TY - JOUR
T1 - Improving Anticancer Activity of Chrysin using Tumor Microenvironment pH-Responsive and Self-Assembled Nanoparticles
AU - Jangid, Ashok Kumar
AU - Solanki, Raghu
AU - Patel, Sunita
AU - Medicherla, Kanakaraju
AU - Pooja, Deep
AU - Kulhari, Hitesh
N1 - Publisher Copyright:
© 2022 The Authors. Published by American Chemical Society.
PY - 2022/5/10
Y1 - 2022/5/10
N2 - Chrysin is a natural bioactive compound with potential biological activities. However, unfavorable physicochemical properties of native chrysin make it difficult to achieve good therapeutic efficacies. In this study, poly(ethylene) glycol (PEG4000)-conjugated chrysin nanoparticles were prepared. The PEG4000 was conjugated to chrysin through cis-aconityl and succinoyl linkers to achieve tumor microenvironment-specific drug release from PEGylated nanoparticles. The conjugation of PEG and chrysin via succinoyl (PCNP-1) and cis-aconityl (PCNP-2) linkers was confirmed by the 1 H NMR and FTIR analysis. The nanoparticles were characterized by DLS, TEM, XRD, and DSC analysis. Comparatively, PCNP-2 showed a better drug release profile and higher anticancer activity against human breast cancer cells than chrysin or PCNP-1. The apoptosis studies and colony formation inhibition assay revealed that the PCNP-2 induced more apoptosis and more greatly controlled the growth of human breast cancer cells than pure chrysin. Thus, the use of PCNPs may help to overcome the issues of chrysin and could be a better therapeutic approach.
AB - Chrysin is a natural bioactive compound with potential biological activities. However, unfavorable physicochemical properties of native chrysin make it difficult to achieve good therapeutic efficacies. In this study, poly(ethylene) glycol (PEG4000)-conjugated chrysin nanoparticles were prepared. The PEG4000 was conjugated to chrysin through cis-aconityl and succinoyl linkers to achieve tumor microenvironment-specific drug release from PEGylated nanoparticles. The conjugation of PEG and chrysin via succinoyl (PCNP-1) and cis-aconityl (PCNP-2) linkers was confirmed by the 1 H NMR and FTIR analysis. The nanoparticles were characterized by DLS, TEM, XRD, and DSC analysis. Comparatively, PCNP-2 showed a better drug release profile and higher anticancer activity against human breast cancer cells than chrysin or PCNP-1. The apoptosis studies and colony formation inhibition assay revealed that the PCNP-2 induced more apoptosis and more greatly controlled the growth of human breast cancer cells than pure chrysin. Thus, the use of PCNPs may help to overcome the issues of chrysin and could be a better therapeutic approach.
UR - http://www.scopus.com/inward/record.url?scp=85129271405&partnerID=8YFLogxK
U2 - 10.1021/acsomega.2c01041
DO - 10.1021/acsomega.2c01041
M3 - Article
AN - SCOPUS:85129271405
SN - 2470-1343
VL - 7
SP - 15919
EP - 15928
JO - ACS Omega
JF - ACS Omega
IS - 18
ER -
