Tryptamine: A privileged scaffold for the management of Alzheimer's disease DOI
Yash Pal Singh, Harish Kumar

Drug Development Research, Год журнала: 2023, Номер 84(8), С. 1578 - 1594

Опубликована: Сен. 7, 2023

Abstract Alzheimer's disease (AD) is a chronic and irreversible neurodegenerative associated with aging. It characterized by the progressive loss of memory other cognitive functions. Although exact etiology AD not well explored, several factors, such as deposition amyloid‐β (Aβ) plaques, hyperphosphorylation tau protein, presence low levels acetylcholine, generation oxidative stress, are key mediators in progression AD. Currently, clinical treatment options for limited based on cholinesterase (ChE) inhibitors (e.g., donepezil, rivastigmine, galantamine), N ‐methyl‐ d ‐aspartic acid receptor antagonists memantine), recently approved Aβ modulator aducanumab). Tryptamine (2‐(1 H ‐indol‐3‐yl)ethan‐1‐amine) small molecule that contains an indole nucleus ethylamine side chain. also active metabolite tryptophan. possesses wide range biological activities related to disorders, ChE inhibition, aggregation antioxidant effects, monoamine‐oxidase neuroprotection. Several tryptamine‐based hybrid analogs currently being investigated multifunctional agents development novel hybrids treatment. Thus, this review article aims provide in‐depth insights into research progress strategies designing used therapy.

Язык: Английский

Therapeutic Potential of Phenolic Compounds in Medicinal Plants—Natural Health Products for Human Health DOI Creative Commons
Wenli Sun, Mohamad Hesam Shahrajabian

Molecules, Год журнала: 2023, Номер 28(4), С. 1845 - 1845

Опубликована: Фев. 15, 2023

Phenolic compounds and flavonoids are potential substitutes for bioactive agents in pharmaceutical medicinal sections to promote human health prevent cure different diseases. The most common found nature anthocyanins, flavones, flavanones, flavonols, flavanonols, isoflavones, other sub-classes. impacts of plant phenolics on promoting diseases curing preventing antioxidant effects, antibacterial impacts, cardioprotective anticancer immune system promoting, anti-inflammatory skin protective effects from UV radiation. This work aims provide an overview phenolic as important sources medical application according recently published studies, well some interesting directions future research. keyword searches flavonoids, phenolics, tannins, coumarins, lignans, quinones, xanthones, curcuminoids, stilbenes, cucurmin, phenylethanoids, secoiridoids were performed by using Web Science, Scopus, Google scholar, PubMed. acids contain a carboxylic acid group addition the basic structure mainly divided into hydroxybenzoic hydroxycinnamic acids. Hydroxybenzoic based C6-C1 skeleton often bound small organic acids, glycosyl moieties, or cell structural components. Common include gallic, syringic, protocatechuic, p-hydroxybenzoic, vanillic, gentistic, salicylic Hydroxycinnamic C6-C3 also molecules such quinic glucose. main caffeic, p-coumaric, ferulic, sinapic

Язык: Английский

Процитировано

350
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress DOI
Zhipei Sang, Keren Wang, Jianghong Dong

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2022, Номер 238, С. 114464 - 114464

Опубликована: Май 20, 2022

Язык: Английский

Процитировано

90
Recent Advances in the Neuroprotective Properties of Ferulic Acid in Alzheimer’s Disease: A Narrative Review DOI Open Access
Silvia Di Giacomo, Ester Percaccio,

Marco Gullì

и другие.

Nutrients, Год журнала: 2022, Номер 14(18), С. 3709 - 3709

Опубликована: Сен. 8, 2022

Alzheimer’s disease (AD) is a progressive degenerative disorder of the central nervous system, characterized by neuroinflammation, neurotransmitter deficits, and neurodegeneration, which finally leads to neuronal death. Emerging evidence highlighted that hyperglycemia brain insulin resistance represent risk factors for AD development, thus suggesting existence an additional form, associated with glucose metabolism impairment, named type 3 diabetes. Owing limited pharmacological options, novel strategies, especially dietary approaches based on consumption polyphenols, have been addressed prevent or, at least, slow down progression. Among ferulic acid hydroxycinnamic derivative, widely distributed in nature, cereal bran fruits, known be endowed many bioactivities, antioxidant, anti-inflammatory antidiabetic, it could exploited as possible neuroprotective strategy. Considering importance bioactive molecule its widespread distribution foods medicinal plants, aim present narrative review provide overview existing preclinical clinical about properties mechanisms action acid, also focusing ability modulate homeostasis, order support further therapeutic interest

Язык: Английский

Процитировано

43
Exploitation of the multitarget role of new ferulic and gallic acid derivatives in oxidative stress-related Alzheimer's disease therapies: design, synthesis and bioevaluation DOI Creative Commons
Fahad Hussain, Ayesha Tahir, Muhammad Saeed Jan

и другие.

