Masuda H, Hirai M, Ohtawara Y, Tajima A, Aso Y
Urological Division, Enshu General Hospital.
Nihon Hinyokika Gakkai Zasshi. 1990 Apr;81(4):577-82. doi: 10.5980/jpnjurol1989.81.577.
Rats with bladder tumor induced by BBN were treated by intravesical instillation of 0.8 mg of (2"R)-4'-O-tetrahydropyranyladriamycin (THP) (9 rats) or adriamycin (ADM) (8 rats) dissolved in 0.2 ml of distilled water. Thirty minutes later, the bladder was removed surgically. Rats without the tumor received the same treatment of THP (8 rats) or ADM (9 rats). THP and ADM infiltrations to the normal bladder tissue and the tumor were estimated by the use of the photonic microscope system, since both drugs were known to emit characteristic fluorescence. It was found that infiltration of THP to the tumor tissue was more prominent in amounts and deeper than that of ADM, while smaller amounts of THP infiltrated into the normal mucosa compared to ADM. The fact might explain the clinical finding that THP instilled intravesically in half a concentration of ADM showed the same effect on the tumor as ADM. Subsequently, tissue concentrations of THP and ADM were estimated by high performance liquid chromatography. Either THP or ADM was instilled intravesically for 30 minutes to 6 rats with bladder tumor. Similarly, either THP or ADM was instilled in 5 rats without the tumors. Contrary to the result of the photonic microscope system, the tissue concentration of THP was not different from that of ADM not only in the tumor tissues but also in the normal bladder ones. Furthermore, the tissue concentration of both drugs in the normal bladder was higher than that in the bladder tumor.(ABSTRACT TRUNCATED AT 250 WORDS)
用N-丁基-N-(4-羟基丁基)亚硝胺(BBN)诱导出膀胱肿瘤的大鼠,通过膀胱内灌注溶解于0.2 ml蒸馏水中的0.8 mg(2"R)-4'-O-四氢吡喃阿霉素(THP)(9只大鼠)或阿霉素(ADM)(8只大鼠)进行治疗。30分钟后,手术切除膀胱。未患肿瘤的大鼠接受相同的THP(8只大鼠)或ADM(9只大鼠)治疗。由于已知这两种药物都会发出特征性荧光,因此使用光子显微镜系统评估THP和ADM在正常膀胱组织和肿瘤中的浸润情况。结果发现,THP在肿瘤组织中的浸润量比ADM更多且更深,而与ADM相比,浸润到正常黏膜中的THP量较少。这一事实可能解释了临床上的一个发现,即膀胱内灌注浓度为ADM一半的THP对肿瘤的疗效与ADM相同。随后,通过高效液相色谱法估算THP和ADM的组织浓度。将THP或ADM膀胱内灌注30分钟,用于6只患有膀胱肿瘤的大鼠。同样,将THP或ADM灌注到5只未患肿瘤的大鼠体内。与光子显微镜系统的结果相反,THP的组织浓度不仅在肿瘤组织中,而且在正常膀胱组织中与ADM并无差异。此外,两种药物在正常膀胱中的组织浓度高于膀胱肿瘤中的浓度。(摘要截断于250字)