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Effects of tetramethylpyrazine treatment in a rat model of spinal cord injury: A systematic review and meta-analysis

Li G, Sng KS, Shu B, Wang YJ, Yao M, Cui XJ

Eur J Pharmacol, 2023 Apr 15;945:175524.
PMID: 36803629 DOI: 10.1016/j.ejphar.2023.175524

Spinal cord injury (SCI) is a serious disabling condition that leads to the loss of motor, sensory, and excretory functions, seriously affecting the quality of life of patients and imposing a heavy burden on the patient's family and society. There is currently a lack of effective treatments for SCI. However, a large number of experimental studies have shown beneficial effects of tetramethylpyrazine (TMP). We performed a meta-analysis to systematically evaluate the effects of TMP on neurological and motor function recovery in rats with acute SCI. English (PubMed, Web of Science, and EMbase) and Chinese (CNKI, Wanfang, VIP, and CBM) databases were searched for literature related to TMP treatment in rats with SCI published until October 2022. Two researchers independently read the included studies, extracted the data, and evaluated their quality. A total of 29 studies were included, and a risk of bias assessment revealed that the methodological quality of the included studies was low. The results of the meta-analysis showed that the Basso, Beattie, and Bresnahan (BBB; n = 429, pooled mean difference [MD] = 3.44, 95% confidence interval [CI] = 2.67 to 4.22, p

Matched MeSH terms: Pyrazines/pharmacology
In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase

Taha M, Ismail NH, Imran S, Rahim F, Wadood A, Al Muqarrabun LM, et al.

Bioorg Chem, 2016 10;68:80-9.
PMID: 27474803 DOI: 10.1016/j.bioorg.2016.07.010

Thymidine phosphorylase (TP) is up regulated in wide variety of solid tumors and therefore presents a remarkable target for drug discovery in cancer. A novel class of extremely potent TPase inhibitors based on benzopyrazine (1-28) has been developed and evaluated against thymidine phosphorylase enzyme. Out of these twenty-eight analogs eleven (11) compounds 1, 4, 14, 15, 16, 17, 18, 19, 20, 24 and 28 showed potent thymidine phosphorylase inhibitory potentials with IC50 values ranged between 3.20±0.30 and 37.60±1.15μM when compared with the standard 7-Deazaxanthine (IC50=38.68±4.42μM). Structure-activity relationship was established and molecular docking studies were performed to determine the binding interactions of these newly synthesized compounds. Current studies have revealed that these compounds established stronger hydrogen bonding networks with active site residues as compare to the standard compound 7DX.

Matched MeSH terms: Pyrazines/pharmacology*
Fulltext Pharmacophore modelling of vanillin derivatives, favipiravir, chloroquine, hydroxychloroquine, monolaurin and tetrodotoxin as MPro inhibitors of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2)

Law WY, Asaruddin MR, Bhawani SA, Mohamad S

BMC Res Notes, 2020 Nov 11;13(1):527.
PMID: 33176880 DOI: 10.1186/s13104-020-05379-6

OBJECTIVES: The aim of this study was to use Ligand-based pharmacophore modelling approach for four established antiviral drugs, namely remdesivir, lopinavir, ritonavir and hydroxychloroquine for COVID-19 inhibitors as training sets. In this study Twenty vanillin derivatives together with monolaurin and tetrodotoxin were used as test sets to evaluate as potential SARS-CoV-2 inhibitors. The Structure-based pharmacophore modelling approach was also performed using 5RE6, 5REX and 5RFZ in order to analyse the binding site and ligand-protein complex interactions.
RESULTS: The pharmacophore modelling mode of 5RE6 displayed two Hydrogen Bond Acceptors (HBA) and one Hydrophobic (HY) interaction. Besides, the pharmacophore model of 5REX showed two HBA and two HY interactions. Finally, the pharmacophore model of 5RFZ showed three HBA and one HY interaction. Based on ligand-based approach, 20 Schiff-based vanillin derivatives, showed strong MPro inhibition activity. This was due to their good alignment and common features to PDB-5RE6. Similarly, monolaurin and tetrodotoxin displayed some significant activity against SARS-CoV-2. From structure-based approach, vanillin derivatives (1) to (12) displayed some potent MPro inhibition against SARS-CoV-2. Favipiravir, chloroquine and hydroxychloroquine also showed some significant MPro inhibition.

Matched MeSH terms: Pyrazines/pharmacology

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