Effects of a Whole Plant Extract of Scutellaria rubropunctata var. rubropunctata on Bone Metabolism with Estrogen Receptor Activation.
Effects of a Whole Plant Extract of Scutellaria rubropunctata var. rubropunctata on Bone Metabolism with Estrogen Receptor Activation.
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DOI：
10.3390/plants11162075
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发表时间：
2022-08-09
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影响因子：
--
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我们筛选了雌激素受体(ER)激活和促进骨代谢活性的自然资源，目的是寻找治疗骨质疏松症的潜在方法。用荧光素酶报告法对琉球植物的1531种提取物进行筛选，鉴定出一种80%的红斑黄芩乙醇提取物。红色斑点藻(SRE)具有剂量依赖的ER转录促进活性。重要的是，SRE对人乳腺癌细胞没有增殖作用。SRE对成骨前细胞MC3T3-E1的碱性磷酸酶(ALP)活性有促进作用，对RAW264.7细胞的TRAP活性无明显影响。实时定量聚合酶链式反应分析显示，SRE在成骨诱导后72 h上调Runx2、Osterix(OSX)、骨桥蛋白(OPN)、骨钙素(OCN)、Smad1、Smad4和Smad5的基因表达，在成骨诱导后21 d上调Runx2、OSx、Smad1、Smad4和Smad5的基因表达。成骨标志物的表达水平分析表明，SRE可能通过作用于分化的早期阶段而不是分化的晚期阶段来促进成骨分化。这些结果表明，SRE通过BMP/Smad途径激活Runx2和OSx，从而激活ER，诱导成骨细胞分化，提示SRE可能用于防治绝经后骨质疏松症。
We screened natural resources for estrogen receptor (ER)-activating and bone metabolism-promoting activities with the aim of finding potential treatments for osteoporosis. A screen of 1531 extracts from Ryukyu Arc plants using a luciferase reporter assay identified an 80% MeOH extract of Scutellaria rubropunctata var. rubropunctata (SRE) with dose-dependent ER transcription-promoting activity. Importantly, SRE had no proliferative effect on human breast cancer cells. SRE enhanced the ALP activity of pre-osteoblast MC3T3-E1 cells after 72 h in culture and slightly enhanced mineralization at 14 and 21 d. SRE did not significantly affect the TRAP activity of RAW264.7 cells. Gene expression analysis in MC3T3-E1 cells by quantitative real-time PCR revealed that SRE upregulated the mRNA levels of Runx2, Osterix (Osx), Osteopontin (Opn), Osteocalcin (Ocn), Smad1, Smad4, and Smad5 at 72 h, and those of Runx2, Osx, Smad1, Smad4, and Smad5 at 21 d of osteogenic induction. Analysis of the expression levels of osteogenic markers suggested that SRE may promote osteogenic differentiation by acting at the early stage of differentiation rather than at the late stage of differentiation. These results indicate that SRE activates ER and induces osteoblast differentiation by activating Runx2 and Osx through the BMP/Smad pathway, suggesting that SRE may be useful for the prevention and treatment of postmenopausal osteoporosis.
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DOI：
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发表时间：
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影响因子：
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