School of Public Health, Shanxi Medical University, Taiyuan, Shanxi, China.
Department of Pharmacology, Shanxi Medical University, Shanxi, China.
Pharm Biol. 2022 Dec;60(1):9-16. doi: 10.1080/13880209.2021.2006723.
Farrerol, a typical natural flavanone isolated from the traditional Chinese herb 'Man-shan-hong' [ L. (Ericaceae)] with phlegm-reducing and cough-relieving properties, is widely used in China for treating bronchitis and asthma.
To present the anti-inflammatory, antioxidant, vasoactive, antitumor, and antimicrobial effects of farrerol and its underlying molecular mechanisms.
The literature was reviewed by searching PubMed, Medline, Web of Knowledge, Scopus, and Google Scholar databases between 2011 and May 2021. The following key words were used: 'farrerol,' 'flavanone,' 'anti-inflammatory,' 'antioxidant,' 'vasoactive,' 'antitumor,' 'antimicrobial,' and 'molecular mechanisms'.
Farrerol showed anti-inflammatory effects mainly mediated via the inhibition of interleukin (IL)-6/8, IL-1β, tumour necrosis factor(TNF)-α, NF-κB, NO, COX-2, JNK1/2, AKT, PI3K, ERK1/2, p38, Keap-1, and TGF-1β. Farrerol exhibited antioxidant effects by decreasing JNK, MDA, ROS, NOX4, Bax/Bcl-2, caspase-3, p-p38 MAPK, and GSK-3β levels and enhancing Nrf2, GSH, SOD, GSH-Px, HO-1, NQO1, and p-ERK levels. The vasoactive effects of farrerol were also shown by the reduced α-SMA, NAD(P)H, p-ERK, p-Akt, mTOR, Jak2, Stat3, Bcl-2, and p38 levels, but increased OPN, occludin, ZO-1, eNOS, CaM, IP3R, and PLC levels. The antitumor effects of farrerol were evident from the reduced Bcl-2, Slug, Zeb-1, and vimentin levels but increased p27, ERK1/2, p38, caspase-9, Bax, and E-cadherin levels. Farrerol reduced α-toxin levels and increased NO production and NF-κB activity to impart antibacterial activity.
This review article provides a theoretical basis for further studies on farrerol, with a view to develop and utilise farrerol for treating of vascular-related diseases in the future.
法乐醇是一种从传统中药“满山红”[L.（杜鹃花科）]中分离得到的典型类黄酮，具有祛痰止咳作用，在中国被广泛用于治疗支气管炎和哮喘。
介绍法乐醇的抗炎、抗氧化、血管活性、抗肿瘤和抗菌作用及其潜在的分子机制。
通过检索 PubMed、Medline、Web of Knowledge、Scopus 和 Google Scholar 数据库，在 2011 年至 2021 年 5 月期间，对文献进行综述。使用了以下关键词：“farrerol”、“flavanone”、“抗炎”、“抗氧化”、“血管活性”、“抗肿瘤”、“抗菌”和“分子机制”。
法乐醇主要通过抑制白细胞介素（IL）-6/8、IL-1β、肿瘤坏死因子（TNF）-α、NF-κB、NO、COX-2、JNK1/2、AKT、PI3K、ERK1/2、p38、Keap-1 和 TGF-1β，发挥抗炎作用。法乐醇通过降低 JNK、MDA、ROS、NOX4、Bax/Bcl-2、caspase-3、p-p38 MAPK 和 GSK-3β水平，增加 Nrf2、GSH、SOD、GSH-Px、HO-1、NQO1 和 p-ERK 水平，表现出抗氧化作用。法乐醇还通过降低α-SMA、NAD（P）H、p-ERK、p-Akt、mTOR、Jak2、Stat3、Bcl-2 和 p38 水平，但增加 OPN、occludin、ZO-1、eNOS、CaM、IP3R 和 PLC 水平，表现出血管活性作用。法乐醇通过降低 Bcl-2、Slug、Zeb-1 和 vimentin 水平，但增加 p27、ERK1/2、p38、caspase-9、Bax 和 E-cadherin 水平，表现出抗肿瘤作用。法乐醇降低α-毒素水平，增加 NO 产生和 NF-κB 活性，从而发挥抗菌作用。
本文综述了法乐醇的抗炎、抗氧化、血管活性、抗肿瘤和抗菌作用及其潜在的分子机制，为进一步研究法乐醇提供了理论依据，以期为今后治疗与血管相关的疾病开发和利用法乐醇提供参考。
