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Synthesis of novel methotrexate derivatives with inhibition activity of nitric oxide synthase

Chinese Chemical Letters 2009年第2期20卷 178-180页

作者： Ming Sheng Feng Ping Guo Li Xun Jiang Jing Bo Shi Yu Ping Cao Qi Zheng Yao Department of Medicinal Chemistry China Pharmaceutical University Nanjing 210009 China Nanjing Hicin Pharmaceutical Co. Ltd. Nanjing 210046 China

Seventeen 4-alkylamino/arylamino-substituted methotrexate （MTX） derivatives 6a-14a were designed and synthesized. Their inhibition activities against inducible nitric oxide synthase （iNOS） were evaluated in vitro. The pharmacological results showed that most of the prepared compounds displayed the potent inhibitory effects on iNOS.

关键词： Tetrahydrobiopterin inhibitor of nitric oxide synthase Synthesis Methotrexate

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Effects of aminoguanidine on retinal apoptosis in mice with oxygen-induced retinopathy

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International Journal of Ophthalmology(English edition) 2013年第4期6卷 436-441页

作者： An-Jie Du Bing Ren Xiao-Wei Gao Lei Yang Yan Fu Xu-Dong Zhao Ophthalmic Center No.474 Hospital of Chinese PLA Department of Ophthalmology Yuncheng Central Hospital Department of Ophthalmology Baoding First Central Hospital

AIM:To explore the protective effects of amino-guanidine(AG) on retinal apoptosis in mice with oxygeninduced retinopathy(OIR).·METHODS:A total of 80 C57BL/6J mice,aged 7 days,were randomly divided into four groups:normal,high oxygen,high oxygen saline and high oxygen treated with *** the normal group,mice were housed in normoxic conditions from postnatal day P7 to *** in the other 3 groups were placed under hyperoxic conditions(75 ±2% O2) in an oxygen-regulated chamber for 5 days and subsequently placed in normoxic conditions for *** in the AG group were treated once daily,from P12 to P17,with AG hemisulfate(100mg/kg body weight,intraperitoneally) dissolved in physiological *** equivalent amount of 0.9% physiological saline was administered,as above,to mice in the high oxygen saline *** mice were randomly selected from each group on P14 and on P17,euthanized and the retinas *** cells in the retina were detected using the terminal-deoxynucleoitidyl transferase mediated nick end labeling(TUNEL) *** expression of nitric oxide synthase(iNOS) in the retina was detected by immunohistochemistry and changes in rod cells were observed using electron microscopy.·RESULTS:TUNEL-positive cells and iNOS immunoreactive neurons were present in the inner nuclear and ganglion cell retinal layers of mice in the high oxygen *** number of TUNEL-positive cells was significantly greater in the high oxygen group compared with the normal group(t =-20.81,P14d<0.05;t =-15.05,P17d<0.05).However,the number of TUNEL-positive cells in the AG treatment group was significantly lower(t =-13.21,P14d<0.05;t =-6.61,P17d<0.05) compared with thehigh oxygen *** expression of iNOS was significantly higher in the high oxygen group compared with the normal group(t =-21.95,P14d<0.05;t =-17.30,P17d<0.05).However,the expression of iNOS in the AG treatment group was significantly lower(t =-12.17,P14d<0.05;t =-10.30,P17d<0.05) com

关键词： aminoguanidine retinopathy of prematurity apoptosis inhibitor of nitric oxide synthase

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