The antimicrobial and cytotoxic activities of the leaf or flower ethanol extracts from Senna and Cassia species.
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•Species belonging to the genera Senna or Cassia are widely used in ...Brazilian traditional medicine.•The antimicrobial and cytotoxic activities of the leaf or flower ethanol extracts from Senna and Cassia species were evaluated.•S. macranthera flower ethanol extract exerted significant antifungal activity that was correlated with a series of phenolic compounds.
In Brazilian traditional medicine, botanical species belonging to the genera Senna and Cassia are widely used as laxative, analgesic, and antifungal agents to treat ringworm and other fungal skin infections. This has motivated us to select and to screen ten species of these genera for their antibacterial, antifungal, and cytotoxic activities. The leaf or flower ethanol extracts were investigated against aerobic and anaerobic oral bacteria and Candida spp.; the microdilution broth method was employed. Cytotoxicity was determined against Vero cells. Among the plant extracts evaluated herein, four extracts at 200.0–400.0 μg mL–1 presented moderate activities against at least two bacterial strains. Concerning the antifungal action, the S. macranthera flower ethanol extract exerted significant antifungal effect with MIC values ranging from 5.9 to 23.4 μg mL–1. This extract was submitted to liquid-liquid extraction, and the resulting fractions were tested. The ethyl acetate fraction showed better antifungal activity (MIC values of 5.9 μg mL–1 for C. glabrata and 23.4 μg mL–1 for C. albicans and C. tropicalis) as compared with amphotericin B (0.1–0.2 μg mL–1), used as positive control. The bioactive metabolites of this fraction were identified by UHPLC–ESI/HRMS/MSn, which revealed the presence of eighteen compounds, including one organic acid (1), two flavan-3-ol (2 and 3), one flavone (4), two glycosylated flavonols (5 and 6), five proanthocyanidin dimers (7–11b), and seven proanthocyanidin trimers (12–18). The antimicrobial activities of some Senna or Cassia species studied here have been reported for the first time. The present results show that S. macranthera flowers are an interesting source of new antifungal agents.
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Previous issue date: 2014-07-17
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES
This work describes the chemical study;
of E. suberosum, aiming to elucidate structures of secondary metabolites in the;
leaves, stem and roots. Cathepsins assays were used to evaluate in vitro;
activity of extracts, fractions and isolated compounds, using fluorogenic;
substrate ZFR-MCA. These enzymes, also known as lysossomal cysteine;
peptidases are involved in many physiological processes, and are associated;
with many pathological conditions. Cathepsins K, L and V are involved in the;
development of diseases such as osteoporosis, skin cancer and;
atherosclerosis, respectively. Based on pathological processes in which;
cathepsins are involved, the search for specific inhibitors can be a new;
approach for the treatment these diseases. The study of ethanolic extract from;
leaves led to the identification of four flavonoids belonging to the flavonol class:;
quercetin and its derivatives 3-O-monoglycosides hyperin and isoquercitrin, and;
3-O-diglycosides, ombuin-3-rutinoside, all previously reported for this species.;
The mixture of flavanols, catechin and epicatechin were isolated from ethanolic;
extract from roots, besides the fatty ester of sitosterol. The mixture of steroids;
campesterol, stigmasterol and β-sitosterol were identified from the stem extract.;
This study also suggests the presence of tropane alkaloids, tropacocaine and;
nortropacocaine, in the ethanolic extract from leaves of E. suberosum, reported;
for the first time in this species. In the evaluation for cathepsins K, L and V, the;
extracts (concentration of 50 mg/mL), showed significant inhibition of all;
enzymes with percentage inhibition values above 60%. The fractions showed;
significant activity against cathepsin V and L when evaluated at concentrations;
of 5 and 50 mg/mL. The quercetin flavonol showed IC50 value of 2.2 ± 0.2 μM;
against cathepsin V and low affinity for cathepsins K and L (100 μM). This is an;
important result since literature reports for flavonoids as inhibitors of cathepsin;
V are quite limited.
O presente trabalho descreve o estudo;
químico de E. suberosum, no intuito de elucidar estruturas de metabólitos;
secundários presentes nas folhas, caule e raiz, além de avaliar, por meio de;
teste in vitro, a atividade dos extratos, frações e, quando possível das;
substâncias isoladas, em busca de inibidores de catepsinas utilizando como;
ferramenta o substrato fluorogênico ZFR-MCA. Estas enzimas, também;
conhecidas como cisteíno peptidases lisossomais, estão envolvidas em;
diversos processos fisiológicos, além de estarem associadas a muitas;
condições patológicas, estando as catepsinas K, L e V, envolvidas no;
desenvolvimento de doenças como osteoporose, câncer de pele e;
aterosclerose, respectivamente. Baseado nos processos patológicos em que;
estas catepsinas estão envolvidas, a busca de inibidores específicos pode ser;
uma nova abordagem para o tratamento destas doenças. O estudo do extrato;
etanólico das folhas levou a identificação de quatro flavonoides pertencentes à;
classe dos flavonois, sendo estes a quercetina e seus derivados 3-Omonoglicosídeos;
hiperina e isoquercitrina e 3-O-diglicosídeo, ombuina-3-;
rutinosídeo, todos já relatados para esta espécie. Do extrato etanólico da raiz,;
foi isolada a mistura dos flavanois catequina e epicatequina, além do éster;
graxo do β-sitosterol. No caule foram identificados a mistura dos esteroides;
campesterol, estigmasterol e β-sitosterol. Este estudo também sugere a;
presença dos alcaloides tropanos, tropacocaína e nortropacocaína no extrato;
etanólico das folhas, sendo estes relatados pela primeira vez na espécie. Nos;
ensaios frente às catepsinas K, L e V, todos os extratos apresentaram inibição;
superior a 60% quando avaliados na concentração de 50 μg/mL. Já as frações;
oriundas da partição líquido-líquido, apresentaram inibição mais expressiva;
frente às catepsinas V e L, quando avaliadas nas concentrações de 5 e 50;
μg/mL. O flavonol quercetina apresentou um valor de IC50 de 2,2 ± 0,2 μM para;
a catepsina V e baixa afinidade para as catepsinas K e L quando avaliado na;
concentração de 100 μM. Este é um resultado importante, uma vez que os;
relatos na literatura para flavonoides como inibidores de catepsinas são;
bastante restritos.
