目的 研究荔枝Litch chinensis核正丁醇部位的化学成分及生物活性。方法 利用硅胶、D101大孔树脂、MCI、ODS、Sephadex LH-20及半制备型高效液相等色谱技术进行分离纯化，根据理化性质和波谱数据鉴定化合物结构；采用Griess法测定化合物对脂多糖诱导的小鼠巨噬细胞RAW264.7产生一氧化氮（NO）的抑制活性；采用1,1-二苯基-2-三硝基苯肼（1,1-diphenyl-2-trinitrophenylhydrazine，DPPH）方法测定化合物的体外抗氧化活性。结果 从荔枝核正丁醇部位分离得到15个化合物，分别鉴定为柚皮素-7-O-(2'',6''-二-O-α-L-鼠李糖基)-β-D-吡喃葡萄糖苷（1）、litchioside D（2）、异鼠李素-3-O-(2'',6''-二-O-α-L-鼠李糖基)-β-D-吡喃葡萄糖苷（3）、山柰酚-3-O-(6-O-啡酰基)-β-葡萄糖基-(1→3)-α-鼠李糖-7-O-α-鼠李糖苷（4）、5'-O-β-D-葡萄糖苷茉莉酮酸甲酯（5）、5'-O-β-D-葡萄糖苷茉莉酮酸丁酯（6）、5'-O-β-D-葡萄糖苷茉莉酮酸（7）、松脂素-4-O-β-D-葡萄糖苷（8）、表松脂素-4-O-β-D-葡萄糖苷（9）、pyrafortunoside A（10）、苯乙基芸香苷（11）、苯甲醇-O-β-D-吡喃葡萄糖苷（12）、methyl-1-(β-D-ribofuranosyl)-imidazolin-2-one-4-carboxylate（13）、莽草酸甲酯（14）和莽草酸（15）。体外抗炎活性结果表明，化合物13能明显抑制脂多糖诱导的RAW264.7细胞NO释放，其半数抑制浓度（median inhibition concentration，IC₅₀）为（27.9±2.8）μmol/L；化合物15具有一定的抑制活性，其IC₅₀为（62.4±9.7）μmol/L。体外抗氧化活性结果表明，化合物4对DPPH自由基具有一定的清除活性，其IC₅₀为（109.8±1.5）μmol/L。结论 化合物1、3～6、9～15为首次从荔枝核中分离得到。化合物13有较强体外抗炎活性，化合物15有一定的体外抗炎活性。化合物4具有一定的体外抗氧化活性。

Objective To study the chemical constituents and biological activities from the n-butanol extract of Lizhihe (Litchi Semen). Methods The compounds were systematically isolated and purified by using various chromatographic separation and analysis techniques, including silica gel, D101 macroporous resins, MCI, ODS, Sephadex LH-20 chromatographies and semi-prepative HPLC. The structures were identified on the basis of physicochemical properties and spectral data. The inhibitory effect of the compound on nitirc oxide production in LPS-induced mouse macrophage RAW264.7 cells was evaluated by Griss assay. Moreover, the antioxidant activities in vitro were tested by DPPH assay. Results A total of 15 compounds were isolated and identified as naringenin-7-O-(2'',6''-di-O-α-L-rhamnopyranosyl)-β-D-glucopyranoside (1), litchioside D (2), isorhamnetin-3-O-(2'',6''-di-O-α-L-rhamnopyranosyl)-β-D-glucopyranoside (3), kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl(1 → 3)-α-rhamnopyranoside]-7-O-α-rhamnopyranoside (4), 5'-O-β-D-glucopyranosyloxyjasmo-nic methyl ester (5), 5'-O-β-Dglucopyranosyloxyjasmonic butyl ester (6), 5'-O-β-D-glucopyranosyloxyjasmonic acid (7), pinoresinol-4-O-β-D-glucopyranoside (8), epipinoresinol-4-O-β-D-glucopyranoside (9), pyrafortunoside A (10), phenylethyl-rutinoside (11), benzyl alcohol-O-β-Dglucopyranoside (12), methyl-1-(β-D-ribofuranosyl)-imidazolin-2-one-4-carboxylate (13), methyl shikimate (14), and shikimic acid (15). Amoung them, compound 13 showed strong inhibitory activities against LPS-induced NO production in RAW264.7 macrophages, with IC₅₀ value of (27.9±2.8) μmol/L, 15 exhibted obvious activities with IC₅₀ value of (62.4±9.7) μmol/L. Additionally, compound 4 displayed a degree of DPPH radical scavenging activities with IC₅₀ value of (109.8±1.5) μmol/L. Conclusion Compounds 1, 3—6, 9—15 are isolated form Litchi Semen for the first time. Compound 13 had strong anti-inflammatory activity in vitro and 15 possessed moderate anti-inflammatory activity. Moreover, Compound 4 was found to have moderate anti-oxidant activity.

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国家自然科学基金资助项目(82260758);国家自然科学基金资助项目(31860092);云南省高层次人才培养支持计划"青年拔尖人才"专项(YNWR-QNBJ-2020-255);云南省基础研究计划面上项目(202101AT070254);云南省南药可持续利用研究重点实验室开放课题重点项目(202105AG070012ZD2201)