College of Pharmacy and and Research Institute of Life and Pharmaceutical Sciences, Sunchon National University, Suncheon, Jeonnam, Korea.
Institute of Jinan Red Ginseng, Jinan, Jinan, Korea.
Nat Prod Res. 2022 Dec;36(24):6414-6420. doi: 10.1080/14786419.2022.2035384. Epub 2022 Feb 8.
Excessive production of melanin causes various dermatological disorders including hyperpigmentation. To search for anti-melanogenesis candidates from natural products, we discovered that leaves of var. (OFA) suppressed melanin production. The extract of OFA leaves and its fractions were subjected to bioactivity-guided separation by targeting active constituents and a total of four triterpenoids were obtained: 3,24-dihydroxyurs-12-en-28 oic acid (), pomolic acid (), maslinic acid (), and corosolic acid (). Compounds and were isolated from this plant for the first time. All compounds were evaluated for their inhibitory activities against melanin production and tyrosinase activity. Active compounds were further investigated to understand their mechanisms of action. Results revealed that they significantly down-regulated TYRP-1 and TYRP-2 expression levels. Our results clarified the whitening property of this plant and provided evidence that active constituents of this plant possessed anti-melanogenesis effect and anti-tyrosinase activity for the first time.
过量的黑色素会导致各种皮肤疾病，包括色素沉着过度。为了从天然产物中寻找抗黑色素生成的候选药物，我们发现 var. （OFA）的叶子能抑制黑色素的产生。我们针对活性成分对 OFA 叶的提取物及其馏分进行了基于生物活性的分离，总共得到了四种三萜类化合物：3,24-二羟基乌苏-12-烯-28 酸（）、熊果酸（）、齐墩果酸（）和科罗索酸（）。化合物 和 是首次从这种植物中分离得到的。所有化合物都评估了它们对黑色素生成和酪氨酸酶活性的抑制活性。活性化合物进一步进行了作用机制的研究。结果表明，它们能显著下调 TYRP-1 和 TYRP-2 的表达水平。我们的研究结果阐明了这种植物的增白特性，并首次提供了证据，证明该植物的活性成分具有抗黑色素生成和抗酪氨酸酶活性的作用。
