Drug Combination Details
| General Information of the Combination (ID: C59960) | |||||
|---|---|---|---|---|---|
| Name | Apigenin NP Info | + | TNF-related apoptosis inducing ligand Drug Info | ||
| Structure |
|
+ |
|
||
| Disease |
Prostate cancer
[ICD-11: 2C82]
|
Investigative | [1] | ||
|
Anaplastic large cell lymphoma
[ICD-11: 2A90]
|
Investigative | [2] | |||
|
Hepatocellular carcinoma
[ICD-11: 2C12]
|
Investigative | [3] | |||
|
Thyroid cancer
[ICD-11: 2D10]
|
Investigative | [4] | |||
|
Lung cancer
[ICD-11: 2C25]
|
Investigative | [5] | |||
| Click to Show/Hide the Whole Disease Information of This Combination | |||||
| Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally | ||||||
|---|---|---|---|---|---|---|
| α. Enhancing Drug Efficacy by This Combination | ||||||
| Achieving Therapeutic Synergy | Click to Show/Hide | |||||
| Experiment 1 Reporting the Effect of This Combination | [4] | |||||
| Molecule(s)
Regulation |
Down-regulation | Expression | AKT1 | Molecule Info |
Pathway MAP
|
|
| Down-regulation | Expression | BCL-2 | Molecule Info |
Pathway MAP
|
||
| In-vitro Model | 8505C | CVCL_1054 | Thyroid gland anaplastic carcinoma | Homo sapiens | ||
| CAL-62 | CVCL_1112 | Thyroid gland anaplastic carcinoma | Homo sapiens | |||
| Experimental
Result(s) |
Apigenin synergizes with TRAIL through regulation of Bcl2 family proteins in inducing cytotoxicity, and suppression of AKT potentiates synergistic cytotoxicity of apigenin with TRAIL in ATC cells. | |||||
| Experiment 2 Reporting the Effect of This Combination | [2] | |||||
| Molecule(s)
Regulation |
Down-regulation | Expression | CFLAR | Molecule Info |
Pathway MAP
|
|
| Up-regulation | Expression | TRAIL-R2 | Molecule Info |
Pathway MAP
|
||
| In-vitro Model | Jurkat | CVCL_0065 | T acute lymphoblastic leukemia | Homo sapiens | ||
| SP+ | CVCL_1Y11 | T cell leukemia | Homo sapiens | |||
| MT-2 | CVCL_2631 | Healthy | Homo sapiens | |||
| Experimental
Result(s) |
Apigenin breaks TRAIL resistance in HTLV-1-associated ATL by transcriptional down-regulation of c-FLIP, a key inhibitor of death receptor signaling, and by up-regulation of TRAIL receptor 2 (TRAIL-R2). | |||||
| Augmenting Drug Sensitivity | Click to Show/Hide | |||||
| Experiment 1 Reporting the Effect of This Combination | [5] | |||||
| Molecule(s)
Regulation |
Down-regulation | Expression | AKT1 | Molecule Info |
Pathway MAP
|
|
| Up-regulation | Expression | BAD | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Expression | BAX | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | BCL-2 | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | BCL-xL | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | ERK1 | Molecule Info |
Pathway MAP
|
||
| Down-regulation | Expression | p105 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Expression | TRAIL-R2 | Molecule Info |
Pathway MAP
|
||
| In-vitro Model | A-549 | CVCL_0023 | Lung adenocarcinoma | Homo sapiens | ||
| NCI-H1299 | CVCL_0060 | Lung large cell carcinoma | Homo sapiens | |||
| Experimental
Result(s) |
Apigenin enhances TRAIL-induced antitumor activity in NSCLC cells by APG via inhibition of the NF-kappaB, AKT and ERK prosurvival regulators. | |||||
| Experiment 2 Reporting the Effect of This Combination | [3] | |||||
| Molecule(s)
Regulation |
Up-regulation | Cleavage | CASP3 | Molecule Info |
Pathway MAP
|
|
| Up-regulation | Cleavage | CASP6 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Cleavage | CASP7 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Cleavage | CASP8 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Cleavage | CASP9 | Molecule Info |
Pathway MAP
|
||
| Up-regulation | Cleavage | PARP1 | Molecule Info |
Pathway MAP
|
||
| Biological
Regulation |
Up-regulation | Ratio of Bax to Bcl-2 | ||||
| In-vitro Model | Huh-7 | CVCL_0336 | Adult hepatocellular carcinoma | Homo sapiens | ||
| Experimental
Result(s) |
Apigenin sensitizes cells to TRAIL-induced apoptosis by activating both intrinsic and extrinsic apoptotic pathway-related caspases. The augmented apoptotic effect by TRAIL/apigenin combination was accompanied by triggering mitochondria-dependent signaling pathway, as indicated by Bax/Bcl-2 ratio up-regulation. | |||||
| Experiment 3 Reporting the Effect of This Combination | [6] | |||||
| Molecule(s)
Regulation |
Up-regulation | Expression | TRAIL-R2 | Molecule Info |
Pathway MAP
|
|
| In-vitro Model | Hep-G2 | CVCL_0027 | Hepatocellular carcinoma | Homo sapiens | ||
| Experimental
Result(s) |
Sub-toxic dose of apigenin sensitizes HepG2 cells to TRAIL through ERK-dependent up-regulation of TRAIL receptor DR5. | |||||
| Experiment 4 Reporting the Effect of This Combination | [1] | |||||
| In-vitro Model | LNCaP | CVCL_0395 | Prostate carcinoma | Homo sapiens | ||
| DU145 | CVCL_0105 | Prostate carcinoma | Homo sapiens | |||
| Experimental
Result(s) |
Apigenin markedly augmented TRAIL-mediated apoptosis in prostate cancer cells . | |||||
