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OBJECTIVE To modify and optimize the structure of osthole derivatives with better antibacterial activities. METHODS First, intermediate 2 was synthesized by oxidation of SeO2 and NaClO2/NaH2PO4 using osthole extract as raw material. Next, intermediate 3 was synthesized through condensation reaction of Boc-L-phenylalanine and amines, followed by deprotection reaction. Then, the target compounds were prepared by recondensing intermediate 2 and 3. Finally, the antibacterial activities of the products were tested by the agar dilution method. RESULTS Twenty-two osthole derivatives were synthesized, and their structures were confirmed by NMR and elemental analysis. The results showed that these compounds had better inhibitory effects on the tested bacteria. The activities of compounds 4o and 4q against E. coli, MRSA and FREC were the most significant, the MIC of 4o was 2, 16, and 4 μg·mL-1 respectively, and the MIC of 4q was 4, 16, and 8 μg·mL-1 respectively, which were superior to that of the control drug oxacillin. CONCLUSION Some derivatives have significant inhibitory effects on both gram-positive and negative bacteria. The introduction of L-phenylalanine into the structure of osthole can enhance its anti-gram-negative bacteria activities.
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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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