Identification of flavonolignans from Silybum marianum seeds as allosteric protein tyrosine phosphatase 1B inhibitors

• Published in: Journal of Enzyme Inhibition and Medicinal Chemistry Vol. 33; no. 1; pp. 1283 - 1291
• Main Authors: Qin, Ningbo, Sasaki, Tatsunori, Li, Wei, Wang, Jian, Zhang, Xiangyu, Li, Dahong, Li, Zhanlin, Cheng, Maosheng, Hua, Huiming, Koike, Kazuo
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 01.01.2018; Informa UK Limited; Taylor & Francis Group
• Subjects: Asteraceae; Asteraceae - chemistry; Dose-Response Relationship, Drug; Enzyme Inhibitors; Enzyme Inhibitors - analysis; Enzyme Inhibitors - pharmacology; flavonolignan; Flavonolignans; Flavonolignans - analysis; Flavonolignans - pharmacology; Humans; isosilybin; Molecular Docking Simulation; Molecular Structure; Protein tyrosine phosphatase 1B; Protein Tyrosine Phosphatase, Non-Receptor Type 1; Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors; Protein Tyrosine Phosphatase, Non-Receptor Type 1 - metabolism; Research Paper; RM1-950; Seeds; Seeds - chemistry; silybin; Silybum marianum; Structure-Activity Relationship; Therapeutics. Pharmacology; Protein tyrosine phosphatase 1B; flavonolignan; Silybum marianum; isosilybin; silybin

Protein tyrosine phosphatase 1B (PTP1B) is an attractive molecular target for anti-diabetes, anti-obesity, and anti-cancer drug development. From the seeds of Silybum marianum, nine flavonolignans, namely, silybins A, B (1, 2), isosilybins A, B (3, 4), silychristins A, B (5, 6), isosilychristin A (7...