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CD-2介导槲皮素高效定向生物合成异槲皮苷及其抗炎活性

Efficient directional biosynthesis of isoquercitrin from quercetin by CD-2 and its anti-inflammatory activity.

作者信息

Han Ju, Ma Jingru, He Ruiqi, Yang Fan, Meng Jingyi, Liu Jiaqi, Shi Fanxing, Duan Jinao, Chen Liangliang, Zhang Sen

机构信息

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Key Laboratory of Chinese Medicinal Resources Recycling Utilization of State Administration of Traditional Chinese Medicine, Nanjing University of Chinese Medicine, China Nanjing Jiangsu.

出版信息

Nat Prod Res. 2024 Nov 13:1-5. doi: 10.1080/14786419.2024.2425802.

Abstract

Isoquercetin, as the sole product, was directionally biosynthesized from quercetin in a non-aqueous system using CD-2 (1 g/L quercetin), and its structure was identified by LC-MS and NMR analysis. CCK8 assays showed no cytotoxicity and good cell proliferation. The anti-inflammatory experiments demonstrated strong inhibition of NO release, transcriptional downregulation of classical effective cellular factors tumour necrosis factor-α, interleukin-6, interleukin-1β, and transcriptional upregulation of interleukin-10 in LPS-induced RAW264.7 cells. Its stronger anti-inflammatory activity than quercetin provided a reference for modifying the structure of quercetin to obtain more compounds with better pharmacological activities for medical industry.

摘要

异槲皮素作为唯一产物,在非水体系中使用CD - 2(1 g/L槲皮素)由槲皮素定向生物合成,其结构通过液相色谱 - 质谱联用(LC - MS)和核磁共振(NMR)分析得以鉴定。细胞计数试剂盒 - 8(CCK8)检测显示无细胞毒性且细胞增殖良好。抗炎实验表明,在脂多糖(LPS)诱导的RAW264.7细胞中,其对一氧化氮(NO)释放有强烈抑制作用,对经典有效细胞因子肿瘤坏死因子 - α、白细胞介素 - 6、白细胞介素 - 1β的转录有下调作用,而对白细胞介素 - 10的转录有上调作用。其比槲皮素更强的抗炎活性为修饰槲皮素结构以获得更多具有更好药理活性的化合物用于医药行业提供了参考。

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