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Determination of the chemical composition and in vitro activity of Laurus azorica against aging-related diseases
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Abstract(s)
O processo de envelhecimento é caracterizado pelo declínio progressivo das funções fisiológicas, marcado por uma diminuição da capacidade do organismo para combater o stress oxidativo e os danos celulares. Esta vulnerabilidade aumenta o risco de desenvolver distúrbios metabólicos, incluindo diabetes mellitus e dislipidemia, e o aparecimento de doenças neurodegenerativas, como a doença de Alzheimer. A maioria das soluções farmacêuticas disponíveis para estas doenças tem como princípio ativo compostos encontrados na natureza, frequentemente produzidos por plantas. Laurus azorica, uma planta endémica do arquipélago dos Açores, está pouco caracterizada no que diz respeito ao seu potencial antienvelhecimento. Neste trabalho, foi realizado um estudo fitoquímico e do potencial antienvelhecimento dos extratos de L. azorica. Extratos de acetona, acetato de etilo e etanol das folhas desta planta, preparados por extração assistida por ultrassons utilizando diferentes tempos de extração, foram fracionados e analisados por técnicas espectroscópicas. Foram isoladas três lactonas sesquiterpénicas, costunolide, reinosina e 1β-hidroxi-arbusculina A, e as suas estruturas químicas foram elucidadas, sendo a última isolada pela primeira vez nesta espécie. No que diz respeito ao efeito antioxidante, os extratos etanólicos apresentaram o maior potencial antioxidante nos ensaios ABTS e DPPH, com valores de IC50 comparáveis ao controlo positivo (Trolox) para o ensaio ABTS. Quanto ao ensaio do radical superóxido, apenas o extrato etanólico (2-LA_3) do tempo de extração mais curto apresentou uma atividade antioxidante significativa (IC50 = 42,61 ± 2,06 μg/mL), cerca do dobro do valor IC50 do controlo positivo, ácido gálico (IC50 = 24,22 ± 1,98 μg/mL). Em geral, os resultados indicaram um aumento da atividade antioxidante com o emprego de um método de extração de tempo mais curto. O potencial antidiabético e antidislipidémico foi testado por ensaios de inibição da α-amilase, α-glicosidase e lipase, mas nenhuma das amostras testadas mostrou atividade à concentração máxima testada (250 μg/mL). Relativamente à atividade anticolinesterásica, foi avaliada a inibição da AChE e da BuChE. Dos extratos, apesar de não apresentarem a melhor atividade anticolinesterásica, apenas os extratos etanólicos foram inibidores duplos. O costunolide demonstrou o maior potencial neuroprotetor de todas as amostras testadas, não só por ser um inibidor duplo, mas também por apresentar o IC50 mais baixo para o ensaio da BuChE (IC50 = 25,38 ± 1,80 μg/mL), comparável ao padrão donepezil (IC50 = 17,77 ± 0,77 μg/mL). Esta investigação mostra resultados encorajadores para a utilização terapêutica de L.azorica.
