Protective effect of aqueous extract, fractions and phenolic compounds of Hancornia speciosa fruits on the inflammatory damage in the lungs of mice induced by Tityus serrulatus envenomation.

Scorpion envenomation has been considered a public health issue around the world. Tityus serrulatus represents a specie of major medical importance in Brazil due to mortality rates of approximately 1% among children and elderly populations. The aim of this work was to evaluate the in vivo anti-inflammatory potential of aqueous extract from Hancornia speciosa fruits, its fractions and its phenolic compounds against T. serrulatus envenomation. After receiving the T. serrulatus venom (TsV, 0.8 mg/kg) intraperitoneally, the animals were treated intravenously with the aqueous extract (20, 30 and 40 mg/kg), the arachnid antivenom (50 µL/animal), the dichloromethane, ethyl acetate and n-butanol fractions (20 mg/kg) as well as rutin and chlorogenic acid (2, 2.5 and 5 mg/kg). The treatment with the aqueous extract, fractions and phenolic compounds decreased the migration of leukocytes to the peritoneal cavity and reduced the levels of IL-1ß, IL-6 and IL-12. Moreover, the pulmonary histopathologic analysis showed a reduction in both interstitial and alveolar edema, as well as in the leukocytes infiltration and vascular ectasia in the mice's lungs, which evidences a protective effect attributed to H. speciosa. This is the first study that demonstrates the inhibitory potential of the aqueous extract from H. speciosa fruits against inflammation induced by TsV. These findings suggest that the bioactive compounds from the aqueous extract, especially chlorogenic acid and rutin, are responsible for the reported anti-inflammatory activity of H. speciosa.

Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content.

PURPOSE: Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaiba oil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil. METHOD: Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed. RESULTS: Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained. CONCLUSION: O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.

Genotoxicity induced by saponified coconut oil surfactant in prokaryote systems.

Surfactants are amphiphilic substances with special properties and chemical structures that allow a reduction in interfacial tension, which permits an increase in molecule solubilization. The critical micelle concentration (CMC) is an important characteristic of surfactants that determines their aggregate state, which is generally related to its functional mechanism. In this work the genotoxic potential of saponified coconut oil (SCO), a surfactant obtained from Cocos nucifera, was analyzed using prokaryote systems. DNA strand breaks were not observed after treatment of a plasmid with SCO. Negative results were also obtained in the SOS Chromotest using Escherichia coli strains PQ35 and PQ37. A moderate toxicity of SCO was observed after treatment of strain CC104 with a concentration above its CMC, in which micelles were found. Nevertheless, this treatment was not cytotoxic to a CC104mutMmutY strain. Furthermore, in this DNA repair-deficient strain treatment with a SCO dose below its CMC, in which only monomers were found, demonstrated the possibility of an antioxidant effect, since a reduction in spontaneous mutagenesis frequency was observed. Finally, in an Ames test without metabolic activation mutagenicity induction was observed in strains TA100 and TA104 with treatment doses below the CMC. The cytotoxic, antioxidant and mutagenic effects of SCO can be influenced by the aggregational state.