Результаты поиска

An overview of mechanism and chemical inhibitors of shikimate kinase.

Tuberculosis is a highly infectious disease other than HIV/AIDS and it is one of the top ten causes of death worldwide. Resistance developme … ous biological macromolecule derivatives, Manzamine Alkaloids derivatives, Dipeptide inhibitor, and Chalcones are discussed in detail. These derivatives bind to the specific target appropriately proving their potential ability through different binding interactions and effectively explored as an effective and selective Sk inhibitor.Communicated by Ramaswamy …

2',6'-dihydroxy-4'-methoxy Dihydrochalcone Improves the Cognitive Impairment of Alzheimer's Disease: A Structure-activity Relationship Study.

BACKGROUND: Chalcones and dihydrochalcones present potent inhibition of acetylcholinesterase, currently considered the most efficient approach for symptomatic treatment of Alzheimer's disease. OBJECTIVE: The present study aimed to explore the potential benefits of 2',6'-dihydroxy-4'-methoxy dihydrochalcone on the cognitive deficits of animals submitted to the streptozotocin-induced Alzheimer's model, as well as evaluating the possible mechanisms of action. METHODS: Learning and memory functions of different groups of animals were submitted to the streptozotocin-induced Alzheimer's model (STZ…

In vitro antiplasmodial activity, targeted LC-MS metabolite profiling, and identification of major natural products in the bioactive extracts of Palicourea and Psychotria species from the Amazonia and Atlantic Forest biomes, Brazil.

INTRODUCTION: A great variety of bioactive natural products has been reported for different Palicourea and Psychotria species (Rubiaceae). H … al natural antimalarial hits. In addition, other metabolite classes such as flavanones, lignans and chalcones were also putatively identified in the bioactive extracts of Psychotria apoda, Psychotria capitata, and Psychotria poeppigiana. CONCLUSION: The present results point to Palicourea and Psychotria species as sources of new antimalarial hits.

Investigation of anti-inflammatory, nitric oxide donating, vasorelaxation and ulcerogenic activities of 1, 3-diphenylprop-2-en-1-one derivatives in animal models.

The main aim of this work is to find out novel chemical moieties with potent anti-inflammatory and vasorelaxant activities with reduced gastric toxicities. For fulfilling the above aim, here we investigated novel chalcones (1, 3-diphenylprop-2-en-1-one derivatives) with nitric oxide (NO) and hydrogen sulphide (H2 S) donating potency for anti-inflammatory activity by carrageenan-induced rat paw oedema. These molecules then further evaluated for in-vitro NO-releasing potency and vasorelaxation effect on isolated adult goat aortic tissue. The promising molecules were further screened for ulceroge…

Inducible nitric oxide synthase inhibitors: A comprehensive update.

Inducible nitric oxide synthase (iNOS), which is expressed in response to bacterial/proinflammatory stimuli, generates nitric oxide (NO) tha … r classified into amidines, five- or six-membered heterocyclics, fused cyclics, steroidal type, and chalcones analogs. Structures of the most/significantly potent compounds from each report are provided to know the functional groups important for incurring iNOS inhibitory activity and selectivity. This review is aimed to provide a comprehensive view to the …

Leishmanicidal, cytotoxicity and wound healing potential of Arrabidaea chica Verlot.

BACKGROUND: Leishmaniasis includes a wide complex of diseases that affect humans and other mammals, and can range from a mild cutaneous form … chemical screening showed that the crude extracts contained flavonoids, tannins, anthocyanidins and chalcones. The leishmanicidal potential of A. chica produced satisfactory results in concentrations of between 60 and 155.9 μg/mL. Cytotoxic assay revealed a 50% reduction in viable cells at a concentration of 189.9 μg/mL. The healing results indicated that t …

Licochalcone C suppresses gastric cancer progression and enhances 5-FU chemosensitivity by targeting RAC3-mediated PI3K-AKT-mTOR signaling.

BACKGROUND: Gastric cancer remains a leading cause of cancer-related mortality worldwide, with limited sensitivity to 5-fluorouracil (5-FU) representing a major obstacle to effective chemotherapy. Licochalcones, bioactive chalcones derived from licorice, have demonstrated broad-spectrum anticancer activities, yet the role of Licochalcone C in enhancing 5-FU sensitivity in gastric cancer remains unexplored. PURPOSE: This study aimed to investigate the antitumor effects of Licochalcone C on gastric cancer and evaluate its potential to enhance 5-FU chemosensitivity, along with elucidating the un…

Potential of MAO-B Inhibitors with Multi-target Inhibition and Antioxidant Properties for the Treatment of Neurodegenerative Disorders.

