Two novel C-glycosylflavones, apigenin-6-C-α-L-arabinopyranosyl-(1-4)-α-L-rhamnopyranoside (hemsleyanoside, 1) and apigenin-8-C-α-L-arabinopyranosyl- (1-4)-α-L-rhamno-pyranoside (isohemsleyanoside, 2), together w...Two novel C-glycosylflavones, apigenin-6-C-α-L-arabinopyranosyl-(1-4)-α-L-rhamnopyranoside (hemsleyanoside, 1) and apigenin-8-C-α-L-arabinopyranosyl- (1-4)-α-L-rhamno-pyranoside (isohemsleyanoside, 2), together with a known compound (apigenin-6,8-di-C-β-D-glucopyranoside, 3), were isolated from the 95% EtOH extract of Tetrastigma hemsleyanum Diels et Gilg. Their structures were elucidated by chemical evidence and spectral analysis.展开更多
Tetrastigma hemsleyanum(T.hemsleyanum)has been regarded as an anticancer food in China.However,its corresponding mechanisms remains unclear.Thus,in this study,the antitumor activity of flavones-rich fraction of root o...Tetrastigma hemsleyanum(T.hemsleyanum)has been regarded as an anticancer food in China.However,its corresponding mechanisms remains unclear.Thus,in this study,the antitumor activity of flavones-rich fraction of root of T.hemsleyanum(FRTH)was investigated in vitro and in vivo.The results indicated that FRTH could inhibit the proliferation and migration of human hepatoellular carcinomas(HepG2)cells in vitro by the phosphatidylinositol 3-kinase/protein kinase B(PI3K/AKT)pathway.FRTH could increase the level of reactive oxygen species and change the mitochondrial membrane potential in HepG2 cells.In addition,FRTH treatment(300 mg/kg and 600 mg/kg,body weight)significantly suppressed tumor growth on HepG2 tumor-bearing nude mice.Besides,immunohistochemistry assays and western blotting revealed that FRTH enhanced the expression level of Bcl-2 associated X protein/B-cell lymphoma-2(Bax/Bcl-2),cytochrome C,caspase-3,caspase-9,and cleaved-caspase-3,and downregulated the expression level of platelet endothelial cell adhesion molecule-1(CD31),ki67,and vascular endothelial growth factor(VEGF)factor in HepG2 tumor-bearing mice.Our study suggests T.hemsleyanum as a kind of promising candidate medicine for liver cancer treatment.展开更多
目的通过网络药理学方法研究三叶青治疗肝细胞癌(HCC)的作用机制,并进行实验验证。方法检索中国知网、万方数据知识服务平台、维普中文期刊服务平台、PubMed、Web of Science,结合TCMSP数据库,筛选三叶青的活性成分及靶点。检索OncoDB....目的通过网络药理学方法研究三叶青治疗肝细胞癌(HCC)的作用机制,并进行实验验证。方法检索中国知网、万方数据知识服务平台、维普中文期刊服务平台、PubMed、Web of Science,结合TCMSP数据库,筛选三叶青的活性成分及靶点。检索OncoDB.HCC、GeneCards、OMIM、DrugBank数据库,收集HCC相关靶点。利用Cytoscape软件构建药物-活性成分-靶点-疾病网络,STRING数据库进行蛋白相互作用(PPI)分析,Metascape数据库进行GO及KEGG通路富集分析,AutoDock对关键靶点及主要活性成分进行分子对接。通过MTT比色法和细胞形态观察检测人肝癌HepG2细胞增殖,细胞划痕实验和Transwell小室实验观察细胞迁移和侵袭,AnnexinⅤ/PI双染法和流式细胞术检测细胞凋亡,RT-PCR和Western blot检测相关蛋白表达。结果网络药理学分析得到三叶青活性成分16个、作用靶点228个,其中与HCC相关靶点157个,JUN、AKT1、MAPK1、TP53等靶点可能是三叶青治疗HCC的核心靶点,与HCC密切相关的富集通路为IL-17信号通路、TNF信号通路、P53信号通路、PI3K-Akt信号通路等。分子对接结果显示,三叶青主要活性成分与核心靶点之间具有良好的结合效果。细胞实验结果显示,三叶青各剂量组可显著抑制HepG2细胞增殖、迁移和侵袭,促进凋亡,下调AP-1、MAPK1表达,上调TP53表达。结论三叶青能抑制人肝癌细胞增殖、迁移和侵袭,促进其凋亡,其治疗HCC的作用机制可能与下调AP-1、MAPK1蛋白表达及上调TP53蛋白表达有关。展开更多
[目的]基于CiteSpace,分析在2000—2022年发表的三叶青中英文文献、研究热点和发展趋势,为今后研究提供参考。[方法]检索中国知网(CNKI)及Web of Science,运用文献计量学及CiteSpace 6.1.R3软件对年发文量、发文期刊、作者、研究机构、...[目的]基于CiteSpace,分析在2000—2022年发表的三叶青中英文文献、研究热点和发展趋势,为今后研究提供参考。[方法]检索中国知网(CNKI)及Web of Science,运用文献计量学及CiteSpace 6.1.R3软件对年发文量、发文期刊、作者、研究机构、关键词共现、聚类和突变7个方面进行可视化网络分析,并结合信息提取的方法对三叶青研究现状及发展趋势进行分析。[结果]《浙江农业科学》和《International of Journal Biological Macromolecules》分别是发表中文、英文文献最多的期刊。彭昕是三叶青研究的中、英文文献主要核心作者,浙江医药高等专科学校和浙江大学分别是中、英文高发文量的研究机构。关键词分析研究表明目前对三叶青主要围绕基础性相关性研究,预测热点研究方向还应是抗炎、抗肿瘤等药理机制和药效物质的挖掘。[结论]三叶青相关研究仍处于发展阶段,需注重研究的深入并加强作者和研究机构的合作,同时还应继续围绕抗炎、抗肿瘤药理、药效和深加工产品开发。展开更多
文摘Two novel C-glycosylflavones, apigenin-6-C-α-L-arabinopyranosyl-(1-4)-α-L-rhamnopyranoside (hemsleyanoside, 1) and apigenin-8-C-α-L-arabinopyranosyl- (1-4)-α-L-rhamno-pyranoside (isohemsleyanoside, 2), together with a known compound (apigenin-6,8-di-C-β-D-glucopyranoside, 3), were isolated from the 95% EtOH extract of Tetrastigma hemsleyanum Diels et Gilg. Their structures were elucidated by chemical evidence and spectral analysis.
