[关键词]
[摘要]
目的 研究高乌头Aconitum sinomontanum 根的化学成分及其抗炎活性。方法 采用硅胶、凝胶柱色谱以及半制备液相色谱等方法进行分离纯化,并结合其理化性质及高分辨质谱(HR-ESI-MS)、红外光谱(IR)、核磁共振等波谱技术进行结构解析。采用脂多糖(lipopolysaccharides,LPS)诱导的RAW 264.7细胞测定分离所得化合物的NO抑制活性。结果 从高乌头80%乙醇提取物中分离得到8个二萜生物碱类化合物,分别鉴定为1α,9ξ,14α,22-四羟基-乌头碱(1)、翠雀灵(2)、vaginatunine C(3)、acoseptrine(4)、acosanine(5)、dehydroacosanine(6)、takaosamine(7)、飞燕草碱(8)。化合物1和5抑制LPS诱导的RAW 264.7细胞中NO释放的半数抑制浓度(median inhibition concentration,IC50)值分别为(65.05±4.58)、(78.38±1.26)μmol/L,阳性药氨基胍基盐酸盐的IC50值为(12.62±1.52)μmol/L。结论 化合物1为新化合物,命名为高乌头碱A;化合物2~7首次从该植物中分离得到,化合物1和5具有一定的抗炎活性。
[Key word]
[Abstract]
Objective To study the chemical constituents and anti-inflammatory activity of roots of Aconitum sinomontanum. Methods The compounds were isolated and purified by silica gel, gel column chromatography and semi-preparative liquid chromatography, and their structures were elucidated by physicochemical properties and spectroscopic techniques such as high resolution electronspray ionization mass spectrometry (HR-ESI-MS), infrared spectrum (IR), and nuclear magnetic resonance. The NO inhibitory activity of the isolated compounds was determined by lipopolysaccharide (LPS)-induced RAW264.7 cells. Results A total of eight compounds were isolated from 80% ethanol extract of A. sinomontanum, all of which were diterpenoid alkaloids and identified as 1α,9ξ,14α,22-tetrahydroxy-aconitine (1), delsoline (2), vaginatunine C (3), acoseptrine (4), acosanine (5), dehydroacosanine (6), takaosamine (7), delcosine (8). The median inhibition concentration (IC50) values of compounds 1 and 5 for inhibiting NO release in LPS-induced RAW264.7 cells were (65.05 ± 4.58) and (78.38 ± 1.26) μmol/L, respectively. The IC50 value of the positive drug aminoguanidine hydrochloride was (12.62 ± 1.52) μmol/L. Conclusion Compound 1 was a new compound, named aconsinomtine A, and compounds 2—7 was isolated from the plant for the first time. Compound 1 and 5 possessed certain anti-inflammatory activity.
[中图分类号]
R284.1
[基金项目]
国家自然科学基金项目(82104368);陕西中医药大学创新团队项目(2023-CXTD-05);国家中医药管理局重点学科项目(zyyzdxk-2023202);陕西中医药大学研究生质量提升工程项目(CXSJ202418);秦创原产业聚集区联合基金项目(L2024-QCY-ZYYJJQ-X32)