Apigenin--strong cytostatic and anti-angiogenic action in vitro contrasted by lack of efficacy in vivo.
The cancer chemopreventive agent apigenin also has strong cytostatic and anti-angiogenic effects in vitro. We now investigated its efficacy against experimental Lewis lung carcinomas (LLC), C-6 gliomas and DHDK 12 colonic cancers in vivo. Tumour bearing mice received 50 mg/kg/day apigenin in three different galenical formulations during 12 days in 8-hourly intervals. Only weak effects of apigenin on the size and the number of new tumour blood vessels of both established and newly transplanted tumours were recorded although the intratumoural necrosis was elevated (45 +/- 15% vs. 20 +/- 7% (control), p < 0.05%). These results contrast sharply with the high in vitro sensitivity of LLC, C-6, DHDK 12 and endothelial cells to apigenin where complete growth suppression occurs at concentrations beyond 30 g/ml. Possible causes are discussed.
Engelmann
C
C
Humboldt University, Charité, Berlin, Germany. carsten.engelmann@charite.de
Blot
E
E
Panis
Y
Y
Bauer
S
S
Trochon
V
V
Nagy
H J
HJ
Lu
H
H
Soria
C
C
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D047310:Apigenin; D002455:Cell Division / Q000187:drug effects; D005419:Flavonoids / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D005910:Glioma / Q000188:drug therapy / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy / Q000473:pathology; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008819:Mice, Nude; D009336:Necrosis; D009368:Neoplasm Transplantation; D051381:Rats; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D005419:Flavonoids; D047310:Apigenin