Journal
FRONTIERS IN PHARMACOLOGY
Volume 12, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2021.755054
Keywords
hydroxyethyl starch; curcumin; hepatocellular carcinoma; apoptosis; autophagy; mitochondria
Categories
Funding
- Funds of Guiding Project for Science and Technology Department of Fujian Province [2020D014]
- Funds of Social Development Project for Bureau of Science and Technology of Fuzhou [2019-S-81]
- Funds of Joint Plan for Health Education of Fujian Province [WKJ2016-2-25]
- Natural Science Foundation of Fujian Province, China [2020J05109]
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The conjugation of CUR with HES to form HES-CUR NPs enhanced the solubility and drug loading efficiency of CUR. HES-CUR NPs exhibited a stronger antiproliferative effect and better apoptosis induction in HepG2 cells compared to CUR. The efficacy of HES-CUR NPs against HepG2 cells might be related to enhanced mitochondrial damage and autophagy induction.
It is well documented that curcumin (CUR), as a polyphenol molecule originated from turmeric, has many advantages such as antioxidative, anti-inflammatory, neuroprotective, and antitumor effects. However, because of its poor water solubility and low bioavailability, the biomedical applications of CUR are limited. So, in this study, we modified CUR with conjugation to a food-derived hydrophilic hydroxyethyl starch (HES) via an ester linkage to fabricate the amphiphilic conjugate HES-CUR prior to self-assembling into uniform nanoparticles (HES-CUR NPs). And, the results of the H-1 NMR spectra and FT-IR spectrum showed successful synthesis of HES-CUR NPs; moreover, the solubility and the drug loading efficiency of CUR were significantly increased. Next, we further explored the differences on the antitumor effects between HES-CUR NPs and CUR in HepG2 cells, and the results of the CCK8-assay and cell counting experiment showed that HES-CUR NPs exhibited a more significant antiproliferative effect than that of CUR in HepG2 cells. And HepG2 cells were more sensitive to apoptosis induced by HES-CUR NPs as evidenced by flow cytometry, increased cytochrome c level, and decreased full length caspase-3 and Bcl-2 protein expressions. Additionally, we found that the efficacy of HES-CUR NPs against HepG2 cells might be related to the enhanced degree of mitochondrial damage (decrease of the mitochondrial membrane potential and ATP) and autophagy (increased levels of Beclin-1 and LC3-II proteins). So, the findings in this study suggest that HES-CUR NPs have a great application potential in antitumor efficacy and play an important role in multiple signal pathways.
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