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体外评价藏红花醛的抗氧化、抗弹性蛋白酶、抗胶原酶、抗透明质酸酶活性及其在皮肤光老化中的防晒因子。

In-vitro evaluation of antioxidant, anti-elastase, anti-collagenase, anti-hyaluronidase activities of safranal and determination of its sun protection factor in skin photoaging.

机构信息

Department of Pharmaceutical Sciences, M. D. University, Rohtak, Haryana 124001, India.

Department of Pharmaceutical Sciences, M. D. University, Rohtak, Haryana 124001, India.

出版信息

Bioorg Chem. 2018 Apr;77:159-167. doi: 10.1016/j.bioorg.2017.12.030. Epub 2018 Jan 4.

DOI:10.1016/j.bioorg.2017.12.030
PMID:29353733
Abstract

Safranal, a monoterpene aldehyde, is present as one of the main volatile constituents of Crocus sativus Linn. (saffron flowers). This volatile constituent not only contributes to the aroma of saffron but has been reported to possess antidiabetic, antiulcer, antiasthamatic, anticonvulsant, antidepressant, cardioprotective, anticancer and UV protective properties. Most of these therapeutic actions are contributed by its potential to quench reactive oxygen species (ROS). Antioxidant properties of phytoconstituents are now being explored for developing photoprotective skin formulations. These bioactives have the potential to protect the epidermal and dermal layers of the skin which mainly comprises of elastin and collagen. When UV rays penetrate the dermal layers, there is an increased production of elastase, collagenase and hyaluronidase leading to degradation of collagen, elastin and hyaluronic acid respectively. These dermal components are responsible to provide strength, elasticity and moisture to the skin. Due to frequent exposure to sunlight, these conditions tend to augment leading to wrinkle formation and sagging of skin. Although antioxidant properties of safranal have been established on various cell lines but till date no studies have been reported regarding the dermal enzyme inhibition activities. In the current research work, a comprehensive in vitro evaluation of antioxidant, anti-elastase, anti-collagenase, anti-hyaluronidase activities of safranal along with determination of sun protection factor (SPF) was carried out. The in vitro antioxidant activity was carried out by diphenylpicrylhydrazyl (DPPH) method and its IC value was found to be 22.7 μg/ml. The enzyme inhibition IC values of safranal for anti elastase activity were found to be 43.6 μg/ml, 70 μg/ml for antihyaluronidase activity and 9.4 μg/ml for anticollagenase activity. Photoprotective activity of safranal was determined by UV absorbance method and SPF calculated by Mansur equation which was found to be 6.6. The significant inhibitory activity of safranal on matrix metalloproteinases (MMPs) responsible for aging and a higher SPF established that this bioorganic molecule is a strong photoprotective agent. Its established free radical scavenging capability along with above characteristics make it a valuable component to be incorporated into herbal antiaging formulations.

摘要

藏红花中的主要挥发性成分之一是单萜醛化合物藏红花醛。这种挥发性成分不仅为藏红花增添了香气,还具有降血糖、抗溃疡、抗哮喘、抗惊厥、抗抑郁、心脏保护、抗癌和抗紫外线等特性。这些治疗作用大多归因于其清除活性氧(ROS)的能力。植物成分的抗氧化特性目前正被用于开发防晒皮肤配方。这些生物活性物质有可能保护皮肤的表皮和真皮层,真皮层主要由弹性蛋白和胶原蛋白组成。当紫外线穿透真皮层时,弹性酶、胶原酶和透明质酸酶的产生会增加,导致胶原蛋白、弹性蛋白和透明质酸分别降解。这些真皮成分负责为皮肤提供强度、弹性和水分。由于经常暴露在阳光下,这些情况往往会加剧,导致皱纹形成和皮肤松弛。尽管藏红花醛的抗氧化特性已在各种细胞系上得到证实,但迄今为止,尚未有关于其抑制真皮酶活性的研究报告。在当前的研究工作中,对藏红花的抗氧化、抗弹性酶、抗胶原酶、抗透明质酸酶活性进行了全面的体外评价,并测定了防晒因子(SPF)。体外抗氧化活性通过二苯基苦基肼(DPPH)法进行测定,其 IC 值为 22.7μg/ml。藏红花对弹性酶抑制活性的 IC 值为 43.6μg/ml,对透明质酸酶抑制活性的 IC 值为 70μg/ml,对胶原酶抑制活性的 IC 值为 9.4μg/ml。藏红花的光保护活性通过紫外吸收法测定,防晒因子(SPF)通过 Mansur 方程计算,结果为 6.6。藏红花对负责衰老的基质金属蛋白酶(MMPs)具有显著的抑制活性,且具有较高的 SPF,这表明该生物有机分子是一种强有力的光保护剂。其已被证实的自由基清除能力以及上述特性使其成为一种有价值的成分,可以被纳入草药抗老化配方中。

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