Department of Pharmacology, Chemical Carcinogenesis and Chemoprevention Program of Penn State Hershey Cancer Institute, CH72, Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
Eur J Med Chem. 2010 Aug;45(8):3265-73. doi: 10.1016/j.ejmech.2010.04.001. Epub 2010 Apr 10.
A series of novel organoselenocyanate compounds (6a-d) having spiro[tetralin-1,3'-pyrrolidine] moiety were synthesized. The compounds were evaluated for their inhibitory activity against cadmium- (Cd) induced toxicity in Swiss Albino mice. All the compounds (6a-d) inhibited the level of lipid peroxidation (LPO) and upregulated the activity of glutathione-S-transferase (GST), superoxide dismutase (SOD), catalase (CAT) and reduced glutathione (GSH) levels in treatment group in comparison to the untreated Cd control group. Serum transaminase activities, e.g., alanine aminotransferase (ALT) and aspartate aminotransferase (AST) were also significantly lowered in the compound-treated mice. Elongation of the alkyl chain length bearing the selenocyanate (SeCN) active group enhanced the potency of the compounds, 6d being the most active one (6d>6c>6b>6a).
一系列具有螺[四氢萘-1,3'-吡咯烷]部分的新型有机硒氰酸酯化合物（6a-d）被合成。评估了这些化合物对瑞士白化病小鼠镉（Cd）诱导毒性的抑制活性。与未处理的 Cd 对照组相比，所有化合物（6a-d）均抑制了脂质过氧化（LPO）水平，并上调了谷胱甘肽-S-转移酶（GST）、超氧化物歧化酶（SOD）、过氧化氢酶（CAT）和还原型谷胱甘肽（GSH）的活性。化合物处理的小鼠血清转氨酶活性，如丙氨酸氨基转移酶（ALT）和天冬氨酸氨基转移酶（AST）也显著降低。具有硒氰酸酯（SeCN）活性基团的烷基链长度的延长增强了化合物的效力，6d 是最有效的一种（6d>6c>6b>6a）。
