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Omeprazole, a proton pump inhibitor, is used for gastric and duodenal ulcers, gastroesophageal reflux disease, Helicobacter pylori infection, etc. Current research is based on the loading of omeprazole on surface silver nanoparticles by chemical method. The appearance of an absorption peak at 421 nm confirmed the synthesis of nanoparticles. The FT-IR further confirmed the conjugation of functional groups present in omeprazole moiety with silver. The size and morphology were elucidated by transmission electron microscopy and X-ray diffraction which revealed a spherical shape with an average particle size of 16–20 nm. To know enhancement in their efficacy, the omeprazole-loaded nanoparticles were evaluated against antibacterial, urease inhibition, and antioxidant activities. Nanoparticles showed significant antibacterial potential against Staphylococcus aureus and Escherichia coli with 12 ± 0.41 and 13.6 ± 1.02 mm zones of inhibition, respectively. Almost 2.43 times enhanced urease inhibitory activity was found for nanoparticles (IC50 = 2.17 ± 0.10 µg·mL−1) as compared to omeprazole (IC50 = 5.28 ± 0.14 µg·mL−1). The radical scavenging activity of nanoparticles also increased significantly. The synthesized nanoparticles were docked in the active site of urease to investigate their binding mode. Due to excellent urease and bacterial inhibition, these nanoparticles can be used for ulcers.

Myocardial infarction (MI) is considered one of the most common cardiac diseases and major cause of death worldwide. The prevalence of MI and MI‐associated mortality have been increasing in recent years due to poor lifestyle habits viz. residency, obesity, stress, and pollution. Synthetic drugs for the treatment of MI provide good chance of survival; however, the demand to search more safe, effective, and natural drugs is increasing. Plants provide fruitful sources for powerful antioxidant and anti‐inflammatory agents for prevention and/or treatment of MI. However, many plant extracts lack exact information about their possible dosage, toxicity and drug interactions which may hinder their usefulness as potential treatment options. Phytoconstituents play cardioprotective role by either acting as a prophylactic or adjuvant therapy to the concurrently used synthetic drugs to decrease the dosage or relief the side effects of such drugs. This review highlights the role of different herbal formulations, examples of plant extracts and types of several isolated phytoconstituents (phenolic acids, flavonoids, stilbenes, alkaloids, phenyl propanoids) in the prevention of MI with reported activities. Moreover, their possible mechanisms of action are also discussed to guide future research for the development of safer substitutes to manage MI. [ABSTRACT FROM AUTHOR]

Horticultural crops are vulnerable to diverse microbial infections, which have a detrimental impact on their growth, fruit quality, and productivity. Currently, chemical pesticides are widely employed to manage diseases in horticultural crops, but they have negative effects on the environment, human health, soil physiochemical properties, and biodiversity. Additionally, the use of pesticides has facilitated the development and spread of resistant pathovars, which have emerged as a serious concern in contemporary agriculture. Nonetheless, the adverse consequences of chemical pesticides on the environment and public health have worried scientists greatly in recent years, which has led to a switch to the use of biocontrol agents such as bacteria, fungi, and insects to control plant pathogens. Biocontrol agents (BCAs) form an integral part of organic farming, which is regarded as the future of sustainable agriculture. Hence, harnessing the potential of BCAs is an important viable strategy to control microbial disease in horticultural crops in a way that is also ecofriendly and can improve the soil health. Here, we discuss the role of the biological control of microbial diseases in crops. We also discuss different microbial-based BCAs such as fungal, bacterial, and viral and their role in disease management. Next, we discuss the factors that affect the performance of the BCAs under field conditions. This review also highlights the genetic engineering of BCAs to enhance their biocontrol efficiency and other growth traits. Finally, we highlight the challenges and opportunities of biocontrol-based disease management in horticulture crops and future research directions to boost their efficacy and applications. [ABSTRACT FROM AUTHOR]

This study introduces chromone-based probes designed for selective cyanide ion detection in acetonitrile. Through various spectroscopic methods, the probes demonstrated a colour change from colourless to yellow, enabling naked-eye detection of cyanide ions. The sensors exhibited high sensitivity (6.2 µM) and selectivity for CN¯ ions over common anions. Computational analyses by FMO, NCI, QTAIM, NBO and EDD analysis confirmed the probes' suitability for cyanide detection. Overall, the synthesised compounds present a promising solution for practical applications in the field of cyanide ion sensing. [ABSTRACT FROM AUTHOR]

