Design And Synthesis Of N-acylated Aza-goniothalamin Derivatives And Evaluation Of Their In Vitro And In Vivo Antitumor Activity.

Herein we describe the synthesis of a focused library of compounds based on the structure of goniothalamin (1) and the evaluation of the potential antitumor activity of the compounds. N-Acylation of aza-goniothalamin (2) restored the in vitro antiproliferative activity of this family of compounds. 1-(E)-But-2-enoyl-6-styryl-5,6-dihydropyridin-2(1H)-one (18) displayed enhanced antiproliferative activity. Both goniothalamin (1) and derivative 18 led to reactive oxygen species generation in PC-3 cells, which was probably a signal for caspase-dependent apoptosis. Treatment with derivative 18 promoted Annexin V/7-aminoactinomycin D double staining, which indicated apoptosis, and also led to G2 /M cell-cycle arrest. In vivo studies in Ehrlich ascitic and solid tumor models confirmed the antitumor activity of goniothalamin (1), without signs of toxicity. However, derivative 18 exhibited an unexpectedly lower in vivo antitumor activity, despite the treatments being administered at the same site of inoculation. Contrary to its in vitro profile, aza-goniothalamin (2) inhibited Ehrlich tumor growth, both on the ascitic and solid forms. Our findings highlight the importance of in vivo studies in the search for new candidates for cancer treatment.

Five Years Of Implementation Of Guidelines In Hematology And Transfusion Medicine In Brazil.

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Prevalence And Treatment Of Hypertension In Urban And Riverside Areas In Porto Velho, The Brazilian Amazon.

Abstract Introduction: Hypertension (HTN) is a preventable cause of cardiovascular morbidity and mortality. To compare the prevalence, awareness, treatment, and control of HTN among urban and riverside populations in Porto Velho, Amazon region. We conducted a cross-sectional study between July and December 2013 based on a household survey of individuals aged 35-80 years. Interviews by using a standardized questionnaire, and blood pressure (BP), weight, height, and waist circumference measurements were performed. HTN was defined when individuals reported having the disease, received antihypertensive medications, or had a systolic BP ≥ 140 mm Hg or diastolic BP ≥ 90 mm Hg. Awareness was based on self-reports and the use of antihypertensive medications. Control was defined as a BP ≤ 140/90 mm Hg. Among the 1410 participants, 750 (53.19%) had HTN and 473 (63.06%) had diagnosis awareness, of whom 404 (85.41%) received pharmacological treatment but with low control rate. The prevalence and treatment rates were higher in the urban areas (55.48% vs. 48.87% [p = 0.02] and 61.25% vs. 52.30% [p < 0.01], respectively). HTN awareness was higher in the riverside area (61.05% vs. 67.36% ; p < 0.01), but the control rates showed no statistically significant difference (22.11% vs. 23.43% ; p = 0.69). HTN prevalence was higher in the urban population than in the riverside population. Of the hypertensive individuals in both areas, <25% had controlled HTN. Comprehensive public health measures are needed to improve the prevention and treatment of systemic arterial HTN and prevent other cardiovascular diseases.