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WANG Xiao-Li, WANG Zhao-Ya, LING Jing-Jing, ZHANG Yi-Hua, YIN Jian. Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (H2S) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents[J]. 中国天然药物, 2016, 14(12): 946-953.
引用本文: WANG Xiao-Li, WANG Zhao-Ya, LING Jing-Jing, ZHANG Yi-Hua, YIN Jian. Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (H2S) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents[J]. 中国天然药物, 2016, 14(12): 946-953.
WANG Xiao-Li, WANG Zhao-Ya, LING Jing-Jing, ZHANG Yi-Hua, YIN Jian. Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (H2S) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents[J]. Chinese Journal of Natural Medicines, 2016, 14(12): 946-953.
Citation: WANG Xiao-Li, WANG Zhao-Ya, LING Jing-Jing, ZHANG Yi-Hua, YIN Jian. Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (H2S) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents[J]. Chinese Journal of Natural Medicines, 2016, 14(12): 946-953.

Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (H2S) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents

Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (H2S) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents

  • 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 H2S, 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 an-tiplatelet agents for the treatment of thrombosis-related ischemic stroke.

     

    Abstract: 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 H2S, 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 an-tiplatelet agents for the treatment of thrombosis-related ischemic stroke.

     

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