Artepillin C and Other Herbal PAK1‐blockers: Effects on Hair Cell Proliferation and Related PAK1‐dependent Biological Function in Cell Culture
PAK1 (RAC/CDC42‐activated kinase 1) is the major oncogenic kinase, and a number of herbal PAK1‐blockers such as propolis and curcumin have been shown to be anti‐oncogenic and anti‐melanogenic as well as anti‐alopecia (promoting hair growth). Previously, we found several distinct PAK1‐inhibitors in O...
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Published in | Phytotherapy research Vol. 30; no. 1; pp. 120 - 127 |
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Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
England
Heyden & Son
01.01.2016
Blackwell Publishing Ltd Wiley Subscription Services, Inc |
Subjects | |
Online Access | Get full text |
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Summary: | PAK1 (RAC/CDC42‐activated kinase 1) is the major oncogenic kinase, and a number of herbal PAK1‐blockers such as propolis and curcumin have been shown to be anti‐oncogenic and anti‐melanogenic as well as anti‐alopecia (promoting hair growth). Previously, we found several distinct PAK1‐inhibitors in Okinawa plants including Alpinia zerumbet (alpinia). Thus, here, we tested the effects of these herbal compounds and their derivatives on the growth of cancer or normal hair cells, and melanogenesis in cell culture of A549 lung cancer, hair follicle dermal papilla cell, and B16F10 melanoma. Among these herbal PAK1‐inhibitors, cucurbitacin I from bitter melon (Goya) turned out to be the most potent to inhibit the growth of human lung cancer cells with the IC₅₀ around 140 nM and to promote the growth of hair cells with the effective dose around 10 nM. Hispidin, a metabolite of 5,6‐dehydrokawain from alpinia, inhibited the growth of cancer cells with the IC₅₀ of 25 μM as does artepillin C, the major anti‐cancer ingredient in Brazilian green propolis. Mimosine tetrapeptides (MFWY, MFYY, and MFFY) and hispidin derivatives (H1–3) also exhibited a strong anti‐cancer activity with the IC₅₀ ranging from 16 to 30 μM. Mimosine tetrapeptides and hispidin derivatives strongly suppressed the melanogenesis in melanoma cells. Copyright © 2015 John Wiley & Sons, Ltd. |
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Bibliography: | http://dx.doi.org/10.1002/ptr.5510 istex:73E3FA4F7DA5A83C52E9E7FC2B4826E3E5DCABF6 ArticleID:PTR5510 ark:/67375/WNG-DZKL9FC4-T ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0951-418X 1099-1573 |
DOI: | 10.1002/ptr.5510 |