State Key Laboratory of Southwestern Chinese Medicine Resources, Key Laboratory of Standardization for Chinese Herbal Medicine, Ministry of Education, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
State Key Laboratory of Southwestern Chinese Medicine Resources, Key Laboratory of Standardization for Chinese Herbal Medicine, Ministry of Education, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
Biomed Pharmacother. 2023 Oct;166:115410. doi: 10.1016/j.biopha.2023.115410. Epub 2023 Sep 4.
Forsythiae Fructus is a traditional Chinese medicine frequently in clinics. It is extensive in the treatment of various inflammation-related diseases and is renowned as 'the holy medicine of sores'. Phillygenin (CHO, PHI) is a component of lignan that has been extracted from Forsythiae Fructus and exhibits notable biological activity. Modern pharmacological studies have confirmed that PHI demonstrates significant activities in the treatment of various diseases, including inflammatory diseases, liver diseases, cancer, bacterial infection and virus infection. Therefore, this review comprehensively summarizes the pharmacological effects of PHI up to June 2023 by searching PubMed, Web of Science, Science Direct, CNKI, and SciFinder databases. According to the data, PHI shows remarkable anti-inflammatory, antioxidant, hepatoprotective, antitumour, antibacterial, antiviral, immunoregulatory, analgesic, antihypertensive and vasodilatory activities. More importantly, NF-κB, MAPK, PI3K/AKT, P2X7R/NLRP3, Nrf2-ARE, JAK/STAT, Ca-calcineurin-TFEB, TGF-β/Smads, Notch1 and AMPK/ERK/NF-κB signaling pathways are considered as important molecular targets for PHI to exert these pharmacological activities. Studies of its toxicity and pharmacokinetic properties have shown that PHI has very low toxicity, incomplete absorption in vivo and low oral bioavailability. In addition, the physico-chemical properties, new formulations, derivatives and existing challenges and prospects of PHI are also reviewed and discussed in this paper, aiming to provide direction and rationale for the further development and clinical application of PHI.
连翘是临床上常用的一味中药，在治疗各种炎症相关性疾病方面应用广泛，素有“疮家圣药”之称。栀子苷（CHO，PHI）是从连翘中提取的木脂素成分，具有显著的生物活性。现代药理学研究证实，PHI 在治疗各种疾病方面具有显著的活性，包括炎症性疾病、肝脏疾病、癌症、细菌感染和病毒感染。因此，本综述通过检索 PubMed、Web of Science、Science Direct、CNKI 和 SciFinder 数据库，全面总结了截至 2023 年 6 月 PHI 的药理学作用。根据这些数据，PHI 显示出显著的抗炎、抗氧化、保肝、抗肿瘤、抗菌、抗病毒、免疫调节、镇痛、降压和血管舒张作用。更重要的是，NF-κB、MAPK、PI3K/AKT、P2X7R/NLRP3、Nrf2-ARE、JAK/STAT、Ca-calcineurin-TFEB、TGF-β/Smads、Notch1 和 AMPK/ERK/NF-κB 信号通路被认为是 PHI 发挥这些药理学作用的重要分子靶点。对其毒性和药代动力学特性的研究表明，PHI 毒性很低，体内不完全吸收，口服生物利用度低。此外，本文还综述和讨论了 PHI 的物理化学性质、新制剂、衍生物以及现有的挑战和前景，旨在为 PHI 的进一步开发和临床应用提供方向和依据。
