目的 研究补骨脂70%乙醇水提取物的环己烷溶性部分的补骨脂酚及其衍生物对脂多糖（LPS）诱导的鼠性巨噬细胞RAW 264.7产生一氧化氮（NO）抑制作用的生物学活性。方法 采用硅胶、高效液相色谱等柱色谱方法进行分离纯化，通过化合物的谱学数据鉴定其结构。采用LPS离体诱导RAW264.7细胞的NO生成模型，研究化合物对NO生成的抑制活性。结果 从补骨脂70%乙醇水提取物的环己烷溶性部分分离出12个化合物，分别鉴定为补骨脂酚（1）、12，13-二氢-12，13-环氧补骨脂酚（2）、Δ³，2-羟基补骨脂酚（3）、12-氧代补骨脂酚（4）、补骨脂醚酚B（5）、补骨脂醚酚C（6）、（12'S）-双补骨脂酚C（7）、Δ^1，3-补骨脂酚（8）、13-甲氧基异补骨脂酚（9）、双补骨脂酚B（10）、双补骨脂酚A（11）和12，13-二氢-12，13-二羟基补骨脂酚（12）。在LPS诱导的RAW 264.7细胞NO生成实验模型中，以L-N⁶-（1-亚胺乙基）-赖氨酸（L-NIL）应用为阳性对照药，其抑制NO生成的半数抑制浓度（IC₅₀）为（10.29±1.10）μmol/L。化合物1、3、5、10、11抑制作用的IC₅₀值大于50 μmol/L，化合物8、9、12的IC₅₀值接近于阳性药，但化合物2、4、7的IC₅₀值皆小于阳性对照药，且具有统计学意义。结论 化合物4为新的天然产物。生物活性实验结果提示化合物2、4、7～9、12可能具有潜在的抗炎作用。

Objective To study bakuchiol and its derivatives of cyclohexane soluble part in 70% ethanol aqueous extract of Psoraleae Fructus and their inhibition on nitric oxide (NO) production in lipopolysaccharides (LPS)-activated murine macrophage RAW 264.7 cell lines. Methods The compounds were separated and purified by silica gel column and high performance liquid chromatographies, and their structures were determined by spectroscopic data analyses. Using LPS-activated RAW 264.7 cell line models in vitro, all of the isolated compounds were evaluated for the inhibition against NO production. Results Twelve compounds were obtained and identified as bakuchiol (1), 12,13-dihydro-12,13-epoxybakuchiol (2), Δ³,2-hydroxylbakuchiol (3), 12-oxobakuchiol (4), psoracorylifol B (5), psoracorylifol C (6), (12'S)-bisbakuchiol C (7), Δ^1,3-bakuchiol (8), 13-methoxyisobakuchiol (9), bisbakuchiol B (10), bisbakuchiol A (11), and 12,13-dihydro-12,13-dihydroxybakuchiol (12), respectively. For the inhibition of NO production in the LPS-activated RAW 264.7 cell line model, a positive inhibitor, L-N⁶-(1-iminoethyl)-lysine (L-NIL), was used and showed the half maximal inhibitory concentration (IC₅₀) value of (10.29 ±1.10) μmol/L. The IC₅₀ values of the assayed compounds 1, 3, 5, 10 and 11 were all more than 50 μmol/L, compounds 8, 9 and 12 were comparable to that of L-NIL, whereas the IC₅₀ values of compounds 2, 4 and 7 were less than that of the positive inhibitor with statistically significance. Conclusion Compound 4 is a new natural product. The results of the bioactivity assays indicated that compounds 2, 4, 7, 8, 9 and 12 are potential anti-inflammatory agents.

R284.1

国家自然科学基金资助项目（81773865）