Rutin inhibits androgen synthesis and metabolism in rat immature Leydig cells in vitro

Fei, Qianjin; Li, Xiaoheng; Zhu, Qiqi; Wang, Yiyan; Ge, Ren‐Shan; Jin, Xiaodong

doi:10.1111/and.14221

Cited by 6 publications

(3 citation statements)

References 32 publications

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“…However, this treatment could be temporary, and patients could eventually relapse and develop castration-resistant PCa as a result of overexpression and/or mutations in the ARs [79]. Studies have shown that rutin can be used as a potential treatment for androgen-sensitive PCa because its mechanism of action revolves around the suppression of androgen biosynthesis and metabolism [80].…”

Section: Discussionmentioning

confidence: 99%

Antioxidant, Anti-Inflammatory and Antiproliferative Effects of Osmanthus fragrans (Thunb.) Lour. Flower Extracts

Huang,

Bueno,

Garcia

et al. 2023

Plants

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Osmanthus fragrans (Thunb.) Lour. flowers (OF-F) have been traditionally consumed as a functional food and utilized as folk medicine. This study evaluated the antioxidant, anti-inflammatory and cytotoxic effects of OF-F extracts on prostate cancer cells (DU-145) and determined possible protein-ligand interactions of its compounds in silico. The crude OF-F extracts—water (W) and ethanol (E) were tested for phytochemical screening, antioxidant, anti-inflammatory, and anti-cancer. Network and molecular docking analyses of chemical markers were executed to establish their application for anticancer drug development. OF-F-E possessed higher total polyphenols (233.360 ± 3.613 g/kg) and tannin (93.350 ± 1.003 g/kg) contents than OF-F-W. In addition, OF-F-E extract demonstrated effective DPPH scavenging activity (IC50 = 0.173 ± 0.004 kg/L) and contained a high FRAP value (830.620 ± 6.843 g Trolox/kg). In cell culture experiments, OF-F-E significantly reduced NO levels and inhibited cell proliferation of RAW-264.7 and DU-145 cell lines, respectively. Network analysis revealed O. fragrans (Thunb.) Lour. metabolites could affect thirteen molecular functions and thirteen biological processes in four cellular components. These metabolites inhibited key proteins of DU-145 prostate cancer using molecular docking with rutin owning the highest binding affinity with PIKR31 and AR. Hence, this study offered a new rationale for O. fragrans (Thunb.) Lour. metabolites as a medicinal herb for anticancer drug development.

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Section: Discussionmentioning

confidence: 99%

Antioxidant, Anti-Inflammatory and Antiproliferative Effects of Osmanthus fragrans (Thunb.) Lour. Flower Extracts

Huang,

Bueno,

Garcia

et al. 2023

Plants

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“…In addition, rutin can improve the expressions of Cyp11a1 and Hsd3b1 , but with no effect on serum testosterone levels in male rats [ 133 ]. However, others reported that rutin rather inhibits basal and LH-induced secretions of androgen by rat immature Leydig cells by decreasing the expressions of Scarb1 , Cyp11a1 and Hsd3b1 [ 134 ].…”

Section: Natural Antioxidants Contributing To the Optimal Production ...mentioning

confidence: 99%

Prevention of Male Late-Onset Hypogonadism by Natural Polyphenolic Antioxidants

Martin,

Touaibia

2024

Nutrients

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Androgen production primarily occurs in Leydig cells located in the interstitial compartment of the testis. In aging males, testosterone is crucial for maintaining muscle mass and strength, bone density, sexual function, metabolic health, energy levels, cognitive function, as well as overall well-being. As men age, testosterone production by Leydig cells of the testes begins to decline at a rate of approximately 1% per year starting from their 30s. This review highlights recent findings concerning the use of natural polyphenolics compounds, such as flavonoids, resveratrol, and phenolic acids, to enhance testosterone production, thereby preventing age-related degenerative conditions associated with testosterone insufficiency. Interestingly, most of the natural polyphenolic antioxidants having beneficial effects on testosterone production tend to enhance the expression of the steroidogenic acute regulatory protein (Star) gene in Leydig cells. The STAR protein facilitates the entry of the steroid precursor cholesterol inside mitochondria, a rate-limiting step for androgen biosynthesis. Natural polyphenolic compounds can also improve the activities of steroidogenic enzymes, hypothalamus-pituitary gland axis signaling, and testosterone bioavailability. Thus, many polyphenolic compounds such as luteolin, quercetin, resveratrol, ferulic acid phenethyl ester or gigantol may be promising in delaying the initiation of late-onset hypogonadism accompanying aging in males.

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“…Abiraterone as an approved anti-prostate cancer drug is a CYP17A1 inhibitor [ 6 , 7 ]. Flavonols are characterized by a hydroxyl group present at C-3 of the flavone skeleton and there are some reports about the CYP17A1 inhibitory activity of flavonoids like rutin, morusflavone, quercetin, kaempferol and isorhamnetin [ 8 – 10 ].…”

Section: Introductionmentioning

confidence: 99%

In-silico activity prediction and docking studies of some flavonol derivatives as anti-prostate cancer agents based on Monte Carlo optimization

Tajiani,

Ahmadi,

Lotfi

et al. 2023

BMC Chemistry

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The QSAR models are employed to predict the anti-proliferative activity of 81 derivatives of flavonol against prostate cancer using the Monte Carlo algorithm based on the index of ideality of correlation (IIC) criterion. CORAL software is employed to design the QSAR models. The molecular structures of flavonols are demonstrated using the simplified molecular input line entry system (SMILES) notation. The models are developed with the hybrid optimal descriptors i.e. using both SMILES and hydrogen-suppressed molecular graph (HSG). The QSAR model developed for split 3 is selected as a prominent model ($${R}_{Validation}^{2}$$ R Validation 2 = 0.727, $${IIC}_{validation}$$ IIC validation = 0.628, $${Q}_{Validation}^{2}$$ Q Validation 2 = 0.642, and $${\overline{r} }_{m}^{2}$$ r ¯ m 2 =0.615). The model is interpreted mechanistically by identifying the characteristics responsible for the promoter of the increase or decrease. The structural attributes as promoters of increase of pIC50 were aliphatic carbon atom connected to double-bound (C…=…, aliphatic oxygen atom connected to aliphatic carbon (O…C…), branching on aromatic ring (c…(…), and aliphatic nitrogen (N…). The pIC50 of eight natural flavonols with pIC50 more than 4.0, were predicted by the best model. The molecular docking is also performed for natural flavonols on the PC-3 cell line using the protein (PDB: 3RUK).

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Rutin inhibits androgen synthesis and metabolism in rat immature Leydig cells in vitro

Cited by 6 publications

References 32 publications

Antioxidant, Anti-Inflammatory and Antiproliferative Effects of Osmanthus fragrans (Thunb.) Lour. Flower Extracts

Antioxidant, Anti-Inflammatory and Antiproliferative Effects of Osmanthus fragrans (Thunb.) Lour. Flower Extracts

Prevention of Male Late-Onset Hypogonadism by Natural Polyphenolic Antioxidants

In-silico activity prediction and docking studies of some flavonol derivatives as anti-prostate cancer agents based on Monte Carlo optimization

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