Effects of 5-Amyno-4-(1,3-benzothyazol-2-yn)-1-(3-methoxyphenyl)-1,2-dihydro-3H-pyrrol-3-one Intake on Digestive System in a Rat Model of Colon Cancer.
BACKGROUND
Pyrrol derivate 5-amyno-4-(1,3-benzothyazol-2-yn)-1-(3-methoxyphenyl)-1,2-dihydro-3H-pyrrol-3-one (D1) has shown antiproliferative activities in vitro, so investigation of the impact of D1 intake on gut organs in rats that experienced colon cancer seems to be necessary.


METHODS
D1 at the dose of 2.3 mg/kg was administered per os daily for 27 (from the 1st day of experiment) or 7 (from the 21st week of experiment) weeks to rats that experienced 1,2-dimethylhydrazine (DMH)-induced colon cancer for 20 weeks. 5-Fluorouracil (5FU) was chosen as reference drug and was administered intraperitoneally weekly for 7 weeks (from the 21st week of experiment) at the dose of 45 mg/kg.


RESULTS
Antitumor activity of D1 comparable with the 5FU one against DMH-induced colon cancer in rats was observed (decrease of tumor number and tumor total area up to 46%). D1 attenuated the inflammation of colon, gastric and jejunal mucosa, and the liver, caused by DMH, unlike 5FU, aggravating the latter. In addition, D1 partially normalized mucosa morphometric parameters suggesting its functional restore.


CONCLUSIONS
D1 possesses, comparable with 5-fluorouracil antitumor efficacy, less damaging effects on the tissues beyond cancerous areas and contributes to partial morphological and functional gut organs recovery.
Institute of Biology, Taras Shevchenko National University, 64/13 Volodymyrska Street, Kyiv 01601, Ukraine.
Halyna M
HM
Kuznietsova
Institute of Biology, Taras Shevchenko National University, 64/13 Volodymyrska Street, Kyiv 01601, Ukraine.
Valentyna K
VK
Luzhenetska
Institute of Biology, Taras Shevchenko National University, 64/13 Volodymyrska Street, Kyiv 01601, Ukraine.
Iryna P
IP
Kotlyar
Institute of Biology, Taras Shevchenko National University, 64/13 Volodymyrska Street, Kyiv 01601, Ukraine.
Volodymyr K
VK
Rybalchenko
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D052160:Benzothiazoles / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D003106:Colon / Q000187:drug effects / Q000473:pathology; D003110:Colonic Neoplasms / Q000097:blood / Q000188:drug therapy*; D004064:Digestive System / Q000187:drug effects* / Q000473:pathology; D004195:Disease Models, Animal; D005472:Fluorouracil / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D009092:Mucous Membrane / Q000187:drug effects; D011760:Pyrrolidinones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D017208:Rats, Wistar
C585406:5-amino-4-(1,3-benzothiazol-2-yl)-1-(3-methoxyphenyl)-1,2-dihydro-3H-pyrrol-3-one; D000970:Antineoplastic Agents; D052160:Benzothiazoles; D011760:Pyrrolidinones; D005472:Fluorouracil