bche

BChE HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

AChE BChE MAO-B-IN-1 is a reversible, non-time-dependent inhibitor of AChE, BChE, and MAO-B that crosses the blood-brain barrier, exhibiting inhibitory effects on hAChE, hBChE, and hMAO-B with IC50s of 7.31, 0.56, and 26.1 μM, respectively. [AChE BChE MAO-B-IN-1] had a neuroprotective effect and was not significantly cytotoxic.

AChE BChE-IN-10 is a potent dual inhibitor of AChE and BChE with IC50 values of 0.176, and 0.47 μM, respectively. AChE BChE-IN-10 exhibits good blood brain barrier permeability. AChE BChE-IN-10 can inhibit Aβ-aggregation.

hBChE-IN-2 is a butyrylcholinesterase (BChE) inhibitor and cannabinoid receptor 2 (CB2R) agonist with neuroprotective activity for the study of Alzheimer's disease-like neurological disorders.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

Lupinine is an alkaloid capable of counteracting ethanol anesthesia. Lupinine is an AChE and BChE inhibitor and potential CD69 activator found in species of Loranthus, Calia, and Lupinus. It may also inhibit heparin.

Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

Questin is an antimicrobial agent derived from Aspergillus florescens with an antimicrobial activity profile that inhibits V. harveyi, V. anguillarum, V. cholerae and V. parahemolyticus with MIC values of 31.25 µg mL, 62.5 µg mL, 62.5 µg mL and 125 µg mL, respectively. Questin has good potential to inhibit AChE, BChE and BACE1 and may be used in the development of drugs for the treatment or prevention of Alzheimer's disease.

Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves

Atherosperminine shows cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Atherosperminine shows strong anti-plasmodial activity against Plasmodium falciparum, with the IC50 value of 5.80 uM, it also s

AChE BChE-IN-21 is an antagonist of the histamine H3 receptor, a calcium channel blocker, and an acetylcholinesterase inhibitor. It exhibits neuroprotective activities against H2O2 and Aβ1-40, and can restore cognitive functions in AD mice.

hBChE-IN-4 (compound 40) serves as an effective activator for hCA and an inhibitor for BChE. It demonstrates affinity for various hCA subtypes with affinity constants (KA) of 266 nM for hCA I, 76.9 nM for hCA II, 918 nM for hCA IV, 893 nM for hCA VB, and 98.0 nM for hCA VII. Inhibition concentrations (IC50) for eeAChE and eqBChE are recorded at 72.1 nM and 4.2 nM, respectively. hBChE-IN-4 is non-cytotoxic and has demonstrated potential cognitive enhancement effects. It holds potential for research in neurodegenerative and other neuropsychiatric disorders.

BChE-IN-35 (Azo-9) is an inhibitor of BChE. This compound exhibits dynamic cis trans conformational changes, with the cis isomer preferentially binding to BChE. Additionally, BChE-IN-35 can be utilized in research on Alzheimer's disease (AD).

AChE BChE-IN-22 (compound 7) exhibits competitive inhibition against both AChE and BChE enzymes, with inhibition constants of 28.18 μM and 41.74 μM respectively.

AChE BChE-IN-23 (Compound 6e) is a dual inhibitor of acetylcholinesterase and butyrylcholinesterase, exhibiting IC50 values of 0.91 μM for AChE, 1.19 μM for eqBChE, and 1.01 μM for hBChE. This compound also demonstrates antioxidant properties and inhibits the aggregation of Aβ1-42 and Tau proteins. Moreover, AChE BChE-IN-23 prevents the activation of microglial cells by inhibiting the release of reactive oxygen species and mitochondrial damage. Additionally, it reduces the levels of the NLRP3 inflammasome in human microglial cells and reverses memory impairment in mice induced by scopolamine.

AChE BChE-IN-24 (compound 5k) functions as a neuroprotective agent by inhibiting acetylcholinesterase. It targets both AChE and BChE, demonstrating IC50 values of 16.38 μM and 10.44 μM, respectively.

AChE BChE-IN-25 (Compound 6e) is an orally active inhibitor of hAChE and eqBChE, with IC50 values of 7.9 nM and 0.79 nM, respectively. This compound exhibits antioxidant activity, effective in scavenging free radicals with an IC50 of 22.91 μM. AChE BChE-IN-25 demonstrates neuroprotective effects by reducing mitochondrial and cellular oxidative stress in a Drosophila Alzheimer's model and improves spatial and cognitive memory impairments induced by Scopolamine in mouse models.

BChE-IN-39 (Compound 7c) selectively inhibits butyrylcholinesterase (BChE) with an IC50 of 0.08 μM, while showing an IC50 of 3.98 μM for acetylcholinesterase (AChE) inhibition. Additionally, BChE-IN-39 downregulates GSK-3β expression, thereby inhibiting the excessive phosphorylation of tau protein.

BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.