Studies on the use of renewable materials for various applications,including polymers,have gained momentum due to global climate change and the push towards a circular economy.In this study,polymer resins were develop...Studies on the use of renewable materials for various applications,including polymers,have gained momentum due to global climate change and the push towards a circular economy.In this study,polymer resins were developed through Michael 1,4-addition.The precursors were synthesized from tall oil-based acetoacetates derived from epoxidized tall oil fatty acids or their methyl esters.Two different epoxidation methods were employed:enzymatic epoxidation of tall oil fatty acids and ion-exchange resin epoxidation of tall oil fatty acid methyl esters.Following oxirane opening and transesterification with trimethylolpropane,further esterification or transesterification was carried out to obtain the acetoacetates.These synthesized acetoacetates were then reacted with acrylates of various functionalities to obtain polymer resins with differing degrees of crosslinking.The developed polymer resins were characterized using differential scanning calorimetry,dynamic mechanical analysis,and thermogravimetric analysis.The results indicated that the glass transition temperature and storage modulus of the polymer resins were significantly influenced by both the functionality of the acrylates used and the epoxidation technique employed.Higher acrylate functionality resulted in increased stiffness,while enzymatic epoxidation enhanced the polymer’s mechanical properties,nearly doubling the storage modulus,achieving approximately 470 MPa,compared to the ion-exchange resin technique.Therefore,selecting the appropriate acrylate functionality and epoxidation method could tailor the mechanical properties of the polymer resins.展开更多
含有杂环的光学活性螺环羟吲哚衍生物因其多种多样的生物活性而备受关注。靛红衍生物的不对称Michael/环化串联反应是构建手性螺环羟吲哚化合物的重要方法。本文将11种有机催化剂用于靛红、4-羟基香豆素与丙二腈的不对称Michael加成/环...含有杂环的光学活性螺环羟吲哚衍生物因其多种多样的生物活性而备受关注。靛红衍生物的不对称Michael/环化串联反应是构建手性螺环羟吲哚化合物的重要方法。本文将11种有机催化剂用于靛红、4-羟基香豆素与丙二腈的不对称Michael加成/环化串联反应。筛选出最佳的催化剂体系为:10 mol%金鸡纳碱衍生物催化剂1f,二氯甲烷(1 m L)为溶剂,室温反应。将最佳条件用于不同取代靛红的反应,以80~88%的产率和最高达96%的对映选择性获得了螺[羟吲哚-3,4′-吡喃色烯]化合物。本研究拓宽了该反应的催化剂类型和底物范围。展开更多
Objective This study aimed to design and evaluate the efficacy of pyrrolidone derivatives as potential therapeutic agents against diffuse large B-cell lymphoma(DLBCL),a common and heterogeneous malignancy of the adult...Objective This study aimed to design and evaluate the efficacy of pyrrolidone derivatives as potential therapeutic agents against diffuse large B-cell lymphoma(DLBCL),a common and heterogeneous malignancy of the adult lymphohematopoietic system.Given the limitations of current therapies,there is a pressing need to develop new and effective drugs for DLBCL treatment.Methods A series of pyrrolidone derivatives were synthesized,and their antitumor activities were assessed,particularly against DLBCL cell lines.Structure-activity relationship(SAR)analysis was conducted to identify key structural components essential for activity.The most promising compound,referred to as compound 7,was selected for further mechanistic studies.The expression levels of relevant mRNA and protein were detected by RT-qPCR and Western blotting,and the expression of mitochondrial membrane potential and ROS was detected using flow cytometry for further assessment of cell cycle arrest and apoptosis.Results The compound 7 exhibited good antitumor activity among the synthesized derivatives,specifically in DLBCL cell lines.SAR analysis highlighted the critical role ofα,β-unsaturated ketones in the antitumor efficacy of these compounds.Mechanistically,compound 7 was found to induce significant DNA damage,trigger an inflammatory response,cause mitochondrial dysfunction,and disrupt cell cycle progression,ultimately leading to apoptosis of DLBCL cells.Conclusion The compound 7 has good antitumor activity and can induce multiple cellular mechanisms leading to cancer cell death.These findings warrant further investigation of the compound 7 as a potential therapeutic agent for DLBCL.展开更多
基金funded by the Latvian State Institute of Wood Chemistry Bioeconomic grant no.04-24“Development of Composites from Polymer Resin Synthesized from Tall Oil Fatty Acids and Reinforced with Various Fillers”(FiTeCo).
