Cribado de extractos naturales a partir de subproductos de la industria frutícola para la obtención de nuevos principios activos con fines dermocosméticos

La industria cosmética se caracteriza por una alta competencia y necesidad de renovación. Dentro de los distintos productos de esta industria, los cosmecéuticos son aquellos que tienen principios activos con actividades beneficiosas que se relacionan con la industria farmacéutica. Los compuestos bioactivos naturales han mostrado diversas actividades relacionadas con la cosmética, entre ellas la actividad antioxidante y la capacidad de protección frente a la radiación solar. El principal objetivo de este trabajo ha sido la búsqueda de principios activos para la obtención de nuevos ingredientes cosméticos a partir de la caracterización, estudio y cribado de diferentes extractos naturales, obtenidos a partir de subproductos de la industria frutícola, en concreto de la industria de la cereza y el aguacate. El extracto scSFE fue elegido entre 3 diferentes extractos de rabo de cereza obtenidos mediante 3 métodos distintos de extracción: solvente a presión, fluido supercrítico y agua subcrítica. Por otro lado, el extracto de piel de aguacate P85 fue escogido entre 6 extractos de semilla y piel de aguacate obtenidos a 3 temperaturas de secado distintas. Ambos extractos han demostrado una alta capacidad antioxidante en diferentes ensayos in vitro, así como la capacidad de proteger frente a la radiación ultravioleta A y B en un modelo celular de piel. Adicionalmente, el extracto scSFE ha mostrado la capacidad de inhibir enzimas que degradan componentes de la matriz extracelular, lo cual se relaciona con una actividad de antienvejecimiento, y el extracto P85 ha mostrado un efecto melanogénico en un modelo celular de melanoma murino. Esta actividad podría deberse a los compuestos mayoritarios de ambos extractos, especialmente los polifenoles, que son compuestos bioactivos producidos por el metabolismo secundario de las plantas y han sido ampliamente utilizados en la medicina tradicional, así como en la industria farmacéutica y cosmética. Estas actividades que han presentado ambos extractos los postula como potenciales candidatos para ser utilizados en productos dermocosméticos, especialmente enfocados a la protección solar y productos antienvejecimiento. No obstante, son necesarios futuros estudios para determinar con total detalle el mecanismo de acción mediante el cual ejercen su efecto.In cosmetic industry, there is a fierce competition, having been claimed the need for renewal. Cosmetic products include cosmeceuticals, which are those that include principles with beneficial activities related to pharmaceutical industry. Natural bioactive compounds have shown various activities related to cosmetics, including antioxidant activity and the ability to protect against solar radiation. The aim of this project has been the search of active principles to obtain new dermocosmetic products. For this purpose, we have studied, characterized and selected extracts obtained from natural sources. These products were obtained from byproducts of sweet cherry and avocado industry. The scSFE extract was chosen from 3 different cherry stem extracts obtained by 3 extraction methods: pressurized solvent extraction, supercritical fluid extraction and subcritical water extraction. Furthermore, the P85 avocado peel extract was chosen from 6 avocado seed and peel extracts dried at three different temperatures. Both extracts, scSFE and P85, have shown a high antioxidant capacity in different in vitro tests, as well as the ability to protect against ultraviolet A and B radiation in a cell model. Additionally, the scSFE extract has shown the ability to inhibit enzymes that degrade components of the extracellular matrix, which is related to an anti-aging activity. Furthermore, the P85 extract has shown a melanogenic effect in a murine melanoma cell model. This activity could be due to the main compounds of both extracts, especially polyphenols. Polyphenols are bioactive compounds produced by the secondary metabolism of plants and have been widely used in traditional medicine and pharmaceutical and cosmetic industries. These activities presented by both extracts show them as potential candidates to be used in dermo-cosmetic products, particularly focused on sun protection and anti-aging products. However, future studies are necessary to determine completely the mechanism of action for these activities

Sweet Cherry Byproducts Processed by Green Extraction Techniques as a Source of Bioactive Compounds with Antiaging Properties

Authors thank GRAFOR BIOTECH S.L. by its support to the project.In the cosmetic industry, there is a continuous demand for new and innovative ingredients for product development. In the context of continual renovation, both cosmetic companies and customers are particularly interested in compounds derived from natural sources due to their multiple benefits. In this study, novel and green-extractive techniques (pressurized solvent, supercritical CO2, and subcritical water extractions) were used to obtain three new extracts from sweet cherry stems, a byproduct generated by the food industry. The extracts were characterized by high-performance liquid chromatography coupled to quadrupole-time-of-flight mass spectrometry (HPLC-ESI-QTOF-MS), and 57 compounds, mainly flavonoids but also organic and phenolic acids, fatty acids, and terpenes, were identified. After analytical characterization, a multistep screening approach, including antioxidant, enzymatic, and photoprotective cellular studies, was used to select the best extract according to its benefits of interest to the cosmetics industry. The extract obtained with supercritical CO2 presented the best characteristics, including a wide antioxidant capacity, especially against lipid peroxyl and •OH free radicals, as well as relevant photoprotective action and antiaging properties, making it a potential new ingredient for consideration in the development of new cosmetics.This research was funded by projects RTI2018-096724-B-C21 and 2018-096724-B-C22 from the Spanish Ministry of Science, Innovation and Universities; APOSTD/2018/097 fellowship from Generalitat Valenciana to M.H-.L. and CIBER (CB12/03/30038, Fisiopatología de la Obesidad y la Nutrición, CIBERobn)

