sábado, 22 de abril de 2017

Efectos de la curcumina libre sobre la inflamación y las funciones cognitivas

Benoit Fillion. Ingeniero Químico. Bruselas, Bélgica. Ponencia en el 9º Congreso de Fitoterapia de SEFIT – IX Jornada Farmacéutica de la Isla del Rey, Menorca, 18-21 de mayo de 2017. Patrocinada por Laboratoire Optim
Tecnología de microencapsulación Sólido-Lípido de la Curcumina Longvida (2)

La curcumina libre es el principal polifenol presente en el rizoma de Curcuma longa (2-5% del peso total seco). Algunos de los múltiples beneficios de la curcumina son su capacidad antiinflamatoria y antioxidante (1). Su bajo peso molecular y su estructura polar le permiten traspasar la barrera hematoencefálica (2). La fórmula de Optim Curcuma ha sido desarrollada por un grupo de científicos de la Universidad de California (UCLA) y permite resolver el problema de la poca asimilación de la curcumina en el organismo. Tras diez años de estudios, la clave de la eficacia de la fórmula se encontró en el proceso de fabricación de la patente del complejo LongVida SLCP™ (Solid-Lipid Curcumin Particle) (2). Este proceso patentado consiste en encapsular cuidadosamente la curcumina con lípidos (lecitina y ácido esteárico) para formar las pequeñas partículas que permiten aumentar hasta 65 veces la asimilación de curcumina libre en plasma. La curcumina se asimila de esta manera y se transporta por el plasma en forma altamente biodisponible (3).

La actividad antiinflamatoria

La actividad antiinflamatoria de la cúrcuma se conoce desde hace varios siglos, pero en las dos pasadas décadas se ha intensificado notablemente su investigación y ha demostrado ser muy útil y utilizada en enfermedades crónicas (1). Se ha demostrado que el efecto antiinflamatorio de la curcumina de la formula Longvida actúa a través de la inhibición del factor nuclear kappaB (NF-kB) que reduce las citoquinas IL-6, y las prostaglandinas E2 (PGE2) (4). La inhibición del NF-kB se considera un objetivo primordial en la prevención y el tratamiento de las inflamaciones crónicas y degenerativas.

Funciones cognitivas

Varios estudios han confirmado el efecto de la curcumina libre sobre las funciones cognitivas. Presentaremos los resultados de un ensayo clínico aleatorizado de la Universidad de Swinburne (Melbourne, Australia). El grupo que tomó durante 4 semanas 400 mg de Longvida (80 mg de curcumina) mostró una mejoría en el estado de ánimo, la memoria de trabajo, el estado de alerta, la fatiga y la sensación de bienestar (5). Los autores atribuyen la reducción de fatiga, el aumento del estado de alerta y la sensación de calma al efecto de la curcumina sobre la serotonina y la dopamina (6). Presentaremos también los resultados de estudios in vivo realizados con la formula Longvida. Se demostró que la curcumina libre reduce la placa beta-amiloide y la formación de ovillos de neurofibrillias en el cortex de ratones (7, 8).

Referencias

1. Jurenka JS. Anti-inflammatory properties of curcumin, a major constituent of Curcuma longa: a review of preclinical and clínical research. Altern Med Rev. 2009;14 (2): 141-53.
2. Begum AN, et al. Curcumin structure-function, bioavailability, and efficacy in models of neuroinflammation and Alzheimer’s disease. J Pharmacol Exp Ther. 2008; 326 (1):196-208.
3. Gota VS, et al. Safety and pharmacokinetics of a solid-lipid curcumin particle formulation in osteosarcoma patients and healthy volunteers. J Agric Food Chem. 2010; 58 (4): 2095-9.
4. Nahar PP, et al. Anti-Inflammatory Effects of Novel Standardized Solid-Lipid Curcumin Formulations. J Med Food. 2014 Dec 9.
5. Cox KH, et al. Investigation of the effects of solid-lipid curcumin on cognition and mood in a healthy older population. J Psychopharmacol. 2014 Oct 2
6.Kulkarni SK, et al. Antidepressant activity of curcumin: involvement of serotonin and dopamine system. Psychopharmacology (Berl). 2008; 201 (3): 435-42.
7. Frautschy S, et al, Alzheimer’s & Dementia: The Journal of the Alzheimer’s Association 2011, 7 (4): S299–S300.
8. Ma QL, et al. Curcumin suppresses soluble tau dimers and corrects molecular chaperone, synaptic, and behavioral deficits in aged human tau transgenic mice. J Biol Chem. 2013; 288 (6): 4056-65.

