affron®, a standardised extract from saffron (Crocus sativus L.) for the treatment of youth anxiety and depressive symptoms: A randomised, double-blind, placebo-controlled study

Background: Saffron has antidepressant and anxiolytic effects in adults with mild-to-moderate depression. However, this is the first study examining its mood-related effects in teenagers. Methods: In this 8-week, randomised, double-blind, placebo-controlled study, youth aged 12–16 years, with mild-to-moderate anxiety or depressive symptoms were given tablets containing placebo or a saffron extract (affron®, 14 mg b.i.d). The youth and parent versions of the Revised Child Anxiety and Depression Scale (RCADS) were used as outcome measures. Results: 80 participants were enrolled and 68 completed the study. Based on youth self-reports, affron®was associated with greater improvements in overall internalising symptoms (p = 0.049), separation anxiety (p = 0.003), social phobia (p = 0.023), and depression (p = 0.016). Total internalising scores decreased by an average of 33% compared to 17% in the placebo group (p = 0.029). However, parental reports of improvements were inconsistent as mean improvements in RCADS scores were greater in the saffron group (40% vs 26%) (p = 0.026), although no other significant differences were identified. affron®was well-tolerated and there was a trend of reduced headaches in participants on the active treatment. Limitations: The use of a self-report instrument, limited study duration, single treatment dose, and non-clinical sample used in this study limit the generalisability of study findings. Conclusion: The administration of a standardised saffron extract (affron®) for 8 weeks improved anxiety and depressive symptoms in youth with mild-to-moderate symptoms, at least from the perspective of the adolescent. However, these beneficial effects were inconsistently corroborated by parents.This study was funded by Pharmactive Biotech Products SL. Pharmactive Biotech Products was not involved in the design of the research, analysis of data, or in the writing of the report. The authors gratefully acknowledge Pharmactive Biotech Products SL Company for funding the project and supplying affron® and LIPA Pharmaceuticals for the preparation of the tablet

Bioaccessibility and Pharmacokinetics of a Commercial Saffron (Crocus sativus L.) Extract

There are few studies about the pharmacokinetics of the low-molecular mass carotenoids crocetin or crocin isomers from saffron (Crocus sativus L.). None has been performed with a galenic preparation of a standardised saffron extract. The aim of the present research work was to study the effect of in vitro digestion process on the main bioactive components of saffron extract tablets and the corresponding pharmacokinetic parameters in humans. Pharmacokinetics were calculated collecting blood samples every 30 min during the first 3 h and at 24 h after administration of two different concentrations (56 and 84 mg of the saffron extract) to 13 healthy human volunteers. Additionally, an in vitro digestion process was performed in order to determine the bioaccessibility of saffron main bioactive compounds. Identification and quantification analysis were performed by HPLC-PAD/MS. Digestion resulted in 40% of bioaccesibility for crocin isomers, whereas, safranal content followed an opposite trend increasing about 2 folds its initial concentration after the digestion process. Crocetin in plasma was detected in a maximum concentration (Cmax) in blood between 60 and 90 min after oral consumption with dose-dependent response kinetics, showing that crocin isomers from galenic preparation of saffron extract are rapidly transformed into crocetin. The results showed that this tested galenic form is an efficient way to administer a saffron extract, since the observed crocetin Cmax was similar and more quickly bioavailable than those obtained by other studies with much higher concentrations of crocetinThe authors gratefully acknowledge the Pharmactive Biotech Products, SL Company, for funding the project and supplying affron®, LIPA Pharmaceuticals for manufacturing the tablets, and RDC Clinical for their management of the clinical tria

Neuroprotective and Anti-Inflammatory Effects of a Hydrophilic Saffron Extract in a Model of Glaucoma

Glaucoma is a neurodegenerative disease characterized by the loss of retinal ganglion cells (RGCs). An increase in the intraocular pressure is the principal risk factor for such loss, but controlling this pressure does not always prevent glaucomatous damage. Activation of immune cells resident in the retina (microglia) may contribute to RGC death. Thus, a substance with anti-inflammatory activity may protect against RGC degeneration. This study investigated the neuroprotective and anti-inflammatory effects of a hydrophilic saffron extract standardized to 3% crocin content in a mouse model of unilateral, laser-induced ocular hypertension (OHT). Treatment with saffron extract decreased microglion numbers and morphological signs of their activation, including soma size and process retraction, both in OHT and in contralateral eyes. Saffron extract treatment also partially reversed OHT-induced down-regulation of P2RY12. In addition, the extract prevented retinal ganglion cell death in OHT eyes. Oral administration of saffron extract was able to decrease the neuroinflammation associated with increased intraocular pressure, preventing retinal ganglion cell death. Our findings indicate that saffron extract may exert a protective effect in glaucomatous pathology

affron®eye, a natural extract of saffron (Crocus sativus L.) with colorant properties as novel replacer of saffron stigmas in culinary and food applications

