An Overview of 1,2,3-triazole-Containing Hybrids and Their Potential Anticholinesterase Activities

Pharmaceuticals, Journal Year: 2023, Volume and Issue: 16(2), P. 179 - 179

Published: Jan. 24, 2023

Acetylcholine (ACh) neurotransmitter of the cholinergic system in brain is involved learning, memory, stress responses, and cognitive functioning. It hydrolyzed into choline acetic acid by two key cholinesterase enzymes, viz., acetylcholinesterase (AChE) butyrylcholinesterase (BuChE). A loss or degeneration neurons that leads to a reduction ACh levels considered significant contributing factor development neurodegenerative diseases (NDs) such as Alzheimer’s disease (AD). Numerous studies have shown inhibitors can raise level and, therefore, enhance people’s quality life, at very least, it temporarily lessen symptoms NDs. 1,2,3-triazole, five-membered heterocyclic ring, privileged moiety, is, central scaffold, capable interacting with variety receptors enzymes exhibit broad range important biological activities. Recently, has been clubbed other pharmacophoric fragments/molecules hope obtaining potent selective AChE and/or BuChE inhibitors. The present updated review succinctly summarizes different synthetic strategies used synthesize 1,2,3-triazole moiety. also highlights anticholinesterase potential various di/trihybrids reported past seven years (2015–2022), including rationale for hybridization an emphasis on their structural features optimization treat

Language: Английский

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Investigation on structural, spectroscopic, DFT, biological activity and molecular docking simulation of essential oil Gamma-Terpinene

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1268, P. 133651 - 133651

Published: July 2, 2022

Language: Английский

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The 1,2,3-triazole ‘all-in-one’ ring system in drug discovery: a good bioisostere, a good pharmacophore, a good linker, and a versatile synthetic tool

Expert Opinion on Drug Discovery, Journal Year: 2022, Volume and Issue: 17(11), P. 1209 - 1236

Published: Sept. 27, 2022

The 1,2,3-triazole ring occupies an important space in medicinal chemistry due to its unique structural properties, synthetic versatility and pharmacological potential making it a critical scaffold. Since is readily available through click for creating compound collections against various diseases, has become emerging area of interest chemists.This review article addresses the properties the1,2,3-triazole nucleus as intriguing system drug discovery while focusing on most recent strategies exploited design development analogs inhibitors biological targets.Evidently, with features enormous diseases pharmacophore, bioisoster or platform. evidence indicates that may be more molecules near future along increasing understanding prominent roles structures. feasibility triazole make certainly ideal libraries constructive structure-activity relationship studies. However, comparative target-specific studies are needed gain deeper molecular recognition.[Figure: see text].

Language: Английский

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Identification and characterization of anthocyanins and non-anthocyanin phenolics from Australian native fruits and their antioxidant, antidiabetic, and anti-Alzheimer potential

Food Research International, Journal Year: 2022, Volume and Issue: 162, P. 111951 - 111951

Published: Sept. 19, 2022

Polyphenols are vital bioactive constituents that have beneficial effects on human health. The aim of this study was to characterize the biologically active phenolic metabolites in Australian native commercial fruits (Kakadu plum, Davidson's quandong peach, and muntries) their antioxidant, α-glucosidase, acetylcholinesterase inhibition activities. were measured through total content (TPC), flavonoid (TFC), condensed tannin (TCT), monomeric anthocyanin (TMAC). Moreover, different in-vitro biological assays (DPPH, ABTS, FICA, OH-RSA, activities) conducted measure anti-diabetic, anti-Alzheimer's potential these selected fruits. LC-ESI-QTOF-MS/MS implied for identification quantification purposes. In study, a 307 (51 acids, 194 flavonoids, 15 tannins, 23 other polyphenols, 5 stilbenes, 12 lignans, 7 terpenoids) putatively identified. A 41 compounds quantified/semi-quantified. Kakadu plum identified with higher concentration polyphenols activities compared Davidson muntries. Molecular docking also discover actual role most abundant α-glucosidase

Language: Английский

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Isolation of Some Phenolic Compounds from Plantago subulata L. and Determination of Their Antidiabetic, Anticholinesterase, Antiepileptic and Antioxidant Activity

Chemistry & Biodiversity, Journal Year: 2022, Volume and Issue: 19(8)

Published: July 7, 2022

Abstract In the current study, some phenolic compounds, including acteoside, isoacteoside, echinacoside, and arenarioside purified characterized from Plantago subulata . These compounds were tested for its antioxidant potential, Fe 3+ Cu 2+ reductive ability chelating effects. The inhibitory effects of isolated towards human carbonic anhydrase I II isoenzymes (hCA hCA II), butyrylcholinesterase (BChE) acetylcholinesterase (AChE), aldose reductase (AR) α‐glycosidase (α‐gly). K i values found these in range 0.24±0.05–1.38±0.34 μM against I, 0.194±0.018–1.03±0.06 II, 0.043±0.01–0.154±0.02 AChE, 3.92±1.08–11.93±4.45 BChE, 0.082±0.0008–1.68±0.42 AR, 6.93±2.74–17.17±6.70 α‐glycosidase. As a result, displayed inhibition studied all metabolic enzymes. They are promising candidates treating disorders like Alzheimer's disease, diabetes mellitus, glaucoma, leukemia, epilepsy.

