醚组分。从氯仿萃取组分中分离出具有更强细胞毒活性的成分熊果酸。因此,入侵植物猫爪藤具有体外细胞毒活性,熊果酸是其体外细胞毒活性的主要成分之一。     

大叶山楝根的化学成分及细胞毒活性研究

该研究从大叶山楝根95%乙醇提取物的乙酸乙酯萃取物中分离得到10个化合物,经波谱解析分别鉴定为schleicheol 2(1),β-扶桑甾醇(2),fregenedadiol(3),异巴西红厚壳素(4),丁香酯素(5),表丁香酯素(6),graminone A(7),sylvatesmin(8),Z-6-十九烯酸甲酯(9),棕榈酸(10)。其中,化合物1-4、化合物7-9为首次从山楝属植物中分离得到。细胞毒活性测试结果表明,化合物1和化合物2对人胃癌细胞SGC-7901生长具有一定的抑制活性。     

香港地区红树植物资源研究(Ⅱ)——红树植物Lumnitzera racemosa(榄李)抑制植物真菌有效成分的分离与鉴定

本文对红树植物榄李(Lumnitzera racemosa)茎的95％乙醇提取物进行了抑制植物真菌(Fusarium oxysporum,Helminthosporium.sp,Stemphyllium.)效能的研究,并对其抑菌有效成份进行了分离与鉴定,研究结果表明,丹宁(tanning)(来自水相提取物)是抑菌的主要活性组份,其它还有黄酮类似物,脂肪酸等(来自于氯仿提取物)也有一些抑菌能力。     

甘草提取物的抑菌活性研究

目的:研究甘草提取物的体外抑菌活性。方法:以甘草为原料,用氯仿、乙酸乙酯、正丁醇、95%乙醇和水五种不同极性的溶剂对其进行提取。以金色葡萄球菌和大肠杆菌为代表菌种,通过纸片扩散法考察这些提取物对的抑制效果。结果:甘草提取物中不同极性成分的物质对两种菌均有一定的抑制效果,而且对金黄色葡萄球菌的抑菌活性比大肠杆菌的抑菌活性强。     

芹菜根中一种具有抗癌活性的双氨基甲酸酯

研究芹菜根(Apium graveolens L.)乙醇提取物的化学成分及其体外抗肿瘤活性。利用多种色谱方法进行分离纯化,现代波谱技术对分离得到的化合物进行结构鉴定;采用MTT法对分离出的单体化合物进行抗肿瘤实验。从芹菜根的乙醇提取物中分离得到3个单体化合物,它们的结构分别为双氨基甲酸酯AG-01 (1)佛手柑内酯(2)芹菜素(3)。化合物1为一新化合物,MTT细胞毒活性显示其对人体胃癌细胞SGC-7901和肝癌细胞BEL-7402的IC50分别为29. 6μM和32. 4μM。     

见血封喉种子中的强心苷类化合物及其细胞毒活性

从海南产见血封喉(Antiaris toxicaria (Pers.) Lesch.)种子的乙醇提取物中分离得到7个强心苷类化合物,通过波谱分析(NMR, MS, IR等),鉴定其结构分别为：杠柳苷元(1)、见血封喉阿洛糖苷(2)、见血封喉去氧阿洛糖苷(3)、毒毛旋花子苷元(4)、毒毛旋花子阿洛糖苷(5)、毒毛旋花子爪哇糖苷(6)和去葡萄糖桂竹香毒苷(7)。化合物7为首次从见血封喉种子中分离得到。细胞毒活性测试结果表明,化合物1~7均对慢性髓原白血病细胞(K562)、人胃癌细胞(SGC-7901)和人肝癌细胞(SMMC-7721)的增殖有较强的生长抑制活性。     

非洲马铃果种子的化学成分含量测定和生物活性研究

以分光光度法测定非洲马铃果种子总生物碱、总黄酮、水溶性多糖含量,MTT法测定乙醇提取物不同分离部位的细胞毒活性,以及DPPH法测定不同分离部位的抗氧化活性。结果表明,非洲马铃果种子总生物碱、总黄酮、水溶性多糖含量分别为5.70%、0.41%和3.04%;各分离部位中总生物碱的细胞毒活性最强,其对人的肝癌细胞株SMMC7721、胃癌细胞株SGC7901和正常肝细胞株Chang-liver的IC 50值分别为11.99±2.22、8.72±6.11和7.31±4.39μg·mL-1;各分离部位中正丁醇相抗氧化活性最强,IC 50值为0.268±0.002 mg·mL-1。     

