ArticleCancer medicine2020
Antitumor activity of celastrol by inhibition of proliferation, invasion, and migration in cholangiocarcinoma via PTEN/PI3K/Akt pathway.
Article in Cancer medicine, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 43 citations in OpenAlex.
- In Silico Perturbation Identifies Transcription Factors as Protective Targets in HSPCs After Irradiation.International journal of molecular sciences · 2026Article
- An Exosome-Liposome Hybrid Platform for Celastrol Delivery Enhances Anti-Tumor Efficacy in Hepatocellular Carcinoma.Current topics in medicinal chemistry · 2026Article
- Anti-neoplastic activity of celastrol in experimentally-induced mammary adenocarcinoma in mice: targeting wnt/β-catenin signaling pathway.Naunyn-Schmiedeberg's archives of pharmacology · 2025Article
- Research Progress of Chinese Medicine Monomers in Treatment of Cholangiocarcinoma.Chinese journal of integrative medicine · 2025Review
- Current Insights into Therapeutic Potential of Terpenoids as Anticancer Agents.Anti-cancer agents in medicinal chemistry · 2025Review
- Degradation-Based Protein Profiling: A Case Study of Celastrol.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Iodine-125 seed inhibits proliferation and promotes apoptosis of cholangiocarcinoma cells by inducing the ROS/p53 axis.Functional & integrative genomics · 2024Article
- The Role of the PTEN Tumor Suppressor Gene and Its Anti-Angiogenic Activity in Melanoma and Other Cancers.Molecules (Basel, Switzerland) · 2024Review
- Celastrol suppresses human pancreatic cancer via mDiscover oncology · 2023Article
- The Nexus of Inflammation-Induced Epithelial-Mesenchymal Transition and Lung Cancer Progression: A Roadmap to Pentacyclic Triterpenoid-Based Therapies.International journal of molecular sciences · 2023Review
- Identification of immune related gene signature for predicting prognosis of cholangiocarcinoma patients.Frontiers in immunology · 2023Article
- Rintatolimod: a potential treatment in patients with pancreatic cancer expressing Toll-like receptor 3.American journal of cancer research · 2023Article
- Paracrine Interaction of Cholangiocellular Carcinoma with Cancer-Associated Fibroblasts and Schwann Cells Impact Cell Migration.Journal of clinical medicine · 2022Article
- BCL2L1 is identified as a target of naringenin in regulating ovarian cancer progression.Molecular and cellular biochemistry · 2022Article
- Research Progress on the Regulation Mechanism of Key Signal Pathways Affecting the Prognosis of Glioma.Frontiers in molecular neuroscience · 2022Review
- Article
- [Preliminary study on the effect of B7H3 interaction with fibronectin on apoptosis of human chronic myeloid leukemia cells].Zhonghua xue ye xue za zhi = Zhonghua xueyexue zazhi · 2021Article
- Actionability evaluation of biliary tract cancer by genome transcriptome analysis and Asian cancer knowledgebase.Oncotarget · 2021Article
- miR‑224‑5p regulates the proliferation, migration and invasion of pancreatic mucinous cystadenocarcinoma by targetingMolecular medicine reports · 2021Article
- Celastrol Inhibits Canine Mammary Tumor Cells by Inducing ApoptosisFrontiers in veterinary science · 2021Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimCholangiocarcinoma is a malignant tumor originating from bile duct epithelium. Currently, the treatment strategy is very limited and the prognosis is poor. Recent studies reported celastrol exhibits antigrowth and antimetastasis properties in many tumors. Our study aimed to assess the anti-CCA effects of cholangiocarcinoma (CCA) and the mechanisms involved in it.
methodsIn this study, the long-term and short-term antiproliferation effects was determined using colony formation and Cell Counting Kit-8 (CCK-8) assays, respectively. Flow cytometry was performed to quantify apoptosis. Furthermore, wound healing and transwell assays were performed to determine the cell migration and invasion capabilities, respectively. To further find the mechanism involved in the celastrol-induced biological functions, LY204002, a PI3K/Akt signaling inhibitor, and an Akt-1 overexpression plasmid were employed to find whether PI3K/Akt pathway was involved in the celastrol-induced CCA cell inhibition. Additionally, short interfering RNA (siRNA) was also used to investigate the mechanism involved in the celastrol-induced PI3K/Akt signaling inhibition. Western blotting and immunofluorescence assays were also performed to detect the degree of relative proteins. Moreover, we validated the antiproliferation and antimetastasis effects of celastrol in vivo by constructing subcutaneous and lung metastasis nude mice models.
resultsWe discovered that celastrol effectively induced apoptotic cell death and inhibited the capacity of migration and invasion in CCA cells. Further mechanistic study identified that celastrol regulated the PI3K/Akt signaling pathway, and the antitumor efficacy was likely due to the upregulation of PTEN, a negative regulator of PI3K/Akt. Blockage of PTEN abolished the celastrol-induced PI3K/Akt signaling inhibition. Additionally, in vivo experiments conformed celastrol inhibited the tumor growth and lung metastasis with no serious side effects.
conclusionsOverall, our study elucidated a mechanistic framework for the anti-CCA effects of celastrol via PTEN/PI3K/Akt pathway.
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