Antileishmanial activity of fucosterol recovered from Lessonia vadosa Searles (Lessoniaceae) by SFE,PSE and CPC |
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| Affiliation: | 1. Pharmacognosy, GQBMRNP-CRIDECIT, FCN, UNPSJB, Ruta provincial n°1, KM 4, Comodoro Rivadavia 9000, Chubut, Argentina;2. Laboratoire de Pharmacognosie, UMR CNRS 8638 COMETE, Faculté de Pharmacie de Paris, Université Paris Descartes, Sorbonne Paris Cité, 4 avenue de l’Observatoire, 75006 Paris, France;3. Biological Chemistry II, GQBMRNP-CRIDECIT, FCN, UNPSJB, Ruta provincial n°1, KM 4, Comodoro Rivadavia 9000, Chubut, Argentina;4. Medicinal Chemistry II, GQBMRNP-CRIDECIT, FCN, UNPSJB, Ruta provincial n°1, KM 4, Comodoro Rivadavia 9000, Chubut, Argentina;5. Société Hitex, Pentaparc BP33601, Rue Lefèvre-Utile, 56036 Vannes Cedex, France;6. Laboratory of Molecular Parasitology, Department of Microbiology, Hellenic Pasteur Institute, 127 Vas. Sofias avenue, 11521 Athens, Greece;1. ICMR-UMR CNRS 7312, Groupe Isolement et Structure, Campus Sciences, Bât. 18, BP 1039, 51687 Reims Cedex 2, France;2. Laboratoire de Chimie Organique Biologique, 01 BPV 34 Abidjan 01, Université Félix-Houphouët Boigny d’Abidjan-Cocody, Cote d’Ivoire;3. ICMR-UMR CNRS 7312, Service Commun d’Analyses, Campus Sciences, Bât. 18, BP 1039, 51687 Reims Cedex 2, France;1. Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China;2. State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau 999078, China;1. Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan;2. Pharmacy Discipline, Life Science School, Khulna University, Khulna 9208, Bangladesh;3. Department of Pharmaceutical Chemistry, University of Dhaka, Dhaka 1000, Bangladesh;4. University of the Philippines Visayas Tacloban College, Tacloban City 6500, Philippines;1. Department of Pharmacognosy, Faculty of Pharmacy, Atatürk University, 25240 Erzurum, Turkey;2. Department of Pharmacognosy, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey;3. Department of Chemistry, Faculty of Science, Atatürk University, 25240 Erzurum, Turkey;1. School of Life Science, Beijing Institute of Technology, Beijing 100081, PR China;2. Beijing BIT&GY Pharmaceutical R&D Co. Ltd., Beijing 100081, PR China |
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| Abstract: | Fucosterol, a triterpene derivative encountered in several alga species, provides a wide range of biological activities, such as protection against metabolic syndrome, or against UV-induced skin damage. We describe here the comparison of extraction by supercritical fluid (SFE) and pressurized solvent (PSE) of the brown alga Lessonia vadosa mainly abundant in the coastal water of Patagonia, followed by the isolation of fucosterol, using centrifugal partition chromatography (CPC), in association with HPLC–UV quantification. After collection, the seaweed was dried, ground and extracted either by PSE or by SFE under various conditions. The yield and the content in fucosterol of each extract were determined by HPLC–UV. Optimization of a biphasic solvent system and KD calculation led to the isolation of pure fucosterol with high recovery rate. Extraction by SFE using CO2 at 180 bar and 50 °C with 20 to 30 % of cellulose as modifier and CPC purification by cyclohexane/acetone/methanol/water 10/1/10/1 with lower layer as mobile phase led to the best results in terms of yield, purity, time and solvent consumption. Natural and semisynthetic steroid derivatives have been previously shown to be potential drug candidates against parasitic diseases including leishmaniasis. In this context fucosterol was evaluated and demonstrated noticeable antileishmanial activity (IC50 < 10 μM) against intracellular amastigotes with limited or no cytotoxicity in host cell macrophages. These results make this compound a valuable starting scaffold for pharmacomodulation. Adaptation of the procedure by slight modifications of the extraction and/or isolation conditions could permit the exploitation of other alga species as raw material. Since SFE and CPC are available for pilot and batch production, this work may serve as a model for further scale-up and industrial development. |
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| Keywords: | Fucosterol SFE PSE CPC Leishmania |
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