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Polyamidoamine-Drug Conjugates Containing Metal-Based Anticancer Compounds
Journal of Inorganic and Organometallic Polymers and Materials ( IF 4 ) Pub Date : 2019-09-17 , DOI: 10.1007/s10904-019-01325-7 B. A. Aderibigbe , A. Mugogodi , M. Nwamadi , S. S. Ray , V. Steenkamp , M. O. Balogun , W. M. R. Matshe
Journal of Inorganic and Organometallic Polymers and Materials ( IF 4 ) Pub Date : 2019-09-17 , DOI: 10.1007/s10904-019-01325-7 B. A. Aderibigbe , A. Mugogodi , M. Nwamadi , S. S. Ray , V. Steenkamp , M. O. Balogun , W. M. R. Matshe
Polyamidoamine drug conjugates containing ferrocene and platinum analogues were prepared in this study. Fourier transform infrared spectra confirmed the successful isolation of the conjugates with signals at 3300 cm−1 for amide N–H stretch and for C=O stretch at 1655–1635 cm−1 resulting from the conjugation of 4-ferrocenylketobutanoic acid. The polyamidoamine drug conjugate particle size was 247.1 nm and 258.3 nm suggesting their ability to exhibit in vitro phagocytosis. The average particle charges were 29 and 30.2, which was indicative of good stability and the capability to resist aggregation. In vitro cytotoxicity studies further revealed that the conjugates 1–5 did not exhibit cytotoxicity towards the normal cell lines (EA.hy926) whereas high cytotoxic activity was noted against the cancer cell lines (MCF-7 and MDA-MB-231) indicating selectivity towards cancer cell lines. Fc-PDA acted as a potentiating agent when incorporated together with DACH PtCl2 in the polymers, resulting in a good inhibitory effect in vitro. However, when combining Fc-PDA with K2PtCl4 in the polymer, an antagonistic effect was noted. The current findings implicate that the prepared conjugates hold the potential as therapeutics for the treatment of breast cancer. Further research is required to confirm this.
中文翻译:
含金属基抗癌化合物的聚酰胺酰胺-药物缀合物
在这项研究中制备了含有二茂铁和铂类似物的聚酰胺胺药物偶联物。傅里叶变换红外光谱证实,成功分离出了4-二茂铁基酮丁酸的共轭产物,在3300 cm -1处的酰胺N–H延伸和C = O延伸在1655–1635 cm -1处的信号被分离。聚酰胺酰胺药物共轭物的粒径为247.1 nm和258.3 nm,表明它们具有表现出体外吞噬作用的能力。平均颗粒电荷为29和30.2,这表明良好的稳定性和抗聚集能力。体外细胞毒性研究进一步表明,结合物1-5对癌细胞系(EA.hy926)没有表现出细胞毒性,而对癌细胞系(MCF-7和MDA-MB-231)的细胞毒活性较高,表明对癌细胞系具有选择性。Fc-PDA与DACH PtCl 2一起掺入到聚合物中时起增效剂的作用,在体外具有良好的抑制作用。然而,当在聚合物中将Fc-PDA与K 2 PtCl 4结合时,观察到拮抗作用。当前的发现暗示所制备的缀合物具有作为治疗乳腺癌的疗法的潜力。需要进一步的研究来确认这一点。
更新日期:2019-09-17
中文翻译:
含金属基抗癌化合物的聚酰胺酰胺-药物缀合物
在这项研究中制备了含有二茂铁和铂类似物的聚酰胺胺药物偶联物。傅里叶变换红外光谱证实,成功分离出了4-二茂铁基酮丁酸的共轭产物,在3300 cm -1处的酰胺N–H延伸和C = O延伸在1655–1635 cm -1处的信号被分离。聚酰胺酰胺药物共轭物的粒径为247.1 nm和258.3 nm,表明它们具有表现出体外吞噬作用的能力。平均颗粒电荷为29和30.2,这表明良好的稳定性和抗聚集能力。体外细胞毒性研究进一步表明,结合物1-5对癌细胞系(EA.hy926)没有表现出细胞毒性,而对癌细胞系(MCF-7和MDA-MB-231)的细胞毒活性较高,表明对癌细胞系具有选择性。Fc-PDA与DACH PtCl 2一起掺入到聚合物中时起增效剂的作用,在体外具有良好的抑制作用。然而,当在聚合物中将Fc-PDA与K 2 PtCl 4结合时,观察到拮抗作用。当前的发现暗示所制备的缀合物具有作为治疗乳腺癌的疗法的潜力。需要进一步的研究来确认这一点。