文摘Studies on the use of renewable materials for various applications,including polymers,have gained momentum due to global climate change and the push towards a circular economy.In this study,polymer resins were developed through Michael 1,4-addition.The precursors were synthesized from tall oil-based acetoacetates derived from epoxidized tall oil fatty acids or their methyl esters.Two different epoxidation methods were employed:enzymatic epoxidation of tall oil fatty acids and ion-exchange resin epoxidation of tall oil fatty acid methyl esters.Following oxirane opening and transesterification with trimethylolpropane,further esterification or transesterification was carried out to obtain the acetoacetates.These synthesized acetoacetates were then reacted with acrylates of various functionalities to obtain polymer resins with differing degrees of crosslinking.The developed polymer resins were characterized using differential scanning calorimetry,dynamic mechanical analysis,and thermogravimetric analysis.The results indicated that the glass transition temperature and storage modulus of the polymer resins were significantly influenced by both the functionality of the acrylates used and the epoxidation technique employed.Higher acrylate functionality resulted in increased stiffness,while enzymatic epoxidation enhanced the polymer’s mechanical properties,nearly doubling the storage modulus,achieving approximately 470 MPa,compared to the ion-exchange resin technique.Therefore,selecting the appropriate acrylate functionality and epoxidation method could tailor the mechanical properties of the polymer resins.
文摘含有杂环的光学活性螺环羟吲哚衍生物因其多种多样的生物活性而备受关注。靛红衍生物的不对称Michael/环化串联反应是构建手性螺环羟吲哚化合物的重要方法。本文将11种有机催化剂用于靛红、4-羟基香豆素与丙二腈的不对称Michael加成/环化串联反应。筛选出最佳的催化剂体系为:10 mol%金鸡纳碱衍生物催化剂1f,二氯甲烷(1 m L)为溶剂,室温反应。将最佳条件用于不同取代靛红的反应,以80~88%的产率和最高达96%的对映选择性获得了螺[羟吲哚-3,4′-吡喃色烯]化合物。本研究拓宽了该反应的催化剂类型和底物范围。
基金financially supported by the National Natural Science Foundation of China(No.81903461)the Natural Science Foundation of Hubei Province(No.ZRMS2023000340).
文摘Objective This study aimed to design and evaluate the efficacy of pyrrolidone derivatives as potential therapeutic agents against diffuse large B-cell lymphoma(DLBCL),a common and heterogeneous malignancy of the adult lymphohematopoietic system.Given the limitations of current therapies,there is a pressing need to develop new and effective drugs for DLBCL treatment.Methods A series of pyrrolidone derivatives were synthesized,and their antitumor activities were assessed,particularly against DLBCL cell lines.Structure-activity relationship(SAR)analysis was conducted to identify key structural components essential for activity.The most promising compound,referred to as compound 7,was selected for further mechanistic studies.The expression levels of relevant mRNA and protein were detected by RT-qPCR and Western blotting,and the expression of mitochondrial membrane potential and ROS was detected using flow cytometry for further assessment of cell cycle arrest and apoptosis.Results The compound 7 exhibited good antitumor activity among the synthesized derivatives,specifically in DLBCL cell lines.SAR analysis highlighted the critical role ofα,β-unsaturated ketones in the antitumor efficacy of these compounds.Mechanistically,compound 7 was found to induce significant DNA damage,trigger an inflammatory response,cause mitochondrial dysfunction,and disrupt cell cycle progression,ultimately leading to apoptosis of DLBCL cells.Conclusion The compound 7 has good antitumor activity and can induce multiple cellular mechanisms leading to cancer cell death.These findings warrant further investigation of the compound 7 as a potential therapeutic agent for DLBCL.
