Polyphenolic compounds have shown to inhibit toxic effects induced by snake venom proteins. In this work, we demonstrate that gallic acid, ferulic acid, caffeic acid, propylgallate and epigallocatechingallate inhibit the enzymatic activity of a phospholipase A2 (PLA2), using egg yolk as substrate. The IC50 values are between 0.38 – 3.93 mM. These polyphenolic compounds also inhibit the PLA2 enzymatic activity when synthetic substrate is used. Furthermore, these compounds decreased the cyotoxic effect induced by a myotoxic PLA2; specifically, epigallocatechin gallate exhibited the best inhibitory capacity with 90.92 ± 0.82%, while ferulic acid showed the lowest inhibitory activity with 30.96 ± 1.42%. Molecular docking studies were performed in order to determine the possible modes of action of phenolic compounds. All polyphenols showed hydrogen bonds with an active site of enzyme; moreover, epigallocatechingallate presented the strongest binding compared with the other compounds. Additionally, a preliminary structure-activity relationship analysis showed a correlation between the IC50 and the topological polar surface area of each compound (p = 0.0491, r = -0.8079 (-0.9878 to -0.2593)), which indicates the surface area required for each molecule to bind with the majority of the enzyme. Furthermore, our results show that propylgallate and epigallocatechingallate are two novel natural products with anti-myotoxic potential. The topical application of these plant polyphenols at the bite site could lead to prevent myotoxicity; however, further in vivo studies would be necessary to confirm the in vitro results.
Biomass recovery through secondary succession in the Cordillera Central de los Andes, Colombia. Estimations on biomass recovery rates by secondary tropical forests are needed to understand the complex tropical succession, and their importance on CO 2 capture, to offset the warming of the planet. We conducted the study in the Porce River Canyon between 550 and 1 700m.a.s.l. covering tropical and premontane moist belts. We established 33 temporary plots of 50mx20m in secondary forests, including fallows to succesional forests, and ranging between 3 and 36 years old; we measured the diameter at breast height (D) of all woody plants with D≥5cm. In each one of these plots we established five 10mx10m subplots, in which we measured the diameter betweem 1cm≤D<5cm of all woody plants. We estimated the biomass of pastures by harvesting 54 plots of 2mx2m, and of shrubs in the fallows by harvesting the biomass in 18 plots of 5mx2m. We modeled Bav (above ground live biomass of woody plants) and Brg (coarse root biomass) as a function of succesional age (t) with the growth model of von Bertalanffy, using 247t/ha and 66t/ha as asymptote, respectively. Besides, we modeled the ratios brg/bav=f(D) and Brg/Bav=f(t). The model estimated that 87 years are required to recover the existing Bav of primary forests through secondary succession, and 217 years for the Brg of the primary forest. The maximum instantaneous growth rate of the Bav was 6.95 t/ha/yr at age 10. The maximum average growth rate of the Bav was 6.26 t/ha/yr at age 17. The weighted average of the absolute growth rate of the Bav reached 4.57t/ha/yr and the relative growth rate 10% annually. The ratio brg/bav decreases with increasing D. The ratio Brg/Bav initially increases very rapidly until age 5 (25%), then decreases to reach 25 years (18%) and increases afterwards until the ratio reaches the asymptote (26.7%).
Envenomation by snakes of the genus Bothrops are a health problem in some tropical countries, not only because of the mortality but given the high percentage of physical disabilities it causes. Phospholipases A2 (PLA2) are abundant constituents in bothropic and crotalic venoms, characterized by inducing irreversible muscle damage. Due to the contribution of plants in the snakebite treatment, we focus on the search of phospholipases inhibitors, either as an alternative treatment or as a therapeutic adjuvant of the current treatments. From a screening of 37 vascular plants and bryophytes in the search for such inhibitors, the species Murraya paniculata was selected due to its promising preliminary activity. Starting from this point further work consisting of bioassay-guided fractionation followed by the evaluation of the inhibitory activity of PLA2, the metabolites responsible for the activity were detected through a tandem of gas chromatography - mass spectrometry in the most active fraction, to propose substrate-enzyme inhibition model. The aims of this project was the search of promising compounds with an inhibitory activity of the PLA2 in vascular plants such as M. paniculata, that could become tools for developing new products to improve the prognosis of the snakebite.
Objetivo. Describir las características demográficas e inmunofenotípicas de los clones de HPN en pacientes con anemia aplásica.
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