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Objective To investigate the inhibition effect of cantharidin on the proliferation of human being carcinoma A549 cell.

目的 研究斑蝥素对人肺癌A549细胞增殖的抑制作用和机制。

Methods MTT assay was used to determine the proliferation inhibition by cantharidin to A549 cell. FACS can were applied to detect the change of cell cycle.

采用MTT法检测斑蝥素对A549细胞增殖的抑制作用;流式细胞仪分析A549细胞周期及斑蝥素对细胞周期的影响。

However, it is very toxic. Nocantharidin, a derivative of cantharidin first synthesized in China, is a new anti-tumor drug with strong anti-tumor activities and increases the number of while blood cells.

去甲基斑蝥素(noncantharidion, NCTD)为斑蝥素的衍生物,是我国首先合成的具有较强抗肿瘤活性和独特升高白细胞作用的新型抗肿瘤药物。

According to results of cantharidin structure-activity relationships, a series of cantharidin derivatives for the first time were designed, synthesized and characterized by IR, NMR and elemental analysis.

用IR、〓H NMR初步证实了斑蝥素衍生物和DCC生成稳定中间体是使含有芳香羧酸的斑蝥素衍生物与氨基葡萄糖及其衍生物不能进行反应的主要因素。

Physical stability of liposomes plays the critical roles in various stages of the applications and development of liposomes. In this study, we applied low molecular weight chitosan to modify the liposomes surface, and investigated the physical stability of liposomes, Moreover, we encapsulated cantharidin to study the effects of chitosan which cause drug leakage.

微脂粒稳定性的研究在其应用发展上占有举足轻重的影响,因此本研究利用低分子量水溶性几丁聚醣来修饰微脂粒表面,观测几丁聚醣对微脂粒物理稳定性的影响,同时也一并探讨包覆抗癌药物斑蝥素,几丁聚醣对微脂粒包覆斑蝥素的渗漏情形。

The study on soluble protein after eclosion when cantharidin synthesis is active in Mylabris calida Palla would help to clarify the synthesis mechanism of cantharidin and involved enzymes of the synthesis.

研究斑蝥素大量合成期的芫菁体内可溶性蛋白,有助于阐明斑蝥素合成相关酶蛋白的种类和合成机理。

Besides, the series of synthetic compounds were tested for their capability to suppress growth of human hepatocellular carcinoma cell line Hep 3B and Hep G2, and myeloid leukemia cell line HL-60. The results showed compound 20, N-(2-amino- 3-nitrophenyl)cantharidinimide, exhibited more potent than others, but it was still less effective than cantharidin.

此外也利用斑蝥胺的衍生物对人类肝癌细胞Hep 3B和Hep G2,以及血癌细胞HL-60的细胞毒性进行测试,结果显示化合物20 [N-(2-amino-3-nitrophenyl)cantharidinimide]有较好的抑制作用,但是效果仍未比斑蝥素好。

Liaoning Medical University, Jinzhou 121001 China)Abstract:Objective To study the distribution and liver targeting of glycyrrhetinic acid derivatives (stearin glycyrrhetinic acid ester-3-O-galactosidase, Gal-GAOSt) modifying norcantharidin liposomes (Gal-GAOStNC-LP) in rats.

目的 研究甘草次酸衍生物(甘草次酸硬脂醇酯-3-O-半乳糖苷,Gal-GAOSt)修饰去甲斑蝥素脂质体(Gal-GAOStNC-LP)在小鼠体内的分布及肝靶向性。方法利用薄膜分散法制备甘草次酸衍生物修饰去甲斑蝥素脂质体后,经小鼠尾静脉给药,采用HPLC法检测去甲斑

Objective:To investigate the effect of cantharides infections on LoVo cell.

复方斑蝥注射液是从斑蝥、刺五加、黄芪、人参等中药中经现代独有的高科技工艺提取的新型多靶点抗肿瘤药,具有抗肿瘤和免疫调整双重作用,在临床上得到了广泛的应用。

Part II: The structural modification of norcantharidin and the discovery and applications of NCS-DMSO combinatorial system: A series of derivatives of 5,6-dehydronorcantharidin was transferred into their corresponding 5,6-epoxynorcantharidin derivatives with Oxone, and finally 14 new compounds have been synthesized; and we also discover the novel combinatorial system NCS-DMSO to make N-aromatic substituted norcantharidin amic acids to their corresponding imides in high yields.

利用十分廉价的Oxone为氧化剂,成功的得到了14个5,6-环氧去甲斑蝥素系列衍生物;同时我们意外地发现了NCS-DMSO组合体系可以使去氢去甲斑蝥素酰胺类化合物实现分子内脱水而生成亚胺类化合物,首次发现和运用该全新的组合体系实现了该类反应。

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