Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer

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...

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Autores principales:	Laphatrada Yurasakpong, Chanin Nantasenamat, Saksit Nobsathian, Kulathida Chaithirayanon, Somjai Apisawetakan
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	betulinic acid HSPA apoptosis colorectal cancer Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/07e16231d1ac4ba6ab4c85dcfb65dfa2
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spelling	oai:doaj.org-article:07e16231d1ac4ba6ab4c85dcfb65dfa22021-11-11T18:24:22ZBetulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer10.3390/molecules262163771420-3049https://doaj.org/article/07e16231d1ac4ba6ab4c85dcfb65dfa22021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6377https://doaj.org/toc/1420-3049Betulinic 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 <i>Piper retrofractum</i> 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.Laphatrada YurasakpongChanin NantasenamatSaksit NobsathianKulathida ChaithirayanonSomjai ApisawetakanMDPI AGarticlebetulinic acidHSPAapoptosiscolorectal cancerOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6377, p 6377 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	betulinic acid HSPA apoptosis colorectal cancer Organic chemistry QD241-441
spellingShingle	betulinic acid HSPA apoptosis colorectal cancer Organic chemistry QD241-441 Laphatrada Yurasakpong Chanin Nantasenamat Saksit Nobsathian Kulathida Chaithirayanon Somjai Apisawetakan Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer
description	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 <i>Piper retrofractum</i> 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.
format	article
author	Laphatrada Yurasakpong Chanin Nantasenamat Saksit Nobsathian Kulathida Chaithirayanon Somjai Apisawetakan
author_facet	Laphatrada Yurasakpong Chanin Nantasenamat Saksit Nobsathian Kulathida Chaithirayanon Somjai Apisawetakan
author_sort	Laphatrada Yurasakpong
title	Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer
title_short	Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer
title_full	Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer
title_fullStr	Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer
title_full_unstemmed	Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer
title_sort	betulinic acid modulates the expression of hspa and activates apoptosis in two cell lines of human colorectal cancer
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/07e16231d1ac4ba6ab4c85dcfb65dfa2
work_keys_str_mv	AT laphatradayurasakpong betulinicacidmodulatestheexpressionofhspaandactivatesapoptosisintwocelllinesofhumancolorectalcancer AT chaninnantasenamat betulinicacidmodulatestheexpressionofhspaandactivatesapoptosisintwocelllinesofhumancolorectalcancer AT saksitnobsathian betulinicacidmodulatestheexpressionofhspaandactivatesapoptosisintwocelllinesofhumancolorectalcancer AT kulathidachaithirayanon betulinicacidmodulatestheexpressionofhspaandactivatesapoptosisintwocelllinesofhumancolorectalcancer AT somjaiapisawetakan betulinicacidmodulatestheexpressionofhspaandactivatesapoptosisintwocelllinesofhumancolorectalcancer
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Betulinic Acid Modulates the Expression of HSPA and Activates Apoptosis in Two Cell Lines of Human Colorectal Cancer

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