Last update 21 Nov 2024

Ochromycinone

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(+)-ochromycinone, (3s)-3.beta.-methyl-8-hydroxy-1,2,3,4,7,12-hexahydrobenzo(a)anthracene-1,7,12-trione, Benz(a)anthracene-1,7,12(2h)-trione, 3,4-dihydro-8-hydroxy-3-methyl-, (s)-

+ [2]

Target

STAT3

Mechanism

STAT3 inhibitors(Signal transducer and activator of transcription 3 inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

Kochi University of Technology

Active Organization-

Inactive Organization

University of Michigan College of Engineering

National Cancer Institute

The Ohio State University

+ [1]

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H14O4

InChIKeyZAWXOCUFQSQDJS-UHFFFAOYSA-N

CAS Registry111540-00-2

100 Clinical Results associated with Ochromycinone

100 Translational Medicine associated with Ochromycinone

100 Patents (Medical) associated with Ochromycinone

Literatures (Medical) associated with Ochromycinone

01 Jan 2024·International Journal of Rheumatic Diseases

STA‐21 regulates Th‐17/Treg balance and synovial fibroblasts functions in rheumatoid arthritis

Article

Author: Mahmud, Shokhan Osman ; Maroof, Avin Mohammad Arif ; Hamad, Badraldin Kareem ; Mohammad, Talar Ahmad Merza

AbstractJAK/STAT signaling pathway plays a significant role in cytokines and growth factors signaling involved in the pathogenesis of rheumatoid arthritis (RA). STAT3 is a major downstream signaling mediator of important pro‐inflammatory cytokines involved in Th‐17 cell differentiation playing a significant role in regulating Th‐17/ Treg balance and the development of autoimmune diseases, especially RA. Studies also have reported the role of the STAT3 pathway in inflammatory and destructive functions of synovial fibroblasts (SFs) in RA. STA‐21 is a small molecule inhibitor that can inhibit STAT3 activation impairing the expression of STAT3 target genes. In this study, we tested whether a STAT3 inhibitor, STA‐21, can alter Th‐17/Treg balance and SF functions in RA. Peripheral blood mononuclear cells (PBMC) and SFs were isolated from 34 RA patients undergoing orthopedic surgery and 15 healthy controls to investigate in vitro effects of STA‐21. The main assays were MTT assay, PI staining, reverse transcription‐PCR (RT‐PCR), flow cytometric analysis, and ELISA. Results showed that STA‐21 reduced the proportion of Th‐17 cells and the expression of STAT3 target genes, RORγt, IL‐21, and IL‐23R involved in Th‐17 cells differentiation while it conversely increased the proportion of Treg cells, which theoretically may result in suppression of inflammation. We found that STAT3 activation and its target gene expression increased in RA‐SFs. In addition, results showed that STA‐21 can reduce the expression of STAT3 target genes related to cell proliferation, apoptosis, and inflammation leading to a decrease in proliferation and conversely increase in apoptosis of RA‐SFs. Overall, our findings provide evidence that STA‐21 can reduce inflammatory immune processes conducted by T cells and RA‐SFs in RA, suggesting that this compound is a suitable option for clinical studies in RA.

01 Jun 2023·International immunopharmacology

STA-21, a small molecule STAT3 inhibitor, ameliorates experimental autoimmune encephalomyelitis by altering Th-17/Treg balance.

Article

Author: Marofi, Faroogh ; Barpour, Nesa ; Gharibi, Tohid ; Safaei, Sahar ; Baradaran, Behzad ; Hosseini, Arezoo ; Nejati-Koshki, Kazem ; Abdollahpour-Alitappeh, Meghdad ; Ebrahimi-Kalan, Abbas ; Mohammadzadeh, Adel ; Baghbani, Elham

BACKGROUNDNumerous studies have demonstrated the role of T helper (Th) 17 and T regulatory (reg) cells and pro-inflammatory and anti-inflammatory cytokines related to these cells in the pathogenesis of MS and its animal model, experimental autoimmune encephalomyelitis (EAE). STAT3 is one of the downstream signaling proteins of IL-23, IL-6, and IL-21 that are required for Th17 cells differentiation. STA-21 is a STAT3 inhibitor that functions by inhibiting STAT3 dimerization and binding to DNA impairing the expression of STAT3 target genes including, RORγt, IL-21 and IL-23R that are also required for Th17 cell differentiation.AIMIn this study, we evaluated the effect of STA-21 on EAE Model and investigated how this small molecule can change Th17/Treg balance leading to amelioration of disease.METHODSAfter EAE induction and treatment with STA-21, its effects were assessed. Major assays were H&E and LFB staining, Flow cytometric analysis, Reverse transcription-PCR (RT-PCR), and ELISA.RESULTSSTA-21 ameliorated the EAE severity and decreased the EAE inflammation and demyelination. It also decreased STAT3 phosphorylation, the proportion of Th17 cells and the protein level of IL-17. In contrast, the balance of Tregs and the level of anti-inflammatory cytokine, IL-10 increased in STA-21-treated mice. Moreover, STA-21 significantly decreased the expression of Th17 related transcription factors, RORɣt and IL-23R while FOXP3 expression associated with Treg differentiation was increased.CONCLUSIONThis study showed that STA-21 has therapeutic effects in EAE by reducing inflammation and shifting inflammatory immune responses to anti-inflammatory and can be used as a suitable treatment strategy for the treatment of EAE. The effectiveness of inhibiting or strengthening the functional cells of the immune system by these small molecules in terms of easy to access, simple construction and inexpensive expansion make them as a suitable tool for the treatment of inflammatory and autoimmune diseases.

01 Jun 2023·International Immunopharmacology

Corrigendum to “STA-21, a small molecule STAT3 inhibitor, ameliorates experimental autoimmune encephalomyelitis by altering Th-17/Treg balance” [Int. Immunopharmacol. 119 (2023) 110160]

Author: Marofi, Faroogh ; Barpour, Nesa ; Gharibi, Tohid ; Safaei, Sahar ; Baradaran, Behzad ; Nejati-Koshki, Kazem ; Hosseini, Arezoo ; Abdollahpour-Alitappeh, Meghdad ; Ebrahimi-Kalan, Abbas ; Mohammadzadeh, Adel ; Baghbani, Elham

100 Deals associated with Ochromycinone

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB15644

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Phase 2	-	University of Michigan College of Engineering	-
Neoplasms	Phase 2	-	The Ohio State University	-
Neoplasms	Phase 2	-	National Cancer Institute	-
Neoplasms	Phase 2	-	Kochi University of Technology	-

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