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New Tyrosinase Inhibitors from Paecilomyces gunnii

机译:拟青霉新的酪氨酸酶抑制剂

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摘要

Through screening 50 strains of entomopathogenic fungi and rescreening of 7 strains of Paecilomyces gunnii, a methanol extract of liquid-cultivated mycelia of P. gunnii was found to have the strongest tyrosinase inhibitory activity. Preparative high-speed counter-current chromatography (HSCCC) guided by high-performance liquid chromatography (HPLC)-electrospray ionization (ESI)-high-resolution mass spectrometry (HRMS) was employed for the isolation and purification of the active components, and three new compounds with half inhibition concentration (IC50) of 0.11, 0.17, and 0.14 mM against diphenolase were obtained from the extract, respectively. Their chemical structures were identified by HRMS, one- and two-dimensional nuclear magnetic resonance (2D NMR) spectroscopy as paecilomycones A, B, and C. Structure and activity studies showed that the tyrosinase inhibition activities are positively related to the number of hydroxyl groups on the paecilomycones.
机译:通过筛选50株昆虫病原性真菌并重新筛选7株古尼拟青霉,发现液体培养的古尼氏菌菌丝体的甲醇提取物具有最强的酪氨酸酶抑制活性。高效液相色谱(HPLC)-电喷雾电离(ESI)-高分辨率质谱(HRMS)指导下的制备型高速逆流色谱(HSCCC)用于分离和纯化活性成分,其中三个从提取物中分别获得了对双酚酶的半数抑制浓度(IC50)为0.11、0.17和0.14 mM的新化合物。通过HRMS,一维和二维核磁共振(2D NMR)光谱法鉴定了它们的化学结构为拟青霉素A,B和C。结构和活性研究表明酪氨酸酶抑制活性与羟基数成正相关在粉刺锥上。

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