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Photoprotective effect of 18β-glycyrrhetinic acid derivatives against ultra violet (UV)-B-Induced skin aging
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2022-09-24 , DOI: 10.1016/j.bmcl.2022.128984
Amit Kumar 1 , Sajida Archo 2 , Chetan Paul Singh 3 , Shahid Hussain Naikoo 2 , Buddh Singh 3 , Sarabjit Kaur 4 , Sheikh Abdullah Tasduq 2
Affiliation  

Excessive exposure to sun can harm the skin, causing sunburn, photo-aging, and even skin cancer. Different benzylidene derivatives (A02-A18 and A19-A34) of 18β-Glycyrrhetinic acid (A01) were designed and synthesized in an effort to discover photo-protective compounds against UV-B -induced skin aging. The synthesized derivatives were subjected to cellular viability test using MTT assay in primary Human Dermal Fibroblasts (HDFs). The results indicate A01, A05, A15, A22, A23, A25, A26, A28, A29, A32, A33, and A34 significantly enhanced cell viability of HDFs. Compound A33 at 10 and 25 μM showed a significant photo-protective effect against UV-B (10 mJ/cm2) –induced damage in HDFs. A33 at 25 μM significantly restored the UV-B -induced damage via its potent anti-oxidant, anti-apoptotic effects and ability to prevent collagen degradation. These findings pave the way for further development of A33 as a photo-protective skin agent.



中文翻译:

18β-甘草次酸衍生物对紫外线(UV)-B-诱导的皮肤老化的光保护作用

过度暴露在阳光下会伤害皮肤,导致晒伤、光老化,甚至皮肤癌。设计和合成了 18β-甘草次酸(A01)的不同亚苄基衍生物(A02-A18A19-A34 ),旨在发现抗 UV-B 诱导的皮肤老化的光保护化合物。在原代人皮肤成纤维细胞 (HDF) 中使用 MTT 测定法对合成的衍生物进行细胞活力测试。结果表明A01、A05、A15、A22、A23、A25、A26、A28、A29、A32、A33 和 A34显着增强了 HDF 的细胞活力。10 和 25 μM 的化合物A33对 UV-B (10 mJ/cm 2 ) 诱导的 HDF 损伤具有显着的光保护作用。25  μ M的A33通过其有效的抗氧化、抗凋亡作用和防止胶原蛋白降解的能力显着恢复了 UV-B 诱导的损伤。这些发现为进一步开发 A33 作为光保护皮肤剂铺平了道路。

更新日期:2022-09-28
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