Byrsonima sericea is a species native to Brazil that is widely used in traditional medicine. The seed ethanol extract (SEE) had the highest content of total phenols (179.35 mg GAE g−1 extract) and ...flavonoids (10.42 mg QE g−1 extract) and was the most active in relation to antioxidant activity (DPPH: IC50=4.25 μg mL−1 and ABTS: IC50=4.82 μg mL−1). The peel/pulp ethanol extract (PEE) had the best anticholinesterase activity (IC50=6.02 μg mL−1). Chromatographic investigation identified gallic acid, isoquercitrin, quercetin and amentoflavone in SEE, and gallic acid, isoquercitrin, quercetin and rutin in PEE. Six fatty acid methyl esters and seven triterpenes were identified, highlighting oleic acid in the seed hexane extract (61.85 %) and in the peel/pulp hexane extract (52.61 %), and betulin in the peel/pulp hexane extract (5.25 %). The substances and biological activities identified in B. sericea characterize this fruit as a functional food for future studies.
This work describes the production of lipases from endophytic fungi: Vermisporium-like, Emericella nidulans, Dichotomophtora portulacae and D. boerhaaviae and the biological activity against the ...dermatophyte fungi Malassezia sp and Microsporum canis and the parasite Leishmania amazonensis. All fungal enzymes extract showed lipolysis action in the media that contains long carbon chain lipids. The proteomic analysis of lipases exhibits several molecules mostly ranging in size from 220 to 20 kDa, with clear differences in protein profile's yield. All fungal enzymes were competent to eliminate promastigote forms of Leishmania amazonensis at 5 mg.mL-1. The antileishmanial activity of lipases from Vermisporium-like, E. nidulans, D. portulacae and D. boerhaaviae in amastigote forms, promoted the reduction in viability of 78.88, 39.65, 63.17 and 98.13%, with selectivity index of 19.56, 30.68, 18.09 and 20.99. In relation to antifungal activity, Dichothomophtora enzymes demonstrate best action with MFC of 14.65 μg.mL-1 against Malassezia sp and Microsporum canis, respectively. These results allow us to infer that lipases from entophytic fungi displays activity against dermatophyte fungi (Malassezia sp. and Microsporum canis) as well as Leishmania.
In this study, the chemical composition of the essential oil (EO) extracted from Croton blanchetianus Baill leaves was identified, and antimicrobial and antibiofilm activities against Staphylococcus ...aureus, Staphylococcus epidermidis, and Escherichia coli strains were determined. Moreover, the effects of EO in combination with ampicillin and tetracycline were investigated. Thirty‐four components, mainly mono‐and sesquiterpenes that represented 94.05 % of the chemical composition, were identified in the EO. The EO showed bacteriostatic and bactericidal activities against all strains tested. Furthermore, the EO showed a synergistic effect with ampicillin and tetracycline. EO significantly inhibited biofilm formation and reduced the number of viable cells in biofilms. The EO may be a promising natural product for preventing bacterial biofilm infections.
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•Mentha essential oils are rich in oxygenated monoterpenes.•The better antioxidant essential oils present piperitenone oxide as the major constituent.•Mentha spicata (Ciudad del Leste ...mint), which showed the best antifungal activity, contains pulegone as main constituent.
The plants of the genus Mentha are widely used in cooking, cosmetics and popular medicine. The present work analyzes the chemical composition of the essential oils of several Mentha species, and evaluates some functional properties such as antioxidant, anticholinesterase and antifungal, to corroborate their medicinal use. The oils obtained by hydrodistillation showed higher levels of the monoterpenes limonene, isomenthone, menthol, menthofuran, d-neoisomenthol, 1,8-cineole (eucalyptol), d-carvone, linalool, linalyl acetate, piperitenone oxide and pulegone. The essential oil of Mentha longifolia (Himalayan silver mint) stood out for its antioxidant activity with IC50 of 0.86±0.01mg/mL by the DPPH method and 0.64±0.02mg/mL by the method of β-carotene/linoleic acid system. Mentha piperita oils (chocolate mint) and Mentha spicata (menthol mint) showed good inhibition of acetylcholinesterase, with enzyme inhibition zones of 1.0cm and 0.9cm, respectively. The antifungal activity of Mentha essential oils showed moderate activity against Trichophyton rubrum and Microsporum canis, and the oil of M. spicata (Ciudad del Leste mint) showed MIC and MFC near to the control. The major components of the essential oils could be responsible for evaluated activities, which are associated with the medicinal properties reported for Mentha species.
