Wang Zhihong, Peng Sheng, Peng Mijun, She Zhigang, Yang Qiuling, Huang Tao
Guangdong Provincial Key Laboratory of Emergency Test for Dangerous Chemicals, Guangdong Institute of Analysis (China National Analytical Center Guangzhou), Guangdong Academy of Sciences, Guangzhou, China.
School of Chemistry, Sun Yat-Sen University, Guangzhou, China.
Ann Transl Med. 2020 Aug;8(16):1004. doi: 10.21037/atm-20-5468.
Oliv. (EUO) was a traditional Chinese herb, its leaves were abundant in China, and polyphenol compounds were considered to be an important active ingredient in Oliv. leaves (EUOL). However, previous research mainly focused on compound identification and extraction process, there were few reported on the efficient enrichment process and biological activity evaluation of polyphenols in EUOL.
The adsorption and desorption characteristics of twelve different resins (HPD-100, HPD-300, HPD-600, D-3250, X-5, D-140, NKA-9, NKA-II, D-101, AB-8, S-8 and Polyamide) were investigated to develop an efficient method for the enrichment of polyphenol from EUOL, and the static adsorption, kinetics, isotherm and thermodynamics of the polyphenol from EUOL were analyzed. The eluted component was obtained through dynamic elution, and its main polyphenol compounds were detected by high-phase liquid chromatography (HPLC) and the inhibitory effects on the enzyme activity of α-amylase and α-glucosidase was also evaluated for different elution components. Meanwhile, the binding of main polyphenol compounds to enzyme was also evaluated.
The selected resins (HPD-300, HPD-600, D-3250, X-5, D-140, NKA-9, D-101 and AB-8) showed adsorption patterns that fitted well to the pseudo second-order kinetics. The intra-particle diffusion model demonstrated that the diffusion of polyphenol compounds on these resins were divided into three processes. For HPD-300, HPD-600 and NKA-9, the Freundlich model better described the adsorption isotherm behavior than the Langmuir model, and the adsorption of polyphenol was a physical, exothermic, and spontaneous process. Subsequently, dynamic elution was performed yielding a higher polyphenol content in a 60% ethanol-water elution component, and it also exhibited a higher inhibitory effect on α-amylase and α-glucosidase activity. Furthermore, as the main polyphenol compounds, chlorogenic acid, rutin, quercetin and kaempferol were used to simulate the binding to the enzyme protein through molecular docking technology. The results showed that quercetin had a higher docking score for α-amylase, while rutin displayed superior binding to α-glucosidase.
Therefore, polyphenols of EUOL could be enriched through macroporous resins and have the potential to be effective enzyme inhibitor.
橄榄(EUO)是一种传统的中草药,在中国其叶子资源丰富,多酚类化合物被认为是橄榄叶(EUOL)中的重要活性成分。然而,以往的研究主要集中在化合物鉴定和提取工艺方面,关于EUOL中多酚的高效富集工艺及生物活性评价的报道较少。
研究了12种不同树脂(HPD - 100、HPD - 300、HPD - 600、D - 3250、X - 5、D - 140、NKA - 9、NKA - II、D - 101、AB - 8、S - 8和聚酰胺)的吸附和解吸特性,以建立从EUOL中富集多酚的高效方法,并分析了EUOL中多酚的静态吸附、动力学、等温线和热力学。通过动态洗脱获得洗脱组分,采用高效液相色谱(HPLC)检测其主要多酚化合物,并评估不同洗脱组分对α -淀粉酶和α -葡萄糖苷酶活性的抑制作用。同时,还评估了主要多酚化合物与酶的结合情况。
所选树脂(HPD - 300、HPD - 600、D - 3250、X - 5、D - 140、NKA - 9、D - 101和AB - 8)的吸附模式与伪二级动力学拟合良好。颗粒内扩散模型表明,多酚化合物在这些树脂上的扩散分为三个过程。对于HPD - 300、HPD - 600和NKA - 9,Freundlich模型比Langmuir模型能更好地描述吸附等温线行为,且多酚的吸附是一个物理、放热和自发的过程。随后进行动态洗脱,在60%乙醇 - 水的洗脱组分中获得了较高的多酚含量,并且它对α -淀粉酶和α -葡萄糖苷酶活性也表现出较高的抑制作用。此外,以绿原酸、芦丁、槲皮素和山奈酚作为主要多酚化合物,通过分子对接技术模拟它们与酶蛋白的结合。结果表明,槲皮素对α -淀粉酶的对接分数较高,而芦丁与α -葡萄糖苷酶的结合能力较强。
因此,EUOL中的多酚可通过大孔树脂进行富集,并且具有成为有效酶抑制剂的潜力。