NPACT- Naturally occuring Plant based Anticancerous Compound-Activity-Target DataBase

Compound: Z-Guggulsterone

TargetsGene NameGene IDCancerCell LinesIC50ED50EC50GI50RemarkReferences
AKT1v-akt murine thymoma viral oncogene homolog 1207Prostate CancerDU-145----Ectopic expression of constitutively active Akt in DU145 cells conferred protection against z-guggulsterone-mediated inhibition of cell migration.18202020
CCND1cyclin D1595Head and neck squamous cell carcinomaUM-22b----In UM-22b cells, expression levels of proteins that promote the transition from the G1 to the S phase of the cell cycle, including cyclin D1 which is a target gene for both STAT3 and NFkappaB, showed modest decreases following 16 h of guggulsterone (10 microM) treatment19762335
CCNE1cyclin E1898Head and neck squamous cell carcinomaUM-22b----In UM-22b cells, expression levels of proteins that promote the transition from the G1 to the S phase of the cell cycle, including cyclin E which is a target gene for both STAT3 and NFkappaB, showed modest decreases following 16 h of guggulsterone (10 microM) treatment19762335
CDK2cyclin-dependent kinase 21017Head and neck squamous cell carcinomaUM-22b----In UM-22b cells, expression levels of proteins that promote the transition from the G1 to the S phase of the cell cycle, including CDK2 which is a target gene for both STAT3 and NFkappaB, showed modest decreases following 16 h of guggulsterone (10 microM) treatment19762335
CDK4cyclin-dependent kinase 41019Head and neck squamous cell carcinomaUM-22b----In UM-22b cells, expression levels of proteins that promote the transition from the G1 to the S phase of the cell cycle, including CDK4 which is a target gene for both STAT3 and NFkappaB, showed modest decreases following 16 h of guggulsterone (10 microM) treatment19762335
CDK6cyclin-dependent kinase 61021Head and neck squamous cell carcinomaUM-22b----In UM-22b cells, expression levels of proteins that promote the transition from the G1 to the S phase of the cell cycle, including CDK6 which is a target gene for both STAT3 and NFkappaB, showed modest decreases following 16 h of guggulsterone (10 microM) treatment19762335
HIF1Ahypoxia inducible factor 13091Head and neck squamous cell carcinomaUM-22b----Data suggest that guggulsterone, a STAT3 inhibitor, primarily affects HIF-1alpha expression at the transcriptional level.19762335
KDRkinase insert domain receptor (a type III receptor tyrosine kinase)3791Prostate CancerDU145----Oral gavage of z-guggulsterone to male nude mice implanted with DU145-Matrigel plugs significantly inhibits in vivo angiogenesis as judged by immunohistochemical analyses for angiogenic markers (factor VIII and CD31). z-guggulsterone administration caused a statistically significant decrease in protein levels of VEGF-R2 compared with control mice.18202020
KDRkinase insert domain receptor (a type III receptor tyrosine kinase)3791Prostate CancerDU-145----Results indicated that the z-guggulsterone-mediated inhibition of angiogenesis was probably accomplished, at least in part, by down-regulation of VEGF-R2 protein level18202020
RB1retinoblastoma 15925Head and neck squamous cell carcinomaUM-22b----In UM-22b cells, expression levels of proteins that promote the transition from the G1 to the S phase of the cell cycle, including phosphorylated Rb which is a target gene for both STAT3 and NFkappaB, showed modest decreases following 16 h of guggulsterone (10 microM) treatment19762335
STAT3signal transducer and activator of transcription 3 (acute-phase response factor)6774Head and neck squamous cell carcinoma1483----After 72 h, guggulsterone-treated 1483 cancer cells demonstrated dose-dependent decreases in both phosphotyrosine STAT3 and total STAT3 that were statistically significant, upon densitometric analysis (P=0.03)19762335
STAT3signal transducer and activator of transcription 3 (acute-phase response factor)6774Head and neck squamous cell carcinomaPCI-37a----After 72 h, guggulsterone-treated PCI-37a cancer cells demonstrated dose-dependent decreases in both phosphotyrosine STAT3 and total STAT3 that were statistically significant, upon densitometric analysis (P=0.03)19762335
STAT3signal transducer and activator of transcription 3 (acute-phase response factor)6774Head and neck squamous cell carcinomaUM-22b----After 72 h, guggulsterone-treated UM-22b cancer cells demonstrated dose-dependent decreases in both phosphotyrosine STAT3 and total STAT3 that were statistically significant, upon densitometric analysis (P=0.03)19762335
STAT3signal transducer and activator of transcription 3 (acute-phase response factor)6774Head and neck squamous cell carcinoma1483----Percentages of terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling-positive cells increased 2.2-fold in 1483 xenografts from mice treated with guggulsterone versus vehicle, indicating that guggulsterone induced apoptosis in this xenografts. A decrease in STAT3 expression of 44.3% in 1483-derived tumors was observed.19762335
STAT3signal transducer and activator of transcription 3 (acute-phase response factor)6774Head and neck squamous cell carcinomaUM-22b----Percentages of terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling-positive cells increased 2.2-fold in UM-22b xenografts from mice treated with guggulsterone versus vehicle, indicating that guggulsterone induced apoptosis in this xenografts. A decrease in STAT3 expression of 87.3% in UM-22b-derived tumors was observed19762335

 






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