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Antiproliferative activity of essential oils against promastigote and amastigote forms of Leishmania amazonensis

Raquel RD Moreira a, Caio H Perego a, André G dos Santos a, Flávio Alexandre de Carvalho a, Carlos Cavaleiro b, Lígia Salgueiro b, Maria do Céu Sousa b, Mara Lane C Cardoso c, Juliana Cogo c, Celso V Nakamura c. Comunicación en forma de póster en el 9º Congreso de Fitoterapia de SEFIT – IX Jornada Farmacéutica de la Isla del Rey, Menorca, 18-21 de mayo de 2017

a UNESP-Univ. Estadual Paulista, Faculdade de Ciências Farmacêuticas de Araraquara, Araraquara, São Paulo, Brasil. b Universidade de Coimbra, Faculdade de Farmácia, Portugal c Universidade Estadual de Maringá, Maringá, Paraná, Brasil.

Tagetes patula. Foto: Rajat0247 (licencia CC)

Introduction
Leishmaniosis is an important public-health problem, manifested in visceral, mucocutaneous, or cutaneous forms. Leishmania amazonensis causes cutaneous leishmaniasis, which ranges from small cutaneous nodules to gross mucosal tissue destruction. The drugs recommended currently for treatment include pentavalent antimonials, amphotericin B, and miltefosine. But, are limited to some extent by their toxicity, lack of efficacy, requirement for hospitalisation, or cost. More efficacious drugs are urgently needed to treat patients with leishmaniasis. So, is urgent the search for new drugs against Leishmania spp. Essential oils (EOs) are a potential source for new antiprotozoal drugs, and can contribute to overcome the drug resistance of protozoan parasites.

Objectives
The present work aims to evaluate action of the EOs of the Melampodium divaricatum (aerial parts), Polygonum acre (aerial parts), Hedychium coronarium (leaves and rhizomes), Tagetes patula (aerial parts) and Casearia sylvestris (leaves) against Leishmania amazonensis (promastigote forms). The most active oils were tested against amastigote forms.

Materials and Methods
EOs were obtained by hydrodistillation in a modified Clevenger apparatus. Promastigote forms of L. amazonensis were inoculated in Warren’s medium supplemented with 10% of inactivated fetal bovine serum containing different EOs, which were added only once to the cultures. Cells were grown in a 24-well plate with each well containing 1 ml of the medium. After cell growth was estimated by counting in a haemocytometer. All experiments were performed in duplicate, and the results expressed as log number cells/ml and as the percentage of growth inhibition. EOs tested were dissolved in DMSO, of which the final concentration did not exceed 1%. Axenic amastigote cultures, obtained by in vitro transformation of infective promastigotes, were maintained in Schneider’s insect medium, pH 4.5, with 20% fetal bovine serum at 32oC.

Results
EOs of M. divaricatum, P. acre, H. coronarium leaves, H. coronarium rhizomes, T. patula and C. sylvestris showed IC50values equal 24.2, 27.5, 91.4, >100 and 29.8 µg/ml, respectively for promastigotes forms. And M. divaricatum, P. acre and C. sylvestris (the most active oils against promastigote forms) showed IC50 values equal 10.7, 6.8 and 14.0 µg/ml against amastigotes forms.

Conclusion
Further studies need to be carried out, in order to understand the mechanisms of action and to evaluate the toxicity of these essential oils and the major compounds.

Support: PADC-FCF-UNESP-Araraquara, São Paulo, Brasil.

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