Stomata in leaves regulate gas exchange between the plant and its atmosphere. Various environmental stimuli elicit abscisic acid (ABA); ABA leads to phosphoactivation of slow anion channel 1 (SLAC1); SLAC1 activity reduces turgor pressure in aperture-defining guard cells; and stomatal closure ensues. We used electrophysiology for functional characterizations of Arabidopsis thaliana SLAC1 (AtSLAC1) and cryoelectron microscopy (cryo-EM) for structural analysis of Brachypodium distachyon SLAC1 (BdSLAC1), at 2.97-Å resolution. We identified 14 phosphorylation sites in AtSLAC1 and showed nearly 330-fold channel-activity enhancement with 4 to 6 of these phosphorylated. Seven SLAC1-conserved arginines are poised in BdSLAC1 for regulatory interaction with the N-terminal extension. This BdSLAC1 structure has its pores closed, in a basal state, spring loaded by phenylalanyl residues in high-energy conformations. SLAC1 phosphorylation fine-tunes an equilibrium between basal and activated SLAC1 trimers, thereby controlling the degree of stomatal opening. [ABSTRACT FROM AUTHOR]

Inhibition of α -glucosidase enzyme activity is a reliable approach towards controlling post-prandial hyperglycemia associated risk factors. During the current study, a series of dihydropyrano[2,3-c] pyrazoles (1 – 35) were synthesized and evaluated for their α -glucosidase inhibitory activity. Compounds 1 , 4 , 22 , 30 , and 33 were found to be the potent inhibitors of the yeast α -glucosidase enzyme. Mechanistic studies on most potent compounds reveled that 1 , 4 , and 30 were non-competitive inhibitors ( K i = 9.75 ± 0.07, 46 ± 0.0001, and 69.16 ± 0.01 μM, respectively), compound 22 is a competitive inhibitor ( K i = 190 ± 0.016 μM ) , while 33 was an uncompetitive inhibitor ( K i = 45 ± 0.0014 μM) of the enzyme. Finally, the cytotoxicity of potent compounds (i.e. compounds 1 , 4 , 22 , 30 , and 33) was also evaluated against mouse fibroblast 3T3 cell line assay, and no toxicity was observed. This study identifies non-cytotoxic novel inhibitors of α -glucosidase enzyme for further investigation as anti-diabetic agents. [ABSTRACT FROM AUTHOR]

Inflammation is associated with multiple life-threatening conditions. Desmidorchis flava is an edible plant and traditionally used for managing various diseases. Three novel molecules, namely desmiflavaside-C ( 1 ), nizwaside ( 2 ), and desmiflanoside ( 3 ) were isolated from Desmidorchis flava , and their structures were confirmed by mass spectrometry and through reported literature. These compounds were in vivo examined for antinociceptive (tonic visceral nociception) and anti-inflammatory (carrageenan induced paw edema) activities. Significant antinociceptive potential was demonstrated by compound 1 at 0.5 and 1 mg/kg doses followed by compounds 2 and 3 . At similar doses, significant anti-inflammatory activity was noted for all the tested compounds. Their antinociceptive and anti-inflammatory activities were comparable to the reference standards. In silico predicted binding modes suggests that these compounds may target allosteric sites of COX-1 and COX-2 enzymes to elicit their anti-inflammatory activities. These isolated natural products may have therapeutic potential in conditions afflicted with pain and inflammation.

