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2000
Volume 21, Issue 5
  • ISSN: 1573-4072
  • E-ISSN: 1875-6646

Abstract

Casticin is a flavonoid that is derived from the Vitex species. Multiple studies have investigated the anticancer properties of casticin against many types of cancer, such as bladder cancer, breast cancer, oral cancer, lung cancer, and leukemia. Research has shown the ability of casticin to inhibit cell growth and induce programmed cell death. The chemical exhibits efficacy against numerous cancer cell lines through various molecular mechanisms. The substance hinders the processes of invasion, migration, and proliferation and triggers programmed cell death by multiple mechanisms, including the generation of reactive oxygen species and the dependence on mitochondria. Additionally, it inhibits the cell cycle at different stages. These effects are achieved by modulating several signaling cascades, specifically NF-κB, PI3K/Akt, FOXO3a/FoxM1, and STAT3. This review provides a concise overview of the chemotherapeutic efficacy of casticin as an anticancer drug.

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2024-08-23
2025-09-28

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References

  1. RamchandaniS. NazI. LeeJ.H. KhanM.R. AhnK.S. An overview of the potential antineoplastic effects of casticin.Molecules2020256128710.3390/molecules25061287 32178324
     [Google Scholar]
  2. GanapatyS. VidyadharK.N. Phytoconstituents and biological activities of Vitex-a review.J. Nat. Rem.200520057595
     [Google Scholar]
  3. ChanE.W. BabaS. ChanH.T. KainumaM. TangahJ. Medicinal plants of sandy shores: A short review on Vitex trifolia L. and Ipomoea pes-caprae (L.) R.Br. Indian J. Nat. Prod. Resour.201672107115
     [Google Scholar]
  4. LeeJ.H. KimC. UmJ.Y. SethiG. AhnK.S. Casticin-induced inhibition of cell growth and survival are mediated through the dual modulation of Akt/mTOR signaling cascade.Cancers (Basel)201911225410.3390/cancers11020254 30813295
     [Google Scholar]
  5. ChanE.W.C. WongS.K. ChanH.T. Casticin from Vitex species: a short review on its anticancer and anti-inflammatory properties.J. Integr. Med.201816314715210.1016/j.joim.2018.03.001 29559215
     [Google Scholar]
  6. HuY. XinH.L. ZhangQ.Y. ZhengH.C. RahmanK. QinL.P. Anti-nociceptive and anti-hyperprolactinemia activities of Fructus viticis and its effective fractions and chemical constituents.Phytomedicine2007141066867410.1016/j.phymed.2007.01.008 17350238
     [Google Scholar]
  7. RasulA. ZhaoB.J. LiuJ. LiuB. SunJ.X. LiJ. LiX.M. Molecular mechanisms of casticin action: an update on its antitumor functions.Asian Pac. J. Cancer Prev.201415219049905810.7314/APJCP.2014.15.21.9049 25422178
     [Google Scholar]
  8. ChouG.L. PengS.F. LiaoC.L. HoH.C. LuK.W. LienJ.C. FanM.J. LaK.C. ChungJ.G. Casticin impairs cell growth and induces cell apoptosis via cell cycle arrest in human oral cancer SCC ‐4 cells.Environ. Toxicol.201833212714110.1002/tox.22497 29098808
     [Google Scholar]
  9. Cowppli-BonyA. ColonnaM. LigierK. JoosteV. DefossezG. MonnereauA. Descriptive epidemiology of cancer in metropolitan France: Incidence, survival and prevalence.Bull. Cancer20191067-861763410.1016/j.bulcan.2018.11.016 30833045
