Anti-cancer activity and mechanisms of 25-anhydrocimigenol-3-O-beta-D-xylopyranoside isolated from Souliea vaginata on hepatomas.
Our previous study first revealed the cytotoxicity and relative selectivity of 25-anhydrocimigenol-3-O-beta-D-xylopyranoside (ACX) on HepG2 and R-HepG2 cells. In the present study, the anti-cancer activity and mechanisms of ACX isolated from S. vaginata were investigated both in vitro and in vivo. ACX showed significant, consistent anti-proliferative activity on hepatoma bel-7402 cells by MTT and clone formation assays with an IC50 value of 18 mumol/l. Morphological observation and flow cytometry results showed that apoptosis and G0/G1 cell cycle arrest contributed to the cytotoxic and cytostatic effects. Further studies showed that Bax and p21 protein expression were upregulated, Bcl-2 protein expression was downregulated, and poly(ADP-ribose) polymerase protein was cleaved. Moreover, ACX also exhibited a dose-dependent inhibition of tumor growth on mice implanted with H22 in vivo. These findings implicate ACX as a promising anti-cancer agent for chemotherapy of certain cancers.
Tian
Ze
Z
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Zhou
Liang
L
Huang
Feng
F
Chen
Sibao
S
Yang
Junshan
J
Wu
Erxi
E
Xiao
Peigen
P
Yang
Mengsu
M
D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation / Q000187:drug effects; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D008297:Male; D051379:Mice; D029626:Ranunculaceae; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D015854:Up-Regulation / Q000187:drug effects; D051028:bcl-2-Associated X Protein / Q000378:metabolism; D018631:ras Proteins / Q000378:metabolism
D000970:Antineoplastic Agents; D014315:Triterpenes; D051028:bcl-2-Associated X Protein; D018631:ras Proteins