Healing activity of proteolytic fraction (P1G10) from Vasconcellea cundinamarcensis in a cutaneous wound excision model.

The proteolytic enzymes from Vasconcellea cundinamarcensis have demonstrated efficacy to accelerate healing of skin lesions. We report here the efficacy of the proteolytic fraction - P1G10 during repair of excisional wounds in rodent model and analyze possible mediators involved. Using 0.05% P1G10 we observed on day 3rd increased wound contraction accompanied by an increase in activated neutrophils and VEGF relative to the control. On day 7th neutrophils returned to normal levels, and at 0.01% P1G10, an increase in NAG activity used to monitor monocyte/macrophage, was observed. On the other hand, on day 7th, we observed a decrease in TGF-ß at 0.05% P1G10, accompanied by an increased transformation of the latent TGF-ß to its active form. Also, on day 7th a reduction in MMP-9 activity and the number of apoptotic cells was observed along with an increase in fibroblast levels. Morphometrically, it appears that treatment with P1G10 accelerates the decline of initial inflammatory phase and reduces some unwanted effects likely caused by remaining TGF-ß or MMPs, thus enhancing the quality of scar. Overall, these data suggest that the active proteolytic fraction P1G10 enhances the efficacy of repair in excisional cutaneous wounds.

Avaliação da atividade citotóxica das sementes de Annona cornifolia A. St.-Hil. (Annonaceae) / Evaluation of the cytotoxic activity of seeds of Annona cornifolia A. St.-Hil. (Annonaceae)

Na família Annonaceae, especialmente o gênero Annona é muito apreciado por fornecer frutos comestíveis. Espécies desse gênero são utilizadas na medicina popular contra diabetes, malária e infecções. Muitas dessas atividades biológicas têm sido relacionadas às acetogeninas de anonáceas. O objetivo deste estudo foi avaliar a atividade citotóxica dos grupos e de uma acetogenina pura (cornifolina) obtidos a partir do extrato etanólico das sementes de Annona cornifolia A. St.-Hil. (Annonaceae). Esta atividade foi avaliada pelo ensaio colorimétrico MTT. Cornifolina (1), a única substância pura testada, apresentou citotoxicidade positiva sobre todas as linhagens tumorais avaliadas. Os grupos testados, todos caracterizados por espectroscopia no infravermelho (IV), apresentaram 68,7% dos valores de CI50 menores que 20,0 µg mL-1, sendo também considerados citotóxicos. As amostras testadas foram mais ativas que o taxol sobre melanoma humano (MeWo) e, ainda, o grupo G10-5 apresentou melhor atividade sobre fibroblasto tumorigênico de camundongo (L929). Além disso, os grupos mostraram menor citotoxidade do que o taxol sobre a linhagem normal (CHO).

The family Annonaceae, especially the genus Annona, is greatly appreciated for providing edible fruits. Species of this genus are used in folk medicine against diabetes, malaria and infections. Many of these biological activities have been related to annonaceous acetogenins. The aim of this study was to evaluate the cytotoxic activity of groups and a pure acetogenin (cornifolin) obtained from the ethanol extract of the seeds of Annona cornifolia A. St.-Hil. (Annonaceae). This activity was evaluated by using MTT colorimetric assay. Cornifolin (1), the only tested substance that was pure, showed positive cytotoxicity on all evaluated tumor cell lines. The tested groups, all characterized by infrared spectroscopy (IR), showed 68.7% of the IC50 values lower than 20.0 µg mL-1, also considered cytotoxic. The tested samples were more active than taxol on human melanoma (MeWo) and the group G10-5 showed better activity on mouse tumorigenic fibroblast (L929). In addition, the tested groups showed less cytotoxicity than taxol on the normal line (CHO).

A mitogenic protein fraction in latex from Carica candamarcensis.

Latex from Caricaceae contains a number of proteins believed to be part of a defense mechanism that protects these plants from wounding. Prior evidence suggests that some components in Carica papaya improve healing of ulcerous wounds in mammals. This study shows the chromatographic isolation of a protein fraction from C. candamarcensis that stimulates cell proliferation of mammalian cells by measuring MTT reduction and thymidine incorporation. The effect appears to be cell specific as L929, MDA-MB231 and BHK-21 cells are stimulated while no effect is seen on CHO cells. The maximal stimulatory effect reaches 2.2-fold 72 h after addition of the active fraction to L929, 1.8-fold in MDA-MB231 cells and 1.6-fold in BHK cells. Proteolytic inactivation of the active fraction suggests that a protein is responsible for the proliferative activity and its size is estimated between 10 and 25 kDa. A potential candidate for this function is a 23 kDa protein found in the fraction that reacts with human EGF antibody.

Chemical characterization and biological activity of Macfadyena unguis-cati (Bignoniaceae).

Macfadyena unguis-cati (L.) has been widely used in folk medicine as an anti-inflammatory, antimalarial and antivenereal. The purpose of this study was to chemically characterize the main plant components, and to evaluate the biological properties of some of the fractions derived from leaves (MACb) and liana (MACa) of this plant. Chemical characterization allowed the identification of the compounds corymboside, vicenin-2, quercitrin, chlorogenic acid, isochlorogenic acid, lupeol, beta-sitosterol, beta-sitosterylglucoside, allantoin and lapachol. The biological screening of fractions and/or purified substances derived from fractions revealed antitumoral and antitrypanosomal activities in fractions MACa/lapachol and MACb/MACb21, respectively. The anti-lipoxygenase and anti-cyclooxygenase effect seen in fractions MACa and MACb showed a partial correlation with the anti-inflammatory property attributed to this plant.