Research Institute for Medicines

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If you cannot beat them, join them: exploring the fruits of the invasive species Carpobrotus edulis (L.) NE Br as a source of bioactive products

Publication . Castañeda-Loaiza, Viana; Placines, Chloé; Rodrigues, Maria João; Pereira, Catarina; Zengin, Gokhan; Uysal, Ahmet; Jeko, Jozsef; Cziaky, Zoltan; Reis, Catarina Pinto; Gaspar, Maria Manuela; Custódio, Luísa

The halophyte species Carpobrotus edulis (L.) N.E. Br, also known as Hottentot-fig, is one of the 20 most aggressive invasive species of coastal areas worldwide. It is native to South Africa, where it is used in traditional medicine for the treatment of several diseases, including tuberculosis and acquired immunodeficiency syndrome (AIDS) caused by the human immunodeficiency virus (HIV). Aiming at a sustainable use of its biomass as a value-added product, this work reports for the first time the in vitro antioxidant, anti-microbial, enzymatic inhibitory properties and toxicity of peel and flesh extracts of Hottentot-fig mature fruits. The extracts' chemical composition was also determined by spectrophotometric methods (total contents of phenolics: TPC; flavonoids: TFC and tannins: TTC), and by high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS). The peels' extracts had generally the highest TPC, TFC and TTC, especially the ethanol ones (TPC: 272.82 mg gallic acid equivalents (GAE)/g dry weight (DW), TFC: 1.58 mg quercetin equivalents (QE)/g DW and TTC: 20.3 mg catechin equivalents (CE)/g DW). The peels' extracts also had the highest diversity of compounds, mostly phenolic acids, flavonoids, and coumarins, as identified by HPLC-ESI-MS/MS. Some molecules were specific to a particular fruit part, for example, coumaric acid and uvaol in the peel, and vanillin and kaempferol-O-(rhamnosyl)hexosylhexoside in the flesh. Some compounds are here described for the first time in Hottentot-fig, such as azelaic acid and emodin. The peel's extracts had the highest anti radical activity, especially the ethanol and acetone towards 2,2-diphenyl-1-picrylhydrazyl (DPPH) (half maximal inhibitory concentration (IC50) values of 0.59 and 0.88 mg/mL, respectively), and the acetone extract against 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) (IC50 = 0.56 mg/mL). Samples had nil capacity to chelate iron, a low copper chelation potential, but a significant capacity to reduce iron, especially the ethanol (IC50 = 0.09 mg/mL) and the acetone extracts of peels (IC50 = 0.10 mg/mL) and flesh (IC50 = 0.11 mg/mL) and also the water peel's extracts (IC50 = 0.18 mg/mL). Samples had nil to low activity towards the enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), alpha-amylase and alpha-glucosidase, but displayed a strong inhibition of tyrosinase, especially the ethanol peel's extracts (29.55 mg kojic acid equivalents (KAE)/g). Samples had nil to low in vitro toxicity towards human keratinocytes. All together our results suggests possible novel biotechnological applications of Hottentot-fig fruits as sources of innovative bioactive ingredients for the food, cosmetic, agriculture and/or pharmaceutical industries.

2020-02Journal article

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Synchronous insight of in vitro and in vivo biological activities of Sambucus nigra L. extracts for industrial uses

Publication . Mota, Ana Henriques; Andrade, Joana M.; Rodrigues, Maria Joao; Custódio, Luísa; Bronze, Maria Rosario; Duarte, Noelia; Baby, Andre; Rocha, Joao; Gaspar, Maria Manuela; Simoes, Sandra; Carvalheiro, Manuela; Fattal, Elias; Almeida, Antonio Jose; Reis, Catarina Pinto

There is a re-emerging interest in natural products as reputable sources of new active pharmaceutical ingredients. This study synchronously reports in vitro, with more than one cell line, and in vivo biological activities of extracts obtained from Sambucus nigra. Using several solvents and techniques, eighteen extracts were obtained from fresh and dried berries, and fresh flowers. The flavonoid content and identification were determined using HPLC-MS/MS. The extracts were then screened for antioxidant activity, total polyphenol content, collagenase, elastase, tyrosinase and acetylcholinesterase inhibition as well as photoprotection. In vitro and in vivo (murine model) anti-inflammatory activity and cytotoxicity (skin and monocytic cells) were also studied. The most promising extracts were those obtained from fresh flowers using either ultrasounds or methanol. These extracts showed similar results to positive controls, particularly the antioxidant activity (74.5 +/- 1.6 %), collagenase inhibition (93.6 +/- 0.6 %), photoprotection (Sun Protection Factor > 50), in vitro anti-inflammatory activity (96.9 +/- 2.9 %), as well as oral/topical anti-inflammatory activity. The ultrasounds/ethanol extract of fresh flowers presented higher collagenase inhibition (88.3 +/- 2.8 %) and in vitro anti-inflammatory activity (101.8 +/- 1.5 %). Cytotoxicity testing confirmed the safety. Chemical characterization allowed the deduction of a correlation between extract composition and biological activities, suggesting a straightforward application in the development of novel products subject to further investigation.

2020-10Journal article

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