LC–MS/MS analysis, antioxidant and anticholinergic properties of galanga (Alpinia officinarum Hance) rhizomes

Antioxidant and acetylcholinesterase inhibition properties of novel bromophenol derivatives.

Rosmarinic acid (RA) is a natural polyphenol contained in many aromatic plants with promising biological activities. Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread and intensively studied metalloenzymes present in higher vertebrates. Acetylcholinesterase (AChE, E.C. 3.1.1.7) is intimately associated with the normal neurotransmission by catalysing the hydrolysis of acetylcholine to acetate and choline and acts in combination with butyrylcholinesterase (BChE) to remove acetylcholine from the synaptic cleft. Lactoperoxidase (LPO) is an enzyme involved in fighting pathogenic microorganisms, whereas glutathione S-transferases (GSTs) are dimeric proteins present both in prokaryotic and in eukaryotic organisms and involved in cellular detoxification mechanisms. In the present study, the inhibition effects of rosmarinic acid on tumour-associated carbonic anhydrase IX and XII isoenzymes, AChE, BChE, LPO and GST enzymes were evaluated. Rosmarinic acid inhibited these enzymes with Kis in the range between micromolar to picomolar. The best inhibitory effect of rosmarinic acid was observed against both AChE and BChE.

https://www.tandfonline.com/doi/pdf/10.3109/14756366.2015.1135914

Rosmarinic acid inhibits some metabolic enzymes including glutathione S-transferase, lactoperoxidase, acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase isoenzymes

Caffeic acid phenethyl ester (CAPE) is an active component of honeybee propolis extracts. Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread and intensively studied metalloenzymes present in higher vertebrates including humans as many diverse isoforms. Acetylcholinesterase (AChE) is responsible for acetyl choline (ACh) hydrolysis and plays a fundamental role in nerve impulse transmission by terminating the action of the ACh neurotransmitter at cholinergic synapses and neuromuscular junctions. Butyrylcholinesterase (BChE) is another enzyme abundantly present in the liver and released into blood in a soluble form. Lactoperoxidase (LPO) is an enzyme involved in fighting pathogenic microorganisms whereas glutathione S-transferases (GSTs) are dimeric proteins present both in prokaryotic and eukaryotic organisms and involved in cellular detoxification mechanisms. In the present study, the inhibition effect of CAPE on human carbonic anhydrase (hCA) isoforms I, II, IX, and XII, AChE, BChE, LPO, and GST was evaluated. CAPE inhibited these enzymes with Kis in the range between micromolar to picomolar. The best inhibitory effect was observed against AChE and BChE.

https://www.tandfonline.com/doi/pdf/10.3109/14756366.2015.1094470

The effect of caffeic acid phenethyl ester (CAPE) on metabolic enzymes including acetylcholinesterase, butyrylcholinesterase, glutathione S-transferase, lactoperoxidase, and carbonic anhydrase isoenzymes I, II, IX, and XII.

N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II.

Sulphamides [1] and sulphonamides [2] are importantbiologically active compounds. In the last decades a lot ofsulphamide and sulphonamide drugs have appeared inthe markets. Quinagolide (1), a dopaminergic drug, isan antihyperprolactinemia agent [3]. Compound 2 (JNJ-26990990) has potential use in the treatment of depression,neuropathic and inﬂammatory pains [4]. The sulphonamidedrug sultiame (3) is an anticonvulsant used in the treatmentof epilepsy and West syndrome [5]. Acetazolamide (AZA, 4), adrug alsoknownas carbonicanhydrase (CA) inhibitor,isusedin the treatment of glaucoma [6] and idiopathic intracranialhypertension [7] (Figure 1).CA (E.C.: 4.2.1.1) is a protein that is well suited to serve as amodel in many types of biophysical, bioanalytical andphysical-organic chemical studies as well as for inhibitordrug design studies. This enzyme catalyses the hydration ofcarbon dioxide (CO

Agri Ibrahim

Papers

Novel Sulphamides and Sulphonamides Incorporating the Tetralin Scaffold as Carbonic Anhydrase and Acetylcholine