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Isocryptotanshinone, a STAT3 inhibitor, induces apoptosis and pro-death autophagy in A549 lung cancer cells
Shuhui Guo1; Weiwei Luo1; Lijuan Liu1; Xiaocong Pang2; Hong Zhu3; Ailin Liu2; Jinjian Lu1; Dik-Lung Ma4; Chung-Hang Leung1; Yitao Wang1; Xiuping Chen1
Source PublicationJournal of Drug Targeting

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.

KeywordApoptosis Autophagy Isocryptotanshinone Stat3
URLView the original
Indexed BySCIE
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000393188000004
The Source to ArticleScopus
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Cited Times [WOS]:24   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, China
2.Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China
3.Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, China
4.Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Shuhui Guo,Weiwei Luo,Lijuan Liu,et al. Isocryptotanshinone, a STAT3 inhibitor, induces apoptosis and pro-death autophagy in A549 lung cancer cells[J]. Journal of Drug Targeting,2016,24(10):934-942.
APA Shuhui Guo,Weiwei Luo,Lijuan Liu,Xiaocong Pang,Hong Zhu,Ailin Liu,Jinjian Lu,Dik-Lung Ma,Chung-Hang Leung,Yitao Wang,&Xiuping Chen.(2016).Isocryptotanshinone, a STAT3 inhibitor, induces apoptosis and pro-death autophagy in A549 lung cancer cells.Journal of Drug Targeting,24(10),934-942.
MLA Shuhui Guo,et al."Isocryptotanshinone, a STAT3 inhibitor, induces apoptosis and pro-death autophagy in A549 lung cancer cells".Journal of Drug Targeting 24.10(2016):934-942.
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