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Synthetic lipopeptides as potential topical therapeutics in wound and skin care: in vitro studies of permeation and skin cells behaviour

机译:伤口和皮肤护理中的合成脂肽作为潜在的局部治疗方法:渗透和皮肤细胞的体外研究

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摘要

Wound healing is an extraordinarily complicated process associating with the cell aging, slowing down of cell renewal mechanism and even loss of protective function to environmentally induced oxidative stress. A lack of effective treatment results in the appearance of skin lesions and chronic wounds. A satisfactory answer to skin care and therapy problems seems to be a molecule Gly-His-Lys of natural origin that promotes synthesis of collagen, inhibits the activity of matrix metalloproteinases (MMPs) and reduces the activity of collagenases. Several Gly-His-Lys analogues were obtained to investigate their antimicrobial properties. Three lipophilic analogues with the structure numbering 1b, 2b, 4b, exhibit significant effect against bacteria and were selected for in vitro evaluation of skin cells behaviour. In the present studies, an in vitro model of wound repair, proliferative cell staining, and tracking of living cells were used. Cell proliferation and cell migration, as important actions during the wound repair process, were studied. All the analogues provided an optimal environment for the growth, development and viability of skin cells. Microscopic changes in the morphology of fibroblasts and keratinocytes confirmed the positive effect of all the analogues on their growth and condition. Franz-type diffusion studies and the behaviour of analogues in the in vitro model of permeation were also performed. Permeability and diffusion coefficients were measured using UV-Vis spectrophotometry and RP-HPLC techniques. A substantial increase of permeability parameters for the lipophilic analogues was noticed. The outcomes of these studies suggest that lipophilic analogues possess a high potential as topical therapeutics. In relation with their proved antimicrobial activity, their safety profile and great tolerance for human skin show that they may be applied in both skin care and wound therapies.
机译:伤口愈合是一种与细胞衰老的非常复杂的过程,减缓细胞更新机制甚至甚至丧失保护功能以对环境诱导的氧化应激。缺乏有效的治疗导致皮肤病变和慢性伤口的出现。对皮肤护理和治疗问题的令人满意的答案似乎是促进胶原蛋白合成的天然来源的分子 - 他的溶解,抑制基质金属蛋白酶(MMP)的活性并减少胶原酶的活性。获得了几种Gly-His-Lys类似物以研究其抗微生物性质。具有结构编号1B,2B,4B的三种亲脂性类似物对细菌具有显着影响,并选择用于对皮肤细胞的体外评估。在本研究中,使用伤口修复,增殖细胞染色的体外模型和活细胞跟踪。研究了细胞增殖和细胞迁移,作为伤口修复过程中的重要作用,是在伤口修复过程中的重要作用。所有类似物都为皮肤细胞的生长,发育和活力提供了最佳环境。成纤维细胞和角质形成细胞形态的显微变化证实了所有类似物对其生长和病症的正效应。还进行了Franz型扩散研究和体外渗透模型中的类似物的行为。使用UV-Vis分光光度法和RP-HPLC技术测量渗透率和扩散系数。注意到亲脂性类似物的显着增加的渗透性参数。这些研究的结果表明,亲脂性类似物具有高潜力作为局部治疗。在其被证明的抗微生物活性方面,他们的安全性曲线和对人体皮肤的巨大耐受性表明它们可以应用于护肤和伤口疗法。

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  • 来源
    《RSC Advances》 |2016年第116期|共12页
  • 作者单位

    Gdansk Univ Technol Fac Chem Dept Organ Chem 11-12 Narutowicza St PL-80233 Gdansk Poland;

    Med Univ Gdansk Fac Med Dept Clin Immunol &

    Transplantol 7 Debinki St PL-80211 Gdansk Poland;

    Gdansk Univ Technol Fac Chem Dept Organ Chem 11-12 Narutowicza St PL-80233 Gdansk Poland;

    Med Univ Gdansk Fac Med Dept Clin Immunol &

    Transplantol 7 Debinki St PL-80211 Gdansk Poland;

    Gdansk Univ Technol Fac Chem Dept Organ Chem 11-12 Narutowicza St PL-80233 Gdansk Poland;

    Med Univ Gdansk Fac Med Dept Clin Immunol &

    Transplantol 7 Debinki St PL-80211 Gdansk Poland;

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  • 正文语种 eng
  • 中图分类 化学;
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