| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1058 | |
| Phytochemical name or plant extracts | Kaempferol | |
| PMID | 31404596 | |
| Literature evidence | Aberrant activity of sirtuins (SIRTs) has strong implications in the metastatic and oncogenic progression of TNBC. | |
| IUPAC name | 3,5,7-trihydroxy-2-(4-hydroxyphenyl)chromen-4-one | |
| Phytochemicals’ class or type of plant extracts | Flavonoid | |
| Source of phytochemicals or plant Extracts | Justicia gendarussa | |
| Geographical availability | Andaman Is., Assam, Bangladesh, Cambodia, East Himalaya, India, Laos, Lesser Sunda Is., Malaya, Myanmar, New Guinea, Philippines, Sri Lanka, Sumatera, Thailand, Vietnam | |
| Plant parts | Leaves | |
| Other cancers | Breast cancer, Bone cancer, Cervical cancer, Lung cancer | |
| Target gene or protein | IQGAP3, CYP1A1, CYP1B1, Survivin, PR, AHR, ERα, GREB1, Aromatase | |
| Gene or Protein evidence | CONCLUSIONS IQGAP3 may be a potential target gene for Kaempferol in the treatment of BC, and upregulation of IQGAP3 inhibits Kaempferol-induced apoptosis in BC cells by ERK1/2 signaling activation. Kaempferol or resveratrol inhibited dioxin-induced cytochrome P450 1A1 (CYP1A1) and CYP1B1 expression levels and recruitment of AHR, ERα and co-activators to CYP1A1 and CYP1B1. Both phytochemicals induced the expression and recruitment of ERα to gene amplified in breast cancer 1 (GREB1). RNAi-mediated knockdown of ERα in T-47D cells did not affect the inhibitory action of either phytochemical on AHR activity. Kaempferol, a natural dietary flavonoid, suppresses 17β-estradiol-induced survivin expression and causes apoptotic cell death in endometrial cancer. Taken together, these data suggest that kaempferol is a unique natural PR modulator that activates PR signaling in vitro and in vivo without triggering PR degradation. The flavonoids, coumestrol, luteolin and kaempferol also decreased aromatase enzyme activity, with Ki values of 1.3, 4.8 and 27.2 microM, respectively. | |
| Target pathways | Kaempferol (10(-5) M) also caused antiproliferative effect on MCF-7 cell in the presence of E2 (10(-11) M) and restored to the addition of excess E2 (10(-7) M), which confirms that antiproliferation of kaempferol was induced via ER-dependent pathway. Further elucidation of the mechanism revealed that kaempferol treatment inhibited the activation of transcription factor activator protein-1 (AP-1) and MAPK signaling pathway. Moreover, kaempferol repressed phorbol-12-myristate-13-acetate (PMA)-induced MMP-9 expression and activity through suppressing the translocation of protein kinase Cδ (PKCδ) and MAPK signaling pathway | |
| IC50 | 23 μg/mL against MDA-MB-468 34 μg/mL against MDA-MB-231 | |
| Potency | Collectively, these results showed that kaempferol may be a potential drug for the effective treatment of TNBC. | |
| Cell line/ mice model | MCF-7, HCT-15, T47D, C-6, BT-549, A549, HEK293,MDA-MB-231, MDA-MB-468 | |
| Additional information | We have identified kaempferol and pentahalogenated pseudilins as efficient inhibitors of migration of MDA-MB-231 breast adenocarcinoma cells. In conclusion, the interplay of efflux transporters (P-gp, BCRP, and MRPs) and UGTs govern the subcellular exposure and corresponding pharmacological activity of kaempferol. | |
| PubChem ID | 5280863 | |
| Additional PMIDs | 20548938 24879482 31404596 31248102 33064762 27745695 24711053 25574182 28852738 27198988 20846786 31605603 25844270 31200254 16756079 25719685 32427405 19356725 25446499 29739490 12058323 15095143 16702307 22700791 25839119 27618000 34311274 34229591 34488594 8049151 10412031 15182386 34400957 34064100 33968897 24289290 26616378 24679058 26885750 15905060 16118406 17335117 21139040 23023566 23441618 26434836 26437391 26736086 26922854 28539711 30293450 10923837 33923148 33647428 25183275 25038699 28337113 15110097 15796157 30333884 17084606 12419914 19617894 19909799 8313386 26878784 22970976 31092862 16833018 15796199 17961621 21232900 24098354 25453494 26909969 29097115 30376625 10601582 16723233 16206043 33341499 31192773 21240759 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:50766-1 | |
| Safety | NA |