Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China.
Shenzhen Key Laboratory of Food Biological Safety Control, The Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen 518057, China.
Nutrients. 2018 Feb 22;10(2):247. doi: 10.3390/nu10020247.
Oleanolic acid (OA) is a triterpenoid with reported bone anti-resorption activities. The present study aimed to characterize its bone protective effects in vivo and to study its effects on vitamin D metabolism, both in vivo and in vitro. OA significantly increased bone mineral density, improved micro-architectural properties, reduced urinary Ca excretion, increased 1,25(OH)₂D₃ and renal CYP27B1 mRNA expression in mature C57BL/6 ovariectomised (OVX) mice. OA also improved bone properties, Ca balance, and exerted modulatory effects on renal CYP27B1 and CYP24A1 expressions in aged normal female Sprague-Dawley rats. In addition, OA significantly increased renal CYP27B1 mRNA and promoter activity, and suppressed CYP24A1 mRNA and protein expressions in human proximal tubule HKC-8 cells. OA exerted bone protective effects in mature OVX mice and aged female rats. This action on bone might be, at least in part, associated with its effects on Ca and vitamin D metabolism. The present findings suggest that OA is a potential drug candidate for the management of postmenopausal osteoporosis.
齐墩果酸(OA)是一种具有报道的抗骨吸收活性的三萜类化合物。本研究旨在体内研究其对骨骼的保护作用,并研究其对维生素 D 代谢的影响,包括体内和体外。OA 可显著增加骨密度,改善微结构特性,减少尿钙排泄,增加 1,25(OH)₂D₃ 和肾脏 CYP27B1mRNA 表达,在成熟 C57BL/6 去卵巢(OVX)小鼠中。OA 还可改善骨特性、钙平衡,并对老年正常雌性 Sprague-Dawley 大鼠的肾脏 CYP27B1 和 CYP24A1 表达具有调节作用。此外,OA 可显著增加人近端肾小管 HKC-8 细胞中肾脏 CYP27B1mRNA 和启动子活性,并抑制 CYP24A1mRNA 和蛋白表达。OA 在成熟 OVX 小鼠和老年雌性大鼠中发挥骨骼保护作用。这种对骨骼的作用可能至少部分与其对钙和维生素 D 代谢的影响有关。本研究结果表明,OA 是治疗绝经后骨质疏松症的潜在药物候选物。