Antidiarrheal activity of extracts from Maytenus gonoclada and inhibition of Dengue virus by lupeol

ABSTRACT Diarrhea is an infectious disease caused by bacterial, virus, or protozoan, and dengue is caused by virus, included among the neglected diseases in several underdeveloped and developing countries, with an urgent demand for new drugs. Considering the antidiarrheal potential of species of Maytenus genus, a phytochemical investigation followed by antibacterial activity test with extracts of branches and heartwood and bark of roots from Maytenus gonoclada were conducted. Moreover, due the frequency of isolation of lupeol from Maytenus genus the antiviral activity against Dengue virus and cytotoxicity of lupeol and its complex with β-cyclodextrins were also tested. The results indicated the bioactivity of ethyl acetate extract from branches and ethanol extract from heartwood of roots of M. gonoclada against diarrheagenic bacteria. The lupeol showed potent activity against Dengue virus and low cytotoxicity in LLC-MK2 cells, but its complex with β-cyclodextrin was inactive. Considering the importance of novel and selective antiviral drug candidates the results seem to be promising.

Pharmacological potential of Maytenus species and isolated constituents, especially tingenone, for treatment of painful inflammatory diseases

ABSTRACT Uses of medicinal plants by people around the world significantly contribute and guide biologically active compounds research that can be useful in the combat against various diseases. Due to a great chemical and structural variety found in their vegetal structures it consolidates ethnopharmacology as an important science for the pharmaceutical section. Inserted in the diversity of medicinal plants, is the Maytenus genus, whose research has already revealed lots of isolated substances which are responsible for a great variety of biological activities, among which we cite analgesic and anti-inflammatory, for the treatment of inflammatory diseases such as rheumatoid arthritis, gastritis, ulcers and gastrointestinal disorders. The aim of this review article is to make a compendium of the Maytenus genus and its isolated chemical compounds, among them tingenone. The elucidation of its mechanism of action reveals promising sources for the development of new drugs specially targeted for the treatment of painful inflammatory diseases.

Maytenus distichophylla and Salacia crassifolia: source of products with potential acetylcholinesterase inhibition

ABSTRACT The phytochemical study of the extract leaves from Maytenus distichophylla Mart. and Salacia crassifolia (Mart. ex Schult.) G. Don, Celastraceae, resulted in the isolation of 3-oxofriedelane, 3β-hydroxyfriedelane, 3β,24-dihydroxyfriedelane, 3-oxo-28,29-dihydroxyfriedelane, two mixtures of pentacyclic triterpenes (α-amyrin with β-amyrin and 3β-stearyloxy-urs-12-ene with 3β-stearyloxy-olean-12-ene), 3β-palmityloxy-urs-12-ene, the steroid β-sitosterol and its glycosylated derivative β-glucosyl-β-sitosterol, tritriacontanoic acid and the natural polymer gutta percha. The chemical structures of these constituents were established by IR, 1H and 13C NMR spectral data. Crude extracts, the mixtures of triterpenes and the isolated constituents were subjected to in vitro acetylcholinesterase inhibitory evaluation. Acetylcholinesterase inhibitory effect was observed for crude chloroform extract leaves from M. distichophylla (100%) and S. crassifolia (97.93 ± 5.63%) and for the triterpenes 3β,24-dihydroxyfriedelane (99.05 ± 1.12%), 3-oxo-28,29-dihydroxyfriedelane (90.59 ± 3.76%) and 3β-palmityloxy-urs-12-ene (97.93 ± 1.47%). The percent inhibitions induced by these natural products were very similar to those produced by physostigmine (93.94 ± 2.10%) a standard acetylcholinesterase inhibitor. Therefore, these results open perspectives for the use of these species as source of compounds with similar physostigmine pharmacological effect.

Psychotria viridis: Chemical constituents from leaves and biological properties

ABSTRACT The phytochemical study of hexane, chloroform and methanol extracts from leaves of Psychotria viridis resulted in the identification of: the pentacyclic triterpenes, ursolic and oleanolic acid; the steroids, 24-methylene-cycloartanol, stigmasterol and β-sitosterol; the glycosylated steroids 3-O-β-D-glucosyl-β-sitosterol and 3-O-β-D-glucosyl-stigmasterol; a polyunsaturated triterpene, squalene; the esters of glycerol, 1-palmitoylglycerol and triacylglycerol; a mixture of long chain hydrocarbons; the aldehyde nonacosanal; the long chain fat acids hentriacontanoic, hexadecanoic and heptadenoic acid; the ester methyl heptadecanoate; the 4-methyl-epi-quinate and two indole alkaloids, N,N-dimethyltryptamine (DMT) and N-methyltryptamine. The chemical structures were determined by means of spectroscopic (IR, 1H and 13C NMR, HSQC, HMBC and NOESY) and spectrometric (CG-MS and LCMS-ESI-ITTOF) methods. The study of biologic properties of P. viridis consisted in the evaluation of the acetylcholinesterase inhibition and cytotoxic activities. The hexane, chloroform, ethyl acetate and methanol extracts, the substances 24-methylene-cycloartanol, DMT and a mixture of 3-O-β-D-glucosyl-β-sitosterol and 3-O-β-D-glucosyl-stigmasterol showed cholinesterase inhibiting activity. This activity induced by chloroform and ethyl acetate extracts was higher than 90%. The methanol and ethyl acetate extracts inhibit the growth and/or induce the death of the tumor cells strains B16F10 and 4T1, without damaging the integrity of the normal cells BHK and CHO. DMT also demonstrated a marked activity against tumor cell strains B16F10 and 4T1.

