目的 研究药西瓜Citrullus colocynthis的化学成分及其体外抗炎活性。方法 综合运用正相硅胶、ODS、Sephadex LH-20凝胶及半制备型高效液相色谱等多种色谱技术进行分离纯化，依据HR-ESI-MS、IR、NMR等谱学技术确定化合物结构。采用CCK-8法筛选化合物对小鼠单核巨噬细胞RAW264.7的细胞毒性，通过脂多糖（lipopolysaccharide，LPS）诱导的RAW264.7细胞炎症模型对低毒性化合物进行抗炎活性评价。结果 从药西瓜醋酸乙酯相中分离得到9个化合物，分别鉴定为 (20R,23E)-2-O-β-D-glucopyranosyl-20-hydroxycucurbita-1,5,23-triene-25-acetoxy-3,11,16,22-tetraone（1）、葫芦素E-2-O-β-D-吡喃葡萄糖苷（2）、colocynthenin G（3）、khekadaengoside G（4）、khekadaengoside H（5）、葫芦素E（6）、colocynin D（7）、endecaphyllacin B（8）和colocynin A（9）。化合物1～3和6（40 μmol/L）对RAW264.7细胞显示出明显的细胞毒性, 化合物4、5、7～9对LPS诱导下RAW264.7细胞释放NO具有一定的抑制作用，IC₅₀为（21.49±3.48）～（39.97±3.50）μmol/L。结论 化合物1为新的葫芦烷型三萜皂苷，命名为葫芦素酮A（cucurbitacone A），化合物8为首次从该植物分离得到；化合物4、5、7～9表现出一定的抗炎活性。

Objective To investigate the chemical constituents of Citrullus colocynthi and their anti-inflammatory activities. Methods The compounds were isolated and purified by using a positive silica gel, ODS, Sephadex LH-20, and semi-preparative HPLC, and their structures were elucidated by HR-ESI-MS, IR, NMR. Screening cytotoxicity of all compounds to RAW264.7 cells using the CCK-8 method, and evaluating the anti-inflammatory activity of low toxicity compounds through the RAW264.7 cell inflammatory model induced by lipopolysaccharide (LPS). Results A total of nine compounds were isolated from the ethyl acetate phase ofC. colocynthisand identified as (20R,23E)-2-O-β-D-glucopyranosyl-20-hydroxycucurbita-1,5,23-triene-25-acetoxy-3,11,16,22-tetraone (1), cucurbitacin E 2-O-β-D-glucopyranoside (2), colocynthenin G (3), khekadaengoside G (4), khekadaengoside H (5), cucurbitacin E (6), colocynin D (7), endecaphyllacin B (8), colocynin A (9). Compounds 1, 2, 3 and 6 (40 μmol/L) showed significant cytotoxicity to RAW264.7 cells, while compounds 4, 5, 7—9 exhibited a certain inhibitory effect on the release of NO by RAW264.7 cells induced by LPS with IC₅₀ value ranging from (21.49 ±3.48) to (39.97 ±3.50) μmol/L. Conclusion Compound 1 is a new compound and named cucurbitacone A, and compound 8 is first isolated from the plant. Compounds 4, 5, 7—9 show certain anti-inflammatory activity.

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伊犁师范大学提升学科综合实力专项项目（22XKZZ08）;国家自然科学基金资助项目（82060774）