Bazedoxifene exhibits anti-inflammation and anti-atherosclerotic effects via inhibition of IL-6/IL-6R/STAT3 signaling

IL-6/STAT3 Signaling Promotes Cardiac Dysfunction by Upregulating FUNDC1-Dependent Mitochondria-Associated Endoplasmic Reticulum Membranes Formation in Sepsis Mice

“…In addition, there are a large number of clinical trials targeting IL-6/STAT3 pathway are currently in progress ( 50 , 51 ). Bazedoxifene is the inhibitor of IL-6/gp130 protein-protein interactions and our present studies find that Bazedoxifene can influence IL-6/gp130 interface and then inhibits IL-6/STAT3 signaling pathway in tumor and cardiovascular disease ( 14 , 15 , 52 ). Bazedoxifene has been used in the clinics for osteoporotic bones in postmenopausal women, and our findings may provide new insights into the indications of Bazedoxifene.…”

“…Bazedoxifene has been approved by the Food and Drug Administration for the treatment of female patients with postmenopausal osteoporosis. We have previously reported that Bazedoxifene could inhibit phosphorylation of STAT3 and prevents chronic cardiovascular diseases ( 14 , 15 ). However, the potential effect of Bazedoxifene in acute cardiovascular diseases remains unclear.…”

Network Pharmacology and Molecular Docking Elucidate the Pharmacological Mechanism of the OSTEOWONDER Capsule for Treating Osteoporosis

“…Here, we found that quercetin has been used as an agent for OP by reducing EGFR, HIF1A, and IL6 expression. EGFR, HIF1A, and IL6 have also been demonstrated as the therapeutic targets of OP ( Fayed et al, 2019 ; Luo et al, 2021 ; Xiong et al, 2021 ). Nobiletin, a polymethoxylated flavone, exhibits anti-oxidative, anti-inflammatory, and anti-cancer properties ( Murakami et al, 2000 ; Hagenlocher et al, 2019 ; Feng et al, 2020 ).…”

Bazedoxifene, a Selective Estrogen Receptor Modulator, Promotes Functional Recovery in a Spinal Cord Injury Rat Model

“…For instance, BZA induced significant reductions in TBI-induced proinflammatory cytokines (IL-1β, IL-6, COX-2, and TNF-α) [21]. In addition, BZA effectively downregulated IL-6 via the signal transducer and activator of transcription 3 (STAT3) pathway in an atherosclerosis model [44]. Interestingly, ER-β agonists have shown to inhibit inflammation in both in vivo and in vitro models of inflammatory bowel disease via downregulation of ERK, JAK2 and STAT, suggesting the general role of estrogen in inflammatory process [45].…”