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OBJECTIVE To design, synthesize and evaluate a series of 3', 4'-ethylendioxy chalcone derivatives as monoamine oxidase B (MAO-B) inhibitors, and summarize the structure-activity relationship (SAR). METHODS The targeted compounds were synthesized via Claisen-Schmidt condensation reaction starting from 6-acetyl-1, 4-benzodioxan and corresponding benzaldehydes. The inhibition of these compounds on human MAO-B (hMAO-B) was determined, and the inhibiting selectivity, dynamics and reversibility were investigated as well. The binding mode between active compounds and hMAO-B was revealed by molecular docking study. Additionally, the inhibitory effect of active compounds on the proliferation of BV2 cell line was determined by MTT assay. RESULTS Sixteen targeted compounds were successfully prepared. Most compounds showed good inhibitory effects on hMAO-B. Representative compounds 9 and 13 exhibited IC50 values of 0.021 and 0.042 μmol·L-1, respectively, which showed high inhibiting selectivity towards hMAO-B. Both compounds acted as competitive and reversible hMAO-B inhibitors. The main interactions between active compounds and hMAO-B were hydrophobic interaction and hydrogen bond. The most active compound 9 exhibited low cytotoxicity in BV2 cells. CONCLUSION This class of 3', 4'-ethylendioxy chalcone derivatives represent potential novel inhibitors of hMAO-B, and compound 9 could be further investigated as a potent lead for future studies.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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