Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.

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,...

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Main Authors: Xiaolong Tang, Lin Liu, Yan Li, Siyu Hao, Yueshui Zhao, Xu Wu, Mingxing Li, Yu Chen, Shuai Deng, Shuang Gou, Dan Cai, Meijuan Chen, Xiaobing Li, Yuhong Sun, Li Gu, Wanping Li, Fang Wang, Zhuo Zhang, Lei Yao, Jing Shen, Zhangang Xiao, Fukuan Du
Format: Article
Language:English
Published: Elsevier 2023-10-01
Series:Biomedicine & Pharmacotherapy
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S075333222301106X
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author Xiaolong Tang
Lin Liu
Yan Li
Siyu Hao
Yueshui Zhao
Xu Wu
Mingxing Li
Yu Chen
Shuai Deng
Shuang Gou
Dan Cai
Meijuan Chen
Xiaobing Li
Yuhong Sun
Li Gu
Wanping Li
Fang Wang
Zhuo Zhang
Lei Yao
Jing Shen
Zhangang Xiao
Fukuan Du
author_facet Xiaolong Tang
Lin Liu
Yan Li
Siyu Hao
Yueshui Zhao
Xu Wu
Mingxing Li
Yu Chen
Shuai Deng
Shuang Gou
Dan Cai
Meijuan Chen
Xiaobing Li
Yuhong Sun
Li Gu
Wanping Li
Fang Wang
Zhuo Zhang
Lei Yao
Jing Shen
Zhangang Xiao
Fukuan Du
author_sort Xiaolong Tang
collection DOAJ
description 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.
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spelling doaj.art-495c5415ede94c0c95665f69fd10e0092023-09-14T04:52:37ZengElsevierBiomedicine & Pharmacotherapy0753-33222023-10-01166115315Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.Xiaolong Tang0Lin Liu1Yan Li2Siyu Hao3Yueshui Zhao4Xu Wu5Mingxing Li6Yu Chen7Shuai Deng8Shuang Gou9Dan Cai10Meijuan Chen11Xiaobing Li12Yuhong Sun13Li Gu14Wanping Li15Fang Wang16Zhuo Zhang17Lei Yao18Jing Shen19Zhangang Xiao20Fukuan Du21Laboratory 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, ChinaLaboratory 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, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, China; Public Center of Experimental Technology, Southwest Medical University, Luzhou 646000, Sichuan, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory 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, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaLaboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, ChinaThe 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, ChinaLaboratory 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; Corresponding authors at: Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, 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; Department of Oncology, Affiliated Hospital of Southwest Medical University, Luzhou 646600, Sichuan, China; Corresponding authors at: Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, 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; Corresponding authors at: Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou 646600, Sichuan, China.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.http://www.sciencedirect.com/science/article/pii/S075333222301106XPolygonum perfoliatum L.Hepatocellular carcinomaMolecular docking simulation
spellingShingle Xiaolong Tang
Lin Liu
Yan Li
Siyu Hao
Yueshui Zhao
Xu Wu
Mingxing Li
Yu Chen
Shuai Deng
Shuang Gou
Dan Cai
Meijuan Chen
Xiaobing Li
Yuhong Sun
Li Gu
Wanping Li
Fang Wang
Zhuo Zhang
Lei Yao
Jing Shen
Zhangang Xiao
Fukuan Du
Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
Biomedicine & Pharmacotherapy
Polygonum perfoliatum L.
Hepatocellular carcinoma
Molecular docking simulation
title Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
title_full Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
title_fullStr Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
title_full_unstemmed Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
title_short Chemical profiling and investigation of molecular mechanisms underlying anti-hepatocellular carcinoma activity of extracts from Polygonum perfoliatum L.
title_sort chemical profiling and investigation of molecular mechanisms underlying anti hepatocellular carcinoma activity of extracts from polygonum perfoliatum l
topic Polygonum perfoliatum L.
Hepatocellular carcinoma
Molecular docking simulation
url http://www.sciencedirect.com/science/article/pii/S075333222301106X
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