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Visual characterization of targeted effect of holo-transferrin-tagged dihydroartemisinin on human breast cancer cells
  • ISSN号:1671-6264
  • 期刊名称:《东南大学学报:医学版》
  • 时间:0
  • 分类:Q754[生物学—分子生物学] TQ461[化学工程—制药化工]
  • 作者机构:[1]Department of Chemistry, Jinan University, Guangzhou 510632, China, [2]Key Laboratory of Optoelectronic Information and Sensing Technologies of Guangdong Higher Education Institutes, Jinan University, Guangzhou 510632, China
  • 相关基金:This work was supported by the National Key Basic Research and Development Program of China (2010CB833603), and the National Natural Science Foundation of China (30828023).
中文摘要:

指向的药能显著地减少细胞毒素的效果并且增加治疗学的活动。Dihydroartemisinin (DHA ) 被显示了在杀死癌症房间有效。然而,它展出非指向的性质。Holo-transferrin (TF ) 是一个合适的药搬运人指向癌症房间,因为癌症房间需要由维持他们的不受管束的生长的调停 TF 的机制熨举起。而且, TF 受体(TF-R ) 高度在癌症房间表面上被表示。在这份报纸,3-( 4,5-dimethylthi-azol-2-yl ) -2,5-diphenyltetrazolium 溴化物( MTT )试金被用来评估4-( 12-Dihydroart-emisininoxy )的不同杀死效果人的乳癌房间( MCF-7 )上的安息香的酸 Hydrozide-transferrin ( DBAH-TF )房间和人的正常的胸( HNB )房间,并且原子力量显微镜学( AFM )被用来视觉上在 MCF-7 房间上观察 DBAH-TF 的指向的效果。MTT 结果证明 DBAH-TF 比在杀死 MCF-7 房间的 DHA 是乘更多的有势力的 172,当 HNB 房间上的 DBAH-TF 的细胞毒素的效果仅仅是到 DHA 的 1/33 时。另外, MCF-7 房间上的 DBAH-TF 的杀死的效果在 HNB 房间上是乘那的 286,显示出指向的效果。而且,在在 DBAH-TF 和 DHA 治疗以后的细胞的表面的超微结构有不同差别。通过 AFM 成像,许多典型的洞在被 DBAH-TF 完成以后在癌症房间表面上被观察,它不同于洞,不规则的形状由 DHA 影响了。这些结果视觉上证明指向的药更有有势力杀死的 DBAH-TF 与 DHA 相比在 MCF-7 上完成房间。

英文摘要:

Targeted drugs could significantly reduce cytotoxic effect and increase therapeutic activity. Dihydroartemisinin (DHA) has been shown to be effective in killing cancer cells. However, it exhibits non-targeted property. Holo-transferrin (TF) is a suitable drug-carrier to target cancer cells, because cancer cells need iron uptake by the TF-mediated mechanism to maintain their uncontrolled growth. Furthermore, TF receptors (TF-R) are highly expressed on cancer cell surfaces. In this paper, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to evaluate the different killing effect of 4-(12-Dihydroartemisininoxy) Benzoic Acid Hydrozide-transferrin (DBAH-TF) on human breast cancer cells (MCF-7) ceils and human normal breast (HNB) cells, and atomic force microscopy (AFM) was used to visually observe the targeted effect of DBAH-TF on MCF-7 cells. MTT results show that DBAH-TF is 172 times more potent than DHA in killing MCF-7 cells, while the cytotoxic effect of DBAH-TF on HNB cells is merely 1/33 to DHA. Also, the killing effect of DBAH-TF on MCF-7 cells is 286 times that on HNB cells, showing targeted effect. Moreover, there are distinct differences in ultrastructures of cellular surfaces after DBAH-TF and DHA treatment. Through AFM imaging, many characteristic holes were observed on the cancer cell surface after being effected by DBAH-TF, which differ from the holes with irregular shapes affected by DHA. These results visually show that the DBAH-TF targeted drug has more potent killing effect on MCF-7 cells compared with DHA.

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期刊信息
  • 《东南大学学报:医学版》
  • 中国科技核心期刊
  • 主管单位:教育部
  • 主办单位:东南大学
  • 主编:唐萌
  • 地址:南京市鼓楼区丁家桥87号
  • 邮编:210009
  • 邮箱:bjb@pub.seu.edu.cn
  • 电话:025-83272481
  • 国际标准刊号:ISSN:1671-6264
  • 国内统一刊号:ISSN:32-1647/R
  • 邮发代号:28-265
  • 获奖情况:
  • 全国优秀学报,铁道部优秀期刊
  • 国内外数据库收录:
  • 美国化学文摘(网络版),波兰哥白尼索引,中国中国科技核心期刊,中国北大核心期刊(2014版)
  • 被引量:8241