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Distinct Fractions of an Artemisia scoparia Extract Contain Compounds With Novel Adipogenic Bioactivity

机译:不同部位的蒿提取物含有具有新型成脂生物活性的化合物

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摘要

Adipocytes are important players in metabolic health and disease, and disruption of adipocyte development or function contributes to metabolic dysregulation. Hence, adipocytes are significant targets for therapeutic intervention in obesity and metabolic syndrome. Plants have long been sources for bioactive compounds and drugs. In previous studies, we screened botanical extracts for effects on adipogenesis in vitro and discovered that an ethanolic extract of Artemisia scoparia (SCO) could promote adipocyte differentiation. To follow up on these studies, we have used various separation methods to identify the compound(s) responsible for SCO's adipogenic properties. Fractions and subfractions of SCO were tested for effects on lipid accumulation and adipogenic gene expression in differentiating 3T3-L1 adipocytes. Fractions were also analyzed by Ultra Performance Liquid Chromatography- Mass Spectrometry (UPLC-MS), and resulting peaks were putatively identified through high resolution, high mass accuracy mass spectrometry, literature data, and available natural products databases. The inactive fractions contained mostly quercetin derivatives and chlorogenates, including chlorogenic acid and 3,5-dicaffeoylquinic acid, which had no effects on adipogenesis when tested individually, thus ruling them out as pro-adipogenic bioactives in SCO. Based on these studies we have putatively identified the principal constituents in SCO fractions and subfractions that promoted adipocyte development and fat cell gene expression as prenylated coumaric acids, coumarin monoterpene ethers, 6-demethoxycapillarisin and two polymethoxyflavones.
机译:脂肪细胞是代谢健康和疾病的重要参与者,并且脂肪细胞发育或功能的破坏会导致代谢失调。因此,脂肪细胞是肥胖症和代谢综合征的治疗干预的重要靶标。长期以来,植物一直是生物活性化合物和药物的来源。在以前的研究中,我们筛选了植物提取物对体外脂肪生成的影响,并发现了蒿属的乙醇提取物(SCO)可以促进脂肪细胞的分化。为了跟踪这些研究,我们使用了多种分离方法来鉴定负责SCO成脂特性的化合物。测试了SCO的馏分和亚馏分对分化3T3-L1脂肪细胞中脂质积累和成脂基因表达的影响。还通过超高效液相色谱-质谱(UPLC-MS)分析了级分,并通过高分辨率,高质量准确度质谱法,文献数据和可用的天然产物数据库推定了所得峰。非活性级分主要包含槲皮素衍生物和绿原酸盐,包括绿原酸和3,5-二咖啡酰奎尼酸,单独测试时对脂肪生成没有影响,因此将它们排除为上合组织中的促脂肪生物活性物质。基于这些研究,我们推定了促进脂肪细胞发育和脂肪细胞基因表达的SCO馏分和亚馏分中的主要成分为异戊烯酸香豆酸,香豆素单萜醚,6-去甲氧基毛细管素和两种聚甲氧基黄酮。

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