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OBJECTIVE To synthesize scutellarein derivatives and study their solubility and bioactivity. METHODS Based on the lead compound scutellarein, 12 compounds were designed and synthesized using functional group substitution, parent nucleus ring opening, and electron rearrangement principles. The structures of the compounds were characterized through 1H-NMR, 13C-NMR and MS, their solubility was tested, and their transient receptor potential vanilloid 3 (TRPV3) inhibitory activities were evaluated through calcium flow detection. An animal model of psoriasis induced by imiquimod (IMQ) was established and the three most active compounds were selected for anti-psoriasis evaluation. RESULTS All compounds had higher solubility than scutellarein. In the calcium flow experiment, compounds I-01, I-04, and I-06 showed stronger TRPV3 inhibition than scutellarein, with I-06 having the strongest activity. Animal experiments on psoriasis showed that I-01, I-04, and I-06 could significantly improve the pathological appearance and inflammatory response of psoriasis mice, and I-06 performed the best. CONCLUSION This type of modified scutellarein has potential therapeutic value for psoriasis and provides a new approach for targeting TRPV3 to treat various skin diseases.
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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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