Mustapha Nadia, Bzéouich Imèn Mokdad, Ghedira Kamel, Hennebelle Thierry, Chekir-Ghedira Leila
Laboratoire de biologie cellulaire et moléculaire, faculté de médecine dentaire, université de Monastir, rue Avicenne, 5000 Monastir, Tunisia; Unité de substances naturelles bioactives et biotechnologie UR12ES12, faculté de pharmacie de Monastir, université de Monastir, rue Avicenne, 5000 Monastir, Tunisia.
Unité de substances naturelles bioactives et biotechnologie UR12ES12, faculté de pharmacie de Monastir, université de Monastir, rue Avicenne, 5000 Monastir, Tunisia.
Biomed Pharmacother. 2015 Feb;69:139-44. doi: 10.1016/j.biopha.2014.11.010. Epub 2014 Nov 18.
Poor therapeutic results have been reported for treatment of malignant melanoma; therefore in this study, we have investigated inhibitory capacity of vitexin-2''-O-rhamnoside as well as the extract from which it was isolated, i.e. the ethyl acetate extract obtained from the leaves of Crataegus azarolus, on mouse melanoma (B16F10) proliferation. Cell viability was determined using the 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. In addition, amounts of melanin and tyrosinase were measured spectrophotometrically at 475nm. Ethyl acetate extract and vitexin-2''-O-rhamnoside exhibited significant anti-proliferative activity against B16F10 melanoma cells after incubation for 48hours with IC50s of 50μg/mL and 20μM, respectively. Furthermore, these two compounds have the ability to reduce the melanin content by inhibiting the tyrosinase activity of B16F10 cells. Thus, further investigations are merited to ascertain their potential application in treating hyperpigmentation disorders.
据报道,恶性黑色素瘤的治疗效果不佳;因此,在本研究中,我们研究了牡荆素 -2''-O-鼠李糖苷及其分离提取物(即从阿扎尔山楂叶中获得的乙酸乙酯提取物)对小鼠黑色素瘤(B16F10)增殖的抑制能力。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐法测定细胞活力。此外,在475nm处用分光光度法测量黑色素和酪氨酸酶的含量。乙酸乙酯提取物和牡荆素 -2''-O-鼠李糖苷在与B16F10黑色素瘤细胞孵育48小时后表现出显著的抗增殖活性,IC50分别为50μg/mL和20μM。此外,这两种化合物能够通过抑制B16F10细胞的酪氨酸酶活性来降低黑色素含量。因此,值得进一步研究以确定它们在治疗色素沉着紊乱方面的潜在应用。