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    新西兰松树皮提取物Enzogenol®的特征成分鉴定、活性评价及构效关系

    Identification, bioactivity evaluation, and structure-activity relationship of characteristic components in New Zealand pine bark extract Enzogenol®

    • 摘要:
      目的 我国松树皮资源丰富,但高值化利用水平仍然不高,主要存在特征功效成分不明、量化质控标准缺失等问题。为此,本研究选取商业化生产的新西兰松树皮提取物(Enzogenol®)为对象,拟系统解析其多酚组成,并与生物活性进行关联分析,以揭示“化学成分−生物活性”之间的关联,从而为开发标准化的国产松树皮产品提供科学依据。
      方法 采用UPLC-QTOF-MS技术建立Enzogenol®的化学指纹图谱,并对其主要成分进行定量分析。在体外活性评价方面,通过DPPH和ABTS自由基清除实验以及Fe2+/Cu2+螯合实验,评估了其抗氧化能力;同时采用微量稀释法测定其对金黄色葡萄球菌和大肠杆菌的抑菌活性。在此基础上,利用Pearson相关性分析方法,进一步探究化学成分与生物活性之间的统计学关联。
      结果 本研究从 Enzogenol® 中成功鉴定并定量了8种特征多酚成分。其中,原花青素B1(含量为2.55 mg/g)和儿茶素(含量为1.17 mg/g)被确定为核心质量标志物,两者在体外表现出较强的自由基清除能力与Fe2+螯合活性,且对金黄色葡萄球菌的抑菌效果显著优于对大肠杆菌。相关性分析进一步显示,原花青素B1、原花青素B2、儿茶素及表儿茶素的含量与上述生物活性指标均呈显著正相关(p < 0.05)。基于成分结构与活性的关联分析表明,核心成分(原花青素B1、儿茶素)的生物活性与其结构特征密切相关:密集分布的酚羟基赋予其突出的自由基清除与金属离子螯合能力,而适中的分子量与疏水性则介导了其选择性抑菌作用。
      结论 本研究证实,原花青素B1和儿茶素是Enzogenol®发挥抗氧化与抗菌活性的核心物质基础,其含量与上述生物活性呈显著正相关。该研究结果为我国松树皮资源的高值化开发及相应质量控制标准的建立提供了重要的理论依据与数据支撑。

       

      Abstract:
      Objective China has abundant pine bark resources, yet their high-value utilization remains underdeveloped, primarily due to unclear characteristic bioactive components and the lack of quantitative quality control standards. This study selected the commercially produced New Zealand pine bark extract (Enzogenol®) to systematically analyze its polyphenol composition and correlate it with bioactivities, aiming to elucidate the relationship between chemical constituents and biological effects. The findings are expected to provide a scientific basis for developing standardized domestic pine bark products.
      Methods The chemical fingerprint of Enzogenol® was established using ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS), and its main components were quantified. In vitro antioxidant activity was evaluated through DPPH and ABTS radical scavenging assays, as well as Fe2+/Cu2+ chelation tests. Antibacterial activity against Staphylococcus aureus and Escherichia coli was determined using the microdilution method. Pearson correlation analysis was further employed to investigate the statistical relationships between chemical components and bioactivities.
      Results Eight characteristic polyphenols were identified and quantified in Enzogenol®. Procyanidin B1 (2.55 mg/g) and catechin (1.17 mg/g) were identified as the core quality markers, demonstrating strong free radical scavenging ability and Fe2+ chelating activity in vitro. Moreover, their antibacterial effect against S. aureus was significantly stronger than that against E. coli. Correlation analysis revealed that the contents of procyanidin B1, procyanidin B2, catechin, and epicatechin were significantly positively correlated (p < 0.05) with the measured bioactivities. Structure-activity relationship analysis indicated that the bioactivity of the core components (procyanidin B1 and catechin) is closely related to their structural features: the dense distribution of phenolic hydroxyl groups contributes to their strong free radical scavenging and metal ion chelation abilities, while their moderate molecular weight and hydrophobicity mediate the selective antibacterial action.
      Conclusion This study confirms that procyanidin B1 and catechin are the core active substances responsible for the antioxidant and antibacterial effects of Enzogenol®, with their contents showing a significant positive correlation with these bioactivities. The results provide important theoretical foundations and data support for the high-value development of China’s pine bark resources and the establishment of corresponding quality control standards.

       

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