A novel approach to Cestrum intermedium (mata-boi): anatomical and physical-chemical characterization, in vitro biological activities, and metabolites of a Brazilian native species

Abstract The Brazilian native species Cestrum intermedium, known as mata-boi, induces hepatotoxicity and death when ingested by cattle. While most studies on this species focus on toxicological features, our study is the first to describe the anatomy and in vitro biological activities of Cestrum intermedium. We investigated adult leaves and stems by histochemistry, described their anatomy, performed physical-chemical analysis, determined in vitro antioxidant and antimicrobial activities, and identified secondary metabolites. A few noteworthy anatomical features were the anomocytic stomata on the abaxial surface and the absence of trichomes, in addition to the circular shaped petiole with two projections on the adaxial surface. Histochemical analysis showed chemical markers such as alkaloids, usually reported as toxic, and terpenoids. Potassium nitrate (ATR-FTIR) and lupeol palmitate (NMR) were detected on the crude stem extract. Thermogravimetric and physical-chemical analysis provided fingerprint parameters for the species. Minimal Inhibitory Concentration (MIC) assay revealed that Staphylococcus aureus, Staphylococcus epidermidis, and Candida albicans were weakly inhibited by extract samples. Chloroform and ethyl acetate fractions presented high phenolic content, which resulted in in vitro antioxidant activity. These novel features expand the knowledge about this species, considering that previous studies mainly focused on its toxicity. Our study also provided characteristics that may help in avoiding misidentification between Cestrum members, especially when taxonomic keys cannot be employed, as in the absence of flowers and fruits.

Evaluation of copaiba oil as enhancer of ibuprofen skin permeation

Abstract The administration of medications on the skin through transcutaneous routes is a practice that has been used by mankind for millennia. Some studies have been reporting the use of terpenes and natural oils rich in terpenes as an enhancer of cutaneous penetration. Copaiba oil, due to its rich content of terpenes, presents itself as a great choice of penetration enhancer for drugs administered on the skin. In this study, we developed two cream formulations containing 5% of ibuprofen (IBU) and copaiba oil: IBCO5 and IBCO10 with 5% and 10% of copaiba oil respectively. Ex vivo cutaneous penetration/permeation studies of IBU were performed using pig ear skin as biological membrane in the Franz-type diffusion cells. The steady-state flux of IBU samples, IBCO5 (35.72 ± 6.35) and IBCO10 (29.78 ± 2.41) were significantly higher when compared with control without copaiba oil (10.32 ±1.52) and with a commercial product (14.44 ± 2.39). In the penetration analysis, the amount of IBU found in the samples IBCO5 and IBCO10 was markedly higher in the dermis than epidermis. Our results showed that copaiba oil possesses attracting properties in promoting skin penetration and permeation of IBU when added into cream formulations.

Molluscicidal effect of three monoterpenes oils on schistosomiasis and fascioliasis vector snails in Egypt

Thymol, Linalool and Eugenol showed considerable molluscicidal effect against Biomphalaria alexandrina, Bulinus trancatus and Lymneae natalensis. The thymol was the potent one at least LC 50 and LC 90 followed by euganol then linalool. L. natalensis were mole sensitive to these compounds followed by B. truncatus and then B. alexandrina. The LC 50 and LC 90 of thymol were 22 and 34 ppm against B. alexandrina, 20 and 30 ppm for B. truncatus and 1 8 and 29 ppm for L. natalensis. These values were higher with Eugenol, 28 and 48 ppm for B. alexnadrina, 24 and 44 ppm for B. truncatus and 22 and 40 ppm for L. natalensis. Linalool showed highest values of LC 50 and LC 90 against B. alexandrina, 34 and 56 ppm, against B. truncatus 30 and 52 ppm and for L. natalensis 28 and 48 ppm, respectively. Maintaining of B. alexandrina at LC 10 of Thymol for one week induced an inhibitory effect in the level of some enzymes [AchE, SDH]. It led to increase in the activity of other enzymes [ACP, ALP and G-6-PD]. Acetylcholine-sterase activity [AchE] of treated B. alexandrina was significantly reduced by 45.9% when compared to control. The results showed a significant decrease in succinate dehydrogenase activity [SDH] by 46.4% together with a concomitant increase in glucose-6-phosphate dehydrogenase activity level [G-6-PD] by 47.5% in comparison with control. The activities of acid phosphatase and alkaline phosphatase enzymes were found to be higher in the treated snails than in control ones. The percentage increases were 47.2% and 73.2% respectively. The results also showed an elevation in the hemolymph glucose content of treated snails by 51.9% while the tissue glycogen content was reduced by 48.1%. The infection of B. alexandrina with S. mansoni miracidia was greatly reduced by thymol LC 10 [sublethal dose]. The infection rate reduction was 43.1%. The treated snails' prepatent period was prolonged [34.2 +/- 3.3 days] compared to control [28.4 +/- 1.2 days]. A highly significant reduction of total cercarial production per snail occurred in experimental snails as compared to control

