scholarly journals Ginsenoside Rg1, a Novel Glucocorticoid Receptor Agonist of Plant Origin, Maintains Glucocorticoid Efficacy with Reduced Side Effects

2011 ◽  
Vol 187 (2) ◽  
pp. 942-950 ◽  
Author(s):  
Juan Du ◽  
Binbin Cheng ◽  
Xiaoyan Zhu ◽  
Changquan Ling
Keyword(s):  
Side Effects ◽  
Glucocorticoid Receptor ◽  
Receptor Agonist ◽  
Ginsenoside Rg1 ◽  
Plant Origin

scholarly journals Ginsenoside Rg1 Acts as a Selective Glucocorticoid Receptor Agonist with Anti-Inflammatory Action without Affecting Tissue Regeneration in Zebrafish Larvae

Cells ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 1107
Author(s):  
Min He ◽  
Mahmoud Halima ◽  
Yufei Xie ◽  
Marcel J. M. Schaaf ◽  
Annemarie H. Meijer ◽  
...  
Keyword(s):  
Side Effects ◽  
Glucocorticoid Receptor ◽  
Tissue Regeneration ◽  
Drug Effects ◽  
Structural Similarity ◽  
Ginsenoside Rg1 ◽  
Zebrafish Larvae ◽  
Wide Range ◽  
Ability To Regenerate ◽  
Anti Inflammatory

Glucocorticoids are effective anti-inflammatory drugs, but their clinical use is complicated due to the wide range of side effects they induce. Patients requiring glucocorticoid therapy would benefit from more selective glucocorticoid receptor (GR) agonists, capable of attenuating the immune response without causing these side effects. Ginsenosides, such as the compound Rg1, are natural plant compounds with structural similarity to classical glucocorticoids and well-documented anti-inflammatory effects. Here, we have investigated the activity of the ginsenoside Rg1 using a zebrafish larval model, in which amputation of the tail fin allows us to assess drug effects on inflammation, while the ability to regenerate the wounded tissue serves as a readout for side effects. We found that Rg1 attenuates neutrophilic inflammation at the amputation site, similarly to a classical glucocorticoid, beclomethasone. Mutation of the Gr abolishes this anti-inflammatory effect of Rg1. Rg1 and beclomethasone differentially modulate gene expression, suggesting that Rg1 induces transrepression, but not transactivation, activity of Gr. Interestingly, we found no effect of Rg1 on tissue regeneration, whereas beclomethasone inhibits tissue regeneration entirely. We conclude that Rg1 is a promising candidate for development as a selective glucocorticoid drug, and that zebrafish larvae provide a useful model system for screening of such GR agonists.

Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics Aspects of Lorcaserin, a Selective Serotonin 5-HT2C Receptor Agonist: An Update

2020 ◽  
Vol 20 (9) ◽  
pp. 768-778
Author(s):  
Sanjay Sharma ◽  
Komal S. Aware ◽  
Ketan Hatware ◽  
Kiran Patil
Keyword(s):  
Side Effects ◽  
Receptor Agonist ◽  
Scale Up ◽  
Mass Spectrometric ◽  
Selective Serotonin ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Step Method ◽  
Comprehensive Information ◽  
Tissue Matrix ◽  
Liquid Chromatographic

This review refers to the all-inclusive details of Lorcaserin Hydrochloride on comprehensive information about the synthesis, analytical methods, pharmacodynamics, pharmacokinetics, drug interactions and adverse effects. Lorcaserin Hydrochloride is chemically (R)-8-Chloro-1-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine hydrochloride. Lorcaserin HCl is a novel, synthetic, centrally-acting selective serotonin C (5-HT2c) receptor, l agonist, which results in increased satiety and decreased food consumption in patients. Headache, dizziness and nausea are the most common side effects associated with this drug. Lorcaserin HCl has two major metabolites, one conjugated with glucuronide called N-carbamoyl glucuronide which is excreted in urine and the second Lorcaserin N-sulfamate, which is circulated in the blood. Lorcaserin HCl is synthesized using four different schemes of which a six-step method that resulted in 92.3% yield with 99.8% of purity is employed for scale-up production. It is analyzed quantitatively in the plasma and brain tissue matrix of rats by Ultra Performance Liquid chromatographic (UPLC) method using MS-MS (Mass Spectrometric) detection.

scholarly journals The Plant-Derived Glucocorticoid Receptor Agonist Endiandrin A Acts as Co-Stimulator of Colonic Epithelial Sodium Channels (ENaC) via SGK-1 and MAPKs

PLoS ONE ◽  
2012 ◽  
Vol 7 (11) ◽  
pp. e49426 ◽  
Author(s):  
Dana Kuntzsch ◽  
Theresa Bergann ◽  
Petra Dames ◽  
Anja Fromm ◽  
Michael Fromm ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Sodium Channels ◽  
Receptor Agonist ◽  
Epithelial Sodium Channels

scholarly journals Computational and Biological Comparisons of Plant Steroids as Modulators of Inflammation through Interacting with Glucocorticoid Receptor

