● 항진균제

Climbazole은 샴푸 또는 컨디셔너와 같은 제형에서 비듬을 관리하고 방부제로 사용되는 이미다졸 계열 항진균제이다. 

클림바졸은 말레세지아 종에 대한 높은 체외 및 체내 효능을 보이며, 이는 비듬균 생성 억제에 대한 중요 역할을 하는 것으로 보인다.

진균 원형질막의 주요 성분인 Ergosterol 합성을 억제하는 작용(Climbazole은 lanosterol을 ergosterol로 전환하는데 필요한 효소인 lanosterol 14 a-demethylase를 억제해 진균막에서 ergosterol의 고갈로 구조와 기능을 방해해 진균 성장을 억제)을 하며 primary keratinocytes에서 small-proline-rich protein 발현을 촉진하는 각질 세포 분화를 상향 조절하는 것으로 나타났다. 

이외에도 모간 고정에 관여하는 모발 protease의 억제 효과도 보고된 바 있다.  

Climbazole (CBZ) is an imidazole antifungal agent used to manage dandruff in formulations such as shampoos or conditioners and as a preservative. It acts by inhibiting the synthesis of ergosterol, a major component in fungal plasma membranes (SCCP, 2009). In addition, CBZ has been shown to upregulate keratinocyte differentiation promoting the expression of small-proline-rich proteins in primary keratinocytes (Pople et al., 2014). 

 Bhogal et al. (2014) also reported inhibitory effects of CBZ on hair proteases involved in anchorage of the hair shaft in an in vitro study.

https://www.sciencedirect.com/science/article/pii/S0378517318305337

※ 클림바졸 MIC

climbazole (CLIM) showed good in vitro activity against M. pachydermatis with the the range of MICs (Minimal Inhibitory Concentration ) was between < 0.06 and 1 ug/ml with an empirical median mean of 0.06 ug/ml.

● 두피장벽 강화 효과

클림바졸은 각질세포막 단백질을 증가시켜 비듬으로 약해진 두피 장벽 강화에 도움을 준다. 

Microarray analysis was performed to profile gene expression changes in climbazole‐treated primary human keratinocyte cells. Results were independently validated using qPCR and analysis of protein expression using ELISA and immunocytochemistry.

Microarray analysis of climbazole‐treated keratinocytes showed statistically significant expression changes in genes associated with the gene ontology groups encompassing epidermal differentiation, keratinization, cholesterol biosynthesis and immune response. Upregulated genes  included a number encoding cornified envelope proteins such as group 3 late‐cornified envelope proteins, LCE3 and group 2 small‐proline‐rich proteins, SPRR2. Protein analysis studies of climbazole‐treated primary keratinocytes using ELISA and immunocytochemistry were able to demonstrate that the increase in gene transcripts translated into increased protein expression of these cornified envelope markers.

Climbazole treatment of primary keratinocytes results in an upregulation in expression of a number of genes including those encoding proteins involved in cornified envelope formation with further studies demonstrating this did translate into increased protein expression. A climbazole‐driven increase in cornified envelope proteins may improve the scalp skin barrier, which is known to be weaker in dandruff. These studies suggest climbazole, besides its antifungal activity, is delivering positive skin benefits helping to relive dandruff symptoms effectively.

Climbazole increases expression of cornified envelope proteins in primary keratinocytes, 2014,  A. E. Moore, D. C. S. Talbot, D. A. Jones, F. L. Lim, 

https://onlinelibrary.wiley.com/doi/abs/10.1111/ics.12137

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#클림바졸 #Climbazole