Improved anticancer activity of betulinic acid on breast cancer through a grafted copolymer-based micelles system.
Animals
Animals, Outbred Strains
Antineoplastic Agents
/ administration & dosage
Breast Neoplasms
/ pathology
Cell Line, Tumor
Chemistry, Pharmaceutical
/ methods
Chickens
Drug Carriers
/ chemistry
Human Umbilical Vein Endothelial Cells
Humans
Hypoxia-Inducible Factor 1
/ drug effects
Membrane Potential, Mitochondrial
/ drug effects
Mice
Micelles
Neovascularization, Pathologic
/ metabolism
Pentacyclic Triterpenes
/ administration & dosage
Polyethylene Glycols
/ chemistry
Polyvinyls
/ chemistry
Reactive Oxygen Species
/ metabolism
Signal Transduction
/ drug effects
Surface Properties
Vascular Endothelial Growth Factor A
/ drug effects
Betulinic Acid
Betulinic acid
DNA damage
Soluplus
angiogenesis
breast cancer
Journal
Drug delivery
ISSN: 1521-0464
Titre abrégé: Drug Deliv
Pays: England
ID NLM: 9417471
Informations de publication
Date de publication:
Dec 2021
Dec 2021
Historique:
entrez:
27
9
2021
pubmed:
28
9
2021
medline:
15
1
2022
Statut:
ppublish
Résumé
Betulinic acid (3β-Hydroxy-20(29)-lupaene-28-oic acid, BA) has excellent anti-cancer activity but poor solubility and low bioavailability. To improve the antitumor activity of BA, a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer (Soluplus) encapsulated BA micelle (Soluplus-BA) was fabricated. The Soluplus-BA micelles presented a mean size of 54.77 ± 1.26 nm and a polydispersity index (PDI) of 0.083. The MTT assay results showed that Soluplus-BA micelles increased the inhibitory effect of BA on MDA-MB-231 cells, mainly due to the enhanced accumulation of reactive oxygen species (ROS) and the destruction of mitochondrial membrane potential (MMP). Soluplus-BA micelles induced the DNA double-strand breaks (DSBs) as the γH2AX foci increased. Moreover, Soluplus-BA also inhibited the tube formation and migration of human umbilical vein endothelial cells (HUVECs), and inhibited the neovascularization of the chicken chorioallantoic membrane (CAM). This angiogenesis inhibitory effect may be accomplished by regulating the HIF-1/VEGF-FAK signaling pathway. The
Identifiants
pubmed: 34565273
doi: 10.1080/10717544.2021.1979125
pmc: PMC8475105
doi:
Substances chimiques
Antineoplastic Agents
0
Drug Carriers
0
Hypoxia-Inducible Factor 1
0
Micelles
0
Pentacyclic Triterpenes
0
Polyvinyls
0
Reactive Oxygen Species
0
Vascular Endothelial Growth Factor A
0
polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer
0
Polyethylene Glycols
3WJQ0SDW1A
Betulinic Acid
4G6A18707N
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1962-1971Références
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