Two new α,β-unsaturated butyrolactone derivatives, 4-(4″-hydroxybenzyl)-3-(3′-hydroxy-phenethyl)furan-2(5H)-one (1) and 3-(3′-hydroxyphenethyl)furan-2(5H)-one (2), together with one known phenolic compound (3), w...Two new α,β-unsaturated butyrolactone derivatives, 4-(4″-hydroxybenzyl)-3-(3′-hydroxy-phenethyl)furan-2(5H)-one (1) and 3-(3′-hydroxyphenethyl)furan-2(5H)-one (2), together with one known phenolic compound (3), were isolated from the tubers of Pleione bulbocodioides (Franch.) Rolfe. Their structures were elucidated by analysis of spectroscopic data.展开更多
目的从1株南沙群岛柳珊瑚来源真菌Aspergillus terreus(NS02-09)中分离鉴定海洋天然产物,对所得化合物进行结核分枝杆菌酪氨酸磷酸激酶(mPTPB)抑制活性评价。方法运用多种色谱手段分离纯化化合物,利用NMR、CD等现代波谱分析方法,对化合...目的从1株南沙群岛柳珊瑚来源真菌Aspergillus terreus(NS02-09)中分离鉴定海洋天然产物,对所得化合物进行结核分枝杆菌酪氨酸磷酸激酶(mPTPB)抑制活性评价。方法运用多种色谱手段分离纯化化合物,利用NMR、CD等现代波谱分析方法,对化合物进行结构鉴定,通过衍生物制备获得2个乙酰化衍生物(2a和2b);并对化合物2及其衍生物2a和2b进行mPTPB酶抑制活性测试。结果鉴定了1个土曲霉酮(1)和1个丁烯酸内酯(2)的结构;2具有较强的mPTPB酶抑制活性,而其乙酰化产物(2a和2b)的mPTPB酶抑制活性显著降低。运用Sybyl X 1.3软件,对2与mPTPB酶的模拟对接计算发现,丁烯酸内酯环及环上的羟基是化合物2发挥酶抑制活性的重要作用基团。结论从柳珊瑚来源真菌A.terreus(NS02-09)中发现了具有mPTPB酶抑制活性的丁烯酸内酯类化合物,并对其作用机制进行了计算研究,该类化合物的相关研究对抗结核药物先导化合物发现具有借鉴作用。展开更多
文摘Two new α,β-unsaturated butyrolactone derivatives, 4-(4″-hydroxybenzyl)-3-(3′-hydroxy-phenethyl)furan-2(5H)-one (1) and 3-(3′-hydroxyphenethyl)furan-2(5H)-one (2), together with one known phenolic compound (3), were isolated from the tubers of Pleione bulbocodioides (Franch.) Rolfe. Their structures were elucidated by analysis of spectroscopic data.
文摘目的从1株南沙群岛柳珊瑚来源真菌Aspergillus terreus(NS02-09)中分离鉴定海洋天然产物,对所得化合物进行结核分枝杆菌酪氨酸磷酸激酶(mPTPB)抑制活性评价。方法运用多种色谱手段分离纯化化合物,利用NMR、CD等现代波谱分析方法,对化合物进行结构鉴定,通过衍生物制备获得2个乙酰化衍生物(2a和2b);并对化合物2及其衍生物2a和2b进行mPTPB酶抑制活性测试。结果鉴定了1个土曲霉酮(1)和1个丁烯酸内酯(2)的结构;2具有较强的mPTPB酶抑制活性,而其乙酰化产物(2a和2b)的mPTPB酶抑制活性显著降低。运用Sybyl X 1.3软件,对2与mPTPB酶的模拟对接计算发现,丁烯酸内酯环及环上的羟基是化合物2发挥酶抑制活性的重要作用基团。结论从柳珊瑚来源真菌A.terreus(NS02-09)中发现了具有mPTPB酶抑制活性的丁烯酸内酯类化合物,并对其作用机制进行了计算研究,该类化合物的相关研究对抗结核药物先导化合物发现具有借鉴作用。
