Betulinic acid and its derivatives as anti-angiogenic agents.
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%.
Mukherjee
Rama
R
Divisions of Experimental Oncology, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201 010, UP, India.
Jaggi
Manu
M
Rajendran
Praveen
P
Siddiqui
Mohammad J A
MJ
Srivastava
Sanjay K
SK
Vardhan
Anand
A
Burman
Anand C
AC
D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000094062:Betulinic Acid
D020533:Angiogenesis Inhibitors; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid