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

Compound: Apigenin

TargetsGene NameGene IDCancerCell LinesIC50ED50EC50GI50RemarkReferences
AKT1v-akt murine thymoma viral oncogene homolog 1207Lung adenocarcinomaA549----Apigenin has been shown to inhibit AKT activation .15947208
CCNB1cyclin B1891Colon CancerSW-480----The steady-state level of cyclin B1 was significantly reduced after apigenintreatment for 48 h at doses of 30 mM and higher.10900467
CDK1cyclin-dependent kinase 1983Human MelanomaOCM-1----Apigenin inhibited CDK-1 in OCM-1 cell line.11322924
CDK1cyclin-dependent kinase 1983Colon CancerHT-29----p34cdc2 kinase activity was significantly reduced by apigenin, at least in the high concentrations of 50-80 mM, for 24 h in each of three cell lines in comparison with the vehicle controls10900467
CDK1cyclin-dependent kinase 1983Colon CancerSW-480----p34cdc2 kinase activity was significantly reduced by apigenin, at least in the high concentrations of 50-80 mM, for 24 h in each of three cell lines in comparison with the vehicle controls10900467
CDK1cyclin-dependent kinase 1983Colorectal AdenocarcinomaCaCo-2----p34cdc2 kinase activity was significantly reduced by apigenin, at least in the high concentrations of 50-80 mM, for 24 h in each of three cell lines in comparison with the vehicle controls10900467
CDKN1Bcyclin-dependent kinase inhibitor 1B (p27, Kip1)1027Human MelanomaOCM-1----The flavone apigenin which arrest cells in G2/M but were without effect on CDK2 activity, affected only marginally the level of p27KIP1 and did not induce p21CIP.11322924
COX-1cytochrome c oxidase subunit I4512Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virusRAW264.722% inhibition at 100 µM---It inhibits cyclooxygenase 1 (Cox-1) activity and it is an anti-inflammatory mechanism.Phytochemistry Reviews 1: 369-377, 2002
CYP19A1cytochrome P450, family 19, subfamily A, polypeptide 11588Adrenocortical CarcinomaH295R20 µM---Apigenin inhibited aromatase activity concentration dependently in H295R cells after a 24 h exposure.A key enzyme in the synthesis of estrogens from androgens is aromatase(cytochromeP45019;CYP19.15319488
CYP19A1cytochrome P450, family 19, subfamily A, polypeptide 11588Breast adenocarcinomaMCF-71 µM---Apigenin inhibited aromatase activity with IC50 value of about 1µM.22209285
CYPIA1cytochrome P450, family 1, subfamily A, polypeptide 11543Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virusRAW264.70.02 µM---Apigenin potently inhibited Cyp1A activity with an IC50 of 0.02 µM Cyp1A, which is e.g. involved in the activation of carcinogens from grilled meat, as a model phase 1 enzyme, and measured the potential of beer constituents to inhibit its enzymatic activity.Phytochemistry Reviews 1: 369-377, 2002
HIF1Ahypoxia inducible factor 13091Lung adenocarcinomaA549----Apigenin specifically inhibited expression of HIF-1alpha but not HIF-1Beta subunit.15947208
IGF1insulin-like growth factor 13479Prostate CancerPC-3----growth of PC-3 tumors in nude mice was significantly inhibited by administration of apigenin to mice18726972
NOS2nitric oxide synthase 2, inducible4843Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virusRAW264.717.5 µM---Nitric oxide (NO) synthase (iNOS) and consequently, enhance the generation of NO. Generally, NO is an important signaling molecule, long-term elevated levels of NO, however, have been linked to early steps in carcinogenesis.It cause inhibition of lipopolysaccharide (LPS)-mediated induction of inducible nitric oxide synthase , which is an anti-inflammatory mechanis.Phytochemistry Reviews 1: 369-377, 2002
NQO1NAD(P)H dehydrogenase, quinone 11728Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virusRAW264.738.6 µM---It induces the QR activity.Induction of phases 2 enzymes contributes to chemopreventive activity. QR is not catalyzing a conjugation reaction, but it is induced co-ordinately with other phase 2 enzymes and contributes to detoxification by reduction of reactive quinones to less reactive hydroquinones.Phytochemistry Reviews 1: 369-377, 2002
RPS6KB1ribosomal protein S6 kinase, 70kDa, polypeptide 16198Lung adenocarcinomaA549----Apigenin inhibited p70S6K1 expression and activation in the cells . p70S6K1 were recently shown to regulate HIF-1 and VEGF transcriptional activation.15947208
VEGFAvascular endothelial growth factor A7422Lung adenocarcinomaA549----Apigenin inhibited VEGF transcriptional activation through the hypoxia-inducible factor 1 (HIF-1) binding site and specifically decreased HIF-1alpha but not HIF-1Beta subunit expression in the cells.15947208

 






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