Pesquisa de atividade biológica de Extratos de plectranthus hadiensis, p. Inflexus, p. Lippio, p. Welshii e p. Mzubulensis
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2019
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Neste trabalho, estudaram-se as atividades antioxidante, antimicrobiana e letalidade
em Artemia salina, de cinco espécies do género Plectranthus (P. hadiensis, P. inflexus, P.
lippio, P. welshii e P. mzubulensis). Para o extrato mais bioativo, P. hadiensis, realizaram-se
ensaios de inibição in vitro da acetilcolinesterase, citotoxicidade, avaliação da atividade
antimicrobiana, fracionamento, isolamento e identificação de um composto bioativo.
O extrato de P. hadiensis apresentou o maior rendimento de extração (13,49% m/m).
A atividade antimicrobiana foi avaliada contra bactérias Gram-positivas, negativas e leveduras
pelo método de difusão em poços (zonas de inibição contra S. aureus - 15 mm e C. albicans
-11 mm) e pelo método de microdiluição (valores de CMI para S. aureus e S. aureus-
CIP106760 de 15,62 e de 3,91 μg/mL, respetivamente). A atividade antioxidante foi avaliada
pelo método de DPPH (36,24%) e a toxidade geral num modelo de Artemia salina (CL50 =
0,880 mg/L). A inibição da acetilcolinesterase foi de 19,98% e a citotoxicidade foi avaliada em
três linhas celulares humanas (HCT116 = 3,45 ± 0,35; MCF-7 = 2,90 ± 0,10; NCI-H460 = 3,00
± 0,10 μg/mL).
Um estudo fitoquímico bioguiado foi realizado e originou o isolamento e
caracterização espetroscópica de 7α-acetoxi-6β-hidroxiroileanona, que é o potencial
responsável pela bioatividade.
In this work, the antioxidant and antimicrobial activities and lethalithy in Artemia salina, of five Plectranthus genus species (P. hadiensis, P. inflexus, P. lippio, P. welshii and P. mzubulensis), were studied. For the most bioactive extract, P. hadiensis, were performed in vitro inhibition assays of acetylcholinesterase, cytotoxicity, antimicrobial activity evaluation, fractionation, isolation and identification of one bioactive compound. P. hadiensis extract showed the highest extraction yeld (13,49% m/m). The antimicrobial activity was evaluated against Gram- positive and negative bacteria and yeasts with the well-difusion method (inhibition zones against S. aureus- 15 mm and C. albicans- 11 mm) and with the microdilution test (MIC values to S. aureus and S. aureus-CIP106760 of 15,62 and 3,91 μg/mL, respectively). The antioxidant activity was evaluated with DPPH method (36,24%) and general toxicity in an Artemia salina model (LC50 = 0,880 mg/L). The acetylcholinesterase inhibition was 19,98% and cytotoxicity was evaluated in three human cell lines (HCT116 = 3,45 ± 0,35; MCF-7 = 2,90 ± 0,10; NCI-H460 = 3,00 ± 0,10 μg/mL). A bioguided phytochemical study was performed and it led to the isolation and spectroscopical characterization of 7α-acetoxy-6β-hidroxyroyleanone, that is the potential responsible for the bioactivity.
In this work, the antioxidant and antimicrobial activities and lethalithy in Artemia salina, of five Plectranthus genus species (P. hadiensis, P. inflexus, P. lippio, P. welshii and P. mzubulensis), were studied. For the most bioactive extract, P. hadiensis, were performed in vitro inhibition assays of acetylcholinesterase, cytotoxicity, antimicrobial activity evaluation, fractionation, isolation and identification of one bioactive compound. P. hadiensis extract showed the highest extraction yeld (13,49% m/m). The antimicrobial activity was evaluated against Gram- positive and negative bacteria and yeasts with the well-difusion method (inhibition zones against S. aureus- 15 mm and C. albicans- 11 mm) and with the microdilution test (MIC values to S. aureus and S. aureus-CIP106760 of 15,62 and 3,91 μg/mL, respectively). The antioxidant activity was evaluated with DPPH method (36,24%) and general toxicity in an Artemia salina model (LC50 = 0,880 mg/L). The acetylcholinesterase inhibition was 19,98% and cytotoxicity was evaluated in three human cell lines (HCT116 = 3,45 ± 0,35; MCF-7 = 2,90 ± 0,10; NCI-H460 = 3,00 ± 0,10 μg/mL). A bioguided phytochemical study was performed and it led to the isolation and spectroscopical characterization of 7α-acetoxy-6β-hidroxyroyleanone, that is the potential responsible for the bioactivity.
Descrição
Orientação: Patrícia Dias Mendonça Rijo
Palavras-chave
MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS, CIÊNCIAS FARMACÊUTICAS, PHARMACEUTICAL SCIENCES, PLANTAS MEDICINAIS, MEDICINAL PLANTS, ACETILCOLINESTERASE, ACETYLCHOLINESTERASE, ANTIOXIDANTES, ANTIOXIDANTS, TOXICIDADE, TOXICITY, ANTIMICROBIANOS, ANTIMICROBIAL