Natural color becomes the first sensory perception in food and improves consumers' acceptability. To this aim, the commercial saffron (Crocus sativus L.) extract affroneye can be directly used in cold dishes due to the follow advantages: absence of microbial load, easily soluble in water and with homogeneous colorant properties due to the presence of the carotenoids crocins which are standardized in all batches by high performance liquid chromatography. In this work two different cold desserts were prepared, employing saffron stigmas or affroneye to study the improvement of their sensory properties and final presentation. The cold recipe prepared with affroneye showed significantly better taste (F = 6.1, p < 0.05) and acceptability by the consumers (F = 7.5, p < 0.05), compared to the recipe with saffron stigmas. The new affroneye extract contributed to this improvement because it is easier and much more precise for dosage control, more safety (free of microorganisms), homogenizes sensory attributes, and therefore the consumer's acceptability.Peer Reviewe

Dietary fiber composition for protecting bioactive compounds during the physiological digestion process

The invention relates to a composition comprising galactomannan in an amount ranged from 36% to 40% w/w, fructooligossacharides in an amount of 2% to 4% w/w and at least one bioactive compound. The invention also relates to the uses of said composition for the administration of said bioactive compounds protected from its degradation during the physiological digestion processPeer reviewedPharmactive Biotech Products, S.L., Consejo Superior de Investigaciones Científicas (España)A1 Solicitud de patente con informe sobre el estado de la técnic

Estudio in vitro de la actividad de Isenolic® en células MDCK-SIAT1 infectadas con el virus de la Influenza A

Resumen del trabajo presentado al XII Congreso Internacional Nutrición, Alimentación y Dietética, celebrado en Madrid el 11 y 12 de abril de 2018.[Introducción] El virus de la Influenza A es responsable de la gripe estacional que cada año causa más de 250.000 muertes según la Organización Mundial de la Salud. Entre los nuevos compuestos de origen natural con actividad antimicrobiana y que podría emplearse como tratamiento de infecciones virales se encuentra el ácido elenólico, presente en las hojas de olivo (Olea europaea L)1,2,3. Isenolic® es un extracto comercial de hojas de olivo con una determinada concentración de ácido elenólico, analizado mediante cromatografía líquida de alta eficacia (HPLC).[Objetivos] Evaluación del potencial antiviral de Isenolic® frente a la actividad infecciosa del virus Influenza A (H3N2).[Métodos] Se emplearon células MDCK-SIAT1 y el virus Influenza A (H3N2) como modelos, comparando la actividad antiviral de Isenolic® con la del Oseltamivir. Se realizó un estudio de citotoxicidad con concentraciones crecientes de Isenolic® (6 a 1200 μg/mL), y se determinó la tasa de viabilidad celular tras 24 horas de incubación mediante el ensayo de reducción de sal de tetrazolio-MTT. Tras un pretratamiento con Isenolic® (1 hora) y la consecutiva exposición al virus (1 hora), se evaluaron la capacidad de inhibición de la actividad neuraminidasa del virus mediante ensayo fluorimétrico (MOI:1, Isenolic® 6-100 μg/mL) y la tasa de viabilidad celular mediante el ensayo de reducción de MTT (MOI:2, Isenolic® 100 μg/mL), en ambos casos a las 48 horas post-infección.[Resultados] Para concentraciones de Isenolic® entre 6 y 60 μg/mL la tasa de viabilidad celular es superior al 90%. A 120 μg/mL la viabilidad celular baja hasta el 70% y concentraciones entre 300 y 1200 μg/mL no se supera el 25%. La concentración citotóxica para el 50% del cultivo celular, CC50, se estima entre 120 y 300 μg/mL. Actividad antiviral: La concentración inhibitoria del 50% de la actividad viral, IC50, se establece en 60 μg/mL. A 100 μg/mL la inhibición de la actividad viral es del 65%, mientras que a las concentraciones de 6 y 12 μg/mL no se alcanza el 5%. Por otro lado, una concentración de Isenolic® de 100 μg/mL, resultó en una tasa de viabilidad celular del 73%.[Discusión] El pretratamiento con Isenolic® muestra actividad antiviral y protectora frente a la infección por el virus Influenza A en células MDCK-SIAT1 probablemente a través de la inhibición de la transcriptasa reversa del virus, lo que limitaría la replicación del virus.[Conclusiones] El tratamiento con Isenolic® a dosis efectivas es seguro, y además es capaz de inhibir la actividad viral de Influenza A hasta en un 65%, mostrando una funcionalidad cercana a del tratamiento gold standard, oseltamivir. El pretratamiento con Isenolic® es capaz de preservar la supervivencia celular frente a concentraciones citotóxicas de Influenza A, conservándose un 75% de la viabilidad celular, resultado similar al obtenido con Oseltamivir. Estos resultados muestran el potencial preventivo de Isenolic® y también como tratamiento de infecciones por Influenza A.Peer reviewe

