Antitumoral activity of patulin and patulin-cysteine adducts.
A comparison between the cytotoxicity and the anti-tumoral activity of patulin and patulin-cysteine adducts has been conducted. In vitro assays using L 1210 and P 388 cells showed that patulin-cysteine adducts had less cytotoxic activity than patulin (IC50 was 4 fold of IC50 patulin). In vivo, cysteine not only reduced the toxicity of patulin but also reduced its antitumoral activity against L 1210 and P 388 mouse leukemias (respectively of 25.7% and 46.6% with 3 mg.kg-1.d-1). By addition on patulin at the 4 or 7 position, cysteine might interfere with the lactone function and the -CH2- in in position 6 which are responsible for the antitumoral activity.
Krivobok
S
S
Laboratoire de Botanique, Cryptogamie, Biologie Cellulaire et Génétique, UFR de Pharmacie, Université, J. Fourier (Grenoble I), Meylan, France.
Seigle-Murandi
F
F
Steiman
R
R
Benoit-Guyod
J L
JL
Bartoli
M H
MH
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D003545:Cysteine / Q000737:chemistry*; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D016685:Mitomycin / Q000494:pharmacology; D010365:Patulin / Q000737:chemistry / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D016685:Mitomycin; D010365:Patulin; D003545:Cysteine