Since the chemical structure of total glucosides from Cynanchum Auriculatum Royle (CA) is similar to that of the steroline of Marsdenia Condurago Reich, a compound which exhibits antitumor activity, research into the ...Since the chemical structure of total glucosides from Cynanchum Auriculatum Royle (CA) is similar to that of the steroline of Marsdenia Condurago Reich, a compound which exhibits antitumor activity, research into the antitumor activity of CA was carried out. Its mechanism of action was studied in vivo with C 57BL/6 mice bearing Lewis lung carcinoma and in vitro, with two mouse tumor cell lines: S180 and EAC. CA inhibited to a certain extent the growth of subcutaneously inoculated Lewis lung carcinoma and its pulmonary metastasis, and augmented the antitumor effect of cyclophosphamide. It showed a killing effect on the EAC and S180 tumor cells of mice in vitro as well. It blocked the tumor cells of solid Lewis lung carcinoma from entering into the S stage from G1 and inhibited DNA synthesis of S180 and EAC tumor cells of mice in vitro. It also markedly increased the number of mononuclear Mφ of tumor bearing mice, stimulated the macrophagic activity of their intraperitoneal Mφ, raised the percentage of ANAE(+) lymphocytes in peripheral blood and enhanced the ABC reaction and antibody formation in tumor bearing mice.展开更多
Receptor tyrosine kinase-like orphan receptor 1(ROR1)is a member of the type I receptor tyrosine kinase family.ROR1 is pivotal in embryonic development and cancer,and serves as a biomarker and therapeutic target.It ha...Receptor tyrosine kinase-like orphan receptor 1(ROR1)is a member of the type I receptor tyrosine kinase family.ROR1 is pivotal in embryonic development and cancer,and serves as a biomarker and therapeutic target.It has soluble and membrane-bound subtypes,with the latter highly expressed in tumors.ROR1 is conserved throughout evolution and may play a role in the development of gastrointestinal cancer through multiple signaling pathways and molecular mechanisms.Studies suggest that overexpression of ROR1 may increase tumor invasiveness and metastasis.Additionally,ROR1 may regulate the cell cycle,stem cell characteristics,and interact with other signaling pathways to affect cancer progression.This review explores the structure,expression and role of ROR1 in the development of gastrointestinal cancers.It discusses current antitumor strategies,outlining challenges and prospects for treatment.展开更多
[Objectives]To study the inhibitory activity of two flavonoid glycosides isolated from Chlorophytum comosum Laxum R.Br on human nasopharyngeal carcinoma(NPC)cell line 5-8F in vitro and its mechanism.[Methods]The flavo...[Objectives]To study the inhibitory activity of two flavonoid glycosides isolated from Chlorophytum comosum Laxum R.Br on human nasopharyngeal carcinoma(NPC)cell line 5-8F in vitro and its mechanism.[Methods]The flavonoid glycosides were isolated and purified from the ethanol alcoholic extract of the roots of Liliaceae plant Chlorophytum comosum by silica gel column chromatography,macroporous resin column chromatography,Sephadex LH-20,and reverse column chromatography(ODS).The inhibitory activity of flavonoid glycosides on human nasopharyngeal carcinoma cells was analyzed by CCK-8 method,and the potential mechanism was preliminarily analyzed by molecular docking.[Results]Two flavonoid glycosides were identified as isovitexin 2″-0-rhamnoside and 7-2″-di-O-β-glucopyranosylisovitexin.Two flavonoid glycosides showed promising inhibitory effect on human nasopharyngeal carcinoma cell line 5-8F,with IC_(50) values of 24.8 and 27.5μmol/L,respectively.Molecular docking results showed that the potential targets of two flavonoid glycosides include CyclinD1,Bcl-2β-Catenin,ILK,TGF-β,in addition,two glycosides showed higher predicted binding affinity towards CyclinD1,which verifies the cytotoxicity of the two compounds on human nasopharyngeal carcinoma cell line 5-8F in vitro.[Conclusions]Two flavonoid glycosides are the active molecules in Chlorophytum comosum that can inhibit the proliferation of human nasopharyngeal carcinoma cells,and have the potential to be used in the research and development of anti nasopharyngeal carcinoma drugs.展开更多
