Gil-Mesón Ana, Roncero Alejandro M, Tobal Ignacio E, Basabe Pilar, Díez David, Mollinedo Faustino, Marcos Isidro S
Departamento de Química Orgánica, Universidad de Salamanca, Plaza de los Caídos 1-5, 37008 Salamanca, Spain.
Instituto de Biología Molecular y Celular del Cáncer, Centro de Investigación del Cáncer, CSIC-Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain.
Molecules. 2015 Dec 30;21(1):E47. doi: 10.3390/molecules21010047.
A series of sesterterpenoid bioconjugates with phospholipids and polyunsaturated fatty acids (PUFAs) have been synthesized for biological activity testing as antiproliferative agents in several cancer cell lines. Different substitution analogues of the original lipidic ether edelfosine (1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine) are obtained varying the sesterterpenoid in position 1 or 2 of the glycerol or a phosphocholine or PUFA unit in position 3. Simple bioconjugates of sesterterpenoids and eicosapentaenoic acid (EPA) have been obtained too. All synthetic derivatives were tested against the human tumour cell lines HeLa (cervix) and MCF-7 (breast). Some compounds showed good IC50 (0.3 and 0.2 μM) values against these cell lines.
已合成了一系列与磷脂和多不饱和脂肪酸（PUFA）结合的倍半萜生物共轭物，用于在几种癌细胞系中作为抗增殖剂进行生物活性测试。通过改变甘油1位或2位的倍半萜或3位的磷酸胆碱或PUFA单元，获得了原始脂质醚依地福新（1-O-十八烷基-2-O-甲基-rac-甘油-3-磷酸胆碱）的不同取代类似物。还获得了倍半萜与二十碳五烯酸（EPA）的简单生物共轭物。所有合成衍生物均针对人肿瘤细胞系HeLa（子宫颈）和MCF-7（乳腺）进行了测试。一些化合物对这些细胞系显示出良好的IC50值（0.3和0.2μM）。
