A Multicenter Randomized Double-blind Placebo-controlled Parallel Group Phase II Study Evaluating the Clinical Efficacy and Safety of GN-037 Cream Used in the Treatment of Mild to Moderate Plaque Psoriasis

This Phase II study was designed as a multicenter, randomized, double-blind, placebo-controlled and 3-parallel arm, to assess clinical efficacy, safety, and tolerability of GN-037 versus clobetasol 17-propionate and placebo in patients diagnosed with mild to moderate plaque psoriasis at least 6 months ago

Start Date07 Dec 2022

Sponsor / Collaborator

Gen Ilaç ve Saglik Ürünleri Sanayi ve Ticaret AS

[+1]

NCT05428202 / CompletedPhase 1IIT

Phase I Study to Assess Safety, Tolerability and Clinical Benefits of Topically Applied GN-037 Cream in Healthy Volunteers and Patients Diagnosed With Psoriasis

In this Phase I study, three different doses (low, medium and high dose, on the basis of surface area applied) of GN-037 cream (12 volunteers in total) and placebo (6 volunteers in total) will be administered to healthy volunteers. In the active dose arm, 4 healthy volunteers will receive GN-037 cream and 2 healthy volunteers will receive placebo. Randomization in each dose arm will be 2:1.

Start Date28 Mar 2022

Sponsor / Collaborator

Tc Erciyes University

[+1]

EUCTR2020-004081-19-DE / Not yet recruitingPhase 3

Double-blind, randomised clinical study comparing efficacy and safety of Betamethasone dipropionate 0.64 mg/g _ Salicylic acid 30 mg/g Ointment (Test) vs. Diprosalic(R) Ointment (Reference) vs. Vehicle in patients with chronic stable plaque psoriasis

Start Date22 Dec 2021

Sponsor / Collaborator

Dermapharm AG

100 Clinical Results associated with GR x COX

100 Translational Medicine associated with GR x COX

0 Patents (Medical) associated with GR x COX

198

Literatures (Medical) associated with GR x COX

01 Dec 2024·Tissue and Cell

Hepatoprotective effect of silymarin-chitosan nanocomposite against aluminum-induced oxidative stress, inflammation, and apoptosis

Article

Author: El-Demerdash, Fatma M. ; Mohamed, Tarek M ; Radwan, Aliaa M. ; El-Demerdash, Fatma M ; Ahmed, Manal M. ; Kang, Wenyi ; Mohamed, Tarek M. ; Radwan, Aliaa M ; Ahmed, Manal M

Aluminum (Al) is abundant in the environment, and its toxicity is attributed to free radical formation and subsequent oxidative stress. While silymarin is a well-known antioxidant, its low water solubility and bioavailability limit its therapeutic effects. This study was designated to formulate silymarin chitosan nanoparticles (SM-CS-NPs) and evaluate its ameliorative effect against hepatotoxicity induced by aluminum chloride (AlCl₃). SM-CS-NPs were prepared by ionotropic gelation method and characterized using different techniques. Rats were distributed into six groups (n=7/group), control, silymarin (SM; 15 mg/kg B.W), silymarin-chitosan nanoparticles (SM-CS-NPs; 15 mg/kg), aluminum chloride (AlCl₃, 34 mg/kg), SM or SM-CS-NPs administrated orally one hour before the treatment with AlCl₃ for 30 days, respectively. Results showed that supplementation of SM-CS-NPs or SM solo improved the antioxidant state and reduced oxidative stress. On the other hand, the pretreatment with SM-CS-NPs or SM followed by AlCl₃ significantly restored liver functions (AST, ALT, ALP, LDH, total protein, albumin, globulin, and bilirubin) and modulated oxidative stress biomarkers (TBARS and H₂O₂), with improved cellular antioxidant defense (SOD, CAT, GPx, GR, GST, and GSH) and maintained normal liver histological structure compared to rats treated with AlCl₃ alone. Furthermore, they alleviated the inflammation and apoptosis by downregulating the expression level of COX-2, caspase-3, and TNFα. This ameliorative effect was stronger with silymarin nanoform than in bulk-state silymarin. According to the findings, silymarin preparation in nanoform boosts its ameliorative and protective effects against AlCl₃ hepatotoxicity.

