月腺大戟的化学成分

目的研究月腺大戟的化学成分.方法运用柱层析进行分离,并对所分得的化合物运用波谱数据进行了结构解析.结果从月腺大戟中分离得到6个化合物并鉴定了其结构,分别为:baccatin(1),3-乙酰-β香树酯醇(2),3,3＇-二乙酰基-4,4′-二甲氧基-2,2′,6,6＇-四羟基二苯甲烷(3),2,4-二羟基-6-甲氧基-3-甲基苯乙酮(4),β-谷甾醇(5),胡萝卜苷(6).结论baccatin为首次从月腺大戟中分离得到.     

月腺大戟中二萜化学成分的研究

从月腺大戟(Euphorbia ebracteolata Hayata)的干燥根中首次分得4种萜类化合物,根据理化数据和光谱分析,鉴定其中2种为新的二萜内酯,分别命名为月腺大戟甲素(ebracteolatanolide A)和月腺大戟乙素(ebracteolatanolide B),另2种为已知化合物Jolkinolide B和3-乙酰α香树脂醇。     

月腺大戟与狼毒大戟对人肝癌细胞BEL-7402体外增殖的影响对比研究

目的:对比研究月腺大戟与狼毒大戟对人肝癌细胞BEL-7402体外增殖的影响。方法:灌胃月腺大戟(0.097、0.485、0.2425g.kg-1)、狼毒大戟(0.05、0.025、0.0125g.kg-1)混悬液,每天1次,连续3d,末次给药后自大鼠腹主动脉采血,以分离的血清加培养液体外培养人肝癌细胞BEL-7402;MTT比色法测定生长抑制率;通过集落形成试验测定克隆形成率。结果:狼毒大戟对BEL-7402细胞增殖和克隆形成率有明显的抑制或降低作用,且与给药剂量呈正相关;月腺大戟对BEL-7402细胞增殖和克隆形成率无明显影响。结论:狼毒大戟对人肝癌细胞BEL-7402体外增殖抑制作用明显强于月腺大戟。     

乌苯美司对白血病细胞生长及 P388 淋巴结转移的抑制作用

目的：观察乌苯美司对白血病细胞生长及淋巴结转移的抑制作用。方法：将ＨＬ－６０，Ｋ５６２，ＭＴ－１，ＭＴ－２，ＭＯＬＴ－４和Ｒａｊｉ白血病细胞分别与乌苯美司培育，计数存活细胞，测定ＭＴ－１和ＭＴ－２的［３Ｈ］ＴｄＲ参入量及Ｐ３８８细胞淋巴结转移。结果：乌苯美司４５００ｍｇ／Ｌ使ＨＬ－６０，ＭＴ－１，ＭＴ－２和Ｒａｊｉ细胞存活数明显减少（Ｐ＜０．０１），０．１，１，１０，１００和１０００ｍｇ／Ｌ可明显抑制ＭＴ－１，ＭＴ－２细胞摄入［３Ｈ］ＴｄＲ（Ｐ＜０．０１）；小鼠每天ｉｐ乌苯美司１，３，１０，３０μｇ／鼠×１１ｄ，转移至淋巴结的Ｐ３８８细胞数明显减少。结论：乌苯美司能抑制人白血病细胞生长及ＭＴ－１，ＭＴ－２细胞的ＤＮＡ合成，有效抑制Ｐ３８８细胞的淋巴结转移。     

雄黄诱导白血病细胞凋亡的研究

目的：检测雄黄诱导白血病细胞凋亡能力，探讨分子机制。方法：应用形态学观察检测细胞凋亡，免疫组化方法检测白血病细胞bcl-2蛋白表达。结果：雄黄可诱导白细胞病细胞发生典型的凋亡，同时雄黄可使白血病细胞bcl-2蛋白表达呈时间依赖性下降。结论：雄黄通过影响白血病细胞bcl-2蛋白的表达，从而导致白血病细胞发生凋亡，这是其治疗白血病的重要分子机制。     