     [Google Scholar]
  10. HaïdaraK. ZamirL. ShiQ.W. BatistG. The flavonoid Casticin has multiple mechanisms of tumor cytotoxicity action.Cancer Lett.2006242218019010.1016/j.canlet.2005.11.017 16387422
     [Google Scholar]
  11. KohD. AhnH. ChungH.S. LeeH. KimY. LeeJ. KimD. HongM. ShinM. BaeH. Inhibitory effects of casticin on migration of eosinophil and expression of chemokines and adhesion molecules in A549 lung epithelial cells via NF-κB inactivation.J. Ethnopharmacol.2011136339940510.1016/j.jep.2011.01.014 21251967
     [Google Scholar]
  12. WangC. ZengL. ZhangT. LiuJ. WangW. Casticin inhibits lipopolysaccharide-induced acute lung injury in mice.Eur. J. Pharmacol.201678917217810.1016/j.ejphar.2016.07.035 27450485
     [Google Scholar]
  13. Lee HyeonHoon LH. Casticin, an active compound isolated from Vitex fructus, ameliorates the cigarette smoke-induced acute lung inflammatory response in a murine model.Int. Immunopharmacol.201528210971101
     [Google Scholar]
  14. FitzmauriceC. AllenC. BarberR.M. BarregardL. BhuttaZ.A. BrennerH. DickerD.J. Chimed-OrchirO. DandonaR. DandonaL. FlemingT. Global, regional, and national cancer incidence, mortality, years of life lost, years lived with disability, and disability-adjusted life-years for 32 cancer groups, 1990 to 2015: a systematic analysis for the global burden of disease study.JAMA Oncol.20173452454810.1001/jamaoncol.2016.5688 27918777
     [Google Scholar]
  15. KyriakopoulosC.E. ChenY.H. CarducciM.A. LiuG. JarrardD.F. HahnN.M. ShevrinD.H. DreicerR. HussainM. EisenbergerM. KohliM. PlimackE.R. VogelzangN.J. PicusJ. CooneyM.M. GarciaJ.A. DiPaolaR.S. SweeneyC.J. Chemohormonal therapy in metastatic hormone-sensitive prostate cancer: long-term survival analysis of the randomized phase III E3805 CHAARTED trial.J. Clin. Oncol.201836111080108710.1200/JCO.2017.75.3657 29384722
     [Google Scholar]
  16. HarrisW.P. MostaghelE.A. NelsonP.S. MontgomeryB. Androgen deprivation therapy: progress in understanding mechanisms of resistance and optimizing androgen depletion.Nat. Clin. Pract. Urol.200962768510.1038/ncpuro1296 19198621
     [Google Scholar]
  17. KarantanosT. CornP.G. ThompsonT.C. Prostate cancer progression after androgen deprivation therapy: mechanisms of castrate resistance and novel therapeutic approaches.Oncogene201332495501551110.1038/onc.2013.206 23752182
     [Google Scholar]
  18. SmaletzO. ScherH.I. Outcome predictions for patients with metastatic prostate cancer.Semin. Urol. Oncol.200220215516310.1053/suro.2002.32938
     [Google Scholar]
  19. LinC.C. ChenK.B. TsaiC.H. TsaiF.J. HuangC.Y. TangC.H. YangJ.S. HsuY.M. PengS.F. ChungJ.G. Casticin inhibits human prostate cancer DU 145 cell migration and invasion via Ras/Akt/NF‐κB signaling pathways.J. Food Biochem.2019437e1290210.1111/jfbc.12902 31353708
     [Google Scholar]
  20. HuangC. ChengY.D. HuangL.H. HsiaoY.T. PengS.F. LuK.W. LienJ.C. YangJ.L. LinT.S. ChungJ.G. Casticin induces DNA damage and impairs DNA repair in human bladder cancer TSGH-8301 cells.Anticancer Res.20193941839184710.21873/anticanres.13291 30952724
     [Google Scholar]
