• 대한의생명과학회지
• /
• 제3권1호
• /
• pp.21-28
• /
• 1997

S-2 (3-aminopropylamino)ethylphosphorothioic acid (WR-2721)이 방사선에 대한 방어 효과에 미치는 영향을 규명 하고자 Sprague-Dawley계 웅성 흰쥐를 대조군, WR-2721 단독투여 군 (200mg/kg), X-선 단독조사군, WR-2721투여 (200mg/kg)후 X-선 조사한 병용군으로 나누어 X-선 8 Gy선량을 전신 조사한 후 1, 3, 7, 10일 간에 각각 혈액을 채취하여 효소활성 치와 glucose함량 변화를 측정하여 다음과 같은 결과를 얻었다. X-선 단독조사군에서는 ALP와 AST의 활성치가 대조군에 비하여 감소하였으나 WR-2721을 병용한 군에서는 그 감소폭이 줄어들었고, ALT와 LDH의 활성치는 X-선 단독조사군에서 대조군에 비하여 증가하였고, WR-2721을 병용한 군에서는 그 증가폭이 감소되었다. 또한 glucose치의 변동은 X-선 단독 조사군에서 대조군에 비하여 유의성 있게 증가하였으나 WR-2721을 병용한 군에서는 그 증가폭이 감소되었다. 이로 미루어 보아 WR-2721이 X-선으로부터 생체내 주요 장기들을 보호하는 작용이 있음을 시사하고 있다.

• Journal of Pharmaceutical Investigation
• /
• 제17권2호
• /
• pp.55-60
• /
• 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
• /
• 제11권2호
• /
• pp.114-122
• /
• 1986

방사선장해(放射線障害) 예방약제(豫防藥劑)의 인체적용(人體適用)은 약제(藥劑)의 부작용(副作用)으로 아직 임상적(臨床的) 이용(利用)이 되지 못한 실정(實情)으로서 생리학적(生理學的) 및 약리학적(藥理學的) 독성(毒性), 물리학적(物理學的) 제성질(諸性質), 약제(藥劑)의 작용기전(作用機轉) 구명(究明) 및 임상적(臨床的) 기술개발(技術開發)이 미흡(未洽)하여 방사선(放射線) 장해자(障害者)에 대(對)한 치료(治療)는 대증료법(對症療法)에 불과(不過)한 실정(實情)이다. 저자(著者)들은 방사선(放射線)에 의(依)한 인체장해예방(人體障害豫防)에 필요(必要)한 기초자료(基礎資料)를 얻기 위하여 현재(現在)까지 비교적(比較的) 독성(毒性)이 적고 화학적(化學的)으로 안정(安定)하며 약효(藥效)가 우수(優秀)하다고 알려진 DDC, MEA, WR-2721을 선정(選定)하여 실험동물(實驗動物) 비근교계(非近交系) Swiss Webster(NIH-GP) 마우스에 이용(利用)한 방사선(放射線) 방호작용(防護作用)에 관(關)한 실험결과(實驗結果)는 다음과 같다. 1) 각종(各種) 방사선(放射線) 방호제(防護劑)(DDC, MEA, WR-2721)의 마우스에 대한 적정(適定) 투여량(投與量)은 각각(各各) DDC; 1,000, MEA; 200, WR-2721; 400 mg/kg 이었다. 2) 실험동물(實驗動物)의 방사선(放射線) 반치사선량(半致死線量) LD50/10에 대(對)한 약제(藥劑)의 방호효과(防護效果) DMF는 DDC; 1.2, MEA; 1.4, WR-2721; 1.9이었고 LD50/30에 대(對)한 DMF는 DDC; 1.7, MEA; 1.8, WR-2721; 2.5이었다. 3) 공장(空腸) 소낭선(小囊腺)(Jejunum crypt)의 방사선평균치사선량(放射線平均致死線量)(Do)에 대(對)한 방호효과(防護效果) DMF는 DDC: 1.07, MEA; 1.21, WR-2721; 1.76이었고, 소낭선세포(小囊腺細胞)의 방사선(放射線) 평균치사선량(平均致死線量)에 대(對)한DMF는 DDC; 1.04, MEA; 1.08, WR-2721; 1.38이었다. 4) 이상(以上)으로 상기(上記) 3종(種)의 방사선(放射線) 방호제중(放護劑中) WR-2721의 방사선(放射線) 방호효과(防護效果)가 가장 우수(優秀)하였고 이 결과(結果)는 향후(向後) 임상적(臨床的) 적용(適用)에 관(關)한 연구(硏究)의 기초자료(基礎資料)가 될 것으로 사료(思料)된다.

• 대한방사선기술학회지:방사선기술과학
• /
• 제20권1호
• /
• pp.91-96
• /
• 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.

• 한국원자력학회:학술대회논문집
• /
• 한국원자력학회 2004년도 추계학술발표회 발표논문집
• /
• pp.1204-1205
• /
• 2004

• Asian Pacific Journal of Cancer Prevention
• /
• 제15권1호
• /
• pp.291-297
• /
• 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
• /
• 제31권9호
• /
• pp.845-854
• /
• 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.