I found the field of Pharmacology & Pharmacy; Chemistry very interesting. Saw the article Synthesis and biological evaluation of chalcone derivatives as neuroprotective agents against glutamate-induced HT22 mouse hippocampal neuronal cell death published in 2020.0. Category: indole-building-block, Reprint Addresses Lee, JW (corresponding author), Korea Inst Sci & Technol KIST, Nat Prod Res Ctr, 679 Saimdang Ro, Kangnung 25451, Gangwon Do, South Korea.; Lee, JW (corresponding author), Korea Inst Sci & Technol KIST, Convergent Res Ctr Diag Treatment & Care Syst Dem, Seoul 02792, South Korea.; Kim, DW (corresponding author), Gangneung Wonju Natl Univ GWNU, Coll Dent, Dept Biochem & Mol Biol, Kangnung 25457, South Korea.; Lee, JW (corresponding author), Univ Sci & Technol UST, Div Biomed Sci & Technol, Daejun 34113, South Korea.. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde
Seventeen chalcone analogues were synthesized from 7-methoxy-3,4-dihydronaphthalen1(2H)-one and various aromatic aldehydes under basic conditions and their therapeutic properties were studied in mouse hippocampal cell line HT-22 against neuronal cell death induced by glutamate. From this study, we selected an analogue C01 as a active compound which showed significantly high neuroprotection. This compound inhibited Ca2+ influx and reactive oxygen species (ROS) accumulation inside cells. The glutamate-induced cell death was analyzed by flow cytometry and it showed that C01 significantly reduced apoptotic or dead cell induced by 5 mM glutamate. Western blot analysis indicates that glutamate-mediated activation of MAPKs were inhibited by compound C01 treatment. In addition, the C01enhanced Bcl-2 and decreased Bax, the anti and pro apoptotic proteins respectively. Further analysis showed that, C01 prevented the nuclear translocation of AIF (apoptosis inducing factor) and inhibited neuronal cell death. Taken together, compound C01 treatment resulted in decreased neurotoxicity induced by 5 mM of glutamate. Our finding confirmed that compound C01 has neuro-therapeutic potential against glutamate-mediated neurotoxicity.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles