AIM: To examine the effect of pseudolaric acid B on the growth of human gastric cancer cell line, AGS, and its possible mechanism of action.METHODS: Growth inhibition by pseudolaric acid B was analyzed using MTT assay...AIM: To examine the effect of pseudolaric acid B on the growth of human gastric cancer cell line, AGS, and its possible mechanism of action.METHODS: Growth inhibition by pseudolaric acid B was analyzed using MTT assay. Apoptotic cells were detected using Hoechst 33258 staining, and confirmed by DNA fragmentation analysis. Western blot was used to detect the expression of apoptosis-regulated gene Bcl-2, caspase 3, and cleavage of poly (ADP-ribose)polymerase-1 (PARP-1).RESULTS: Pseudolaric acid B inhibited the growth of AGS cells in a time- and dose-dependent manner by arresting the cells at G2/M phase, which was accompanied with a decrease in the levels of cdc2.AGS cells treated with pseudolaric acid B showed typical characteristics of apoptosis including chromatin condensation and DNA fragmentation. Moreover,treatment of AGS cells with pseudolaric acid B was also associated with decreased levels of the anti-apoptotic protein Bcl-2, activation of caspase-3, and proteolytic cleavage of PARP-1.CONCLUSION: Pseudolaric acid B can dramatically suppress the AGS cell growth by inducing apoptosis after G2/M phase arrest. These findings are consistent with the possibility that G2/M phase arrest is mediated by the down-regulation of cdc2 levels. The data also suggest that pseudolaric acid B can trigger apoptosis by decreasing Bcl-2 levels and activating caspase-3 protease.展开更多
Objective:Pseudolaric acid B(PB)is a newly identified diterpenoid isolated from Tujinpi(Cortex Pseudolaricis).In the present study,we aimed to explore the anti-inflammatory effects of PB on atopic dermatitis(AD),as we...Objective:Pseudolaric acid B(PB)is a newly identified diterpenoid isolated from Tujinpi(Cortex Pseudolaricis).In the present study,we aimed to explore the anti-inflammatory effects of PB on atopic dermatitis(AD),as well as the molecular mechanisms underlying its effects.Methods:BALB/c mice treated with 2,4-dinitrofluorobenzene were orally administered with PB(10 mg?kg-1?d-1).After evaluating the AD score,serum levels of IgE and the mRNA expression of NLRP3 inflammasome and IL-1βwere measured by ELISA and qRT-PCR respectively.Results:The results showed that PB treatment significantly ameliorated the development of AD-like clinical symptoms and effectively suppressed the infiltration of inflammatory cells.Furthermore,PB inhibited the expression of NLRP3 inflammasome and IL-1βin skin lesions,and downregulated serum IgE levels.Conclusion:The anti-inflammatory properties of PB were demonstrated using the 2,4-dinitrofluorobenzene-induced mouse model of AD-like skin lesions.Our study highlighted the potential use of PB as a novel therapeutic agent for the treatment of inflammation-associated skin diseases.展开更多
Studies on the synthesis of antifungal and anticancer natural product,pseudolaric acid B,have led to the enantioselective synthesis of di-epi-trans-fused[5-7]-bicyclic co re skeleton.The synthesis was achieved in 10 l...Studies on the synthesis of antifungal and anticancer natural product,pseudolaric acid B,have led to the enantioselective synthesis of di-epi-trans-fused[5-7]-bicyclic co re skeleton.The synthesis was achieved in 10 linear steps,which features the Sharpless asymmetric epoxidation,cyanide-opening reaction of epoxide,and intramolecular[5+2]cycloaddition reaction as the key transformations.The stereochemistry was determined by the X-ray crystallographic analysis.展开更多
【目的】探讨土槿皮乙酸对宫颈癌HeLa细胞凋亡和增殖的作用。【方法】通过Hoechst 33342荧光染色等观察细胞核固缩和染色体碎片等形态学变化,MTT法测定土槿皮乙酸对HeLa细胞的生长抑制作用,采用流式细胞仪和免疫印迹实验检测HeLa细胞的...【目的】探讨土槿皮乙酸对宫颈癌HeLa细胞凋亡和增殖的作用。【方法】通过Hoechst 33342荧光染色等观察细胞核固缩和染色体碎片等形态学变化,MTT法测定土槿皮乙酸对HeLa细胞的生长抑制作用,采用流式细胞仪和免疫印迹实验检测HeLa细胞的生长凋亡情况及其相关蛋白的表达变化。【结果】土槿皮乙酸对宫颈癌HeLa细胞具有明显的生长抑制作用,并能诱导细胞发生凋亡,随着药物浓度的增加和作用时间的延长,细胞的生长抑制率及细胞凋亡率均明显升高。土槿皮乙酸抑制细胞生长及诱导细胞发生凋亡的过程中,细胞磷脂酰肌醇-3激酶(PI3K)、蛋白激酶B(Akt)、糖原合酶激酶3(GSK3)、FKHRL(Forkhead like family)表达水平及活性显著降低,导致抑制凋亡抑制因子bcl-2受到表达抑制,同时Bax表达增加。【结论】土槿皮乙酸能够通过多条信号途径促进人子宫颈癌HeLa细胞发生凋亡,通过抑制PI3K/Akt的活性是其体外诱导人子宫颈癌HeLa细胞发生凋亡和抑制增值的重要作用机制。展开更多
