An insight on genistein as potential pharmacological and therapeutic agent

Rahman, Syed Azizur; Islam, Rezuanul; Swaraz, A.M.; Ansari, Anesa; Parvez, Md. Masud; Paul, Depak Kumar

doi:10.1016/s2221-1691(12)60522-x

Cited by 11 publications

(3 citation statements)

References 127 publications

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“…It is well known that natural compounds, the base of folk medicine and, consequently, pharmacognosy, represent excellent sources of inspiration for modern medicine, continuously offering a wellspring of new remedies [ 1 ]. Genistein (Gen) is one of the most studied phytocompounds in the class of isoflavones [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

Genistein in 1:1 Inclusion Complexes with Ramified Cyclodextrins: Theoretical, Physicochemical and Biological Evaluation

Danciu

Şoica

Oltean

et al. 2014

IJMS

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Genistein is one of the most studied phytocompound in the class of isoflavones, presenting a notable estrogenic activity and in vitro and/or in vivo benefits in different types of cancer such as those of the bladder, kidney, lung, pancreatic, skin and endometrial cancer. A big inconvenience for drug development is low water solubility, which can be solved by using hydrophilic cyclodextrins. The aim of this study is to theoretically analyze, based on the interaction energy, the possibility of a complex formation between genistein (Gen) and three different ramified cyclodextrins (CD), using a 1:1 molar ratio Gen:CD. Theoretical data were correlated with a screening of both in vitro and in vivo activity. Proliferation of different human cancer cell lines, antimicrobial activity and angiogenesis behavior was analyzed in order to see if complexation has a beneficial effect for any of the above mentioned activities and if so, which of the three CDs is the most suitable for the incorporation of genistein, and which may lead to future improved pharmaceutical formulations. Results showed antiproliferative activity with different IC50 values for all tested cell lines, remarkable antimicrobial activity on Bacillus subtilis and antiangiogenic activity as revealed by CAM assay. Differences regarding the intensity of the activity for pure and the three Gen complexes were noticed as explained in the text. The data represent a proof that the three CDs can be used for furtherer research towards practical use in the pharmaceutical and medical field.

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Section: Introductionmentioning

confidence: 99%

Genistein in 1:1 Inclusion Complexes with Ramified Cyclodextrins: Theoretical, Physicochemical and Biological Evaluation

Danciu

Şoica

Oltean

et al. 2014

IJMS

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“…Genistein (Gen), recognized as the predominant isoflavone in soybean enriched foods, is one of the most extensively studied phytoestrogens which are available in Asian diets 1 . Epidemiological studies have provided evidence for a protective role of isoflavones against the development of numerous cancers including breast cancer, cervical cancer and prostate cancer 2 .…”

Section: Introductionmentioning

confidence: 99%

Genistein Promotes Proliferation of Human Cervical Cancer Cells Through Estrogen Receptor-Mediated PI3K/Akt-NF-κB Pathway

Chen¹,

Chen²,

Zheng³

et al. 2018

J. Cancer

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Phytoestrogens are polyphenol compounds which have similar structure to 17β-estradiol (E2), a kind of main estrogen in women. Thus, phytoestrogens may affect the reproductive and endocrine systems, leading to the development of estrogen-related cancers. The effect of genistein (Gen), one of the most studied phytoestrogens, on human cervical cancer cells (HeLa) was investigated in this study. It was found that Gen at concentrations of 0.001, 0.01, 0.1 and 1 µmol·L-1 promoted the proliferation of HeLa cells in a dose-dependent manner. Gen increased the portion of HeLa cells in S phase and decreased the portion of the cells in G1 phase. Besides, apoptosis rate of the cells was significantly lower when treated with Gen compared with the control group. It was also found that the expression of ERα, Akt or nuclear NF-κB p65 protein was activated by Gen. The correlation between these three proteins may be as following: ERα was the upstream, followed by Akt, and then nuclear NF-κB p65 protein. In addition, the downstream genes of activated nuclear NF-κB p65 were found to be associated with cell cycle and apoptosis of cancer cells. Our results suggested that Gen may stimulate cell proliferation partially through the estrogen receptor-mediated PI3K/Akt-NF-κB pathway and the further activation of the downstream genes of nuclear NF-κB p65.

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“…Most of the scientific interest in genistein is owed to its health-prolonging effects, which were shown both in vivo and in vitro, and result in its possible application in the prevention and treatment of the diseases of affluence, i.e. obesity, diabetes and cancer, and genetic diseases (Rahman et al, 2012;Gilbert & Liu, 2013). Isonicotinamide is a pharmaceutically acceptable coformer widely used in cocrystallization of various carboxyl-and hydroxy-derived molecules, including quercetin (Smith et al, 2011), fisetin and luteolin (Sowa et al, 2013), diclofenac and clofibric acid (Bá thori et al, 2011), 3-nitrophenol (Ratajczak et al, 2013) and orcinol (Mukherjee et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

A 1:2 cocrystal of genistein with isonicotinamide: crystal structure and Hirshfeld surface analysis

2013

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Genistein, a naturally occurring polyphenolic compound, was combined with isonicotinamide, a pharmaceutically acceptable coformer, to yield a 1:2 cocrystal [systematic name: 5,7-dihydroxy-3-(4-hydroxyphenyl)chromen-4-one-pyridine-4-carboxamide (1/2)], C15H10O5·2C6H6N2O. The molecules in the cocrystalline phase are present in their neutral forms, and assemble a molecular layer by means of hydrogen bonding.

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An insight on genistein as potential pharmacological and therapeutic agent

Cited by 11 publications

References 127 publications

Genistein in 1:1 Inclusion Complexes with Ramified Cyclodextrins: Theoretical, Physicochemical and Biological Evaluation

Genistein in 1:1 Inclusion Complexes with Ramified Cyclodextrins: Theoretical, Physicochemical and Biological Evaluation

Genistein Promotes Proliferation of Human Cervical Cancer Cells Through Estrogen Receptor-Mediated PI3K/Akt-NF-κB Pathway

A 1:2 cocrystal of genistein with isonicotinamide: crystal structure and Hirshfeld surface analysis

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