CRAF inhibitors(C-Raf kinase inhibitors), MEK1 inhibitors(Dual specificity mitogen-activated protein kinase kinase 1 inhibitors), MEK2 inhibitors(Dual specificity mitogen-activated protein kinase kinase 2 inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersSkin and Musculoskeletal Diseases

Active Indication

Colorectal CancerMelanoma

Inactive Indication-

Originator Organization

Zhengzhou University

Active Organization

Zhengzhou University

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with Erianin

100 Translational Medicine associated with Erianin

100 Patents (Medical) associated with Erianin

Literatures (Medical) associated with Erianin

01 Apr 2025·Environmental Toxicology

RETRACTION: Erianin Suppressed Lung Cancer Stemness and Chemotherapeutic Sensitivity via Triggering Ferroptosis

Article

RETRACTION: J. Lv, Z. Wang, and H. Liu, “Erianin Suppressed Lung Cancer Stemness and Chemotherapeutic Sensitivity via Triggering Ferroptosis,” Environmental Toxicology 39, no. 2 (2024): 479‐486, https://doi-org.libproxy1.nus.edu.sg/10.1002/tox.23832.The above article, published online on 20 May 2023, in Wiley Online Library (http://onlinelibrary.wiley.com.libproxy1.nus.edu.sg/), has been retracted by agreement between the journal Editor‐in‐Chief, Christyn Bailey; and Wiley Periodicals LLC. Following an investigation by the publisher, the parties have concluded that this article was accepted solely on the basis of a compromised peer review process. Therefore, the article must be retracted.

01 Mar 2025·Journal of Advanced Research

Erianin serves as an NFATc1 inhibitor to prevent breast cancer-induced osteoclastogenesis and bone destruction

Article

Author: Dai, Wenqi ; Li, Ruopeng ; He, Weili ; Zheng, Jiehuang ; Chen, Fengsheng ; Liang, Qinghe ; Tan, Yanhui ; Li, Xiaojuan ; Chen, Yan ; Li, Lihong ; Chen, Ziye

INTRODUCTIONBreast cancer-related bone metastasis can lead to skeletal-related events (SREs), which decrease patient quality of life. Inhibition of osteoclastogenesis is a key treatment for SREs; however, the availability of clinical drugs remains limited, and all existing ones disrupt physiological bone formation, while exhibiting no effect on patient survival time.OBJECTIVESThis study aimed to identify a novel osteoclast inhibitor for the treatment of breast cancer-induced SREs.METHODSThe MDA-MB-231 breast cancer cell-induced bone loss model was used to investigate the therapeutic effects of erianin in vivo. Then, we evaluated the inhibitory effects of erianin on osteoclastogenesis and signalling in bone marrow-derived macrophages (BMMs) induced by conditioned medium from MDA-MB-231 breast cancer cells (231 CM) and receptor activator of nuclear factor-κB ligand (RANKL) in vitro. Next, a Cellular Thermal Shift Assay and siRNA-mediate knockdown were performed, to investigate the target of erianin during osteoclast formation. The effects of erianin on human osteoclastogenesis were evaluated using CD14⁺ monocytes obtained from patients with breast cancer.RESULTSErianin effectively improved breast cancer cells-induced bone destruction at doses of 2 and 20 mg/kg/day in vivo, while suppressing osteoclastogenesis and the upregulation of SRC-NFATc1, INTEGRIN β3-MMP9 signals induced by 231 CM and RANKL in vitro. Furthermore, erianin interacted with NFATc1 but not SRC, and Nfatc1 knockdown eliminated the inhibitory effects of erianin on osteoclastogenesis. Notably, lower expression of NFATc1 positively correlated with longer survival in patients with cancer and a high risk of bone metastasis. We further revealed that 62.5-250 nM erianin suppresses NFATc1 and excessive osteoclastogenesis in CD14⁺ monocytes from patients with breast cancer.CONCLUSIONErianin acts as an NFATc1 inhibitor that attenuates breast cancer-induced osteoclastogenesis and bone destruction.

01 Mar 2025·European Journal of Pharmacology

Erianin alleviates autoimmune myocarditis by suppressing the M1 polarization of macrophages via the NF-κB/NLRP3 signaling pathway

Article

Author: Mao, Yuyuan ; Liu, Wenhu ; Wang, Yan ; Hu, Jing ; Gan, Ting ; Wang, Ya ; Li, Han ; Wang, Zhaohui

BACKGROUNDMyocarditis tends to lead to a poor prognosis, but there are no satisfactory preventive or therapeutic strategies. Erianin, a natural benzene compound, has been found to have antioxidant and anti-inflammatory effects. However, the effects of erianin on myocarditis remain unclear. This study aimed to investigate the effects of erianin on myocarditis and the involved mechanisms.METHODSWe developed a mouse model of experimental autoimmune myocarditis (EAM) and assessed the effects of erianin using echocardiography and pathological staining. In vitro experiments, flow cytometry, immunofluorescence and western blotting were performed to determine whether erianin inhibits macrophage activation.RESULTSErianin ameliorated cardiac fibrosis and cardiac dysfunction and reduced the percentage of M1-type macrophages and the secretion of inflammatory factors. Mechanistically, erianin inhibits the activation of the NLRP3 inflammasome by inhibiting the NF-κB pathway.CONCLUSIONErianin could be a natural therapeutic drug for EAM by inhibiting NLRP3 activation and M1 macrophage-mediated inflammation through the IκBα/NF-κB pathway.

100 Deals associated with Erianin

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Preclinical	China	Zhengzhou University	06 Mar 2023
Melanoma	Preclinical	China	Zhengzhou University	06 Mar 2023

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