2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Mohamed A. Morsy ◽  
Snehal S. Patel ◽  
Azza A. K. El-Sheikh ◽  
Jignasa K. Savjani ◽  
Anroop B. Nair ◽  
...  
Keyword(s):  
Side Effects ◽  
Glucocorticoid Receptor ◽  
Tumor Necrosis ◽  
Serum Levels ◽  
Withaferin A ◽  
Boswellic Acid ◽  
Cotton Pellet ◽  
Anti Inflammatory ◽  
Necrosis Factor

Despite the usefulness of glucocorticoids, they may cause hazardous side effects that limit their use. Searching for compounds that are as equally efficient as glucocorticoids, but with less side effects, the current study compared plant steroids, namely, glycyrrhetinic acid, guggulsterone, boswellic acid, withaferin A, and diosgenin with the classical glucocorticoid, fluticasone. This was approached both in silico using molecular docking against glucocorticoid receptor (GR) and in vivo in two different animal models. All tested compounds interacted with GR, but only boswellic acid and withaferin A showed docking results comparable to fluticasone, as well as similar in vivo anti-inflammatory effects, by significantly decreasing serum levels of interleukin-6 and tumor necrosis factor-α in cotton pellet-induced granuloma in rats. In addition, both compounds significantly decreased the percent of change in ear weight in croton oil-induced ear edema in mice and the granuloma weight in cotton pellet-induced granuloma in rats, to levels comparable to that of fluticasone. Both boswellic acid and withaferin A had no effect on adrenal index, but only withaferin A significantly increased the thymus index. In conclusion, boswellic acid may have comparable anti-inflammatory effects to fluticasone with fewer side effects.

The use of phytotherapy in diseases caused by parasitic protozoa

2014 ◽  
Vol 60 (1) ◽  
pp. 1-8 ◽  
Author(s):  
Monika Derda ◽  
Edward Hadaś
Keyword(s):  
Side Effects ◽  
Chronic Diseases ◽  
Conventional Treatment ◽  
Therapeutic Agents ◽  
Pharmaceutical Market ◽  
Parasitic Diseases ◽  
Plant Origin ◽  
Parasitic Protozoa ◽  
Herbal Preparations ◽  
Increasing Demand

AbstractThe paper presents an overview of the use of natural therapeutic agents in combating parasitic diseases. Nowadays there is increasing demand for proven plant therapies, which often are found to be more effective than synthetic pharmaceuticals in chronic diseases. In many cases herbal preparations perfectly supplement the conventional treatment and at the same time do not cause side effects. On the pharmaceutical market there are many drugs of plant origin which have been applied in the treatment of parasitic diseases. However, researchers are still looking for new plants, or specific substances isolated from them, which can be used in therapy. In this paper, drugs of plant origin used in the treatment of amoebiasis, giardiasis, malaria, leishmaniasis, trypanosomiasis and acanthamoebiasis are described.

scholarly journals Acquired Glucocorticoid Resistance Due to Homologous Glucocorticoid Receptor Downregulation: A Modern Look at an Age-Old Problem

Cells ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 2529
Author(s):  
Lee-Maine L. Spies ◽  
Nicolette J. D. Verhoog ◽  
Ann Louw
Keyword(s):  
Transcription Factor ◽  
Side Effects ◽  
Pharmaceutical Industry ◽  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
Molecular Mechanisms ◽  
Protein Levels ◽  
Current Review ◽  
Role Players ◽  
Receptor Conformation

For over 70 years, the unique anti-inflammatory properties of glucocorticoids (GCs), which mediate their effects via the ligand-activated transcription factor, the glucocorticoid receptor alpha (GRα), have allowed for the use of these steroid hormones in the treatment of various autoimmune and inflammatory-linked diseases. However, aside from the onset of severe side-effects, chronic GC therapy often leads to the ligand-mediated downregulation of the GRα which, in turn, leads to a decrease in GC sensitivity, and effectively, the development of acquired GC resistance. Although the ligand-mediated downregulation of GRα is well documented, the precise factors which influence this process are not well understood and, thus, the development of an acquired GC resistance presents an ever-increasing challenge to the pharmaceutical industry. Recently, however, studies have correlated the dimerization status of the GRα with its ligand-mediated downregulation. Therefore, the current review will be discussing the major role-players in the homologous downregulation of the GRα pool, with a specific focus on previously reported GC-mediated reductions in GRα mRNA and protein levels, the molecular mechanisms through which the GRα functional pool is maintained and the possible impact of receptor conformation on GC-mediated GRα downregulation.

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