In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-h...In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.展开更多
目的:探讨在脂多糖(LPS)诱导的海马神经炎症中,5z-7-氧杂烯醇(OZ)对TAK1/NF-κB信号通路的调控及对新生神经元的保护作用。方法:通过腹腔注射LPS方法制备ICR小鼠神经炎症,治疗组同时腹腔注射OZ。免疫荧光检测海马齿状回Iba-1阳性小胶质...目的:探讨在脂多糖(LPS)诱导的海马神经炎症中,5z-7-氧杂烯醇(OZ)对TAK1/NF-κB信号通路的调控及对新生神经元的保护作用。方法:通过腹腔注射LPS方法制备ICR小鼠神经炎症,治疗组同时腹腔注射OZ。免疫荧光检测海马齿状回Iba-1阳性小胶质细胞的表达和双皮质素(DCX)阳性新生神经元的数量;Western blot检测海马TAK1和NF-κB磷酸化水平和NOX2、COX2、iNOS的表达变化。结果:LPS能够增加Iba-1、p-TAK1和p-NF-κB的表达水平,与对照组比较分别增高1.45±0.12、1.43±0.11和2.07±0.25倍,而OZ处理显著下调上述蛋白的表达水平(P<0.05)。免疫荧光检测发现,LPS组海马齿状回Iba-1阳性区域面积较对照组明显增加(5.38%±0.97%vs 1.89%±1.02%,P<0.05),而OZ处理显著下调Iba-1阳性区域面积(P<0.05)。进一步检测还发现,LPS组齿状回DCX阳性神经元数量较对照组明显减少(51.67±12.10 vs 87.33±11.93),而OZ处理能够增加DCX阳性细胞的数量(P<0.05)。此外,LPS组氧化应激相关蛋白NOX2、COX2和iNOS的表达水平较对照组分别增加1.42±0.09、1.44±0.17和2.74±0.54倍,而OZ处理能够显著下调上述蛋白的表达水平(P<0.05)。结论:OZ能够通过抑制TAK1/NF-κB信号通路,缓解LPS诱导的海马神经炎症,减少新生神经元的损伤。展开更多
The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized...The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.展开更多
基金Scientific Research Program Funded by Shaanxi Provincial Education Department(No.18JK0837)Natural Science Basic Research Plan Funded by Shaanxi Province of China(No.2018JM2045)+2 种基金Science and Technology Projects of Xianyang City(No.2017k02-19)Scientific Research Project Funded by Xianyang Normal University(No.XSYK18006)Qing-Lan Talents Project Funded by Xianyang Normal University(No.XSYQL201904)。
文摘In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.
文摘目的:探讨在脂多糖(LPS)诱导的海马神经炎症中,5z-7-氧杂烯醇(OZ)对TAK1/NF-κB信号通路的调控及对新生神经元的保护作用。方法:通过腹腔注射LPS方法制备ICR小鼠神经炎症,治疗组同时腹腔注射OZ。免疫荧光检测海马齿状回Iba-1阳性小胶质细胞的表达和双皮质素(DCX)阳性新生神经元的数量;Western blot检测海马TAK1和NF-κB磷酸化水平和NOX2、COX2、iNOS的表达变化。结果:LPS能够增加Iba-1、p-TAK1和p-NF-κB的表达水平,与对照组比较分别增高1.45±0.12、1.43±0.11和2.07±0.25倍,而OZ处理显著下调上述蛋白的表达水平(P<0.05)。免疫荧光检测发现,LPS组海马齿状回Iba-1阳性区域面积较对照组明显增加(5.38%±0.97%vs 1.89%±1.02%,P<0.05),而OZ处理显著下调Iba-1阳性区域面积(P<0.05)。进一步检测还发现,LPS组齿状回DCX阳性神经元数量较对照组明显减少(51.67±12.10 vs 87.33±11.93),而OZ处理能够增加DCX阳性细胞的数量(P<0.05)。此外,LPS组氧化应激相关蛋白NOX2、COX2和iNOS的表达水平较对照组分别增加1.42±0.09、1.44±0.17和2.74±0.54倍,而OZ处理能够显著下调上述蛋白的表达水平(P<0.05)。结论:OZ能够通过抑制TAK1/NF-κB信号通路,缓解LPS诱导的海马神经炎症,减少新生神经元的损伤。
文摘The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.