RSC Advances, Год журнала: 2024, Номер 14(15), С. 10304 - 10321

Опубликована: Янв. 1, 2024

Monoamine oxidases (MAOs) inhibitors could decrease reactive oxygen species (ROS) generation, enhance mono-aminergic neural transmission, and have major therapeutic benefits for the treatment of Alzheimer's disease (AD).

Язык: Английский

Процитировано

11
Safety issues of donepezil combined with memantine in Alzheimer’s disease population: real-world pharmacovigilance DOI
Yi Zeng,

Bingshuo Liu,

Lisi Zhou

и другие.

Expert Opinion on Drug Safety, Год журнала: 2025, Номер unknown

Опубликована: Фев. 14, 2025

Alzheimer's disease (AD) is the most common form of dementia. The combination Donepezil and Memantine only FDA-approved therapy for AD, but its adverse drug reactions (ADRs) lack systematic analysis. This study carried out analysis AD population to provide evidence support clinical safety use. Using FAERS database reports (January 2004-January 2024) with as primary suspected drugs, four disproportionality methods - ROR, PRR, BCPNN, EBGM were applied identify positive ADR signals. Subgroup analyses conducted by age gender. A total 712 analyzed (54.6% female, 55.1% aged 65-85). Across population, 42 ADRs identified, including hypertensive crisis, hyperglycemia, hyperosmolar nonketotic syndrome, proteinuria, hydronephrosis, many which newly reported. revealed prostate hypertrophy, acute kidney injury, cerebral infarction in males, while females experienced more severe cardiovascular events, such complete AV block ventricular extrasystole. Additional included hyperkalemia, sinus bradycardia, extrapyramidal disorders. Despite partial consistency combined instructions, new signals emerged, significant differences subgroups.

Язык: Английский

Процитировано

1
Natural Products as Sources of Multitarget Compounds: Advances in the Development of Ferulic Acid as Multitarget Therapeutic DOI
Rajwinder Kaur, Ankita Sood, Damanpreet Kaur Lang

и другие.

Current Topics in Medicinal Chemistry, Год журнала: 2022, Номер 22(5), С. 347 - 365

Опубликована: Янв. 18, 2022

Nature has provided therapeutic substances for millennia, with many valuable medications derived from plant sources. Multitarget drugs become essential in the management of various disorders, including hepatic neurological diabetes, and carcinomas. Ferulic acid is a significant potential agent, which easily available at low cost, possesses toxicity profile, minimum side effects. exhibits actions by modulation signal transduction pathways such as Nrf2, p38, mTOR. The exhibited ferulic include anti-apoptosis, antioxidant, anti-inflammatory, antidiabetic, anticarcinogenic, hepatoprotection, cardioprotection, activation transcriptional factors, expression genes, regulation enzyme activity, neuroprotection, further help treating pathophysiological conditions cancer, skin diseases, brain Parkinson's disease, Alzheimer's hypoxia, H1N1 flu, viral infections. current review focuses on significance natural products sources multitarget compounds, primary focus been made its mechanism, role, protective action ailments.

Язык: Английский

Процитировано

32
Medicine–food herb:Angelica sinensis, a potential therapeutic hope for Alzheimer's disease and related complications DOI
Yu Long, Dan Li, Shuang Yu

и другие.

Food & Function, Год журнала: 2022, Номер 13(17), С. 8783 - 8803

Опубликована: Янв. 1, 2022

As a typical medicine–food herb, Angelica sinensis can alleviate AD and complications based on pharmaceutical material dietary supply.

Язык: Английский

Процитировано

30
Molecular mechanisms underlying cyclophosphamide-induced cognitive impairment and strategies for neuroprotection in preclinical models DOI Creative Commons

Kamilia M. Ibrahim,

Samar F. Darwish, Eman M. Mantawy

и другие.

