Planta Med 2014; 80 - P1L151
DOI: 10.1055/s-0034-1394808

Anti-tyrosinase, antioxidant and UV-protective agents obtained from natural sources: A high-throughput bioguided approach

E Chaita 1, 2, N Aligiannis 1, H Pratsinis 3, D Kletsas 3, M Ralli 2, N Guldbrandsen 4, M Hamburger 4, V Dumontet 5, D Stein 5, G Fouche 6, M Gupta 7, AL Skaltsounis 1
  • 1Department of Pharmacognosy & Natural Products Chemistry, Faculty of Pharmacy, University of Athens, Zografou, 15771, Greece
  • 2Korres S.A. Natural Products, 57th Athens-Lamia National Road, 32011, Inofyta, Greece
  • 3Laboratory of Cell Proliferation & Ageing, Institute of Biology, National Centre for Scientific Research ''Demokritos'' 153 10 Athens, Greece
  • 4Division of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland
  • 5Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, C.N.R.S., 91198 Gif-sur-Yvette Cedex, France
  • 6Biosciences, CSIR, PO Box 395, Pretoria 0001, South Africa
  • 7Centro de Investigaciones Farmacognsaticas de la Flora Panamena, Facultad de Farmacia, Universidad de Panamá, Panama

Tyrosinase is regarded as a target enzyme in skin-whitening and in therapeutic interventions for dermatological disorders associated with melanin hyperpigmentation. Abnormal melanin pigments are an aesthetic problem prevalent in middle-aged and elderly individuals [1], but may also occur upon UV radiation [2]. Skin ageing on the other hand, is associated with free radical formation and UV light exposure through activation of the reactive oxygen species (ROS) system [3]. Since many known agents have been proven toxic [4], tyrosinase inhibitors and antioxidant compounds from natural sources are in the center of research interest for the development of cosmeceutical products.This project with the acronym AGROCOS (FP7) aimed to carry to the stage of development candidates, plant derived small molecules with skin-whitening, antioxidant and UV-protective properties. 460 natural compounds with structurally diverse scaffolds and decoration patterns were evaluated for the above mentioned properties. The screens addressed radical scavenging properties, protection against reactive oxygen species (ROS) and UV-induced cell death in cell-based assays, and anti-tyrosinase properties. Based on this screening, a collection of 3600 extracts from biodiversity hotspots plants was emerged and screened on the same targets. 31 most antioxidant extracts, including many representatives from Myrtaceae and Fabaceae families, and 13 extracts with anti-tyrosinase properties, such as Glycyrrhiza glabra and Caesalpinia schlechteri were prioritized for an HPLC-based bioguided microfractionation. Active fractions were submitted to a final purification of bioactive compounds.This unique extract library combined with a high-throughput approach proved to be an efficient tool for the discovery of natural agents with antioxidant, UV-protective and anti-tyrosinase properties.

Keywords: tyrosinase, antioxidant, UV-protection

References:

[1] Noh, J-M et al. (2011) Food Chem. Volume 125, Issue 3, Pages 953 – 957

[2] Panich, U. et al. (2012) Photochem Photobiol B. 108 Pages 16 – 22

[3] Herrling, T. et al (2006) Spectrochim. Acta A Mol. Biomo.l Spectrosc. 63(4):840 – 845

[4] Juris P. et al. (2007) Bioorg. Med. Chem. Lett. 17 6871 – 6875