BAPTA-AM is a well-known membrane-permeable Ca2+ chelator, to prevent cell injury by allaying the intracellular calcium overload[1].
The IC50 value of BAPTA-AM was investigated using a MTT assay. The IC50 value of BAPTA-AM was determined as 13.6 μM in the breast cancer 4T1 cell line.In order to determine the combined effects of bortezomib and BAPTA-AM,The cells were treated with various doses of bortezomib (1 nM and 10 nM) and BAPTA-AM (0.5 and 5 μM). The combination of 10 nM bortezomib + 5 μM BAPTA-AM was more effective compared with monotherapies (10 nM bortezomib or 5 μM BAPTA-AM alone)[2]
The calcium chelator BAPTA-AM was used to test the efficacy of calcium chelator treatment in iron overload-induced chondrocyte damage. BAPTA-AM significantly reduced iron levels in chondrocytes and inhibited iron overload-induced cell apoptosis and the expression of MMPs, thus providing new insights into the treatment of iron overload-induced diseases[3]
Restoring IP3R and Ca2+ homeostasis by pretreatment with BAPTA-AM could alleviate HTV-induced lung injury and inflammation. Assessment of the dose-dependent effects of BAPTA-AM revealed that 2.5mg/kg was sufficient to prevent the excessive ER Ca2+ release induced by HTV. The results were assessed by histopathology, W/D ratio, BALF protein levels, the number of infiltrating cells and the levels of the inflammatory cytokines IL-1β, IL-6 and TNF-α[4]
References:
[1]. Fu Z, Fan Q, et al. Elimination of Intracellular Calcium Overload by BAPTA-AM-Loaded Liposomes: A Promising Therapeutic Agent for Acute Liver Failure. ACS Appl Mater Interfaces. 2019 Oct 30;11(43):39574-39585.
[2]. Yerlikaya A, Erdo?an E, et al. A novel combination treatment for breast cancer cells involving BAPTA-AM and proteasome inhibitor bortezomib. Oncol Lett. 2016 Jul;12(1):323-330.
[3]. Jing X, Wang Q, et al. Calcium chelator BAPTA AM protects against iron overload induced chondrocyte mitochondrial dysfunction and cartilage degeneration. Int J Mol Med. 2021 Oct;48(4):196.
[4]. Ye L, Zeng Q, et al.Inhibition of IP3R/Ca2+ Dysregulation Protects Mice From Ventilator-Induced Lung Injury via Endoplasmic Reticulum and Mitochondrial Pathways. Front Immunol. 2021 Sep 15;12:729094.
BAPTA-AM 是一种众所周知的可透过膜的 Ca2+ 螯合剂，可通过减轻细胞内钙过载来防止细胞损伤[1]。
使用 MTT 测定法研究了 BAPTA-AM 的 IC50 值。 BAPTA-AM 在乳腺癌 4T1 细胞系中的 IC50 值为 13.6 μM。硼替佐米（1 nM 和 10 nM）和 BAPTA-AM（0.5 和 5 μM）。与单一疗法（单独使用 10 nM 硼替佐米或 5 μM BAPTA-AM）相比，10 nM 硼替佐米 + 5 μM BAPTA-AM 的组合更有效[2]
钙螯合剂 BAPTA-AM 用于测试钙螯合剂治疗铁过载诱导的软骨细胞损伤的疗效。 BAPTA-AM显着降低软骨细胞铁含量，抑制铁超载诱导的细胞凋亡和MMPs的表达，为铁超载相关疾病的治疗提供新思路[3]
通过 BAPTA-AM 预处理恢复 IP3R 和 Ca2+ 稳态可减轻 HTV 引起的肺损伤和炎症。评估 BAPTA-AM 的剂量依赖性效应表明，2.5mg/kg 足以防止 HTV 诱导的 ER Ca2+ 过度释放。通过组织病理学、W/D 比值、BALF 蛋白水平、浸润细胞数量和炎性细胞因子 IL-1β、IL-6 和 TNF-α 水平评估结果[4]