|
|
Pharmacy Information 2026
补骨脂素药理活性研究进展
|
Abstract:
补骨脂素(Psoralen)是一种天然线性呋喃香豆素类化合物，主要来源于补骨脂(Psoralea corylifolia L.)种子，也广泛存在于多种植物中。近年来，补骨脂素因其广泛的药理活性受到广泛关注。本文系统综述了补骨脂素的抗骨质疏松、抗肿瘤、抗抑郁、抗微生物、抗炎、雌激素样、神经保护、抗氧化及保肝等药理作用及其分子机制，同时总结了其药代动力学特征与安全性(肝毒性、胚胎毒性)。补骨脂素通过调控BMP/Smad、MAPK、Wnt/β-catenin、NF-κB、内质网应激、5-HT能系统及HPA轴等多条信号通路发挥生物效应。然而，其肝毒性等问题限制了临床转化。本文旨在为补骨脂素的进一步研究与开发利用提供参考。
Psoralen is a naturally occurring linear furanocoumarin compound primarily derived from the seeds of Psoralea corylifolia L. and widely present in various plants. In recent years, psoralen has received extensive attention due to its broad pharmacological activities. This article systematically reviews the pharmacological effects and molecular mechanisms of psoralen, including anti-osteoporosis, anti-tumor, antidepressant, antimicrobial, anti-inflammatory, estrogen-like, neuroprotective, antioxidant, and hepatoprotective activities. Meanwhile, its pharmacokinetic properties and safety profiles (hepatotoxicity, embryotoxicity) are also summarized. Psoralen exerts its biological effects by regulating multiple signaling pathways such as BMP/Smad, MAPK, Wnt/β-catenin, NF-κB, endoplasmic reticulum stress, the serotonergic system, and the HPA axis. However, issues such as hepatotoxicity and phototoxicity limit its clinical translation. This review aims to provide a reference for further research, development, and utilization of psoralen.
| [1] | Jamalis, J., Yusof, F.S.M., Chander, S., Wahab, R.A., P. Bhagwat, D., Sankaranarayanan, M., et al. (2020) Psoralen Derivatives: Recent Advances of Synthetic Strategy and Pharmacological Properties. Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry, 19, 222-239. https://doi.org/10.2174/1871523018666190625170802 |
| [2] | Zhang, X., Zhao, W., Wang, Y., Lu, J. and Chen, X. (2016) The Chemical Constituents and Bioactivities of Psoralea corylifolia Linn.: A Review. The American Journal of Chinese Medicine, 44, 35-60. https://doi.org/10.1142/s0192415x16500038 |
| [3] | Ren, Y., Song, X., Tan, L., Guo, C., Wang, M., Liu, H., et al. (2020) A Review of the Pharmacological Properties of Psoralen. Frontiers in Pharmacology, 11, Article ID: 571535. https://doi.org/10.3389/fphar.2020.571535 |
| [4] | Wu, C., Sun, Z., Ye, Y., Han, X., Song, X. and Liu, S. (2013) Psoralen Inhibits Bone Metastasis of Breast Cancer in Mice. Fitoterapia, 91, 205-210. https://doi.org/10.1016/j.fitote.2013.09.005 |
| [5] | Xu, Q., Pan, Y., Yi, L., Li, Y., Mo, S., Jiang, F., et al. (2008) Antidepressant-Like Effects of Psoralen Isolated from the Seeds of Psoralea Corylifolia in the Mouse Forced Swimming Test. Biological and Pharmaceutical Bulletin, 31, 1109-1114. https://doi.org/10.1248/bpb.31.1109 |
| [6] | Wang, Y., Hong, C., Zhou, C., Xu, D. and Qu, H. (2011) Screening Antitumor Compounds Psoralen and Isopsoralen from Psoralea corylifolia L. Seeds. Evidence-Based Complementary and Alternative Medicine, 2011, 1-7. https://doi.org/10.1093/ecam/nen087 |
