Hyperactivation of DNA repairing pathway is highly associated with the chemosensitivity and chemoresistance of cancer cells.In this manuscript,guided by cascaded one strain many compounds-global natural products socia...Hyperactivation of DNA repairing pathway is highly associated with the chemosensitivity and chemoresistance of cancer cells.In this manuscript,guided by cascaded one strain many compounds-global natural products social molecular networking(OSMAC-GNPS)strategy,a pair of epimeric environmental-induced metabolites were isolated from Aspergillus sp.EGF 15-0-3.Structurally,sterpiperazines A(1)and B(2)represent the first steroid-based indole alkaloids with unprecedented backbones.Biologically,compound 1 could be identified as a novel tyrosyl-DNA phosphodiesterase 1(Tdp1)inhibitor with a unique mechanism distinct from the reported modulators,and was able to significantly enhance the sensitivity of NCI-H460 cells to the clinic chemotherapeutic drug through inhibiting the DNA repairment and enhanced the DNA damage of cancer cells.展开更多
目的:探讨康复新液对口腔溃疡患者EGF、EGFR影响及疗效机制。方法:选取我院收治的口腔溃疡患者300例,根据治疗方法的不同,分为两组,每组各150例。试验组150例,予康复新液10 m L口含5 min后咽下,日3次,7 d为1个疗程,治疗1个疗程;对照组15...目的:探讨康复新液对口腔溃疡患者EGF、EGFR影响及疗效机制。方法:选取我院收治的口腔溃疡患者300例,根据治疗方法的不同,分为两组,每组各150例。试验组150例,予康复新液10 m L口含5 min后咽下,日3次,7 d为1个疗程,治疗1个疗程;对照组150例,予碘甘油涂布,日3次,7 d为1个疗程,治疗1个疗程。治疗后,观察并比较两组患者的溃疡持续时间、疼痛指数,EGF、EGFR情况,以及临床疗效。结果:与对照组相比较,试验组的溃疡持续时间、疼痛指数明显降低(P<0.05),EGF、EGFR情况改善(P<0.05),临床疗效显著提高(P<0.05),CRP水平降低(P<0.05)。结论:康复新液治疗口腔溃疡能够缩短溃疡持续时间,降低疼痛指数,改善EGF、EGFR,临床效果显著,值得临床推广使用。展开更多
基金supported by the National Natural Science Foundation of China(Nos.82273845,82304331,and 82360695)Guangxi Natural Science Foundation project(No.2023GXNSFBA026305).
文摘Hyperactivation of DNA repairing pathway is highly associated with the chemosensitivity and chemoresistance of cancer cells.In this manuscript,guided by cascaded one strain many compounds-global natural products social molecular networking(OSMAC-GNPS)strategy,a pair of epimeric environmental-induced metabolites were isolated from Aspergillus sp.EGF 15-0-3.Structurally,sterpiperazines A(1)and B(2)represent the first steroid-based indole alkaloids with unprecedented backbones.Biologically,compound 1 could be identified as a novel tyrosyl-DNA phosphodiesterase 1(Tdp1)inhibitor with a unique mechanism distinct from the reported modulators,and was able to significantly enhance the sensitivity of NCI-H460 cells to the clinic chemotherapeutic drug through inhibiting the DNA repairment and enhanced the DNA damage of cancer cells.