Olivactive® inhibits the enzymatic activity in vitro of α-glucosidase and α-amylase

Resumen del trabajo presentado al XII Congreso Internacional Nutrición, Alimentación y Dietética, celebrado en Madrid el 11 y 12 de abril de 2018.[Introducción] Inhibitors of α-glucosidase and α-amylase like acarbose provides an approach in the management of the diabetes by delaying carbohydrate digestion, prolonging the overall carbohydrate digestion time, and consequently reducing the rate of glucose absorption. Extracts of olive leaves containing multifunctional bioactive compounds may reduce the postprandial rise in blood glucose, secretion of insulin and the risk for suffering associated infections. Therefore, the extracts are good candidate for treating diabetes and its complications. To the best of our knowledge, no previous studies on the inhibitory effect of Olivactive® on α-glucosidase and α-amylase have been conducted.[Objetivos] The present research aimed to study the inhibitory effects of Olivactive®, a commercial olive (Olea europaea L) leaves extract, on the enzymatic activity of α-glucosidase and α-amylase; as well as, to identify major bioactive compounds contributing to these properties.[Métodos] Bioactive components analyses: Oleuropein and flavonoids in Olivactive® samples were analyzed by high performance liquid chromatography coupled to diode array and mass detectors (HPLC-PAD/MS) according to the method proposed by Inarejos et al., 2009. Quantification of oleuropein and total flavonoids (including Luteolin and Luteolin-7-o-glucoside) were performed by the respective calibration standard curves of Oleuropein (280 nm) and rutin (355 nm). Enzymatic inhibition assay: The study of the inhibition of α-glucosidase by Olivactive® was performed according to Berthelot et al. (1999). Alpha-amylase inhibition assay was performed using the Ultra Amylase Assay Kit - EnzCheck from Thermo Fisher Scientific. Acarbose was employed as inhibitor of reference.[Resultados] Bioactive profile: Oleuropein is the major bioactive component present in Olivactive®, concentrated at 20% (dry weight), whereas total bioflavonoids were about 2% (as rutin equivalents, dry weight). Luteolin and Luteolin-7-glucoside were identified and quantified in Olivactive® in concentrations of 100μg/g and 6mg/g, respectively. Enzymatic inhibition assay: Olivactive® inhibited the activity of α-glucosidase and α-amylase. Acarbose showed IC50 values of 0.012 mg/mL and 19.83 mg/mL for α-glucosidase and α-amylase, respectively. Similar trend was observed for Olivactive® which inhibitory effect was more effective for α-glucosidase (IC50=0.32 mg/mL) than that observed for α-amylase (IC50=57.08 mg/mL).[Discusión] The presence of Luteolin and Luteolin-7-glucoside in Olivactive® may contribute to the observed inhibitory effect by forming Hbonds between functional groups at the activity sites of α-glucosidase and α-amilase enzymes and the hydroxyl groups forming the B-ring of their flavonoid skeleton (De Sales et al., 2002).[Conclusiones] Olivactive®, the commercial olive leaf extract standardized to oleuropein and flavonoids by HPLC, may be a good candidate for a better control of diabetics reducing their risk of complications. Further in vivo studies should be conducted to confirm the in vitro preliminary results reported in the present work.Peer reviewe

