中药不论在直接抑制肿瘤生长,还是辅助西医治疗肿瘤方面都发挥着不容忽视的作用.本文经检索中国知网、万方、维普、Pubmed、Web of Science等数据库,纳入中药汤剂联合化疗治疗非小细胞肺癌(NSCLC)的随机对照试验,通过Meta、用药规律、...中药不论在直接抑制肿瘤生长,还是辅助西医治疗肿瘤方面都发挥着不容忽视的作用.本文经检索中国知网、万方、维普、Pubmed、Web of Science等数据库,纳入中药汤剂联合化疗治疗非小细胞肺癌(NSCLC)的随机对照试验,通过Meta、用药规律、网络药理学和细胞实验等分析方法系统评价中药联合化疗治疗NSCLC的疗效、安全性及作用机制,最终纳入56篇文献进行统计分析,共4992例患者、57首处方、172味中药.结果显示,中药联合化疗治疗组的1年生存率、肝功能损伤、总有效率、胃肠道不良反应等方面均优于单纯化疗组.用药频次>20的有7味:药味以甘苦为主,药性以寒温为主,主要归为肺经和肝经.得到5个高频药物聚类,关联规则分析得到置信度最高的4条药物组合为:天花粉-麦冬、玉竹-麦冬、北沙参-玉竹-麦冬、白术-黄芪-党参.收集到核心中药成分潜在作用靶点与NSCLC交集靶点126个;PPI分析得到3个核心靶点:AKT1、EGFR、SRC;KEGG分析表明关键通路为PI3K-Akt信号通路;筛选得到3个关键成分:木犀草素、槲皮素、山柰酚;分子对接结果表明关键成分和核心靶点均能稳定结合.细胞实验结果表明,木犀草素可有效抑制A549细胞的增殖、活力和迁移,诱导其发生凋亡,并使其形态发生变化.本文结果表明,中药联合化疗治疗NSCLC可以提高其临床疗效、降低化疗的毒副作用;黄芪、麦冬、党参、北沙参等核心中药多种成分可通过多靶点、多途径协同治疗NSCLC;关键中药的核心成分木犀草素可抑制A549细胞的增殖、活力和迁移,并可诱导其发生凋亡.展开更多
The direct transformation of dinitrogen(N_(2)) into nitrogen-containing organic compounds holds substantial importance.In this work,we report a titanium-promoted method for the conversion of N_(2) to N-methylimides.In...The direct transformation of dinitrogen(N_(2)) into nitrogen-containing organic compounds holds substantial importance.In this work,we report a titanium-promoted method for the conversion of N_(2) to N-methylimides.Initially,the N_(2)-bridging end-on dititanium side-on dipotassium complex[{(Tren^(TMS))Ti}_(2)(μ-η^(1):η^(1):η^(2):η^(2)-N_(2)K_(2))] underwent simultaneous disproportionation and N-methylation reactions in the presence of methyl trifluoromethanesulfonate(Me OTf),yielding [{(N^(Me,TMS)NN^(TMS)_(2))Ti}(μ-NMe)]_(2) with complete cleavage of the N≡N bond.The nucleophilicity of the N-methylated intermediate allowed it to react with electrophilic reagents such as trimethylchlorosilane(TMSCl) to form heptamethyldisilazane,or with acyl chlorides to generate N-methylimides.Moreover,nitrogen-15(^(15)N) labeled experiments provided a novel approach to synthesizing ^(15)N-labeled methylimides.展开更多
文摘中药不论在直接抑制肿瘤生长,还是辅助西医治疗肿瘤方面都发挥着不容忽视的作用.本文经检索中国知网、万方、维普、Pubmed、Web of Science等数据库,纳入中药汤剂联合化疗治疗非小细胞肺癌(NSCLC)的随机对照试验,通过Meta、用药规律、网络药理学和细胞实验等分析方法系统评价中药联合化疗治疗NSCLC的疗效、安全性及作用机制,最终纳入56篇文献进行统计分析,共4992例患者、57首处方、172味中药.结果显示,中药联合化疗治疗组的1年生存率、肝功能损伤、总有效率、胃肠道不良反应等方面均优于单纯化疗组.用药频次>20的有7味:药味以甘苦为主,药性以寒温为主,主要归为肺经和肝经.得到5个高频药物聚类,关联规则分析得到置信度最高的4条药物组合为:天花粉-麦冬、玉竹-麦冬、北沙参-玉竹-麦冬、白术-黄芪-党参.收集到核心中药成分潜在作用靶点与NSCLC交集靶点126个;PPI分析得到3个核心靶点:AKT1、EGFR、SRC;KEGG分析表明关键通路为PI3K-Akt信号通路;筛选得到3个关键成分:木犀草素、槲皮素、山柰酚;分子对接结果表明关键成分和核心靶点均能稳定结合.细胞实验结果表明,木犀草素可有效抑制A549细胞的增殖、活力和迁移,诱导其发生凋亡,并使其形态发生变化.本文结果表明,中药联合化疗治疗NSCLC可以提高其临床疗效、降低化疗的毒副作用;黄芪、麦冬、党参、北沙参等核心中药多种成分可通过多靶点、多途径协同治疗NSCLC;关键中药的核心成分木犀草素可抑制A549细胞的增殖、活力和迁移,并可诱导其发生凋亡.
基金Financial supports from the National Natural Science Foundation of China (Nos.22025109,22371283)the National Key R&D Program of China (No.2023YFA1507902)+1 种基金CAS Project for Young Scientists in Basic Research (No.YSBR-050)the State Key Laboratory of Fine Chemicals,Dalian University of Technology (No.KF2102) are gratefully acknowledged。
文摘The direct transformation of dinitrogen(N_(2)) into nitrogen-containing organic compounds holds substantial importance.In this work,we report a titanium-promoted method for the conversion of N_(2) to N-methylimides.Initially,the N_(2)-bridging end-on dititanium side-on dipotassium complex[{(Tren^(TMS))Ti}_(2)(μ-η^(1):η^(1):η^(2):η^(2)-N_(2)K_(2))] underwent simultaneous disproportionation and N-methylation reactions in the presence of methyl trifluoromethanesulfonate(Me OTf),yielding [{(N^(Me,TMS)NN^(TMS)_(2))Ti}(μ-NMe)]_(2) with complete cleavage of the N≡N bond.The nucleophilicity of the N-methylated intermediate allowed it to react with electrophilic reagents such as trimethylchlorosilane(TMSCl) to form heptamethyldisilazane,or with acyl chlorides to generate N-methylimides.Moreover,nitrogen-15(^(15)N) labeled experiments provided a novel approach to synthesizing ^(15)N-labeled methylimides.
