Ibrahim Hairul-Islam Mohamed, Darrag Hossam M, Alhajhoj Mohammed Refdan, Khalil Hany Ezzat
Biological Sciences Department, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Pondicherry Centre for Biological Sciences and Educational Trust, Kottakuppam 605104, India.
Plants (Basel). 2020 Nov 20;9(11):1610. doi: 10.3390/plants9111610.
has used in folk medicine as palatable and nutraceutical herb. It also regulates hypocholesterolemia, hypoglycemia, and has showed anti-inflammatory activities as well as antioxidants efficacy. Osteoporosis is a one of bone metabolic disorders and is continuously increasing worldwide. In the present study, caffeic acid was isolated from and identified using 1 D- and 2 D-NMR spectroscopic data. Caffeic acid was investigated on osteoblast and osteoclast in vitro using mice bone marrow-derived mesenchymal cells. Caffeic acid played reciprocal proliferation between osteoblast and osteoclast cells and accelerated the bone mineralization. It was confirmed by cytotoxicity, alkaline phosphatase (ALP), alizarin red S (ARS), and Tartrate resistant acid phosphatase (TRAP) assay. Caffeic acid regulated the osteogenic marker and upregulated the osteopontin, osteocalcin, and bone morphogenic proteins (BMP). Quantitative real time PCR and Western blot were used to quantify the mRNA and protein markers. It also regulated the matrix metalloprotease-2 (MMP-2) and cathepsin-K proteolytic markers in osteoclast cells. In addition, caffeic acid inhibited bone resorption in osteoclast cells. On the other hand, it upregulate osteoblast differentiation through stimulation of extracellular calcium concentrations osteoblast differentiation, respectively. The results also were confirmed through in silico docking of caffeic acid against cathepsin-B and cathepsin-K markers. These findings revealed that caffeic acid has a potential role in bone-metabolic disorder through its multifaceted effects on osteoblast and osteoclast regulations and controls osteoporosis.
已在民间医学中用作美味且具有营养保健作用的草药。它还能调节低胆固醇血症、低血糖,并且具有抗炎活性以及抗氧化功效。骨质疏松症是一种骨代谢紊乱疾病,在全球范围内呈持续上升趋势。在本研究中,从[具体来源未提及]中分离出咖啡酸,并利用一维和二维核磁共振光谱数据对其进行鉴定。使用小鼠骨髓来源的间充质细胞在体外对咖啡酸进行了成骨细胞和破骨细胞方面的研究。咖啡酸在成骨细胞和破骨细胞之间发挥相互增殖作用,并加速骨矿化。这通过细胞毒性、碱性磷酸酶(ALP)、茜素红S(ARS)和抗酒石酸酸性磷酸酶(TRAP)检测得以证实。咖啡酸调节成骨标志物,上调骨桥蛋白、骨钙素和骨形态发生蛋白(BMP)。采用定量实时PCR和蛋白质印迹法对mRNA和蛋白质标志物进行定量分析。它还调节破骨细胞中的基质金属蛋白酶-2(MMP-2)和组织蛋白酶-K蛋白水解标志物。此外,咖啡酸抑制破骨细胞中的骨吸收。另一方面,它分别通过刺激细胞外钙浓度上调成骨细胞分化。这些结果还通过咖啡酸与组织蛋白酶-B和组织蛋白酶-K标志物的计算机模拟对接得到证实。这些发现表明,咖啡酸通过对成骨细胞和破骨细胞的多方面调节作用,在骨代谢紊乱中具有潜在作用,并可控制骨质疏松症。