Purification and Preliminary Crystallographic Analysis of a New Lys49-PLA2 from B. Jararacussu

BjVIII is a new myotoxic Lys49-PLA2 isolated from Bothrops jararacussu venom that exhibits atypical effects on human platelet aggregation. To better understand the mode of action of BjVIII, crystallographic studies were initiated. Two crystal forms were obtained, both containing two molecules in the asymmetric unit (ASU). Synchrotron radiation diffraction data were collected to 2.0 Å resolution and 1.9 Å resolution for crystals belonging to the space group P212121 (a = 48.4 Å, b = 65.3 Å, c = 84.3 Å) and space group P3121 (a = b = 55.7 Å, c = 127.9 Å), respectively. Refinement is currently in progress and the refined structures are expected to shed light on the unusual platelet aggregation activity observed for BjVIII

Purification And Preliminary Crystallographic Analysis Of A New Lys49-pla2 From B. Jararacussu.

BjVIII is a new myotoxic Lys49-PLA2 isolated from Bothrops jararacussu venom that exhibits atypical effects on human platelet aggregation. To better understand the mode of action of BjVIII, crystallographic studies were initiated. Two crystal forms were obtained, both containing two molecules in the asymmetric unit (ASU). Synchrotron radiation diffraction data were collected to 2.0 A resolution and 1.9 A resolution for crystals belonging to the space group P2(1)2(1)2(1) (a = 48.4 A, b = 65.3 A, c = 84.3 A) and space group P3(1)21 (a = b = 55.7 A, c = 127.9 A), respectively. Refinement is currently in progress and the refined structures are expected to shed light on the unusual platelet aggregation activity observed for BjVIII.9736-5

Cytotoxicity Of Active Ingredients Extracted From Plants Of The Brazilian Cerrado"."

Cytotoxicity assays are needed for the screening of natural products with potential anti-inflammatory. The purpose of this study was to compare the basal cytotoxicity of active ingredients extracted from plants of the Brazilian cerrado. The viability was assayed with the neutral red uptake assay in Mac Coy cells after 24h of exposition. The dose evaluated was 50 microg/microL. The test substances were: cinnamic acid, p-coumaric acid, chlorogenic acid, syringic acid, vannilic acid, homogentisic acid, scandenin, palustric acid, diosgenin, cabraleone. Studies of cytotoxicity demonstrated that all active compounds evaluated have low toxicity in vitro. The substances showed cell viability above 60% for the concentration used. However, the cinnamic acid, sacandenin and palustric acid showed highest toxicity with a 50% reduction in cell viability for the dose of 50 microg/microL. Cytotoxic screening results are useful to estimate the best concentrations of those compounds with potential anti-inflammatory without their cause cell death.6983-

Modulation of the Pharmacological Activities of Secretory Phospholipase A2 from Crotalus durissus cascavella Induced by Naringin

In this work we have characterized the action of the naringin, a flavonoid found in grapefruit and known for its various pharmacological effects, which include antioxidant blood lipid lowering and anticancer activity, on the structure and biochemical activities of a secretory phospholipase A (sPLA2) from Crotalus durissus cascavella, an important protein involved in the releasinge of arachidonic acid in phospholipid membranes. sPLA2 was incubated with naringin (mol:mol) at 37 °C and a discrete reduction in the UV scanning signal and a modification of the circular dichroism spectra were observed after treatment with naringin, suggesting modifications of the secondary structure of the protein. This flavonoid was able to decrease enzymatic activity and some pharmacological effects, such as myonecrosis, platelet aggregation, and neurotoxic activity caused by sPLA2, however, the inflammatory effect was not affected by naringin. In addition, small angle X-ray scattering (SAXS) data were collected for sPLA2 and naringin-treated sPLA2 to evaluate possible modifications of the protein structure. These structural investigations have shown that sPLA2 is an elongated dimer in solution and after treatment with naringin a conformational change in the dimeric configuration was observed. Our results suggest that structural modification may be correlated with the loss of enzymatic activity and alterations in pharmacological properties