Department of Pharmaceutical Analysis, School of Pharmacy, Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University, 1160 Shenli Street, Yinchuan, 750004, China.
Laboratory for Functional Foods and Human Health, Center for Excellence in Post Harvest Technologies, North Caroline A & T State University, North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC, 28081, USA.
Biomed Pharmacother. 2020 Nov;131:110747. doi: 10.1016/j.biopha.2020.110747. Epub 2020 Sep 12.
2'-Acetylacteoside-(2'-AA), a bioactive constituent isolated from Cistanche deserticola, has been proven to possess a variety of important pharmacological effects, thus brought an increased amount of scientists' attention. As the extract of C. deserticola exhibited significant anti-osteoporotic bioactivity in our previous study, we proposed that 2'-AA maybe one of the responsibilities. As a result, 2'-AA (10, 20 and 40 mg/kg body weight/day) exhibited significant anti-osteoporotic effects on ovariectomized (OVX) mice after 12 weeks of oral administration, confirmed by the increased bone mineral density, enhanced bone strength and improved trabecular bone micro-architecture including bone mineral content, tissue mineral content, trabecular number, and trabecular separation of OVX mice. Moreover, the properties of bone resorption markers including cathepsin K, TRAP and deoxypyridinoline were significantly suppressed, whereas the activities of bone formation index like ALP and BGP as well as the weights of the body, uterus, and vagina were seemingly not influenced by 2'-AA intervention. Mechanistically, the above therapeutic effect of 2'-AA on bone resorption of OVX mice operated maybe mainly through RANKL/RANK/TRAF6-mediated NF-κB/NFATc1 pathway, which was confirmed by the down-regulated expressions of RANK, TRAF6, IκB kinase β, NF-κB and NFATc1. Summarily, 2'-AA exhibited significant anti-osteoporotic activity and may be regarded as a promising anti-osteoporotic candidate for future clinical trial.
2'-乙酰阿卡糖甙（2'-AA）是从肉苁蓉中分离得到的一种具有多种重要药理作用的生物活性成分，因此引起了越来越多的科学家的关注。在我们之前的研究中，肉苁蓉提取物表现出显著的抗骨质疏松生物活性，我们提出 2'-AA 可能是其中的一种责任。结果表明，2'-AA（10、20 和 40mg/kg 体重/天）在口服给药 12 周后对去卵巢（OVX）小鼠表现出显著的抗骨质疏松作用，这通过增加骨矿物质密度、增强骨强度和改善小梁骨微结构得到证实，包括骨矿物质含量、组织矿物质含量、小梁数量和小梁分离度。此外，骨吸收标志物的特性，包括组织蛋白酶 K、TRAP 和脱氧吡啶啉，被显著抑制，而骨形成指数如 ALP 和 BGP 的活性以及体重、子宫和阴道的重量似乎不受 2'-AA 干预的影响。在机制上，2'-AA 对 OVX 小鼠骨吸收的上述治疗作用可能主要通过 RANKL/RANK/TRAF6 介导的 NF-κB/NFATc1 通路发挥作用，这通过下调 RANK、TRAF6、IκB 激酶 β、NF-κB 和 NFATc1 的表达得到证实。总之，2'-AA 表现出显著的抗骨质疏松活性，可作为未来临床试验的有前途的抗骨质疏松候选药物。
