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Physico-chemical and Biological Evaluation of Flavonols: Fisetin, Quercetin and Kaempferol Alone and Incorporated in beta Cyclodextrins.
- Source :
-
Anti-cancer agents in medicinal chemistry [Anticancer Agents Med Chem] 2017; Vol. 17 (4), pp. 615-626. - Publication Year :
- 2017
-
Abstract
- Background: Fisetin,quercetin and kaempferol are among the important representatives of flavonols, biological active phytocomounds, with low water solubility.<br />Objective: To evaluate the antimicrobial effect, respectively the antiproliferative and pro apoptotic activity on the B164A5 murine melanoma cell line of pure flavonols and their beta cyclodextrins complexes.<br />Method: Incorporation of fisetin, quercetin and kaempferol in beta cyclodextrins was proved by scanning electron microscopy (SEM), differencial scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). Pure compounds and their complexes were tested for antiproliferative (MTT) and pro-apoptotic activity (Annexin V-PI) on the B164A5 murine melanoma cell line and for the antimicrobial properties (Disk Diffusion Method) on the selected strains.<br />Results: The phytocompounds presented in a different manner in vitro chemopreventive activity against B164A5 murine melanoma cell line and weak antimicrobial effect.<br />Conclusion: The three flavonols: fisetin, quercetin and kaempferol were successfully incorporated in beta-cyclodextrin (BCD) and hydroxylpropyl-beta-cyclodextrin (HPBCD). Incorporation in beta cyclodextrins had a mix effect on the biological activity conducing to decrease, increase or consistent effect compared to pure phytocompound, depending on the screened process and on the chosen combination.<br /> (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
- Subjects :
- Animals
Anti-Bacterial Agents chemistry
Anti-Bacterial Agents isolation & purification
Antineoplastic Agents chemistry
Antineoplastic Agents isolation & purification
Apoptosis drug effects
Bacteria drug effects
Cell Proliferation drug effects
Cell Survival drug effects
Chemistry, Physical
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Flavonoids chemistry
Flavonoids isolation & purification
Flavonols
Kaempferols chemistry
Kaempferols isolation & purification
Mice
Microbial Sensitivity Tests
Molecular Structure
Quercetin chemistry
Quercetin isolation & purification
Structure-Activity Relationship
Tumor Cells, Cultured
beta-Cyclodextrins chemistry
beta-Cyclodextrins isolation & purification
Anti-Bacterial Agents pharmacology
Antineoplastic Agents pharmacology
Flavonoids pharmacology
Kaempferols pharmacology
Quercetin pharmacology
beta-Cyclodextrins pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1875-5992
- Volume :
- 17
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Anti-cancer agents in medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27338298
- Full Text :
- https://doi.org/10.2174/1871520616666160621105306