Synthesis and Multi‐Target Inhibition of Bis‐Schiff Bases of Barbituric Acid: in Vitro α‐glucosidase, α‐amylase Inhibitory Activities With Docking and DFT Studies DOI Open Access

M H Zahir,

Aftab Alam,

Faheem Jan

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 10(1)

Published: Dec. 31, 2024

Abstract The current research is based on the synthesis of some novel bis ‐Schiff bases bearing barbituric acid moiety followed by characterization through modern spectroscopic techniques and their in vitro inhibitory effects against enzymes α‐glucosidase α‐amylase were subsequently investigated. In series, four compounds 8 (IC 50 = 5.62 ± 0.18 3.12 0.13 µM), 10 7.13 1.03 8.19 1.11 9 12.81 1.92 12.11 1.32 11 15.07 0.38 16.01 0.28 µM) attributed notable dual inhibition better than standard acarbose drug 16.16 0.15 16.65 0.17 µM). molecular docking study was performed to explored binding affinities key interactions synthesized with targeted proteins (α‐amylase α‐glucosidase). Furthermore, stability all verified density functional theory (DFT) method at B3LYP/6–311++G(d,p). For account intramolecular interaction, DFT‐D3 reduced gradient (RDG) methods utilized. addition, utilising CAM‐B3LYP 6–311++G(d,p), TD‐DFT approach used examine different reactivity circumstances.

Language: Английский

Captivity increased the abundance of high-risk antibiotic resistance genes in the giant panda gut microbiome DOI

Tian-Gui Cai,

Jindong Zhang, Lu Lu

et al.

Environmental Research, Journal Year: 2024, Volume and Issue: unknown, P. 120220 - 120220

Published: Oct. 1, 2024

Language: Английский

Citations

1
Synthesis and Molecular Docking Study of Hydrazone Schiff Bases of α‐Naphthalene‐Containing Alkyl Phenyl Ether Fragment as Potent α‐Amylase and α‐Glucosidase Inhibitors DOI

Tanzeela Ahmad Shah,

Aftab Alam,

Zainab Zainab

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(42)

Published: Nov. 1, 2024

Abstract In this study, new Schiff base derivatives of α‐naphthalene acetic acid containing alkyl phenyl ether fragment have been effectively synthesized through multistep reaction process, characterized by 1 H‐NMR and 13 C‐NMR spectroscopy. These tested for their in vitro α‐amylase α‐glucosidase inhibitory activities. the series, 8 compounds ( 2j, 2f, 2e, 2m, 2a, 2b, 2l, 2c ) exhibited promising inhibition with IC 50 values from 5.38 ± 0.36 to 14.59 0.64 µg/mL. Similarly, case activity, 10 2c, 2i, 2d, 2l excellent activity having 6.96 0.39 16.27 0.31 µg/mL, wheras remaining good‐to‐least antidiabetic potential. The ADME properties were calculated all using Swiss‐ADME web tool. Furthermore, docking studies identified binding modes compounds.

Language: Английский

Citations

1
Synthesis and biological evaluation of diclofenac acid derivatives as potential lipoxygenase and α-glucosidase inhibitors DOI Creative Commons
Asma Sardar,

Obaid-ur-Rahman Abid,

Wajid Rehman

et al.

Royal Society Open Science, Journal Year: 2024, Volume and Issue: 11(11)

Published: Nov. 1, 2024

Inflammation is a complex physiological response associated with the onset and progression of various disorders, including diabetes. In this study, we synthesized series diclofenac acid derivatives evaluated their potential anti-diabetic anti-inflammatory activities. The compounds were specifically assessed for ability to inhibit 15-lipoxygenase (15-LOX) α-glucosidase enzymes. structures confirmed through 1 H nuclear magnetic resonance (NMR), 13 C-NMR high-resolution mass spectrometry (electron ionization) analysis. All these exhibited varying degrees inhibitory activity against LOX, when compared standard drugs, 5a (half-maximal concentration (IC 50 ) 14 ± µM), 5b 61 µM) 7c 67 showed good LOX enzyme. While results revealed that most significant drug acarbose (376 µM). potent as α - glucosidase inhibitors 7b (3 4b (5 7a (7 8b (11 active found be least toxic maintained mononuclear cells viability at 96–97% controls determined by multi-transaction translator assay. Molecular docking studies further reiterated significance ‘lead’ great target enzymes in process discovery.

Language: Английский

Citations

1
Quantitative real-time PCR analysis of gut microbiota in rheumatoid arthritis patients compared to healthy controls DOI Creative Commons
Azin Masroor, Abolfazl Gholipour, Milad Shahini Shams Abadi

et al.

