目的 研究亚麻叶白千层Melaleuca linariifolia枝、叶中的化学成分。方法 采用硅胶、Sephadex LH-20、ODS、以及Pre-HPLC等现代分离方法进行系统地分离纯化，并根据化合物的理化性质和波谱数据进行结构鉴定。采用CCK8法初步评价化合物1~6对6种肿瘤细胞（人肺腺癌NCI-H441细胞、人大细胞肺癌NCI-H460细胞、人肺癌A549细胞、人卵巢腺癌SKOV3细胞、人宫颈癌HeLa细胞和人肾透明细胞癌caki-1细胞）的体外细胞增殖抑制活性。结果 从亚麻叶白千层醋酸乙酯部位分离得到15个化合物，分别鉴定为3-O-乙酰熊果酸（1）、3β-acetoxy-11-ursen-13α，30-olide （2）、betulinal （3）、diospyrolide （4）、3β-O-（E）-cumaroyl-alphitolinsaeure （5）、3'，4'-二羟基肉桂酸白桦脂酸酯（6）、熊果醇（7）、白桦脂醇（8）、豆甾-4-烯-3-酮（9）、5，7，4'-三羟基黄酮3-O-α-L-毗喃鼠李糖苷（10）、山柰酚-3-O-（6''-没食子酰基）-β-D-葡萄糖苷（11）、α-生育酚（12）、methoxytocopherol （13）、α-tocopherolquinone （14）、植醇（15）。CCK8测试结果显示，化合物1、3、5、6对人类肿瘤细胞显示出中等强度的增殖抑制作用。结论 所有化合物均为首次从该植物中分离得到，其中化合物2、4、5、9~11、13、14为首次从该属植物中分离得到。化合物1、3、5、6对人类肿瘤细胞表现出一定的细胞毒活性，半数抑制浓度（IC₅₀）值在3.85~25.63μmol/L。

Objective To investigate the chemical constituents from the twigs and leaves of Melaleuca linariifolia. Methods The compounds were isolated and purified by silica gel, Sephadex LH-20, ODS column chromatography, and preparative HPLC. Their structures were elucidated on basis of spectral data and physicochemical properties. Furthermore, the inhibitory effects of compounds 1-6 on proliferation of six human cancer cell lines (NCI-H441, NCI-H460, A549, SKOV3, HeLa, and caki-1) in vitro were tested by CCK8 method. Results Fifteen compounds were isolated from the ethyl acetate extract of M. linariifolia and identified as 3-O-acetyl ursolic acid (1), 3β-acetoxy-11-ursen-13α,30-olide (2), betulinal (3), diospyrolide (4), 3β-O-(E)-cumaroyl- alphitolinsaeure (5), pyracrenic acid (6), uvaol (7), betulin (8), stigmast-4-ene-3-one (9), 5,7,4'-trihydroxyl-flavone 3-O-α-L-rhamnopyranoside (10), kaempferol 3-O-(6''-galloyl)-β-D-glucoside (11), α-tocopherol (12), methoxytocopherol (13), α-tocopherolquinone (14), and phytol (15), respectively. CCK8 test results showed that compounds 1, 3, 5, and 6 exhibited moderate antiproliferative activities on six human cancer cells. Conclusion All the compounds were isolated from M. linariifolia for the first time, in which compounds 2, 4-5, 9-11, and 13-14 are isolated from the plants in genus Melaleuca for the first time. Compounds 1, 3, 5, and 6 showed certain cytotoxic activity against human tumor cells with IC₅₀ values ranging from 3.85 to 25.63 μmol/L.

R284.1

中南大学研究生自主探索创新项目（1053320184128，2019zzts767）