Role of the carbonyl group of local anesthetics in their anesthetic effect

1972 ◽  
Vol 73 (5) ◽  
pp. 553-556
Author(s):  
V. M. Belobrov ◽  
I. V. Komissarov ◽  
L. E. Makarova ◽  
N. Z. Rudenko ◽  
E. V. Titov
Keyword(s):  
Carbonyl Group ◽  
Local Anesthetics ◽  
Anesthetic Effect

scholarly journals Local anesthetics impair the growth and self-renewal of glioblastoma stem cells by inhibiting ZDHHC15-mediated GP130 palmitoylation

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Xiaoqing Fan ◽  
Haoran Yang ◽  
Chenggang Zhao ◽  
Lizhu Hu ◽  
Delong Wang ◽  
...  
Keyword(s):  
Stem Cells ◽  
Western Blot ◽  
Local Anesthetics ◽  
Molecular Mechanisms ◽  
Biological Activities ◽  
Xenograft Model ◽  
Cell Counting ◽  
Migration And Invasion ◽  
Self Renewal

Abstract Background A large number of preclinical studies have shown that local anesthetics have a direct inhibitory effect on tumor biological activities, including cell survival, proliferation, migration, and invasion. There are few studies on the role of local anesthetics in cancer stem cells. This study aimed to determine the possible role of local anesthetics in glioblastoma stem cell (GSC) self-renewal and the underlying molecular mechanisms. Methods The effects of local anesthetics in GSCs were investigated through in vitro and in vivo assays (i.e., Cell Counting Kit 8, spheroidal formation assay, double immunofluorescence, western blot, and xenograft model). The acyl-biotin exchange method (ABE) assay was identified proteins that are S-acylated by zinc finger Asp-His-His-Cys-type palmitoyltransferase 15 (ZDHHC15). Western blot, co-immunoprecipitation, and liquid chromatograph mass spectrometer-mass spectrometry assays were used to explore the mechanisms of ZDHHC15 in effects of local anesthetics in GSCs. Results In this study, we identified a novel mechanism through which local anesthetics can damage the malignant phenotype of glioma. We found that local anesthetics prilocaine, lidocaine, procaine, and ropivacaine can impair the survival and self-renewal of GSCs, especially the classic glioblastoma subtype. These findings suggest that local anesthetics may weaken ZDHHC15 transcripts and decrease GP130 palmitoylation levels and membrane localization, thus inhibiting the activation of IL-6/STAT3 signaling. Conclusions In conclusion, our work emphasizes that ZDHHC15 is a candidate therapeutic target, and local anesthetics are potential therapeutic options for glioblastoma.

scholarly journals Correlation between the increased release of catecholamines evoked by local anesthetics and their analgesic and adverse effects: Role of K + channel inhibition

2016 ◽  
Vol 124 ◽  
pp. 21-26 ◽  
Author(s):  
Carmen Sircuta ◽  
Alexandra Lazar ◽  
Leonard Azamfirei ◽  
Mária Baranyi ◽  
E. Sylvester Vizi ◽  
...  
Keyword(s):  
Adverse Effects ◽  
Local Anesthetics ◽  
K Channel ◽  
Channel Inhibition
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