Antipyretic activity of cinnamyl derivatives and related compounds in influenza virus-infected mice
Antipyretic activity of cinnamyl derivatives and related compounds in influenza virus-infected mice
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DOI：
10.1016/s0014-2999(98)00121-6
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发表时间：
1998-05-01
影响因子：
5
通讯作者：
Shiraki, K
中科院分区：
文献类型：
--
作者：
Kurokawa, M;Kumeda, CA;Shiraki, K
Kakkon-to由七种中草药组成，在小鼠鼻内流感病毒感染模型中通过抑制干扰素反应产生的IL-1a显示出新的解热活性。利用该模型，从中草药中鉴定出具有新生物活性的解热化合物。肉桂有机溶剂提取物具有明显的解热活性。我们从48个肉桂基衍生物及可能主要涉及的相关化合物中筛选出6个解热化合物。其解热活性与IL-1α调节活性显著相关。其中四种药物将白介素1α的产生抑制到基础水平，并在注射白介素1α的小鼠中显示出与阿司匹林不同的解热作用模式。这四个化合物的结构-生物活性关系表明，酯键对解热和白细胞介素1α的调节活性都起着重要的作用。这些化合物可能有助于分析发热过程中产生白介素1α的细胞，以及通过抑制干扰素诱导的白介素1α产生而退热的机制。(C)1998年爱思唯尔科学公司。
Kakkon-to is composed of seven medicinal herbs and exhibited novel antipyretic activity by suppressing interleukin-la production responsive to interferon in a murine intranasal influenza virus infection model. Using this model, antipyretic compounds with such novel biological activities were characterized from the herbs. The organic solvent-extractable fractions of Cinnamomum cassia among the herbs showed antipyretic activity. We selected six antipyretic compounds from 48 cinnamyl derivatives and related compounds that may be mainly involved in the fractions. Their antipyretic activity was significantly correlated with interleukin-1 alpha regulatory activity. Four of them suppressed interleukin-1 alpha production to a basal level and showed different mode of antipyretic action from that of aspirin in interleukin-1 alpha-injected mice. Structure-bioactivity relationship of the four suggested that an ester bond played an important role for both antipyretic and interleukin-1 alpha regulatory activities. These compounds may be useful in analyzing interleukin-1 alpha-producing cells in fever production and the mechanism of defervescence by suppressing interferon-induced interleukin-1 alpha production. (C) 1998 Elsevier Science B.V.