Sweet Cherry Byproducts Processed by Green Extraction Techniques as a Source of Bioactive Compounds with Antiaging Properties

In the cosmetic industry, there is a continuous demand for new and innovative ingredients for product development. In the context of continual renovation, both cosmetic companies and customers are particularly interested in compounds derived from natural sources due to their multiple benefits. In this study, novel and green-extractive techniques (pressurized solvent, supercritical CO2, and subcritical water extractions) were used to obtain three new extracts from sweet cherry stems, a byproduct generated by the food industry. The extracts were characterized by high-performance liquid chromatography coupled to quadrupole-time-of-flight mass spectrometry (HPLC-ESI-QTOF-MS), and 57 compounds, mainly flavonoids but also organic and phenolic acids, fatty acids, and terpenes, were identified. After analytical characterization, a multistep screening approach, including antioxidant, enzymatic, and photoprotective cellular studies, was used to select the best extract according to its benefits of interest to the cosmetics industry. The extract obtained with supercritical CO2 presented the best characteristics, including a wide antioxidant capacity, especially against lipid peroxyl and •OH free radicals, as well as relevant photoprotective action and antiaging properties, making it a potential new ingredient for consideration in the development of new cosmetics

Rosemary (Rosmarinus officinalis) extract causes ROS-induced necrotic cell death and inhibits tumor growth in vivo

Colorectal cancer is the third most common diagnosed cancer globally. Although substantial advances have been obtained both in treatment and survival rates, there is still a need for new therapeutical approaches. Natural compounds are a realistic source of new bioactive compounds with anticancer activity. Among them, rosemary polyphenols have shown a vast antiproliferative capacity against colon cancer cells in vitro and in animal models. We have investigated the antitumor activity of a rosemary extract (RE) obtained by using supercritical fluid extraction through its capacity to inhibit various signatures of cancer progression and metastasis such as proliferation, migration, invasion and clonogenic survival. RE strongly inhibited proliferation, migration and colony formation of colon cancer cells regardless their phenotype. Treatment with RE led to a sharp increase of intracellular ROS that resulted in necrosis cell death. Nrf2 gene silencing increased RE cytotoxic effects, thus suggesting that this pathway was involved in cell survival. These in vitro results were in line with a reduction of tumor growth by oral administration of RE in a xenograft model of colon cancer cells using athymic nude mice. These findings indicate that targeting colon cancer cells by increasing intracellular ROS and decreasing cell survival mechanisms may suppose a therapeutic option in colon cancer through the combination of rosemary compounds and chemotherapeutic drugs.Tis work was supported by projects AGL2011-29857-C03-02 and AGL2011-29857-C03-03 (Spanish Ministry of Science and Innovation); AGL2015-67995-C3-1-R (Spanish Ministry of Economy and Competitiveness (MINECO); PROMETEO/2012/007, PROMETEO/2016/006, ACOMP/2013/093, ACIF/2013/064, ACIF/2015/158, APOTIP/2017/003 and APOSTD/2017/023 (Generalitat Valenciana), and CIBER (CB12/03/30038, Fisiopatologia de la Obesidad y la Nutricion, CIBERobn, Instituto de Salud Carlos III. Spain).Peer reviewe

Intestinal Permeability Study of Clinically Relevant Formulations of Silibinin in Caco-2 Cell Monolayers

An ever-growing number of preclinical studies have investigated the tumoricidal activity of the milk thistle flavonolignan silibinin. The clinical value of silibinin as a bona fide anti-cancer therapy, however, remains uncertain with respect to its bioavailability and blood–brain barrier (BBB) permeability. To shed some light on the absorption and bioavailability of silibinin, we utilized the Caco-2 cell monolayer model of human intestinal absorption to evaluate the permeation properties of three different formulations of silibinin: silibinin-meglumine, a water-soluble form of silibinin complexed with the amino-sugar meglumine; silibinin-phosphatidylcholine, the phytolipid delivery system Siliphos; and Eurosil85/Euromed, a milk thistle extract that is the active component of the nutraceutical Legasil with enhanced bioavailability. Our approach predicted differential mechanisms of transport and blood–brain barrier permeabilities between the silibinin formulations tested. Our assessment might provide valuable information about an idoneous silibinin formulation capable of reaching target cancer tissues and accounting for the observed clinical effects of silibinin, including a recently reported meaningful central nervous system activity against brain metastases