Molecular and Cellular Biochemistry, Год журнала: 2023, Номер 479(8), С. 1873 - 1893

Опубликована: Июль 31, 2023

Cyclophosphamide has drastically enhanced the expectancy and quality of life cancer patients. However, it is accompanied by diverse neurological complications which are considered a dose-limiting adverse effect. Neurotoxicity caused cyclophosphamide can manifest in numerous manners including anxiety, depression, motor dysfunction cognitive deficits. This review article offers an overview on cyclophosphamide-induced neurotoxicity, providing unified point view possible underlying molecular mechanisms oxidative brain damage, neuroinflammation, apoptotic neuronal cell death as well disruption balance neurotransmitters neurotrophic factors. Besides, this sheds light promising protective agents that have been investigated using preclinical animal models their biological targets protection mechanisms. Despite results experimental models, none these studied clinical trials. Thus, there lack evidence to advocate use any neuroprotective agent setting. Furthermore, evaluated for its effect anticancer activity tumor-bearing animals. Therefore, great necessity adequate well-designed studies evaluation therapeutic values candidates. Conclusively, summarizes accounting neurotoxicity together with potential strategies seeking downgrading complication, thus enhancing well-being patients treated cyclophosphamide.

Язык: Английский

Процитировано

23
Ferulic acid-loaded polymeric nanoparticles prepared from nano-emulsion templates facilitate internalisation across the blood–brain barrier in model membranes DOI Creative Commons

Luna Garcia,

Sujey Palma-Florez, V. Espinosa

и другие.

Nanoscale, Год журнала: 2023, Номер 15(17), С. 7929 - 7944

Опубликована: Янв. 1, 2023

A hydroxycinnamic acid derivative, namely ferulic (FA) has been successfully encapsulated in polymeric nanoparticles (NPs) based on poly(lactic-co-glycolic acid) (PLGA). FA-loaded NPs were prepared from O/W nano-emulsion templates using the phase inversion composition (PIC) low-energy emulsification method. The obtained PLGA exhibited high colloidal stability, good drug-loading capacity, and particle hydrodynamic diameters range of 74 to 117 nm, depending FA concentration used. In vitro drug release studies confirmed a diffusion-controlled mechanism through which amount released reached plateau at 60% after 6 hours-incubation. Five kinetic models used fit data as function time. Weibull distribution Korsmeyer-Peppas equation provided best our experimental suggested quasi-Fickian diffusion behaviour. Moderate dose-response antioxidant radical scavenging activities demonstrated DPPH˙ assay achieving inhibition close 60 40%, respectively. Cell culture that not toxic according MTT colorimetric assay, able internalise efficiently SH-SY5Y neuronal cells supressed intracellular ROS-level induced by H2O2 leading 52% 24.7% cellular viability 0.082 0.041 mg mL-1, permeability blood brain barrier was tested with an organ-on-a-chip model evaluate ability non-loaded penetrate brain. barrier, but decreased when loaded. These results are promising for use loaded management neurological diseases.

Язык: Английский

Процитировано

21
Synthesis and evaluation of multitarget new 2‐aminothiazole derivatives as potential anti‐Alzheimer's agents DOI Creative Commons
Merve Bardakkaya, Burcu Kılıç, Rahşan Ilıkçı Sağkan

и другие.

Archiv der Pharmazie, Год журнала: 2023, Номер 356(8)

Опубликована: Июнь 5, 2023

In this study, two diverse series of 2-aminothiazole-based multitarget compounds, one propenamide and the other propanamide derivatives, were designed synthesized. Subsequently, their anticholinesterease antioxidant (ORAC) activities tested. Among them, compound 3e was most potent acetylcholinesterase (AChE) inhibitor (AChE IC50 = 0.5 μM, butyrylcholinesterase [BChE] 14.7 μM) 9e BChE 3.13 0.9 μM). Kinetic experiments showed that both compounds mixed-type inhibitors. According to activity results, five (3e, 4e, 5e, 9d, 9e) selected for further studies, all which are dual cholinesterase Then, investigated in terms metal chelation activity. Moreover, neuroprotective effects against H2 O2 -induced damage PC12 cell line evaluated at 10 μM results effect 53% compared with reference ferulic acid (77%). 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) revealed noncytotoxic. Additionally, more effective reducing lipopolysaccharides-induced interleukin-1β (IL-1β), IL-6, tumor necrosis factor-α (TNF-α), nitric oxide (NO) production human monocyte derived from patient acute monocytic leukemia compounds. Finally, a molecular docking study also performed.

Язык: Английский

Процитировано

18