基金Supported by the National Natural Science Foundation of China, No. 30371243
文摘AIM: To examine the effect of pseudolaric acid B on the growth of human gastric cancer cell line, AGS, and its possible mechanism of action.METHODS: Growth inhibition by pseudolaric acid B was analyzed using MTT assay. Apoptotic cells were detected using Hoechst 33258 staining, and confirmed by DNA fragmentation analysis. Western blot was used to detect the expression of apoptosis-regulated gene Bcl-2, caspase 3, and cleavage of poly (ADP-ribose)polymerase-1 (PARP-1).RESULTS: Pseudolaric acid B inhibited the growth of AGS cells in a time- and dose-dependent manner by arresting the cells at G2/M phase, which was accompanied with a decrease in the levels of cdc2.AGS cells treated with pseudolaric acid B showed typical characteristics of apoptosis including chromatin condensation and DNA fragmentation. Moreover,treatment of AGS cells with pseudolaric acid B was also associated with decreased levels of the anti-apoptotic protein Bcl-2, activation of caspase-3, and proteolytic cleavage of PARP-1.CONCLUSION: Pseudolaric acid B can dramatically suppress the AGS cell growth by inducing apoptosis after G2/M phase arrest. These findings are consistent with the possibility that G2/M phase arrest is mediated by the down-regulation of cdc2 levels. The data also suggest that pseudolaric acid B can trigger apoptosis by decreasing Bcl-2 levels and activating caspase-3 protease.
基金grants from the National Nature Science Foundation of China(81202843)Science Foundation of Logistics University of the Chinese People's Armed Police Force(WHJ2016013).
文摘Objective:Pseudolaric acid B(PB)is a newly identified diterpenoid isolated from Tujinpi(Cortex Pseudolaricis).In the present study,we aimed to explore the anti-inflammatory effects of PB on atopic dermatitis(AD),as well as the molecular mechanisms underlying its effects.Methods:BALB/c mice treated with 2,4-dinitrofluorobenzene were orally administered with PB(10 mg?kg-1?d-1).After evaluating the AD score,serum levels of IgE and the mRNA expression of NLRP3 inflammasome and IL-1βwere measured by ELISA and qRT-PCR respectively.Results:The results showed that PB treatment significantly ameliorated the development of AD-like clinical symptoms and effectively suppressed the infiltration of inflammatory cells.Furthermore,PB inhibited the expression of NLRP3 inflammasome and IL-1βin skin lesions,and downregulated serum IgE levels.Conclusion:The anti-inflammatory properties of PB were demonstrated using the 2,4-dinitrofluorobenzene-induced mouse model of AD-like skin lesions.Our study highlighted the potential use of PB as a novel therapeutic agent for the treatment of inflammation-associated skin diseases.
基金the financial support from the National Natural Science Foundation of China(Nos.21302078,21572089,21732001,21672017)the Program for Changjiang Scholars and the Innovative Research Team in Universities(PCSIRT:No.IRT_15R28)+3 种基金the State Key Basic Research Program of the PRC(No.2018YFC0310900)Shenzhen Science and Technology Innovation Committee(No.JCYJ20180504165454447)Shenzhen Basic Research Program(No.20180202)the National Ten Thousand Talent Program(the Leading Talent Tier)。
文摘Studies on the synthesis of antifungal and anticancer natural product,pseudolaric acid B,have led to the enantioselective synthesis of di-epi-trans-fused[5-7]-bicyclic co re skeleton.The synthesis was achieved in 10 linear steps,which features the Sharpless asymmetric epoxidation,cyanide-opening reaction of epoxide,and intramolecular[5+2]cycloaddition reaction as the key transformations.The stereochemistry was determined by the X-ray crystallographic analysis.
文摘【目的】探讨土槿皮乙酸对宫颈癌HeLa细胞凋亡和增殖的作用。【方法】通过Hoechst 33342荧光染色等观察细胞核固缩和染色体碎片等形态学变化,MTT法测定土槿皮乙酸对HeLa细胞的生长抑制作用,采用流式细胞仪和免疫印迹实验检测HeLa细胞的生长凋亡情况及其相关蛋白的表达变化。【结果】土槿皮乙酸对宫颈癌HeLa细胞具有明显的生长抑制作用,并能诱导细胞发生凋亡,随着药物浓度的增加和作用时间的延长,细胞的生长抑制率及细胞凋亡率均明显升高。土槿皮乙酸抑制细胞生长及诱导细胞发生凋亡的过程中,细胞磷脂酰肌醇-3激酶(PI3K)、蛋白激酶B(Akt)、糖原合酶激酶3(GSK3)、FKHRL(Forkhead like family)表达水平及活性显著降低,导致抑制凋亡抑制因子bcl-2受到表达抑制,同时Bax表达增加。【结论】土槿皮乙酸能够通过多条信号途径促进人子宫颈癌HeLa细胞发生凋亡,通过抑制PI3K/Akt的活性是其体外诱导人子宫颈癌HeLa细胞发生凋亡和抑制增值的重要作用机制。
