College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea.
Arch Pharm Res. 2010 Jan;33(1):75-80. doi: 10.1007/s12272-010-2228-4. Epub 2010 Feb 27.
A new norlupane-triterpene, 3alpha,11alpha-dihydroxy-20,23-dioxo-30-norlupane-28-oic acid (1), and four known compounds; 3alpha,11alpha-dihydroxy-23-oxo-lup-20(29)-en-28-oic acid (2), 3alpha,11alpha-dihydroxylup-20(29)-en-28-oic acid (3), ent-kaur-16-en-19-oic acid (4), and betulabuside B (5) were isolated from the methanolic extract of the leaves of Acanthopanax koreanum. Their chemical structures were elucidated by mass, 1D- and 2D-NMR spectroscopy. To investigate the bioactivities of these compounds, their effects on the differentiation of osteoblastic MC3T3-E1 cells were tested. Compounds 3 and 4 significantly increased osteoblastic cell growth and differentiation as assessed by the MTT assay and collagen content, respectively (p < 0.05). Compounds 1 and 5 significantly increased the growth of MC3T3-E1 cells and caused a significant elevation of osteoblastic cell differentiation as assessed by the alkaline phosphatase activity. These results suggest that the compounds isolated from A. koreanum leaves have a direct stimulatory effect on bone formation in vitro and may contribute to the prevention for osteoporosis.
一种新的诺鲁烷三萜,3α,11α-二羟基-20,23-二氧代-30-降诺鲁烷-28-酸(1),以及四种已知化合物;3α,11α-二羟基-23-氧代-升-20(29)-烯-28-酸(2),3α,11α-二羟基升-20(29)-烯-28-酸(3),ent-贝壳杉-16-烯-19-酸(4)和 betulabuside B(5)从朝鲜刺五加的甲醇提取物中分离得到。通过质谱、1D 和 2D-NMR 光谱学阐明了它们的化学结构。为了研究这些化合物的生物活性,测试了它们对成骨细胞 MC3T3-E1 细胞分化的影响。化合物 3 和 4 通过 MTT 测定和胶原蛋白含量分别显著增加成骨细胞的生长和分化(p<0.05)。化合物 1 和 5 显著增加 MC3T3-E1 细胞的生长,并通过碱性磷酸酶活性显著提高成骨细胞的分化。这些结果表明,从朝鲜刺五加叶中分离得到的化合物对体外骨形成具有直接的刺激作用,可能有助于预防骨质疏松症。