背景:Tribloside,一种天然黄酮类化合物,从中药TribulusterrestrisL中提取。,在治疗各种疾病方面显示出有效的疗效。在中国,荆棘的果实.长期以来一直被用来缓解头痛,头晕,瘙痒,和白癜风。来自TribulusterrestrisL的水基提取物。可以通过提高α-黑素细胞刺激激素(α-MSH)和黑皮质素-1受体(MC-1R)的表达来增强小鼠毛囊黑素细胞的黑素生成。然而,在实验室环境和活生物体中,缺乏有关藤黄苷对色素沉着的影响的信息。
目的:本研究的目的是研究杜松子皂苷对色素沉着的影响,并深入研究潜在的机制。
方法:在人表皮黑素细胞(HEMCs)中施用杜松子醇苷后,我们利用了酶标仪,Masson-Fontana氨色银染,透射电子显微镜(TEM)和扫描电子显微镜(SEM)测量黑色素含量,枝晶长度,黑素体计数;L-DOPA氧化测定以指示酪氨酸酶活性,蛋白质印迹法评估黑色素生成和相关磷酸二酯酶(PDE)/环磷酸腺苷(cAMP)/环AMP依赖性蛋白激酶A(PKA)途径蛋白的表达。还进行了PDE-Glo测定以验证三叶皂甙对PDE的抑制作用。此外,我们在斑马鱼模型和人类皮肤样本中检测了三叶皂苷对色素沉着的影响。
结果:丁香苷对黑素细胞中黑色素的产生有显著影响,斑马鱼,和人体皮肤样本.这些功能可能归因于杜仲糖苷对PDE的抑制作用,这可以增加细胞内的cAMP水平以刺激cAMP反应元件结合(CREB)的磷酸化。一旦激活,它诱导小眼症相关转录因子(MITF)的表达并增加酪氨酸酶的表达,Rab27a和细胞分裂周期蛋白42(Cdc42),最终促进黑色素生成,黑素细胞树突,和黑色素运输。
结论:Tribuloside作用于PDE/cAMP/PKA途径,以增强黑色素生成,黑素细胞树突,和黑体运输;同时,三叶皂苷对细胞没有任何毒性作用,可以引入临床处方中以促进色素沉着。
BACKGROUND: Tribuloside, a natural flavonoid extracted from Chinese medicine Tribulus terrestris L., has shown potent efficacy in treating various diseases. In
China, the fruits of Tribulus terrestris L. have long been utilized for relieving headache, dizziness, itchiness, and vitiligo. Water-based extract derived from Tribulus terrestris L. can enhance melanogenesis in mouse hair follicle melanocytes by elevating the expression of α-
melanocyte stimulating hormone (α-MSH) and melanocortin-1 recepter (MC-1R). Nevertheless, there is a lack of information regarding the impact of tribuloside on pigmentation in both laboratory settings and living organisms.
OBJECTIVE: The present research aimed to examine the impact of tribuloside on pigmentation, and delve into the underlying mechanism.
METHODS: Following the administration of tribuloside in human epidermal melanocytes (HEMCs), we utilized microplate reader, Masson-Fontana ammoniacal silver stain, transmission electron microscopy (TEM) and scanning electron microscopy (SEM) to measure melanin contents, dendrite lengths, melanosome counts; L-DOPA oxidation assay to indicate tyrosinase activity, Western blotting to evaluate the expression of melanogenic and associated phosphodiesterase (PDE)/cyclic adenosine monophosphate (cAMP)/cyclic-AMP dependent protein kinase A (PKA) pathway proteins. A PDE-Glo assay to verify the inhibitory effect of tribuloside on PDE was also conducted. Additionally, we examined the impact of tribuloside on the pigmentation in both zebrafish model and human skin samples.
RESULTS: Tribuloside had a notable impact on the production of melanin in melanocytes, zebrafish, and human skin samples. These functions might be attributed to the inhibitory effect of tribuloside on PDE, which could increase the intracellular level of cAMP to stimulate the phosphorylation of cAMP-response element binding (CREB). Once activated, it induced microphthalmia-associated transcription factor (MITF) expression and increased the expression of tyrosinase, Rab27a and cell division cycle protein 42 (Cdc42), ultimately facilitating melanogenesis,
melanocyte dendricity, and melanin transport.
CONCLUSIONS: Tribuloside acts on the PDE/cAMP/PKA pathway to enhance melanogenesis,
melanocyte dendricity, and melanosome transport; meanwhile, tribuloside does not have any toxic effects on cells and may be introduced into clinical prescriptions to promote pigmentation.