Wyżga Beata, Kamiński Kamil, Głowacka Kinga, Hąc-Wydro Katarzyna
Jagiellonian University, Faculty of Chemistry, Gronostajowa 2, Kraków 30-387, Poland; Jagiellonian University, Doctoral School of Exact and Natural Sciences, Łojasiewicza 11, Kraków 30-348, Poland.
Jagiellonian University, Faculty of Chemistry, Gronostajowa 2, Kraków 30-387, Poland.
Chem Phys Lipids. 2025 Aug;270:105511. doi: 10.1016/j.chemphyslip.2025.105511. Epub 2025 Jun 11.
Hinokitiol (β-thujaplicin) is a natural antimicrobial agent used in cosmetics. The aim of presented studies was to gain insight into the interactions of hinokitiol with lipids in model membranes and to correlate this with the selective effect of hinokitiol on cells. To reach this goal, the toxicity of hinokitiol was evaluated using keratinocyte and fibroblast cell lines, and studies were performed on lipid monolayers (both one component and mixed systems). During investigations the surface pressure - area measurements, penetration studies and Brewster angle microscopy experiments were done. The analysis of the parameters calculated from the experimental data and the comparison of BAM images evidenced that, at membrane - related surface pressure, hinokitiol does not insert into model keratinocyte and fibroblast membranes and its impact on these systems is very weak. This important conclusion correlates with the in vitro experiments. The results for one component systems evidenced that the effect of hinokitiol on mammalian lipid films depends on the monolayer organisation and the lipid structure (especially the lipid polar head). In consequence, the type and proportion of lipids determines the effect of hinokitiol on the mixed films. The latter corroborates with the differences in the influence of hinokitiol on bacteria compared to mammalian lipids. It was concluded that hinokitiol exhibits selective activity toward bacterial cells compared to mammalian cells and their corresponding model membranes. Thus, the predominance of hinokitiol's antibacterial properties over its toxicity to skin cells may therefore be related to interactions of this compound with membrane lipids.
扁柏酚（β-崖柏素）是一种用于化妆品的天然抗菌剂。本研究的目的是深入了解扁柏酚与模型膜中脂质的相互作用，并将其与扁柏酚对细胞的选择性作用相关联。为实现这一目标，使用角质形成细胞和成纤维细胞系评估了扁柏酚的毒性，并对脂质单层（单组分和混合体系）进行了研究。在研究过程中，进行了表面压力-面积测量、渗透研究和布鲁斯特角显微镜实验。对从实验数据计算出的参数进行分析，并比较布鲁斯特角显微镜图像，结果表明，在与膜相关的表面压力下，扁柏酚不会插入模型角质形成细胞和成纤维细胞膜中，其对这些体系的影响非常微弱。这一重要结论与体外实验相关。单组分体系的结果表明，扁柏酚对哺乳动物脂质膜的影响取决于单层结构和脂质结构（尤其是脂质极性头部）。因此，脂质的类型和比例决定了扁柏酚对混合膜的影响。这一点与扁柏酚对细菌和哺乳动物脂质影响的差异相佐证。得出的结论是，与哺乳动物细胞及其相应的模型膜相比，扁柏酚对细菌细胞具有选择性活性。因此，扁柏酚的抗菌特性优于其对皮肤细胞的毒性，这可能与该化合物与膜脂质的相互作用有关。
