白背叶提取物A对人肿瘤细胞增殖的抑制作用研究

目的 观察白背叶提取物A对肿瘤细胞增殖的抑制作用.方法 采用四唑盐比色实验(MTT法),以半数抑制浓度(IC_50)为评价抗肿瘤活性强度的指标,分别对4种常见的人恶性肿瘤细胞进行抗肿瘤活性的筛选.结果 白背叶提取物A在浓度为5 μg/ml时对人胃癌细胞SGC-7901,人肺癌细胞A549有明显抑制作用(P<0.05或P<0.01),其IC_50分别为27.14 μg/ml,33.08 μg/ml;在浓度为20 μg/ml 时对人结肠癌细胞LoVo有抑制作用(P<0.05),其IC_(50)为36.82 μg/ml;在浓度为40 μg/ml 时对人肝癌细胞Bel-7404有抑制作用(P<0.05),其IC_50为37.70μg/ml.结论 白背叶提取物A对以上4种肿瘤细胞的增殖均有抑制作用.     

三叶青脂溶性提取物对A375细胞增殖及黑色素合成的影响

目的探讨三叶青三氯甲烷提取物对人恶性黑色素瘤A375细胞增殖、酪氨酸酶活性及黑色素合成的影响。方法采用MTT比色法,测定不同浓度三叶青三氯甲烷提取物对A375细胞体外抑制作用;比色法测定酪氨酸酶活性和黑色素含量;采用光学显微镜法观察其对细胞形态的影响。结果三叶青三氯甲烷提取物在6～500μg/ml浓度范围内对A375细胞增殖有显著的抑制作用(P<0.01),且呈时间-剂量依赖性;浓度小于50μg/ml时,对酪氨酸酶活性和黑色素合成抑制有增加趋势;在100～500μg/ml时,对A375肿瘤细胞有较强的抑制作用;光学显微镜下可见典型凋亡细胞形态学改变。结论三叶青三氯甲烷提取物对A375细胞增殖、酪氨酸酶活性及黑色素合成具有抑制作用。     

白背叶提取物A的体外抗肿瘤机制的研究

目的 研究白背叶提取物A对SGC-7901人胃癌细胞增殖抑制作用的发生机制.方法 采用RT-PCR检测白背叶提取物A对SGC-7901人胃癌细胞抑癌基因p53,癌基因Bcl-2表达的影响.结果 不同浓度的白背叶提取物A作用于SGC-7901细胞后:p53的mRNA表达均有增强,10,20,40 μg/ml浓度的p53 mRNA表达均显著高于空白组(P<0.01);各实验浓度的白背叶提取物A作用下SGC-7901细胞的Bcl-2 mRNA表达均有降低,与空白组相比具有显著性差异(P<0.01),且该作用有一定的剂量依赖性.结论 对抑癌基因p53、癌基因Bcl-2表达的影响是白背叶提取物A抗肿瘤的作用机制之一.     

藤茶蛇葡萄素对人卵巢癌细胞和人恶性黑色素瘤细胞增殖的抑制作用

目的:探讨藤茶蛇葡萄素(APS)的体外抗肿瘤作用。方法:采用MTT法观察APS对人卵巢癌细胞SK-OV-3和人恶性黑色素瘤A375细胞抑制作用。结果:APS能明显抑制体外培养的SK-OV-3、A375细胞的生长。MTT结果显示,APS对SK-OV-3细胞的IC50为24.24μg/ml;对A375细胞的IC50为18.29μg/ml。结论:APS对体外SK-OV-3、A375细胞的生长均有明显的抑制作用。     

多蕊蛇菰甲醇提取物体外抗肿瘤活性研究

目的:研究多蕊蛇菰甲醇提取物的体外抗肿瘤活性。方法:采用MTT法检测多蕊蛇菰甲醇提取物对人肝癌细胞Bel-7402和宫颈癌细胞Hela生长增殖的影响。结果:多蕊蛇菰甲醇提取物对人肝癌细胞Bel-7402和宫颈癌细胞Hela的细胞毒性IC50值分别为22.77μg/m L和28.42μg/m L。结论:多蕊蛇菰甲醇提取物对人肝癌细胞Bel-7402和宫颈癌细胞Hela均有抑制作用,并呈现出剂量-效应关系;多蕊蛇菰甲醇提取物具有显著抗肿瘤活性。     

