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/10.1002/tox.23832.The above article, published online on 20 May 2023, in Wiley Online Library (http://onlinelibrary.wiley.com/), has been retracted by agreement between the journal Editor‐in‐Chief, Christyn Bailey; and Wiley Periodicals LLC.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.

2025-03-01·Journal of Advanced Research

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

Article

作者: 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.

2025-03-01·European Journal of Pharmacology

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

Article

作者: 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.

项与 Erianin 相关的新闻（医药）

2023-03-22

·生物谷

双重靶向CRAF和MEK1/2为黑色素瘤和结肠癌症提供了一种有希望的治疗靶点

RAS-RAF-MEK-ERK信号传导级联（促分裂活化蛋白激酶途径）在调节细胞生长、分化和存活方面发挥着重要作用。然而，在许多携带RAS或RAF突变的肿瘤中，该途径经常被组成性激活。 RAS-RAF-MEK-ERK信号传导级联（促分裂活化蛋白激酶途径）在调节细胞生长、分化和存活方面发挥着重要作用。然而，在许多携带RAS或RAF突变的肿瘤中，该途径经常被组成性激活。据统计，KRAS突变发生在40%的结直肠癌和35%的非小细胞肺癌（NSCLC）中。此外，近20%的恶性黑色素瘤存在NRAS突变。RAF V600E突变发生在66%的皮肤黑色素瘤和25%的结直肠癌中。通常，没有B/CRAF激酶的空间激活和二聚化的BRAF V600E/K突变可以引起MAPK信号通路的持续组成型激活，而不依赖于RAS的启动。图片来源：https://doi.org/10.1038/s41392-023-01329-3 近日，来自郑州大学的研究者们在Signal Transduction and Targeted Therapy杂志上发表了题为“Erianin suppresses constitutive activation of MAPK signaling pathway by inhibition of CRAF and MEK1/2”的文章，该研究通过CRAF和MEK1/2的双重靶向性，为BRAF V600E或RAS突变黑色素瘤和结肠癌症提供了一种有希望的先导化合物。 RAS-RAF-MEK-ERK信号通路（MAPK通路）的组成性激活经常发生在许多携带RAS或RAF致癌突变的癌症中。由于单一使用BRAF或MEK抑制剂诱导的反常激活，双靶点RAF和MEK治疗被认为是一种有前途的策略。在这项工作中，研究者评估了erianin是一种新的CRAF和MEK1/2激酶抑制剂，从而抑制由BRAF V600E或RAS突变诱导的MAPK信号通路的组成型激活。KinaseProfiler酶谱分析、表面等离子体共振（SPR）、等温滴定量热法（ITC）、细胞热位移分析、计算对接和分子动力学模拟用于筛选和鉴定Eranin与CRAF和MEK1/2的结合。研究了激酶测定法、发光ADP检测法和酶动力学测定法，以确定MAPK在CRAF和MEK1/2激酶活性中的效率。值得注意的是，erinin通过抑制MEK1/2和CRAF而非BRAF激酶活性来抑制BRAF V600E或RAS突变黑色素瘤和结直肠癌细胞。此外，erinin在体内可减轻黑色素瘤和癌症。该模型描述了在BRAF V600E或RAS突变癌症中，MAPK蛋白抑制MAPK信号通路的组成型激活图片来源：https://doi.org/10.1038/s41392-023-01329-3 总之，erianin是CRAF和MEK1/2激酶的新型双重抑制剂，并抑制MAPK信号通路的组成型激活。基于这项研究，它在体内外显示了对各种BRAF V600E或KRAS突变癌症的活性，包括黑色素瘤和癌症。重要的是，本研究为黑色素瘤和结直肠癌的临床治疗提供了一种有前途的先导化合物，需要进一步的临床开发。（生物谷 Bioon.com）参考文献 Penglei Wang et al. Erianin suppresses constitutive activation of MAPK signaling pathway by inhibition of CRAF and MEK1/2. Signal Transduct Target Ther. 2023 Mar 6;8(1):96. doi: 10.1038/s41392-023-01329-3.