期刊
ACS OMEGA
卷 7, 期 18, 页码 15919-15928出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.2c01041
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资金
- Central University of Gujarat, Gandhinagar
- National Forensic Sciences University, Gandhinagar
- Department of Science and Technology (DST), New Delhi
- DST-SERB, New Delhi
- SERB, DST, New Delhi
- Council of Scientific and Industrial Research, New Delhi
In this study, poly(ethylene) glycol (PEG4000) conjugated chrysin nanoparticles were prepared to achieve tumor microenvironment-specific drug release. The conjugated nanoparticles showed better drug release profile and higher anticancer activity against human breast cancer cells.
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 1H 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.
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