Mukherjee Rama, Jaggi Manu, Rajendran Praveen, Siddiqui Mohammad J A, Srivastava Sanjay K, Vardhan Anand, Burman Anand C
Divisions of Experimental Oncology, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201 010, UP, India.
Bioorg Med Chem Lett. 2004 May 3;14(9):2181-4. doi: 10.1016/j.bmcl.2004.02.044.
Betulinic acid (1) significantly caused cytotoxicity to endothelial cell line ECV304 (IC(50) 1.26+/-0.44 microg/mL) in a 5-day MTT assay. Novel and more potent derivatives of betulinic acid (2, 4, 6-8) have been synthesized with IC(50) less than 0.4 microg/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further betulinic acid (1) inhibited TLS formation of ECV304 cells on Matrigel(TM) by 5.5% while its derivatives caused an inhibition of 13.1-49.2%.
在为期5天的MTT试验中，桦木酸（1）对内皮细胞系ECV304具有显著的细胞毒性（半数抑制浓度[IC(50)]为1.26±0.44微克/毫升）。已合成了新型且更有效的桦木酸衍生物（2、4、6 - 8），其IC(50)小于0.4微克/毫升。测定了对人肿瘤细胞系DU145、L132、A549和PA - 1的内皮细胞特异性。此外，桦木酸（1）使ECV304细胞在基质胶上的管状结构形成减少了5.5%，而其衍生物导致的抑制率为13.1% - 49.2%。