| [7] | 韩宇, 郭晏华, 于艳. 补骨脂素介导Hedgehog信号通路促进骨髓MSC成骨分化作用研究[J]. 辽宁中医杂志, 2019, 46(6): 1133-1137. |
| [8] | Zhang, J., Tian, J., Weiyang, W., Yang, Y., Li, Y., Ye, X., et al. (2026) Psoralen Promotes SOCS5 to Inhibit JAK/STAT3 to Alleviate Cartilage Degeneration in Knee Osteoarthritis. Phytomedicine, 150, Article 157643. https://doi.org/10.1016/j.phymed.2025.157643 |
| [9] | Fan, Z., Gao, J., Chen, Y., Chen, Q., Peng, Q., Le, J., et al. (2025) Psoralen Remodels the Articular Cartilage Microenvironment by Pharmacologically Regulating the NRF2 Pathway in Osteoarthritis Treatment. International Immunopharmacology, 149, Article 114221. https://doi.org/10.1016/j.intimp.2025.114221 |
| [10] | Chen, S., Wang, Y., Yang, Y., Xiang, T., Liu, J., Zhou, H., et al. (2017) Psoralen Inhibited Apoptosis of Osteoporotic Osteoblasts by Modulating IRE1-ASK1-JNK Pathway. BioMed Research International, 2017, 1-9. https://doi.org/10.1155/2017/3524307 |
| [11] | 史博, 杨健, 张立喜. 补骨脂素通过miR-101/PI3K/Akt轴对骨肉瘤细胞侵袭、转移的影响[J]. 西北药学杂志, 2024, 39(4): 64-69. |
| [12] | Guo, Y., Xu, S., Pan, X., Xin, W., Cao, W., Ma, W., et al. (2024) Psoralen Protects Neurons and Alleviates Neuroinflammation by Regulating Microglial M1/M2 Polarization via Inhibition of the Fyn-PKCδ Pathway. International Immunopharmacology, 137, Article 112493. https://doi.org/10.1016/j.intimp.2024.112493 |
| [13] | Yu, X., Wen, Y., Liang, C., Liu, J., Ding, Y. and Zhang, W. (2017) Design, Synthesis and Antifungal Activity of Psoralen Derivatives. Molecules, 22, Article 1672. https://doi.org/10.3390/molecules22101672 |
| [14] | Asgaonkar, K.D., Patil, S.M., Chitre, T.S., Prabhu, A., Shevate, K.S., Sagar, A.K., et al. (2024) Use of Pharmacophore Modeling, 3D-Atom-Based QSAR, ADMET, Docking, and Molecular Dynamics Studies for the Development of Psoralen-Based Derivatives as Antifungal Agents. Anti-Infective Agents, 22, 33-47. https://doi.org/10.2174/0122113525279683231228130206 |
| [15] | 曹柳, 唐晓晴, 罗青, 等. 补骨脂素对溃疡性结肠炎小鼠肠道屏障及继发性肝损伤的改善作用[J]. 天然产物研究与开发, 2024, 36(7): 1121-1129, 1148. |
| [16] | Wang, Y., Zhang, J., Xu, S., Li, J., Liu, W., Jiang, M., et al. (2025) Psoralen Alleviates Acute Lung Injury by Covalently Targeting Cys106 of HMGB1 in Macrophages to Inhibit Inflammatory Responses. Phytomedicine, 142, Article 156807. https://doi.org/10.1016/j.phymed.2025.156807 |
| [17] | Cao, L., Tang, X., Wang, X., Wang, Y. and Dai, W. (2025) Psoralen Alleviates Ulcerative Colitis by Suppressing Inflammation, Modulating Oxidative Stress, and Regulating Ferroptosis. European Journal of Pharmacology, 1005, Article 178081. https://doi.org/10.1016/j.ejphar.2025.178081 |
| [18] | 瞿晶田, 王家龙, 柴士伟, 等. 补骨脂素和补骨脂酚舒张血管的作用机制研究[J]. 中国药房, 2019, 30(24): 3364-3368. |
| [19] | 谢何昕. 补骨脂素的植物雌激素作用及其机制[J]. 中国畜牧兽医文摘, 2018, 34(6): 115. |
| [20] | 刘磊. 补骨脂素对白癜风的疗效探讨[J]. 世界最新医学信息文摘, 2021, 21(42): 197-198. |
| [21] | 蒲位凌, 夏宁, 张孝莹, 等. 基于代谢组学的补骨脂素在2d和3d培养模型的肝毒性差异研究[J]. 中国药理学通报, 2024, 40(2): 399-400. |
| [22] | 裴天仙, 李福珍, 陈梦颖, 等. 补骨脂素对正常大鼠和阴虚大鼠肝脏毒性差异研究及机制初探[J]. 中国药理学通报, 2025, 41(5): 843-850. |
