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Antifungal activities of Eugenia umbelliflora Berg. (Myrtaceae) were tested in vitro against a panel of standard and clinical isolates of human fungal pathogens (dermatophytes and opportunistic saprobes). Methanol extracts of leaves and fruits of E. umbelliflora were separately prepared and partitioned, to yield dichloromethane (DCM), ethyl acetate (EtOAc) and aqueous fractions (Aq). Three compounds (1-3) were obtained from the DCM extract using chromatographic procedures. Antifungal assays were performed using agar dilution techniques. Both extracts (fruits and leaves), their DCM and EtOAc fractions, and compound 2 (betulin and betulinic acid) presented selective antifungal activity against dermatophytes (Epidermophyton floccosum, Microsporum canis, Microsporum gypseum, Trichophyton rubrum, Trichophyton mentagrophytes), with MIC values between 200 and 1000 µg/mL, and interestingly, inhibited 4/5 species with MIC values of ≤500 µg/mL. The aqueous fractions of fruits and leaves, and compounds 1 (α, β amyrin) and 3 (taraxerol) were inactive up to the maximum concentrations tested (1000 µg/mL).

Cyclic imides are known for their antitumor activity, especially the naphthalimide derivatives, such as Mitonafide and Amonafide. Recently, we have demonstrated the cytotoxic effect of a series of naphthalimide derivatives against B16F10 melanoma cells. On the basis of this fact, we have developed a study starting from the synthesis of different cyclic imides and the evaluation of their cytotoxic properties on human acute leukemia cells (K562 and Jurkat). Initially, a screening test was conducted to select the compound with the best cytotoxic effect, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. After this selection, structural modifications were performed in the most active compound to obtain five more derivatives. All compounds presented a good cytotoxic effect. The results of cell cycle analysis, fluorescence microscopy, and Annexin V-FITC assay confirmed that the cells observed in the sub-G0/G1 phase were undergoing apoptosis. From this set of results, cyclic imides 8, 10, and 12 were selected for the evaluation of the mechanisms involved in the apoptotic process. The results demonstrate the involvement of the intrinsic pathway of apoptosis, evidenced by the reduction in mitochondrial potential, an increase in the level of AIF protein expression, a decreased level of expression of anti-apoptotic Bcl-2 protein, and an increased level of expression of pro-apoptotic protein Bax in both K562 and Jurkat cells treated with cyclic imides (8, 10, and 12). Furthermore, cyclic imides 8 and 10 caused an increase in the level of Fas expression in Jurkat cells, indicating the additional involvement of the extrinsic apoptosis pathway. The compounds (8, 10, and 12) also caused a decreased level of expression of anti-apoptotic protein survivin. The biological effects observed with these cyclic imide derivatives in this study suggest promising applications against acute leukemia.

Resumo:O envelhecimento é um processo lento e gradual, que afeta principalmente a pele, não é possível evitar esse processo, entretanto tem-se conseguido gerenciar o envelhecimento. Existem várias maneiras de se tratar o envelhecimento cutâneo, entre elas destaca-se o uso tópico da vitamina A tópica e seus derivados. Neste contexto o objetivo deste artigo é analisar os benefícios da utilização tópica da vitamina A e seus derivados, na prevenção do envelhecimento cutâneo, através de uma revisão bibliográfica descritiva com abordagem qualitativa. Os resultados demonstram que a vitamina A é um micronutriente lipossolúvel que o corpo humano não fabrica, é um termo genérico que abrange o retinol, retinal, ácido retinóico e éster de retilina, também inclui os carotenoides. Estes ativos apresentam diversas funções, dentre as quais as atividades antioxidante, regeneradora dérmica, renovadores epidérmicos e tensores. Concluiu-se que a utilização da vitamina A e seus derivados, traz benefícios, na prevenção do envelhecimento cutânePalavras-chaves: Envelhecimento Cutâneo; Ativos Cosméticos; Vitamina A e seus derivados. Abstract: Aging is a slow and gradual process, which mainly affects the skin, it is not possible to avoid this process, however, aging has been managed. There are several ways to treat skin aging, among them the topical use of topical vitamin A and its derivatives. In this context, the objective of this article is to analyze the benefits of the topical use of vitamin A and its derivatives, in the prevention of skin aging, through a descriptive literature review with a qualitative approach. The results demonstrate that vitamin A is a fat-soluble micronutrient that the human body does not manufacture, it is a generic term that encompasses retinol, retinal, retinoic acid and retilin ester, it also includes carotenoids. These actives have several functions, including antioxidant, dermal regenerator, epidermal renewers and tensor activities. It was concluded that the use of vitamin A and its derivatives brings benefits in the prevention of skin aging.Keywords: Skin Aging; Cosmetic Assets; Vitamin A and its derivatives.