AMB Express, Journal Year: 2024, Volume and Issue: 14(1)

Published: Dec. 18, 2024

Rheumatoid arthritis (RA) is an autoimmune disorder with synovial inflammation of joints and extra articular manifestations. The results recent researches consider the relationship between microbiota immune system as a double-edged sword. Considering that composition intestinal immunological clinical status body has been confirmed, it very important to investigate effect each genus species bacteria on state system. current study was determined using 16S rRNA gene sequencing explore 4 selected gut from 25 people suffering rheumatism (RA group) time interval at least 3 years onset disease Healthy by real PCR. Gut dysbiosis in patients rheumatoid identified alongside key serological markers such C-reactive protein (CRP), erythrocyte sedimentation rate (ESR), immunofluorescence (IF), anti-cyclic citrullinated peptide (Anti-CCP), white blood cell count (WBC), mean corpuscular volume (MCV), aspartate aminotransferase (AST), alanine (ALT), urea nitrogen (BUN), Platelet (PLT), thyroid-stimulating hormone (TSH), creatinine (Cr), hemoglobin (Hb). Additionally, data individuals incomplete or unverified records were excluded ensure accuracy reliability. Bacteroides fragilis, Roseburia faecis Fusobacterium nucleatum genera showed much lower median comparison healthy (P > 0.001, p = 0.002, P < 0.001 respectively). While difference E. coli not significant two studied groups (p 0.31). In way change normal flora homeostasis reduction beneficial faecis, genera, may stimulate initiate autoimmunity.

Language: Английский

Citations

1
Utilization of Lactobacillus rhamnosus as probiotic adjunct culture for the development of tempeh DOI Creative Commons
Naveed Ahmed, Muhammad Saeed, Aasma Asghar

et al.

International Journal of Food Properties, Journal Year: 2024, Volume and Issue: 27(1), P. 1279 - 1289

Published: Sept. 12, 2024

Language: Английский

Citations

0
Dose and age dependent effects of lactate supplementation in shaping gut microbiota DOI Creative Commons

Futing Luo,

Tao Shao,

Xiangdong Liu

et al.

Journal of Functional Foods, Journal Year: 2024, Volume and Issue: 122, P. 106467 - 106467

Published: Sept. 18, 2024

Language: Английский

Citations

0
Deciphering the impact of stickwater hydrolysate on growth performance, immune response, and IGF-1/PI3K/AKT/mTOR signaling pathway in Siberian sturgeon (Acipenser baerii) fingerlings DOI

Mahdad Mahdabi,

Mehdi Shamsaie Mehrgan, Houman Rajabi Islami

et al.

Fish Physiology and Biochemistry, Journal Year: 2024, Volume and Issue: 50(6), P. 2605 - 2618

Published: Oct. 7, 2024

Language: Английский

Citations

0
Pyrrolidine derivatives as α-amylase and α-glucosidase Inhibitors: Design, synthesis, structure-activity relationship (SAR), docking studies and HSA binding DOI Creative Commons
Aeyaz Ahmad Bhat, Nitin Tandon, Iqubal Singh

et al.

Heliyon, Journal Year: 2024, Volume and Issue: 10(20), P. e39444 - e39444

Published: Oct. 1, 2024

Language: Английский

Citations

0
Chitosan-based functional materials combined with plant extract: A promising strategy in the stimulation of wound healing process DOI

Yasir Iqbal,

Faheem Amin, Mahvish Fatima

et al.

Journal of Drug Delivery Science and Technology, Journal Year: 2024, Volume and Issue: unknown, P. 106314 - 106314

Published: Oct. 1, 2024

Language: Английский

Citations

0
Encapsulation of Lacticaseibacillus rhamnosus by Extrusion Method to Access the Viability in Saffron Milk Dessert and Under Simulated Gastrointestinal Conditions DOI Creative Commons
Mohammad Ganje, Seyed Saeed Sekhavatizadeh,

Fatemeh Teymouri

et al.

Food Science & Nutrition, Journal Year: 2024, Volume and Issue: 12(11), P. 9714 - 9726

Published: Oct. 23, 2024

ABSTRACT The effectiveness of probiotics in delivering health benefits may be associated with their capacity to maintain a minimum concentration 10 6 CFU/g during food storage and successfully colonize the gastrointestinal tract (GI). Lacticaseibacillus rhamnosus (LR) is probiotic that does not exhibit adequate stability under harsh conditions. To enhance survival LR storage, alginate (ALG) was used as primary encapsulating layer through extrusion microencapsulation. Subsequently, camelina seed mucilage (CSM) protein (CSP) were applied secondary layers at varying concentrations (0%–4%). Among tested formulations, ALG‐CSM‐CSP (1.5%, 4%, 4% w/w) exhibited significantly higher encapsulation efficiency (94.15%) provided appropriate SEM image. Three saffron milk desserts (SMD) containing free (FLR), microencapsulated (MLR), control (C) prepared, followed by physicochemical microbiological assessments samples. result showed end SMD had lowest pH (6.21), highest acidity (30°D), maintained permissible limit bacteria (6.7 log cfu/mL) among In GI, MLR FLR rates 43% 45.4%, respectively on 14th day respectively. hardness (313.70 g), adhesiveness (2.01 mJ), chewiness (9.36) gumminess (58.8) greatest values Moreover, images relatively denser structure for MLR. conclusion, this study highlights potential CSM CSP protect probiotics, offering valuable insights developing new functional foods improved GI.

Language: Английский

Citations

0