Hao Jie, Wang Yuanshuo, Xiao Yang, He Songhua, Chen Mingqi, Mao Xin, Huang Qiuju, Su Zhiheng, Lu Qinpei, Guo Hongwei
Guangxi Key Laboratory of Bioactive Molecules Research and Evaluation, College of Pharmacy, Guangxi Medical University, Nanning 530021, China; Key Laboratory of Longevity and Aging-related Diseases of Ministry of Education, Center for Translational Medicine, Guangxi Medical University, Nanning 530021, China.
Guangxi Institute for Food and Drug Control, Nanning 530021, China.
Int J Biol Macromol. 2025 May;308(Pt 3):142641. doi: 10.1016/j.ijbiomac.2025.142641. Epub 2025 Mar 30.
Lychee (Litchi chinensis) is a subtropical fruit known for its potential health benefits. In this study, proanthocyanidins (condensed tannins) from lychee seeds (LSPAs) were isolated using a bioactivity-guided approach. Their structural characteristics, as well as antioxidant, anticancer, anti-α-amylase, and anti-tyrosinase activities, were comprehensively analyzed. Structural analysis using mass spectrometry revealed that LSPAs are polymeric compounds predominantly composed of procyanidins (PCs), with a number-average molecular weight (Mn) of 5803 Da as determined by gel permeation chromatography (GPC). LSPAs exhibited significant antioxidant activity in DPPH, ABTS, and hydroxyl radical scavenging assays, with IC values of 28.8 ± 1.3, 24.29 ± 1.93, and 119.67 ± 32.85 μg/mL, respectively. The FRAP assay showed antioxidant activity of 0.45 ± 0.01 μM Fe(II) equivalent/g DW. The CCK-8 assay demonstrated potent anti-breast cancer efficacy of LSPAs (IC = 25.78 ± 0.37 μg/mL). Notably, LSPAs suppressed mammosphere formation and downregulated Sox2 and NICD1 expression in breast cancer stem cells (BCSCs). Molecular docking and dynamics simulations confirmed stable interactions between LSPAs and Sox2, primarily mediated by van der Waals forces. Enzyme kinetics and fluorescence spectroscopy further revealed that LSPAs effectively inhibited both α-amylase (IC = 0.12 ± 0.004 μg/mL) and tyrosinase (IC = 66.34 ± 0.37 μg/mL) activities by inducing conformational alterations and modifying the amino acid microenvironment of these enzymes. These findings establish LSPAs as promising multifunctional inhibitors with potential applications in food, cosmetics, and pharmaceuticals.
荔枝（Litchi chinensis）是一种亚热带水果，因其潜在的健康益处而闻名。在本研究中，采用生物活性导向法从荔枝种子中分离出原花青素（缩合单宁，LSPAs）。对其结构特征以及抗氧化、抗癌、抗α-淀粉酶和抗酪氨酸酶活性进行了全面分析。质谱结构分析表明，LSPAs是主要由原花青素（PCs）组成的聚合物化合物，凝胶渗透色谱（GPC）测定其数均分子量（Mn）为5803 Da。LSPAs在DPPH、ABTS和羟基自由基清除试验中表现出显著的抗氧化活性，IC值分别为28.8±1.3、24.29±1.93和119.67±32.85μg/mL。FRAP试验显示抗氧化活性为0.45±0.01μM Fe（II）当量/g DW。CCK-8试验证明LSPAs具有强大的抗乳腺癌功效（IC = 25.78±0.37μg/mL）。值得注意的是，LSPAs抑制乳腺癌干细胞（BCSCs）中乳腺球的形成，并下调Sox2和NICD1的表达。分子对接和动力学模拟证实LSPAs与Sox2之间存在稳定的相互作用，主要由范德华力介导。酶动力学和荧光光谱进一步表明，LSPAs通过诱导构象改变和修饰这些酶的氨基酸微环境，有效抑制α-淀粉酶（IC = 0.12±0.004μg/mL）和酪氨酸酶（IC = 66.34±0.37μg/mL）的活性。这些发现表明LSPAs是有前景的多功能抑制剂，在食品、化妆品和制药领域具有潜在应用价值。
