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It is reported that alkannin and shikonin isolated from the roots of Lithospermum erthyrorhizon or Alkanna tinctoria and their acylshikonin derivatives are potent selective inhibitors of DNA Topoisomerase Ⅰ.

文献报导紫草素和酰基紫草素等具有DNA拓扑异构酶Ⅰ的选择性抑制活性。本组曾合成得到少量环异紫草素(8),它对小鼠白血病P-388肿瘤细胞具有强烈的抑制作用。

The cytotoxicity of these compounds were valuated by MTT and SRB methods using three cancer cell lines: HL-60, A-549, P-388. Cyclo-shikonin, and cyclo-alkannin have high cytotoxicity against HL-60.The chiral center of side chain has no effect on their activity. 2- 1-(Acetyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (105) has strong inhibition effect on P-388 cells. 2- 1-(isooctyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (108) and 2- 1-(2-furoyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (112) have high inhibition on A-549.Shikonin (1), alkannin (2), and their derivatives have the structural features of a planar chromophores and short side chain. We examined the ability to inhibit the telomerase.

抗肿瘤活性初步筛选测试采用小鼠白血病P-388肿瘤细胞和人肺癌A-549肿瘤细胞进行,结果表明侧链羟基的手性对抗肿瘤活性无明显影响;有数个化合物具有很好的体外抑制活性,特别是化合物2-(1-异辛酰氧基-4-甲基-3-戊烯基)-5,8-二羟基-1,4-萘醌(108)和2-[1-(2-呋喃甲酰氧基)-4-甲基-3-戊烯基]-5,8-二羟基-1,4-萘醌(112)体外显示对人肺癌A-549肿瘤细胞有强效;2-(1-乙酰氧基-4-甲基-3-戊烯基)-5,8-二羟基-1,4-萘醌(105)对小鼠白血病P-388肿瘤细胞有强效;环紫草素和环异紫草素对人白血病HL-60细胞有强烈抑制作用。

Objective To explore the inhibitory effect and cycle defect of arsenic trioxide on human B lymphoma cells.

目的 研究三氧化二砷对B淋巴瘤细胞Raji的抑制作用和周期阻滞作用。

With an orthogonal experiment design , the telomerase inhibitors [azidothymidine , AZT 300 mg/ and lamivudine 150 mg/, per os , bid ,×2 weeks ] and X2irradiation [ total dose 10 Gy (2 Gy ×5) in 1 week ] were used to treat BALB/ c mice carrying breast cancer MA782 for evaluating the influence on peripheral blood cells , bone marrow nucleated cells and telomerase activity.

为了探讨端粒酶抑制剂联合X 线照射对荷瘤小鼠的骨髓抑制作用,采用正交实验设计,应用端粒酶抑制剂[AZT 300 mg/, lamivudine 150 mg/ ]联合X 线照射(2 Gy ×5次/ 1 周)处理移植性乳腺癌(MA782 )小鼠,观察其对骨髓有核细胞、外周血像及骨髓端粒酶活性的影响。

It was also demonstrated the inhibitors could inhibit the activities of enzymes to a great degree, the bacitracin and casein showed the prominent effect.

同时也证明了加入酶抑制剂能够对rHV2提供很大程度的保护,其中杆菌肽和酪蛋白的酶抑制作用比较突出。

OBJECTIVE:To investigate the growth inhibition of sodium butyrate on human endometrial cancer and to gain an insight into the possible underlying pathways.

目的:探讨丁酸钠对人子宫内膜癌细胞株HHUA裸鼠皮下移植瘤的生长抑制作用及其作用机制。

The present invention relates to a novel compound and its uses, which is an extract isolated and purified from Antrodia camphorate, in particular to 4-hydroxy- 2,3- dimethoxy- 6-methyl-5(3,7,11-trimethyl-dodeca-2,6,10-trienyl)-cyclohex-2-- enone, and its use in tumor growth inhibition.

大意:本发明涉及一种从牛樟芝提取分离、纯化的新型化合物抑制癌细胞活性成分4-hydroxy-2,3- dimethoxy-6-methyl-5(3,7,11-trimethyl-dodeca-2,6,10-trienyl-cyclohex-2-enone及其用途,使用在肿瘤生长的抑制作用。

Twenty-six of them wereeach given this drug lmg daily after the first coition during the cycle,and 12 womenused 2 mg for once for postcoital contraception.

所有服药妇女的子宫内膜发育均受不同程度抑制,对在周期早期开始服药者内膜的抑制作用较后期服药者明显。

The inhibition of SPG-Rg3 on the growth of MCF-7 cells was detected by MTT assay,IC50 was calculated to obtain the effective concentration; flow cytometry was used to observe the cell cycle of MCF-7 cells; AO/EB fluorescence double-dye technology was performed to observe the apoptosis of cells in morphology,immunocellularchemistry and RT-PCR were utilized to investigate the apoptosis of MCF-7 cells and its relationship with caspase-8 from protein level and molecule level.

采用MTT法观察SPG-Rg3对MCF-7细胞生长的抑制作用,并计算出IC50,依据IC50值确定SPG-Rg3的有效浓度;流式细胞术检测SPG-Rg3作用后MCF-7细胞周期的变化;AO/EB双染从形态学上观察SPG-Rg3对MCF-7细胞凋亡的作用;免疫细胞化学染色和RT-PCR技术分别从蛋白水平和分子水平上检测SPG-Rg3对MCF-7细胞的诱导凋亡作用及其与caspase-8基因的关系。

Experiment results showed as follows: 1 Two kinds of reactive oxygen species exhibited remarkable damage to larvae on 3 types of different development stage.The treatment of reactive oxygen species could result in decrease of larva survival rate and inhibit metamorphosis rate of cyprid.

实验结果表明:1、二种类型的活性氧对东方小藤壶三种不同发育时期的幼虫均具有伤害作用,在其作用下,幼虫存活率的下降,变态过程受到抑制,且表现出一定的剂量效应;三种不同发育时期的幼虫对活性氧作用的敏感性存有明显的差异性,Ⅵ期无节幼虫对羟自由基的作用最为敏感。

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