Introduction: The pandemic caused by SARS-CoV-2 significantly impacted human life around the globe. Numerous unexpected modifications of the SARS-CoV-2 genome have resulted in the emergence of new types and have caused great concern globally., Method: Inhibitory effects of bioactive phytochemicals derived from natural and synthetic sources are promising for pathogenic viruses. in vitro and in silico techniques were used in the current study to identify novel inhibitors of coumarin clubbed thiazolo[3,2-b][1,2,4]triazoles against the SARS-CoV-2 spike protein., Result: Interestingly, all the tested molecules demonstrated substantial inhibition of spike protein with 91.81-57.90% inhibition. The spike protein was remarkably inhibited by compounds 6k (91.83%), 6j (89.75%), 6m (87.69%),6i (86.60%), 6l (85.40%), 6h (84.70%), 6l (84.70%), 6g (83.40%), 6b (82.60%), 6f (81.90%), while compounds 6d 6a, 6c, and 6e exhibited significant activity against spike protein with 79.60%, 77.10%, 75.30%, and 57.90% inhibition, respectively. The binding mechanism of these novel inhibitors with spike protein was deduced in silico, which reflects that the active molecules firmly bind with the receptor binding domain (RBD) of spike protein, thereby inhibiting its function., Conclusion: The combined in vitro and in silico investigations unfold the therapeutic potential of coumarin-thiazolotriazole scaffolds in the treatment of SARS-CoV-2 infection., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Introduction: Prolyl oligopeptidase (POP) is a pivotal druggable target implicated in diverse biological processes and linked to the development of various ailments, including neurodegenerative disorders. While conventional peptide-based inhibitors have been a centerpiece, their limitations, such as restricted bioavailability, necessitate exploration of non-peptidic inhibitors for their therapeutic potential., Method: This study focuses on designing, synthesizing, and assessing morpholine-based hydrazones targeting the catalytic serine residue of POP. The hydrazones (5a-o), reported as moderately potent analogs compared to the renowned Z-Pro-Prolinal, demonstrated in vitro POP inhibition with IC50 values ranging from 13.60 ± 2.51 to 36.51 ± 1.82 μM. The derivative 5h, with an IC50 of 13.60 ± 2.51 μM, emerged as the most potent inhibitor., Results: Moreover, the in vitro kinetic study of compound 5h indicated that it exhibited concentration-dependent type of inhibition. in silico docking studies of 5h revealed robust interactions in the POP enzyme's active site, yielding a docking score of -6.30 Kcal/- mol, consistent with experimental results., Conclusion: All findings underscored the potential of synthesized derivatives for drug development., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Diabetes mellitus has become a major global health burden because of several related consequences, including heart disease, retinopathy, cataracts, metabolic syndrome, collapsed renal function, and blindness. In the recent study, thirty Schiff base derivatives of 1,3-diphenylurea were synthesized and their anti-diabetic activity was evaluated by targeting α-glucosidase. The compounds exhibited an overwhelming inhibitory potential for α-glucosidase with higher potency ranging from 2.49-37.16 μM. The most effective compound, 5h, showed competitive inhibition of α-glucosidase ( K i = 3.96 ± 0.0048 μM) in the kinetic analysis and strong binding interactions with key residues α-glucosidase in docking analysis, indicating its potential for better glycemic control in diabetes patients., Competing Interests: The authors have declared no conflict of interest., (This journal is © The Royal Society of Chemistry.)

Background: Patient adherence to therapy and compliance is always a challenge for care providers in the management of chronic disorders with multiple medications., Objective: Our study focused on formulating concurrently prescribed ARB (Angiotensin Receptor Blocker), i.e., losartan potassium, and a cholesterol-lowering statin derivative, i.e., rosuvastatin calcium, in a fixed-dose combination tablet., Methods: The drugs were selected based on the presence of synergism and variation in solubility characteristics. Trial batches with fixed concentrations of both active pharmaceutical ingredients (APIs) and varying quantities of different excipients were prepared by dry granulation technique and subjected to different quality control tests for tablets. Batch F5 was selected on the basis of in-process quality control data for the development of a drug release protocol. Experimental conditions were optimized. Based on the sink condition, phosphate buffer (pH 6.8) was selected as the dissolution medium. Simultaneous determination of both APIs in samples collected at predetermined time intervals was carried out using the RP-HPLC technique with acetonitrile, methanol, and water (20:25:55 v/v/v) as mobile phase., Results: Complete dissolution of both APIs in the FDC tablet was achieved in 45 min in 900 mL of the selected medium. The in vitro drug release protocol was validated for accuracy and precision without interference with sample analysis., Conclusion: In this study, a validated, accurate, and robust dissolution testing method was developed for the newly formulated FDC tablet., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)