• Biomedical Science Letters
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• v.3 no.1
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• pp.21-28
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• 1997

Male rats of Albino strain were divided into four groups, control group, X-irradiated group, WR-2721 treatment group and X-irradiated group treated with WR-2721. The radioprotective effect of treatment with S-2 (3-aminopropylamino)ethylphosphorothioic acid (WR-2721) in the dose of 200mg/kg by intraperitonial injection on rats 20min prior to wholebody X-irradiation (8Gy) was studied. Each group determined serum alkaline phosphatase (ALP), aspartate aminotransferase (ASI), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) activities and contents of serum glucose after 1, 3, 7 and 10 days. The ALP and AST activities of X-irradiated group were significantly decreased (p<0.05) compared with that of control group, but X-irradiated group treated with WR-2721 less decreased those enzyme activities compared with the X-irradiated group. X-irradiated group was significantly increased (p＜0.05) ALT and LDH activities compared with that of control group, but X-irradiated group treated with WR-2721 less increased those enzyme activities compared with the X-irradiated group. The concentration of serum glucose of X-irradiated group was significantly increased (p<0.05) compared with that of control group, but X-irradiated group treated with WR-2721 less increased compared with that of X-irradiated group. It may be considered that WR-2721 provided radioprotective effect of organs of body from X-irradiation.

• Journal of Pharmaceutical Investigation
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• v.17 no.2
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• pp.55-60
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• 1987

WR 2721 (S-2-(3-aminopropylaminoethylphosphorothioate) is a radioprotective drug that is now undergoing clinical trials in the United States and Japan. a liquid chromatographic electrochemical method for the determination of WR 2721 an WR 3689 [S-2-(3-methylaminopropylamino)ethylphorothioate] in human plasma was developed in this study. This method includes the use of a Hg/Au electrochemical detector and a cyano column for the direct measurement of WR 2721 and WR 3689 in plasma. An analog of WR 2721, WR 149846 was used as an internal standard. WR 2721 and WR 3689 could be well separated from the solvent front, with a mobile phase of acetonitrile-water (20:80), 0.1M acetic acid and 1.2 mM sodium octane sulfonate. This method was shown to be precise. Both intra-day and inter-day results were within 10% CV. Also, sample preparation was fairly simple. Since WR 2721 and WR 3689 were unstable at room temperature, it was essential to use an automatic sample processor with a refrigerator, especially for carrying out routine analyses.

• Journal of Radiation Protection and Research
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• v.11 no.2
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• pp.114-122
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• 1986

At present, the treatments of the radiation-induced diseases are only performing by the palliative treatment technique. Moreover, radiation protective agents are a little toxic for human being and this seriously limits their applicability with various complications in clinical uses. Accordingly, as a part of the aim of gain of the basic data for protective roles of some radioprotectors, the present investigation was carried out to evaluate the comparative radioprotective effects by the administration of DDC, MEA, WR-2721. Results are shown for statistically significant analysis and correlation with each group as follows; 1. The proper doses of the radioprotectors were DDC; 1,550 mg/kg, MEA; 450 mg/kg, WR-2721; 780 mg/kg of the mouse body weight. 2. DMF(Dose modification factor) of LD 50/10 and LD 50/30 for whole body irradiation was DDC; 1.2, MEA; 1.4, WR-2721; 1.9 and DDC; 1.7, MEA; 1.8, WR-2721; 2.5 respectively. 3. DMF for radiation reaction of jejunal crypt was DDC: 1.07, MEA: 1.21 and WR-2721: 1.76 and that of jejunal crypt cell was DDC: 1.04, MEA: 1.08 and WR-2721: 1.38 respectively. 4. Conclusively, WR-2721 was the most effective drung among the three radioprotectors and this result must be a supportive data for further study for clinical application.