Cancer is the leading cause of human death which seriously threatens human life.The antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer properties.Simultaneously,a varie...Cancer is the leading cause of human death which seriously threatens human life.The antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer properties.Simultaneously,a variety of target-selective artemisinin-related compounds with high efficiency have been discovered.Many researches indicated that artemisinin-related compounds have cytotoxic effects against a variety of cancer cells through pleiotropic effects,including inhibiting the proliferation of tumor cells,promoting apoptosis,inducing cell cycle arrest,disrupting cancer invasion and metastasis,preventing angiogenesis,mediating the tumor-related signaling pathways,and regulating tumor microenvironment.More importantly,artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer patients.Therefore,we concentrated on the new advances and development of artemisinin and its derivatives as potential antitumor agents in recent 5 years.It is our hope that this review could be helpful for further exploration of novel artemisinin-related antitumor agents.展开更多
Cancer is a serious threat to human health.Fungal polysaccharide is a polar biological macromolecule with low toxicity.It has a wide range of biological activities,including immune regulation,antitumor activity,and an...Cancer is a serious threat to human health.Fungal polysaccharide is a polar biological macromolecule with low toxicity.It has a wide range of biological activities,including immune regulation,antitumor activity,and antiviral activity.In recent years,the research results have shown that polysaccharides from fungus in traditional Chinese medicine have excellent antitumor effect in liver cancer,gastric cancer,breast cancer,colon cancer,esophageal cancer,and lung cancer.Therefore,the research and development of fungal polysaccharides are of great significance for the development of antitumor drugs in the future.展开更多
运用网络药理学和分子对接方法研究芦笋抗肿瘤作用的潜在靶点和分子机制。通过中国知网(CNKI)、PubMed和Web of Science查阅文献,获得芦笋的成分并运用TCMSP、Pubchem和Swiss Target Prediction获取芦笋成分对应靶点,通过OMIM、GeneCard...运用网络药理学和分子对接方法研究芦笋抗肿瘤作用的潜在靶点和分子机制。通过中国知网(CNKI)、PubMed和Web of Science查阅文献,获得芦笋的成分并运用TCMSP、Pubchem和Swiss Target Prediction获取芦笋成分对应靶点,通过OMIM、GeneCards和DisGeNET获得肿瘤疾病相关靶点,并使用Cytoscape软件进行芦笋-成分-靶点网络图构建,再利用芦笋的靶基因与肿瘤的靶基因交集构建PPI网络。通过DAVID数据库进行GO功能分析与KEGG通路富集分析,最后采用AutoDock软件进行关键成分与核心靶点的分子对接验证。筛选出芦笋活性成分20个,潜在作用靶点172个。GO功能分析表明,芦笋发挥抗肿瘤作用的机制可能是通过调节信号传导、酶活性激活与蛋白结合等发挥抗肿瘤作用;KEGG通路富集分析表明,芦笋通过调节HIF-1信号通路、RAP1信号通路、PI3K-Akt信号通路和VEGF通路等起到抗肿瘤作用;分子对接结果表明,配体和受体的结合能均小于-20.93 kJ/mol,表明配体和受体有良好的结合性。本研究揭示芦笋中的槲皮素、山柰素、雅姆皂苷、赖氨酸、香叶木素、原儿茶酸和木犀草素等可能是发挥抗肿瘤作用的关键成分,涉及的主要靶点有AKT1、SRC、PIK3R1和MAPK1等,并遵循了中药多成分-多靶点-多途径的抗肿瘤作用特点,同时也阐明了芦笋发挥抗肿瘤作用的潜在靶点和分子机制。展开更多
文摘Since the chemical structure of total glucosides from Cynanchum Auriculatum Royle (CA) is similar to that of the steroline of Marsdenia Condurago Reich, a compound which exhibits antitumor activity, research into the antitumor activity of CA was carried out. Its mechanism of action was studied in vivo with C 57BL/6 mice bearing Lewis lung carcinoma and in vitro, with two mouse tumor cell lines: S180 and EAC. CA inhibited to a certain extent the growth of subcutaneously inoculated Lewis lung carcinoma and its pulmonary metastasis, and augmented the antitumor effect of cyclophosphamide. It showed a killing effect on the EAC and S180 tumor cells of mice in vitro as well. It blocked the tumor cells of solid Lewis lung carcinoma from entering into the S stage from G1 and inhibited DNA synthesis of S180 and EAC tumor cells of mice in vitro. It also markedly increased the number of mononuclear Mφ of tumor bearing mice, stimulated the macrophagic activity of their intraperitoneal Mφ, raised the percentage of ANAE(+) lymphocytes in peripheral blood and enhanced the ABC reaction and antibody formation in tumor bearing mice.
