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Drug Res (Stuttg) 2018; 68(03): 132-138
DOI: 10.1055/s-0043-120662
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Anti-degenerative effect of Apigenin, Luteolin and Quercetin on human keratinocyte and chondrocyte cultures: SAR evaluation

Lucia Crascì
1   Department of Drug Sciences, University of Catania, Viale A. Doria, Catania, Italy
,
Venera Cardile
2   Department of Biomedical and Biotechnological Sciences, Section of Physiology, University of Catania, Catania, Italy
,
Giusy Longhitano
1   Department of Drug Sciences, University of Catania, Viale A. Doria, Catania, Italy
,
Francesco Nanfitò
3   Department of Medical and Surgery Specialties, Section of Plastic Surgery, Cannizzaro Hospital, Catania, Italy
,
Annamaria Panico
1   Department of Drug Sciences, University of Catania, Viale A. Doria, Catania, Italy
› Author Affiliations
Further Information

Publication History

received 27 July 2017

accepted 02 October 2017

Publication Date:
06 November 2017 (online)

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Abstract

Background Inflammation is a dynamic process that occur on vascularized tissue in response to different stimuli causing cell injury and tissue degeneration. Reactive oxygen and nitrogen species (ROS and RNS) and advanced glycation end products (AGEs) have a key mediatory role in the development and progression of degenerative tissue process. The bioflavonoids possess a broad-spectrum of pharmacological activities. Their capability is related to their chemical structure.

Methods In this study we evaluated and compare antioxidant, anti-glycative and anti-degenerative actions of two flavones apigenin and luteolin and a flavonol quercetin, in function of their hydroxyl groups arrangement. Moreover we assay, on NCTC 2544 and chondrocytes cultures, the flavonoids capacity to modulate NO and glycosamminoglycans levels, index of antidegenerative capacity.

Results All tested flavonoids act as free radicals scavengers (ROO• and NO•) and advanced glycation end products inhibitors, in agreement with their BDE, IP and molecular planarity. Quercetin showed a high ORAC value (2.70±0.12 ORAC Units), according to a low BDE (74.54 Kcal/mol) and IP (174.44 Kcal/mol) values. Luteolin is the most active compound in the NO (48.19±0.18%) and AGEs (60.06±0.52%) inhibition, in function of a low torsion angle (16.3°) between the 3-OH moiety and C’6 carbon atom.

Conclusion All tested flavonoids posses a protective role on degenerative tissue events. They acts in different manner depending on the functional groups, the biological substrate and the concentration used. In any case, it can be considered a suitable product preventing a degenerative processes.

Key words

nitric oxide - anti-inflammatory drugs - antioxidants/NO pathways drugs
 

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