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  1. General Info
  2. Effects Info
  3. Reference
Drug Interaction Details
01. General Information
Pair Name Shikonin, Gefitinib
Phytochemical Name Shikonin (PubChem CID: 479503 )
Anticancer drug Name Gefitinib (PubChem CID: 123631 )
Structure of
Phytochemical
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2D MOL 3D MOL
Structure of
Anticancer Drug
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 286
Pair Name Shikonin, Gefitinib
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Gene Regulation Down-regulation Expression CCND1 hsa595
Down-regulation Expression PKM hsa5315
Down-regulation Phosphorylation STAT3 hsa6774
In Vitro Model A-549 Lung adenocarcinoma Homo sapiens (Human) CVCL_0023
In Vivo Model Mice were injected with A549 (1×10⁷) in the dorsal area.
Result These results provide a promising therapeutic approach for the treatment of wild-type EGFR non-small cell lung cancer.
Reversing Drug Resistance
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Combination Pair ID: 733
Pair Name Shikonin, Gefitinib
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Biological Phenomena Induction-->ROS generation
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Up-regulation Expression BAD hsa572
Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Down-regulation Expression BCL-xL hsa598
Up-regulation Cleavage CASP3 hsa836
Down-regulation Expression EGFR hsa1956
Down-regulation Phosphorylation MAPK1 hsa5594
Up-regulation Expression PARP1 hsa142
In Vitro Model NCI-H1650 Minimally invasive lung adenocarcinoma Homo sapiens (Human) CVCL_1483
NCI-H1975 Lung adenocarcinoma Homo sapiens (Human) CVCL_1511
Result Shikonin-induced cell apoptosis is closely associated with ROS elevation in the cells. These findings indicate that Shikonin can be an effective small molecule treating gefitinib-resistant NSCLC.
03. Reference
No. Title Href
1 Shikonin enhances sensitization of gefitinib against wild-type EGFR non-small cell lung cancer via inhibition PKM2/stat3/cyclinD1 signal pathway. Life Sci. 2018 Jul 1;204:71-77. doi: 10.1016/j.lfs.2018.05.012. Click
2 Shikonin inhibits gefitinib-resistant non-small cell lung cancer by inhibiting TrxR and activating the EGFR proteasomal degradation pathway. Pharmacol Res. 2017;115:45-55. doi:10.1016/j.phrs.2016.11.011 Click
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