Instituto de Biología Molecular y Celular (IBMC) and Instituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universitas Miguel Hernández, 03202, Elche, Spain.
Programs of Molecular Mechanisms and Experimental Therapeutics in Oncology (ONCOBell), Catalan Institute of Oncology, Bellvitge Institute for Biomedical Research, Granvia de l'Hopitalet 199, 08908, L'Hospitalet de Llobregat, 08907 Barcelona, Spain.
Int J Mol Sci. 2019 Apr 30;20(9):2148. doi: 10.3390/ijms20092148.
Ultraviolet (UV) radiation, especially types A (UVA) and B (UVB), is one of the main causes of skin disorders, including photoaging and skin cancer. Ultraviolent radiation causes oxidative stress, inflammation, p53 induction, DNA damage, mutagenesis, and oxidation of various molecules such as lipids and proteins. In recent decades, the use of polyphenols as molecules with an antioxidant and anti-inflammatory capacity has increased. However, some of these compounds are poorly soluble, and information regarding their absorption and bioavailability is scarce. The main objective of this study was to compare the intestinal absorption and biological activity of apigenin and its more soluble potassium salt (apigenin-K) in terms of antioxidant and photoprotective capacity. Photoprotective effects against UVA and UVB radiation were studied in human keratinocytes, and antioxidant capacity was determined by different methods, including trolox equivalent antioxidant capacity (TEAC), ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity (ORAC) assays. Finally, the intestinal absorption of both apigenins was determined using an in vitro Caco-2 cell model. Apigenin showed a slightly higher antioxidant capacity in antioxidant activity assays when compared with apigenin-K. However, no significant differences were obtained for their photoprotective capacities against UVA or UVB. Results indicated that both apigenins protected cell viability in approximately 50% at 5 J/m of UVA and 90% at 500 J/m of UVB radiation. Regarding intestinal absorption, both apigenins showed similar apparent permeabilities (), 1.81 × 10 cm/s and 1.78 × 10 cm/s, respectively. Taken together, these results suggest that both apigenins may be interesting candidates for the development of oral (nutraceutical) and topical photoprotective ingredients against UVA and UVB-induced skin damage, but the increased water solubility of apigenin-K makes it the best candidate for further development.
紫外线(UV)辐射,尤其是 A 型(UVA)和 B 型(UVB),是皮肤疾病的主要原因之一,包括光老化和皮肤癌。紫外线辐射会导致氧化应激、炎症、p53 诱导、DNA 损伤、突变和各种分子如脂质和蛋白质的氧化。在过去几十年中,多酚类化合物作为具有抗氧化和抗炎能力的分子的使用有所增加。然而,其中一些化合物的溶解度较差,关于它们的吸收和生物利用度的信息也很缺乏。本研究的主要目的是比较芹菜素及其更易溶解的钾盐(芹菜素-K)在抗氧化和光保护能力方面的肠吸收和生物学活性。在人角质形成细胞中研究了它们对 UVA 和 UVB 辐射的光保护作用,抗氧化能力通过不同方法确定,包括 Trolox 等效抗氧化能力(TEAC)、铁还原抗氧化能力(FRAP)和氧自由基吸收能力(ORAC)测定法。最后,使用体外 Caco-2 细胞模型测定了两种芹菜素的肠吸收。与芹菜素-K 相比,芹菜素在抗氧化活性测定中表现出稍高的抗氧化能力。然而,它们对 UVA 或 UVB 的光保护能力没有显著差异。结果表明,两种芹菜素在 5 J/m 的 UVA 和 500 J/m 的 UVB 辐射下,细胞存活率分别约为 50%和 90%。关于肠吸收,两种芹菜素的表观渗透率()相似,分别为 1.81×10 和 1.78×10 cm/s。综上所述,这些结果表明,两种芹菜素都可能是开发口服(营养)和局部光保护成分以对抗 UVA 和 UVB 诱导的皮肤损伤的有前途的候选物,但芹菜素-K 的水溶性增加使其成为进一步开发的最佳候选物。
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