The mosquitoes
and
are vectors of arboviruses that cause dengue, zika and chikungunya. Bioactive compounds from plants are environmentally sustainable alternatives to control these vectors and thus ...the arboviruses transmitted by them. The present study evaluated the larvicidal activity of an acetogenin-rich fraction (ACERF) and its main constituent annonacin obtained from
seeds on
and
. The larvicidal assays were performed using different concentrations to calculate the LC
and LC
values observed 24 h after exposure to the treatment. Annonacin was more active against
(LC
2.65 μg·mL
) in comparison with
(LC
8.34 μg·mL
). In contrast, the acetogenin-rich fraction was more active against
(LC
3.41 μg·mL
) than
(LC
12.41 μg·mL
). ACERF and annonacin treated larvae of
and
showed significant differences in the inhibition of their metabolic enzymes when compared to untreated larvae. The results demonstrate the relevant larvicidal action of the acetogenin-rich fraction and annonacin showing the potential to develop new products for the control of
and
.
Thymol and eugenol derivatives as anti-leishmanial agents
In Northeastern Brazil visceral leishmaniasis is endemic with lethal cases among humans and dogs. Treatment is toxic and 5–10% of humans die ...despite treatment. The aim of this work was to survey natural active compounds to find new molecules with high activity and low toxicity against Leishmania infantum chagasi. The compounds thymol and eugenol were chosen to be starting compounds to synthesize acetyl and benzoyl derivatives and to test their antileishmanial activity in vitro and in vivo against L. i. chagasi. A screening assay using luciferase-expressing promastigotes was used to measure the growth inhibition of promastigotes, and an ELISA in situ was performed to evaluate the growth inhibition of amastigote. For the in vivo assay, thymol and eugenol derivatives were given IP to BALB/c mice at 100mg/kg/day for 30days. The thymol derivatives demonstrated the greater activity than the eugenol derivatives, and benzoyl-thymol was the best inhibitor (8.67±0.28μg/mL). All compounds demonstrated similar activity against amastigotes, and acetyl-thymol was more active than thymol and the positive control drug amphotericin B. Immunohistochemistry demonstrated the presence of Leishmania amastigote only in the spleen but not the liver of mice treated with acetyl-thymol. Thus, these synthesized derivatives demonstrated anti-leishmanial activity both in vitro and in vivo. These may constitute useful compounds to generate new agents for treatment of leishmaniasis.
Grape pomace (Vitis vinifera L.), Benitaka variety, grown in the semiarid region of Northeast Brazil was evaluated in relation to chemical composition, and content of minerals and functional ...properties. Its microbiological quality and toxic potential, using Artemia salina sp, were also investigated. The results showed that the flour obtained from these residues had below neutral pH (3.82), moisture (3.33g/100g), acidity of (0.64g of citric acid/100g), and ash (4.65 g/100g). The amount of total dietary fiber (46.17g/100g) stood out quantitatively compared to the content of carbohydrate (29.2g/100 g), protein (8.49g/100g), and lipids (8.16g/100g). The total energy was 224Kcal/100g. With regard to the compounds with functional properties, higher values of insoluble fiber 79% (36.4 g/100 g); vitamin C (26.25 mg of acid ascorbic/100g), and anthocyanins (131mg/100g) were found. The minerals iron, potassium, zinc, manganese, and calcium were present in higher concentrations. There were no significant copper values. The results showed that the grape residues are an important source of nutrients and compounds with functional properties suggesting that they can be incorporated as an ingredient in the diet and/or used as a dietary supplement aiming at health benefits. The residues did not show microbiological contamination and were considered nontoxic.
