Bioactivity of genistein: A review of in vitro and in vivo studies

Ganai, Ajaz Ahmad; Farooqi, Humaira

doi:10.1016/j.biopha.2015.10.026

Cited by 202 publications

(102 citation statements)

References 107 publications

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“…The phytoestrogens genistein and daidzein are isoflavones, found in soybean, one of the most important food components in Asian diet (156, 157). These compounds received considerable attention based on epidemiological studies demonstrating that the soybean-containing diets were associated with a lower incidence of particular cancers in Asian population (158).…”

Section: Natural Erβ Ligands and Melanomamentioning

confidence: 99%

Estrogen Receptor β in Melanoma: From Molecular Insights to Potential Clinical Utility

et al. 2016

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Cutaneous melanoma is an aggressive tumor; its incidence has been reported to increase fast in the past decades. Melanoma is a heterogeneous tumor, with most patients harboring mutations in the BRAF or NRAS oncogenes, leading to the overactivation of the MAPK/ERK and PI3K/Akt pathways. The current therapeutic approaches are based on therapies targeting mutated BRAF and the downstream pathway, and on monoclonal antibodies against the immune checkpoint blockade. However, treatment resistance and side effects are common events of these therapeutic strategies. Increasing evidence supports that melanoma is a hormone-related cancer. Melanoma incidence is higher in males than in females, and females have a significant survival advantage over men. Estrogens exert their effects through estrogen receptors (ERα and ERβ) that affect cancer growth in an opposite way: ERα is associated with a proliferative action and ERβ with an anticancer effect. ERβ is the predominant ER in melanoma, and its expression decreases in melanoma progression, supporting its role as a tumor suppressor. Thus, ERβ is now considered as an effective molecular target for melanoma treatment. 17β-estradiol was reported to inhibit melanoma cells proliferation; however, clinical trials did not provide the expected survival benefits. In vitro studies demonstrate that ERβ ligands inhibit the proliferation of melanoma cells harboring the NRAS (but not the BRAF) mutation, suggesting that ERβ activation might impair melanoma development through the inhibition of the PI3K/Akt pathway. These data suggest that ERβ agonists might be considered as an effective treatment strategy, in combination with MAPK inhibitors, for NRAS mutant melanomas. In an era of personalized medicine, pretreatment evaluation of the expression of ER isoforms together with the concurrent oncogenic mutations should be considered before selecting the most appropriate therapeutic intervention. Natural compounds that specifically bind to ERβ have been identified. These phytoestrogens decrease the proliferation of melanoma cells. Importantly, these effects are unrelated to the oncogenic mutations of melanomas, suggesting that, in addition to their ERβ activating function, these compounds might impair melanoma development through additional mechanisms. A better identification of the role of ERβ in melanoma development will help increase the therapeutic options for this aggressive pathology.

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Section: Natural Erβ Ligands and Melanomamentioning

confidence: 99%

Estrogen Receptor β in Melanoma: From Molecular Insights to Potential Clinical Utility

et al. 2016

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“…Moreover, HOTAIR was shown to enhance the AR-mediated transcriptional program and drive castration-resistant prostate cancer (CRPC) [55]. Microarray analysis for expression profiling indicated that HOTAIR was highly regulated by genistein, a soy-derived isoflavanoid compound acting as a chemotherapeutic agent against several cancer types [56]. In the link to miRNA, silencing of HOTAIR decreased proliferation, migration, invasion, and induced apoptosis; miR-34a directly targeted HOTAIR in PCa cells, which showed that genistein inhibited the growth of PCa cells by downregulating oncogenic HOTAIR that was also targeted by the tumor suppressor miR-34a [57].…”

Section: Hotair In Prostate Cancermentioning

confidence: 99%

HOTAIR: An Oncogenic Long Non-Coding RNA in Human Cancer

Tang

Hann

2018

Cell Physiol Biochem

215

135

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Long non-coding RNAs (LncRNAs) represent a novel class of noncoding RNAs that are longer than 200 nucleotides without protein-coding potential and function as novel master regulators in various human diseases, including cancer. Accumulating evidence shows that lncRNAs are dysregulated and implicated in various aspects of cellular homeostasis, such as proliferation, apoptosis, mobility, invasion, metastasis, chromatin remodeling, gene transcription, and post-transcriptional processing. However, the mechanisms by which lncRNAs regulate various biological functions in human diseases have yet to be determined. HOX antisense intergenic RNA (HOTAIR) is a recently discovered lncRNA and plays a critical role in various areas of cancer, such as proliferation, survival, migration, drug resistance, and genomic stability. In this review, we briefly introduce the concept, identification, and biological functions of HOTAIR. We then describe the involvement of HOTAIR that has been associated with tumorigenesis, growth, invasion, cancer stem cell differentiation, metastasis, and drug resistance in cancer. We also discuss emerging insights into the role of HOTAIR as potential biomarkers and therapeutic targets for novel treatment paradigms in cancer.

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“…Genistein were used in both prophylaxis and treatment of diseases in recent years, acting such as antioxidant (Ganai & Farooqi 2015;Kanazawa et al 1995), anticancer properties (Sarkar & Li 2002;Qi et al 2011), cardioprotection (Deodato et al 1999) and immunosupressor agent (Yellayi et al 2002). Puerarin has been demonstrated to possess a variety of beneficial activities on alleviating angiocardiopathy (Pan et al 2009), osteoporosis (Wong & Rabie 2007) and hangover (Penetar et al 2012).…”

Section: Discussionmentioning

confidence: 99%