Correlations among neck circumference and anthropometric indicators to estimate body adiposity in people living with HIV

Abstract INTRODUCTION: Neck circumference (NC) and anthropometric data of people living with HIV (PLWH) are correlated. METHODS: Socioeconomic, NC, body mass index (BMI), tricipital skinfold thickness (TSF), mid-arm circumference (MAC), mid-arm muscle circumference (MAMC), waist-hip ratio (WHR), waist-to-height ratio (WHtR), waist circumference (WC), and hip circumference (HC) data of 72 PLWH were correlated. RESULTS Higher adiposity was observed in NC (40.3% [n=29]) and WC (31.9% [n=23]). Correlations between NC/BMI, NC/WC, NC/HC, NC/MAC, NC/MAMC, and NC/WHtR were significant. Increased NC (40.3%[n=29]) and WC (31.9 [n=23]) were associated with higher cardiometabolic risk. CONCLUSIONS: NC correlations are adequate for estimating cardiometabolic risk.

Antibacterial substances from leaves of Protium spruceanum (Burseraceae): in vitro and in silico evaluation

Due to the increase of bacterial resistance, the search for new antibiotics is necessary and the medicinal plants represent its most important source. The aim of this study was to evaluate the antibacterial property of extract and fractions from Protium spruceanum leaves, against pathogenic bacteria. By means of diffusion and microdilution assays, the crude extract was active against the nine bacteria tested being the hydromethanolic fraction the most active. During phytochemical procedures, procyanidin (1) and catechin (2) were identified as the main antibacterial constituents of this fraction. In silico results obtained using PASSonline tool indicated 1 and 2 as having good potential to interact with different targets of currently used antibiotics. These results no indicated potential to none DNA effect and indicated the cell wall as mainly target. Electrophoresis result supported that had no DNA damage. Cell wall damage was confirmed by propidium iodide test that showed increased membrane permeability and by cell surface deformations observed in scanning electronic microscopy. The in vitro assays together with the in silico prediction results establish the potential of P. spruceanum as source of antibacterial compounds that acts on important bacterial targets. These results contribute to the development of natural substances against pathogenic bacteria and to discovery of new antibiotics.

Lupeol and its esters: NMR, powder XRD data and in vitro evaluation of cancer cell growth

ABSTRACT The triterpene lupeol (1) and some of its esters are secondary metabolites produced by species of Celastraceae family, which have being associated with cytotoxic activity. We report herein the isolation of 1, the semi-synthesis of eight lupeol esters and the evaluation of their in vitro activity against nine strains of cancer cells. The reaction of carboxylic acids with 1 and DIC/DMAP was used to obtain lupeol stearate (2), lupeol palmitate (3) lupeol miristate (4), and the new esters lupeol laurate (5), lupeol caprate (6), lupeol caprilate (7), lupeol caproate (8) and lupeol 3',4'-dimethoxybenzoate (9), with high yields. Compounds 1-9 were identified using FT-IR, 1H, 13C-NMR, CHN analysis and XRD data and were tested in vitro for proliferation of human cancer cell activity. In these assays, lupeol was inactive (GI50> 250µg/mL) while lupeol esters 2 -4 and 7 - 9 showed a cytostatic effect. The XRD method was a suitable tool to determine the structure of lupeol and its esters in solid state. Compound 3 showed a selective growth inhibition effect on erythromyeloblastoid leukemia (K-562) cells in a concentration-dependent way. Lupeol esters 4 and 9 showed a selective cytostatic effect with low GI50 values representing promising prototypes for the development of new anticancer drugs.