Language: Английский

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Synthesis, characterization and molecular docking studies of highly selective new hydrazone derivatives of anthranilic acid and their ring closure analogue Quinazolin-4(3H)-ones against lung cancer cells A549

Journal of Molecular Structure, Journal Year: 2023, Volume and Issue: 1282, P. 135176 - 135176

Published: Feb. 16, 2023

Language: Английский

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Astragalus Polysaccharide Ameliorates Renal Inflammatory Responses in a Diabetic Nephropathy by Suppressing the TLR4/NF-κB Pathway

Drug Design Development and Therapy, Journal Year: 2023, Volume and Issue: Volume 17, P. 2107 - 2118

Published: July 1, 2023

Diabetic nephropathy (DN), as a chronic inflammatory complication of diabetes, is characterized by hyperglycemia, albuminuria and edema, which ultimately becomes the leading cause end-stage renal disease (ESRD). Astragalus polysaccharide (APS), extracted from membranaceus, was widely used in treatment diabetes mellitus. However, functional roles APS ameliorate responses DN, remain poorly understood. Therefore, purpose this study to explore molecular mechanism on DN vivo vitro models. We explored beneficial effects streptozotocin (STZ)-induced rat model high glucose (HG)-treated glomerular podocyte model. The fasting blood (FBG) ratio kidney weight body were measured after 4 weeks treatment. injury parameters containing serum creatinine (Scr), urea nitrogen (BUN) 24 h urinary protein evaluated. pathological examination observed hematoxylin-eosin (HE) staining. levels IL-1β, IL-6 MCP-1 evaluated ELISA assay. proliferation podocytes determined using CCK-8 assay flow cytometry. qRT-PCR Western blot analysis performed determine amounts TLR4/NF-κB-related gene expression. Our results indicated that effectively decreased FBG, BUN, Scr damage when compared with STZ-induced group. Additionally, significantly ameliorated reducing cytokines IL-6, expression inhibiting TLR4/NF-κB pathway activity rats. Consistent vitro, HG-induced response also alleviated through administration. found injury, mechanisms perhaps related relieving attenuating signaling pathway.

Language: Английский

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A Comparative Study for Nutritional and Phytochemical Profiling of Coffea arabica (C. arabica) from Different Origins and Their Antioxidant Potential and Molecular Docking

Molecules, Journal Year: 2022, Volume and Issue: 27(16), P. 5126 - 5126

Published: Aug. 11, 2022

Coffee is the most widely used beverage globally and contains many bioactive compounds, including phenolic alkaloids, triterpenes, organic acids, amino hormones, fatty acids. The main objective of this study was comparative profiling Australian, Colombian, Ethiopian, Peruvian C. arabica using LC-ESI-QTOF-MS/MS. In study, we tentatively identified 136 metabolites, five (05) six (06) three (03) acids (l-phenylalanine, l-tyrosine, l-pyroglutamic acid), two (02) hormones (melatonin serotonin), one (01) furopyrans (goniothalenol), carotenoid (crocetin), terpenoids, thirty-eight (38) forty-one (41) flavonoids, stilbenes, lignans twenty-three (23) other polyphenols in arabica. highest TPC value (17.74 ± 0.32 mg GAE/g) measured Colombian coffee while lowest (10.24 0.73 coffee. has a higher antioxidant potential than studied samples. A total nineteen metabolites were mapped through LC-MS/MS. Quinic acid derivatives quantified concentrations metabolites. Furthermore, molecular docking predicted that chlorogenic compound contributes to anti-Alzheimer anti-diabetic activities obtained results indicate vast number compounds which have health benefits. research could be conducted validate effect these on flavor profile beverages.

Language: Английский

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Antioxidant, Antiglaucoma, Anticholinergic, and Antidiabetic Effects of Kiwifruit (Actinidia deliciosa) Oil: Metabolite Profile Analysis Using LC-HR/MS, GC/MS and GC-FID

Life, Journal Year: 2023, Volume and Issue: 13(9), P. 1939 - 1939

Published: Sept. 20, 2023

Determining the antioxidant abilities and enzyme inhibition profiles of medicinally important plants their oils is great importance for a healthy life treatment some common global diseases. Kiwifruit (Actinidia deliciosa) oil was examined researched using several bioanalytical methods comprehensively first time in this research to determine its antioxidant, antiglaucoma, antidiabetic anti-Alzheimer's capabilities. Additionally, kiwifruit inhibitory effects on acetylcholinesterase (AChE), carbonic anhydrase II (CA II), α-amylase, which are linked number metabolic illnesses, were established. Furthermore, LC-HRMS analysis used assess phenolic content oil. It came light that contained 26 different compounds. According findings, abundant apigenin (74.24 mg/L oil), epigallocatechin (12.89 caryophyllene oxide luteolin (5.49 oil). In addition, GC-MS GC-FID studies ascertain quantity chemical composition essential Squalene (53.04%), linoleoyl chloride (20.28%), linoleic acid (2.67%), palmitic (1.54%) most compounds For radical scavenging activities oil, 1,1-diphenyl-2-picryl-hydrazil (DPPH•) 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS•+) radicals techniques examined. These effectively demonstrated potent properties (IC50: 48.55 μg/mL DPPH•, IC50: 77.00 ABTS•+ scavenging). Also, reducing capabilities, iron (Fe3+), copper (Cu2+), Fe3+-2,4,6-tri(2-pyridyl)-S-triazine (TPTZ) studied. Moreover, showed considerable effect towards hCA 505.83 μg/mL), AChE 12.80 α-amylase 421.02 μg/mL). The results revealed use pharmaceutical procedure has very due anti-Alzheimer, antidiabetic, antiglaucoma effects.

Language: Английский

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An updated review on 1,2,3-/1,2,4-triazoles: synthesis and diverse range of biological potential

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: July 27, 2024

Language: Английский

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