  21. QiaoZ. ChengY. LiuS. MaZ. LiS. ZhangW. Casticin inhibits esophageal cancer cell proliferation and promotes apoptosis by regulating mitochondrial apoptotic and JNK signaling pathways.Naunyn Schmiedebergs Arch. Pharmacol.2019392217718710.1007/s00210‑018‑1574‑5 30448926
     [Google Scholar]
  22. KalavrezosN. ScullyC. Mouth cancer for clinicians part 2: epidemiology.Dent. Update201542435435910.12968/denu.2015.42.4.354 26062260
     [Google Scholar]
  23. KimH. YiJ.M. KimN.S. LeeY.J. KimJ. OhD.S. OhS.M. BangO.S. LeeJ. Cytotoxic compounds from the fruits of Vitex rotundifolia against human cancer cell lines.J. Korean Soc. Appl. Biol. Chem.201255343343710.1007/s13765‑012‑2027‑3
     [Google Scholar]
  24. LiW.X. CuiC.B. CaiB. WangH.Y. YaoX.S. Flavonoids from Vitex trifolia L. inhibit cell cycle progression at G2/M phase and induce apoptosis in mammalian cancer cells.J. Asian Nat. Prod. Res.20057461562610.1080/10286020310001625085 16087636
     [Google Scholar]
  25. LiY.J. GuoY. YangQ. WengX.G. YangL. WangY.J. ChenY. ZhangD. LiQ. LiuX.C. KanX.X. ChenX. ZhuX.X. KmoníèkováE. ZídekZ. Flavonoids casticin and chrysosplenol D from Artemisia annua L. inhibit inflammation in vitro and in vivo.Toxicol. Appl. Pharmacol.2015286315115810.1016/j.taap.2015.04.005 25891417
     [Google Scholar]
  26. FanL. ZhangY. ZhouQ. LiuY. GongB. LüJ. ZhuH. ZhuG. XuY. HuangG. Casticin inhibits breast cancer cell migration and invasion by down-regulation of PI3K/Akt signaling pathway.Biosci. Rep.2018386BSR2018073810.1042/BSR20180738 30401729
     [Google Scholar]
  27. ShangH.S. ChenK.W. ChouJ.S. PengS.F. ChenY.L. ChenP.Y. HuangH.C. LuH.F. ChangH.Y. ShihY.L. HuangW.W. Casticin inhibits in vivo growth of xenograft tumors of human oral cancer SCC-4 cells in vivo.In Vivo20203452461246710.21873/invivo.12061 32871773
     [Google Scholar]
  28. WuZ.Y. LienJ.C. HuangY.P. LiaoC.L. LinJ.J. FanM.J. KoY.C. HsiaoY.P. LuH.F. ChungJ.G. Casticin inhibits A375. S2 human melanoma cell migration/invasion through downregulating NF-κB and matrix metalloproteinase-2 and-1.Molecules201621338410.3390/molecules21030384 27007357
     [Google Scholar]
  29. LiuE. KuangY. HeW. XingX. GuJ. Casticin induces human glioma cell death through apoptosis and mitotic arrest.Cell. Physiol. Biochem.201331680581410.1159/000350098 23816816
     [Google Scholar]
  30. SongX. ZhangY. WangX. ZhangW. WangZ. ZhangF. ZhangY. LuJ. MeiJ. HuY. ChenL. LiH. YeY. LiuY. GuJ. Casticin induces apoptosis and G0/G1 cell cycle arrest in gallbladder cancer cells.Cancer Cell Int.2017171910.1186/s12935‑016‑0377‑3 28070171
     [Google Scholar]
  31. XieY. ZhongL. DuanD. LiT. Casticin inhibits invasion and proliferation via downregulation of β‐catenin and reversion of EMT in oral squamous cell carcinoma.J. Oral Pathol. Med.2019481089790510.1111/jop.12930 31318467
     [Google Scholar]
  32. GongQ. CaoX. CaoJ. YangX. ZengW. Casticin suppresses the carcinogenesis of small cell lung cancer H446 cells through activation of AMPK/FoxO3a signaling.Oncol. Rep.20184031401141010.3892/or.2018.6547 30015975
     [Google Scholar]
