Aim: Resolvins, maresins and lipoxins are lipid mediators issued from essential polyunsaturated fatty acids which are the first anti-inflammatory and pro-resolving signals identified during the resolution phase of inf...Aim: Resolvins, maresins and lipoxins are lipid mediators issued from essential polyunsaturated fatty acids which are the first anti-inflammatory and pro-resolving signals identified during the resolution phase of inflammation. As borage oil and/or borage seed extracts have shown beneficial action in treatment of atopic dermatitis or eczema in human and canine, we have modified a borage oil component by using biotechnology in order to get a compound structurally related to a polyunsaturated fatty acid, and we have studied its ability to reduce inflammation mediators production through the generation of resolvins, maresins and/or lipoxins. Additionally, we have demonstrated the potent anti-inflammatory effect of this new compound which consists in borage seed oil aminopropanediol amides, through an in vivo study concerning subjects suffering from psoriasis or atopic dermatitis. Study Design/Methods: For the in vitro study, inflammation was induced in co-cultures of human dendritic cells and normal keratinocytes by the addition of PMA and the calcium ionophore A23187. Ability of our borage seed oil aminopropanediol amides to increase resolvin D2, maresin 1 and lipoxins A4 and B4 synthesis was then measured. Pro-inflammatory cytokines (IL-1β, IL-6, IL-8) and PGE2 productions were also quantified. For the in vivo study, 36 subjects suffering from psoriasis or atopic dermatitis have used twice a day during 30 days, a formulation containing borage seed oil aminopropanediol amides. Before the beginning of the study and after 30 days’ treatment, the severity of psoriasis and of atopic dermatitis was evaluated by using the PGA and the SCORAD scoring scales, respectively. Results: Borage seed oil aminopropanediol amides were able to significantly increase the resolvin D2, maresin 1 and lipoxins A4 and B4 synthesis. Concomitantly, they were also able to significantly inhibit the production of IL-1β, IL-6, IL-8 and PGE2 induced by the PMA and the calcium ionophore A23187 in the in vitro co-culture model used. Introduced in formulation, borage seed oil aminopropanediol amides significantly reduced the clinical manifestations of psoriasis and atopic dermatitis. Conclusion: Our in vitro and in vivo study clearly showed the anti-inflammatory activity of borage seed oil aminopropanediol amides and emphasized the putative role of pro-resolving lipid mediators in the treatment of atopic dermatitis, psoriasis or other inflammation-induced skin diseases.展开更多
鱼油因较低的水溶性限制了其应用。该研究通过在鱼油中添加不同浓度的磷脂,构建鱼油-磷脂自乳化体系,表征其理化性质,并结合药代动力学分析,系统评价该体系的体内吸收效果。结果表明,鱼油中添加6%(质量分数)磷脂能形成良好的自乳化乳液...鱼油因较低的水溶性限制了其应用。该研究通过在鱼油中添加不同浓度的磷脂,构建鱼油-磷脂自乳化体系,表征其理化性质,并结合药代动力学分析,系统评价该体系的体内吸收效果。结果表明,鱼油中添加6%(质量分数)磷脂能形成良好的自乳化乳液,可显著降低油水界面张力和乳液油滴粒径,抑制液滴聚并,增强乳液的稳定性;药代动力学实验表明,该磷脂-鱼油自乳化体系能显著缩短鱼油中二十碳五烯酸(eicosapentaenoic acid,EPA)和二十二碳六烯酸(docosahexaenoic acid,DHA)的达峰时间(T_(max)最快至1.5 h)并提高最大血药浓度(C_(max)达1.39 mg/mL),显著改善不同类型鱼油的体内吸收效果,其中EPA的0~24 h的血药浓度-时间曲线下面积(area under the plasma concentration-time curve from time 0 to 24 hours,AUC_(0-24h))可提升至2.66~3.74倍,DHA的AUC_(0-24h)可提升至3.20~7.44倍。该研究为高生物利用度的鱼油制剂产品开发提供了数据支撑和技术参考。展开更多
文摘Aim: Resolvins, maresins and lipoxins are lipid mediators issued from essential polyunsaturated fatty acids which are the first anti-inflammatory and pro-resolving signals identified during the resolution phase of inflammation. As borage oil and/or borage seed extracts have shown beneficial action in treatment of atopic dermatitis or eczema in human and canine, we have modified a borage oil component by using biotechnology in order to get a compound structurally related to a polyunsaturated fatty acid, and we have studied its ability to reduce inflammation mediators production through the generation of resolvins, maresins and/or lipoxins. Additionally, we have demonstrated the potent anti-inflammatory effect of this new compound which consists in borage seed oil aminopropanediol amides, through an in vivo study concerning subjects suffering from psoriasis or atopic dermatitis. Study Design/Methods: For the in vitro study, inflammation was induced in co-cultures of human dendritic cells and normal keratinocytes by the addition of PMA and the calcium ionophore A23187. Ability of our borage seed oil aminopropanediol amides to increase resolvin D2, maresin 1 and lipoxins A4 and B4 synthesis was then measured. Pro-inflammatory cytokines (IL-1β, IL-6, IL-8) and PGE2 productions were also quantified. For the in vivo study, 36 subjects suffering from psoriasis or atopic dermatitis have used twice a day during 30 days, a formulation containing borage seed oil aminopropanediol amides. Before the beginning of the study and after 30 days’ treatment, the severity of psoriasis and of atopic dermatitis was evaluated by using the PGA and the SCORAD scoring scales, respectively. Results: Borage seed oil aminopropanediol amides were able to significantly increase the resolvin D2, maresin 1 and lipoxins A4 and B4 synthesis. Concomitantly, they were also able to significantly inhibit the production of IL-1β, IL-6, IL-8 and PGE2 induced by the PMA and the calcium ionophore A23187 in the in vitro co-culture model used. Introduced in formulation, borage seed oil aminopropanediol amides significantly reduced the clinical manifestations of psoriasis and atopic dermatitis. Conclusion: Our in vitro and in vivo study clearly showed the anti-inflammatory activity of borage seed oil aminopropanediol amides and emphasized the putative role of pro-resolving lipid mediators in the treatment of atopic dermatitis, psoriasis or other inflammation-induced skin diseases.
文摘鱼油因较低的水溶性限制了其应用。该研究通过在鱼油中添加不同浓度的磷脂,构建鱼油-磷脂自乳化体系,表征其理化性质,并结合药代动力学分析,系统评价该体系的体内吸收效果。结果表明,鱼油中添加6%(质量分数)磷脂能形成良好的自乳化乳液,可显著降低油水界面张力和乳液油滴粒径,抑制液滴聚并,增强乳液的稳定性;药代动力学实验表明,该磷脂-鱼油自乳化体系能显著缩短鱼油中二十碳五烯酸(eicosapentaenoic acid,EPA)和二十二碳六烯酸(docosahexaenoic acid,DHA)的达峰时间(T_(max)最快至1.5 h)并提高最大血药浓度(C_(max)达1.39 mg/mL),显著改善不同类型鱼油的体内吸收效果,其中EPA的0~24 h的血药浓度-时间曲线下面积(area under the plasma concentration-time curve from time 0 to 24 hours,AUC_(0-24h))可提升至2.66~3.74倍,DHA的AUC_(0-24h)可提升至3.20~7.44倍。该研究为高生物利用度的鱼油制剂产品开发提供了数据支撑和技术参考。
