A series of novel coumarin-stilbenes hybrids called 3-arylcoumarins were synthesized via Perkin reaction and evaluated as potential antitumor agents.The results showed that some compounds exhibited in vitro activity a...A series of novel coumarin-stilbenes hybrids called 3-arylcoumarins were synthesized via Perkin reaction and evaluated as potential antitumor agents.The results showed that some compounds exhibited in vitro activity against KB,KV,MCF-7,MCF-7/ ADR cell lines to some extent.Compound 3a showed remarkable effect against KB tumor cells with an IC50 value of 5.18μmol/L.展开更多
Two bioactive natural 4-arylcoumarins,5,7,4＇-trimethoxy-4-phenylcoumarin（1a）,5,7-dimethoxy-4-phenylcoumarin（1b） and five closely related derivatives 1c-g were synthesized.In vitro evaluation with a catechol subun...Two bioactive natural 4-arylcoumarins,5,7,4＇-trimethoxy-4-phenylcoumarin（1a）,5,7-dimethoxy-4-phenylcoumarin（1b） and five closely related derivatives 1c-g were synthesized.In vitro evaluation with a catechol subunit for antioxidant and antimicrobial activity,these compounds using standard methods showed that compounds 1d,1f displayed promise radical scavenging activity and 1f was found to be the most active one against Bacillus dysenteriae.展开更多
A new series of 7-substituted 3-arylcoumarins was designed, synthesized and evaluated as novel antitumor agents in vitro. It was found that several compounds of them exhibit activity in vitro against SK-HEP-l（hepatoc...A new series of 7-substituted 3-arylcoumarins was designed, synthesized and evaluated as novel antitumor agents in vitro. It was found that several compounds of them exhibit activity in vitro against SK-HEP-l（hepatocellular carcinoma）, HepG2（hepatocellular carcinoma） and SGC7901（gastric carcinoma） cell lines to some extent. Moreover, compounds 5a, 5b, 6a and 6b have better activity against HeLa（cervical carcinoma） cell and their half maximal inhibitory concentration（IC50） values are less than 10μmol/L.展开更多
为揭示3-芳基香豆素衍生物3-(4′-羟基苯基)-6-羟基香豆素(SJ-6)对抗血管钙化的作用机制,采用晚期糖基化终产物(AGEs)对人体主动脉血管平滑肌细胞(HCASMCs)进行钙化诱导并通过茜素红染色及定量进行钙化鉴定。分别检测了化合物SJ-6对碱...为揭示3-芳基香豆素衍生物3-(4′-羟基苯基)-6-羟基香豆素(SJ-6)对抗血管钙化的作用机制,采用晚期糖基化终产物(AGEs)对人体主动脉血管平滑肌细胞(HCASMCs)进行钙化诱导并通过茜素红染色及定量进行钙化鉴定。分别检测了化合物SJ-6对碱性磷酸酶(ALP)活力、细胞增殖率、钙含量、总活性氧(ROS)、超氧化物歧化酶(SOD)、AGEs、肿瘤坏死因子-α(TNF-α)、白细胞介素6(1L-6)、白细胞介素β(1L-β)、成骨相关转录因子2 m RNA(Runx2 m RNA)、晚期糖基化终产物受体(RAGE)、核因子κB(NF-κB)、NADPH氧化酶-1(NOX-1)、蛋白激酶C(PKC)、蛋白激酶B(AKT)、p38丝裂原活化蛋白激酶(p38 MAPK)、α-平滑肌肌动蛋白(SMA-α)蛋白表达的影响。根据研究结果发现化合物SJ-6可明显降低钙化细胞模型中AGEs含量、ALP活性、细胞内钙离子含量、ROS含量、Runx2 m RNA以及炎症因子TNF-α、1L-6和1L-β的含量(P<0.05),并升高SOD的含量(P<0.01),这些作用与阳性对照药氨基胍盐酸盐(AGH)相似。进一步对化合物SJ-6进行深入的药理机制研究,发现化合物SJ-6能够明显抑制钙化细胞模型中关键信号蛋白RAGE、NF-κB、NOX-1、PKC、Akt、p-p38等蛋白的表达(P<0.01),并增加平滑肌动蛋白SMA-α的表达(P<0.01),通过抑制氧化应激和AGEs/RAGE、Akt/PKC及NF-κB信号通路的表达抑制血管钙化,提示化合物SJ-6有望成为治疗血管钙化的新型药物。展开更多
基金National Key Technology R&D Program,Science and Technology Program of Guangdong Province and Strategic Cooperation Program between Guangdong Province and Chinese Academy of Sciences,PR China(Nos. 2007BAD82B02,2006B35604002,and 2009B091300125) for financial support
文摘A series of novel coumarin-stilbenes hybrids called 3-arylcoumarins were synthesized via Perkin reaction and evaluated as potential antitumor agents.The results showed that some compounds exhibited in vitro activity against KB,KV,MCF-7,MCF-7/ ADR cell lines to some extent.Compound 3a showed remarkable effect against KB tumor cells with an IC50 value of 5.18μmol/L.
