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含假丁香提取物的局部制剂:体外抗氧化活性及对 UV-B 诱导的氧化应激的体内功效。

Topical formulations containing Pimenta pseudocaryophyllus extract: In vitro antioxidant activity and in vivo efficacy against UV-B-induced oxidative stress.

机构信息

Departamento de Ciências Farmacêuticas, Universidade Estadual de Londrina-UEL, Avenida Robert Koch, 60, Hospital Universitário, Vila Operária, 86039-440, Londrina, Paraná, Brazil.

出版信息

AAPS PharmSciTech. 2014 Feb;15(1):86-95. doi: 10.1208/s12249-013-0049-8. Epub 2013 Nov 19.

Abstract

Pimenta pseudocaryophyllus is a Brazilian native plant that presents high concentrations of flavonoids and other polyphenolic compounds. Herein, we evaluated: (1) the chemical properties of P. pseudocaryophyllus ethanolic extract (PPE), (2) the in vitro antioxidant activity (AA) of PPE and of two different topical formulations (F1 and F2) containing PPE, (3) physico-chemical and functional stability, (4) in vitro release of PPE, and (5) in vivo capacity of formulations to prevent UV-B irradiation-induced skin damage. Results show that the polyphenol and flavonoid contents in PPE were 199.33 and 28.32 mg/g, respectively, and HPLC results show the presence of eugenol, tannic acid, and rutin. Evaluation of the in vitro AA of PPE demonstrated a dose-dependent effect and an IC50 of 4.75 μg/mL in 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 3.0 μg/mL in 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The ferric-reducing antioxidant power (FRAP assay) was 0.046 μmol/L trolox equivalent/μg/mL of extract. Among the AA, only the capacity to scavenge DPPH radical of PPE was maintained in F1 and F2. In addition, both formulations satisfactorily released the extract. The evaluation of the functional stability of F1 and F2 did not demonstrate loss of activity by storage at room temperature and at 4°C/6 months. In irradiated mice, treatment with F1 and F2 added with PPE significantly increased the capacity to scavenge ABTS radical and the FRAP of skin compared to vehicle-treated mice. In conclusion, the present results suggest that formulations containing PPE may be a topical source of antioxidant compounds to decrease oxidative damages of the skin.

摘要

假丁香是一种巴西本土植物,其含有高浓度的类黄酮和其他多酚类化合物。在此,我们评估了:(1)假丁香的乙醇提取物(PPE)的化学性质,(2)PPE 及其两种不同局部制剂(F1 和 F2)的体外抗氧化活性(AA),(3)物理化学和功能稳定性,(4)PPE 的体外释放,以及(5)制剂预防 UV-B 照射诱导的皮肤损伤的体内能力。结果表明,PPE 中的多酚和类黄酮含量分别为 199.33 和 28.32mg/g,HPLC 结果表明存在丁香酚、单宁酸和芦丁。PPE 的体外 AA 评估表明存在剂量依赖性效应,在 2,2-二苯基-1-苦基肼基(DPPH)测定法中,IC50 为 4.75μg/mL,在 2,2'-联氮双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)测定法中,IC50 为 3.0μg/mL。铁还原抗氧化能力(FRAP 测定法)为 0.046μmol/L trolox 当量/μg/mL 提取物。在 AA 中,只有 PPE 清除 DPPH 自由基的能力在 F1 和 F2 中得以维持。此外,两种制剂均能满意地释放提取物。F1 和 F2 的功能稳定性评估表明,在室温下和 4°C/6 个月的储存条件下,制剂的活性没有丧失。在照射的小鼠中,与载体处理的小鼠相比,添加 PPE 的 F1 和 F2 处理显著增加了皮肤清除 ABTS 自由基和 FRAP 的能力。总之,本研究结果表明,含有 PPE 的制剂可能是一种局部抗氧化化合物的来源,以减少皮肤的氧化损伤。

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