Discovery of 8-prenylnaringenin from hop (<i>Humulus lupulus</i>L.) as a potent monoacylglycerol lipase inhibitor for treatments of neuroinflammation and Alzheimer's disease

Tung, Min‐Che; Fung, Kit-Man; Hsu, H.-C.; Tseng, Tien‐Sheng

doi:10.1039/d1ra05311f

Cited by 11 publications

(7 citation statements)

References 92 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…reversibly inhibited MAGL and reduces neuroinflammation, promising for Alzheimer’s disease. 101 Extracts from Myristica fragrans exhibited anxiolytic and antidepressant effects, with significant MAGL inhibitory activity. 102 …”

Section: Endocannabinoid Systemmentioning

confidence: 99%

“…Through the establishment of the pharmacophore model Phar-MAGL, combined with molecular docking and Ligplot analysis, NP-2/8-PN (IC 50 = 9.5 ± 1.2 μM), NP-5 (IC 50 = 14.5 ± 1.3 μM), and NP-3 (IC 50 = 15.2 ± 1.4 μM) were successfully screened for their promising in vitro inhibitory activities of MAGL. 101 Interestingly, 8-PN also had a positive metamorphic modulatory effect on GABAA that was not mediated through a high-affinity benzodiazepine binding site, and its potential anxiolytic effect could be further investigated. 103 Phenylethanoid glycosides from C. phelypeae 104 and Jewenol A from S. pseudorosmarinus 105 also demonstrated good MAGL inhibitory activity through enzymatic assays and molecular docking.…”

Section: Endocannabinoid Systemmentioning

confidence: 99%

See 1 more Smart Citation

Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs

Zhao,

Liu,

Cai

et al. 2024

DDDT

View full text Add to dashboard Cite

Section: Endocannabinoid Systemmentioning

confidence: 99%

Section: Endocannabinoid Systemmentioning

confidence: 99%

Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs

Zhao,

Liu,

Cai

et al. 2024

DDDT

View full text Add to dashboard Cite

“…copper [154]; iron [155]; zinc [156] Copper [157]; iron [158] Mitochondria and metabolic functions MCL1 [159] ROCK [160], δ-opioid receptor [161] Mutated/misfolded proteins Amyloid-β [162]; β-secretase [163]; γ-secretase [164]; GSK3-β [165]; RAGE [166]; Tau [167] DJ1 [168]; LRRK2 [169]; Pink1 [170]; αsynuclein [171]; CK1δ [172]; CK1δ+GSK3b [173] Neuroinflammation NRLP3 inflammasome [174] Adenosine receptors [175]; cannabinoid receptor 2 [176]; monoacylglycerol lipase [177]; NRLP3 Inflammasome [178]; PPAR [179]; TRPC5 [180] Neuroprotection Apoptosis [181]; ferroptosis [182]; sigma 1 and 2 receptors [183] Apoptosis [184]; autophagy/neuroinflammation [185]; CDNF peptidomimetic [186]; ferroptosis [187]; nurr1 [188]; sigma 1 and 2 receptors [189] Oxidative stress Antioxidants [190]; NRF2 signaling pathway [191] Aldose reductase [192]; NRF2 signaling pathway [193] Synaptic activity AChE [110]; α7nAChR [194]; butyrylcholinesterase…”

Section: Metal Dyshomeostasismentioning

confidence: 99%

Drug Development for Alzheimer’s and Parkinson’s Disease: Where Do We Go Now?

Sequeira,

Benfeito,

Fernandes

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

Neurodegenerative diseases (NDs) are a set of progressive, chronic, and incurable diseases characterized by the gradual loss of neurons, culminating in the decline of cognitive and/or motor functions. Alzheimer’s disease (AD) and Parkinson’s disease (PD) are the most common NDs and represent an enormous burden both in terms of human suffering and economic cost. The available therapies for AD and PD only provide symptomatic and palliative relief for a limited period and are unable to modify the diseases’ progression. Over the last decades, research efforts have been focused on developing new pharmacological treatments for these NDs. However, to date, no breakthrough treatment has been discovered. Hence, the development of disease-modifying drugs able to halt or reverse the progression of NDs remains an unmet clinical need. This review summarizes the major hallmarks of AD and PD and the drugs available for pharmacological treatment. It also sheds light on potential directions that can be pursued to develop new, disease-modifying drugs to treat AD and PD, describing as representative examples some advances in the development of drug candidates targeting oxidative stress and adenosine A2A receptors.

show abstract

“…The study was determined with an inhibitor (NP-2 and/or 8-PN) of hops. 59 Alzheimer's disease (AD) is characterized by neuroinflammation associated with common neuronal death. 60 It has been reported that NPs possess inhibition effects of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), which are important enzymes of AD.…”

Section: Anti-alzheimer Activitymentioning

confidence: 99%

**Major Bioactive Prenylated Flavonoids from Humulus lupulus L., Their Applications in Human Diseases and Structure-Activity Relationships (SAR) – A Review**

Comert Onder,

Kalin,

Sahin

et al. 2023

Pharm Sci

View full text Add to dashboard Cite

In recent years, the incidence of cancers, inflammatory diseases, Alzheimer’s disease, glucose metabolism disorder and diabetes has increased alarmingly which demands more research into the discovery of new drug candidates to treat these human diseases. Main phytochemicals from Humulus lupulus L. (hops) have been demonstrated to have positive impacts on human health, and prenylated flavonoids are one of the major groups of bioactive phytochemicals found in this plant. Thus, this review summarizes the role of major prenylated components in hops in human diseases including cancer, inflammation and viral infections. In silico studies of prenylated bioactive compounds against various drug targets such as histone deactylases (HDACs), sirtuins (SIRTs), and acetylcholinesterase (AChE), and the molecular molecular interactions between protein and ligand have also been included. Furthermore, the structure-activity relationships (SAR) studies on these compounds are highlighted. This review concludes that the prenylated phytochemicals from H. lupulus L., including xanthohumol (XN), isoxanthohumol (IXN), 8-prenylnaringenin (8-PN) and 6-prenylnaringenin (6-PN), have promising roles in human health and may contribute to new drug discovery and development.

show abstract

Discovery of 8-prenylnaringenin from hop (Humulus lupulusL.) as a potent monoacylglycerol lipase inhibitor for treatments of neuroinflammation and Alzheimer's disease

Abstract: Discovery of natural product inhibitors against human monoacylglycerol lipase by pharmacophore-based drug screening, LibDock molecular docking and in vitro biochemical examinations.

Cited by 11 publications

References 92 publications

Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs

Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs

Drug Development for Alzheimer’s and Parkinson’s Disease: Where Do We Go Now?

**Major Bioactive Prenylated Flavonoids from Humulus lupulus L., Their Applications in Human Diseases and Structure-Activity Relationships (SAR) – A Review**

Contact Info

Product

Resources

About