基金This research was based on the‘Functional food research and development of Tetrastigma hemsleyanum’funded by the Shanghai Zhengyue Enterprise Management Co.,Ltd.and the Science and Technology Department of Zhejiang Province(No.2018C02045),China.
文摘Tetrastigma hemsleyanum(T.hemsleyanum)has been regarded as an anticancer food in China.However,its corresponding mechanisms remains unclear.Thus,in this study,the antitumor activity of flavones-rich fraction of root of T.hemsleyanum(FRTH)was investigated in vitro and in vivo.The results indicated that FRTH could inhibit the proliferation and migration of human hepatoellular carcinomas(HepG2)cells in vitro by the phosphatidylinositol 3-kinase/protein kinase B(PI3K/AKT)pathway.FRTH could increase the level of reactive oxygen species and change the mitochondrial membrane potential in HepG2 cells.In addition,FRTH treatment(300 mg/kg and 600 mg/kg,body weight)significantly suppressed tumor growth on HepG2 tumor-bearing nude mice.Besides,immunohistochemistry assays and western blotting revealed that FRTH enhanced the expression level of Bcl-2 associated X protein/B-cell lymphoma-2(Bax/Bcl-2),cytochrome C,caspase-3,caspase-9,and cleaved-caspase-3,and downregulated the expression level of platelet endothelial cell adhesion molecule-1(CD31),ki67,and vascular endothelial growth factor(VEGF)factor in HepG2 tumor-bearing mice.Our study suggests T.hemsleyanum as a kind of promising candidate medicine for liver cancer treatment.
文摘目的通过网络药理学方法研究三叶青治疗肝细胞癌(HCC)的作用机制,并进行实验验证。方法检索中国知网、万方数据知识服务平台、维普中文期刊服务平台、PubMed、Web of Science,结合TCMSP数据库,筛选三叶青的活性成分及靶点。检索OncoDB.HCC、GeneCards、OMIM、DrugBank数据库,收集HCC相关靶点。利用Cytoscape软件构建药物-活性成分-靶点-疾病网络,STRING数据库进行蛋白相互作用(PPI)分析,Metascape数据库进行GO及KEGG通路富集分析,AutoDock对关键靶点及主要活性成分进行分子对接。通过MTT比色法和细胞形态观察检测人肝癌HepG2细胞增殖,细胞划痕实验和Transwell小室实验观察细胞迁移和侵袭,AnnexinⅤ/PI双染法和流式细胞术检测细胞凋亡,RT-PCR和Western blot检测相关蛋白表达。结果网络药理学分析得到三叶青活性成分16个、作用靶点228个,其中与HCC相关靶点157个,JUN、AKT1、MAPK1、TP53等靶点可能是三叶青治疗HCC的核心靶点,与HCC密切相关的富集通路为IL-17信号通路、TNF信号通路、P53信号通路、PI3K-Akt信号通路等。分子对接结果显示,三叶青主要活性成分与核心靶点之间具有良好的结合效果。细胞实验结果显示,三叶青各剂量组可显著抑制HepG2细胞增殖、迁移和侵袭,促进凋亡,下调AP-1、MAPK1表达,上调TP53表达。结论三叶青能抑制人肝癌细胞增殖、迁移和侵袭,促进其凋亡,其治疗HCC的作用机制可能与下调AP-1、MAPK1蛋白表达及上调TP53蛋白表达有关。
文摘[目的]基于CiteSpace,分析在2000—2022年发表的三叶青中英文文献、研究热点和发展趋势,为今后研究提供参考。[方法]检索中国知网(CNKI)及Web of Science,运用文献计量学及CiteSpace 6.1.R3软件对年发文量、发文期刊、作者、研究机构、关键词共现、聚类和突变7个方面进行可视化网络分析,并结合信息提取的方法对三叶青研究现状及发展趋势进行分析。[结果]《浙江农业科学》和《International of Journal Biological Macromolecules》分别是发表中文、英文文献最多的期刊。彭昕是三叶青研究的中、英文文献主要核心作者,浙江医药高等专科学校和浙江大学分别是中、英文高发文量的研究机构。关键词分析研究表明目前对三叶青主要围绕基础性相关性研究,预测热点研究方向还应是抗炎、抗肿瘤等药理机制和药效物质的挖掘。[结论]三叶青相关研究仍处于发展阶段,需注重研究的深入并加强作者和研究机构的合作,同时还应继续围绕抗炎、抗肿瘤药理、药效和深加工产品开发。
