Department of Pharmacology, Faculty of Pharmacy, Universidad de Sevilla, 41012 Seville, Spain.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Universidad de Sevilla, 41012 Seville, Spain.
Mar Drugs. 2018 Oct 10;16(10):378. doi: 10.3390/md16100378.
Microalgae represent a source of bio-active compounds such as carotenoids with potent anti-inflammatory and antioxidant properties. We aimed to investigate the effects of fucoxanthin (FX) in both in vitro and in vivo skin models. Firstly, its anti-inflammatory activity was evaluated in LPS-stimulated THP-1 macrophages and TNF-α-stimulated HaCaT keratinocytes, and its antioxidant activity in UVB-irradiated HaCaT cells. Next, in vitro and ex vivo permeation studies were developed to determine the most suitable formulation for in vivo FX topical application. Then, we evaluated the effects of a FX-containing cream on TPA-induced epidermal hyperplasia in mice, as well as on UVB-induced acute erythema in hairless mice. Our results confirmed the in vitro reduction of TNF-α, IL-6, ROS and LDH production. Since the permeation results showed that cream was the most favourable vehicle, FX-cream was elaborated. This formulation effectively ameliorated TPA-induced hyperplasia, by reducing skin edema, epidermal thickness, MPO activity and COX-2 expression. Moreover, FX-cream reduced UVB-induced erythema through down-regulation of COX-2 and iNOS as well as up-regulation of HO-1 protein via Nrf-2 pathway. In conclusion, FX, administered in a topical formulation, could be a novel natural adjuvant for preventing exacerbations associated with skin inflammatory pathologies as well as protecting skin against UV radiation.
微藻是生物活性化合物的来源,如具有强大抗炎和抗氧化特性的类胡萝卜素。我们旨在研究岩藻黄素 (FX) 在体外和体内皮肤模型中的作用。首先,在 LPS 刺激的 THP-1 巨噬细胞和 TNF-α 刺激的 HaCaT 角质形成细胞中评估其抗炎活性,并在 UVB 照射的 HaCaT 细胞中评估其抗氧化活性。接下来,进行了体外和离体渗透研究,以确定最适合体内 FX 局部应用的配方。然后,我们评估了含有 FX 的乳膏对 TPA 诱导的小鼠表皮增生以及无毛小鼠 UVB 诱导的急性红斑的影响。我们的结果证实了体外 TNF-α、IL-6、ROS 和 LDH 产生减少。由于渗透结果表明乳膏是最有利的载体,因此制备了 FX 乳膏。该配方通过降低皮肤水肿、表皮厚度、MPO 活性和 COX-2 表达,有效改善了 TPA 诱导的增生。此外,FX 乳膏通过下调 COX-2 和 iNOS 以及通过 Nrf-2 途径上调 HO-1 蛋白,减轻了 UVB 诱导的红斑。总之,局部应用 FX 可能是预防与皮肤炎症性病变相关的恶化以及保护皮肤免受 UV 辐射的新型天然佐剂。