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抗氧化化合物基里醇和甲基-ent-16α,17-二羟基贝壳杉-19-烯酸甲酯的生物活性指导分离物可通过抑制细胞内 ROS 产生来减弱 MITF 介导的黑色素生成。

Antioxidant Compounds, Kirenol and Methyl ent-16α, 17-dihydroxy-kauran-19-oate Bioactivity-Guided Isolated from Attenuates MITF-Mediated Melanogenesis via Inhibition of Intracellular ROS Production.

机构信息

Department of Food Science and Biotechnology, Sunchon National University, 255 Jungangno, Suncheon-si 57922, Korea.

College of Pharmacy and Research Institute of Life and Pharmaceutical Sciences, Sunchon National University, 255 Jungangno, Suncheon-si 57922, Korea.

出版信息

Molecules. 2021 Mar 30;26(7):1940. doi: 10.3390/molecules26071940.

Abstract

(Compositae), an annual herb indigenous to Korean mountainous regions and has been eaten as a food in Korea. This study investigated ABTS, DPPH and nitric oxide (NO) radical-scavenging activities, and melanin production and TYR inhibitory effects-guided fractionation to identify therapeutic phytochemicals from that can attenuate oxidation and melanogenesis in murine melanoma B16F10 cells. Nine compounds with inhibitory effects on melanin production, and TYR activity, and ABTS, DPPH, and NO radical scavenging activity were isolated from the 100% ethanol fraction from . Among the nine compounds, kirenol (K), methyl ent-16α, 17-dihydroxy-kauran-19-oate (MDK) had strong inhibitory effects on melanin production and TYR activity with antioxidant effects. Western blot analysis revealed that K and MDK suppressed tyrosinase-related protein (TYRP)-1, TYRP-2 and microphthalmia-associated transcription factor (MITF) expression. Moreover, these two compounds inhibited intracellular reactive oxygen species (ROS) level in tert-butyl hydroperoxide (-BHP)-treated B16F10 cells. Our results suggest that containing active compounds such as K and MDK, which has antioxidant and antimelanogenesis effects, is the potent therapeutic and functional material for the prevention of oxidation-induced hyperpigmentation.

摘要

(菊科),一种原产于朝鲜山区的一年生草本植物,在朝鲜一直被当作食物食用。本研究调查了 ABTS、DPPH 和一氧化氮(NO)自由基清除活性,以及黑色素生成和 TYR 抑制作用导向的分馏,以从 中鉴定出可减轻小鼠黑色素瘤 B16F10 细胞氧化和黑色素生成的治疗性植物化学物质。从 100%乙醇部分分离出 9 种具有抑制黑色素生成和 TYR 活性以及 ABTS、DPPH 和 NO 自由基清除活性的化合物。在这 9 种化合物中,基伦醇(K)和甲基-ent-16α,17-二羟基-卡诺-19-酸酯(MDK)对黑色素生成和 TYR 活性具有很强的抑制作用,具有抗氧化作用。Western blot 分析显示,K 和 MDK 抑制了酪氨酸酶相关蛋白(TYRP)-1、TYRP-2 和小眼畸形相关转录因子(MITF)的表达。此外,这两种化合物抑制了叔丁基过氧化物(-BHP)处理的 B16F10 细胞内的活性氧(ROS)水平。我们的研究结果表明, 含有基伦醇和 MDK 等活性化合物,具有抗氧化和抗黑色素生成作用,是预防氧化诱导的色素沉着的有效治疗和功能性物质。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfc1/8036764/1893caaa90db/molecules-26-01940-g001.jpg

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