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敏感性肌肤作为令人困扰的皮肤问题已经成为影响生活质量的关键因素之一。敏感肌肤通常伴随末梢神经感受器的过度反应,尤其是由于TRPV1过度活跃所导致的灼烧、刺痛的等不良感觉。之前的研究显示,末梢神经感受器的TRPV1受体对于辣椒素的敏感性与自述的敏感肌肤现象具有明确的相关性。通过筛选我们确认4-叔丁基环己烷作为特定的TRPV1拮抗剂,并经人体测试证明可有效阻断由辣椒素引起的灼烧感或刺痛感,从而有效舒缓肌肤不适感。体外测试In vitro:H EK293细胞能够稳定地表达重组人类TRPV1受体,可用来筛选潜在的TRPV1拮抗剂。由于辣椒素能激活TRPV1,诱导FLEX系统中钙离子浓度的变化(钙离子的连续变化),并对钙离子浓度的变化进行测定。体内测试In vivo:30位志愿者对辣椒素的敏感性进行研究测试,使用两种不同的软膏涂于面部,一种含有辣椒素,另一种含有辣椒素和0.4%的4-叔丁基环己烷。在随后的3分钟评价其刺痛感和灼烧感,按以下几个等级评分:0(没有感觉)——4(强烈的感觉);使用Wilcoxon平行对照方法进行统计分析。4-叔丁基环己烷可以抑制由于辣椒素诱导的通过TRPV1的钙离子流量,在人体测试中,其IC50为34μM。刺痛的感觉评分显著降低,由1.6降至0.6(p<0.001),灼烧感的感觉评分也明显降低,从2.8降至0.8(p<0.0001)。基于这些结果,我们确认4-叔丁基环己烷是有效的TRPV1拮抗剂,无论体外实验还是活体实验都得到了很好的证明。此外,该活性物能有效舒缓敏感肌肤,从而抑制刺痛感和灼烧感。
Sensitive skin as a disturbing skin problem has become one of the key factors affecting the quality of life. Sensitive skin is often accompanied by excessive reaction of peripheral nerve receptors, especially due to burning, tingling and other bad feelings due to TRPV1 over-activity. Previous studies have shown that peripheral sensillum TRPV1 receptors have a clear correlation between the sensitivity to capsaicin and self-described sensitive skin phenomena. We identified 4-tert-butylcyclohexane as a specific TRPV1 antagonist by screening and have been shown to be effective in blocking the sensation of burning or tingling caused by capsaicin as a result of human testing, thereby effectively alleviating skin discomfort. In Vitro Testing In vitro: H EK293 cells stably express the recombinant human TRPV1 receptor and can be used to screen potential TRPV1 antagonists. Since capsaicin activates TRPV1, it induces a change in the concentration of calcium ions in the FLEX system (a continuous change in calcium ions), and changes in the concentration of calcium ions are measured. In vivo: In vivo: 30 volunteers tested their sensitivity to capsaicin using two different ointments applied to the face, one containing capsaicin and the other containing capsaicin and 0.4% 4-tert-butylcyclohexane alkyl. The tingling sensation and burning sensation were evaluated in the following 3 minutes, and were rated as follows: 0 (no sensation) - 4 (strong sensation); statistical analysis was performed using the Wilcoxon parallel control method. 4-tert-Butylcyclohexane inhibits Ca2 + flux through TRPV1 induced by capsaicin and has an IC50 of 34 μM in human tests. The tingling sensory score was significantly reduced from 1.6 to 0.6 (p <0.001), and the sensation of burning sensation was also significantly reduced from 2.8 to 0.8 (p <0.0001). Based on these results, we confirmed that 4-tert-butylcyclohexane is a potent TRPV1 antagonist and is well demonstrated both in vitro and in vivo. In addition, the active agent effectively soothes sensitive skin, thereby inhibiting tingling and burning sensation.