Apoptotic Effects of Genistein, Biochanin-A and Apigenin on LNCaP and PC-3 Cells by p21 through Transcriptional Inhibition of Polo-like Kinase-1

Seo, Young Jin; Park, Dong Jin; Chun, So Young; Park, Yoon Kyu; Kang, Ku Seong; Kwon, Tae Gyun

doi:10.3346/jkms.2011.26.11.1489

Cited by 82 publications

(58 citation statements)

References 23 publications

(27 reference statements)

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“…Recently, treatment with biochanin A has been shown to reduce PLK-1 and increase p21 expression in LNCaP and PC-3 cell lines of prostate cancer, causing delayed mitosis [42]. As elevation of p21 after PLK-1 inhibition has been regarded as a general phenomenon in normal and cancer cells [43], the retarded growth of HERP-treated tumours may also be associated with the inhibitory effects of biochanin A on tumour cell proliferation.…”

Section: Experimental Animalmentioning

confidence: 99%

Inhibition of DMBA‐induced Oral Squamous Cells Carcinoma Growth by Brazilian Red Propolis in Rodent Model

Ribeiro

Alves

Santos

et al. 2015

Basic Clin Pharma Tox

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Abstract:We investigated the effect of oral administration of hydroalcoholic extract of Brazilian red propolis (HERP) on DMBA-induced oral squamous cell carcinomas (OSCC) in rodents. The chemical components of the HERP were assessed by high-performance liquid chromatography (HPLC). Carcinogenesis was topically induced in the lower lip of 25 rats using 9,10-dimethyl-1,2-benzanthracene (DMBA); the tumour was treated with saline (TUM1) and Tween 80 (TUM2) as well as HERP at 10, 50 and 100 mg/kg (HERP10, HERP50 and HERP100, respectively) for 20 weeks. Topical application of saline and oral administration of 100 mg/kg HERP was used in five rats as a control group (CTR). After 26 weeks, the histological malignancy grading and immunohistochemical expression of INK4A were assessed in the tumours/tissue samples. The compounds identified were propyl gallate, daidzein, catechin, epicatechin, formononetin and biochanin A. Formononetin, daidzein and biochanin A showed concentration of 23.29, 0.38 and 0.67 mg/g of HERP, respectively. HERP at doses of 50 and 100 mg/ kg inhibited 40% of OSCC growth and promoted a 3-week delay in development of clinically detectable tumours. Epithelial dysplasia was observed in all samples with no clinical tumour, except in CTR. No significant difference in the immunoexpression of INK4A was observed between HERP-treated and saline/Tween 80-treated groups (p > 0.05). Our results suggest that HERP exerts chemopreventive activity on the progression of DMBA-induced epithelial dysplasia to OSCC in an experimental model of labial carcinogenesis; however, this effect is not associated with Ki-67 and p16INK4A immunoexpression.Propolis is a natural, resinous hive product that honeybees manufacture by mixing their own waxes and salivary secretions with resins collected from cracks in tree barks and leaf buds [1]. Propolis samples from different regions of Brazil display different colours and chemical compositions, depending on the local flora at the site of collection [2]. Brazilian green propolis, derived from Baccharis dracunculifolia (Asteraceae) [3], is the most popular and well-studied Brazilian propolis.In the last few years, a red variety of Brazilian propolis has been described and characterized by various authors [4][5][6], demonstrating that the botanical origin influences directly its chemical composition. Isoflavones are chemical constituents usually identified in ethanolic extracts of red propolis, being formononetin, daidzein and biochanin A more often found [5,7].Brazilian

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Section: Experimental Animalmentioning

confidence: 99%

Inhibition of DMBA‐induced Oral Squamous Cells Carcinoma Growth by Brazilian Red Propolis in Rodent Model

Ribeiro

Alves

Santos

et al. 2015

Basic Clin Pharma Tox

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“…Genistein can bind to both the Estrogen Receptor alpha (ER ) and the Estrogen Receptor beta (ER ), although it has a higher affinity for the ER [19], and genistein is thought to exert its estrogenic effects through mechanisms similar to those of estradiol [20]. Biochanin A ( ) is the 4 -O-methyl derivative of genistein and biochanin A is the predominant isoflavone found in alfalfa, Trifolium pratense, and Cicer arietinum [21] which has an inhibitory and apoptogenic effect on certain cancer cells such as pancreatic cancer and prostate cancer [22,23].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and Antioxidant Activities of Genistein, Biochanin A, and Their Analogues

Sherif

Tekluu

2018

Journal of Chemistry

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A series of naturally occurring genistein ( ) and biochanin A ( ) compounds and their analogues were synthesized from phloroglucinol. The structures of all the synthesized compounds were established by the combined use of 1 HNMR, 13 CNMR, IR spectral data, and mass spectrometry; their antioxidant activities were investigated. Most of the synthesized compounds show moderate-to-high activity; only two compounds exhibit no significant activity.

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“…Apoptosis rates are 27 and 37% for the cells treated with flavone compared to 13 and 25% for control group respectively in MDA-MB-231 and MCF-7 cells (24). Apoptosis is increased about 2.4-to 3.1-fold induced by flavonoid for 36 h in LNCaP cells (33). Our previous study showed that apoptotic rate was 15.15±0.20% when treated by 200 µM flavone compared to 4.90±1.23% of control group in breast cancer cells (32).…”

Section: Discussionmentioning

confidence: 86%

The co‑treatment of metformin with flavone synergistically induces apoptosis through inhibition of PI3K/AKT pathway in breast cancer cells

et al. 2018

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Abstract. Metformin, a widely used antidiabetic drug, exhibits anticancer effects which are mediated by the phosphatidylinositol 3-kinase (PI3K)/serine/threonine kinase (AKT) signaling pathway. However, its use in anticancer therapy combined with other natural products remains unclear. Flavone as the core structure of flavonoids has been demonstrated to induce cell apoptosis without causing serious side effect. Murine double minute X (MDMX) inhibits tumor suppressor gene p53 whose function is associated with the PI3K/AKT pathway. The results presented herein revealed that the combination of metformin and flavone significantly inhibited cell viability, and increased apoptosis of human breast cancer cells compared with metformin or flavone alone. The combination decreased the protein expression of MDMX, activated p53 through the PI3K/AKT signaling pathway, regulated p53 downstream target genes Bcl-2 apoptosis regulator, BCL2 associated X apoptosis regulator and cleaved caspase3, subsequently inducing apoptosis in MDA-MB-231 and MCF-7 breast cancer cells. These results indicated that dietary flavone may potentiate breast cancer cell apoptosis induced by metformin, and PI3K/AKT is involved in regulating MDMX/p53 signaling. This data suggests that dietary supplementary of flavone is a promising strategy for metformin mediated anticancer effects.

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Apoptotic Effects of Genistein, Biochanin-A and Apigenin on LNCaP and PC-3 Cells by p21 through Transcriptional Inhibition of Polo-like Kinase-1

Cited by 82 publications

References 23 publications

Inhibition of DMBA‐induced Oral Squamous Cells Carcinoma Growth by Brazilian Red Propolis in Rodent Model

Inhibition of DMBA‐induced Oral Squamous Cells Carcinoma Growth by Brazilian Red Propolis in Rodent Model

Synthesis, Characterization, and Antioxidant Activities of Genistein, Biochanin A, and Their Analogues

The co‑treatment of metformin with flavone synergistically induces apoptosis through inhibition of PI3K/AKT pathway in breast cancer cells

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