Leishmaniasis is a group of neglected diseases caused by parasites of the Leishmania genus. The treatment of Leishmaniasis represents a great challenge, because the available drugs present high ...toxicity and none of them is fully effective. Caryocar is a botanical genus rich in phenolic compounds, which leaves extracts have already been described by its antileishmanial action. Thus, we investigated the effect of pulp and peel extracts of the Caryocar coriaceum fruit on promastigote and amastigote forms of Leishmania amazonensis. Both extracts had antipromastigote effect after 24, 48, and 72 h, and this effect was by apoptosis-like process induction, with reactive oxygen species (ROS) production, damage to the mitochondria and plasma membrane, and phosphatidylserine exposure. Knowing that the fruit extracts did not alter the viability of macrophages, we observed that the treatment reduced the infection of these cells. Thereafter, in the in vitro infection context, the extracts showed antioxidant proprieties, by reducing NO, ROS, and MDA levels. Besides, both peel and pulp extracts up-regulated Nrf2/HO-1/Ferritin expression and increase the total iron-bound in infected macrophages, which culminates in a depletion of available iron for L. amazonensis replication. In silico, the molecular modeling experiments showed that the three flavonoids presented in the C. coriaceum extracts can act as synergistic inhibitors of Leishmania proteins, and compete for the active site. Also, there is a preference for rutin at the active site due to its greater interaction binding strength.
Communicated by Ramaswamy H. Sarma
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•A. mucosa ethanolic extract (EEAM) showed larvicidal activity against Ae. aegypti and Ae. albopictus.•Rolliniastatin 1 was the most active substance against larvae.•Biochemical ...changes were observed in larvae treated with EEAM, rollinicin and rolliniastatin 1.•EEAM caused histological changes in the midgut of the treated larvae.•EEAM, rollinicin and rolliniastatin 1 can be used in the control of Ae. aegypti and Ae. albopictus.
Annona mucosa Jacq. (Annonaceae) is an edible plant whose fruit is appreciated in the Amazon region of Brazil. The seeds of this plant are rich sources of acetogenins, substances that have antimicrobial, anticancer, repellent, insecticide and larvicidal activities. However, studies on larvicidal evaluation of these substances are almost always limited to the species Aedes aegypti, with few studies with the species Aedes albopictus. In this research, it was investigated the larvicidal effect and mechanisms of action of the ethanolic extract and of the main constituents of Annona mucosa against Ae. aegypti and Ae. albopictus. The compounds were isolated from the ethanolic seed extract by successive silica gel chromatographic columns and characterized by NMR and Infrared spectroscopic analysis, as well as by comparison with literature data, as the acetogenins rolliniastatin 1 and rollinicin. Third- and fourth-instar larvae were submitted to different concentrations of ethanolic extract, rolliniastatin 1 and rollinicin to estimate the LC50 and LC90 after 24 h exposure. The ethanolic extract and rolliniastatin 1 were more active against Ae. albopictus, with LC50 values of 0.55 and 0.20 μg.mL−1, respectively, compared with Ae. aegypti, on which they exhibited values of 2.60 and 0.43 μg.mL−1, respectively. Rollinicin was, on the contrary, more active against Ae. aegypti (LC50 of 0.78 μg.mL−1) than against Ae. albopictus (LC50 of 1.13 μg.mL−1). Significant differences were observed among enzymatic activities of larvae treated with natural products obtained from Annona mucosa and histopathological analysis of the midgut of treated larvae suggested the existence of two action mechanisms. EEAM and main acetogenins, rolliniastatin 1 and rollinicin did not present toxicity against zebrafish. The results demonstrate the larvicidal potential of seeds ethanolic extract and acetogenins from A. mucosa as green larvicidal agents for the control of Ae. aegypti and Ae. albopictus.