Please use this identifier to cite or link to this item: https://dspace.ctu.edu.vn/jspui/handle/123456789/4565
Title: Flavokawain derivative Fls induced g2/M arrest and apoptosis on breast cancer McF-7 cell line
Authors: Ali, Norlaily Mohd
Huỳnh, Kỳ
Ho, Wan Yong
Tan, Sheau Wei
Zareen, Seema
Abu, Nadiah
Kamarul, Tunku
Ismail, Jamil Bin
Theen, Noorjahan Banu Ali
Ong, Han Kiat Alan
Lim, Kian Lam
Akhtar, M. Nadeem
Yeap, Swee Keong
Keywords: (E)-1-(2′-Hydroxy-4′,6′-dimethoxyphenyl)-3-(4-methylthio)phenyl)prop-2-ene-1- one (FLS)
MCF-7
G2/M arrest
Apoptosis
Cell cycle
PLK-1
p53
Caspase
Issue Date: 2016
Series/Report no.: Drug Design, Development and Therapy;10 .- p.1897–1907
Abstract: Known as naturally occurring biologically active compounds, flavokawain A and B are the leading chalcones that possess anticancer properties. Another flavokawain derivative, (E)-1-(2′-Hydroxy-4′,6′-dimethoxyphenyl)-3-(4-ethylthio)phenyl)prop-2-ene-1-one (FLS) was characterized with H-nuclear magnetic resonance, electron-impact mas spectrometry, infrared spectroscopy, and ultraviolet (¹H NMR, EI-MS, IR, and UV) spectroscopic Techniques. FLS cytotoxic efficacy against human cancer cells (MCF-7, MDA-MB-231, and MCF-10A) resulted in the reduction of IC₅₀ values in a time- and dose-dependent mode with high specificity on MCF-7 (IC₅₀ of 36 μM at 48 hours) against normal breast cell MCF-10A (no IC₅₀ detected up to 180 μM at 72 hours). Light, scanning electron, and fluorescent microscopic analysis of MCF-7 cells treated with 36 μM of FLS displayed cell shrinkage, apoptotic body, and DNA fragmentation. Additionally, induction of G2/M cell arrest within 24 hours and apoptosis at subsequent time points was discovered via flow cytometry analysis. The roles of PLK-1, Wee-1, and phosphorylation of CDC-2 in G2/M arrest and proapoptotic factors (Bax, caspase 9, and p53) in promotion of apoptosis of FLS against MCF-7 cells were discovered using fluorometric, quantitative real-time polymerase chain reaction, and Western blot analysis. Interestingly, the presence of SCH₃ (thiomethyl group) on ring B structure contributed to the selective cytotoxicity against MCF-7 cells compared to other chalcones, flavokawain A and B. Overall, our data suggest potential therapeutic value for flavokawain derivative FLS to be further developed as a new anticancer drug.
URI: http://dspace.ctu.edu.vn/jspui/handle/123456789/4565
Appears in Collections:Tạp chí quốc tế

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