Abstract：
BACKGROUND: Transient receptor potential vanilloid 1 (TRPV1) is associated with skin sensitivity and mainly activated by capsaicin and heat. Interestingly, troxerutin can inhibit TRPV1 activation. However, its efficacy in reducing skin sensitivity remains undetermined.
OBJECTIVE: We evaluated the efficacy of troxerutin in alleviating skin sensitivity using clinical tests and in vitro experiments.
METHODS: For the in vitro experiment, HaCaT keratinocytes were pretreated with different concentrations of troxerutin, followed by incubation with 50 μM capsaicin for 1, 24, or 48 h. The gene and protein expressions of four inflammatory cytokines involved in skin irritation were determined. Among 35 Korean women with sensitive skin recruited for the clinical trial, 13 were involved in assessing the immediate soothing effects of 0.1% and 0.0095% troxerutin following capsaicin irritation, whereas 22 participated in evaluating the preventive soothing effect of 10% and 1% troxerutin over 4 weeks against capsaicin- and heat-induced irritation. We evaluated the soothing rate using skin redness, visual analog scale, and high temperature sensitive index as evaluation indices.
RESULTS: Troxerutin inhibited the mRNA and protein expressions of cytokines in capsaicin-treated keratinocytes. In the clinical study, 0.1% and 0.0095% troxerutin promptly alleviated capsaicin-induced skin redness, whereas 10% troxerutin notably decreased both the visual analog scale and high temperature sensitive index for capsaicin- and heat-related irritation. However, 1% troxerutin was only effective in reducing the visual analog scale in response to capsaicin irritation.
CONCLUSIONS: Troxerutin can inhibit TRPV1 activation in clinical and in vitro tests.
OBJECTIVE: We evaluated the efficacy of troxerutin in alleviating skin sensitivity using clinical tests and in vitro experiments.
METHODS: For the in vitro experiment, HaCaT keratinocytes were pretreated with different concentrations of troxerutin, followed by incubation with 50 μM capsaicin for 1, 24, or 48 h. The gene and protein expressions of four inflammatory cytokines involved in skin irritation were determined. Among 35 Korean women with sensitive skin recruited for the clinical trial, 13 were involved in assessing the immediate soothing effects of 0.1% and 0.0095% troxerutin following capsaicin irritation, whereas 22 participated in evaluating the preventive soothing effect of 10% and 1% troxerutin over 4 weeks against capsaicin- and heat-induced irritation. We evaluated the soothing rate using skin redness, visual analog scale, and high temperature sensitive index as evaluation indices.
RESULTS: Troxerutin inhibited the mRNA and protein expressions of cytokines in capsaicin-treated keratinocytes. In the clinical study, 0.1% and 0.0095% troxerutin promptly alleviated capsaicin-induced skin redness, whereas 10% troxerutin notably decreased both the visual analog scale and high temperature sensitive index for capsaicin- and heat-related irritation. However, 1% troxerutin was only effective in reducing the visual analog scale in response to capsaicin irritation.
CONCLUSIONS: Troxerutin can inhibit TRPV1 activation in clinical and in vitro tests.
摘要：
背景：瞬时受体电位香草素1（TRPV1）与皮肤敏感性有关，主要由辣椒素和热激活。有趣的是,曲克鲁丁可以抑制TRPV1的激活。然而,其降低皮肤敏感性的功效尚不确定。
目的：我们通过临床试验和体外实验评估了曲克鲁丁减轻皮肤敏感性的功效。
方法：对于体外实验，HaCaT角质形成细胞用不同浓度的曲克鲁丁预处理，然后用50μM辣椒素孵育1、24或48小时。测定与皮肤刺激有关的四种炎性细胞因子的基因和蛋白表达。在为临床试验招募的35名皮肤敏感的韩国女性中，13参与评估辣椒素刺激后0.1％和0.0095％曲克鲁丁的即时舒缓效果，22人参与评估10%和1%曲克鲁丁在4周内对辣椒素和热刺激的预防性舒缓效果。我们用皮肤发红来评估舒缓率，视觉模拟量表,和高温敏感指数作为评价指标。
结果：Troxerutin抑制辣椒素处理的角质形成细胞中细胞因子的mRNA和蛋白表达。在临床研究中,0.1%和0.0095%曲克鲁丁迅速缓解辣椒素诱导的皮肤发红，而10％的曲克鲁丁显着降低了辣椒素和热相关刺激的视觉模拟量表和高温敏感指数。然而,1％曲克鲁丁仅可有效降低辣椒素刺激的视觉模拟量表。
结论：曲克鲁丁在临床和体外实验中均能抑制TRPV1的活化。
目的：我们通过临床试验和体外实验评估了曲克鲁丁减轻皮肤敏感性的功效。
方法：对于体外实验，HaCaT角质形成细胞用不同浓度的曲克鲁丁预处理，然后用50μM辣椒素孵育1、24或48小时。测定与皮肤刺激有关的四种炎性细胞因子的基因和蛋白表达。在为临床试验招募的35名皮肤敏感的韩国女性中，13参与评估辣椒素刺激后0.1％和0.0095％曲克鲁丁的即时舒缓效果，22人参与评估10%和1%曲克鲁丁在4周内对辣椒素和热刺激的预防性舒缓效果。我们用皮肤发红来评估舒缓率，视觉模拟量表,和高温敏感指数作为评价指标。
结果：Troxerutin抑制辣椒素处理的角质形成细胞中细胞因子的mRNA和蛋白表达。在临床研究中,0.1%和0.0095%曲克鲁丁迅速缓解辣椒素诱导的皮肤发红，而10％的曲克鲁丁显着降低了辣椒素和热相关刺激的视觉模拟量表和高温敏感指数。然而,1％曲克鲁丁仅可有效降低辣椒素刺激的视觉模拟量表。
结论：曲克鲁丁在临床和体外实验中均能抑制TRPV1的活化。
