从贯叶连翘中提取物体外抗肝癌活性的化学成分分析及作用机制研究
Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
机构信息
Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, China; Cell Therapy & Cell Drugs of Luzhou Key Laboratory, Luzhou 646000, Sichuan, China; South Sichuan Institute of Translational Medicine, Luzhou 646600, Sichuan, China; The Key Laboratory for Human Disease Gene Study of Sichuan Province and Department of Laboratory Medicine, Sichuan Provincial People's Hospital, University of Electronic Science and Technology of China, Chengdu 610072, China; Research Unit for Blindness Prevention of Chinese Academy of Medical Science (2019RU026), Sichuan Academy of Medical Sciences, Chengdu 610072, China.
Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, China; Cell Therapy & Cell Drugs of Luzhou Key Laboratory, Luzhou 646000, Sichuan, China; South Sichuan Institute of Translational Medicine, Luzhou 646600, Sichuan, China.
出版信息
Biomed Pharmacother. 2023 Oct;166:115315. doi: 10.1016/j.biopha.2023.115315. Epub 2023 Aug 12.
Polygonum perfoliatum L. is an herbal medicine that has been extensively used in traditional Chinese medicine to treat various health conditions ranging from ancient internal to surgical and gynecological diseases. Numerous studies suggest that P. perfoliatum extract elicits significant anti-tumor, anti-inflammatory, anti-bacterial, and anti-viral effects. Nevertheless, the underlying mechanisms of its anti-liver cancer effects remain poorly understood. Our study suggests that P. perfoliatum stem extract (PPLA) has a favorable safety profile and exhibits a significant anti-liver cancer effect both in vitro and in vivo. We identified that PPLA activates the cGMP-PKG signaling pathway, and key regulatory genes including ADRA1B, PLCB2, PRKG2, CALML4, and GLO1 involved in this activation. Moreover, PPLA modulates the expression of genes responsible for the cell cycle. Additionally, we identified four constituents of PPLA, namely taxifolin, myricetin, eriodictyol, and pinocembrin, that plausibly act via the cGMP-PKG signaling pathway. Both in vitro and in vivo experiments confirmed that PPLA, along with its constituting compounds taxifolin, myricetin, and eriodictyol, exhibit potent anti-cancer activities and hold the promise of being developed into therapeutic agents.
翻白草（Polygonum perfoliatum L.）是一种草药，在中国传统医学中被广泛用于治疗各种健康状况，从古代内科到外科和妇科疾病。许多研究表明，翻白草提取物具有显著的抗肿瘤、抗炎、抗菌和抗病毒作用。然而，其抗肝癌作用的机制尚不清楚。我们的研究表明，翻白草茎提取物（PPLA）具有良好的安全性，并在体外和体内均表现出显著的抗肝癌作用。我们发现 PPLA 激活了 cGMP-PKG 信号通路，并且涉及该激活的关键调节基因包括 ADRA1B、PLCB2、PRKG2、CALML4 和 GLO1。此外，PPLA 调节了负责细胞周期的基因的表达。此外，我们鉴定出 PPLA 的四种成分，即杨梅素、槲皮素、圣草酚和松属素，它们可能通过 cGMP-PKG 信号通路发挥作用。体外和体内实验均证实，PPLA 及其组成化合物杨梅素、槲皮素和圣草酚具有很强的抗癌活性，有望开发成治疗药物。
Zotero 插件