月腺大戟的化学成分及其乳腺癌细胞毒活性研究

目的 研究大戟科植物月腺大戟的化学成分及其对乳腺癌细胞毒活性。方法 采用多种色谱技术对化合物进行分离纯化,根据化合物的理化性质和光谱数据分析鉴定化合物的结构。采用噻唑蓝（MTT）比色法研究化合物对6种乳腺癌细胞的抑制活性。结果 月腺大戟植物中分离得到10个化合物,分别鉴定为：2,4-二羟基-6-甲氧基-3-甲酰基苯乙酮（1）;2,4-二羟基-6-甲氧基-3-甲基苯乙酮（2）;月腺大戟素A（3）;3,3''-乙酰基-4,4''-二甲氧基-2,2'',6,6''-四羟基二苯基甲烷（4）;岩大戟内酯B（5）;岩大戟内酯A（6）;亚油酸（7）;fischeria A（8）;β-香树脂醇乙酸酯（9）;单十九酸甘油酯（10）。乳腺癌细胞毒活性研究显示：化合物3对乳腺癌细胞MDA-MB-231、Sum149、MCF7、ZR-75-1、SKBr3、BT474的IC₅₀值分别为6.69、5.50、5.50、7.08、8.64、5.42 μmol/L。结论 化合物6、7、8、10为首次从该植物中分离得到;化合物3对乳腺癌细胞具有显著的抑制活性。     

P13K/Akt在细胞凋亡及白血病耐药方面的研究进展

白血病是起源于造血系统的恶性肿瘤,其发生机制与发展过程已经证实与多种遗传学相关,多种原因导致二类基因突变,I类突变导致细胞增殖或抑制凋亡,Ⅱ类突变导致细胞分化受抑,二类突变同时存在而导致白血病.     

番荔枝内酯诱导白血病细胞凋亡的机理

目的　研究番荔枝内酯(squamocin)诱导白血病细胞凋亡的机理。方法　DNA凝胶电泳法、荧光染色等检测细胞凋亡。试剂盒检测caspase-3的活性。Westernblot法检测PARP和caspase-3的剪切片断和磷酸化的SAPK/JNK量的变化。结果　Squamocin处理HL-60细胞后,导致染色质浓缩、片断化,DNA梯形条带出现,完整PARP的116ku条带逐渐减少,而85ku的片断逐渐增加,caspase-3酶的活性也增加。Caspase-3的特异性抑制剂DEVD-CHO预处理HL-60细胞,可阻止squamocin诱导的DNA片断化、PARP的剪切和细胞死亡。Squamocin激活HL-60细胞中SAPK/JNK。结论　Squamocin诱导HL-60细胞凋亡依赖caspase-3途径的激活,squamocin激活caspase-3可能与SAPK/JNK的激活相关     

三氧化二砷诱导粒细胞性白血病原代细胞凋亡的研究

目的：探讨三氧化二砷（As2O3)对慢性粒细胞性白血病（CML）慢性期原代细胞生长的影响。方法：通过细胞增殖,活力检测,形态学观察,粒系髓系集落形成（CFU－GM）集落培养,凝胶电泳等方法检测。结果：As2O3可抑制CML原代细胞增殖,经平均浓度5．0umol.L^-1 As2O3处理5d时抑制率为50％,经大于等于2．6－5．0umol.L^-1 As2O3培养2－5d,可引起细胞凋亡的形态学改变及DNA片段化,As2O3浓度2．5umol.L^-1,CFU－GM的形成抑制率＞50％,结论：As2O3可以抑制CML慢性期原代细胞的增殖,并诱导凋。     

An isopimarane diterpene from Euphorbia ebracteolata Hayata

From the ethanolic extract of the roots of Euphorbia ebracteolata Hayata four compounds were isolated. They are 24-methylenecycloartanone, tirucallol, procesterol and a new isopimarane diterpene, namely yuexiandajisu C. The structure of yuexiandajisu C was elucidated by spectral analysis. The bioassay in vitro showed yuexiandajisu C exhibited immunomodulatory activity.     

Chemical Constituents of Euphorbia ebracteolata

Aim To study the chemical constituents of Euphorb/a ebracteolata Hayata. Methods Column chromatography was used in the isolation procedure, while the structures of isolated compounds were elucidated by spectral data. Results Six compounds were isolated and their structures were identified as baccatin (1), 3-acetyl-β-amyrin (2), 3,3‘-diacetyl-4,4‘-dim-ethoxy- 2,2‘, 6,6‘-tetrah ydroxy diphenylmethane (3), 2,4- dihydroxy-6-methoxy-3-methyl acetophenone (4), β-sitosterol（5), and daucosterol (6). Conclusion Baccatin was obtained from Euphorbia ebracteolata for the first time.     

An Isopimarane Diterpene from Euphorbia Ebracteolata Hayata

Abstract

From the ethanolic extract of the roots of Euphorbia ebracteolata Hayata four compounds were isolated. They are 24-methylenecycloartanone, tirucallol, procesterol and a new isopimarane diterpene, namely yuexiandajisu C. The structure of yuexiandajisu C was elucidated by spectral analysis. The bioassay in vitro showed yuexiandajisu C exhibited immunomodulatory activity.     