Estudo da teratogenicidade do alfa-terpinemo em ratos

Fornece dados sobre o potencial embriofeto-tóxico do alfa-terpineno no rato. O alfa-terpinemo dissolvido em óleo de milho, foi administrado por entubaçäo gástrica a ratas wistar do dia 6 ao dia 15 de gravidez. As ratas foram pesadas diariamente. No dia 21 de gestaçäo as fêmeas foram anestesiadas com éter etílico, sacrificadas por decapitaçäo e submetidas à cesariana. O n§ de sítios de implantaçäo, de fetos vivos e mortos, de reabsorçoes e de corpos lúteos gravídicos foi registrado. Todos os fetos foram pesados, examinados para malformaçoes visíveis externamente, numerados com caneta especial e fixados em soluçäo de formol a 5 por cento. Um terço dos fetos de cada ninhada, excolhidos ao acaso, foram avaliados quanto a ocorrência de anomalias viscerais por meio de uma técnica de microdissecçäo. O fígado, baço, rins, coraçäo, pulmoes e o timo dos fetos microdissecados também foram pesados. Os fetos retantes foram examinados para detecçäo de malformaçoes de esqueleto, após diafanizaçäo com hidróxido de potássio e coloraçäo com Alizarina Red S. A reduçäo de ganho de peso entre os dias 6 e 11 de gravidez, assim como durante toda a gestaçäo descontado o peso do útero gravídico, indicaram que as duas maiores doses testadas (125 e 250 mg de alfa-terpinemo/Kg peso corporal foram tóxicas para a mäe. A dose mais alta de alfa-terpinemo (250 mg/Kg de peso corporal po) reduziu a razäo entre o n§ de ratas grávidas e o n§ de ratas cruzadas. Uma frequência aumentada de sinais de retardo do crescimento fetal e uma maior incidência de malformaçoes esqueléticas de menor gravidade, foram encontradas em doses superiores a 30 mg de alfa-terpinemo/Kg de peso corporal po. A partir dos dados obtidos neste estudo experimental, o nível máximo de doses em que näo se observam efeitos adversos (NOAEL) para embriofeto-toxic pode ser fixado de 30 mg de alfa-terpinemo/Kg de peso corporal po. Embora näo haja dados disponíveis sobre a exposiçäo humana ao alfa-terpinemo é razoável admitir que níveis de dose comparáveis a este NOAEL obtidos experimentalmente säo improváveis de serem atingidos quando o homem é exposto a óleos essenciais contendo o alfa-terpinemo empregados como aditivos aromatizantes em alimentos ou através do uso de remédios da medicina popular.

Empleo de la ciclosporina en la dermatitis por contacto severa / Cyclosporin in acute contact dermatitis

Tratamos a un paciente con dermatitis por contacto severa por terpenos, con ciclosporina A (CyA) 5 mg/kg/día. Durante 28 años recibió corticoides por vía general; presentaba aspecto cushingoide e hipertensión arterial. Las pruebas de fotosensibilidad e histopatología permitieron desechar un reticuloide actínico o reactor persistente a la luz. La CyA produjo involución total de las lesiones permitiendo la supresión del corticoide y sus complicaciones. Esta droga es un recurso terapéutico en dermatitis de contacto prolongadas y resistentes a otros tratamientos