Publication:
Betulinic acid modulates the expression of hspa and activates apoptosis in two cell lines of human colorectal cancer

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Issued Date

2021

Resource Type

Article

Language

eng

File Type

application/pdf

ISSN

14203049

DOI

10.3390/molecules26216377

Other identifier(s)

2-s2.0-85117570002

Rights Holder(s)

Scopus

Bibliographic Citation

Molecules. Vol 26, No.21 (2021)

Suggested Citation

Yurasakpong L., Nantasenamat C., Nobsathian S., Chaithirayanon K., Apisawetakan S. Betulinic acid modulates the expression of hspa and activates apoptosis in two cell lines of human colorectal cancer. Molecules. Vol 26, No.21 (2021). doi:10.3390/molecules26216377 Retrieved from: https://hdl.handle.net/20.500.14740/8144

Title

Betulinic acid modulates the expression of hspa and activates apoptosis in two cell lines of human colorectal cancer

Author(s)

Yurasakpong L.
 Nantasenamat C.
 Nobsathian S.
 Chaithirayanon K.
 Apisawetakan S.

Abstract

Betulinic acid (BA) is a pentacyclic triterpene usually isolated from botanical sources. Numerous studies have reported the inhibitory effect of BA against human colorectal cancer cells (CRC). However, its effect on the expression of the molecular chaperone HSPA is unclear. The aim of this research is to investigate the anti-cancer activities of BA purified from Piper retrofractum and study its effect on the expression of HSPA in colorectal cancer HCT116 and SW480 cells. The viability of both cancer cells was reduced after they were treated with an increasing dosage of BA. Flow cytometry assay revealed that levels of cell apoptosis significantly increased after incubation with BA in both cancer cells. Pro-apoptotic markers including Bax, cleaved-caspase-3 and cleaved-caspase-9 were increased while anti-apoptotic marker Bcl-2 was decreased after BA treatment. Western blot also showed that the expression of HSPA fluctuated upon BA treatment, whereby HSPA was increased at lower BA concentrations while at higher BA concentrations HSPA expression was decreased. Preliminary molecular docking assay showed that BA can bind to the nucleotide binding domain of the HSP70 at its ADP-bound state of the HSP70. Although further research is needed to comprehend the BA-HSPA interaction, our findings indicate that BA can be considered as potential candidate for the development of new treatment for colorectal cancer. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

Subject(s)

Antineoplastic agent
 Betulic acid
 Heat shock protein 70
 Pentacyclic triterpene
 Apoptosis
 Cell proliferation
 Cell survival
 Chemistry
 Colorectal tumor
 Conformation
 Dose response
 Drug effect
 Flow cytometry
 Gene expression regulation
 Genetics
 Human
 Metabolism
 Molecular docking
 Molecular dynamics
 Structure activity relation
 Tumor cell line
 Antineoplastic Agents, Phytogenic
 Apoptosis
 Cell Line, Tumor
 Cell Proliferation
 Cell Survival
 Colorectal Neoplasms
 Dose-Response Relationship, Drug
 Flow Cytometry
 Gene Expression Regulation, Neoplastic
 HSP70 Heat-Shock Proteins
 Humans
 Molecular Conformation
 Molecular Docking Simulation
 Molecular Dynamics Simulation
 Pentacyclic Triterpenes
 Structure-Activity Relationship

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URI

https://hdl.handle.net/20.500.14740/8144

Collections

Scopus: Year 1983-2021

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