Ren Yali, Song Xiaominting, Tan Lu, Guo Chuanjie, Wang Miao, Liu Hui, Cao Zhixing, Li Yuzhi, Peng Cheng
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Key Laboratory of Standardization for Chinese Herbal Medicine, Ministry of Education, National Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, Chengdu, China.
Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China, Pharmaceutical University, Nanjing, China.
Front Pharmacol. 2020 Sep 4;11:571535. doi: 10.3389/fphar.2020.571535. eCollection 2020.
Psoralen is the principal bioactive component in the dried fruits of (L.) Medik (syn. L), termed "Buguzhi" in traditional Chinese medicine (TCM). Recent studies have demonstrated that psoralen displays multiple bioactive properties, beneficial for the treatment of osteoporosis, tumors, viruses, bacteria, and inflammation. The present review focuses on the research evidence relating to the properties of psoralen gathered over recent years. Firstly, multiple studies have demonstrated that psoralen exerts strong anti-osteoporotic effects regulation of osteoblast/osteoclast/chondrocyte differentiation or activation due to the participation in multiple molecular mechanisms of the wnt/β-catenin, bone morphogenetic protein (BMP), inositol-requiring enzyme 1 (IRE1)/apoptosis signaling kinase 1 (ASK1)/c-jun N-terminal kinase (JNK) and the Protein Kinase B(AKT)/activator protein-1 (AP-1) axis, and the expression of miR-488, peroxisome proliferators-activated receptor-gamma (PPARγ), and matrix metalloproteinases (MMPs). In addition, the antitumor properties of psoralen are associated with the induction of ER stress-related cell death enhancement of PERK: Pancreatic Endoplasmic Reticulum Kinase (PERK)/activating transcription factor (ATF), 78kD glucose-regulated protein (GRP78)/C/EBP homologous protein (CHOP), and 94kD glucose-regulated protein (GRP94)/CHOP signaling, and inhibition of P-glycoprotein (P-gp) or ATPase that overcomes multidrug resistance. Furthermore, multiple articles have shown that the antibacterial, anti-inflammatory and neuroprotective effects of psoralen are a result of its interaction with viral polymerase (Pol), destroying the formation of biofilm, and regulating the activation of tumor necrosis factor alpha (TNF-α), transforming growth factor beta (TGF-β), interleukin 4/5/6/8/12/13 (IL-4/5/6/8/12/13), GATA-3, acetylcholinesterase (AChE), and the hypothalamic-pituitary-adrenal (HPA) axis. Finally, the toxic effects and mechanisms of action of psoralen have also been reviewed.
补骨脂素是补骨脂（学名：Psoralea corylifolia L.，异名：Bakuchi L.）干燥果实中的主要生物活性成分，在传统中药中称为“补骨脂”。最近的研究表明，补骨脂素具有多种生物活性，对治疗骨质疏松症、肿瘤、病毒、细菌和炎症有益。本综述重点关注近年来收集的有关补骨脂素特性的研究证据。首先，多项研究表明，补骨脂素通过参与Wnt/β-连环蛋白、骨形态发生蛋白（BMP）、肌醇需求酶1（IRE1）/凋亡信号激酶1（ASK1）/c-Jun氨基末端激酶（JNK）以及蛋白激酶B（AKT）/激活蛋白-1（AP-1）轴的多种分子机制，以及miR-488、过氧化物酶体增殖物激活受体γ（PPARγ）和基质金属蛋白酶（MMPs）的表达，对成骨细胞/破骨细胞/软骨细胞的分化或激活发挥强大的抗骨质疏松作用。此外，补骨脂素的抗肿瘤特性与内质网应激相关细胞死亡的诱导有关，这增强了蛋白激酶R样内质网激酶（PERK）/激活转录因子（ATF）、78kD葡萄糖调节蛋白（GRP78）/C/EBP同源蛋白（CHOP）以及94kD葡萄糖调节蛋白（GRP94）/CHOP信号通路，并抑制了克服多药耐药性的P-糖蛋白（P-gp）或ATP酶。此外，多篇文章表明，补骨脂素的抗菌、抗炎和神经保护作用是其与病毒聚合酶（Pol）相互作用、破坏生物膜形成以及调节肿瘤坏死因子α（TNF-α）、转化生长因子β（TGF-β）、白细胞介素4/5/6/8/12/13（IL-4/5/6/8/12/13）、GATA-3、乙酰胆碱酯酶（AChE）以及下丘脑-垂体-肾上腺（HPA）轴激活的结果。最后，还综述了补骨脂素的毒性作用及其作用机制。
