Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Extracts obtained from 10 trees used in South African traditional medicine were screened for antibacterial, anti-inflammatory (COX-1 and COX-2) and anti-cholinesterase activities and investigated for potential mutagenic effects using the Ames test. Antibacterial activity was detected using the disc-diffusion and micro-dilution assays. The extracts were tested against Gram-positive bacteria: Bacillus subtilis, Staphylococcus aureus, Micrococcus luteus and Gram-negative bacteria: Escherichia coli and Klebsiella pneumoniae. Of the 78 different plant extracts investigated, 80% showed activity against both Gram-positive and Gram-negative bacteria in the disc-diffusion assay. In the micro-dilution assay, 60% of the plant extracts showed minimum inhibitory concentration (MIC) values < or =1.56 mg ml(-1). The lowest MIC value (0.092 mg ml(-1)) was recorded for an ethyl acetate root extract of Acacia sieberiana against Staphylococcus aureus and Escherichia coli. In the anti-inflammatory assay, 70% of the investigated plant extracts (0.25 mg ml(-1)) inhibited both COX-1 and COX-2 activity (>50% and 70% for water and organic solvent extracts, respectively). An ethyl acetate leaf extract of Trichilia dregeana showed selective inhibition of COX-2 (81%). In the acetylcholinesterase inhibitory test, 21% of the plant extracts were active at a concentration < or =1 mg ml(-1) using the micro-dilution assay. The lowest IC(50) value was 0.04 mg ml(-1) obtained with an ethanol bark extract of Combretum kraussii. None of the investigated plants showed any potential mutagenic effects.
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PMID:Antibacterial, anti-inflammatory, anti-cholinesterase and mutagenic effects of extracts obtained from some trees used in South African traditional medicine. 1623 65

New tetrahydro-1H-pyrazolo[3,4-b]quinoline derivatives were designed, synthesized and characterized as dual anticholinestrase and cyclooxygenase-2 inhibitors. The in vitro and in vivo anti-cholinesterase evaluation exhibited promising activities with lower hepatotoxicity for many candidates compared to tacrine as a reference. Furthermore, their anti-inflammatory activity using in vitro (COX-1/COX-2) inhibitory assay demonstrated superior activity to celecoxib with higher selectivity indices for some compounds. In addition, some candidates showed extended anti-inflammatory activity by inhibiting COX-2 protein induction. Besides, in silico docking experiments of the active compounds against hAChE rationalized the observed in vitro AChE inhibitory activity. In conclusion, this work provides an extension of the chemical space of tetrahydro-1H-pyrazolo[3,4-b]quinoline chemotype for the anticholinestrase and anti-inflammatory activity. This would aid to minimize the possible neuroinflammation linked to the pathogenesis of Alzheimer's disease.
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PMID:Synthesis, biological evaluation and modeling of hybrids from tetrahydro-1H-pyrazolo[3,4-b]quinolines as dual cholinestrase and COX-2 inhibitors. 3241 26