| 摘要: | 近年來多數國家人口逐漸進入高齡化社會,具有抗老化活性之藥妝產品漸漸受到消費者的注意,決定皮膚光老化的主要原因之一是膠 原蛋白,而基質金屬蛋白酶-1 (matrix metalloproteinase, MMP-1) 會影 響膠原蛋白的降解,因此 MMP-1 在皮膚抗光老化的作用扮演重要的 角色。臺灣火刺木 ( Pyracantha koidzumii (Hanyata) Rehder) 為薔薇科 (Rosaceae) 火刺木屬 (Pyracantha) 之常綠灌木,屬於臺灣特有種植物。過去研究指出臺灣火刺木具有美白作用,本研究以其果實之 95% 乙醇萃取物進行部分劃分,利用活性追蹤方式探討在 WS-1 細胞之抗 光老化作用,結果顯示粗萃物、乙酸乙酯、正丁醇及水層之萃取物對 細胞存活率影響不大,且乙酸乙酯層萃取物具較明顯抑制 MMP-1 活 性。將乙酸乙酯層萃取物進行藥物奈米劑型的探討,得到奈米等級 (粒徑= 148.3 nm)、穩定 (多分散性指數= 0.131) 且包覆率為 90% 之 藥物劑型。進一步從乙酸乙酯層萃取物進行成分分離純化,經理化及 光譜相關數據與參考文獻比對得到三個化合物:分別為 PK1, PK2 及 PK3。在人類纖維母細胞 (WS-1) 中具有抑制 MMP-1 之活性,且 PK2 和 PK3 具有細胞內抗氧化的作用。期望透過本研究在未來對臺灣火 刺木發展抗光老化及奈米劑型有良好貢獻。
In recent years, most countries have gradually entered the ageing society, so cosmeceuticals that possess anti-photoaging activities have attracting more and more attention. Matrix metalloprpteinase-1 (MMP-1) affects the degradation of collagen, which is one of the main cause of skin photoaging. Therefore MMP-1 inhibitor plays an important role in anti-photoaging of the skin. Pyracantha koidzumii (Hanyata) Rehder (Rosaceae), an evergreen, is one of Taiwanese endemic plants. Previous study indicated that P. koidzumii has whitening activity. In this study, fruits of P. koidzumii were extracted with 95% ethanol and then partitioned with a sequence of n-hexane, ethyl acetate (EA), and n-butanol (n-BuOH). We evaluated the activities of the extracts and partitioned fractions in human fibroblast (WS-1). The results showed that EA fraction significantly decreased the MMP-1 activity in WS-1 cells. The EA fraction was performed to explore the pharmaceutical dosage form of fraction. We acquired the nano level (particle size= 148.3 nm) and stable (polydispersity index= 0.131) dosage form. After bio-guided column chromatography, we obtain three known compounds. The structures of these compounds were identified as PK1, PK2 and PK3 by comparing with the physical and spectroscopic characterizations. Among these compounds, PK2 significantly decreased the MMP-1 activity in WS-1 cells. PK2 and PK3 significantly decrease the intracellular reactive oxygen species (ROS) contents in WS-1 cells. The present results imply that P. koidzumii and the EA fraction nanometer particles may be useful in anti-photoaging design in the future. |
