Department of Pharmacology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand.
Graduate School, Chiang Mai University, Chiang Mai 50200, Thailand.
Int J Mol Sci. 2023 Aug 5;24(15):12450. doi: 10.3390/ijms241512450.
Re-epithelialization is delayed in aged skin due to a slow rate of keratinocyte proliferation, and this may cause complications. Thus, there has been development of new therapies that increase treatment efficacy for skin wounds. Epidermal growth factor (EGF) has been clinically used, but this agent is expensive, and its activity is less stable. Therefore, a stable compound possessing EGF-like properties may be an effective therapy, especially when combined with EGF. The current study discovered that pinocembrin (PC) effectively synergized with EGF in increasing keratinocyte viability. The combination of PC and EGF significantly enhanced the proliferation and wound closure rate of the keratinocyte monolayer through activating the phosphorylation of ERK and Akt. Although these effects of PC were like those of EGF, we clearly proved that PC did not transactivate EGFR. Recent data from a previous study revealed that PC activates G-protein-coupled receptor 120 which further activates ERK1/2 and Akt phosphorylation. Therefore, this clearly indicates that PC possesses a unique property to stimulate the growth and survival of keratinocytes through activating a different receptor, which subsequently conveys the signal to cross-talk with the effector kinases downstream of the EGFR, suggesting that PC is a potential compound to be combined with EGF.
在衰老的皮肤中,由于角质形成细胞增殖缓慢,上皮细胞再形成延迟,这可能导致并发症。因此,已经开发出了新的治疗方法来提高皮肤伤口的治疗效果。表皮生长因子 (EGF) 已在临床上使用,但这种药物价格昂贵,活性不稳定。因此,具有类似 EGF 特性的稳定化合物可能是一种有效的治疗方法,尤其是与 EGF 联合使用时。本研究发现,乔松素(PC)可与 EGF 协同有效增加角质形成细胞活力。PC 和 EGF 的组合通过激活 ERK 和 Akt 的磷酸化显著增强了角质形成细胞单层的增殖和伤口闭合率。尽管 PC 的这些作用类似于 EGF,但我们明确证明 PC 不会转导 EGFR。之前一项研究的最新数据表明,PC 激活 G 蛋白偶联受体 120,进一步激活 ERK1/2 和 Akt 磷酸化。因此,这清楚地表明,PC 通过激活不同的受体来刺激角质形成细胞的生长和存活,从而将信号传递给 EGFR 下游的效应激酶进行串扰,表明 PC 是一种与 EGF 结合的潜在化合物。