Analysis of monotherapy prostate brachytherapy in patients with prostate cancer. Initial PSA and Gleason are important for recurrence?

Purpose To evaluate the clinical outcome of a cohort of localized prostate cancer patients treate with 125-I permanent brachytherapy at the São José Hospital – CHLC, Lisbon. Materials and Methods A retrospective analysis was carried out on 429 patients with low and intermediate-risk of prostate adenocarcinoma, according to the recommendations of the EORTC, who underwent 125I brachytherapies in intraoperative dosimetry “real-time” system between September 2003 and September 2013. Results The mean follow-up was 71.98 months. Biochemical relapse of disease by rising PSA (Phoenix criterion) was observed in 18 patients (4.2%). Through the application of Kaplan-Meier survival curves in this sample, the rate of survival at 6 years without biochemical relapse was higher than 95%. By Iog rank test comparing biochemical relapse with initial PSA (15-10 and <10) and Gleason values (7 and <7), there was no statistical difference (P=0.830) of the initial PSA in the probability of developing biochemical relapse. In relation to Gleason score, it was noted a statistical difference (P<0.05), demonstrating that patients with Gleason 7 are more likely to develop biochemical relapse. Conclusions Brachytherapy as monotherapy is at present an effective choice in the treatment of localized prostate adenocarcinoma. Biochemical relapses are minimal. The initial PSA showed no statistically difference in the rate of relapses, unlike the value Gleason, where it was demonstrated that patients with Gleason 7 have a higher probability of biochemical relapse. Cases with PSA bounce should be controlled before starting a salvage treatment. .

Efetividade de um programa de exercícios no condicionamento físico, perfil metabólico e pressão arterial de pacientes hipertensos / Exercise program effectiveness on physical fitness, metabolic profile and blood pressure of hypertensive patients

HISTÓRICO E OBJETIVO: Tem sido mostrado que exercícios aeróbios são úteis na redução da pressão arterial. Contudo, a efetividade de um programa de exercícios ainda é controversa e não foi bem analisada em populações de baixa renda. O objetivo do presente estudo foi estabelecer um programa de condicionamento físico individualizado - Projeto Hipertensão - focado em pessoas hipertensas, pacientes da Unidade Básica de Saúde (UBS) e, logo após, investigar os efeitos deste programa no condicionamento físico, perfil metabólico e níveis de pressão. MÉTODOS: Dezesseis mulheres hipertensas (56 ± 3 anos) sob tratamento farmacológico regular foram submetidas a 4 meses de um programa de exercícios aeróbios e de alongamento (3 sessões/semana, 90 min/sessão, 60 por cento de VO2max.) Diversas variáveis físicas e metabólicas foram comparadas antes e depois de 4 meses de treinamento. RESULTADOS: O treinamento diminuiu significativamente a pressão arterial sistólica (PAS, -6 por cento); melhorou o condicionamento cardiorrespiratório (+42 por cento do VO2max), flexibilidade (+11 por cento) e conteúdo de glicose plasmática (-4 por cento). IMC e por cento de gordura não tiveram modificação. Além de modificar o perfil metabólico, observou-se que o treinamento apresentou correlações significativas entre os valores iniciais individuais de nível de colesterol total (CT), lipoproteína de alta densidade (HDL-C) e lipoproteína de baixa densidade (LDL-C) e suas respostas após exercício. CONCLUSÕES: O estudo mostra que programas de exercício podem ser personalizados para pacientes hipertensos da UBS e confirma a efetividade do exercício na PA, condicionamento físico, flexibilidade e perfil lipídico em pacientes hipertensos. A redução expressiva de PA em sujeitos hipertensos sugere que esta intervenção de exercícios deve ser enfatizada em outros centros que assistam populações de baixa renda.

BACKGROUND AND OBJECTIVE: It has been shown that aerobic exercise is useful to reduce arterial pressure, however, the effectiveness of an exercise program is still controversial and not very well analyzed among populations with low-income. The objective of the present study was to set up an individualized physical fitness program - Projeto Hipertensão - focused on hypertensive people, patients from a Health Basic Unit (HBU) and, after that, to investigate the effects of this program on physical fitness, metabolic profile and pressure levels. METHODS: Sixteen hypertensive women (56 ± 3yrs) under regular pharmacological treatment underwent 4 months of a supervised aerobic and stretching exercise program (3 sessions/wk, 90 min/session, 60 percent of VO2 max). Several physical and metabolic variables were compared before and after 4 months of training. RESULTS: Training significantly reduced systolic arterial pressure (SAP, -6 percent), improved cardiorespiratory fitness (+42 percent of VO2max), flexibility (+11 percent) and plasma glucose content (-4 percent). BMI and percent fat did not change. Besides modifying metabolic profile, it was found that training presented significant correlations between individual initial values of cholesterol total level (CT), high density lipoprotein (HDL-C) and low density lipoprotein (LDL-C) and its responses after exercise. CONCLUSIONS: The study shows that exercise programs can be personalized for hypertensive patients from a HBU and confirms the effectiveness of exercise on AP, physical fitness, flexibility and lipid profile on hypertensive patients. The expressive reduction of AP in hypertensive subjects suggests that this exercise intervention should be emphasized on other health centers which assist low-income population.