Isocryptotanshinone, a STAT3 inhibitor, induces apoptosis and pro-death autophagy in A549 lung cancer cells.
Identifieur interne : 000D66 ( Main/Exploration ); précédent : 000D65; suivant : 000D67Isocryptotanshinone, a STAT3 inhibitor, induces apoptosis and pro-death autophagy in A549 lung cancer cells.
Auteurs : Shuhui Guo [République populaire de Chine] ; Weiwei Luo [République populaire de Chine] ; Lijuan Liu [République populaire de Chine] ; Xiaocong Pang [République populaire de Chine] ; Hong Zhu [République populaire de Chine] ; Ailin Liu [République populaire de Chine] ; Jinjian Lu [République populaire de Chine] ; Dik-Lung Ma [Hong Kong] ; Chung-Hang Leung [République populaire de Chine] ; Yitao Wang [République populaire de Chine] ; Xiuping Chen [République populaire de Chine]Source :
- Journal of drug targeting [ 1029-2330 ] ; 2016.
Descripteurs français
- KwdFr :
- Antinéoplasiques (), Antinéoplasiques (pharmacologie), Apoptose (), Autophagie (), Facteur de transcription STAT-3 (antagonistes et inhibiteurs), Facteurs temps, Humains, Liaison aux protéines, Lignée cellulaire tumorale, Phosphorylation, Phénanthrènes (), Phénanthrènes (pharmacologie), Prolifération cellulaire (), Quinones (), Quinones (pharmacologie), Relation dose-effet des médicaments, Simulation de docking moléculaire, Sites de fixation.
- MESH :
- antagonistes et inhibiteurs : Facteur de transcription STAT-3.
- pharmacologie : Antinéoplasiques, Phénanthrènes, Quinones.
- Antinéoplasiques, Apoptose, Autophagie, Facteurs temps, Humains, Liaison aux protéines, Lignée cellulaire tumorale, Phosphorylation, Phénanthrènes, Prolifération cellulaire, Quinones, Relation dose-effet des médicaments, Simulation de docking moléculaire, Sites de fixation.
English descriptors
- KwdEn :
- Abietanes (chemistry), Abietanes (pharmacology), Antineoplastic Agents (chemistry), Antineoplastic Agents (pharmacology), Apoptosis (drug effects), Autophagy (drug effects), Binding Sites, Cell Line, Tumor, Cell Proliferation (drug effects), Dose-Response Relationship, Drug, Humans, Molecular Docking Simulation, Phenanthrenes (chemistry), Phenanthrenes (pharmacology), Phosphorylation, Protein Binding, Quinones (chemistry), Quinones (pharmacology), STAT3 Transcription Factor (antagonists & inhibitors), Time Factors.
- MESH :
- chemical , antagonists & inhibitors : STAT3 Transcription Factor.
- chemical , chemistry : Abietanes, Antineoplastic Agents, Phenanthrenes, Quinones.
- chemical , pharmacology : Abietanes, Antineoplastic Agents, Phenanthrenes, Quinones.
- drug effects : Apoptosis, Autophagy, Cell Proliferation.
- Binding Sites, Cell Line, Tumor, Dose-Response Relationship, Drug, Humans, Molecular Docking Simulation, Phosphorylation, Protein Binding, Time Factors.
Abstract
Signal transducer and activator of transcription 3 (STAT3) is a potential drug target for chemotherapy. Cryptotanshinone (CTS) was identified as a potent STAT3 inhibitor, while the effect of other tanshinones remains unknown. In this study, the influence of eight tanshinones on STAT3 activity was initially screened and isocryptotanshinone (ICTS) significantly inhibited STAT3 activity in a dual luciferase assay. ICTS inhibited the constitutive and inducible phosphorylation of STAT3 at Y705 without affecting the phosphorylation of STAT3 at S727 in A549 lung cancer cells. Furthermore, ICTS inhibited the nuclear translocation of STAT3. Compared with CTS, ICTS exhibited a stronger inhibitory effect on STAT3 phosphorylation and on A549 cytotoxicity. ICTS induced autophagy as evidenced by the accumulation of autophagic vacuoles and the increased expression of LC3 protein and autophagosomes. ICTS-induced cell death was partially reversed by the autophagy inhibitor chloroquine. The docking assay predicted that both ICTS and CTS bind the SH2 domain of STAT3. ICTS formed hydrogen bonds and pi-pi interaction with the nearby amino acid residues of Lys591, Arg609, and Ser636. These findings suggested that ICTS, a natural compound, is a potent STAT3 inhibitor. ICTS induced apoptosis and pro-death autophagy in A549 cells.
