Furthermore, bisPMB was more potent at inhibiting CA I, CA II and AChE compared with commercially available inhibitors.
📌 3 Key Takeaways
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Objective & Hypothesis:BisPMB (1,8-(bis- p -methoxyphenyl)-2,3,7-trithiaocta-4-ene 7-oxide) is a synthetic analogue of the natural compound ajoene, which is a bioactive natural product obtained from rearrangement of the unstable and reactive organosulfur compound allicin produced when garlic is freshly crushed.
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Key Findings & Data:In this study, the inhibition effects of E / Z -bisPMB and Z -bisPMB against human carbonic anhydrase isozymes I and II (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were investigated in which E / Z -bisPMB and Z -bisPMB showed similar inhibition profiles against the four enzymes tested, with the IC 50 values ranging from 10.9 to 439.7 nM and the K i values ranging from 5.4 to 195.4 nM.
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Conclusion & Impact:Furthermore, bisPMB was more potent at inhibiting CA I, CA II and AChE compared with commercially available inhibitors.
BisPMB (1,8-(bis- p -methoxyphenyl)-2,3,7-trithiaocta-4-ene 7-oxide) is a synthetic analogue of the natural compound ajoene, which is a bioactive natural product obtained from rearrangement of the unstable and reactive organosulfur compound allicin produced when garlic is freshly crushed. BisPMB has been shown to have superior cancer-cell cytotoxicity compared with ajoene and a modest selectivity towards cancer cells over non-cancerous ones. In this study, the inhibition effects of E / Z -bisPMB and Z -bisPMB against human carbonic anhydrase isozymes I and II (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were investigated in which E / Z -bisPMB and Z -bisPMB showed similar inhibition profiles against the four enzymes tested, with the IC 50 values ranging from 10.9 to 439.7 nM and the K i values ranging from 5.4 to 195.4 nM. Furthermore, bisPMB was more potent at inhibiting CA I, CA II and AChE compared with commercially available inhibitors.
Stellenboom, N. (2019). Inhibition of Carbonic Anhydrase, Acetylcholinesterase and Butyrylcholinesterase by BisPMB, A Synthetic Analogue of Ajoene. Journal of the Turkish Chemical Society Section A: Chemistry, Volume: 6 Issue: 2. https://doi.org/10.18596/jotcsa.484444
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