Hesperidin is one of the most important natural flavonoids, known for its antioxidant, anti-inflammatory, anti-mutagenic, and anti-hypertensive properties. Despite its various biological activities, hesperidin is rarely used in the dermo-cosmetic field because of its poor solubility in both water and oil phases that makes difficult formulation, distribution and bioavailability through the skin layers. Moreover, hesperidin is still underestimated in skin care products, and literature data on its stability into a topical formulation are not yet available. In this paper we report the synthesis of five different derivatives of hesperidin and their evaluation in terms of antioxidant, antifungal, antiproliferative, and apoptotic effects on human leukemic K562 cells. Preliminary antiproliferative effects were considered since hyper-proliferation is involved in several cutaneous problems particularly in the case of photo-exposition and environmental pollution. Esp4 and Esp5 were found to be more active in inhibiting K562 cell growth than parent hesperidin. Esp3 exhibited different biological properties, i.e., antioxidant activity in the absence of antiproliferative effects.

Novel lipidized derivatives of the bioflavonoid hesperidin: Dermatological, cosmetic and chemopreventive applications

Bino, Alessia
Primo
Methodology
;
Vicentini, Chiara Beatrice
Secondo
Supervision
;
Vertuani, Silvia
Funding Acquisition
;
Lampronti, Ilaria
Formal Analysis
;
Gambari, Roberto
Conceptualization
;
Durini, Elisa
Formal Analysis
;
Manfredini, Stefano
Penultimo
Supervision
;
Baldisserotto, Anna
Ultimo
Writing – Original Draft Preparation
2018

Abstract

Hesperidin is one of the most important natural flavonoids, known for its antioxidant, anti-inflammatory, anti-mutagenic, and anti-hypertensive properties. Despite its various biological activities, hesperidin is rarely used in the dermo-cosmetic field because of its poor solubility in both water and oil phases that makes difficult formulation, distribution and bioavailability through the skin layers. Moreover, hesperidin is still underestimated in skin care products, and literature data on its stability into a topical formulation are not yet available. In this paper we report the synthesis of five different derivatives of hesperidin and their evaluation in terms of antioxidant, antifungal, antiproliferative, and apoptotic effects on human leukemic K562 cells. Preliminary antiproliferative effects were considered since hyper-proliferation is involved in several cutaneous problems particularly in the case of photo-exposition and environmental pollution. Esp4 and Esp5 were found to be more active in inhibiting K562 cell growth than parent hesperidin. Esp3 exhibited different biological properties, i.e., antioxidant activity in the absence of antiproliferative effects.
2018
Bino, Alessia; Vicentini, Chiara Beatrice; Vertuani, Silvia; Lampronti, Ilaria; Gambari, Roberto; Durini, Elisa; Manfredini, Stefano; Baldisserotto, Anna
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2398745
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