ABSTRACT: The aging process is characterized by the progressive decline in physiological functions, marked by a diminished ability of the body to combat oxidative stress and cellular damage. This vulnerability increases the risk of developing metabolic disorders, like diabetes mellitus and dyslipidemia and the onset of neurodegenerative disorders, like Alzheimer's disease. Most of the pharmaceutical solutions available for these diseases have compounds found in nature as their active principle, often produced by plants. Laurus azorica, a plant endemic to the Azores archipelago, is poorly characterized in regard to its anti-aging-related disorders potential. In this work, a phytochemical and antiaging potential study of Laurus azorica extracts was conducted. Acetone, ethyl acetate and ethanolic leaf extracts, prepared by ultrasound-assisted extraction using different extraction time, were fractioned and pure compounds analyzed by spectroscopic techniques. Three sesquiterpenic lactones, costunolide, reynosin and 1β-hydroxy arbusculin A were isolated and their chemical structures elucidated, with the latter being isolated for the first time in this species. Concerning antioxidant effect, ethanol extracts showed the greatest antioxidant potential in the ABTS and DPPH assays, with IC50 values comparable to the positive control (Trolox) for the ABTS assay. As for the superoxide scavenging assay, only the ethanol extract (2-LA_3) from shortest extraction time exhibited significant antioxidant activity (IC50 = 42.61 ± 2.06 μg/mL), about twice the IC50 value of the positive control gallic acid (IC50 = 24.22 ± 1.98 μg/mL). Overall, results indicated an enhancement in antioxidant activity with the employment of a shorter time extraction method. Antidiabetic and antidyslipidemic potential were tested by α-amylase, α-glucosidase and lipase inhibition assays, but none of the tested samples showed activity at the maximum tested concentration (250 μg/mL). Regarding anticholinesterasic activity, inhibition of AChE and BuChE was evaluated. As for the extracts, despite not exhibiting the greatest anticholinesterasic activity, only the ethanol extracts were dual inhibitors. Costunolide demonstrated the greatest neuroprotective potential of all tested samples, not only being a dual inhibitor, but also presenting the lowest IC50 for BuChE assay (IC50 = 25.38 ± 1.80 μg/mL), comparable to the standard donepezil (IC50 = 17.77 ± 0.77 μg/mL). This research shows encouraging outcomes for L.azorica therapeutic use.
ABSTRACT: The aging process is characterized by the progressive decline in physiological functions, marked by a diminished ability of the body to combat oxidative stress and cellular damage. This vulnerability increases the risk of developing metabolic disorders, like diabetes mellitus and dyslipidemia and the onset of neurodegenerative disorders, like Alzheimer's disease. Most of the pharmaceutical solutions available for these diseases have compounds found in nature as their active principle, often produced by plants. Laurus azorica, a plant endemic to the Azores archipelago, is poorly characterized in regard to its anti-aging-related disorders potential. In this work, a phytochemical and antiaging potential study of Laurus azorica extracts was conducted. Acetone, ethyl acetate and ethanolic leaf extracts, prepared by ultrasound-assisted extraction using different extraction time, were fractioned and pure compounds analyzed by spectroscopic techniques. Three sesquiterpenic lactones, costunolide, reynosin and 1β-hydroxy arbusculin A were isolated and their chemical structures elucidated, with the latter being isolated for the first time in this species. Concerning antioxidant effect, ethanol extracts showed the greatest antioxidant potential in the ABTS and DPPH assays, with IC50 values comparable to the positive control (Trolox) for the ABTS assay. As for the superoxide scavenging assay, only the ethanol extract (2-LA_3) from shortest extraction time exhibited significant antioxidant activity (IC50 = 42.61 ± 2.06 μg/mL), about twice the IC50 value of the positive control gallic acid (IC50 = 24.22 ± 1.98 μg/mL). Overall, results indicated an enhancement in antioxidant activity with the employment of a shorter time extraction method. Antidiabetic and antidyslipidemic potential were tested by α-amylase, α-glucosidase and lipase inhibition assays, but none of the tested samples showed activity at the maximum tested concentration (250 μg/mL). Regarding anticholinesterasic activity, inhibition of AChE and BuChE was evaluated. As for the extracts, despite not exhibiting the greatest anticholinesterasic activity, only the ethanol extracts were dual inhibitors. Costunolide demonstrated the greatest neuroprotective potential of all tested samples, not only being a dual inhibitor, but also presenting the lowest IC50 for BuChE assay (IC50 = 25.38 ± 1.80 μg/mL), comparable to the standard donepezil (IC50 = 17.77 ± 0.77 μg/mL). This research shows encouraging outcomes for L.azorica therapeutic use.
Description
Dissertação de Mestrado, Ciências Biomédicas, 07 de julho de 2025, Universidade dos Açores.
Keywords
Laurus azorica ultrasound-assisted extraction specialized metabolites antidiabetic anticholinesterasic Antioxidant
Pedagogical Context
Citation
LUCAS, Maria Francisca Fortuna Soares Albergaria. (2025). "Determination of the chemical composition and in vitro activity of Laurus azorica against aging-related diseases". Ponta Delgada: Universidade dos Açores, 80 p. Dissertação de Mestrado em Ciências Biomédicas. Disponível em http://hdl.handle.net/10400.3/8742