ABSTRACT 6-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (Ke ) 0.0070 min-1 and a short life half time of (T1/2 ) lower that 120 min. The distribution study showed that 6MC has high accumulation in the liver, and widespread distribution in all the organs evaluated.

C. viridivittatus, picudo de los cítricos está distribuido en región andina y cafetera de Colombia. Las larvas se alimentan de raíces y los adultos de hojas y flores. En tres fincas citrícolas del Valle del Cauca se aislaron y evaluaron hongos y nematodos entomopatógenos M. anisopliae y B. bassiana y Steinernema sp. y Heterorabditis sp. sobre larvas de C. viridivittatus 26, 36, 48 y 53 días de edad. En 120 de 132 muestras de suelo se encontraron 21 aislamientos de Metarhizium y Beauveria y ninguna con nematodos entomopatógenos. B. bassiana comercial, B9 y B10 causaron el 100 % de mortalidad en adultos en 4 y 4,3 días. M. anisopliae M6 y M7 causaron el 94 % y 97 % de mortalidad a los 4,3 y 5 días. Steinernema sp. UNS09 causó 65 % de mortalidad sobre larvas de 48 y 53 días de edad en siete días. No hubo diferencia entre Steinernema UNS09 y Heterorhabditis UNH16. Steinernema sp. UNS09 causó 85,7 % mortalidad a larvas de 53 días y 81,9 % y 81,1 % a larvas de 36 y 26 días y Heterorhabditis sp. UNH16 con 79 %, 81 % y 75,4 % de mortalidad sobre larvas de 36, 26 y 56 días a los siete días. En síntesis, los hongos y nematodos entomopatógenos pueden considerarse como alternativa de manejo de larvas de C. viridivittatus.

C. viridivittatus, citrus weevil distributed throughout the coffee maker and Andean region of Colombia. The larvae feed on roots and adults on leaves and flowers. On three citrus farms of the Valley were isolate and evaluated fungi and entompathogenic nematodes M. anisopliae and B. bassiana and Steinernema sp. and Heterorabditis sp. on larvae of C. viridivittatus 26, 36, 48 and 53 days of age. In 120 from 132 soil samples were found 21 fungi and none nematodes. Commercial B. bassiana B9 and B10 caused 100 % adult mortality in a time of 4.3 and 4 days. M. anisopliae M6 y M7 caused 94 % and 97 % of mortality to the 4.3 and 5 days. Steinernema sp. UNS09 caused 65 % of mortality on larvae of 48 and 53 days of age, seven days later. No were differences between UNS09 Steinernema and Heterorhabditis UNH16. Steinernema sp. UNS09 caused 85.7 % of mortality on 53 days larvae and 81.9 % and 81.1 % to larvae of 36 and 26 days. Heterorhabditis sp. UNH16 killed larvae of 36, 26 and 56 days was 79 %, 81 % and 75.4 % seven days later. In conclusion, fungi and nematodes can be an alternative to management of C. viridivittatus larvae.

Se evaluó el efecto de extractos metanólicos y acuosos de las especies vegetales Critoniella acuminata, Salvia rubescens, Phenax rugosus (Poir.) Wedd y Tabebuia chrysanta G. Nicholson sobre las enzimas elastasa y mieloperoxidasa, relacionadas con el proceso de desgranulación leucocitaria, y se determinó el potencial efecto inhibitorio directo sobre la enzima o la inhibición de la desgranulación de los neutrófilos polimorfonucleares. Los extractos de Critoniella acuminata y Salvia rubescens presentaron efectos sobre el proceso de desgranulación y la actividad de las enzimas mieloperoxidasa y elastasa; en el caso de los extractos de Phenax rugosus, estos no mostraron un efecto significativo sobre ninguna de las enzimas. De la especie Tabebuia chrysanta solamente el extracto metanólico mostró efecto sobre la inhibición de la actividad elastasa.

In this work, the effect of aqueous and methanolic extracts of the plants species Critoniella acuminata, Salvia rubescens, Phenax rugosus (Poir.) Wedd and Tabebuia chrysanta G. on the enzymes elastase and myeloperoxidase, involved in degranulation leukocyte process, was evaluated, identifying the potential direct inhibitory effect on the enzyme and/or inhibition of the desgranulation of polymorphonuclear neutrophils. Extracts of Critoniella acuminata and Salvia rubescens presented effects on the degranulation process and the inhibition of the enzyme elastase and myeloperoxidase; the extracts of Phenax rugosus do not showed significant effect. Tabebuia chrysanta methanolic extract only showed effect on inhibition of elastase activity.