Bolzán Alejandro D, Bianchi Martha S
Laboratorio de Citogenética y Mutagénesis, Instituto Multidisciplinario de Biología Celular (IMBICE), C.C. 403, 1900, La Plata, Argentina.
Mutat Res. 2002 Dec;512(2-3):121-34. doi: 10.1016/s1383-5742(02)00044-3.
Streptozotocin (Streptozocin, STZ, CAS No. 18883-66-4) is a monofunctional nitrosourea derivative isolated from Streptomyces achromogenes. It has broad spectrum antibiotic activity and antineoplastic properties and is often used to induce diabetes mellitus in experimental animals through its toxic effects on pancreatic beta cells. STZ is a potent alkylating agent known to directly methylate DNA and is highly genotoxic, producing DNA strand breaks, alkali-labile sites, unscheduled DNA synthesis, DNA adducts, chromosomal aberrations, micronuclei, sister chromatid exchanges, and cell death. This antibiotic was found to be mutagenic in bacterial assays and eukaryotic cells. STZ is also carcinogenic; a single administration induces tumors in rat kidney, liver, and pancreas. Several lines of evidence indicate that free radicals are involved in the production of DNA and chromosome damage by this compound. Because of the use of STZ as an antineoplastic agent, the study of its genotoxicity has considerable practical significance. The purpose of this review is to present our current knowledge regarding the genotoxicity of STZ.
链脲佐菌素（链脲霉素，STZ，化学物质登记号：18883-66-4）是一种从产色链霉菌中分离得到的单功能亚硝基脲衍生物。它具有广谱抗生素活性和抗肿瘤特性，常通过对胰腺β细胞的毒性作用来诱导实验动物患糖尿病。STZ是一种强效烷化剂，已知可直接使DNA甲基化，具有高度遗传毒性，会导致DNA链断裂、碱不稳定位点、非预定DNA合成、DNA加合物、染色体畸变、微核、姐妹染色单体交换以及细胞死亡。这种抗生素在细菌试验和真核细胞中具有致突变性。STZ也具有致癌性；单次给药可诱导大鼠肾脏、肝脏和胰腺产生肿瘤。多条证据表明自由基参与了该化合物导致的DNA和染色体损伤。由于STZ被用作抗肿瘤药物，对其遗传毒性的研究具有相当大的实际意义。本综述的目的是介绍我们目前关于STZ遗传毒性的知识。
