Cargando…
The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells
Jesridonin, a small molecule obtained through the structural modification of Oridonin, has extensive antitumor activity. In this study, we evaluated both its in vitro activity in the cancer cell line EC109 and its in vivo effect on tumor xenografts in nude mice. Apoptosis induced by Jesridonin was d...
Autores principales: | , , , , , , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2015
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4477902/ https://www.ncbi.nlm.nih.gov/pubmed/26103161 http://dx.doi.org/10.1371/journal.pone.0130284 |
_version_ | 1782377825995587584 |
---|---|
author | Wang, Cong Jiang, Liping Wang, Saiqi Shi, Hongge Wang, Junwei Wang, Ran Li, Yongmei Dou, Yinhui Liu, Ying Hou, Guiqin Ke, Yu Liu, Hongmin |
author_facet | Wang, Cong Jiang, Liping Wang, Saiqi Shi, Hongge Wang, Junwei Wang, Ran Li, Yongmei Dou, Yinhui Liu, Ying Hou, Guiqin Ke, Yu Liu, Hongmin |
author_sort | Wang, Cong |
collection | PubMed |
description | Jesridonin, a small molecule obtained through the structural modification of Oridonin, has extensive antitumor activity. In this study, we evaluated both its in vitro activity in the cancer cell line EC109 and its in vivo effect on tumor xenografts in nude mice. Apoptosis induced by Jesridonin was determined using an MTT assay, Annexin-V FITC assay and Hoechest 33258 staining. Apoptosis via mitochondrial and death receptor pathways were confirmed by detecting the regulation of MDM2, p53, and Bcl-2 family members and by activation of caspase-3/-8/-9. In addition, vena caudalis injection of Jesridonin showed significant inhibition of tumor growth in the xenograft model, and Jesridonin-induced cell apoptosis in tumor tissues was determined using TUNEL. Biochemical serum analysis of alkaline phosphatase (ALP), alanine transaminase (ALT), aspartate transaminase (AST), gamma-glutamyl transferase (GGT), total protein (TP) and albumin (ALB) indicated no obvious effects on liver function. Histopathological examination of the liver, kidney, lung, heart and spleen revealed no signs of JD-induced toxicity. Taken together, these results demonstrated that Jesridonin exhibits antitumor activity in human esophageal carcinomas EC109 cells both in vitro and in vivo and demonstrated no adverse effects on major organs in nude mice. These studies provide support for new drug development. |
format | Online Article Text |
id | pubmed-4477902 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-44779022015-07-02 The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells Wang, Cong Jiang, Liping Wang, Saiqi Shi, Hongge Wang, Junwei Wang, Ran Li, Yongmei Dou, Yinhui Liu, Ying Hou, Guiqin Ke, Yu Liu, Hongmin PLoS One Research Article Jesridonin, a small molecule obtained through the structural modification of Oridonin, has extensive antitumor activity. In this study, we evaluated both its in vitro activity in the cancer cell line EC109 and its in vivo effect on tumor xenografts in nude mice. Apoptosis induced by Jesridonin was determined using an MTT assay, Annexin-V FITC assay and Hoechest 33258 staining. Apoptosis via mitochondrial and death receptor pathways were confirmed by detecting the regulation of MDM2, p53, and Bcl-2 family members and by activation of caspase-3/-8/-9. In addition, vena caudalis injection of Jesridonin showed significant inhibition of tumor growth in the xenograft model, and Jesridonin-induced cell apoptosis in tumor tissues was determined using TUNEL. Biochemical serum analysis of alkaline phosphatase (ALP), alanine transaminase (ALT), aspartate transaminase (AST), gamma-glutamyl transferase (GGT), total protein (TP) and albumin (ALB) indicated no obvious effects on liver function. Histopathological examination of the liver, kidney, lung, heart and spleen revealed no signs of JD-induced toxicity. Taken together, these results demonstrated that Jesridonin exhibits antitumor activity in human esophageal carcinomas EC109 cells both in vitro and in vivo and demonstrated no adverse effects on major organs in nude mice. These studies provide support for new drug development. Public Library of Science 2015-06-23 /pmc/articles/PMC4477902/ /pubmed/26103161 http://dx.doi.org/10.1371/journal.pone.0130284 Text en © 2015 Wang et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited. |
spellingShingle | Research Article Wang, Cong Jiang, Liping Wang, Saiqi Shi, Hongge Wang, Junwei Wang, Ran Li, Yongmei Dou, Yinhui Liu, Ying Hou, Guiqin Ke, Yu Liu, Hongmin The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells |
title | The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells |
title_full | The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells |
title_fullStr | The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells |
title_full_unstemmed | The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells |
title_short | The Antitumor Activity of the Novel Compound Jesridonin on Human Esophageal Carcinoma Cells |
title_sort | antitumor activity of the novel compound jesridonin on human esophageal carcinoma cells |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4477902/ https://www.ncbi.nlm.nih.gov/pubmed/26103161 http://dx.doi.org/10.1371/journal.pone.0130284 |
work_keys_str_mv | AT wangcong theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT jiangliping theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangsaiqi theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT shihongge theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangjunwei theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangran theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT liyongmei theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT douyinhui theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT liuying theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT houguiqin theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT keyu theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT liuhongmin theantitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangcong antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT jiangliping antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangsaiqi antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT shihongge antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangjunwei antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT wangran antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT liyongmei antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT douyinhui antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT liuying antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT houguiqin antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT keyu antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells AT liuhongmin antitumoractivityofthenovelcompoundjesridoninonhumanesophagealcarcinomacells |