In vitro activity of 2-pyridinecarboxylic acid against trypanosomes of the subgenus Schizotrypanum isolated from the bat Phyllostomus hastatus / Atividade in vitro do ácido 2-piridinocarboxílico em tripanossoma do subgênero Schizotrypanum isolado do morcego Phyllostomus hastatus

The effect of 2-pyridinecarboxylic acid (picolinic acid) on trypanosomes of the subgenus Schizotrypanum isolated from the bat Phyllostomus hastatus was determined in this study. Picolinic acid, at 50 µg mL-1, inhibited epimastigote growth by 99% after 12 days incubation. In addition, trypomastigote motility decreased by 50% after 6h and completely after 24h in the presence of 50 µg mL-1 picolinic acid. The 50% cytotoxic concentration on HEp-2 cell line was 275 µg mL-1 after 4 days incubation. Altogether, these results indicate higher toxicity against trypanosomes. The inhibitory effect of picolinic acid on epimastigote growth can be partially reversed by nicotinic acid and L-tryptophan, suggesting a competitive inhibition. Furthermore, two anti-Trypanosoma (Schizotrypanum) cruzi drugs were also evaluated with regard to bat trypanosome growth. Benznidazole, at 50 µg mL-1, inhibited epimastigote growth by 90% after 12 days incubation. Nifurtimox, at the same concentration, caused 96% growth inhibition after four days incubation. Corroborating a previous study, bat trypanosomes are a good model for screening new trypanocidal compounds. Moreover, they can be used to study many biological processes common to human pathogenic trypanosomatids.

O efeito do ácido 2-piridinocarboxílico (ácido picolínico) sobre um tripanossoma do subgênero Schizotrypanum isolado do morcego Phyllostomus hastatus foi determinado neste estudo. O ácido picolínico, na concentração de 50 µg mL-1, inibiu 99% do crescimento de epimastigotas após 12 dias de incubação. Além disso, houve um decréscimo de 50 e 100% na mobilidade dos tripomastigotas após 6 e 24h, respectivamente, em presença de ácido picolínico na concentração de 50 µg mL-1. A concentração citotóxica 50% para células HEp-2 foi de 275 µg mL-1 após quatro dias de incubação. Esses resultados indicam maior toxicidade contra os tripanossomas. O efeito inibitório do ácido picolínico sobre o crescimento de epimastigotas pode ser parcialmente revertido por ácido nicotínico e L-triptofano, sugerindo inibição competitiva. Adicionalmente, o efeito de dois fármacos com atividade anti-Trypanosoma (Schizotrypanum) cruzi foi avaliado sobre o crescimento do tripanossoma de morcego. Benzonidazol, na concentração de 50 µg mL-1, inibiu 90% do crescimento de epimastigotas após 12 dias de incubação. Nifurtimox, na mesma concentração, causou 96% de inibição do crescimento após quatro dias de incubação. Corroborando trabalhos anteriores, tripanossomas de morcegos são bons modelos para seleção inicial de novos compostos tripanocidas. Além disso, eles podem ser utilizados para estudar vários processos biológicos comuns aos tripanossomatídeos patogênicos ao homem.

Anti-trypanosomal activity of pentacyclic triterpenes isolated from Austroplenckia populnea (Celastraceae)

Four pentacyclic triterpenes isolated from Austroplenckia populnea and four compounds of known anti T. cruzi or anti-malarial activity were tested. Of those triterpenes tested 20alpha-hydroxy-tingenone showed high activity, epikatonic acid was less active, while populnilic and populninic acids were inactive against the trypanosome of the subgenus Schizotrypanum tested. Benzonidazole, nifurtimox, ketoconazole and primaquine presented a remarkable dose-dependent inhibitory effect reaching practically to a total growth inhibition of the parasite at the end of incubation time. The trypanosome tested appear to be a suitable model for preliminary screen for anti T. (S.) cruzi compounds

Constituintes químicos e atividade antiespermatogênica em folhas de Austroplenckia populnea (Celastraceae)

Folhas de Austroplenckia populnea (mangabarana, marmelinho do campo) foram submetidos a estudo fitoquímico. Do extrato hexânico foram isolados e identificados três triterpenos pentacíclicos e um sesquiterpeno agarofurânico inédito. Realizou-se testes de atividade antiespermatogência utilizando parte deste extrato. Os resultados mostraram uma redução significativa do número de espermatozóides no epidídimo.