  33. YangJ. YangY. TianL. ShengX.F. LiuF. CaoJ.G. Casticin-induced apoptosis involves death receptor 5 upregulation in hepatocellular carcinoma cells.World J. Gastroenterol.201117384298430710.3748/wjg.v17.i38.4298 22090786
     [Google Scholar]
  34. MaJ. YinG. LuZ. XieP. ZhouH. LiuJ. YuL. Casticin prevents DSS induced ulcerative colitis in mice through inhibitions of NF‐κB pathway and ROS signaling.Phytother. Res.20183291770178310.1002/ptr.6108 29876982
     [Google Scholar]
  35. JiangC. ShiR. ChenB. YanX. TangG. Casticin elicits inflammasome-induced pyroptosis through activating PKR/JNK/] NF-κB signal in 5-8F cells.Biomed. Pharmacother.202012310957610.1016/j.biopha.2019.109576 31951974
     [Google Scholar]
  36. AyanI.C. ÇetinkayaS. DursunH.G. GüneşC.E. ŞirinS. Anticancer effect and phytochemical profile of the extract from achillea ketenoglui against human colorectal cancer cell lines. Anti-Cancer Agent.Med. Chem.20222291769177910.2174/1871520621666210908110422
     [Google Scholar]
  37. FuC. ZhangK. WangM. QiuF. Casticin and chrysosplenol D from Artemisia annua L. induce apoptosis by inhibiting topoisomerase IIα in human non-small-cell lung cancer cells.Phytomedicine202210015409510.1016/j.phymed.2022.154095 35398735
     [Google Scholar]
  38. XuH. ShiH.L. HaoJ.W. ShuK.P. ZhangY.T. HouT.Q. Casticin inhibits the proliferation, migration and invasion of bladder cancer cells by inhibition of TM7SF4 expression.Zhonghua Zhong Liu Za Zhi2022444334340 35448921
     [Google Scholar]
  39. LiuL.P. CaoX.C. LiuF. QuanM.F. ShengX.F. RenK.Q. Casticin induces breast cancer cell apoptosis by inhibiting the expression of forkhead box protein M1.Oncol. Lett.2014751711171710.3892/ol.2014.1911 24765206
     [Google Scholar]
  40. YangF. HeK. HuangL. ZhangL. LiuA. ZhangJ. Casticin inhibits the activity of transcription factor Sp1 and the methylation of RECK in MGC803 gastric cancer cells.Exp. Ther. Med.201713274575010.3892/etm.2016.4003 28352361
     [Google Scholar]
  41. HeG. CaoX. HeM. ShengX. WuY. AiX. Casticin inhibits self-renewal of liver cancer stem cells from the MHCC97 cell line.Oncol. Lett.2014762023202810.3892/ol.2014.1972 24932283
     [Google Scholar]
  42. HeL. YangX. CaoX. LiuF. QuanM. CaoJ. Casticin induces growth suppression and cell cycle arrest through activation of FOXO3a in hepatocellular carcinoma.Oncol. Rep.201329110310810.3892/or.2012.2076 23064420
     [Google Scholar]
  43. ZhouY. TianL. LongL. QuanM. LiuF. CaoJ. Casticin potentiates TRAIL-induced apoptosis of gastric cancer cells through endoplasmic reticulum stress.PLoS One201383e5885510.1371/journal.pone.0058855 23536831
     [Google Scholar]
/content/journals/cbc/10.2174/0115734072330991240819103258
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Casticin: A Short Review on its Pharmacological Activity as an Anticancer Drug
Curr. Bioact. Compd. 21, E15734072330991 (2025); https://doi.org/10.2174/0115734072330991240819103258
/content/journals/cbc/10.2174/0115734072330991240819103258
/content/journals/cbc/10.2174/0115734072330991240819103258
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  • Article Type:     Review Article
Keyword(s): Apoptosis; cancer; casticin; flavonoid; MAPK signaling; vitex species

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