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日用化学工业(中英文) ›› 2023, Vol. 53 ›› Issue (4): 390-397.doi: 10.3969/j.issn.1001-1803.2023.04.004

• 开发与应用 • 上一篇    下一篇

吡罗克酮乙醇胺盐的蛋白酶抑制作用及与硫酸锌复配的防脱发功效研究

Ranjit Kaur Bhogal1,陈旭斌2,David Messenger1,宫哲慧2,孙佳凝2,皮瑛瑛2,顾佳音2,*()   

  1. 1.联合利华科沃斯研发中心 人类生物科学与技术,贝德福德郡 MK44 1LQ,英国
    2.联合利华上海研发中心 美容健康事业部,上海 200335
  • 收稿日期:2023-03-03 修回日期:2023-04-11 出版日期:2023-04-22 发布日期:2023-04-25

Novel role of piroctone olamine on protease inhibition in vitro, and reduction in human hair shedding in combination of zinc sulfate in vivo

Kaur Bhogal Ranjit1,Chen Xubin2,Messenger David1,Gong Zhehui2,Sun Jianing2,Pi Yingying2,Gu Jiayin2,*()   

  1. 1. Human Biology Science & Technology, Unilever Research & Development Colworth Center, Bedfordshire MK44 1LQ, UK
    2. Beauty & Wellbeing, Unilever Research & Development Shanghai Center, Shanghai 200335, China
  • Received:2023-03-03 Revised:2023-04-11 Online:2023-04-22 Published:2023-04-25
  • Contact: * E-mail: jiayin.gu@unilever.com.

摘要:

蛋白水解机制导致棒状末端发根和毛囊之间的细胞粘附分解是头发脱落的最终步骤。在休止期晚期和脱落期,蛋白酶活性的增加导致大量脱发。利用EnzChekTM蛋白酶试剂盒,基于荧光方法检测了吡罗克酮乙醇胺盐在体外对蛋白酶的抑制作用;并对含吡罗克酮乙醇胺盐和硫酸锌的洗发水进行了两组含受脱发困扰的男性和女性参与者的临床防脱发功效测试。结果表明,吡罗克酮乙醇胺盐可以有效抑制蛋白酶的活性,0.5%吡罗克酮乙醇胺盐在体外可使胰蛋白酶的活性减少最高达53%。硫酸锌可以增强低浓度吡罗克酮乙醇胺盐对胰蛋白酶活性的抑制作用。两组临床测试显示,使用含0.5%吡罗克酮乙醇胺盐和0.018%硫酸锌的洗发水4周,8周和12周后,头发密度较使用前均有显著性增加,12周后分别增加2.7根/cm2和7.5根/cm2;较空白对照组,在8周和12周后均有显著性提高。由此提示了吡罗克酮乙醇胺盐对于棒状毛发的保留作用和含吡罗克酮乙醇胺盐和硫酸锌洗发水的防脱发功效。

关键词: 脱发, 脱落期, 毛发密度, 蛋白酶, 吡罗克酮乙醇胺盐, 硫酸锌

Abstract:

The process leading to the final step of hair shedding is reported to be driven by proteolytic activity and contributes to the detachment of club hair. During late telogen and exogen, increased protease activity may lead to excessive and unwanted hair loss. Materials that can correct proteolytic activity could be beneficial in reducing excessive hair loss. Piroctone olamine was assessed for the protease inhibition efficacy in vitro by deploying a direct fluorescence-based assay for detecting metallo-, serine, acid and sulfhydryl proteases. The assay detects protease activity by the means of a labelled pH-insensitive fluorescent dye where an increase in fluorescence is proportional to protease activity. The assay allows the assessment of materials that may inhibit protease activity of the target enzymes. Since serine proteases have been shown to play a role in the exogen phase of the hair growth cycle, trypsin a known serine protease was used as the target enzyme. Piroctone olamine was found to inhibit trypsin protease activity in a dose-dependent manner. The inhibitory effect was boosted with the addition zinc sulfate. The combination of zinc sulfate with piroctone olamine was formulated into a shampoo base for the evaluation of hair density efficacy in vivo. Male and female participants with hair loss concerns treated their scalp with a shampoo wash (treatment or placebo) 3 times per week for 12 weeks. Hair density was assessed at baseline followed by 4 weekly intervals. The results showed a significant increase in hair density following shampoo treatment versus baseline and versus placebo suggesting the combination of piroctone olamine and zinc sulfate plays a role in retaining hairs and consequently reducing hair fall.

Key words: hair shedding, exogen, hair density, protease, piroctone olamine, zinc sulfate

中图分类号: 

  • TQ658