title: Isoquercitrin inhibits the progression of liver cancer in vivo and in vitro via the MAPK signalling pathway.
abstract: Liver cancer is a malignant tumour with high morbidity and fatality rates that is common worldwide. At present, the clinical approaches to treating primary liver cancer include partial hepatectomy, systemic or local chemotherapy, radiotherapy, radiofrequency ablative surgery and liver transplantation. However, all of these approaches have shortcomings, including poor prognosis and numerous side-effects. A large number of studies have proven that many effective ingredients in traditional Chinese medicine, particularly the flavonoid compounds extracted from plants, have achieved breakthroughs in terms of enhancing the effects and reducing the toxicity of chemotherapy and radiotherapy, preventing tumour metastasis and relapse after surgery, alleviating the clinical symptoms of advanced tumours, improving the quality of life of the patient with tumours and extending patient long‑term survival. The purpose of the present study was to investigate the impact of isoquercitrin, the flavonoid from Bidens bipinnata L. extract, on the progression of liver cancer and to achieve a deeper understanding of the biological characteristics of isoquercitrin's involvement in the progression of liver cancer. In the in vitro experiments, isoquercitrin was found to strongly inhibit the proliferation of human liver cancer cells, promote the apoptosis of human liver cancer cells, and block the cell cycle in the G1 phase. Isoquercitrin activated caspase-3, -8 and -9, inhibited the expression level of ERK and p38MAPK protein phosphorylation, and promoted the phosphorylation of JNK. Additionally, isoquercitrin reduced the expression level of PKC in human liver cancer cells. In the in vivo experiments, isoquercitrin was also found to significantly inhibit the growth of transplanted tumours in nude mice. The present study confirmed that isoquercitrin could inhibit the progression of human liver cancer in vivo and in vitro, and the molecular mechanism of isoquercitrin may be closely associated with the MAPK and PKC signalling pathways.
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Guihong
authors.initials: G
authors.lastname: Huang
authors.affiliation: Department of Hepatobiliary Surgery, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Bo
authors.initials: B
authors.lastname: Tang
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Kun
authors.initials: K
authors.lastname: Tang
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Dong
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Jungang
authors.initials: J
authors.lastname: Deng
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Luqin
authors.initials: L
authors.lastname: Liao
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Zengzhen
authors.initials: Z
authors.lastname: Liao
authors.affiliation: Department of Pharmacy, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Hua
authors.initials: H
authors.lastname: Yang
authors.affiliation: Department of Hepatobiliary Surgery, Guilin Medical University, Affiliated Hospital, Guilin, Guangxi 541001, P.R. China.
authors.forename: Songqing
authors.initials: S
authors.lastname: He
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3 / Q000096:biosynthesis; D053181:Caspase 8 / Q000096:biosynthesis; D053453:Caspase 9 / Q000096:biosynthesis; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018450:Disease Progression; D048049:Extracellular Signal-Regulated MAP Kinases / Q000096:biosynthesis; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D048031:JNK Mitogen-Activated Protein Kinases / Q000378:metabolism; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000517:prevention & control; D020935:MAP Kinase Signaling System / Q000187:drug effects*; D008297:Male; D008516:Medicine, Chinese Traditional; D051379:Mice; D008819:Mice, Nude; D010766:Phosphorylation; D011794:Quercetin / Q000031:analogs & derivatives* / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays; D048051:p38 Mitogen-Activated Protein Kinases / Q000096:biosynthesis / Q000378:metabolism
chemical_list: C016527:isoquercitrin; D011794:Quercetin; D048049:Extracellular Signal-Regulated MAP Kinases; D048031:JNK Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases; D053148:Caspase 3; D053181:Caspase 8; D053453:Caspase 9