Molecular Mechanism of Enhanced Anticancer Effect of Nanoparticle Formulated LY2835219 via p16-CDK46-pRb Pathway in Colorectal Carcinoma Cell Line
Joint Authors
Tang, Xu
Zeng, Bin
Gao, Jian-Kun
Liu, Han-Qiang
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-09-20
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
LY2835219 is a dual inhibitor to CDK4 and CDK6.
This study was to prepare LY2835219-loaded chitosan nanoparticles (CNP/LY) and LY2835219-loaded hyaluronic acid-conjugated chitosan nanoparticles (HACNP/LY) and revealed their anticancer effect and influence on p16-CDK4/6-pRb pathway against colon cell line.
The nanoparticle sizes of CNP/LY and HACNP/LY were approximately 195 ± 39.6 nm and 217 ± 31.1 nm, respectively.
The zeta potentials of CNP/LY and HACNP/LY were 37.3 ± 1.5 mV and 30.3 ± 2.2 mV, respectively.
And the preparation process showed considerable drug encapsulation efficiency and loading efficiency.
LY2835219, CNP/LY, and HACNP/LY inhibited HT29 cell proliferation with 0.68, 0.54, and 0.30 μM of IC50, respectively.
G1 phase was arrested by LY2835219 and its formulations.
Furthermore, inhibition of CDK4/6 by LY2835219 formulations induced CDK4, CDK6, cyclin D1, and pRb decrease and p16 increase at both protein and mRNA levels.
Overall, nanoparticle formulated LY2835219 could enhance the cytotoxicity and cell cycle arrest, and HACNP/LY strengthened the trend furtherly compared to CNP/LY.
It is the first time to demonstrate the anticancer effect and mechanism against HT29 by LY2835219 and its nanoparticles.
The drug and its nanoparticle formulations delay the cell growth and arrest cell cycle through p16-CDK4/6-pRb pathway, while the nanoparticle formulated LY2835219 could strengthen the process.
American Psychological Association (APA)
Tang, Xu& Zeng, Bin& Gao, Jian-Kun& Liu, Han-Qiang. 2016. Molecular Mechanism of Enhanced Anticancer Effect of Nanoparticle Formulated LY2835219 via p16-CDK46-pRb Pathway in Colorectal Carcinoma Cell Line. Journal of Nanomaterials،Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1109039
Modern Language Association (MLA)
Tang, Xu…[et al.]. Molecular Mechanism of Enhanced Anticancer Effect of Nanoparticle Formulated LY2835219 via p16-CDK46-pRb Pathway in Colorectal Carcinoma Cell Line. Journal of Nanomaterials No. 2016 (2016), pp.1-8.
https://search.emarefa.net/detail/BIM-1109039
American Medical Association (AMA)
Tang, Xu& Zeng, Bin& Gao, Jian-Kun& Liu, Han-Qiang. Molecular Mechanism of Enhanced Anticancer Effect of Nanoparticle Formulated LY2835219 via p16-CDK46-pRb Pathway in Colorectal Carcinoma Cell Line. Journal of Nanomaterials. 2016. Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1109039
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1109039