Steroid Receptors in Health and Disease

Moudgil, Virinder K.

doi:10.1007/978-1-4684-5541-0_1

Cited by 9 publications

(5 citation statements)

References 121 publications

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“…This can be explained by active consumption of testosterone during alloxan-dependent stress that increased the number of free AR enabled to interact with radioactive androgen H 3 -methyltrionolone (R-1881). At subsequent stages the increased testosterone deficiency induced by experimental diabetes was associated with drastic down-regulation of AR expression and signaling (due to their "masking") (Tepperman, 1968;Moudgil, 1988Moudgil, ,1990). Table 1.…”

Section: Resultsmentioning

confidence: 99%

Effect of Methyltrienolone on the Metabolic Disorders in Rat Model of Alloxan-Induced Diabetes

MBiol¹,

Kandelaki²,

Kakabadze³

et al. 2017

ESJ

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Aim: The aim of the study was to investigate the restoration of metabolic imbalance related with deficiency of insulin by the exogenous androgen supplementation in the experimental model of alloxan-induced diabetes in Wistar male rats. Methods: The experimental diabetes was induced by a single intraperitoneal administration of alloxan. The concentrations of glucose, immunereactive insulin, corticosterone, testosterone and estradiol were examined in blood, the intensity of DNA and RNA synthesis and androgen receptor expression were studied in the liver Results:The induction of diabetes increased the concentrations of glucose, corticosterone and estradiol while decreases insulin and testosterone concentration in blood as well as DNA/RNA synthesis and androgen receptors expression in hepatocytes. The administration of exogenous androgen significantly restored the metabolic imbalance and the expression of androgen receptors and increased DNA/RNA synthesis in liver cells maintained close to control level. Conclusion: The administration of methyltrienolone reduced the effect of "diabetic stress" and restored the hormonal dysfunction induced by alloxan.

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Section: Resultsmentioning

confidence: 99%

Effect of Methyltrienolone on the Metabolic Disorders in Rat Model of Alloxan-Induced Diabetes

MBiol¹,

Kandelaki²,

Kakabadze³

et al. 2017

ESJ

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“…2 Steroids as well as their derivatives have the potential to be developed as drugs for the treatment of a large number of diseases including cardiovascular, autoimmune diseases, brain tumours, breast cancer, osteoarthritis, prostate cancer etc. [3][4][5][6] The promise of using steroids for development of lead molecules lies in the regulation of a variety of biological processes by these molecules and being a fundamental class of signalling molecules. 7,8 Benign prostatic hyperplasia (BPH) and Prostate Cancer (PC), are the leading disorders of the old age men.…”

Section: Introductionmentioning

confidence: 99%

In silico Identification of potential 5α‒reductase inhibitors for prostatic diseases: QSAR modelling, molecular docking, and pre ADME predictions

Dhingra¹

2018

MOJDDT

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Background: Benign Prostatic Hyperplasia and prostate cancer are some of the most common old age men diseases and caused by augmented level of potent androgen dihydrotestosterone (DHT). Preventing DHT synthesis via 5α-reductase (5-AR) inhibition has been shown to have a remarkable effect on prostatic disease with low toxicity. Thus, there is much interest in the potential role for 5-AR inhibitors (5-ARIs) in the management of prostatic diseases. Some of the natural products, semi synthetic derivatives especially steroidal molecules, are effective inhibitors of 5AR. However, given the limited number of clinically approved inhibitors and the associated side effects, the discovery of new inhibitors is urgent. Here, the In silico approaches have been performed to identify new potential inhibitors of 5-AR. Methods: In the present study, two and three-dimensional (2D and 3D) QSAR models have been developed using a selected series of steroidal derivatives as 5ARIs, in order to elucidate the structural properties required for 5α-Reductase (5AR) inhibitory activity and anticancer activity. Further In-silico studies (molecular docking and pre-ADME) of selected series have also been carried out to identify the binding orientation and the receptor ligand interactions responsible for exhibited activity and the drug like properties. Results: Best 2D-QSAR model was generated using Simulated Annealing-Partial Least Square (SA-PLS) method (r 2 =0.9669, q 2 =0.8720, F-value=109.4339 and pred-r 2 =0.8289), whereas simulated annealing-k nearest neighbor (SA-kNN) approach provided us with best 3D-QSAR model (q 2 =0.9523 and pred-r 2 =0.8068). The compounds were further sorted by applying ADME properties against prostate cancer cell lines PC-3. Docking analysis indicated that the selected series of compounds have comparable binding affinity with the receptor protein and suggested that hydrophobic and electrostatic moieties can have a key role in the inhibition mechanism. These findings can provide a new strategy to develop new steroidal 5ARIs useful in prostatic disease.

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“…Steroids have always attracted considerable attention because of being a fundamental class of biological signaling molecules. Their profound biological, scientific, and clinical importance is now well validated. , They can regulate a variety of biological processes and thus have the potential to be developed as drugs for the treatment of a large number of diseases , including cardiovascular, autoimmune diseases, and cancer . In recent years, a variety of steroids with unusual and interesting structures have been isolated from a wide range of marine organisms, particularly from sponges and echinoderms …”

Section: Introductionmentioning

confidence: 99%

Total Synthesis and Pharmacological Characterization of Solomonsterol A, a Potent Marine Pregnane-X-Receptor Agonist Endowed with Anti-Inflammatory Activity

et al. 2011

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Recently, we reported the identification of a novel class of pregnane-X-receptor (PXR) agonists, solomonsterols A and B, isolated from the marine sponge Theonella swinhoei. Preliminary pharmacological studies demonstrated that these natural compounds are potential leads for the treatment of human disorders characterized by dysregulation of innate immunity. In this article, we describe the first total synthesis of solomonsterol A and its in vivo characterization in animal models of colitis. Using transgenic mice expressing the human PXR, we found that administration of synthetic solomonsterol A effectively protects against development of clinical signs and symptoms of colitis and reduced the generation of TNFα, a signature cytokine for this disorder. In addition, we have provided the first evidence that solomonsterol A might act by triggering the expression of TGFβ and IL-10, potent counter-regulatory cytokines in inflammatory bowel diseases (IBD). Finally, we have shown that solomonsterol A inhibits NF-κB activation by a PXR dependent mechanism. In summary, solomonsterol A is a marine PXR agonist that holds promise in the treatment of inflammation-driven immune dysfunction in clinical settings.

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Steroid Receptors in Health and Disease

Cited by 9 publications

References 121 publications

Effect of Methyltrienolone on the Metabolic Disorders in Rat Model of Alloxan-Induced Diabetes

Effect of Methyltrienolone on the Metabolic Disorders in Rat Model of Alloxan-Induced Diabetes

In silico Identification of potential 5α‒reductase inhibitors for prostatic diseases: QSAR modelling, molecular docking, and pre ADME predictions

Total Synthesis and Pharmacological Characterization of Solomonsterol A, a Potent Marine Pregnane-X-Receptor Agonist Endowed with Anti-Inflammatory Activity

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