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Cytotoxic and Anti-inflammatory Terpenoids from the Whole Plant of Vaccinium emarginatum
Planta Medica ( IF 2.1 ) Pub Date : 2020-07-09 , DOI: 10.1055/a-1192-6225
Ping-Chen Tu, Yu-Chia Liang, Guan-Jhong Huang, Ming-Kuem Lin, Ming-Ching Kao, Te-Ling Lu, Ping-Jyun Sung, Yueh-Hsiung Kuo

Two new Δ12 ursene-type triterpenoid coumaroyl esters (1: and 2: ), one new Δ7,15 isopimarane-type diterpenoid glycoside (20: ), and two new irido-δ-lactone-type iridoids (21: and 22: ), together with 17 known pentacyclic triterpenoids (3: - 19: ), were isolated during the phytochemical investigation of a methanol extract of the whole plant of Vaccinium emarginatum. Their structures were determined by detailed analysis of standard spectroscopic data (MS, IR, 1D, and 2D NMR) and comparison with data of known analogs. The isolates were evaluated for their cytotoxicity against the PC-3 and Du145 prostate cancer cell lines (as assessed by an MTT cell proliferation assay), as well as for their anti-inflammatory activity via the inhibition of nitric oxide production in lipopolysaccharide-induced murine macrophage RAW 264.7 cells. Among the isolates, the triterpenoid coumaroyl and feruloyl esters (1, 3: , and 4: ) exhibited strong cytotoxicity against PC-3 prostate cancer cells, with 85.6 - 90.2% inhibition at 10.0 µg/mL. The pomolic acid coumaroyl and feruloyl esters (1: and 3: ) also showed moderate anti-inflammatory activity against nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells, with 59.2 (± 1.0) and 47.1% (± 0.2) inhibition at 12.5 µg/mL, respectively.

中文翻译:

越橘全株的细胞毒抗炎萜类化合物

两种新的 Δ12 熊烯型三萜香豆酰酯(1: 和 2: )、一种新的 Δ7,15 异海松烷型二萜糖苷(20: )和两种新的环烯醚-δ-内酯型环烯醚萜(21: 和 22: )与 17 种已知的五环三萜类化合物 (3: - 19: ) 一起,在对牛痘全植物甲醇提取物的植物化学研究中被分离出来。它们的结构是通过对标准光谱数据(MS、IR、1D 和 2D NMR)的详细分析并与已知类似物的数据进行比较来确定的。评估了分离株对 PC-3 和 Du145 前列腺癌细胞系的细胞毒性(通过 MTT 细胞增殖试验评估),以及它们通过抑制脂多糖诱导的小鼠中一氧化氮产生的抗炎活性巨噬细胞 RAW 264.7 细胞。在隔离区中,三萜类香豆酰酯和阿魏酸酯(1、3: 和 4: )对 PC-3 前列腺癌细胞表现出很强的细胞毒性,在 10.0 µg/mL 时抑制率为 85.6 - 90.2%。在脂多糖诱导的 RAW 264.7 细胞中,泊莫酸香豆酸酯和阿魏酸酯(1: 和 3: )也显示出对一氧化氮产生的中等抗炎活性,在 12.5 µg 时抑制率为 59.2 (± 1.0) 和 47.1% (± 0.2) /mL,分别。
更新日期:2020-07-09
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