Li Zhiqiang, Zhang Haonan, Li Wanting, Yao Min, Yu Huimin, He Mingzhen, Feng Yulin, Li Zhifeng
Jiangxi University of Chinese Medicine, No. 818 Yunwan Road, Nanchang 330002, PR China.
State Key Laboratory of Innovative Drug and Efficient Energy-Saving Pharmaceutical Equipment, No. 56 Yangming Road, Nanchang 330006, PR China.
Bioorg Chem. 2023 Sep;138:106604. doi: 10.1016/j.bioorg.2023.106604. Epub 2023 May 10.
Traditional Chinese medicine is the main source of natural products due to its remarkable clinical efficacy. Syringa oblata Lindl (S. oblata) was widely used because of its extensive biological activities. However, to explore the antioxidant components of S. oblata against tyrosinase, the experiments of antioxidation in vitro were employed. At the same time, the determination of TPC was also use to assess the antioxidant ability of CE, MC, EA and WA fractions and the liver protective activity of the EA fraction was evaluated by mice in vivo. Next, UF-LC-MS technology was performed to screen and identify the efficient tyrosinase inhibitors in S. oblata. The results showed that alashinol (G), dihydrocubebin, syripinin E and secoisolariciresinol were characterized as potential tyrosinase ligands and their RBA values were 2.35, 1.97, 1.91 and 1.61, respectively. Moreover, these four ligands can effectively dock with tyrosinase molecules, with binding energies (BEs) ranging from 0.74 to -0.73 kcal/mol. In addition, tyrosinase inhibition experiment was employed to evaluate the tyrosinase inhibition activities of four potential ligands, the result showed that compound 12 (alashinol G, IC = 0.91 ± 0.20 mM) showed the strongest activity to tyrosinase, followed by secoisolariciresinol (IC = 0.99 ± 0.07 mM), dihydrocubebin (IC = 1.04 ± 0.30 mM) and syripinin E (IC = 1.28 ± 0.23 mM), respectively. The results demonstrate that S. oblata might have excellent antioxidant activity, and UF-LC-MS technique is a effective means to filter out tyrosinase inhibitors from natural products.
由于其显著的临床疗效,传统中药是天然产物的主要来源。紫丁香因其广泛的生物活性而被广泛应用。然而,为了探索紫丁香对酪氨酸酶的抗氧化成分,进行了体外抗氧化实验。同时,还采用总酚含量测定来评估CE、MC、EA和WA组分的抗氧化能力,并通过小鼠体内实验评估EA组分的肝脏保护活性。接下来,利用超高效液相色谱-质谱联用技术筛选和鉴定紫丁香中有效的酪氨酸酶抑制剂。结果表明,阿拉新醇(G)、二氢荜澄茄素、紫丁香素E和开环异落叶松脂素被鉴定为潜在的酪氨酸酶配体,它们的相对结合亲和力(RBA)值分别为2.35、1.97、1.91和1.61。此外,这四种配体可以有效地与酪氨酸酶分子对接,结合能(BEs)范围为0.74至-0.73千卡/摩尔。此外,采用酪氨酸酶抑制实验评估四种潜在配体的酪氨酸酶抑制活性,结果表明化合物12(阿拉新醇G,IC = 0.91±0.20毫摩尔)对酪氨酸酶的活性最强,其次是开环异落叶松脂素(IC = 0.99±0.07毫摩尔)、二氢荜澄茄素(IC = 1.04±0.30毫摩尔)和紫丁香素E(IC = 1.28±0.23毫摩尔)。结果表明,紫丁香可能具有优异的抗氧化活性,超高效液相色谱-质谱联用技术是从天然产物中筛选酪氨酸酶抑制剂的有效手段。