5,7-Dihydroxychromone-2-carboxylic acid and it's transition-metal (Mn and Zn) chelates as non-thiol radioprotective agents.
5,7-Dihydroxychromone-2-carboxylic acid (DHCCA) and its related complexes with manganese and zinc were prepared and evaluated for radioprotection activity against gamma irradiation in mice. The LD(50) values were found to be more than 1500 and 1000 mg/kg for DHCCA and it's complexes, respectively. For studying radioprotective effects, 1.0 mmol/kg and 0.5 mmol/kg doses of compounds were administrated subcutaneously 24 h prior to 8.2 Gy gamma irradiation. The percentages of 30-day survival of mice for these compounds were 26%-50%. DHCCA exhibited significant action in delaying deaths as well as effective protection against gamma rays-induced mortality compared to reference drug amifostine. Amifostine provides effective radiation protection when administrated immediately prior to radiation exposure, but administration of DHCCA, even 24 h prior to gamma irradiation, provides a significant protection.
Hosseinimehr
Seyed Jalal
SJ
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. sjhosseinim@yahoo.com
Emami
Saeed
S
Taghdisi
Seyed Mohammad
SM
Akhlaghpoor
Shahram
S
D000818:Animals; D002614:Chelating Agents / Q000737:chemistry*; D002867:Chromones / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D015195:Drug Design; D005720:Gamma Rays; D008274:Magnesium / Q000737:chemistry*; D008297:Male; D051379:Mice; D011837:Radiation-Protective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D013438:Sulfhydryl Compounds / Q000737:chemistry; D015996:Survival Rate; D014916:Whole-Body Irradiation; D015032:Zinc / Q000737:chemistry*
C529651:5,7-dihydroxychromone-2-carboxylic acid; D002614:Chelating Agents; D002867:Chromones; D011837:Radiation-Protective Agents; D013438:Sulfhydryl Compounds; D008274:Magnesium; D015032:Zinc