title: Isobavachalcone and bavachinin from Psoraleae Fructus modulate Aβ42 aggregation process through different mechanisms in vitro.
abstract: Spontaneous aggregation of Aβ is a key factor in the development of Alzheimer's disease. In searching for Aβ aggregation inhibitors from traditional Chinese herbal medicines, we identified two active compounds from Psoraleae Fructus, namely isobavachalcone and bavachinin. We further demonstrated that the two compounds modulate Aβ42 aggregation process through different mechanisms. Isobavachalcone significantly inhibits both oligomerization and fibrillization of Aβ42, whereas bavachinin inhibits fibrillization and leads to off-pathway aggregation. Both of the compounds attenuated Aβ42-induced toxicity in a SH-SY5Y cell model. These findings may provide valuable information for new drug development and Alzheimer's therapy in the future.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Xiumin
authors.initials: X
authors.lastname: Chen
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Yang
authors.forename: Yingtao
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D005419:Flavonoids / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry*; D006801:Humans; D010446:Peptide Fragments / Q000037:antagonists & inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D055503:Protein Multimerization / Q000187:drug effects; D029907:Psoralea / Q000737:chemistry*; D047309:Flavones
chemical_list: D016229:Amyloid beta-Peptides; D047188:Chalcones; D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42); C468754:isobavachalcone; C468752:bavachinin; D047309:Flavones
keywords: AD; Aggregation inhibitor; Alzheimer’s disease; Amyloid beta; Aβ; BC; BCN; BKC; Bavachinin; IBC; IPL; Isobavachalcone; NBIF; PFE; PL; PLD; Psoraleae Fructus; ThT; amyloid-beta peptide; bakuchiol; bavachin; bavachinin; isobavachalcone; isopsoralen; methanol extract of Psoraleae Fructus; neobavaisoflavone; psoralen; psoralidin; thioflavin T