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药用昆虫凹纹胡蜂化学成分及抗炎活性研究
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作者 刘超贺 庞秀琴 +7 位作者 李成功 许静蕾 钱晓莉 常雅萍 杨志斌 杨银河 王家鹏 肖怀 《中草药》 CAS CSCD 北大核心 2023年第22期7351-7357,共7页
目的研究药用昆虫凹纹胡蜂Vespa velutina auraria的化学成分及其抗炎活性。方法采用硅胶柱色谱、Sephadex LH-20凝胶和半制备高效液相等色谱技术进行分离纯化,通过核磁共振技术对化合物的结构进行表征和解析。以脂多糖(lipopolysacchar... 目的研究药用昆虫凹纹胡蜂Vespa velutina auraria的化学成分及其抗炎活性。方法采用硅胶柱色谱、Sephadex LH-20凝胶和半制备高效液相等色谱技术进行分离纯化,通过核磁共振技术对化合物的结构进行表征和解析。以脂多糖(lipopolysaccharide,LPS)联合γ干扰素(interferon-γ,IFN-γ)诱导小鼠巨噬细胞RAW264.7作为炎症模型,探讨提取物及单体对炎症因子mRNA表达的影响。结果从凹纹胡蜂醋酸乙酯部位分离鉴定了16个化合物,分别为邻苯二酚(1)、对羟基苯甲醛(2)、对羟基苯丙酸甲酯(3)、4-羟基苯醋酸乙酯(4)、3,4-二羟基苯乙醇(5)、3,4-二羟基苯酰乙醇(6)、3,4-二羟基苯甲酸(7)、N-乙酰基-2-乙氧基-2-(3,4-二羟基苯基)乙胺(8)、2-(2-羟基丙酰氧基)丙酸甲酯(9)、对甲氧基苯甲醇(10)、3,4-二羟基苯甲酸甲酯(11)、α-乙基葡萄糖苷(12)、2-羟基-3-苯基丙酸甲酯(13)、N-乙酰基-2-(3,4-二羟基苯基)乙胺(14)、对甲基苯乙醇(15)和胸腺嘧啶(16)。凹纹胡蜂醇提物及提取物醋酸乙酯部位、正丁醇部位和水部位在300μg/mL时均能有效减少由LPS联合IFN-γ诱导RAW264.7细胞炎症因子一氧化氮合酶(inducible nitric oxide synthase,iNOS)基因相对表达量;化合物2、3、5、6、9~11对LPS联合IFN-γ诱导RAW264.7细胞肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)m RNA表达有抑制作用(P<0.01)。结论凹纹胡蜂醇提物及不同极性部位能降低炎症细胞中iNOS的表达,具有一定的抗炎作用。化合物1~16均为首次从凹纹胡蜂分离鉴定,其中2、3、5、6、9~11可能为潜在的活性单体。 展开更多
关键词 凹纹胡蜂 抗炎活性 对羟基苯甲醛 3 4-二羟基苯乙醇 2-(2-羟基丙酰氧基)丙酸甲酯 对甲氧基苯甲醇
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Proliferation Inhibitory Activity of Quinones from Blaps rynchopetera Defense Secretion on Colorectal Tumor Cells
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作者 QIAN Xiao-li Meng Di +6 位作者 liu Heng liu chao-he ZHOU Ping YANG Yin-he WANG Jia-peng XIAO Huai DING Zhong-tao 《Chinese Journal of Integrative Medicine》 SCIE CAS CSCD 2023年第8期683-690,共8页
Objective: To explore the proliferation inhibitory effect of quinones from Blaps rynchopetera defense secretion on colorectal tumor cell lines. Methods: Human colorectal cancer cell HT-29, human colorectal adenocarcin... Objective: To explore the proliferation inhibitory effect of quinones from Blaps rynchopetera defense secretion on colorectal tumor cell lines. Methods: Human colorectal cancer cell HT-29, human colorectal adenocarcinoma cell Caco-2 and normal human colon epithelial cell CCD841 were chosen for the evaluation of inhibitory activity of the main quinones of B. rynchopetera defense secretion, including methyl p-benzoquinone(MBQ), ethyl p-benzoquinone(EBQ), and methyl hydroquinone(MHQ), through methyl thiazolyl tetrazolium assay. The tumor-related factors, cell cycles, related gene expressions and protein levels were detected by enzyme-linked immunosorbent assy, flow cytometry, RT-polymerase chain reaction and Western blot, respectively. Results: MBQ, EBQ, and MHQ could significantly inhibit the proliferation of Caco-2, with half maximal inhibitory concentration(IC50) values of 7.04±0.88, 10.92±0.32, 9.35±0.83, HT-29, with IC50values of 14.90±2.71, 20.50±6.37, 13.90±1.30, and CCD841, with IC50values of 11.40±0.68, 7.02±0.44 and 7.83±0.05 μg/mL, respectively. Tested quinones can reduce the expression of tumor-related factors tumor necrosis factor α, interleukin(IL)-10, and IL-6 in HT-29 cells, selectively promote apoptosis, and regulate the cell cycle which can reduce the proportion of cells in the G1phase and increase the proportion of the S phase.Meanwhile, tested quinones could up-regulate mRNA and protein expression of GSK-3β and APC, while down-regulate that of β-catenin, Frizzled1, c-Myc, and CyclinD1 in the Wnt/β-catenin pathway of HT-29 cells.Conclusion: Quinones from B. rynchopetera defense secretion could inhibit the proliferation of colorectal tumor cells and reduce the expression of related factors, which would be functioned by regulating cell cycle, selectively promoting apoptosis, and affecting Wnt/β-catenin pathway-related mRNA and protein expressions. 展开更多
关键词 Blaps rynchopetera Chinese medicine QUINONES anti-colorectal tumor Wnt/β-catenin pathway
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