薏苡茎叶提取物的体外抗肿瘤活性研究

目的研究薏苡茎、叶不同提取物的体外抗肿瘤活性。方法分别用水、乙醇、甲醇、丙酮和氯仿等5种不同溶剂对薏苡茎、叶进行回流提取,采用MTT法测定不同浓度的薏苡茎、叶水提取液、乙醇提取液、甲醇提取液、丙酮提取液、氯仿提取液对Hela细胞增殖的影响,并计算其IC50。结果不同溶剂的薏苡茎、叶提取液对Hela细胞增殖均有一定的抑制作用,其中以水提取液、乙醇提取液对Hela细胞增殖抑制作用最明显,茎水提取液、叶水提取液、茎乙醇提取液和叶乙醇提取液的IC50分别为0.134 3,0.126 6,0.348 2,0.181 8 g/ml,叶提取物活性高于茎提取物活性。结论薏苡茎、叶提取物能抑制人宫颈癌Hela细胞的增殖,具有抗癌活性。     

开口箭提取物体外抗肿瘤实验研究

目的：探讨开口箭提取物体外抗肿瘤作用。方法：采用四甲基偶氮唑盐（MTT）比色法。结果：开口箭提取物、总皂苷、30%乙醇洗脱部分和70%乙醇洗脱部分对人宫颈癌Hela细胞和人鼻咽癌CNE-1细胞的抑制作用明显,与阴性对照组比差异有显著性（P〈0.05,P〈0.01）,对Hela细胞的IC50分别为114.99μg/m l、72.25μg/m l、39.40μg/m l和45.82μg/m l,对CNE-1细胞的IC50分别为106.82μg/m l、89.75μg/m l、60.72μg/m l和64.45μg/m l。结论：开口箭提取物体外有抗肿瘤作用。。     

红缘拟层孔菌子实体中抗肿瘤活性成分研究

目的对红缘拟层孔菌Fomitopsis pinicola子实体的石油醚提取物、氯仿提取物、水层提取物和氯仿提取物中获得的化合物A(3-乙酰氧基-8,24-羊毛甾二烯-21-酸)进行了体内外抗肿瘤活性和细胞凋亡实验研究。方法通过测定脾脏指数、胸腺指数以及血清中白介素-2(IL-2)的含量,检测了各提取物对荷瘤小鼠免疫功能的影响。结果氯仿提取物和化合物A对H22荷瘤小鼠具有较高的抑瘤率,当氯仿提取物剂量为200 mg.kg-1.d-1时,抑瘤率为52.97%,胸腺指数明显高于对照组和环磷酰胺(CTX)组(P<0.05),而接近于正常组(P>0.05);脾脏指数接近于对照组和CTX组而明显高于正常组(P<0.01);IL-2的含量明显升高;化合物A具有较好的抗肿瘤作用,各剂量组之间存在良好的剂量关系;且同对照组相比存在显著性差异(P<0.01);在剂量为10mg.kg-1.d-1时,抑瘤率最高可达到52.31%。体外实验研究结果表明化合物A对人肝癌细胞SMMC-7721和人乳腺癌细胞MCF-7均具有良好的抑制作用,其抑制率最大分别为77.63%和90.29%,IC50分别为213.80μg/ml和123.03μg/ml。化合物A作用后的细胞凋亡率仅为23.2%,接近阴性对照组的20.9%,促进细胞凋亡效果不明显。结论结合体内外实验可推断化合物A(3-乙酰氧基-8,24-羊毛甾二烯-21-酸)为红缘拟层孔菌抗肿瘤活性成分之一,提高机体免疫活性可能是其抗肿瘤作用的机理之一。     

