IPM712, a vanillin derivative as potential antitumor agents, displays better antitumor activity in colorectal cancers cell lines.


Journal

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
ISSN: 1879-0720
Titre abrégé: Eur J Pharm Sci
Pays: Netherlands
ID NLM: 9317982

Informations de publication

Date de publication:
01 Sep 2020
Historique:
received: 28 03 2020
revised: 08 07 2020
accepted: 10 07 2020
pubmed: 16 7 2020
medline: 22 6 2021
entrez: 16 7 2020
Statut: ppublish

Résumé

Colorectal cancer (CRC), a major health threat in the world, ranks third in incidence and second in mortality among cancers. Chemotherapy, an important treatment for colorectal cancer, have be limited in the clinic due to the resistance and side effect. Studies have shown that PI3K-related regulatory pathways play a colossal role in colorectal cancer. Therefore, it is a good strategy to find a new drug which works by affecting the PI3K signaling pathway. In this paper, we obtained a new vanillin derivative (IPM712) by modifying the structure of IPM711 and tested its anticancer activity in vitro and toxicity in vivo. Results showed that IPM712 has a better anticancer activity than 5-Fu in HCT116 and SW480 cell lines. Furthermore, IPM712 can inhibit cell proliferation, migration and induce the apoptosis by affecting PI3K-related protein expression. Acute toxicity experiments show that IPM712 has no significant toxicity at therapeutic concentrations. Based on these results, IPM712 is a promising anticancer drug candidate for human colorectal cancer therapy.

Identifiants

pubmed: 32668313
pii: S0928-0987(20)30253-0
doi: 10.1016/j.ejps.2020.105464
pii:
doi:

Substances chimiques

Antineoplastic Agents 0
Benzaldehydes 0
vanillin CHI530446X
Proto-Oncogene Proteins c-akt EC 2.7.11.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

105464

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Comperting Interest The authors declare no conflicts of interests.

Auteurs

Wantong Ma (W)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Qianqian Zhang (Q)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Xue Li (X)

College of Chemistry and Chemical Engineering, Lanzhou University, 222 Tianshui South Road, Lanzhou, 730000, PR China.

Yunhao Ma (Y)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Yuheng Liu (Y)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Shujian Hu (S)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Zhongkun Zhou (Z)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Rentao Zhang (R)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Kangjia Du (K)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Ashikujaman Syed (A)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China.

Xiaojun Yao (X)

Macau Institute for Applied Research in Medicine and Health, State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau, PR China.

Peng Chen (P)

School of Pharmacy, Lanzhou University, 199 Donggang West Road, Lanzhou, 730000, PR China. Electronic address: chenpeng@lzu.edu.cn.

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Classifications MeSH