Pharmacological Characteristics of the Hydroethanolic Extract of Acmella oleracea (L) R. K. Jansen Flowers: ADME/Tox In Silico and In Vivo Antihypertensive and Chronic Toxicity Evaluation.

Acmella oleracea (L.) R. K. Jansen, popularly known as jambu in Northern Brazil, is widely used in folk medicine and local cuisine. Its consumption in different ways reinforces the need for safety assessments. In this study, the major compounds found in the hydroethanolic extract of A. oleracea flowers (EHFAO) were characterized by ultra-performance liquid mass spectrometry (UHPLC-ESI-QTOF-MS/MS). The effects of oral administration of 100/mg/kg of EHFAO extract over 60 days in male spontaneously hypertensive (SHR) and Wistar (WR) rats and the in silico ADME/Tox predictions, lipophilicity, and water solubility were accomplished for the compounds identified. Spilanthol was detected as the foremost major compound at a concentration of 97.7%, followed by 1.53% scopoletin and 0.77% d-limonene. The treatment with EHFAO did not alter the animals´ weight over the studied period. Moderate alterations were observed solely in the hepatic enzymes AST (WR = 97 UI/L and SHR = 150 UI/L ∗ p < 0.05) and ALT (WR = 55 UI/L and SHR = 95 UI/L ∗ p < 0.05), while no relevant histopathological alterations were found. The in-silico study confirmed the in vivo findings, as the identified compounds were considered highly bioactive orally, due to their drug similarity profiles, adequate lipid solubility, bioavailability, and pharmacokinetics. Therefore, the chronic treatment with EHFAO was found safe at the concentration of 100/mg/kg, with no interference in the blood pressure levels neither appreciable toxic effects.

Antimicrobial Prenylated Isoflavones from the Leaves of the Amazonian Medicinal Plant Vatairea guianensis Aubl.

Vatairea guianenis Aubl. (Fabaceae) is an Amazonian medicinal plant species traditionally used for treating skin diseases. In an initial screening, a V. guianensis leaf extract and its subextracts showed antibacterial and antifungal activities. The EtOAc subextract was selected for chemical workup and afforded five known (1-4 and 8) and six undescribed isoflavones, vatairenones C-H (5-7 and 9-11). All isoflavones are prenylated in position C-8, displaying either chain-prenylated (1-7) or ring-closed forms (8-11). The most bioactive compound (3) exhibited in vitro activity against clinically relevant bacteria and fungi with IC50 values ranging from 6.8 to 26.9 µM. Due to its broad antimicrobial activity and low general toxicity, compound 3 is a potential lead compound for structural modifications. The results of the present study support the ethnomedicinal use of V. guianensis in the treatment of dermatological disorders. 1H NMR spectra of some of the isolated compounds showed intricate signal patterns, which might explain repeated errors in assigning the correct structure of the isoflavonoid B-ring in the literature and which we resolved by higher order spectra simulations.

HTLV-1/2 prevalence in two Amazonian communities.

INTRODUCTION: The human T-cell lymphotropic virus type 1 (HTLV-1) is aetiologically linked to myelopathy/tropical spastic paraparesis (HAM/TSP) and adult T cell leukaemia (ATL) besides other less incident pathologies, while the type 2 has not been definitively linked to any diseases. OBJECTIVES: To determine the HTLV-1/2 seroprevalence in two Brazilian communities in northern Brazil. METHODS: In 2010 and 2015, HTLV-1/2 serological surveys were carried out in the Oiapoque county at the Brazilian border with French Guiana and in Santa Cruz do Arari, Marajó Island. Serum and breast-milk samples from 317 women (pregnant, lactating and non-pregnant non-lactating) resident in the Oiapoque county, together with serum samples from 217 females and 70 males living in Santa Cruz do Arari county, were twice screened by two distinct commercial immunoassay methods for antibodies to HTLV-1/2. Seroreactivity was confirmed by a commercial Western blot technique. Participants were interviewed for data concerning their health, socioeconomic and educational status. RESULTS: None of the Oiapoque women, mostly young and descendants of migrants, had antibodies to HTLV-1/2, despite the high HTLV-1 prevalence in neighbouring French Guiana and Caribbean Islands, while five females and three males living in Santa Cruz do Arari county were HTLV-1 infected as confirmed by Western blot testing. In contrast, the Santa Cruz do Arari community lives in relative isolation and is descended mostly from black African people with high consanguinity. CONCLUSION: Despite the proximity between Oiapoque and Santa Cruz do Arari counties, ethnic, age differences, community isolation and consanguinity may explain the distinct HTLV-1/2 epidemiology in these areas of northern Brazil.

Antimicrobial activity of amazonian medicinal plants.

OBJECTIVES: The aqueous extracts of currently utilized Amazonian medicinal plants were assayed in vitro searching for antimicrobial activity against human and animal pathogenic microorganisms. METHODS: Medium resuspended lyophilized aqueous extracts of different organs of Amazonian medicinal plants were assayed by in vitro screening for antimicrobial activity. ATCC and standardized microorganisms obtained from Oswaldo Cruz Foundation/Brazil were individually and homogeneously grown in agar plate, and holes previously perforated in the gel were filled with diluted plant aqueous extracts. Inhibition halos were evaluated and controlled by the use of the fluoroquinolone ciprofloxacin. RESULTS: The Amazonian medicinal plants, Hymenelobium petraeum showed inhibitory activity over Staphylococcus aureus, Enterococcus faecalis, Salmonella enterica serovar Typhi, Acinetobacter baumannii and Candida albicans, while Vatairea guianensis and Symphonia globulifera presented inhibitory activity exclusively for Staphylococcus aureus. Also, Ptychopetalum olacoides and Pentaclethra macroloba inhibited the growth of Klebsiella ozaenae and Acinetobacter baumannii. CONCLUSION: The aqueous botanic extracts that showed activity against microroganisms of ATTC and Osvaldo Cruz strains had at least 40% of antimicrobial activity when compared to halo inhibition produced by the commercial antibiotic ciprofloxacin utilized as a control. Of all plants extracts assayed, the Hymenelobium petraeum had the best performance, sometimes exhibiting higher activity than ciprofloxacin. It is not well-defined by the physicians the exact indication of the majority of medicinal plants in the Amazon area in Brazil. Natives utilize the plants according to their symptoms, based on the traditional knowledge transmitted orally from generation to generation, among Amerindians, Afrodescendents and ethnic mixed populations. A significant number of Amazonian medicinal plants are totally unknown related to their medicinal properties including mechanism of action and therapeutic effects, as very few information is reported in the scientific literature. A tiny amount of data is presented, as the preliminary antimicrobial properties of the medicinal plants here accessed, under the urgent necessity of new antibiotics in the market and in face of the increased resistance of infectious microorganisms to antimicrobials.