烟草提取物对十一种植物病原真菌的抑制作用

采用菌丝生长速率法研究烟叶95%乙醇提取物和正己烷提取物对苹果腐烂病菌等11种植物病原真菌的抑菌活性,并通过液相色谱及气质联用色谱对烟叶提取物中多酚类、黄酮类、萜烯类等抑菌活性成分进行测定。实验结果表明,0.5 g/m L(工作浓度5 mg/m L)的两种溶剂提取物对11种病原真菌的菌丝生长均有抑制作用,其中对苹果腐烂病菌(V.mali)的抑制作用最强,且同浓度的正己烷提取物的抑菌活性优于95%乙醇提取物。根据不同材料提取物及几种纯物质溶液的抑菌特点,推测西柏三烯二醇可能是烟叶提取物中主要的抑菌活性物质。     

小桐子提取物除草活性的生物测定

为全面了解小桐子(Jatropha curcas L. )提取物的除草活性,以萝卜(Raphanus sativus L. )、苋(Amaranthus tricolor L. )、苏丹草[Sorghum sudanense (Piper) Stapf]和黑麦草(Lolium perenne L. )为实验材料,对小桐子果壳和枝叶的水、乙醇(体积分数95%)、正丁醇、乙酸乙酯、氯仿和石油醚粗提物的除草活性进行了生物测定,并从中筛选出抑制作用最强的水粗提物进行进一步的活性组分分离及其除草活性的生物测定.测定结果显示,小桐子果壳和枝叶的6种溶剂提取物(10 g·L~(-1))对供试的4种植物幼苗的根长和茎高均有不同程度的抑制作用,其中水粗提物和乙醇(体积分数95%)粗提物的抑制作用较强,且水粗提物对供试的4种植物幼苗的根长和茎高的抑制作用均在75%以上,显著高于其他溶剂粗提物(P<0.05);石油醚粗提物的抑制作用最小,均在10%以下.小桐子果壳和枝叶水粗提物的石油醚、氯仿、乙酸乙酯、正丁醇和水萃取物(10 g·L~(-1))对萝卜和苏丹草幼苗的根长和茎高均有不同程度的抑制作用,其中水、正丁醇和乙酸乙酯萃取物的抑制作用显著高于氯仿和石油醚萃取物,抑制率均在70%以上;水萃取物的抑制作用最强,抑制率均在80%以上;石油醚萃取物的抑制作用最小,抑制率均在10%以下.研究结果表明,小桐子果壳和枝叶的水粗提物具有一定的除草活性,其有效成分为极性较大的组分.     

Phytochemical composition and antimicrobial,antioxidant and cytotoxic activities of <Emphasis Type="Italic">Anchusa officinalis</Emphasis> L. extracts

The aim of this study is to examine phytochemical composition and evaluation of antimicrobial, antioxidant and cytotoxic activity of Anchusa officinalis plant extracts in different solutions: ethanol, chloroform, petroleum, acetone and ethyl acetate. A comparative analysis has shown that ethanol extract had the highest concentration of phenols (104.03?±?0.63 mgGA/g), and the highest concentration of flavonoids (30.26?±?0.40 mgRU/g). The highest concentration of the condensed tannins recorded in chloroform extract (74.65?±?0.57 mg GA/g). The ethanol extract showed the strongest antioxidant and the best antimicrobial activity as compared to all other tested extracts, while the chloroform and the acetone extracts showed the best cytotoxic activity on cell line of mouse fibroblast carcinoma (L2OB). This is the first report of citotoxic activity of extract A. officinalis plant from Balkan region on tumor cell lines. HPLC analysis of A. officinalis plant extracts confirmed that the predominant polyphenol components were: rosmarinic acid, chlorogenic acid, naringenin, lutein-glycoside and rutin.     

蓖麻根提取物对HepG2,NCI-H460和SGC-7901细胞增殖及凋亡作用的影响

探讨蓖麻根不同提取物对肝癌HepG2细胞株、肺癌NCI-H460细胞株和胃癌SGC-7901细胞株增殖及其凋亡的影响.采用MTT法检测蓖麻根不同提取物处理48h、72h对HepG2细胞、NCI-H460细胞和SGC-7901细胞增殖的抑制率;Hoechst 33258荧光染料染色法观察HepG2细胞凋亡,流式细胞术检测...     