透骨草提取物对肿瘤细胞体外增殖的影响

目的:探讨透骨草提取物对人卵巢癌SK-OV-3细胞、人乳腺癌MCF-7细胞、人宫颈癌Hela细胞、人肝癌HepG-2细胞、人肺癌A549细胞体外增殖的影响。方法:用不同浓度的透骨草提取物分别处理肿瘤细胞,采用MTT法和集落形成试验观察透骨草提取物对肿瘤细胞体外增殖的影响。结果:3.125～100μg/mL透骨草提取物处理的肿瘤细胞增殖抑制率与对照组相比显著增加(P<0.05)。3.125～100μg/mL透骨草提取物处理的肿瘤细胞集落形成率与对照组相比显著降低(P<0.05)。结论:透骨草提取物对人卵巢癌SK-OV-3细胞、人乳腺癌MCF-7细胞、人宫颈癌胞Hela细、人肝癌HepG-2细胞、人肺癌A549细胞增殖有显著的抑制作用,且呈一定的剂量依赖性。     

毛叶黄杞提取物对人肝癌细胞增殖抑制作用的实验研究

目的:探讨毛叶黄杞体外抗肿瘤的作用。方法:以MTT法观察毛叶黄杞对人肝癌BEL-7404细胞的体外抑制作用。结果:毛叶黄杞终浓度为50、33.33、22.22、14.81、9.88μg/ml时,均能有效地抑制体外培养的BEL-7404细胞的生长,与细胞对照组比较,差异有显著性意义(P<0.01),MTT法IC50为27.05μg/ml。结论:毛叶黄杞提取物对体外培养的BEL-7404细胞有抑制作用。     

In vitro anti-proliferative and antioxidant studies on Devil's Club Oplopanax horridus

Devil's Club, Oplopanax horridus (OH), is a widely used folk medicine in Alaska and British Columbia for treating a variety of ailments including arthritis, fever and diabetes. HPLC profiling shows that numerous compounds are present in the 70% ethanolic extract of OH dry root bark powder. OH extract inhibited K562, HL60, MCF7 and MDA-MB-468 cell growth with the 50% inhibition (IC(50)) estimated at 1/2700, 1/1700, 1/500 and 1/2500 dilutions, respectively. Non-cytotoxic concentrations (相似文献   

In vitro culture studies of Sutherlandia frutescens on human tumor cell lines

Sutherlandia frutescens is a South African herb used traditionally by the natives to treat cancer, and more recently to improve the overall health in HIV/AIDS patients. Gas chromatography/mass spectrometer profiling and liquid chromatographic/mass spectral investigation confirmed and quantified the presence of canavanine, GABA and arginine in the herbal preparation used in this study. In vitro study demonstrated a concentration dependent effect of Sutherlandia on several tumor cell lines, with 50% inhibition (IC50) of proliferation of MCF7, MDA-MB-468, Jurkat and HL60 cells at 1/250, 1/200, 1/150 and 1/200 dilutions, respectively. Sutherlandia treatment did not induce HL60 differentiation along the macrophage/monocyte or granulocyte lineage. It demonstrated antioxidant activity in reducing free radical cations with an estimated activity of 0.5 microl of Sutherlandia extract equivalent to that of 10 microM of Trolox. However, it did not significantly suppress lipopolysaccharide stimulated nitric oxide production by murine macrophage/monocyte RAW 264.7 cells, nor did it significantly inhibit IL-1beta and TNF-alpha mRNA expression in RAW 264.7 cells. In conclusion, Sutherlandia ethanolic extract showed a concentration dependent antiproliferative effect on several human tumor cell lines but did not show significant antioxidant effects. Further studies are needed to explore the activities of this multipurpose South African herbal preparation.     

