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 Jul 2023·European Journal of Pharmacology

Erianin alleviated liver steatosis by enhancing Nrf2-mediated VE-cadherin expression in vascular endothelium

Article

Author: Lu, Bin ; Ouyang, Hao ; Wei, Mengjuan ; Huang, Zhenlin ; Xu, Hong ; Li, Jian ; Wang, Zhengtao ; Ji, Lili ; Zhang, Tianyu

Non-alcoholic fatty liver disease (NAFLD) is emerging as the most common chronic liver disease and is closely associated with metabolic syndrome. Endothelial dysfunction was involved in many metabolic diseases, but the concrete participation of hepatic vascular endothelial dysfunction in liver steatosis that is an early stage of NAFLD is still unclear. In this study, the formation of liver steatosis and the elevation of serum insulin content were observed accompanying with the decreased vascular endothelial cadherin (VE-cadherin) expression in hepatic vessels from db/db mice, Goto-Kakizaki (GK) and high-fat diet (HFD)-fed rats. Liver steatosis was obviously enhanced in mice after the application of VE-cadherin neutralizing antibody. In vitro results showed that insulin decreased VE-cadherin expression and caused endothelial barrier breakdown. Furthermore, the alteration of VE-cadherin expression was found to be positively related with the transcriptional activation of nuclear erythroid 2-related factor 2 (Nrf2), and chromatin immunoprecipitation (ChIP) assay displayed that Nrf2 could directly regulate VE-cadherin expression. Insulin reduced Nrf2 activation by decreasing sequestosome-1 (p62/SQSTM1) expression downstream of insulin receptor. Moreover, the p300-mediated Nrf2 acetylation was weakened by enhancing the competitive binding of transcription factor GATA-binding protein 4 (GATA4) to p300. Finally, we found that erianin, a natural compound, could promote VE-cadherin expression by inducing Nrf2 activation, thereby alleviating liver steatosis in GK rats. Our results suggest that hepatic vascular endothelial dysfunction owing to the VE-cadherin deficiency dependent on the reduced Nrf2 activation promoted liver steatosis, and erianin alleviated liver steatosis through enhancing Nrf2-mediated VE-cadherin expression.

Frontiers in Plant Science

Integrated metabolomic and transcriptomic analyses of Dendrobium chrysotoxum and D. thyrsiflorum reveal the biosynthetic pathway from gigantol to erianin

Article

Author: Ma, Yao ; Xie, Lihang ; Chen, Qiuying ; Cheng, Najing ; Liu, Kangdong ; Zhang, Yue ; Zhang, Yueteng

Erianin is one of the most representative bibenzyls with significant inhibitory activity against a wide range of tumor cells. However, the low erianin level in natural materials has severely inhibited its further development in health care. Our aim was to uncover the erianin biosynthetic pathway to lay the foundation for promoting its production. Firstly, we screened and obtained two Dendrobium species (Dendrobium thyrsiflorum stems with lower erianin content and D. chrysotoxum stems with higher erianin content), belonging to the same Dendrobium section (Chrysotoxae). A systematic analysis of bibenzyl structure and content in two stems revealed that gigantol might be an erianin biosynthetic intermediate, which was verified by introducing deuterium-labeled gigantol. Chemical structure analyses indicated that gigantol was modified by two kinds of enzymes (hydroxylases and O-methyltransferases), leading to erianin synthesis. Up-regulated hydroxylases and O-methyltransferases (OMTs) were screened out and were performed by molecular docking simulation experiments. We propose a rational biosynthetic pathway from gigantol to erianin, as well as relevant enzymes involved in the process. Our findings should significantly contribute to comprehensive resolution of the erianin biosynthetic pathway, promote its large-scale industrial production as well as contribute to biosynthesis studies of other bibenzyls.

100 Deals associated with Erianin

R&D Status

10 top R&D records.

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

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