白黎芦醇对胃癌SGC 一7 901 细胞V EGF 表达的影响

目的：探讨白藜芦醇（resveratrol,Res）在体外对胃癌SGC-7901细胞VEGF表达的影响。方法：体外培养胃癌SGC-7901细胞,MTT法检测白藜芦醇对SGC-7901细胞的增殖抑制作用,RT—PCR方法检测VEGFmRNA表达,免疫细胞化学检测VEGF蛋白的表达。结果：白藜芦醇呈时间剂量性抑制胃癌细胞SGC7901的增殖;胃癌SGC-7901细胞高水平表达VEGF,白藜芦醇能显著降低胃癌SGC-7901细胞VEGFmRNA和蛋白表达。结论：白藜芦醇可以下调胃癌SGC-7901细胞VEGF的表达,抑制胃癌细胞的增殖。     

海洋真菌Penicillium sp. WP-13次级代谢产物研究

本研究分析了海洋真菌Penicillium sp. WP-13的活性次级代谢产物。采用多种柱色谱技术对其发酵液的乙酸乙酯提取物进行分离纯化;根据波谱数据和理化常数分析,并结合文献比对鉴定单体化合物的结构;采用MTT法测定化合物对肿瘤细胞的细胞毒活性。从Penicillium sp. WP-13发酵液的乙酸乙酯提取物中分离鉴定了5个单体化合物,其中2个内酯类化合物为1-hydroxy-3,10-dimethoxy- 8-methyl-6,11-dioxo-6,11-dihydrodibenzo[b,e]oxepine-9-carboxylic acid (1)和1,8-dihydroxy-10-methoxy- 3-methyl-dibenzo[b,e]oxepine-6,11-dione (2);3个蒽醌类化合物为endocrocin methyl ester (3)、2-chloro-1,3,8-trihydroxy-6-methyl-9,10-anthracenedione (4)和emodin (5)。活性测试结果显示,化合物3和5均对人慢性髓原白血病细胞株K562、人肝癌细胞株BEL-7402、人胃癌细胞株SGC-7901和人宫颈癌细胞株HeLa具有一定的细胞毒活性。化合物1为新化合物,化合物3的核磁数据为首次报道,化合物1-4均首次分离自青霉属真菌。     

海南大风子活性成分研究

用色谱技术对海南大风子(Hydnocarpus hainanensis (Merr.) Sleum.)枝条的乙醇提取物进行分离纯化,从中分离得到了6个化合物,经波谱数据分析与文献数据对照,分别鉴定为eoniferaldehyde (1)、mulberroside C(2)、mulberrofuran G(3)、mulb...     

Design,synthesis and antitumor activities of novel 7-arylseleno-7-deoxydaunomycinone derivatives

7-Arylseleno-7-deoxydaunomycinone derivatives 3a–e and 7-thiophenyl-7-deoxydaunomycinones (7 and 8) were synthesized and the antitumor activities of them were evaluated against human stomach cancer SGC-7901 and human leukaemia HL60. The cytotoxic assay show that seleno daunomycinone derivatives are much better inhibitory activity than thiodaunomycinone and the structure–activity relationship was discussed. 7-Deoxydaunomycinone 4 was obtained when selenophenols were used in excess and the possible mechanism was proposed.     

Xanthatin and xanthinosin from the burs of Xanthium strumarium L. as potential anticancer agents

Xanthatin and xanthinosin, 2 sesquiterpene lactones isolated from the burs of Xanthiun strumarium L. (cocklebur), showed moderate to high in vitro cytotoxic activity in the human cancer cell lines WiDr ATCC (colon), MDA-MB-231 ATCC (breast), and NCI-417 (lung). Xanthatin and xanthinosin were purified as the result of a multi-screening bioassay-guided study of wild plant species of the family Asteraceae, collected from various sites in Saskatchewan, Canada. Seventy-five extracts at a single concentration of 100 microg/mL were evaluated for in vitro cytotoxicity to the human cancer cell lines used. The chloroform extract of Carduus nutans L. (nodding thistle) aerial parts (IC50, 9.3 microg/mL) and the hexane extract of Echinacea angustifolia DC. (narrow-leaved purple coneflower) root (IC50, 4.0 microg/mL) were moderately to highly cytotoxic to the lung cancer cell line. The chloroform extracts of X. strumarium L. burs and Tanacetum vulgare L. (tansy) aerial parts exhibited the highest cytotoxicity for all cell lines tested; their IC50 values, obtained from multidose testing, ranged from 0.1 to 6.2 microg/mL (X. strumarium) and from 2.4 to 9.1 microg/mL (T. vulgare). Further purification of the chloroform fraction of X. strumarium yielded xanthatin and xanthinosin in high yields. This is the first time that these compounds have been reported in the burs of X. strumarium. Their IC50 values are also reported herein.     