Two novel phloroglucinol derivatives from Euphorbia ebracteolata hayata

Two new phloroglucinol derivatives, named ebracteolatain A and ebracteolatain B, along with three known phloroglucinol derivatives were isolated from Euphorbia ebracteolata Hayata., and their structures were elucidated as 3,3′-diacetyl-2,4′-dimethoxy-2′,4,6,6′-tetrahydroxy-5′-methyl diphenylmethane (1) and 1-[3,5-bis-(3-acetyl-2,6-dihydroxy-4-methoxy-benzyl)-2,4,6-trihydroxy-phenyl]-ethanone (2) on the basis of spectroscopic techniques and chemical methods.     

Yuexiandajisu D, a novel 18-nor-rosane-type dimeric diterpenoid from Euphorbia ebracteolata Hayata

Yuexiandajisu D, a novel 18-nor-rosane-type dimeric diterpenoid, was isolated from the roots of Euphorbia ebracteolata Hayata. Its structure was elucidated as 6,3':7,2'-diepoxy-di-2,3-dihydroxy-18-nor-ros-1(10),2,4,15-tetraene by spectroscopic techniques (HSQC, HMBC, DQF-COSY, TOCSY, NOESY) and chemical methods. Yuexiandajisu D showed moderate cytotoxic activity against cancer cell lines on HCT-8 and Bel-7402, with IC₅₀ values of 2.66 and 3.76 μM, respectively.     

Yuexiandajisu D,a novel 18-nor-rosane-type dimeric diterpenoid from Euphorbia ebracteolata Hayata

Yuexiandajisu D, a novel 18-nor-rosane-type dimeric diterpenoid, was isolated from the roots of Euphorbia ebracteolata Hayata. Its structure was elucidated as 6,3′:7,2′-diepoxy-di-2,3-dihydroxy-18-nor-ros-1(10),2,4,15-tetraene by spectroscopic techniques (HSQC, HMBC, DQF-COSY, TOCSY, NOESY) and chemical methods. Yuexiandajisu D showed moderate cytotoxic activity against cancer cell lines on HCT-8 and Bel-7402, with IC₅₀ values of 2.66 and 3.76 μM, respectively.     

狼毒生品及炮制品的体外抗肿瘤活性研究

目的对从狼毒中分离得到的4种提取物进行体外抗肿瘤活性筛选。方法采用四甲基偶氮唑盐法研究狼毒提取物对SMMC-7721、HeLa、HepG2、H460 4种人癌细胞株增殖的影响。结果狼毒提取物可以不同程度地抑制4种人癌细胞株的增殖。其中炮制品石油醚部位抑制作用最强,对SMMC-7721、HepG2、H460细胞株增殖抑制率分别为81.08%,80.39%和89.81%;炮制品乙酸乙酯部位的抑制率分别为79.06%,78.36%和67.33%。结论狼毒炮制品石油醚部位和乙酸乙酯部位是狼毒抗肿瘤作用的主要活性部位,值得进一步深入探讨和研究。     

Effect of the cisplatin-procaine complex DPR in combination with several anticancer agents on murine P388 leukemic cells in vitro and in vivo

We evaluated in vitro the antiproliferative activity of DPR (Fig. 1), a new cisplatin-derived compound, in combination with five conventional anticancer drugs: the antimetabolites 5-fluorouracil (5FU) and methotrexate (MTX), the alkylating agent mitomycin C (MMC), the antimicrotubule agent taxol (TAX) and the intercalating agent of the antracycline group doxorubicin (DOX), against murine P388 leukemic cells. MTT assay was used to determine growth inhibition after incubation of cells for 72 hours in the presence of single or combined drugs. The additive, synergistic or antagonistic nature of the combined drug effect was determined using the isobole method.In our cellular model, synergism was the prevailing result observed when DPR was combined with MMC. Conversely, antagonism was observed when DPR was combined with TAX. When DPR was administered together with the other antineoplastic drugs, the final effect was dependent on the concentrations of single agents.The study in vitro of the association between DPR and MMC was extended in vivo in BDF-1 female mice bearing ip P388 leukemic cells. Our data in vivo confirmed those obtained in vitro, demonstrating the therapeutic advantage of the association of ineffective doses of DPR (2 and 7 mg/kg) and MMC (3.2 mg/kg) over the administration of MMC alone.