01 Oct 2024·The Journal of Steroid Biochemistry and Molecular Biology

Investigation on the mechanism of androsta-4,6,8,14-tetraene-3,11,16-trione against acute lymphoblastic leukemia

Article

Author: Chen, Dongjie ; Cheng, Guiguang ; Zhao, Tianrui ; Liu, Yaping ; Wang, Yongpeng ; Wen, Yan ; Xiao, Shanshan ; Cao, Jianxin

Steroids are potential anti-leukemia agents, and Epigynum auritum is a Yunnan folk medicine with high levels of androsterone, pregnane, and steroid derivatives. However, the underlying therapeutic mechanism of androsta-4,6,8,14-tetraene-3,11,16-trione (ATT), an androsterone isolated from Epigynum auritum, is not yet clear. This study aimed to explore the anti-leukemia mechanism of ATT using molecular biology, network pharmacology, and molecular docking technology. The cell viability results showed that ATT had an anti-proliferation effect in acute lymphoblastic leukemia cells (CEM/C1, MOLT-4, Jurkat, BALL-1, Nalm-6, and RS4;11). Further studies showed that ATT reduced the mitochondrial membrane potential in B-cell acute lymphoblastic leukemia cell lines (BALL-1, Nalm-6, and RS4;11) and induced cell cycle arrest in MOLT-4 and BALL-1. ATT induced BALL-1 cell apoptosis by activating Caspase 3/7 activity and causing DNA fragmentation. Network pharmacology results suggested that ATT exerts its anti-leukemia activity via the PI3K/Akt signaling pathway. In addition, molecular docking analysis showed that ATT had high scores in docking with PTGS2, NR3C1, and AR. Western blotting results showed that ATT reduced the relative protein level of P-PI3K and P-Akt, thereby increasing the relative level of pro-apoptosis protein Bax and reducing the relative level of anti-apoptosis protein Bcl-2, the apoptosis downstream protein pro-caspase3, and cell proliferation-related proteins (P-GSK3B and CyclinD1). In conclusion, these results demonstrated that ATT could be a potential candidate drug with apoptosis-induction and cell cycle arrest effects for further investigation in acute lymphoblastic leukemia therapy.

18 Sep 2024·Journal of Agricultural and Food Chemistry

Gypenoside LXXV Alleviates Colitis by Reprograming Macrophage Polarization via the Glucocorticoid Receptor Pathway

Article

Author: Wu, Wenjing ; Zhou, Yifa ; Qu, Xian ; Cheng, Hairong ; Hu, Chenxing ; Zhu, Xuepeng ; Wan, Mengqi

An imbalance in the macrophage phenotype is closely related to various inflammatory diseases. Here, we discovered that gypenoside LXXV (GP-75), a type of saponin from Gynostemma pentaphyllum, can reprogram M1-like macrophages into M2-like ones. On a mechanistic level, GP-75 inhibits NF-κB-COX2 signaling by targeting the glucocorticoid receptor (GR). Administration of GP-75, either orally or by intraperitoneal injection, significantly alleviates ulcerative colitis in mice, a pathogenesis associated with macrophage polarization. Clodronate liposomes, which deplete macrophages in mice, as well as GR antagonist RU486, abrogate the anticolitis effect of GP-75, thus confirming the pivotal role of macrophages in GP-75 function. We also showed that GP-75 has no toxicity in mice. Overall, this is the first report that demonstrates the effect of GP-75 on macrophage reprograming and as an agent against colitis. Because G. pentaphyllum is gaining popularity as a functional food, our findings offer new perspectives on the use of gypenosides as potential nutraceuticals for medical purposes.

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