A novel cytotoxic ternary copper(II) complex of 1,10-phenanthroline and L-threonine with DNA nuclease activity

A novel ternary copper(II) complex, [Cu(phen)(L-Thr)(H2O)](ClO4) (phen=1,10-phenanthroline, L-Thr=L-threonine), has been synthesized and structurally characterized. The complex crystallized in a triclinic system with space group P1 , a=7.526(15) A, b=11.651(2) A, c=12.127(2) A, alpha=115.41(3) degrees , beta=102.34(3) degrees and gamma=91.33(3) degrees . The copper(II) center is situated in a distorted square-pyramidal geometry. At a concentration of 10(-6) mol L(-1), the complex exhibited potent cytotoxic effects against human leukemia cell line HL-60 and human stomach cancer cell line SGC-7901 with inhibition rates of over 90%, however, less pronounced effects were observed for human liver carcinoma cell line BEL-7402 and human non-small-cell lung cancer cell line A-549. The complex was shown to bind DNA by intercalation and cleave pBR322 DNA in the presence of ascorbate.     

3-(3-Methoxyphenyl)-6-(3-amino-4-methoxyphenyl)-7H-[1,2,4] triazolo [3,4-b][1,3,4] thiadiazine,a novel tubulin inhibitor,evokes G2/M cell cycle arrest and apoptosis in SGC-7901 and HeLa cells

Gastric cancer and cervical cancer are two major malignant tumors that threaten human health. The novel chemotherapeutic drugs are needed urgently to treat gastric cancer and cervical cancer with high anticancer activity and metabolic stability. Previously we have reported the synthesis, characterization and identification of a novel combretastatin A-4 analog, 3-(3-methoxyphenyl)-6-(3-amino-4- methoxyphenyl) -7H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazine (XSD-7). In this study, we sought to investigate its anticancer mechanisms in a human gastric cancer cell line (SGC-7901 cells) and human cervical carcinoma cell line (HeLa cells). The 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay showed that XSD-7 induced cytotoxicity in SGC-7901 and HeLa cells with inhibitory concentration 50 values of 0.11 ± 0.03 and 0.12 ± 0.05 µM, respectively. Immunofluorescence studies proved that XSD-7 inhibited microtubule polymerization during cell division in SGC-7901 and HeLa cells. Then, these cells were arrested at G2/M cell cycle and subsequently progressed into apoptosis. In further study, mitochondrial membrane potential analysis and Western blot analysis demonstrated that XSD-7 treatment-induced SGC-7901 cell apoptosis via both the mitochondria-mediated pathway and the death receptor-mediated pathway. In contrast, XSD-7 induced apoptosis in HeLa cells mainly via the mitochondria-mediated pathway. Hence, our data indicate that XSD-7 exerted antiproliferative activity by disrupting microtubule dynamics, leading to cell cycle arrest, and eventually inducing cell apoptosis. XSD-7 with novel structure has the potential to be developed for therapeutic treatment of gastric cancer and cervical cancer.     

In-vitro antibacterial,antioxidant potentials and cytotoxic activity of the leaves of Tridax procumbens

The present study explored the phytochemicals, antibacterial, antioxidant and cytotoxic effect of Tridax procumbens leaves. The leaves were dried and extracted with various organic solvents. The leaves contained the phytochemicals such as alkaloids, carbohydrates, polyphenols and tannins respectively. Antimicrobial potentials of the extracts were determined by performing the disc diffusion techniques. Results revealed that different organic solvents extracts namely methanol, ethanol and ethyl acetate extracts documented comparatively good activity against the studied microbial strains. The methanol extract of leaves of T. procumbens showed combatively better antioxidant potential. The tested plant leaf extract showed high activity against human lung cancer cells than breast cancer cell lines. 250 µg/ml plants extract showed 84 ± 2.8% toxicity against human lung cancer cells.