Lee Hyo Jin, Kim Daehoon, Choi Hyo Jeong, Kim Suhyeok, Shin Minhee, Kwak Seongsung, Lee Dong-Kyu, Kang Won-Ho
Gwanggyo R&D Center, Medytox Inc., Suwon-si, Korea.
J Cosmet Dermatol. 2024 Feb;23(2):666-675. doi: 10.1111/jocd.15984. Epub 2023 Sep 12.
This study aimed to investigate and verify the effect of cell-penetrating peptide (CPP)-conjugated soluble N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE) motif of vesicle-associated membrane protein 2 (VAMP2)-patterned peptide (INCI name: Acetyl sh-Oligopeptide-26 sh-Oligopeptide-27 SP, trade name: M.Biome-BT) on improving skin function in vitro.
The cytotoxicity of CPP-conjugated SNARE motif of VAMP2-patterned peptide (CVP) was investigated using the 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyl tetrazolium bromide (MTT) assay against B16-F10 cells and human dermal fibroblasts (HDFs) and a reconstructed skin irritation test. The anti-wrinkle activity of M.Biome-BT was determined by assessing the release of norepinephrine and dopamine in PC-12 cells via ELISA. The skin-whitening effects of CVP were assessed in B16-F10 cells by measuring the intra- and extracellular melanin contents and expression levels of melanin production-related genes, such as microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), and TRP-2.
CVP is not cytotoxic to B16-F10 cells and HDFs, and no skin irritation was observed. CVP treatment considerably diminished K -induced norepinephrine and dopamine secretion compared with the non-treated control group (62% and 40%, respectively). Additionally, the inhibition ability of CVP on norepinephrine and dopamine release was comparable to that of botulinum neurotoxin type A (BoNT/A). CVP also increased intracellular melanin content in a dose-dependent manner, whereas extracellular melanin content decreased (76%-85%). However, CVP treatment did not affect the mRNA expression of MITF, TYR, TRP-1, and TRP-2. These results suggest that CVP does not inhibit melanin production; however, it may induce a whitening effect by inhibiting melanin transport.
Taken together, our findings indicate that CVP could be used as an active and safe cosmeceutical ingredient for antiaging applications.
本研究旨在调查并验证细胞穿透肽（CPP）偶联的囊泡相关膜蛋白2（VAMP2）模式肽的可溶性N - 乙基马来酰亚胺敏感因子附着蛋白受体（SNARE）基序（国际化妆品原料名称：乙酰化sh - 寡肽 - 26 sh - 寡肽 - 27 SP，商品名：M.Biome - BT）在体外改善皮肤功能的效果。
使用3 -（4,5 - 二甲基噻唑 - 2 - 基）- 2,5 - 二苯基溴化四氮唑（MTT）法检测CPP偶联的VAMP2模式肽的SNARE基序（CVP）对B16 - F10细胞和人皮肤成纤维细胞（HDFs）的细胞毒性，并进行重建皮肤刺激性试验。通过酶联免疫吸附测定法评估PC - 12细胞中去甲肾上腺素和多巴胺的释放，以确定M.Biome - BT的抗皱活性。通过测量B16 - F10细胞内、外黑色素含量以及小眼畸形相关转录因子（MITF）、酪氨酸酶（TYR）、酪氨酸酶相关蛋白 - 1（TRP - 1）和TRP - 2等黑色素生成相关基因的表达水平，评估CVP的皮肤美白效果。
CVP对B16 - F10细胞和HDFs无细胞毒性，且未观察到皮肤刺激性。与未处理的对照组相比，CVP处理显著减少了K诱导的去甲肾上腺素和多巴胺分泌（分别为62%和40%）。此外，CVP对去甲肾上腺素和多巴胺释放的抑制能力与A型肉毒杆菌神经毒素（BoNT/A）相当。CVP还以剂量依赖性方式增加细胞内黑色素含量，而细胞外黑色素含量降低（76% - 85%）。然而，CVP处理不影响MITF、TYR、TRP - 1和TRP - 2的mRNA表达。这些结果表明，CVP不抑制黑色素生成；然而，它可能通过抑制黑色素转运诱导美白效果。
综上所述，我们的研究结果表明，CVP可作为一种活性且安全的药妆成分用于抗老化应用。
