Studies on apoptosis induced by B-norcholesteryl benzimidazole compounds in HeLa cells

[Display omitted] •B-norcholesteryl Benzimidazole Compounds can change cervical cancer HeLa cell morphology and inhibit its proliferation, invasion and metastasis.•Furthermore, the compound can induce apoptosis of HeLa cells.•The compounds block HeLa cell proliferation in the early stage of DNA synt...

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Veröffentlicht in:Steroids 2021-04, Vol.168, p.108802, Article 108802
Hauptverfasser: Huang, Xiaotong, Wu, Yulan, Huang, Yanmin, Liu, Qinzhou, Chen, Hualong, Dai, Feng, Liang, Fengyan, Gan, Chunfang
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container_start_page 108802
container_title Steroids
container_volume 168
creator Huang, Xiaotong
Wu, Yulan
Huang, Yanmin
Liu, Qinzhou
Chen, Hualong
Dai, Feng
Liang, Fengyan
Gan, Chunfang
description [Display omitted] •B-norcholesteryl Benzimidazole Compounds can change cervical cancer HeLa cell morphology and inhibit its proliferation, invasion and metastasis.•Furthermore, the compound can induce apoptosis of HeLa cells.•The compounds block HeLa cell proliferation in the early stage of DNA synthesis (G0/G1 phase) and causes the mitochondrial membrane potential Δψm collapse.•Compound 1 can improve the expression of p53 mRNA.•Compound 2 down-regulated the expression of p53 and p21 mRNA.•Compound 3 upgrade the expression of p21 and p53 mRNA. Certain B-norcholesteryl benzimidazole compounds were found to mediate marked anti-tumor proliferative effects in vitro in our earlier study. Here, the mechanism of action of these anti-tumor effects was evaluated using HeLa human cervical cancer cells. Methods for detecting cell invasion and migration, Annexin V-PI double staining, cell cycle status, and mitochondrial membrane potential Δψm were employed. These compounds were confirmed to significantly inhibit the proliferation of HeLa cells in vitro. Compound 1 induced apoptosis in S phase, compound 2induced apoptosis in the G0/G1 phase and compound 3 induced late apoptosis in the G2/M phase. These compounds induced HeLa cell apoptosis through depolarization of mitochondrial membrane potential Δψm in a dose-dependent manner. B-norcholesteryl benzimidazole compounds induced morphological changes in HeLa cells and inhibited proliferation, invasion and metastasis. Apoptosis was promoted by mechanisms involving p21 and p53 in this cervical cancer cell line.
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Certain B-norcholesteryl benzimidazole compounds were found to mediate marked anti-tumor proliferative effects in vitro in our earlier study. Here, the mechanism of action of these anti-tumor effects was evaluated using HeLa human cervical cancer cells. Methods for detecting cell invasion and migration, Annexin V-PI double staining, cell cycle status, and mitochondrial membrane potential Δψm were employed. These compounds were confirmed to significantly inhibit the proliferation of HeLa cells in vitro. Compound 1 induced apoptosis in S phase, compound 2induced apoptosis in the G0/G1 phase and compound 3 induced late apoptosis in the G2/M phase. These compounds induced HeLa cell apoptosis through depolarization of mitochondrial membrane potential Δψm in a dose-dependent manner. B-norcholesteryl benzimidazole compounds induced morphological changes in HeLa cells and inhibited proliferation, invasion and metastasis. 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Certain B-norcholesteryl benzimidazole compounds were found to mediate marked anti-tumor proliferative effects in vitro in our earlier study. Here, the mechanism of action of these anti-tumor effects was evaluated using HeLa human cervical cancer cells. Methods for detecting cell invasion and migration, Annexin V-PI double staining, cell cycle status, and mitochondrial membrane potential Δψm were employed. These compounds were confirmed to significantly inhibit the proliferation of HeLa cells in vitro. Compound 1 induced apoptosis in S phase, compound 2induced apoptosis in the G0/G1 phase and compound 3 induced late apoptosis in the G2/M phase. These compounds induced HeLa cell apoptosis through depolarization of mitochondrial membrane potential Δψm in a dose-dependent manner. B-norcholesteryl benzimidazole compounds induced morphological changes in HeLa cells and inhibited proliferation, invasion and metastasis. Apoptosis was promoted by mechanisms involving p21 and p53 in this cervical cancer cell line.</description><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Apoptosis</subject><subject>Apoptosis - drug effects</subject><subject>B-norcholesteryl benzimidazole compounds</subject><subject>Benzimidazoles - chemistry</subject><subject>Benzimidazoles - pharmacology</subject><subject>Cell cycle</subject><subject>Cell Cycle - drug effects</subject><subject>Cell Movement - drug effects</subject><subject>Cell Proliferation - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>HeLa</subject><subject>HeLa Cells</subject><subject>Humans</subject><subject>Membrane Potential, Mitochondrial - drug effects</subject><subject>Mitochondrial membrane potential</subject><issn>0039-128X</issn><issn>1878-5867</issn><issn>1878-5867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEtr3DAUhUVISaZJ_kLQshtP9bD12DUJbVMY6KIPuhN63KEabMuR7MLk11dmkm67unA5555zP4RuKdlSQsX7w7bMkFMMZcsIo3WpFGFnaEOVVE2nhDxHG0K4bihTvy7R21IOhBDBNbtAl5x3SmomN-jnt3kJEQpOI7ZTmuZUYsFxDIuHgN0R3zdjyv536mENPPbYwfgchxjsc91hn4YpLWNYPfgRdhZ76Ptyjd7sbV_g5mVeoR-fPn5_eGx2Xz9_ebjbNZ4LNTfUa-UsZ9Kz1nbBOR1AWOpar5loJWe2tgRKrQDt9ozsOylbJ7Xn3hICgV-hd6e7U05PS61ohljWBnaEtBTDWk0o6wRlVSpOUp9TKRn2ZspxsPloKDErU3Mwr0zNytScmFbj7UvG4gYI_2yvEKvgw0kA9dM_EbIpPsJYAcYMfjYhxf9l_AUuJozj</recordid><startdate>202104</startdate><enddate>202104</enddate><creator>Huang, Xiaotong</creator><creator>Wu, Yulan</creator><creator>Huang, Yanmin</creator><creator>Liu, Qinzhou</creator><creator>Chen, Hualong</creator><creator>Dai, Feng</creator><creator>Liang, Fengyan</creator><creator>Gan, Chunfang</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>202104</creationdate><title>Studies on apoptosis induced by B-norcholesteryl benzimidazole compounds in HeLa cells</title><author>Huang, Xiaotong ; 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subjects Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Apoptosis - drug effects
B-norcholesteryl benzimidazole compounds
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Cell cycle
Cell Cycle - drug effects
Cell Movement - drug effects
Cell Proliferation - drug effects
Dose-Response Relationship, Drug
HeLa
HeLa Cells
Humans
Membrane Potential, Mitochondrial - drug effects
Mitochondrial membrane potential
title Studies on apoptosis induced by B-norcholesteryl benzimidazole compounds in HeLa cells
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