Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17-19, 44121 Ferrara, Italy.
Molecules. 2011 Aug 18;16(8):7068-80. doi: 10.3390/molecules16087068.
We here report the results of our investigations carried out on verbascoside, a phenylpropanoid glycoside known for its antioxidant, anti-inflammatory and photoprotective actions. Verbascoside was obtained from Buddleia davidii meristematic cells, obtained in turn using a sustainable biotechnology platform which employs an in vitro plant cell culture technology. Verbascoside was first investigated to assess the behaviour of the active ingredient in solution or in finished preparations, in view of its potential topical use, especially in skin protection. Stability studies were performed by HPLC, and a PCL assay was adopted to determine the radical scavenging activity toward superoxide anion. The high hydrophilic character of verbascoside, suggested in a somewhat limited range of possible applications, leading us to explore its derivatization to obtain the semi-synthetic derivative VPP, an acyl derivative of verbascoside, with an improved range of applications due to its lower hydrophilic profile. Alone, VPP revealed increased antioxidant activity, both as an active ingredient and in dermocosmetic preparations. Stability studies showed a greater stability of VPP in lipophilic vehicles, whereas the parent verbascoside proved more stable in an O/W emulsions. Verbascoside was also stable in suppositories, an interesting pharmaceutical form for possible applications in treatment of inflammation of the intestinal mucosa.
我们在此报告对毛蕊花糖苷的研究结果，毛蕊花糖苷是一种苯丙素糖苷，具有抗氧化、抗炎和光保护作用。毛蕊花糖苷从醉鱼草茎尖细胞中获得，醉鱼草茎尖细胞又是使用一种可持续的生物技术平台获得的，该平台采用体外植物细胞培养技术。首先研究了毛蕊花糖苷在溶液或成品制剂中的行为，因为它具有潜在的局部用途，特别是在皮肤保护方面。通过 HPLC 进行了稳定性研究，并采用 PCL 测定法测定了对超氧阴离子自由基的清除活性。毛蕊花糖苷具有较高的亲水性，这表明其在一定范围内可能具有应用前景，因此我们探索了其衍生化以获得半合成衍生物 VPP，即毛蕊花糖苷的酰基衍生物，由于其亲水性较低，应用范围更广。VPP 单独使用时，无论是作为活性成分还是在皮肤护理制剂中，其抗氧化活性都有所提高。稳定性研究表明，VPP 在亲脂性载体中更稳定，而母体毛蕊花糖苷在 O/W 乳液中更稳定。毛蕊花糖苷在栓剂中也很稳定，栓剂是一种有趣的药物形式，可能适用于治疗肠道黏膜炎症。