Cytotoxic sesquiterpenoids from the ethanol extract of fruits of Celastrus orbiculatus

AIM OF THE STUDY: To investigate the cytotoxic compounds against human melanoma A375-S2 and human cervical carcinoma Hela cell lines from the fruits of Celastrus orbiculatus. MATERIALS AND METHODS: The ethanol extract of the fruits of C. orbiculatus was found to exhibit significant cytotoxic activity. After partition, the column chromatography and Semi-preparative HPLC were used for activity guided fractionation from the active petroleum ether-soluble part. NMR and ESI-MS spectra for structure analysis were recorded on spectrometers, respectively. The cytotoxic activities of the isolated compounds were determined using the MTT assay. RESULTS: Four sesquiterpenoids (1-4) were isolated by activity guided fractionation from the ethanol extract of the fruits of C. orbiculatus. Compounds 1-3 exhibited promising cytotoxicities against the Hela cells and A375-S2 cells. The cytotoxic activities of compounds 1-3 seemed to be dose-dependent, which exhibited more potent inhibition for the proliferation of two cell lines when increased the concentrations of every compounds. Among these compounds, compound 2 showed most cytotoxicities against either Hela cells or the A375-S2 cells. CONCLUSIONS: The cytotoxic activity of the ethanol extract of fruits of C. orbiculatus against human melanoma A375-S2 and human cervical carcinoma Hela cells due to its content of sesquiterpenoids, supports its potential therapeutic value for the treatment of tumor.     

紫甘蓝提取液对人乳腺癌细胞生长和迁移的抑制作用

目的:探讨紫甘蓝提取物对乳腺癌细胞MCF7生长和迁移的抑制作用。方法:应用MTT法检测不同浓度紫甘蓝提取物对MCF7增殖的抑制作用,并用倒置相差显微镜观察细胞形态,Annexin V-FITC/PI染色细胞后用流式细胞术检测不同浓度紫甘蓝提取物对MCF7凋亡的影响,采用Transwell法检测不同浓度紫甘蓝提取物对MCF7迁移的影响。采用SPSS16.0软件对实验结果进行统计学处理。结果:紫甘蓝提取物可抑制MCF7的增殖,并呈浓度依赖性和时间依赖性(P0.05),也使MCF7形态发生了异常变化,紫甘蓝提取物可诱导MCF7凋亡、抑制其迁移,且呈浓度-效应关系(P0.05)。结论:紫甘蓝提取物可抑制乳腺癌细胞MCF7生长和迁移。     

Cytotoxic sesquiterpene lactones from the leaves of Vernonia guineensis Benth. (Asteraceae)

Ethnopharmacological relevance

Vernonia guineensis Benth. (Asteraceae) preparations are used in folk medicine in Cameroon to treat a number of ailments, including prostate cancer and malaria, and is used as an anthelmintic, adaptogen and antidote. The aim of this study was to continue the validation of the activity of Vernonia guineensis Benth. extracts and isolated molecules against cancer cell lines following the previous isolation of an anti-prostate cancer sugar ester from the root extract.

Materials and methods

Acetone extracts of Vernonia guineensis Benth. leaves were tested for activity against 10 cancer cell lines (Breast—MDA-MB-231, Breast—MCF-7, Colon—HCT-116, Leukemia—HL-60, Lung—A549, Melanoma—A375, Ovarian—OVCAR3, Pancreas—Mia-paca, Prostate—PC-3 and Prostate—DU-145). The acetone extract was subjected to bioactivity guided fractionation. Anti-proliferation and clonogenic activity of the isolated compounds were tested. The WST-1 assay was used for the anti-proliferation activity, while the standard clonogenic test was used to determine the clonogenic activity.

Results

The acetone extract of Vernonia guineensis Benth. demonstrated in vitro activity ranging from IC₅₀ 4–26 μg/mL against the 10 cell lines. Activity guided fractionation of this extract yielded two sesquiterpene lactones, isolated for the first time from the genus Vernonia. The compounds were characterized using spectroscopic experiments, including a combination of 1D and 2D NMR data. Vernopicrin (1) and Vernomelitensin (2) demonstrated in vitro activity against human cancer cell lines with IC₅₀ ranging from 0.35–2.04 μM (P<0.05) and 0.13–1.5 μM (P<0.05), respectively, between the most and least sensitive cell lines for each compound. Vernopicrin was most active against the human melanoma (A375) cell line and least active against the lung cancer (A549) cell line, while Vernomelitensin was also most active against the human melanoma (A375) cell line and least active against the breast cancer (MCF-7) cell line. Both compounds also demonstrated anticlonogenic activity.