基金We thank the Science and Technology Program of Guangdong Province,Strategic Cooperation Program between Guangdong Province and Chinese Academy of Sciences and National Key Technology R&D Program,China(Nos. 2003B31603,2006B35604002,2009B091300125 and 2007BAD82B02) for financial support
文摘Two bioactive natural 4-arylcoumarins,5,7,4＇-trimethoxy-4-phenylcoumarin（1a）,5,7-dimethoxy-4-phenylcoumarin（1b） and five closely related derivatives 1c-g were synthesized.In vitro evaluation with a catechol subunit for antioxidant and antimicrobial activity,these compounds using standard methods showed that compounds 1d,1f displayed promise radical scavenging activity and 1f was found to be the most active one against Bacillus dysenteriae.
基金the National Natural Science Foundation of China
文摘A new series of 7-substituted 3-arylcoumarins was designed, synthesized and evaluated as novel antitumor agents in vitro. It was found that several compounds of them exhibit activity in vitro against SK-HEP-l（hepatocellular carcinoma）, HepG2（hepatocellular carcinoma） and SGC7901（gastric carcinoma） cell lines to some extent. Moreover, compounds 5a, 5b, 6a and 6b have better activity against HeLa（cervical carcinoma） cell and their half maximal inhibitory concentration（IC50） values are less than 10μmol/L.
文摘为揭示3-芳基香豆素衍生物3-(4′-羟基苯基)-6-羟基香豆素(SJ-6)对抗血管钙化的作用机制,采用晚期糖基化终产物(AGEs)对人体主动脉血管平滑肌细胞(HCASMCs)进行钙化诱导并通过茜素红染色及定量进行钙化鉴定。分别检测了化合物SJ-6对碱性磷酸酶(ALP)活力、细胞增殖率、钙含量、总活性氧(ROS)、超氧化物歧化酶(SOD)、AGEs、肿瘤坏死因子-α(TNF-α)、白细胞介素6(1L-6)、白细胞介素β(1L-β)、成骨相关转录因子2 m RNA(Runx2 m RNA)、晚期糖基化终产物受体(RAGE)、核因子κB(NF-κB)、NADPH氧化酶-1(NOX-1)、蛋白激酶C(PKC)、蛋白激酶B(AKT)、p38丝裂原活化蛋白激酶(p38 MAPK)、α-平滑肌肌动蛋白(SMA-α)蛋白表达的影响。根据研究结果发现化合物SJ-6可明显降低钙化细胞模型中AGEs含量、ALP活性、细胞内钙离子含量、ROS含量、Runx2 m RNA以及炎症因子TNF-α、1L-6和1L-β的含量(P<0.05),并升高SOD的含量(P<0.01),这些作用与阳性对照药氨基胍盐酸盐(AGH)相似。进一步对化合物SJ-6进行深入的药理机制研究,发现化合物SJ-6能够明显抑制钙化细胞模型中关键信号蛋白RAGE、NF-κB、NOX-1、PKC、Akt、p-p38等蛋白的表达(P<0.01),并增加平滑肌动蛋白SMA-α的表达(P<0.01),通过抑制氧化应激和AGEs/RAGE、Akt/PKC及NF-κB信号通路的表达抑制血管钙化,提示化合物SJ-6有望成为治疗血管钙化的新型药物。
