In Vitro Anthelminthic Activity and Ultrastructural Analysis of Barbatic Acid against Schistosomulae and Juvenile Worms of Schistosoma mansoni**

Schistosomiasis affects about 260 million people worldwide and the search for new schistosomicidal compounds is urgent. In this study we evaluated the in vitro effect of barbatic acid against schistosomulae and young worms of Schistosoma mansoni. The barbatic acid was evaluated through the bioassay of motility and mortality, cellular viability and ultrastructural analysis of juvenile stages through Scanning Electron Microscopy. Barbatic acid showed a schistosomicidal effect against schistosomulae and young worms of S. mansoni after 3 h of exposure. At the end of 24 h, barbatic acid showed 100 %, 89.5 %, 52 % and 28.5 % of lethality for schistosomulae at the concentrations of 200, 100, 50 and 25 μM, respectively. For young worms, barbatic acid showed 100 % and 31.7 % of lethality at the concentrations of 200 and 100 μM, respectively. Motility changes were observed at all sublethal concentrations. There was a significant reduction in the viability of young worms after exposure to barbatic acid at 50, 100 and 200 μM. Extensive damage to the schistosomulae and young worm's tegument, was observed from 50 μM. This report provides data showing the schistosomicidal effect of barbatic acid on schistosomulae and young worms of S. mansoni, causing death, motility changes and ultrastructural damage to worms.     

Evaluation of the in vitro activity of dermaseptin 01, a cationic antimicrobial peptide, against Schistosoma mansoni

Schistosomiasis is a neglected tropical disease that remains a considerable public health problem worldwide. Since the mainstay of schistosomiasis control is chemotherapy with a single drug, praziquantel, drug resistance is a concern. Here, we examined the in vitro effects of dermaseptin 01 (DS 01), an antimicrobial peptide found in the skin secretion of frogs of the genus Phyllomedusa, on Schistosoma mansoni adult worms. DS 01 at a concentration of 100 μg/ml reduced the worm motor activity and caused the death of all worms within 48 h in RPMI 1640 medium. At the highest sublethal concentration of antimicrobial peptide (75 μg/ml), a 100% reduction in egg output of paired female worms was observed. Additionally, DS 01 induced morphological alterations on the tegument of S. mansoni, and a quantitative analysis carried out by confocal microscopy revealed extensive destruction of the tubercles in a dose-dependent manner over the concentration range of 50-200 μg/ml. It was the first time that an anthelmintic activity towards schistosomes has been reported for a dermaseptin.     

Essential Oils from Piper caldense C. DC. and Piper xylosteoides (Kunth) Steud.: Seasonal Variation of the Chemical Composition and Antimicrobial Activity

The essential oils (EOs) chemical composition can be affected by several environmental factors, impacting their desired biological activities. In this sense, this work aimed to evaluate the seasonal variation of the chemical composition and antimicrobial activity of Piper caldense and Piper xylosteoides leaves EOs. Their chemical composition was determined by GC/MS and GC-FID analyses, resulting in the identification of eighty compounds. P. caldense EOs were mainly consisted of sesquiterpene hydrocarbons, whereas in P. xylosteoides EOs, monoterpene hydrocarbons were predominant. EOs from both species strongly inhibited B. subtilis (MIC=0.25 mg mL⁻¹), while only P. caldense EOs showed strong activity against S. aureus (MIC=0.50 mg mL⁻¹). P. caldense spring EO showed the broadest spectrum of antimicrobial action amongst all samples. For each species, PCA seasonally differentiated EOs chemical composition. In addition, as expected, PCA of all samples showed a distinction between the two species. This study has successfully demonstrated the importance of evaluating the seasonal variation of EOs chemical composition and antimicrobial activity in obtaining a product with the desired properties.     

Chemical Profile and Biological Activities of Fungal Strains Isolated from Piper nigrum Roots: Experimental and Computational Approaches

The current report describes the chemical investigation and biological activity of extracts produced by three fungal strains Fusarium oxysporum, Penicillium simplicissimum, and Fusarium proliferatum isolated from the roots of Piper nigrum L. growing in Vietnam. These fungi were namely determined by morphological and DNA analyses. GC/MS identification revealed that the EtOAc extracts of these fungi were associated with the presence of saturated and unsaturated fatty acids. These EtOAc extracts showed cytotoxicity towards cancer cell lines HepG2, inhibited various microbacterial organisms, especially fungus Aspergillus niger and yeast Candida albicans (the MIC values of 50–100 μg/mL). In α-glucosidase inhibitory assay, they induced the IC₅₀ values of 1.00-2.53 μg/mL were better than positive control acarbose (169.80 μg/mL). The EtOAc extract of F. oxysporum also showed strong anti-inflammatory activity against NO production and PGE-2 level. Four major compounds linoleic acid (37.346 %), oleic acid (27.520 %), palmitic acid (25.547 %), and stearic acid (7.030 %) from the EtOAc extract of F. oxysporum were selective in molecular docking study, by which linoleic and oleic acids showed higher binding affinity towards α-glucosidase than palmitic and stearic acids. In subsequent docking assay with inducible nitric oxide synthase (iNOS), palmitic acid, oleic acid and linoleic acid could be moderate inhibitors.     

A Review on Metabolites from Onchidium Genus: Chemistry and Bioactivity

The Onchidium genus (Mollusca, Gastropoda, Pulmonata, Systellommatophora, Onchidiidae family) is used as the important economical shellfish, due to the high nutritional value and medicinal value. Research over the previous decades indicated that Onchidium sp. mainly contains polypropionates, depsipeptides, terpenoids and other chemical components. Many biological activities of Onchidium (e. g., cytotoxic activities against tumor cells, anti-viral and anti-bacterial activities) have been reported. This review reports a total of 60 compounds, synthetic work and biological studies on Onchidium genus, covering the literature from 1978 to date, with a view to providing a reference and helping for the in-depth research of this genus.     

Natural Multi‐Target Inhibitors of Cholinesterases and Monoamine Oxidase Enzymes with Antioxidant Potential from Skin Extracts of Hypsiboas cordobae and Pseudis minuta (Anura: Hylidae)

Alzheimer's disease (AD) is the most common cause of dementia, characterized by loss of selective neuronal and normal brain functions. Every year, ten million new cases are diagnosed worldwide. AD is a complex disease associated with all kind of different pathways, making their simultaneous modulation necessary. Nowadays anti‐AD treatments are focused on enzymatic inhibitors. The study of the amphibians’ skin had acquired great importance in the fields of biology and human health and represents an attractive and novel source for natural compounds with high potential in the development of new drugs. The present work exhibits the power of amphibian skins as a source of bioactive compounds. Herein we report the activity of extracts of two species from Hylidae family (H. cordobae and P. minuta) as reversible inhibitors of acetylcholinesterase and butyrylcholinesterase enzymes. Furthermore, the extracts inhibit MAO?B enzyme and showed antioxidant activities, acting on four important pathways of AD.