卫矛(Polygonum perfoliatum L.) 是一种在中国传统医学中被广泛用于治疗从古代内科到外科和妇科疾病的草药。大量研究表明，卫矛提取物具有显著的抗肿瘤、抗炎、抗菌和抗病毒作用。然而，其抗肝癌作用的潜在机制尚不明确。我们的研究表明，卫矛茎提取物（PPLA）具有良好的安全性，并在体外和体内均显示出显著的抗肝癌作用。我们发现，PPLA激活cGMP-PKG信号通路，并激活了ADRA1B、PLCB2、PRKG2、CALML4和GLO1等关键调控基因。此外，PPLA调节了负责细胞周期的基因的表达。我们还鉴定了四种PPLA成分，即槲皮素、杨梅花素、鼠李糖苷和五糖苷酮，其通过cGMP-PKG信号通路发挥作用。体外和体内实验证实，PPLA及其成分槲皮素、杨梅花素和鼠李糖苷均具有强大的抗癌活性，并有望成为治疗药物的开发方向。版权所有© 2023 作者。由Elsevier Masson SAS出版。保留所有权利。

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.Copyright © 2023 The Authors. Published by Elsevier Masson SAS.. All rights reserved.