Molecular Pro-Apoptotic Activities of Flavanone Derivatives in Cyclodextrin Complexes: New Implications for Anticancer Therapy

This study evaluates the antiproliferative potential of flavanones, chromanones and their spiro-1-pyrazoline derivatives as well as their inclusion complexes. The main goal was to determine the biological basis of molecular pro-apoptotic activities and the participation of reactive oxygen species (R...

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Bibliographic Details
Published in:International journal of molecular sciences 2024-08, Vol.25 (15), p.8488
Main Authors: Adamus-Grabicka, Angelika A, Hikisz, Pawel, Stepniak, Artur, Malecka, Magdalena, Paneth, Piotr, Sikora, Joanna, Budzisz, Elzbieta
Format: Article
Language:English
Subjects:
anticancer properties
Antimitotic agents
Antineoplastic agents
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Apoptosis - drug effects
Bioavailability
biocompatibility
Biological activity
Blood
Breast cancer
Cancer
Cancer therapies
Care and treatment
Cell Line, Tumor
Cell Proliferation - drug effects
crystal structure
cyclodextrines
Cyclodextrins - chemistry
Cyclodextrins - pharmacology
Cytotoxicity
docking studies
Drugs
Estrogens
Flavanones - chemistry
Flavanones - pharmacology
flavonoid derivatives
Hemolysis - drug effects
Humans
Hydrocarbons
Medical examination
Membrane Potential, Mitochondrial - drug effects
Metabolism
Nitrogen
Photographic industry
Reactive oxygen species
Reactive Oxygen Species - metabolism
Thrombin
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Summary:This study evaluates the antiproliferative potential of flavanones, chromanones and their spiro-1-pyrazoline derivatives as well as their inclusion complexes. The main goal was to determine the biological basis of molecular pro-apoptotic activities and the participation of reactive oxygen species (ROS) in shaping the cytotoxic properties of the tested conjugates. For this purpose, changes in mitochondrial potential and the necrotic/apoptotic cell fraction were analyzed. Testing with specific fluorescent probes found that ROS generation had a significant contribution to the biological anticancer activity of complexes of flavanone analogues. TT (thrombin time), PT (prothrombin time) and APTT (activated partial tromboplastin time) were used to evaluate the influence of the compounds on the extrinsic and intrinsic coagulation pathway. Hemolysis assays and microscopy studies were conducted to determine the effect of the compounds on RBCs.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms25158488