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Exploring the anticancer effects of brominated plastoquinone analogs with promising cytotoxic activity in MCF-7 breast cancer cells via cell cycle arrest and oxidative stress induction

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dc.contributor.authorYILMAZ GÖLER, AYŞE MİNE
dc.contributor.authorYILMAZ, BETÜL
dc.contributor.authorsJannuzzı A. T., Yılmaz Göler A. M., Bayrak N., Yıldız M., Yıldırım H., Yılmaz B., Shilkar D., Jayaprakash Venkatesan R., Jayaprakash V., Tuyun A. F.
dc.date.accessioned2023-07-10T13:05:04Z
dc.date.available2023-07-10T13:05:04Z
dc.date.issued2022-06-01
dc.description.abstractPlastoquinone analogs are privileged structures among the known antiproliferative natural product-based compound families. Exploiting one of these analogs as a lead structure, we report the investigation of the brominated PQ analogs (BrPQ) in collaboration with the National Cancer Institute of Bethesda within the Developmental Therapeutics Program (DTP). These analogs exhibited growth inhibition in the micromolar range across leukemia, non-small cell lung cancer (EKVX, HOP-92, and NCI-H522), colon cancer (HCT-116, HOP-92), melanoma (LOX IMVI), and ovarian cancer (OVCAR-4) cell lines. One brominated PQ analog (BrPQ5) was selected for a full panel five-dose in vitro assay by the NCI’s Development Therapeutic Program (DTP) division to determine GI50, TGI, and LC50parameters. The brominated PQ analog (BrPQ5) displayed remarkable activity against most tested cell lines, with GI50values ranging from 1.55 to 4.41 µM. The designed molecules (BrPQ analogs) obeyed drug-likeness rules, displayed a favorable predictive Absorption, Distribution, Metabolism, and Excretion (ADME) profile, and an in silico simulation predicted a possibleBrPQ5interaction with proteasome catalytic subunits. Furthermore, the in vitro cytotoxic activity ofBrPQ5was assessed, and IC50values for U-251 glioma, MCF-7 and MDA-MB-231 breast cancers, DU145 prostate cancer, HCT-116 colon cancer, and VHF93 fibroblast cell lines were evaluated using an MTT assay. MCF-7 was the most affected cell line, and the effects ofBrPQ5on cell proliferation, cell cycle, oxidative stress, apoptosis/necrosis induction, and proteasome activity were further investigated in MCF-7 cells. The in vitro assay results showed thatBrPQ5caused cytotoxicity in MCF-7 breast cancer cells via cell cycle arrest and oxidative stress induction. However,BrPQ5did not inhibit the catalytic activity of the proteasome. These results provide valuable insights for further discovery of novel antiproliferative agents.
dc.identifier.citationJannuzzı A. T., Yılmaz Göler A. M., Bayrak N., Yıldız M., Yıldırım H., Yılmaz B., Shilkar D., Jayaprakash Venkatesan R., Jayaprakash V., Tuyun A. F., "Exploring the Anticancer Effects of Brominated Plastoquinone Analogs with Promising Cytotoxic Activity in MCF-7 Breast Cancer Cells via Cell Cycle Arrest and Oxidative Stress Induction", Pharmaceuticals, cilt.15, ss.777-799, 2022
dc.identifier.doi10.3390/ph15070777
dc.identifier.endpage799
dc.identifier.issn1424-8247
dc.identifier.startpage777
dc.identifier.urihttps://avesis.marmara.edu.tr/api/publication/45912933-b863-4e41-90eb-479a8a3a09fa/file
dc.identifier.urihttps://hdl.handle.net/11424/291044
dc.identifier.volume15
dc.language.isoeng
dc.relation.ispartofPharmaceuticals
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectTıp
dc.subjectTemel Eczacılık Bilimleri
dc.subjectEczacılık
dc.subjectSağlık Bilimleri
dc.subjectTemel Tıp Bilimleri
dc.subjectMedicine
dc.subjectBasic Pharmaceutics Sciences
dc.subjectPharmacology and Therapeutics
dc.subjectHealth Sciences
dc.subjectFundamental Medical Sciences
dc.subjectKlinik Tıp (MED)
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectKlinik Tıp
dc.subjectFarmakoloji ve Toksikoloji
dc.subjectTIP, GENEL & DAHİLİ
dc.subjectFARMAKOLOJİ VE ECZACILIK
dc.subjectClinical Medicine (MED)
dc.subjectLife Sciences (LIFE)
dc.subjectCLINICAL MEDICINE
dc.subjectPHARMACOLOGY & TOXICOLOGY
dc.subjectMEDICINE, GENERAL & INTERNAL
dc.subjectPHARMACOLOGY & PHARMACY
dc.subjectGenel Sağlık Meslekleri
dc.subjectFarmakoloji
dc.subjectFarmakoloji, Toksikoloji ve Eczacılık (çeşitli)
dc.subjectGenel Farmakoloji, Toksikoloji ve Eczacılık
dc.subjectPatofizyoloji
dc.subjectTemel Bilgi ve Beceriler
dc.subjectDeğerlendirme ve Teşhis
dc.subjectFarmakoloji (tıbbi)
dc.subjectDahiliye
dc.subjectAile Sağlığı
dc.subjectİlaç Rehberleri
dc.subjectTıp (çeşitli)
dc.subjectGenel Tıp
dc.subjectYaşam Bilimleri
dc.subjectPharmacy
dc.subjectGeneral Health Professions
dc.subjectPharmacology
dc.subjectPharmacology, Toxicology and Pharmaceutics (miscellaneous)
dc.subjectGeneral Pharmacology, Toxicology and Pharmaceutics
dc.subjectPathophysiology
dc.subjectFundamentals and Skills
dc.subjectAssessment and Diagnosis
dc.subjectPharmacology (medical)
dc.subjectInternal Medicine
dc.subjectFamily Practice
dc.subjectDrug Guides
dc.subjectMedicine (miscellaneous)
dc.subjectGeneral Medicine
dc.subjectLife Sciences
dc.subjectquinone
dc.subjectplastoquinones
dc.subjectantiproliferative activity
dc.subjectcytotoxicity
dc.subjectcell cycle
dc.subjectoxidative stress
dc.subjectADME
dc.subjectDRUG DISCOVERY
dc.subjectPROTEASOME
dc.subjectDERIVATIVES
dc.subjectINSTITUTE
dc.titleExploring the anticancer effects of brominated plastoquinone analogs with promising cytotoxic activity in MCF-7 breast cancer cells via cell cycle arrest and oxidative stress induction
dc.typearticle
dc.type.subanimation
dspace.entity.typePublication
local.avesis.id45912933-b863-4e41-90eb-479a8a3a09fa
local.indexed.atWOS
local.indexed.atPUBMED
local.indexed.atSCOPUS
relation.isAuthorOfPublication8a72311b-9078-47c0-9fd8-bd73292b7739
relation.isAuthorOfPublication81633a07-e5fb-4760-b3ef-bf0878d87827
relation.isAuthorOfPublication.latestForDiscovery8a72311b-9078-47c0-9fd8-bd73292b7739

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