[Radiosensitization of human tumor HeLa cells induced by methyl ester of 6-oxo-6-[2,2-ethylenedioxy-5-(dimethoxycarbonylmethyl)-cyclope nt- 1-yL]-hexanoic acid].
Methyl ester of 6-oxo-6-[2,2-ethylenedioxy-5-(dimethoxycarbonylmethyl)- cyclopent-1-yl]-hexanoic acid (7-keto-9,9-ethylenedioxiprostanoid, that is analogue of 11-deoxy-PGE1 with modified chains) at concentration 10(-6) mol/l displayed maximal (25%) sensitizing effect when was tested in a range of concentrations 10(-7)-10(-5) mol/l and HeLa cells were gamma-irradiated at dose of 2 Gy, that was compared with metronidazol action. Optimal time of prostanoid contact with cells was between 30 and 60 min, and metronidazol--60 min. Prostanoid effect was exhibited at irradiation doses from 2 to 4 Gy and reached maximum of 46% at 4 Gy, its DMF was 1.5 as well as that of metronidazol. Cytotoxicity of comparable compounds was approximately equal. By its chemical structure and sensitizing features this 7-keto-9,9-ethylenedioxiprostanoid is a prototype of new radiosensitizing drug.
Dad'kov
I G
IG
Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Minsk.
Kuz'mitskiĭ
B B
BB
Antonevich
I P
IP
Lakhvich
F A
FA
D000527:Alprostadil / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells / Q000187:drug effects* / Q000528:radiation effects; D006801:Humans; D011836:Radiation Tolerance / Q000187:drug effects; D011838:Radiation-Sensitizing Agents / Q000737:chemistry* / Q000494:pharmacology*; D011878:Radiotherapy
C409230:7-keto-9,9-ethylenedioxiprostanoid; D011838:Radiation-Sensitizing Agents; D000527:Alprostadil; C034008:11-deoxyprostaglandin E1