Millions of people worldwide are affected by neurodegenerative disorders (NDs), which include a broad range of clinical ailments that affect … progression. An overview of the current state of numerous scaffolds, such as chromones, coumarins, chalcones, propargylamines, benzothiazoles, aminoisoquinolines, and the natural compounds, including ferulic acid, resveratrol, and chrysin, which combine antioxidant capability and hMAO inhibition is given in this review, with particular attention given to e …

Phytochemical Composition and Antimicrobial and Antioxidant Activity of Hedysarum semenowii (Fabaceae).

This paper provides a comprehensive phytochemical analysis of extracts obtained from the leaves and roots of Hedysarum semenowii using HPLC/ … e aboveground parts. Our study also identified flavones like luteolin, flavanones (naringenin), and chalcones (liquiritigenin) in various parts. Additionally, the phenolic acids gallic and ferulic acids, as well as the organic acids malic and citric acid, were also detected. The extracts demonstrated differential antimicrobial and antifungal activities in a …

Thymus satureioides Coss.: Mineral Composition, Nutritional Value, Phytochemical Profiling, and Dermatological Properties.

Zaitra, Thymus satureioides, is an aromatic plant with a long history of use in traditional medicine. In this study, we assessed the mineral … prises 46 secondary metabolites, identified through LC-MS/MS analysis, belonging to phenolic acids, chalcones, and flavonoids. The extract elicited pronounced antioxidant activities, inhibited the growth of P. aeruginosa (MIC = 50 mg/mL), and reduced biofilm formation by up to 35.13% using the ¼ sub-MIC of 12.5 mg/mL. Moreover, bacterial extracellular prote …

Synthetic flavokawain analog (E)-1-(2'-hydroxy-4',6'-dimethoxyphenyl)-3-(3-methoxy-4-(3-morpholinopropoxy)phenyl)prop-2-en-1-one (FK-morph) effectively regresses endometriotic implants in rats.

Endometriosis is an estrogen-dependent inflammatory gynecological disorder that is pathologically defined as the growth of endometrial gland … n our previous study, we designed and synthesized serial analogs of naturally occurring flavokawain chalcones. Among these molecules, FK-morph exhibited excellent anti-inflammatory activity and showed therapeutic potential in vitro and in vivo. In the current study, we demonstrate the beneficial effects of FK-morph on a surgically induced endometriosis rat …

β-Amino acid derivatives as mitochondrial complex III inhibitors of L. donovani: A promising chemotype targeting visceral leishmaniasis.

β-amino acids and their analogues are gathering increased attention not only because of their antibacterial and antifungal activity, but also for their use in designing peptidomimetics with increased oral bioavailability and resistance to metabolic degradation. In this study, a series of α-phenyl substituted chalcones, α-phenyl, β-amino substituted dihydrochalcones and β-amino acid derivatives were synthesized and evaluated for their antileishmanial efficacy against experimental visceral leishmaniasis (VL). Among all synthesized derivatives, 10c showed promising antileishmanial efficacy agains…

Development of a Predictive Pharmacophore Model and a 3D-QSAR Study for an in silico Screening of New Potent Bcr-Abl Kinase Inhibitors.

Chronic myelogenous leukemia (CML) is a myeloproliferative disorder, characterized, in most cases, by the presence of the Bcr-Abl fusion onc … MFA and CoMSIA studies were carried out on the 33 novel Abl kinase inhibitors (E)-α-benzylthio chalcones synthesized by Reddy et al. A five-point pharmacophore with a hydrogen bond acceptor, two hydrophobic groups and two aromatic rings as pharmacophore features, and a statistically significant 3D-QSAR model with excellent predictive power were develop …

Natural variation in IBF1 confers antimicrobial activity through altered flavonoid accumulation in rice hulls.

Secondary metabolites perform diverse physiological functions, and studies have identified genes and mechanisms underlying their biosynthesis. However, the genetic basis of intraspecific variation in secondary metabolism remains poorly understood, particularly in less-studied tissues such as rice hulls. In this study, we identified variants in the F-box protein IBF1 that underlie genotypic differences in hull color and flavonoid accumulation using positional cloning. While IR64 (straw-white hull) harbors the functional IBF1, DJ123 (pigmented hull) harbors frame-shift mutations that result in t

Synthesis of 2, 4-disubstituted-1H-benzo[b][1,4]diazepine derivatives as promising anticancer agents.