Conclusion

The cytotoxicity demonstrated by the crude extract and isolated sesquiterpenes against cancer cell lines highlights the medicinal potential of V. guineensis. The selective anti-proliferation and dose dependent anticlonogenic activities suggest that the identified sesquiterpenes could be potential antitumor agents.     

粟米草三萜类化学成分及其活性研究

目的研究粟米草Mollugo pentaphylla中的三萜类化学成分,寻找其中具有细胞毒活性化合物。方法综合运用大孔吸附树脂、硅胶柱色谱、半制备型高效液相及SephadexLH-20凝胶柱色谱等各种色谱技术进行系统化学研究,根据其理化性质和MS、NMR等波谱数据鉴定化合物结构,同时对所得的三萜皂苷进行细胞毒活性测试。结果从粟米草干燥地上部分醇提取物中共分离得到6个三萜类化合物,分别鉴定为粟米草苷E(1)、3-O-[α-L-rhamnopyranosy1(1→2)-α-L-arabinopyranosyl]-28-O-[β-D-glucopyranosyl (1→6)-β-D-glucopyranosyl] oleanolic acid(2)、竹节香附皂苷R8(3)、竹节香附素A(4)、mollugogenolsA(5)、齐墩果酸(6)。细胞毒活性显示,化合物1~5对人前列腺癌DU145细胞、人宫颈癌HeLa细胞及人早幼粒白血病HL-60细胞均显示一定的抑制作用,尤其是对人早幼粒急性白血病HL-60细胞,其IC50分别为10.21、38.43、40.28、20.59、83.16μmol/L。结论化合物1为新的齐墩果酸型三萜皂苷,2~4为首次从该植物中分离得到。细胞毒活性显示,化合物1~5对人前列腺癌DU145细胞、人宫颈癌HeLa细胞及人早幼粒白血病HL-60细胞均显示一定的抑制作用。     

A flavonoid glycoside isolated from Smilax china L. rhizome in vitro anticancer effects on human cancer cell lines

The anticancer activity of eight crude extracts of Smilax china L. rhizome (SCR) against HeLa cells was assessed by MTT assay and clonogenic assay, the fraction rich in flavonoids had show good activity against HeLa cells. A bioassay-guided separation on this extract lead to the detection of kaempferol-7-O-beta-D-glucoside (KG), which belongs to flavonoid glycoside, displayed marked anticancer activity. We evaluated its in vitro cytotoxicity and antiproliferative effect in a panel of established cancer cell lines by MTT assay and clonogenic assay. KG induces A375 and HL60 cells apoptosis, which was demonstrated by morphological changes, DNA fragmentation and flow cytometric analysis. Fluorescent staining with Hoechst 33258 showed fragmentation and condensation of chromatin in the A375 and HL60 cells. Flow cytometric analysis shown that A375 and HL60 cells treated with KG resulted in the appearance of a hypodiploid peak (A0 region), probably due to the presence of apoptosing cells and/or apoptotic bodies with DNA content less than 2n. Quantitation of the hypodiploid cells shows a dose-dependent response to KG, and this result is in good accordance with that of the DNA fragmentation assay by agarose gel electrophoresis. Our results suggested that cell cycle arrest at G(1) phase and induce apoptosis as a mechanism by which KG exerts an antiproliferative effect.     

白花蛇舌草核苷体外抗肿瘤作用实验研究

目的 探讨白花蛇舌草中核苷的体外抗肿瘤作用.方法 采用24孔板培养法和MTT法观察白花蛇舌草核苷对人红白血病细胞株K562、人非小细胞肺癌细胞株A549的抑制作用.结果 显微镜下观察24孔板,白花蛇舌草核苷呈现明显的抗肿瘤作用.体外抑瘤实验表明,白花蛇舌草核苷对两种细胞株起效的最低药物浓度分别为100 μg/ml和50μg/ml,半数致死量IC50分别是248.1 μg/ml和147.7 μg/ml.结论 白花蛇舌草核苷具有抗肿瘤活性.