PMID- 33996996 OWN - NLM STAT- MEDLINE DCOM- 20210622 LR - 20220423 IS - 2314-6141 (Electronic) IS - 2314-6133 (Print) VI - 2021 DP - 2021 TI - Antiprostate Cancer Activity of Ineupatolide Isolated from Carpesium cernuum L. PG - 5515961 LID - 10.1155/2021/5515961 [doi] LID - 5515961 AB - OBJECTIVE: The aim of the study was to investigate the antiprostate cancer effects and mechanism of ineupatolide (T-21), a natural product isolated from the Compositae plant Carpesium cernuum L., on PC-3 human prostate cancer cells. METHODS: The effect of T-21 on the proliferation of PC-3 cells was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, cell migration, and invasion experiments; the morphology of cell apoptosis was observed by Hoechst-propidium iodide staining; the effects of T-21 on PC-3 cell apoptosis and the cell cycle were evaluated by flow cytometry; and the effect of T-21 on the expression levels of phosphorylated protein kinase B (p-AKT), AKT, X-linked inhibitor of apoptosis protein (xlAP), procaspase-3, and poly (ADP-ribose) polymerase (PARP) in PC-3 cells was measured by western blotting. RESULTS: T-21 significantly inhibited the proliferation of cells, and its half-maximal inhibitory concentrations at 12, 24, and 48 h were 38.46 +/- 1.01, 24.63 +/- 0.70, and 7.36 +/- 0.58 muM, respectively. T-21 may promote cell apoptosis in a concentration-dependent manner and block the cell cycle in the G2 and S phases. In addition, T-21 significantly reduced the protein expression levels of p-AKT, AKT, xlAP, procaspase-3, and PARP. CONCLUSION: T-21 exhibits antiproliferation effects on PC-3 cells by promoting apoptosis and arresting the cell cycle in the G2 and S phases. The possible mechanism underlying its potential therapeutic effects against prostate cancer is related to the AKT/xlAP pathway. CI - Copyright (c) 2021 Yuan-she Huang et al. FAU - Huang, Yuan-She AU - Huang YS AD - College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China. AD - Anshun College, Anshun Guizhou 561000, China. FAU - Mao, Jing-Xin AU - Mao JX AUID- ORCID: 0000-0002-2813-1702 AD - College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China. FAU - Zhang, Lai AU - Zhang L AD - Anshun College, Anshun Guizhou 561000, China. FAU - Guo, Hong-Wei AU - Guo HW AD - An Shun City People's Hospital, Anshun 561000, China. FAU - Yan, Chen AU - Yan C AUID- ORCID: 0000-0001-9563-5604 AD - An Shun City People's Hospital, Anshun 561000, China. FAU - Chen, Min AU - Chen M AUID- ORCID: 0000-0002-0140-4192 AD - College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China. LA - eng PT - Journal Article DEP - 20210429 PL - United States TA - Biomed Res Int JT - BioMed research international JID - 101600173 RN - 0 (Antineoplastic Agents, Phytogenic) RN - 0 (Phytochemicals) RN - 0 (X-Linked Inhibitor of Apoptosis Protein) RN - 0 (XIAP protein, human) RN - EC 2.7.11.1 (Proto-Oncogene Proteins c-akt) SB - IM MH - Antineoplastic Agents, Phytogenic/*pharmacology MH - Apoptosis/drug effects MH - Asteraceae/*chemistry MH - Cell Proliferation/drug effects MH - Humans MH - Male MH - PC-3 Cells MH - Phytochemicals/*pharmacology MH - Prostatic Neoplasms/*metabolism MH - Proto-Oncogene Proteins c-akt/metabolism MH - Signal Transduction/drug effects MH - X-Linked Inhibitor of Apoptosis Protein/metabolism PMC - PMC8105106 COIS- All authors declare that there are no commercial or associative interests that represent a conflict of interest in connection with the work submitted. EDAT- 2021/05/18 06:00 MHDA- 2021/06/23 06:00 PMCR- 2021/04/29 CRDT- 2021/05/17 06:17 PHST- 2021/02/16 00:00 [received] PHST- 2021/03/27 00:00 [revised] PHST- 2021/04/09 00:00 [accepted] PHST- 2021/05/17 06:17 [entrez] PHST- 2021/05/18 06:00 [pubmed] PHST- 2021/06/23 06:00 [medline] PHST- 2021/04/29 00:00 [pmc-release] AID - 10.1155/2021/5515961 [doi] PST - epublish SO - Biomed Res Int. 2021 Apr 29;2021:5515961. doi: 10.1155/2021/5515961. eCollection 2021.