Global transcriptome analysis reveals partial estrogen-like effects of karanjin in MCF-7 breast cancer cells

Bhatt, Gaurav; Gupta, Akshita; Rangan, Latha; Limaye, Anil Mukund

doi:10.1016/j.gene.2022.146507

Cited by 7 publications

(7 citation statements)

References 55 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…1A). This suggests that karanjin may be a potential ERα agonist, which is possibly reflected in the partial E2-like effects of karanjin described earlier 8 .…”

Section: Resultsmentioning

confidence: 60%

“…The enrichment of estrogen-response-early genes in the karanjin-modulated transcriptome of the ERα-positive MCF-7 breast cancer cells 8 15 . Following validation of the molecular docking protocol as described in Materials and Methods, we docked karanjin to ERα-LBD extracted from eight wild-type agonist (E2)-or two antagonist (OHT or RAL)-bound structures.…”

Section: Resultsmentioning

confidence: 99%

“…The enrichment of estrogen-response-early genes in the karanjin-modulated transcriptome of the ERα-positive MCF-7 breast cancer cells 8 instigated us to hypothesize ERα as a functional target. The availability of agonist- or antagonist-bound crystal structures of ERα ligand binding domain (LBD) facilitated in silico molecular docking experiments to explore karanjin-ERα interaction.…”

Section: Resultsmentioning

confidence: 99%

See 2 more Smart Citations

Karanjin alters gene expression through ERα: a preliminary study

Bhatt,

Rangan,

Limaye

2024

Preprint

Self Cite

View full text Add to dashboard Cite

Karanjin is an abundant furanoflavonoid-constitutent of pongamia oil. Among several biological actions of karanjin, the antiproliferative effect of karanjin has gained traction in the recent years; raising speculations about its anticancer potential. In the backdrop of partial estrogen-like alteration of gene expression by karanjin in ERα positive MCF-7 breast cancer cells, we present preliminary evidences supporting of the role of ERα in karanjin-mediated effects.

show abstract

“…1A). This suggests that karanjin may be a potential ERα agonist, which is possibly reflected in the partial E2-like effects of karanjin described earlier 8 .…”

Section: Resultsmentioning

confidence: 60%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Karanjin alters gene expression through ERα: a preliminary study

Bhatt,

Rangan,

Limaye

2024

Preprint

Self Cite

View full text Add to dashboard Cite

show abstract

“…Roy et al (2021) reported that karanjin restricted cervical cancer cell growth by inhibiting the hyaluronic acid‐CD44 pathway. A recent study suggested that karanjin had a partial estrogen‐like activity, thereby presenting an anticancer potential in BC cells (Bhatt et al, 2022). Thus, we speculated that besides the PI3K/Akt pathway, other pathways may be involved in the anti‐BC effect of karanjin.…”

Section: Discussionmentioning

confidence: 99%

“…(2021) reported that karanjin restricted cervical cancer cell growth by inhibiting the hyaluronic acid-CD44 pathway. A recent study suggested that karanjin had a partial estrogen-like activity, thereby presenting an anticancer potential in BC cells (Bhatt et al, 2022).…”

Section: Discussionmentioning

confidence: 99%

The cytotoxicity of karanjin toward breast cancer cells is involved in the PI3K/Akt signaling pathway

Han

et al. 2022

Drug Development Research

View full text Add to dashboard Cite

Karanjin is a bioactive furanoflavonoid with various pharmacological activities including anticancer activities. However, the effect and the related mechanism of karanjin in breast cancer (BC) have not been revealed. The potential targets of karanjin and BC were predicted using SwissTargetPrediction and GeneCards databases, respectively. The overlapping targets between karanjin and BC were identified using the Venn diagram. DAVID database was used for the Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment pathway analysis. Cell viability, proliferation, and apoptosis were examined by MTT (3-(4, 5-dimethyl-2thiazolyl)-2, 5-diphenyl-tetrazolium bromide), EdU (5-ethynyl-2′-deoxyuridine) incorporation, and TUNEL (terminal deoxynucleotidyl transferase-mediated dUTP digoxigenin nick-end labeling) assays, respectively. The protein levels were measured by western blot analysis. We screened out 28 overlapping targets between karanjin and BC. KEGG analysis showed that the targets of karanjin in BC were associated with the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) pathway.Karanjin inhibited cell viability and impeded the proliferative ability of BC cells.Moreover, karanjin treatment induced apoptosis in BC cells. Additionally, karanjin treatment blocked the PI3K/Akt signaling pathway and activation of the PI3K/Akt pathway reversed the antitumor effect of karanjin on BC cells. In conclusion, karanjin exerted antitumor activity in BC cells by regulating the PI3K/Akt signaling pathway.

show abstract