目的:研究新疆阿魏Ferula sinkiangensis K. M. Shen地上部位的化学成分,以发现新的抗炎活性先导化合物。方法:采用硅胶、Sephadex LH-20凝胶、半制备液相等色谱方法对新疆阿魏地上部位的二氯甲烷部位进行分离纯化,通过紫外光谱、红外...目的:研究新疆阿魏Ferula sinkiangensis K. M. Shen地上部位的化学成分,以发现新的抗炎活性先导化合物。方法:采用硅胶、Sephadex LH-20凝胶、半制备液相等色谱方法对新疆阿魏地上部位的二氯甲烷部位进行分离纯化,通过紫外光谱、红外光谱、高分辨质谱、核磁共振波谱、圆二色散谱和Mosher反应等对化合物结构进行鉴定,并对其体外抗炎活性进行筛选。结果:从新疆阿魏地上部位95%乙醇提取物的二氯甲烷部位分离得到1对新的非对映异构体(4′R,5′S,6′R,9′R)-新疆阿魏醇A (1)和(4′S,5′R,6′R,9′R)-新疆阿魏醇A (2),其对脂多糖诱导的小鼠单核巨噬细胞RAW264.7产生一氧化氮具有不同程度的抑制作用。结论:化合物1和2为从新疆阿魏地上部位中分离得到的1对新的非对映异构体且具有一定的抗炎活性。展开更多
Influenza virus infection is a global public health issue.The effectiveness of antiviral agents for influenza has been limited by the emergence of drugresistant virus strains.Therefore,there is an urgent need to ident...Influenza virus infection is a global public health issue.The effectiveness of antiviral agents for influenza has been limited by the emergence of drugresistant virus strains.Therefore,there is an urgent need to identify novel antiviral therapies.Our previous studies have found that Cryptoporus volvatus extract could potently inhibit influenza virus replication in vitro and in vivo.However,the effective component of Cryptoporus volvatus which mediated the antiviral activity hasn′t been identified.Here,we identified a novel anti-influenza molecule,cryptoporic acid E(CAE),from Cryptoporus volvatus.Our results showed that CAE had broad-spectrum anti-influenza activity against 2009 pandemic strain A/Beijing/07/2009(H1N1/09),seasonal strain A/Jiangxi/262/05(H3N2),mouse adapted strains A/WSN/33(H1N1)and A/PR8/34(H1N1).We further investigated the mode of CAE action,and found that CAE directlyattenuated influenza virus infectivity.Time-course-analysis indicated that CAE exerted its inhibition mainly at middle stage of the replication cycle of influenza virus.Subsequently,we confirmed that CAE blocked virus RNA replication and transcription in MDCK cells and CAE repressed influenza virus RNA polymerase activity.In addition,we found that CAE impaired influenza virus infectivity by directly targeting virus particles.Our data suggest that CAE is a major effective component of Cryptoporus volvatus and might be a potential candidate for the development of a new anti-influenza virus therapy.展开更多
文摘目的:研究新疆阿魏Ferula sinkiangensis K. M. Shen地上部位的化学成分,以发现新的抗炎活性先导化合物。方法:采用硅胶、Sephadex LH-20凝胶、半制备液相等色谱方法对新疆阿魏地上部位的二氯甲烷部位进行分离纯化,通过紫外光谱、红外光谱、高分辨质谱、核磁共振波谱、圆二色散谱和Mosher反应等对化合物结构进行鉴定,并对其体外抗炎活性进行筛选。结果:从新疆阿魏地上部位95%乙醇提取物的二氯甲烷部位分离得到1对新的非对映异构体(4′R,5′S,6′R,9′R)-新疆阿魏醇A (1)和(4′S,5′R,6′R,9′R)-新疆阿魏醇A (2),其对脂多糖诱导的小鼠单核巨噬细胞RAW264.7产生一氧化氮具有不同程度的抑制作用。结论:化合物1和2为从新疆阿魏地上部位中分离得到的1对新的非对映异构体且具有一定的抗炎活性。
基金The project supported by Young Scientist Funding from Beijing Natural Science Foundation(7154225)by Innovative Research Team in IMPLAD
文摘Influenza virus infection is a global public health issue.The effectiveness of antiviral agents for influenza has been limited by the emergence of drugresistant virus strains.Therefore,there is an urgent need to identify novel antiviral therapies.Our previous studies have found that Cryptoporus volvatus extract could potently inhibit influenza virus replication in vitro and in vivo.However,the effective component of Cryptoporus volvatus which mediated the antiviral activity hasn′t been identified.Here,we identified a novel anti-influenza molecule,cryptoporic acid E(CAE),from Cryptoporus volvatus.Our results showed that CAE had broad-spectrum anti-influenza activity against 2009 pandemic strain A/Beijing/07/2009(H1N1/09),seasonal strain A/Jiangxi/262/05(H3N2),mouse adapted strains A/WSN/33(H1N1)and A/PR8/34(H1N1).We further investigated the mode of CAE action,and found that CAE directlyattenuated influenza virus infectivity.Time-course-analysis indicated that CAE exerted its inhibition mainly at middle stage of the replication cycle of influenza virus.Subsequently,we confirmed that CAE blocked virus RNA replication and transcription in MDCK cells and CAE repressed influenza virus RNA polymerase activity.In addition,we found that CAE impaired influenza virus infectivity by directly targeting virus particles.Our data suggest that CAE is a major effective component of Cryptoporus volvatus and might be a potential candidate for the development of a new anti-influenza virus therapy.
