Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor

Abstract Malignant peripheral nerve sheath tumors (MPNSTs) are an aggressive form of soft tissue neoplasm with extremely poor prognosis and no effective medical options currently available. MPNSTs can occur either sporadically or in association with the neurofibromatosis type 1 (NF1) syndrome. Impor...

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Main Authors: Xiao‐Xiao Li, Shi‐Jie Zhang, Amy P. Chiu, Lilian H. Lo, Jian Huang, Dewi K. Rowlands, Jinhui Wang, Vincent W. Keng
Format: Article
Language:English
Published: Wiley 2018-09-01
Series:Cancer Medicine
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Online Access:https://doi.org/10.1002/cam4.1732
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author Xiao‐Xiao Li
Shi‐Jie Zhang
Amy P. Chiu
Lilian H. Lo
Jian Huang
Dewi K. Rowlands
Jinhui Wang
Vincent W. Keng
author_facet Xiao‐Xiao Li
Shi‐Jie Zhang
Amy P. Chiu
Lilian H. Lo
Jian Huang
Dewi K. Rowlands
Jinhui Wang
Vincent W. Keng
author_sort Xiao‐Xiao Li
collection DOAJ
description Abstract Malignant peripheral nerve sheath tumors (MPNSTs) are an aggressive form of soft tissue neoplasm with extremely poor prognosis and no effective medical options currently available. MPNSTs can occur either sporadically or in association with the neurofibromatosis type 1 (NF1) syndrome. Importantly, activation of RAS/RAF/MEK/ERK, PI3K/AKT/mTOR, and WNT/CTNNB1 signaling pathways has been reported in both NF1‐related and late‐stage sporadic MPNSTs. In this study, we found that DAW22, a natural sesquiterpene coumarin compound isolated from Ferula ferulaeoides (Steud.) Korov., could inhibit cell proliferation and colony formation in five established human MPNST cancer cell lines. Further molecular mechanism exploration indicated that DAW22 could target the main components in the MPNST tumorigenic pathways: namely suppress phosphorylation of AKT and ERK, and reduce levels of non‐phospho (active) CTNNB1. Using the xenograft mouse model transplanted with human MPNST cancer cell line, daily treatment with DAW22 for 25 days was effective in reducing tumor growth. These results support DAW22 as an alternative therapeutic compound for MPNST treatment by affecting multiple signaling transduction pathways in its disease progression.
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spelling doaj-art-0db10cd2d8874526bbe8274b43af2f432025-08-20T03:04:30ZengWileyCancer Medicine2045-76342018-09-01794791480010.1002/cam4.1732Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumorXiao‐Xiao Li0Shi‐Jie Zhang1Amy P. Chiu2Lilian H. Lo3Jian Huang4Dewi K. Rowlands5Jinhui Wang6Vincent W. Keng7Department of Applied Biology and Chemical Technology The Hong Kong Polytechnic University Kowloon Hong KongInstitute of Clinical Pharmacology Guangzhou University of Chinese Medicine Guangzhou ChinaDepartment of Applied Biology and Chemical Technology The Hong Kong Polytechnic University Kowloon Hong KongDepartment of Applied Biology and Chemical Technology The Hong Kong Polytechnic University Kowloon Hong KongDepartment of Medicinal Chemistry and Natural Medicine Chemistry (State‐Province Key Laboratories of Biomedicine‐Pharmaceutics of China) Harbin Medical University Harbin ChinaLaboratory Animal Services Centre The Chinese University of Hong Kong Sha Tin New Territories Hong KongDepartment of Medicinal Chemistry and Natural Medicine Chemistry (State‐Province Key Laboratories of Biomedicine‐Pharmaceutics of China) Harbin Medical University Harbin ChinaDepartment of Applied Biology and Chemical Technology The Hong Kong Polytechnic University Kowloon Hong KongAbstract Malignant peripheral nerve sheath tumors (MPNSTs) are an aggressive form of soft tissue neoplasm with extremely poor prognosis and no effective medical options currently available. MPNSTs can occur either sporadically or in association with the neurofibromatosis type 1 (NF1) syndrome. Importantly, activation of RAS/RAF/MEK/ERK, PI3K/AKT/mTOR, and WNT/CTNNB1 signaling pathways has been reported in both NF1‐related and late‐stage sporadic MPNSTs. In this study, we found that DAW22, a natural sesquiterpene coumarin compound isolated from Ferula ferulaeoides (Steud.) Korov., could inhibit cell proliferation and colony formation in five established human MPNST cancer cell lines. Further molecular mechanism exploration indicated that DAW22 could target the main components in the MPNST tumorigenic pathways: namely suppress phosphorylation of AKT and ERK, and reduce levels of non‐phospho (active) CTNNB1. Using the xenograft mouse model transplanted with human MPNST cancer cell line, daily treatment with DAW22 for 25 days was effective in reducing tumor growth. These results support DAW22 as an alternative therapeutic compound for MPNST treatment by affecting multiple signaling transduction pathways in its disease progression.https://doi.org/10.1002/cam4.1732AKTapoptosisDAW22ERKMPNST
spellingShingle Xiao‐Xiao Li
Shi‐Jie Zhang
Amy P. Chiu
Lilian H. Lo
Jian Huang
Dewi K. Rowlands
Jinhui Wang
Vincent W. Keng
Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
Cancer Medicine
AKT
apoptosis
DAW22
ERK
MPNST
title Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
title_full Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
title_fullStr Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
title_full_unstemmed Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
title_short Targeting of AKT/ERK/CTNNB1 by DAW22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
title_sort targeting of akt erk ctnnb1 by daw22 as a potential therapeutic compound for malignant peripheral nerve sheath tumor
topic AKT
apoptosis
DAW22
ERK
MPNST
url https://doi.org/10.1002/cam4.1732
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