Oh Jung Hwan, Karadeniz Fatih, Lee Jung Im, Seo Youngwan, Jang Mi-Soon, Kong Chang-Suk
Marine Biotechnology Center for Pharmaceuticals and Foods, College of Medical and Life Sciences, Silla University, Busan 46958, Republic of Korea.
Division of Marine Bioscience, Korea Maritime and Ocean University, Busan 49112, Republic of Korea.
Evid Based Complement Alternat Med. 2020 Oct 29;2020:8894910. doi: 10.1155/2020/8894910. eCollection 2020.
Luteolin is a common phytochemical from the flavonoid family with a flavone structure. Studies reported several bioactivities for luteolin and similar flavones. Attenuating the increased adipogenesis of bone marrow cells (hBM-MSCs) has been regarded as a therapeutic target against osteoporotic bone disorders. In the present study, the potential roles of luteolin and its sulfonic acid derivative luteolin-OSONa in regulating adipogenic differentiation of hBM-MSCs were investigated. Adipo-induced cells were treated with or without compounds, and their effect on adipogenesis was evaluated by adipogenic marker levels such as lipid accumulation and PPAR pathway activation. Luteolin hindered the adipogenic lipid accumulation in adipo-induced hBM-MSCs. Immunoblotting and reverse transcription-polymerase chain reaction analysis results indicated that luteolin downregulated PPAR and downstream factors of C/EBP and SREBP1c expression which resulted in inhibition of adipogenesis. Luteolin-OSONa showed similar effects; however, it was significantly less effective compared to luteolin. Investigating p38, JNK, and ERK MAPKs and AMPK activation indicated that luteolin suppressed the MAPK phosphorylation while stimulating AMPK phosphorylation. On the other hand, luteolin-OSONa was not able to notably affect the MAPK and AMPK activation. In conclusion, this study suggested that luteolin inhibited adipogenic differentiation of hBM-MSCs via upregulating AMPK activation. Replacing its 4'-hydroxyl group with sulfonic acid sodium salt diminished its antiadipogenic effect indicating its role in regulating AMPK activation. The general significance is that luteolin is a common phytochemical with various health-beneficial effects. The current study suggested that luteolin may serve as a lead compound for developing antiosteoporotic substances with antiadipogenic properties.
木犀草素是一种常见的黄酮类植物化学物质，具有黄酮结构。研究报道了木犀草素及类似黄酮的多种生物活性。减轻骨髓细胞（hBM-MSCs）脂肪生成增加被视为治疗骨质疏松性骨疾病的一个治疗靶点。在本研究中，研究了木犀草素及其磺酸衍生物木犀草素-OSONa在调节hBM-MSCs脂肪生成分化中的潜在作用。用或不用化合物处理脂肪诱导的细胞，并通过脂质积累和PPAR途径激活等脂肪生成标志物水平评估其对脂肪生成的影响。木犀草素阻碍了脂肪诱导的hBM-MSCs中的脂肪生成脂质积累。免疫印迹和逆转录-聚合酶链反应分析结果表明，木犀草素下调了PPAR以及C/EBP和SREBP1c表达的下游因子，从而导致脂肪生成受到抑制。木犀草素-OSONa显示出类似的效果；然而，与木犀草素相比，其效果明显较差。对p38、JNK和ERK MAPKs以及AMPK激活的研究表明，木犀草素抑制MAPK磷酸化，同时刺激AMPK磷酸化。另一方面，木犀草素-OSONa不能显著影响MAPK和AMPK激活。总之，本研究表明木犀草素通过上调AMPK激活来抑制hBM-MSCs的脂肪生成分化。用磺酸钠盐取代其4'-羟基会减弱其抗脂肪生成作用，表明其在调节AMPK激活中的作用。一般意义在于木犀草素是一种具有多种有益健康作用的常见植物化学物质。当前研究表明木犀草素可能作为开发具有抗脂肪生成特性的抗骨质疏松物质的先导化合物。
