基于受体-配体亲和力的筛选和分离，从火木层孔菌中筛选出水溶性 5-脂氧合酶抑制剂。
Receptor-ligand affinity-based screening and isolation of water-soluble 5-lipoxygenase inhibitors from Phellinus igniarius.
机构信息
Central Laboratory, Changchun Normal University, No. 677 North Changji Road, Erdao District, Changchun 130032, China.
Central Laboratory, Changchun Normal University, No. 677 North Changji Road, Erdao District, Changchun 130032, China.
出版信息
J Chromatogr B Analyt Technol Biomed Life Sci. 2022 Oct 15;1209:123415. doi: 10.1016/j.jchromb.2022.123415. Epub 2022 Aug 11.
We developed an efficient combination method for extraction, biological activity screening, and preparation of 5-lipoxygenase inhibitors from Phellinus igniarius. 5-Lipoxygenase inhibitors were rapidly screened using ultrafiltration-liquid chromatography based on the receptor-ligand affinity. Parameters such as extraction time, extraction times, and temperature as well as liquid-solid ratio were optimized using response surface methodology to maximize the total yield of the three target compounds. Next, bioactive ingredients were isolated using high-speed countercurrent chromatography and semi-preparative liquid chromatography. Three active ingredients, phellibaumin E, protocatechuic aldehyde, and osmundacetone, were obtained via ultrafiltration-liquid chromatography. Subsequently, the potential anti-dementia effects of the obtained bioactive compounds were verified using molecular docking assays. The above-mentioned target compounds, with purities of 98.82%, 98.89%, and 99.51%, respectively, were separated using a two-phase solvent system consisting of n-hexane-ethyl acetate-ethanol-water (2.5:2:0.75:3, v/v/v/v) coupled with semi-preparative liquid chromatography.
我们开发了一种从桑黄中提取、筛选 5-脂氧合酶抑制剂并制备 5-脂氧合酶抑制剂的高效组合方法。基于受体-配体亲和力，采用超滤-液相色谱快速筛选 5-脂氧合酶抑制剂。利用响应面法优化提取时间、提取次数、温度和液固比等参数，以最大限度地提高三种目标化合物的总产率。然后，采用高速逆流色谱和半制备液相色谱分离生物活性成分。通过超滤-液相色谱获得三种活性成分：桑黄甲素 E、原儿茶醛和欧山芹酮。随后，通过分子对接试验验证了所得生物活性化合物的潜在抗痴呆作用。上述目标化合物分别用正己烷-乙酸乙酯-乙醇-水（2.5:2:0.75:3，v/v/v/v）两相溶剂系统和半制备液相色谱分离，纯度分别为 98.82%、98.89%和 99.51%。
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