Liboost® induce la liberación de óxido nítrico en células endoteliales in vitro

Resumen del trabajo presentado al XII Congreso Internacional Nutrición, Alimentación y Dietética, celebrado en Madrid el 11 y 12 de abril de 2018.[Introducción] La disfunción eréctil (DE) es la incapacidad de conseguir una erección suficiente para mantener una relación sexual satisfactoria debido a distintos factores fisiopatológicos. Actualmente, el citrato de sildenafilo es el tratamiento más común de la DE masculina, pero presenta efectos secundarios. Liboost® es un extracto natural de hojas de damiana (Turnera difussa W.) concentrado en flavonoides glicosilados que son marcadores de calidad del producto, y que inducen la liberación de óxido nítrico (NO), compuesto relacionado con la vasodilatación y prevención de la DE.[Objetivos] El objetivo principal de este trabajo es caracterizar mediante cromatografía líquida de alta eficacia (HPLC) los flavonoides biofuncionales de liboost®, y estudiar su efecto in vitro en la liberación de NO en células endoteliales HUVEC.[Métodos] La identificación de los flavonoides biofuncionales de liboost® se realizó mediante HPLC siguiendo el método propuesto por Bezerra y colaboradores6. Mediante curvas de calibrado externo se cuantificaron flavonoides de forma individual (acacetina, luteolin-7-o-glucosido, apigenin-7-o-glucosido) y flavonoides totales como equivalentes de rutina. Para la determinación de la citotoxicidad del extracto se realizó el ensayo WST-1 en células HUVEC de acuerdo con las instrucciones del fabricante (WST-1 Cell Proliferation Assay Kit, Roche Applied Science). La liberación de NO se determinó cuantificando la acumulación de nitrito en el sobrenadante del cultivo mediante la reacción de Griess7 (Nitric Oxide Assay Kit, Calbiochem).[Resultados] Las muestras de liboost® empleadas en el estudio tenían una concentración en flavonoides totales superior al 1,5% (como rutina, base seca). Los flavonoides funcionales mostraron una concentración mínima individual similar: luteolina-7-O-glucósido (0,15mg/g), apigenina-7-O-glucósido (0,25mg/g) y acacetina (0,15mg/g). El tratamiento de las células HUVEC con liboost® a una concentración de 40 y 10μg/ml no dio lugar a una disminución significativa de la viabilidad celular con respecto al control. Por ello, la liberación del NO en las células HUVEC fue medida después del tratamiento con liboost® a ambas concentraciones. Finalmente, en presencia de Liboost® (10μg/ml), las células endoteliales HUVEC producen un incremento significativo en la concentración de óxido nítrico con respecto al control.[Discusión] El aumento en la producción de óxido nítrico en células endoteliales en presencia de liboost® puede ser debido la activación de la enzima eNOS por los flavonoides presentes en el extracto de damiana.[Conclusiones] Liboost®, es el primer extracto de damiana comercial titulado en flavonoides por HPLC, que induce in vitro la liberación de óxido nítrico en células endoteliales, y por tanto, podría tener un efecto potencial preventivo en la DE masculina.Peer reviewe

Dietary fiber composition for protecting bioactive compounds during the physiological digestion process

[EN] The invention relates to a composition comprising galactomannan in an amount ranged from 36 to 40% w/w, fructooligossacharides in an amount of 2 to 4% (w/w) and at least one extract of polar nature containing bioactive compounds, with a concentration between 30 and 49% in the composition. The invention also relates to the uses of said composition for the administration of said bioactive compounds contained in the extract, protecting from their degradation during the physiological digestion[FR] L'invention concerne une composition comprenant du galactomannane en une quantité allant de 36 à 40 % p/p, des fructo-oligosaccharides en une quantité de 2 à 4 % (p/p) et au moins un extrait de nature polaire contenant des composés bioactifs, en une concentration comprise entre 30 et 49 % dans la composition. L'invention concerne également les utilisations de ladite composition pour l'administration desdits composés bioactifs contenus dans l'extrait, ce qui les protège de la dégradation pendant la digestion physiologiquePeer reviewedPharmactive Biotech Products, S.L., Consejo Superior de Investigaciones Científicas (España), Universidad Autónoma de MadridA1 Solicitud de patente con informe sobre el estado de la técnic