RESUMO
Chemically stable ester derivatives of taxifolin have become a focus of interest for their role in the satisfactory effects on human health. Accordingly, the aim of this study was to evaluate the physical and chemical stability of different formulations containing 0.02% taxifolin tetra-octanoate, which was proved to possess higher inhibitory effect on tyrosinase activity compared with taxifolin in a cell-free system. In the studies of physical stability, a Brookfield viscometer was used to determine rheological behavior of formulations containing taxifolin tetra-octanoate, and a portable pH meter was used to determine pH change. Moreover, chemical stability was determined by HPLC with UV detection. Formulations were evaluated for 12 weeks stored at 25 and 40°C. Results showed that storage time had no significant influence on viscosity of the formulations containing taxifolin tetra-octanoate, and pH value was relatively stable, which was within the limits of normal skin pH range. In the chemical stability studies, taxifolin tetra-octanoate in the essence formulation was most unstable at 40°C with about 81% degradation in 12 weeks of storage, however, the percentage of remaining taxifolin tetra-octanoate in cream formulation stored for 12 weeks at 25°C was the highest, about 93%. The results in this study may contribute to the development of more stable formulations containing taxifolin tetra-octanoate.
Assuntos
Caprilatos/farmacologia , Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Quercetina/análogos & derivados , Caprilatos/síntese química , Caprilatos/química , Cromatografia Líquida de Alta Pressão , Composição de Medicamentos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Concentração de Íons de Hidrogênio , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Quercetina/síntese química , Quercetina/química , Quercetina/farmacologia , Relação Estrutura-Atividade , ViscosidadeRESUMO
Berberine has abundant beneficial properties including anti-cancer effects. In the present study, we examined the inhibitory effect of berberine on α-melanocyte-stimulating hormone (α-MSH)-induced melanogenesis in B16F1 melanoma cells. The results showed that berberine decreased the expression of tyrosinase and microphthalmia-associated transcription factor (MITF) in a dose-dependent manner. In order to observe the potential target for the inhibitory effect of berberine, we examined the effect of berberine on TRP-1 and TRP-2. The results showed that berberine led to a reduction of TRP-1, while the change of TRP-2 was inconspicuous. In the end, we observed the specific effect of berberine on zebrafish skin pigmentation. Overall, the results suggested that berberine inhibits tyrosinase activity and melanin synthesis by attenuating the expression of tyrosinase and MITF. Therefore, these findings may contribute to the potential application of berberine in medicinal or cosmetic products.
Assuntos
Berberina/farmacologia , Melaninas/biossíntese , Melanoma Experimental/tratamento farmacológico , Animais , Berberina/isolamento & purificação , Linhagem Celular Tumoral , Coptis chinensis , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/farmacologia , Oxirredutases Intramoleculares/metabolismo , Melanoma Experimental/metabolismo , Camundongos , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Oxirredutases/metabolismo , Peixe-Zebra , alfa-MSH/antagonistas & inibidoresRESUMO
In order to find microorganisms showing antifungal activities against Plasmodiophora brassicae, which causes club root, Korean salt-fermented fishery products were tested. Several fermented broths of microorgansims isolated from Ammodytes personatus fishery products showed high antifungal activities. The identification of microorganisms and their in vivo antifungal activities are reported herein.