Novel PDE4 inhibitors derived from Chinese medicine forsythia.
Novel PDE4 inhibitors derived from Chinese medicine forsythia.
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DOI：
10.1371/journal.pone.0115937
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发表时间：
2014
期刊：
影响因子：
3.7
通讯作者：
Chen BB
中科院分区：
文献类型：
--
作者：
Coon TA;McKelvey AC;Weathington NM;Birru RL;Lear T;Leikauf GD;Chen BB
Cyclic adenosine monophosphate (cAMP) is a crucial intracellular second messenger molecule that converts extracellular molecules to intracellular signal transduction pathways generating cell- and stimulus-specific effects. Importantly, specific phosphodiesterase (PDE) subtypes control the amplitude and duration of cAMP-induced physiological processes and are therefore a prominent pharmacological target currently used in a variety of fields. Here we tested the extracts from traditional Chinese medicine, Forsythia suspense seeds, which have been used for more than 2000 years to relieve respiratory symptoms. Using structural-functional analysis we found its major lignin, Forsynthin, acted as an immunosuppressant by inhibiting PDE4 in inflammatory and immune cell. Moreover, several novel, selective small molecule derivatives of Forsythin were tested in vitro and in murine models of viral and bacterial pneumonia, sepsis and cytokine-driven systemic inflammation. Thus, pharmacological targeting of PDE4 may be a promising strategy for immune-related disorders characterized by amplified host inflammatory response.
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影响因子：
3.3
作者：
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通讯作者：
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影响因子：
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作者：
Ghiadoni, Lorenzo;Versari, Daniele;Taddei, Stefano
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作者：
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通讯作者：
Camacho CJ
DOI：
10.1016/s0140-6736(03)13413-7
发表时间：
2003-05-24
期刊：
Lancet (London, England)
影响因子：
--
作者：
Nicholls JM;Poon LL;Lee KC;Ng WF;Lai ST;Leung CY;Chu CM;Hui PK;Mak KL;Lim W;Yan KW;Chan KH;Tsang NC;Guan Y;Yuen KY;Peiris JS
通讯作者：
Peiris JS
影响因子：
4.5
作者：
Hassimotto, Neuza Mariko Ayrnoto;Genovese, Maria Ines;Lajolo, Franco Maria
通讯作者：
Lajolo, Franco Maria