Kostenich G A, Zhuravkin I N, Zhavrid E A
Department of Chemoradiotherapy, Research Institute of Oncology and Medical Radiology, Minsk, Belarus.
J Photochem Photobiol B. 1994 Mar;22(3):211-7. doi: 10.1016/1011-1344(93)06974-8.
The toxicity, pharmacokinetics and antitumour effect of chlorin e6 after light irradiation were studied. The LD50 value of chlorin e6 in C3H mice is 189 +/- 9 mg kg-1 and in Wistar white rats is 113 +/- 18 mg kg-1 14 days after intraperitoneal injection. The concentration of chlorin e6 in blood, liver, kidney, spleen and tumors (sarcoma M-1 and sarcoma 45) of the rats was determined by a fluorescence method, 3, 6, 12, 18, 24, 48 and 72 h after administration at a dose of 10 mg kg-1. For this purpose, chlorin e6 was extracted from tissues by the detergent Triton X-100. The depth of necrosis in sarcoma 45, the regression rate of sarcoma M-1 and the animal cure rate were evaluated after chlorin e6 administration at doses of 1-10 mg kg-1 and subsequent irradiation with krypton laser light. Depending on the dose and the time interval between chlorin e6 injection and irradiation, the depth of necrosis in sarcoma 45 varied from 5.0 to 15.0 mm. The cure rate of the animals with sarcoma M-1 varied from 10% to 60%. The antitumor effect was directly proportional to the chlorin e6 dose and light energy exposure and inversely proportional to the time interval between photosensitizer injection and irradiation.
研究了二氢卟吩e6光照后的毒性、药代动力学及抗肿瘤作用。腹腔注射14天后，二氢卟吩e6在C3H小鼠中的半数致死量（LD50）值为189±9 mg·kg-1，在Wistar大白鼠中为113±18 mg·kg-1。以10 mg·kg-1的剂量给药后，于3、6、12、18、24、48和72小时，采用荧光法测定大鼠血液、肝脏、肾脏、脾脏及肿瘤（肉瘤M-1和肉瘤45）中二氢卟吩e6的浓度。为此，用去污剂Triton X-100从组织中提取二氢卟吩e6。给予1-10 mg·kg-1剂量的二氢卟吩e6并随后用氪激光照射后，评估肉瘤45的坏死深度、肉瘤M-1的消退率及动物治愈率。根据二氢卟吩e6注射与照射之间的剂量和时间间隔，肉瘤45的坏死深度在5.0至15.0 mm之间变化。患有肉瘤M-1的动物治愈率在10%至60%之间变化。抗肿瘤作用与二氢卟吩e6剂量和光能暴露成正比，与光敏剂注射和照射之间的时间间隔成反比。
