Cymbopogon citratus Protects Erythrocytes from Lipid Peroxidation in vitro.

INTRODUCTION: Essential oils are complex mixtures of volatile compounds, primarily composed of terpenes and abundant aromatic plants. For example, Cymbopogon citratus (lemongrass) is an aromatic plant that produces a monoterpene-rich essential oil, and studies show that this essential oil has excellent antioxidant activity. Erythrocytes incubated under high sugar levels are constantly exposed to reactive oxygen species, which results in the oxidation of their membranes. OBJECTIVE: The aim of this article is to investigate the antioxidant activity of lemongrass essential oil and its protective effect on erythrocytes exposed to high levels of glucose. MATERIALS AND METHODS: The essential oil was obtained by steam dragging distillation; blood cell suspensions were incubated with glucose 5, 20, 50, and 100 mmol/L. The amount of TBARS produced was measured at 532 nm. In addition, the percentage of antioxidant activity was assessed by DPPH free radical assay. RESULTS: Lemongrass essential oil showed an increase in the antioxidant activity up to 240 mg/ml, while ascorbic acid used as positive control showed a dose-dependent increase in antioxidant activity starting at 1 mmol/L up to 18 mmol/L. However, such a lemongrass dose prevented peroxidation in erythrocytes incubated under a high glucose media, whereas ascorbic acid showed a protective effect only at a concentration of 1 mmol/L. CONCLUSION: Lemongrass essential oil has high antioxidant activity compared to standard antioxidant as ascorbic acid, and also acts as a protective agent against erythrocyte lipoperoxidation due to hyperglycemia in vitro.

Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-adrenergic receptor blocking properties.

We described herein the discovery of 1-(2-(benzo[d] [1,3]dioxol-6-yl)ethyl)-4-(2-methoxyphenyl) piperazine (LASSBio-772), as a novel potent and selective alpha 1A/1D adrenoceptor (AR) antagonist selected after screening of functionalized N-phenylpiperazine derivatives in phenylephrine-induced vasoconstriction of rabbit aorta rings. The affinity of LASSBio-772 for alpha 1A and alpha 1B AR subtypes was determined through displacement of [(3)H]prazosin binding. We obtained Ki values of 0.14 nM for the alpha 1A-AR, similar to that displayed by tamsulosin (K(i) = 0.13 nM) and 5.55 nM for the alpha 1B-AR, representing a 40-fold higher affinity for alpha 1A-AR. LASSBio-772 also presented high affinity (K(B) = 0.025 nM) for the alpha 1D-AR subtype in the functional rat aorta assay, showing to be equipotent to tamsulosin (K(B) = 0.017 nM).