AIMS: A novel series of 1H-benzo[b][1,4]diazepine derivatives bearing different substitutions at positions 2 and 4 was designed, synthesized, and tested as anticancer agents. MARTIALS AND METHODS: The reaction of chalcone derivatives 5a-h with o-phenylenediamine (OPDA) in ethanol and the presence of acetic acid as a catalyst afforded the targeted 1H-benzo[b][1,4]diazepine derivatives (6a-h). The structures of the newly synthesized compounds were confirmed via spectral data and elemental analyses. These compounds were tested as in vitro anti-cancer agents against MCF7, PC3 cancer cells and BJ

Synthesis, Spectroscopic Characterization, Molecular Docking Studies Toward the GABAA Receptor, ADMET Prediction, GABA Aminotransferase Inhibition, and Anxiolytic Evaluation of Novel Thiazine Derivatives.

Background: The current study uses a computational technique to investigate synthesized thiazine compounds that exhibit potential interactions with the GABAA receptor. A series of novel thiazine derivatives was synthesized via the cyclization reaction of chalcone with thiourea. Methods: For the synthesized compounds, spectroscopic characterization, namely FT-IR, 1H NMR, 13C NMR, and mass spectrometry, was carried out. In addition, the AutoDock Vina 4.2 software was applied to carry out an in silico docking study. Results: The synthesized compounds C3 and C6 exhibited comparable predicted docki

Rational design of a ratiometric indicator-displacement assay for the monitoring of chlortetracycline and intracellular imaging.

Chlortetracycline (CTC), one of the tetracyclic antibiotics, has been widely employed for the inhibition of bacteria. Due to the potential threat to human health posed by the residual CTC, the development of ratiometric fluorescent probes that can achieve accurate measurement and in-situ imaging is urgently needed but remains challenged. Here, a bovine serum albumin (BSA)-involved host-guest system was designed as the novel ratiometric probe (C3@BSA) for CTC based on the indicator-displacement assay principle. Significantly, the fluorescence difference between the CTC@BSA complex and other tet

Novel apocynin regulates TRPV1 activity in the trigeminal system and controls pain in a temporomandibular joint neurogenic model.

OBJECTIVE: Herein, we investigate the potential analgesic effect of a newly synthesized chalcone-derived apocynin in a neurogenic pain model. METHODS: Molecular docking was used to foretell the apocynin binding features and dynamics with the TRPV1 channel, and the activity was tested in vitro, using transfected HEK 293T cells with the rat TRPV1 receptor. The analgesic effect of apocynin was investigated using a capsaicin-induced pain model. The expression of TRPV1, TRPA1, TRPM8, and MAPKs was assessed by electrophoresis, and immunosorbent assays were performed to quantify the neurotransmitter

The chromosome-level genome assembly of Astragalus sinicus and comparative genomic analyses provide new resources and insights for understanding legume-rhizobial interactions.

The legume species Astragalus sinicus (Chinese milk vetch [CMV]) has been widely cultivated for centuries in southern China as one of the most important green manures/cover crops for improving rice productivity and preventing soil degeneration. In this study, we generated the first chromosome-scale reference genome of CMV by combining PacBio and Illumina sequencing with high-throughput chromatin conformation capture (Hi-C) technology. The CMV genome was 595.52 Mb in length, with a contig N50 size of 1.50 Mb. Long terminal repeats (LTRs) had been amplified and contributed to genome size expansi

An overview of the potential anticancer properties of cardamonin.

Cancer is one of the leading causes of mortality, contributing to 9.6 million deaths globally in 2018 alone. Although several cancer treatments exist, they are often associated with severe side effects and high toxicities, leaving room for significant advancements to be made in the field. In recent years, several phytochemicals from plants and natural bioresources have been extracted and tested against various human malignancies using both in vitro and in vivo preclinical model systems. Cardamonin, a chalcone extracted from the Alpinia species, is an example of a natural therapeutic agent that

Совпадение в полном тексте источника
… Naturally, chalcones are found in the leaf, fruit, or root of numerous plant species. Also, several chalcones can be artificially synthesized in laboratories through the acid-base catalyzation of an aldehyde or ketone for preclinical studies [ 30 ]. … Gender-related pharmacokinetics and bioavailability of a novel anticancer chalcone, cardamonin, in rats determined by liquid chromatography tandem mass spectrometry. …