• Journal of radiological science and technology
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• v.20 no.1
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• pp.91-96
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• 1997

Male rats of Albino strain were divided into four groups. The radioprotective effect of treatment with S-2(3-aminopropylamino)ethylphosphorothioic acid(WR-2721) using the dose of 200 mg/kg by intraperitonial injection on rats for 20 min prior to whole body x-ray irradiation (8 Gy) was studied. The harzardous effects of x-ray irradiation were greatly corrected In the treated group. The concentrations of total serum cholesterol, HDL-cholesterol, triglyceride, and phospholipid were greatly affected, showing insignificant changes in the treated group of animals. The drastic hyperglycemic effect of x-ray irradiation in the untreated group decreased to a normal level. These results show the potentiality of WR-2721 as a radioprotective agent.

• Proceedings of the Korean Nuclear Society Conference
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• 2004.10a
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• pp.1204-1205
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• 2004

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.1
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• pp.291-297
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• 2014

The radioprotective effects of a single administration of kojic acid (KA) against ionizing radiation were evaluated via assessment of 30-day survival and alterations of peripheral blood parameters of adult C57BL/6 male mice. The 30-day survival rate of mice pretreated with KA (75 or 300 mg/kg body weight, KA75 or KA300) subcutaneously 27 h prior to a lethal dose (8 Gy, 153.52 cGy/min) of gamma irradiation was higher than that of mice irradiated alone (40% or 60% vs 0%). It was observed that the white blood cell (WBC) count/the red blood cell (RBC) count, haemoglobin content, haematocrit and platelet count of mice with or without KA pretreatment as exposed to a sub-lethal dose (4 Gy, 148.14 cGy/min) of gamma irradiation decreased maximally at day 4/day 8 post-irradiation. Although the initial WBC values were low in KA300 or WR-2721 (amifostine) groups, they significantly recovered to normal at day 19, whereas in the control group they did not. The results from the cytotoxicity and cell viability assays demonstrated that KA could highly protect Chinese hamster ovary (CHO) cells against ionizing radiation with low toxicity. In summary, KA provides marked radioprotective effects both in vivo and in vitro.

• Journal of Chest Surgery
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• v.31 no.9
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• pp.845-854
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• 1998

Background: S-2-(3 aminoprophlamino) ethylphosphorothioic acid(WR-2721) is one of the radical scavenging thiols. We tested its protective effects in the reperfused heart. Material and Method: The experimental setup was the constant pressure Langendorffs perfusion system. We investigated the radical scavenging properties of this compound in isolated rat hearts which were exposed to 20 minutes ischemia and 20 minutes reperfusion. Four experimental groups were used:group I, control, Amifostine 50 mg(1 mL) peritoneal injection 30 minutes before ischemia(group II), Amifostine 10 mg(0.2 mL) injection during ischemia through coronary artery(group III),and Amifostine 50 mg(1 mL) peritoneal injection 2 hrs before ischemia(group IV). The experimental parameters were the levels of latate, CK-MB, and adenosine deaminase(ADA) in frozen myocardium, the quantity of coronary flow,and left ventricular developed pressure, and it's dp/dt. Statistical analysis was performed using repeated measured analysis of variance and student t-test. Result: The coronary flow of group II and IV were less than group I and III at equilibrium state but recovery of coronary flow at reperfusion state of group II, III, and IV were more increased compared with group I. The change of systolic left ventricular devoloping pressure of group II and IV were less than control group at equilibrium state, which seemed to be the influence of the pharmacological hypotensive effect of amifostine. But it was higher compared with group I at reperfusion state. The lactic acid contents of group II were less than control group in frozen myocardium.(Group I was 0.20 0.29 mM/g vs Group II, which was 0.10 0.11 mM/g). The quantity of CK-MB in myocardial tissue was highest in group IV (P=0.026 I: 120.0 97.8 U/L vs IV: 242.2 79.15 U/L). The adenosine deaminase contents in the coronary flow and frozen myocardium were not significantly different among each group. Conclusion: Amifostine seemed to have significant cardioprotective effect during ischemia and reperfusion injuries of myocardium.