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[摘要]
目的 通過紅花中酪氨酸酶抑制劑的篩選,明確紅花中酪氨酸酶抑制劑成分,為美白祛斑劑的研發(fā)提供實(shí)驗(yàn)依據(jù)。方法 采用索氏提取法依次提取紅花石油醚、氯仿、醋酸乙酯、正丁醇和水5種提取物,分別檢測其對酪氨酸酶的抑制作用;針對活性組分通過UPLC-Q/TOF鑒定活性成分,并結(jié)合分子對接和酶學(xué)檢測驗(yàn)證藥效成分。結(jié)果 初步篩選結(jié)果顯示紅花水層提取物具有較強(qiáng)的抑制作用,并進(jìn)一步通過液相色譜分離,質(zhì)譜檢測,以及分子對接預(yù)測技術(shù),推測其中9種成分可能具有酪氨酸酶抑制作用,選取代表性單體羥基紅花黃色素A進(jìn)行驗(yàn)證,確認(rèn)其具有較強(qiáng)的抑制作用。結(jié)論 譜效結(jié)合構(gòu)效的篩選模式為天然產(chǎn)物中美白祛斑成分的篩選提供了便捷方法;紅花中羥基紅花黃色素A對酪氨酸酶具有明顯的抑制作用。
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[Abstract]
Objective To confirm the effective inhibitory components through screening the tyrosinase inhibitor from Carthami Flos, and to provide a basis for the development of whitening agent. Methods Soxhlet extraction system was used by petroleum ether, chloroform, ethyl acetate, butanol, and water solvent in proper sequence to extract the effective fraction of Carthami Flos and to detect the inhibition of tyrosinase activity. UPLC-Q/TOF was used to analyze and identify the active ingredients, and the molecular docking and enzymological method were used to validate their efficacy composition. Results The water layer showed a strong inhibition on the activity of tyrosinase. Through UPLC-Q/TOF system and molecular docking prediction technology, nine kinds of compounds were confirmed. Hydroxyl safflower yellow pigment A was validated to have an observable inhibition on tyrosinase activity by comparison with the standard product. Conclusion The high throughput screening system established for the white spot component screening provides a convenient method in the natural product. Especially the hydroxyl safflower yellow pigment A extracted from Carthami Flos has a significant tyrosinase inhibitory effect.
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