BuChE-IN-2

BuChE-IN-2 is an excellent inhibitor of butylcholinesterase (BuChE) with IC50 values of 1.28 μM for BuChE and 0.67 μM for NO. It inhibits Aβ aggregation, ROS formation, and Cu2+ chelation, shows proper blood-brain barrier (BBB) penetration, and is suitable for Alzheimer's disease research.

AChE/BuChE-IN-2 (Compound 5f) is an orally active inhibitor of AChE and BuChE with IC50 values of 0.72 μM and 0.16 μM, respectively, and can cross the BBB. AChE/BuChE-IN-2 shows potent inhibition of self-induced β-amyloid (Aβ) aggregation with an IC50 of 62.52 μM and demonstrates non-competitive inhibition with AChE [1].

AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent inhibitor of AChE, BuChE, and hu MAO-B, with respective IC50 values of 5.3 μM, 12.4 μM, and 1.9±0.08 μM, indicating good in vitro blood-brain barrier (BBB) permeability. It effectively reduces excessive AChE and BuChE levels associated with Alzheimer's disease (AD) and holds potential for anti-Alzheimer's research [1].

BuChE-IN-20 is a selective hBuChE inhibitor (IC50= 0.13 μM) with the ability to cross the blood-brain barrier (BBB). This compound, a derivative of L-Tryptophan, exhibits neuroprotective effects by inhibiting nitric oxide (NO) production and reducing reactive oxygen species (ROS) levels. It effectively suppresses the self-aggregation of amyloid-beta (Aβ) peptides and is applicable in Alzheimer's disease research.

BuChE-IN-21 (compound SXF3) is a potent and selective inhibitor of BuChE, demonstrating inhibitory effects on eqBuChE and hBuChE with IC50 values of 0.05 and 0.04 μM, respectively. Additionally, BuChE-IN-21 exhibits significant anti-inflammatory activity.

AChE/BuChE-IN-1, a selective butyrylcholinesterase (BuChE) inhibitor derived from chrysin, exhibits a potent efficacy with an IC50 of 0.48 μM against BuChE and a lesser inhibitory effect on acetylcholinesterase (AChE) with an IC50 of 7.16 μM. It demonstrates significant hydroxyl radical (·OH) scavenging activity, achieving an IC50 of 0.1674 μM, and effectively inhibits reactive oxygen species (ROS) and Aβ 1-42 aggregation, including self-aggregation, copper (Cu 2+)-induced, and AChE-induced aggregation. Characterized by high blood-brain barrier (BBB) permeability, bioavailability, and low cellular toxicity, AChE/BuChE-IN-1 holds promising potential for Alzheimer's disease (AD) research.

Feralolide, a dihydroisocoumarin from the methanolic extract of aloe vera resin, functions as a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 55 μg/mL and 52 μg/mL, respectively. It exhibits antioxidant properties, effectively inhibiting 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS). Research suggests feralolide's potential in studying cognitive disorders, including Alzheimer's disease, for its memory restoration and enhancement capabilities [1].