基金Supported by the Hangzhou Medical Health Science and Technology Project,No.B20220173the Public Welfare Technology Project of Zhejiang Province,No.LGF21H160033Zhejiang Medical Technology Plan Project,No.2021KY047.
文摘Receptor tyrosine kinase-like orphan receptor 1(ROR1)is a member of the type I receptor tyrosine kinase family.ROR1 is pivotal in embryonic development and cancer,and serves as a biomarker and therapeutic target.It has soluble and membrane-bound subtypes,with the latter highly expressed in tumors.ROR1 is conserved throughout evolution and may play a role in the development of gastrointestinal cancer through multiple signaling pathways and molecular mechanisms.Studies suggest that overexpression of ROR1 may increase tumor invasiveness and metastasis.Additionally,ROR1 may regulate the cell cycle,stem cell characteristics,and interact with other signaling pathways to affect cancer progression.This review explores the structure,expression and role of ROR1 in the development of gastrointestinal cancers.It discusses current antitumor strategies,outlining challenges and prospects for treatment.
基金Supported by Youth Fund Project of Zhaoqing University(QZ202235)Zhaoqing Science and Technology Plan Project(2022040311011).
文摘[Objectives]To study the inhibitory activity of two flavonoid glycosides isolated from Chlorophytum comosum Laxum R.Br on human nasopharyngeal carcinoma(NPC)cell line 5-8F in vitro and its mechanism.[Methods]The flavonoid glycosides were isolated and purified from the ethanol alcoholic extract of the roots of Liliaceae plant Chlorophytum comosum by silica gel column chromatography,macroporous resin column chromatography,Sephadex LH-20,and reverse column chromatography(ODS).The inhibitory activity of flavonoid glycosides on human nasopharyngeal carcinoma cells was analyzed by CCK-8 method,and the potential mechanism was preliminarily analyzed by molecular docking.[Results]Two flavonoid glycosides were identified as isovitexin 2″-0-rhamnoside and 7-2″-di-O-β-glucopyranosylisovitexin.Two flavonoid glycosides showed promising inhibitory effect on human nasopharyngeal carcinoma cell line 5-8F,with IC_(50) values of 24.8 and 27.5μmol/L,respectively.Molecular docking results showed that the potential targets of two flavonoid glycosides include CyclinD1,Bcl-2β-Catenin,ILK,TGF-β,in addition,two glycosides showed higher predicted binding affinity towards CyclinD1,which verifies the cytotoxicity of the two compounds on human nasopharyngeal carcinoma cell line 5-8F in vitro.[Conclusions]Two flavonoid glycosides are the active molecules in Chlorophytum comosum that can inhibit the proliferation of human nasopharyngeal carcinoma cells,and have the potential to be used in the research and development of anti nasopharyngeal carcinoma drugs.
基金supported by CAS"Light of West China"Program([2014]91 to Z.Z.)the Basic Research Plan of Yunnan Provincial Science and Technology Department(grant number 2014FA042)+1 种基金CAS Strategic biological resources service network(ZSTH-021)the Strategic Priority Research Program of the Chinese Academy of Sciences,Grant No.XDA12030206.
文摘Cancer is the leading cause of human death which seriously threatens human life.The antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer properties.Simultaneously,a variety of target-selective artemisinin-related compounds with high efficiency have been discovered.Many researches indicated that artemisinin-related compounds have cytotoxic effects against a variety of cancer cells through pleiotropic effects,including inhibiting the proliferation of tumor cells,promoting apoptosis,inducing cell cycle arrest,disrupting cancer invasion and metastasis,preventing angiogenesis,mediating the tumor-related signaling pathways,and regulating tumor microenvironment.More importantly,artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer patients.Therefore,we concentrated on the new advances and development of artemisinin and its derivatives as potential antitumor agents in recent 5 years.It is our hope that this review could be helpful for further exploration of novel artemisinin-related antitumor agents.
文摘Cancer is a serious threat to human health.Fungal polysaccharide is a polar biological macromolecule with low toxicity.It has a wide range of biological activities,including immune regulation,antitumor activity,and antiviral activity.In recent years,the research results have shown that polysaccharides from fungus in traditional Chinese medicine have excellent antitumor effect in liver cancer,gastric cancer,breast cancer,colon cancer,esophageal cancer,and lung cancer.Therefore,the research and development of fungal polysaccharides are of great significance for the development of antitumor drugs in the future.
