摘要
In the present study, a series of novel nitric oxide-hydrogen sulfide releasing derivatives of(S)-3-n-butylphthalide((S)-NBP) were designed, synthesized, and evaluated as potential antiplatelet agents. Compound NOSH-NBP-5 displayed the strongest activity in inhibiting the arachidonic acid(AA)- and adenosine diphosphate(ADP)-induced platelet aggregation in vitro, with 3.8- and 7.0-fold more effectiveness than(S)-NBP, respectively. Furthermore, NOSH-NBP-5 could release moderate levels of NO and H2 S, which would be beneficial in improving cardiovascular and cerebral circulation. Moreover, NOSH-NBP-5 could release(S)-NBP when incubated with rat brain homogenate. In conclusion, these findings may provide new insights into the development of novel antiplatelet agents for the treatment of thrombosis-related ischemic stroke.
In the present study, a series of novel nitric oxide-hydrogen sulfide releasing derivatives of（S）-3-n-butylphthalide（（S）-NBP） were designed, synthesized, and evaluated as potential antiplatelet agents. Compound NOSH-NBP-5 displayed the strongest activity in inhibiting the arachidonic acid（AA）- and adenosine diphosphate（ADP）-induced platelet aggregation in vitro, with 3.8- and 7.0-fold more effectiveness than（S）-NBP, respectively. Furthermore, NOSH-NBP-5 could release moderate levels of NO and H2 S, which would be beneficial in improving cardiovascular and cerebral circulation. Moreover, NOSH-NBP-5 could release（S）-NBP when incubated with rat brain homogenate. In conclusion, these findings may provide new insights into the development of novel antiplatelet agents for the treatment of thrombosis-related ischemic stroke.
基金
supported by the National Natural Science Foundation for Young Scientists of China(Nos:21502071 and 21302068)
the Natural Science Foundation of Jiangsu Province,China(Nos:BK20140154 and BK20130127)
the Fundamental Research Funds for the Central Universities(Nos:JUSRP51411B and JUSRP51629B)
作者简介
[Corresponding author] Tel： 86-25-8327- 1015, Fax： 86-25-83271015, E-mail： zyhtgd@163.com
[Corresponding author] Tel： 86-510-85328229, Fax： 86-510-8532- 8229, E-mail： jianyin@jiangnan.edu.cn