DOI: 10.3109/1061186X.2016.1157882
PubMed: 26904961
Affiliations:
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</wicri:noRegion></affiliation></author><author><name sortKey="Pang, Xiaocong" sort="Pang, Xiaocong" uniqKey="Pang X" first="Xiaocong" last="Pang">Xiaocong Pang</name><affiliation wicri:level="1"><nlm:affiliation>b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing </wicri:regionArea><wicri:noRegion>Beijing </wicri:noRegion></affiliation></author><author><name sortKey="Zhu, Hong" sort="Zhu, Hong" uniqKey="Zhu H" first="Hong" last="Zhu">Hong Zhu</name><affiliation wicri:level="1"><nlm:affiliation>c Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences , Zhejiang University , Hangzhou , Zhejiang , China.</nlm:affiliation><country xml:lang="fr">République populaire de 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sortKey="Guo, Shuhui" sort="Guo, Shuhui" uniqKey="Guo S" first="Shuhui" last="Guo">Shuhui Guo</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author><author><name sortKey="Luo, Weiwei" sort="Luo, Weiwei" uniqKey="Luo W" first="Weiwei" last="Luo">Weiwei Luo</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author><author><name sortKey="Liu, Lijuan" sort="Liu, Lijuan" uniqKey="Liu L" first="Lijuan" last="Liu">Lijuan Liu</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author><author><name sortKey="Pang, Xiaocong" sort="Pang, Xiaocong" uniqKey="Pang X" first="Xiaocong" last="Pang">Xiaocong Pang</name><affiliation wicri:level="1"><nlm:affiliation>b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing </wicri:regionArea><wicri:noRegion>Beijing </wicri:noRegion></affiliation></author><author><name sortKey="Zhu, Hong" sort="Zhu, Hong" uniqKey="Zhu H" first="Hong" last="Zhu">Hong Zhu</name><affiliation wicri:level="1"><nlm:affiliation>c Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences , Zhejiang University , Hangzhou , Zhejiang , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>c Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences , Zhejiang University , Hangzhou , Zhejiang </wicri:regionArea><wicri:noRegion>Zhejiang </wicri:noRegion></affiliation></author><author><name sortKey="Liu, Ailin" sort="Liu, Ailin" uniqKey="Liu A" first="Ailin" last="Liu">Ailin Liu</name><affiliation wicri:level="1"><nlm:affiliation>b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing </wicri:regionArea><wicri:noRegion>Beijing </wicri:noRegion></affiliation></author><author><name sortKey="Lu, Jinjian" sort="Lu, Jinjian" uniqKey="Lu J" first="Jinjian" last="Lu">Jinjian Lu</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author><author><name sortKey="Ma, Dik Lung" sort="Ma, Dik Lung" uniqKey="Ma D" first="Dik-Lung" last="Ma">Dik-Lung Ma</name><affiliation wicri:level="1"><nlm:affiliation>d Department of Chemistry , Hong Kong Baptist University , Kowloon Tong , Hong Kong.</nlm:affiliation><country xml:lang="fr">Hong Kong</country><wicri:regionArea>d Department of Chemistry , Hong Kong Baptist University , Kowloon Tong </wicri:regionArea><wicri:noRegion>Kowloon Tong </wicri:noRegion></affiliation></author><author><name sortKey="Leung, Chung Hang" sort="Leung, Chung Hang" uniqKey="Leung C" first="Chung-Hang" last="Leung">Chung-Hang Leung</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author><author><name sortKey="Wang, Yitao" sort="Wang, Yitao" uniqKey="Wang Y" first="Yitao" last="Wang">Yitao Wang</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author><author><name sortKey="Chen, Xiuping" sort="Chen, Xiuping" uniqKey="Chen X" first="Xiuping" last="Chen">Xiuping Chen</name><affiliation wicri:level="1"><nlm:affiliation>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau </wicri:regionArea><wicri:noRegion>Macau </wicri:noRegion></affiliation></author></analytic><series><title level="j">Journal of drug targeting</title><idno type="eISSN">1029-2330</idno><imprint><date when="2016" type="published">2016</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Abietanes (chemistry)</term><term>Abietanes (pharmacology)</term><term>Antineoplastic Agents (chemistry)</term><term>Antineoplastic Agents (pharmacology)</term><term>Apoptosis (drug effects)</term><term>Autophagy (drug effects)</term><term>Binding Sites</term><term>Cell Line, Tumor</term><term>Cell Proliferation (drug effects)</term><term>Dose-Response Relationship, Drug</term><term>Humans</term><term>Molecular Docking Simulation</term><term>Phenanthrenes (chemistry)</term><term>Phenanthrenes (pharmacology)</term><term>Phosphorylation</term><term>Protein Binding</term><term>Quinones (chemistry)</term><term>Quinones (pharmacology)</term><term>STAT3 Transcription Factor (antagonists & inhibitors)</term><term>Time Factors</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Antinéoplasiques ()</term><term>Antinéoplasiques (pharmacologie)</term><term>Apoptose ()</term><term>Autophagie ()</term><term>Facteur de transcription STAT-3 (antagonistes et inhibiteurs)</term><term>Facteurs temps</term><term>Humains</term><term>Liaison aux protéines</term><term>Lignée cellulaire tumorale</term><term>Phosphorylation</term><term>Phénanthrènes ()</term><term>Phénanthrènes (pharmacologie)</term><term>Prolifération cellulaire ()</term><term>Quinones ()</term><term>Quinones (pharmacologie)</term><term>Relation dose-effet des médicaments</term><term>Simulation de docking moléculaire</term><term>Sites de fixation</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>STAT3 Transcription Factor</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Abietanes</term><term>Antineoplastic Agents</term><term>Phenanthrenes</term><term>Quinones</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Abietanes</term><term>Antineoplastic Agents</term><term>Phenanthrenes</term><term>Quinones</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Facteur de transcription STAT-3</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Apoptosis</term><term>Autophagy</term><term>Cell Proliferation</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antinéoplasiques</term><term>Phénanthrènes</term><term>Quinones</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Binding Sites</term><term>Cell Line, Tumor</term><term>Dose-Response Relationship, Drug</term><term>Humans</term><term>Molecular Docking Simulation</term><term>Phosphorylation</term><term>Protein Binding</term><term>Time Factors</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Antinéoplasiques</term><term>Apoptose</term><term>Autophagie</term><term>Facteurs temps</term><term>Humains</term><term>Liaison aux protéines</term><term>Lignée cellulaire tumorale</term><term>Phosphorylation</term><term>Phénanthrènes</term><term>Prolifération cellulaire</term><term>Quinones</term><term>Relation dose-effet des médicaments</term><term>Simulation de docking moléculaire</term><term>Sites de fixation</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Signal transducer and activator of transcription 3 (STAT3) is a potential drug target for chemotherapy. Cryptotanshinone (CTS) was identified as a potent STAT3 inhibitor, while the effect of other tanshinones remains unknown. In this study, the influence of eight tanshinones on STAT3 activity was initially screened and isocryptotanshinone (ICTS) significantly inhibited STAT3 activity in a dual luciferase assay. ICTS inhibited the constitutive and inducible phosphorylation of STAT3 at Y705 without affecting the phosphorylation of STAT3 at S727 in A549 lung cancer cells. Furthermore, ICTS inhibited the nuclear translocation of STAT3. Compared with CTS, ICTS exhibited a stronger inhibitory effect on STAT3 phosphorylation and on A549 cytotoxicity. ICTS induced autophagy as evidenced by the accumulation of autophagic vacuoles and the increased expression of LC3 protein and autophagosomes. ICTS-induced cell death was partially reversed by the autophagy inhibitor chloroquine. The docking assay predicted that both ICTS and CTS bind the SH2 domain of STAT3. ICTS formed hydrogen bonds and pi-pi interaction with the nearby amino acid residues of Lys591, Arg609, and Ser636. These findings suggested that ICTS, a natural compound, is a potent STAT3 inhibitor. ICTS induced apoptosis and pro-death autophagy in A549 cells.</div></front></TEI><affiliations><list><country><li>Hong Kong</li><li>République populaire de Chine</li></country></list><tree><country name="République populaire de Chine"><noRegion><name sortKey="Guo, Shuhui" sort="Guo, Shuhui" uniqKey="Guo S" first="Shuhui" last="Guo">Shuhui Guo</name></noRegion><name sortKey="Chen, Xiuping" sort="Chen, Xiuping" uniqKey="Chen X" first="Xiuping" last="Chen">Xiuping Chen</name><name sortKey="Leung, Chung Hang" sort="Leung, Chung Hang" uniqKey="Leung C" first="Chung-Hang" last="Leung">Chung-Hang Leung</name><name sortKey="Liu, Ailin" sort="Liu, Ailin" uniqKey="Liu A" first="Ailin" last="Liu">Ailin Liu</name><name sortKey="Liu, Lijuan" sort="Liu, Lijuan" uniqKey="Liu L" first="Lijuan" last="Liu">Lijuan Liu</name><name sortKey="Lu, Jinjian" sort="Lu, Jinjian" uniqKey="Lu J" first="Jinjian" last="Lu">Jinjian Lu</name><name sortKey="Luo, Weiwei" sort="Luo, Weiwei" uniqKey="Luo W" first="Weiwei" last="Luo">Weiwei Luo</name><name sortKey="Pang, Xiaocong" sort="Pang, Xiaocong" uniqKey="Pang X" first="Xiaocong" last="Pang">Xiaocong Pang</name><name sortKey="Wang, Yitao" sort="Wang, Yitao" uniqKey="Wang Y" first="Yitao" last="Wang">Yitao Wang</name><name sortKey="Zhu, Hong" sort="Zhu, Hong" uniqKey="Zhu H" first="Hong" last="Zhu">Hong Zhu</name></country><country name="Hong Kong"><noRegion><name sortKey="Ma, Dik Lung" sort="Ma, Dik Lung" uniqKey="Ma D" first="Dik-Lung" last="Ma">Dik-Lung Ma</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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