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The Anti-Angiogenic Effect of Cynara cardunculus L. subsp. cardunculus Waste Product
Anna Cacciola1, Valeria D'Angelo1, Federica De Gaetano1
1Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale F. Stagno d'Alcontres 31, 98166 Messina, Italy.
Insights
Wild cardoon leaf waste contains bioactive compounds that inhibit collagenase and angiogenesis. Complexing these compounds with cyclodextrin significantly enhances their biological activity, offering potential for health-promoting ingredients.
Area of Science:
- Pharmacology and Phytochemistry
- Biotechnology and Circular Economy
Background:
- Wild cardoon (Cynara cardunculus L.) is recognized for culinary uses and health benefits.
- Valorizing agricultural byproducts like wild cardoon leaf waste aligns with circular economy principles.
- Understanding its impact on angiogenesis and collagenase activity can identify new health-promoting ingredients.
Purpose of the Study:
- To analyze the chemical composition of wild cardoon leaf waste extract.
- To evaluate the extract's in vivo antiangiogenic and collagenase inhibitory activities.
- To investigate the effect of hydroxypropyl-β-cyclodextrin (HP-β-CD) complexation on these activities.
Main Methods:
- Phytochemical analysis to identify bioactive compounds (flavonoids, hydroxycinnamic acids, luteolin-7-O-rutinoside).
- In vivo studies using zebrafish embryos and chick chorioallantoic membrane assays for antiangiogenesis.
- Enzyme inhibition assays to assess collagenase activity, including IC50 determination.
- Molecular docking simulations to explore compound-collagenase interactions.
- Complexation with HP-β-CD to evaluate enhanced biological effects.
Main Results:
- The extract contains significant levels of flavonoids, hydroxycinnamic acids, and luteolin-7-O-rutinoside.
- Dose-dependent antiangiogenic effects were observed in vivo.
- The extract demonstrated collagenase inhibitory activity comparable to a standard inhibitor.
- Complexation with HP-β-CD enhanced antiangiogenic effects and increased collagenase inhibition by 4.5-fold.
- Molecular docking provided insights into the interaction mechanisms of key compounds with collagenase.
Conclusions:
- Wild cardoon leaves are a rich source of bioactive compounds with therapeutic potential.
- Complexation with cyclodextrins significantly boosts the biological activity of wild cardoon leaf extract.
- This research supports the valorization of wild cardoon leaf waste as a source for health-promoting ingredients.
Abstract:
Cynara cardunculus L. subsp. cardunculus (Cynara cardunculus L. var. sylvestris (Lam.) Fiori), the wild cardoon, is known for its culinary applications and potential health benefits. Due to this, and given the growing interest in circular economies, deepening our under-standing of the effects of wild cardoon leaf waste on angiogenesis and collagenase activity represents a valuable opportunity to valorise agricultural byproducts as health-promoting ingredients. In this study, the waste product of wild cardoon leaves was extracted to examine its chemical composition and biological activities. Analytical techniques identified several bioactive compounds, including flavonoids, hydroxycinnamic acids such as dicaffeoyl-succinoylquinic acids, and luteolin-7-O-rutinoside. In vivo tests in zebrafish embryos and the chick chorioallantoic membrane demonstrated dose-dependent antiangiogenic effects, particularly enhanced by the complexation with hydroxypropyl-β-cyclodextrin (HP-β-CD). Considering the link between angiogenesis and collagenase, the potential effects of the extract on collagenase activity was investigated. The extract alone inhibited collagenase with an IC50 value comparable to that of the standard inhibitor while its complexed form exhibited a 4.5-fold greater inhibitory activity. A molecular docking study examined the interaction between the main compounds and collagenase. In conclusion, wild cardoon leaves can represent a valuable source of bioactive compounds. This study demonstrated that the complexation of the extract with cyclodextrin determines an increase in its biological activity.
