Bazedoxifene 抑制人非小细胞肺癌细胞的细胞活力、集落形成活性和细胞迁移,并提高紫杉醇和吉西他滨的治疗效果。
Bazedoxifene Inhibits Cell Viability, Colony-Forming Activity, and Cell Migration in Human Non-Small Cell Lung Cancer Cells and Improves the Treatment Efficacy of Paclitaxel and Gemcitabine.
发表日期:2024 Aug
作者:
Yaochen Huang, Jiayuh Lin, Xiangning Fu, Lequn Li, Shenging Fu
来源:
PHARMACOLOGY & THERAPEUTICS
摘要:
Bazedoxifene 是第三代选择性雌激素受体调节剂,通过抑制 IL6 诱导的 GP130 同二聚化来抑制 IL6/IL6R/GP130 信号通路。考虑到IL6/IL6R/GP130信号通路在肿瘤发生和转移中的重要作用,巴多昔芬被认为具有抗肿瘤作用,该作用已在乳腺癌和胰腺癌中得到初步证实,但尚未在非小细胞肺癌中进行研究(非小细胞肺癌)。本研究旨在评估巴多昔芬在 NSCLC 中的抗肿瘤作用。采用 A549 和 H1299 NSCLC 细胞系并暴露于不同浓度的巴多昔芬、紫杉醇、吉西他滨及其组合,进行细胞活力、集落形成和伤口愈合测定,以证明MTT 细胞活力、集落形成和伤口愈合测定表明,巴多昔芬能够以剂量依赖性方式抑制细胞活力、集落形成和细胞迁移。此外,巴多昔芬能够与紫杉醇或吉西他滨协同作用,抑制细胞活力、集落形成和细胞迁移。这项研究证明了巴多昔芬潜在的抗肿瘤作用及其提高紫杉醇和吉西他滨治疗效果的能力。© 2024作者。约翰·威利出版的《临床呼吸杂志》
Bazedoxifene is a third-generation selective estrogen receptor modulator that inhibits the IL6/IL6R/GP130 signaling pathway by inhibiting IL6-induced homodimerization of GP130. Considering that the IL6/IL6R/GP130 signaling pathway is important in tumorigenesis and metastasis, bazedoxifene is thought to have an antitumor effect, which has been proven preliminarily in breast cancer and pancreatic cancer but has not yet been studied in non-small cell lung cancer (NSCLC). This study is aimed at evaluating the antitumor effect of bazedoxifene in NSCLC.A549 and H1299 NSCLC cell lines were employed and exposed to various concentrations of bazedoxifene, paclitaxel, gemcitabine, and their combinations for cell viability, colony formation, and wound healing assays to demonstrate the antitumor effect of bazedoxifene with or without paclitaxel or gemcitabine.MTT cell viability, colony formation, and wound healing assays showed that bazedoxifene was capable of inhibiting cell viability, colony formation, and cell migration in a dose-dependent manner. In addition, bazedoxifene was capable of working with paclitaxel or gemcitabine synergistically to inhibit cell viability, colony formation, and cell migration.This study demonstrated the potential antitumor effect of bazedoxifene and its ability to improve the treatment efficacy of paclitaxel and gemcitabine.© 2024 The Author(s). The Clinical Respiratory Journal published by John Wiley & Sons Ltd.