Innovative research on natural drug
WANG Zui, YOU Yuejiao, LIU Chuang, ZHANG Wei, WANG Yifei, WANG Zhiping
Objective: To isolate terpenoids from supercritical carbon dioxide extracts of Artemisia argyi L. and evaluae their anti-inflammatory and anti-tumour activities, in order to provide a basis for the development of highly effective and low-toxicity anti-inflammatory and anti-tumour drug leads. Methods: The essential oil was extracted by supercritical carbon dioxide extraction technique after crushing the air-dried Artemisia argyi leaves. The crude extracts of essential oil were separated and purified using various separation chromatographic columns (silica gel columns, ODS, MCI, LH-20, semi-preparative HPLC, etc). The structures of the isolated compounds were identified by nuclear magnetic resonance spectroscopy. The anti-inflammatory activity of the compounds on the lipopolysaccharide (LPS)-induced RAW264.7 cell inflammation model was determined by the Griess method; the anti-tumor activity of the compounds and their toxicity to normal cells were determined by the CCK8 method. Results: Twenty-eight monomer compounds were isolated from Artemisia argyi leaves, including 3 monoterpenes, 21 sesquiterpenes, 1 diterpene compound and 3 aliphatic alcohols compounds. Compounds 4, 5, 6, 9, 10, 14 and 15 were found to have anti-inflammatory activity, among which compounds 4, 9 and 15 showed significant anti-inflammatory activity, with IC50s of (1.8±0.3) μmol/L, (1.2±0.1) μmol/L, (1.5±0.2) μmol/L, and CC50s of (28.6±1.5) μmol/L, (15.6±0.6) μmol/L, (18.9±0.7) μmol/L. Compounds 4, 5, 6, 9 and 14 possessed anti-tumour activity, of which compounds 4 and 5 were more significant, the IC50s were (5.9±0.6) μmol/L, (6.3±0.1) μmol/L and (13.5±0.9) μmol/L, (20.5±0.6) μmol/L for tumour cells U251 and A549, and the CC50s were (41.0±1.2) μmol/L and (37.4±0.2) μmol/L for normal cells BV2, which provided a certain degree of safety. Conclusion: A total of 28 compounds were isolated from the supercritical carbon dioxide extract of Artemisia argyi L. Compounds 1, 9, 11, 12, 23, and 24 were isolated from Artemisia argyi L for the first time. Compounds 4, 9, and 15 showed significant anti-inflammatory activity, while compounds 4 and 5 had significant anti-tumor activity and had pharmacological value for further study.