Chrysikopoulou Vasiliki, Rampaouni Aikaterini, Koutsia Eleni, Ofrydopoulou Anna, Mittas Nikolaos, Tsoupras Alexandros
Hephaestus Laboratory, School of Chemistry, Faculty of Sciences, Kavala University Campus, Democritus University of Thrace, St. Lucas, 65404 Kavala, Greece.
Nutrients. 2025 Aug 14;17(16):2643. doi: 10.3390/nu17162643.
BACKGROUND/OBJECTIVES: Vitamin C is frequently used in several dietary supplements due to its proposed health-promoting properties, while phenolic compounds and especially flavonoids have been suggested to provide synergistic antioxidant and cardiovascular benefits. However, the specific interactions between these compounds and their individual contributions to biological activity remain underexplored. This study aimed to evaluate the antioxidant potential and anti-inflammatory and antiplatelet biological effects of a high-dose (1 g) vitamin C-low-dose (50 mg) bioflavonoid (VCF)-based supplement using both in vitro and in vivo approaches in human platelets.
Total phenolic content was quantified and antioxidant capacity was assessed using DPPH, FRAP, and ABTS assays and compared to individual phenolic standard compounds, including (simple phenolics like gallic acid, flavonoids like quercetin and catechin, and polyphenols like curcumin and tannin), and a standard supplement containing only high-dose vitamin C (VC). ATR-FTIR spectroscopy was used to assess molecular interactions between vitamin C and flavonoids. In vitro anti-inflammatory and antiplatelet activities of all supplements and standards were assessed by quantifying their IC values against ADP, PAF, and thrombin-induced platelet aggregation. The in vivo evaluation of the efficacy and synergy of VCF supplement versus VC was achieved by a two-arm clinical study in healthy volunteers by quantifying their platelet reactivity, which was measured via EC values on the aforementioned platelet agonists (PAF, ADP, and Thrombin) before (t = 0) and after receiving either solely VC or VCF supplementation for four weeks.
From all phenolic standards, the flavonoids and especially a mixture of flavonoids (catechin + quercetin) showed higher in vitro antioxidant capacity and anti-inflammatory and antiplatelet efficacy, followed by polyphenols and then simple phenolics. The VCF supplement showed the most potent antioxidant capacity, but also the strongest anti-inflammatory and antiplatelet activities too, in comparison to the VC and the mixture of flavonoids, suggesting higher synergy and thus bio-efficacy as a result of the co-presence of flavonoids and vitamin C in this supplement. Platelet reactivity decreased over time for PAF and thrombin in both arms of the trial, but no significant differences were observed between treatment groups, suggesting that the number of flavonoids used was not sufficient to translate the in vitro findings to the in vivo setting.
VC-containing supplements provide antioxidant, anti-inflammatory, and antiplatelet benefits, while the incorporation of flavonoids may provide synergistic health benefits, but more in vivo assessment is needed to fully evaluate the dose efficacy.
背景/目的：由于维生素C具有促进健康的特性，它经常被用于多种膳食补充剂中，而酚类化合物尤其是黄酮类化合物被认为具有协同抗氧化和心血管益处。然而，这些化合物之间的具体相互作用及其对生物活性的各自贡献仍未得到充分研究。本研究旨在通过体外和体内方法评估高剂量（1克）维生素C - 低剂量（50毫克）生物类黄酮（VCF）补充剂对人血小板的抗氧化潜力、抗炎和抗血小板生物学效应。
使用DPPH、FRAP和ABTS测定法对总酚含量进行定量并评估抗氧化能力，并与包括（如没食子酸等简单酚类、如槲皮素和儿茶素等黄酮类以及如姜黄素和单宁等多酚类）的单个酚类标准化合物以及仅含高剂量维生素C（VC）的标准补充剂进行比较。使用衰减全反射傅里叶变换红外光谱（ATR - FTIR）评估维生素C与黄酮类之间的分子相互作用。通过量化所有补充剂和标准品对ADP、PAF和凝血酶诱导的血小板聚集的IC值来评估其体外抗炎和抗血小板活性。通过对健康志愿者进行双臂临床研究，量化他们的血小板反应性来实现对VCF补充剂与VC疗效和协同作用的体内评估，血小板反应性通过在接受单独的VC或VCF补充剂四周之前（t = 0）和之后对上述血小板激动剂（PAF、ADP和凝血酶）的EC值进行测量。
在所有酚类标准品中，黄酮类尤其是黄酮类混合物（儿茶素 + 槲皮素）显示出更高的体外抗氧化能力、抗炎和抗血小板功效，其次是多酚类，然后是简单酚类。与VC和黄酮类混合物相比，VCF补充剂显示出最强的抗氧化能力，同时也具有最强的抗炎和抗血小板活性，表明由于该补充剂中黄酮类和维生素C同时存在，具有更高的协同作用以及因此更高的生物功效。在试验的两个组中，PAF和凝血酶诱导的血小板反应性随时间下降，但治疗组之间未观察到显著差异，这表明所使用的黄酮类数量不足以将体外研究结果转化为体内情况。
含VC的补充剂具有抗氧化、抗炎和抗血小板益处，而加入黄酮类可能提供协同的健康益处，但需要更多的体内评估来全面评估剂量疗效。
