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首页 » 纳米医学 » Mol Can Therap:纳米脂质体携带特效药可靶向杀灭黑色素瘤细胞

Mol Can Therap:纳米脂质体携带特效药可靶向杀灭黑色素瘤细胞

来源:生物谷 2014-10-27 09:59

2014年10月27日 讯 /生物谷BIOON/ --近日,来自宾州州立大学医学院(Penn State College of Medicine)的研究人员通过研究开发了一种纳米颗粒,其可以将治疗黑色素瘤的药物直接运输到癌症患处,相关研究刊登于国际杂志Molecular Cancer Therapeutics上。

将癌症药物运输至患处非常困难,科学家们一直致力于开发新技术来克服药物的天然局限性,比如如何将药物装载至纳米颗粒中;研究者Gavin Robertson表示,药物可以被包装装载于脂质球中,这种脂质球明显小于头发的宽度,这就可以使得脂质球溶解于血流中从而抑制副作用的产生。包含药物的纳米颗粒随后会随着血流运输至肿瘤患处,在肿瘤患处不断积累并且释放药物杀灭癌细胞。

此前研究中研究者发现来自松树皮的一种名为leelamine的衍生物具有抗癌特性,但是由于其在胃肠道吸收较差因此不能口服,而且由于其对红细胞具有损伤作用也不能通过静脉进行注射。本文中,研究者Robertson和其同时开发了一种装载leelamine的纳米脂质体-Nanolipolee-007,其可以通过静脉注射而不损伤红细胞,随后Nanolipolee-007会在肿瘤患处积累,由于其尺寸较小因此其可以在肿瘤部位释放leelamine来杀灭癌细胞。

Leelamine是一种独特的药物,其可以抑制癌细胞周围的胆固醇运动从而关闭癌细胞生存所需的关键信号,一些诸如PI3K、MAPK和STAT3的蛋白质通路往往处于高度激活状态,帮助癌细胞复制扩散,但在leelamine的作用下其都会被关闭从而引发癌细胞死亡,正常细胞中这些蛋白通路水平并不会太高。

研究者表示,纳米颗粒可以帮助leelamine进一步迈向临床试验中,而我们也揭示了Nanolipolee-007对培养皿中生长的细胞的效应,以及其对小鼠肿瘤生长的抑制作用,leelamine可以有效抑制小鼠肿瘤的发展而不引发任何副作用。

目前包含leelamine的Nanolipolee-007是一种新型的药物,其可以通过抑制癌细胞的胆固醇运输来靶向杀灭癌细胞,未来还需要进行更多的研究来证明其安全可靠性,研究人员希望Nanolipolee-007可以早日进入到临床试验中来真正为开发治疗黑色素瘤的靶向疗法带来帮助。(生物谷Bioon.com)

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Nanolipolee-007, a Novel Nanoparticle-Based Drug Containing Leelamine for the Treatment of Melanoma

Raghavendra Gowda1,2,3,4, SubbaRao V. Madhunapantula1, Arati Sharma1,2,3,4, Omer F. Kuzu1,2, and Gavin P. Robertson1,2,3,4,5,6,7,*

Malignant melanoma is a difficult cancer to treat due to the rapid development of resistance to drugs targeting single proteins. One response to this observation is to identify single pharmacologic agents that, due to a unique mechanism of action, simultaneously target multiple key pathways involved in melanoma development. Leelamine has been identified as functioning in this manner but has poor bioavailability in animals and causes lethality when administered intravenously. Therefore, a nanoliposomal-based delivery system has been developed, called Nanolipolee-007, which stably loads 60% of the compound. The nanoparticle was as effective at killing melanoma cells as leelamine dissolved in DMSO and was more effective at killing cultured melanoma compared with normal cells. Mechanistically, Nanolipolee-007 inhibited PI3K/Akt, STAT3, and MAPK signaling mediated through inhibition of cholesterol transport. Nanolipolee-007 inhibited the growth of preexisting xenografted melanoma tumors by an average of 64% by decreasing cellular proliferation, reducing tumor vascularization, and increasing cellular apoptosis, with negligible toxicity. Thus, a unique clinically viable nanoparticle-based drug has been developed containing leelamine for the treatment of melanoma that acts by inhibiting the activity of major signaling pathways regulating the development of this disease. Mol Cancer Ther; 13(10); 2328–40. ©2014 AACR.

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