ИСТИНА

Aquaporins are tetrameric membrane-bound channels that facilitate transport of water and other small solutes across cell membranes. Within the aquaporin family, aquaporin 3 (AQP3) is expressed in the skin epidermis and is associated with the degree of skin hydration, regulation of proliferation of keratinocytes, wound healing. In addition, recent data suggest that water and glycerol transport by AQP3 is involved in the pathogenesis of atopic dermatitis, psoriasis, and skin ageing. Search of novel substances that could increase the expression of this protein is currently being sought. Thus, our research has focused on the development of a novel plant-based substance and evaluation its biological activity for targeted AQP3 regulation in skin keratinocytes. Through DiffDock computational modelling to predict affinity for AQP3 and biological activity profile, Aloe vera extract and trimethylglycine were chosen. Moreover, the dose finding cytotoxicity assay of selected substances was performed with MTT indicator on HaCaT cells. Finally, the substances’ ability to increase amount of AQP3 on keratinocytes was evaluated in the keratinocytes’ cell culture with ELISA immunoassay after 24 hours incubation. According to the results obtained, the EC70 for Aloe vera extract and trimethylglycine was 24.50% and 39.00%, respectively. Following the development and research, substance based on Aloe vera extract and trimethylglycine at a mass ratio of 1:1 had a good cytotoxicity profile, with an EC70 value of 11.95%. Furthermore, it was shown that the plant-based substance had a clear synergetic effect on stimulation and increase amount of AQP3. The complex at a mass ratio of 1:1 induced a significant increase of AQP3 amount up to 219%, compared to that of negative control (p<0.001). This effect was higher than the individual substances-mediated effect. Thus, the novel plant-based substance has a promising potential for the AQP3 regulation in skin and an interest in the development of dermatological drugs.