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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Elsevier
2023-10-01
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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. |
first_indexed | 2024-03-12T01:10:37Z |
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institution | Directory Open Access Journal |
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language | English |
last_indexed | 2024-03-12T01:10:37Z |
publishDate | 2023-10-01 |
publisher | Elsevier |
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series | Biomedicine & Pharmacotherapy |
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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