LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells

Gastric cancer is a global health problem. In this study, we investigate the role of a novel Indole derivative, named LCT-3d, in inhibiting the growth of gastric cancer cells by MTT assay. The Western blotting results showed that LCT-3d modulated the mitochondrial-related proteins and Cleaved-Caspas...

Full description

Saved in:
Bibliographic Details
Main Authors: Menglin Wang, Xinxin Wu, Lu Yu, Zi-yun Hu, Xiaobo Li, Xia Meng, Chun-tao Lv, Gi-Young Kim, Yung Hyun Choi, Zhenya Wang, Hai-Wei Xu, Cheng-Yun Jin
Format: Article
Language:English
Published: Frontiers Media S.A. 2021-04-01
Series:Frontiers in Oncology
Subjects:
Online Access:https://www.frontiersin.org/articles/10.3389/fonc.2021.658608/full
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1849689697716011008
author Menglin Wang
Xinxin Wu
Lu Yu
Zi-yun Hu
Xiaobo Li
Xia Meng
Chun-tao Lv
Gi-Young Kim
Yung Hyun Choi
Zhenya Wang
Hai-Wei Xu
Cheng-Yun Jin
Cheng-Yun Jin
author_facet Menglin Wang
Xinxin Wu
Lu Yu
Zi-yun Hu
Xiaobo Li
Xia Meng
Chun-tao Lv
Gi-Young Kim
Yung Hyun Choi
Zhenya Wang
Hai-Wei Xu
Cheng-Yun Jin
Cheng-Yun Jin
author_sort Menglin Wang
collection DOAJ
description Gastric cancer is a global health problem. In this study, we investigate the role of a novel Indole derivative, named LCT-3d, in inhibiting the growth of gastric cancer cells by MTT assay. The Western blotting results showed that LCT-3d modulated the mitochondrial-related proteins and Cleaved-Caspases 3/9, to induce cell apoptosis. The up-regulation of Death receptor 5 (DR5) in MGC803 cells was observed with LCT-3d treatment. Knockdown of DR5 on MGC803 cells partially reversed the LCT-3d-induced mitochondrial apoptosis. The level of Reactive Oxygen Species (ROS) in MGC803 cells was increased with LCT-3d treatment and could be blocked with the pretreatment of the ROS inhibitor N-Acetylcysteine (NAC). The results demonstrate that the elevating ROS can up-regulate the expression of DR5, resulting in apoptosis via mitochondrial pathway. Although the nuclear factor erythroid-2 related factor 2 (Nrf2) pathway served an important role in protecting gastric cancer cells against the injury of ROS, it can’t reverse LCT-3d-induced cell apoptosis. Taken together, our study showed that LCT-3d induced apoptosis via DR5-mediated mitochondrial apoptotic pathway in gastric cancer cells. LCT-3d could be a novel lead compound for development of anti-cancer activity in gastric cancer.
format Article
id doaj-art-e2a25caed06b43b4ab783e669b5d0c04
institution DOAJ
issn 2234-943X
language English
publishDate 2021-04-01
publisher Frontiers Media S.A.
record_format Article
series Frontiers in Oncology
spelling doaj-art-e2a25caed06b43b4ab783e669b5d0c042025-08-20T03:21:32ZengFrontiers Media S.A.Frontiers in Oncology2234-943X2021-04-011110.3389/fonc.2021.658608658608LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer CellsMenglin Wang0Xinxin Wu1Lu Yu2Zi-yun Hu3Xiaobo Li4Xia Meng5Chun-tao Lv6Gi-Young Kim7Yung Hyun Choi8Zhenya Wang9Hai-Wei Xu10Cheng-Yun Jin11Cheng-Yun Jin12Key Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaDepartment of Marine Life Sciences, Jeju National University, Jeju, South KoreaDepartment of Biochemistry, College of Oriental Medicine, Dong-Eui University, Busan, South KoreaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaKey Laboratory of Advanced Technology for Drug Preparation, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaState Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou University, Zhengzhou, ChinaGastric cancer is a global health problem. In this study, we investigate the role of a novel Indole derivative, named LCT-3d, in inhibiting the growth of gastric cancer cells by MTT assay. The Western blotting results showed that LCT-3d modulated the mitochondrial-related proteins and Cleaved-Caspases 3/9, to induce cell apoptosis. The up-regulation of Death receptor 5 (DR5) in MGC803 cells was observed with LCT-3d treatment. Knockdown of DR5 on MGC803 cells partially reversed the LCT-3d-induced mitochondrial apoptosis. The level of Reactive Oxygen Species (ROS) in MGC803 cells was increased with LCT-3d treatment and could be blocked with the pretreatment of the ROS inhibitor N-Acetylcysteine (NAC). The results demonstrate that the elevating ROS can up-regulate the expression of DR5, resulting in apoptosis via mitochondrial pathway. Although the nuclear factor erythroid-2 related factor 2 (Nrf2) pathway served an important role in protecting gastric cancer cells against the injury of ROS, it can’t reverse LCT-3d-induced cell apoptosis. Taken together, our study showed that LCT-3d induced apoptosis via DR5-mediated mitochondrial apoptotic pathway in gastric cancer cells. LCT-3d could be a novel lead compound for development of anti-cancer activity in gastric cancer.https://www.frontiersin.org/articles/10.3389/fonc.2021.658608/fullLCT-3dDR5reactive oxygen speciesNrf2apoptosisgastric cancer
spellingShingle Menglin Wang
Xinxin Wu
Lu Yu
Zi-yun Hu
Xiaobo Li
Xia Meng
Chun-tao Lv
Gi-Young Kim
Yung Hyun Choi
Zhenya Wang
Hai-Wei Xu
Cheng-Yun Jin
Cheng-Yun Jin
LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells
Frontiers in Oncology
LCT-3d
DR5
reactive oxygen species
Nrf2
apoptosis
gastric cancer
title LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells
title_full LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells
title_fullStr LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells
title_full_unstemmed LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells
title_short LCT-3d Induces Oxidative Stress-Mediated Apoptosis by Upregulating Death Receptor 5 in Gastric Cancer Cells
title_sort lct 3d induces oxidative stress mediated apoptosis by upregulating death receptor 5 in gastric cancer cells
topic LCT-3d
DR5
reactive oxygen species
Nrf2
apoptosis
gastric cancer
url https://www.frontiersin.org/articles/10.3389/fonc.2021.658608/full
work_keys_str_mv AT menglinwang lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT xinxinwu lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT luyu lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT ziyunhu lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT xiaoboli lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT xiameng lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT chuntaolv lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT giyoungkim lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT yunghyunchoi lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT zhenyawang lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT haiweixu lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT chengyunjin lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells
AT chengyunjin lct3dinducesoxidativestressmediatedapoptosisbyupregulatingdeathreceptor5ingastriccancercells