Journal of Drug Discovery and Therapeutics

Preparation, characterization, and antimicrobial evaluation of 5–(4-Morpholin-4-YL)- 3- Nitrobenzene - 1 - Sulfonyl) - 4, 5, 6, 7 -Tetrahydrothieno [3,2-C] Pyridine

2025-07-09T12:26:29+00:00

A novel series of thienopyridine derivatives, particularly 5–(4-morpholin-4-yl)-3-nitrobenzene-1-sulfonyl)-4,5,6,7-tetrahydrothieno[3,2-c] pyridine, was synthesized and evaluated for antimicrobial activity. Structural characterization was carried out using spectral techniques, including IR, NMR, and mass spectrometry. The synthesized compounds were tested against a panel of Gram-positive and Gram-negative bacterial strains (S. aureus, S. pyogenes, E. coli, P. aeruginosa) and fungal species (A. niger) using the broth dilution method to determine minimum inhibitory concentrations (MICs). Among the tested compounds, derivatives with piperazine and piperidine moieties demonstrated better activity profiles compared to morpholine analogs. The findings suggest the potential of these sulfonylated thienopyridines as promising antimicrobial agents with further optimization.

Keywords: Thienopyridine derivatives, Morpholine analog, antimicrobial activity, Broth dilution method, Minimum inhibitory concentration (MIC)

Bioanalysis Strategies of Polypeptide LC-MS in Biological Matrices – A Case Analysis of Glucagon and Its Analogs in Plasma

2025-07-09T12:29:50+00:00

Glucagon and its analogs are polypeptide drugs developed for treating metabolic conditions such as hypoglycemia, diabetes, and obesity. Due to their high potency, these drugs are typically present at low concentrations in plasma during pharmacokinetic (PK) studies, requiring a highly sensitive bioanalytical method. This work describes a rapid and sensitive LC-MS/MS method using protein precipitation (PPT) with acidified acetonitrile for sample preparation. Analytes were separated on an ACE C18 column using a linear gradient of water and acetonitrile with 0.1% acetic acid. Detection was performed on an AB Sciex mass spectrometer in positive electrospray ionization mode, using the 5+ charge state as the precursor ion. Selective MS/MS fragment ion monitoring improved signal-to-noise ratio and minimized endogenous interference. The assay demonstrated a linear range of 0.5–500 ng/mL with high accuracy, precision, and robustness. It offers high sensitivity, selectivity, low matrix effects, and is suitable for routine PK analysis with high throughput and low cost.

Keywords: LC-MS/MS, Polypeptide bioanalysis, Glucagon, GLP-1, GLP-2, Plasma matrix

Determination of chlorpyrifos and its metabolites in cells and culture media by liquid chromatography-electro spray ionization tandem mass spectrometry (lc-ms/ms)

2025-07-09T12:32:13+00:00

A sensitive and specific method was developed for the simultaneous quantification of chlorpyrifos (CPF), its active metabolite chlorpyrifos oxon (CPO), and the detoxified product 3,5,6-trichloro-2-pyridinol (TCP). Sample preparation involved liquid-liquid extraction for culture media samples and protein precipitation for cell samples. Detection was performed using LC-MS/MS with multiple reaction monitoring (MRM) in positive ion mode for CPF and CPO, and selected ion recording (SIR) in negative ion mode for TCP. The method demonstrated linear ranges of 5–500 ng/mL for CPF, 0.2–20 ng/mL for CPO, and 20–2000 ng/mL for TCP in media samples, and 0.5–50 ng/million cells for CPF, 0.02–2 ng/million cells for CPO, and 2–200 ng/million cells for TCP in cell samples. The method was fully validated for selectivity, linearity, precision, accuracy, recovery, stability, and dilution integrity. It has been successfully applied to investigate the neurotoxicity and metabolism of chlorpyrifos in a human neuronal cell model.

Keywords: Chlorpyrifos, Chlorpyrifos Oxon, TCP, Neuron, Metabolism, Neurotoxicity, Culture Media, LC-MS/MS

A Review on Role of Neurotransmitters in Psychiatric Disorders: Pharmacological Interventions.

2025-07-10T04:15:10+00:00

Neurotransmitters are essential biochemical mediators that regulate the central nervous system’s function, influencing cognition, emotion, and behavior. Psychiatric disorders such as depression, schizophrenia, anxiety, and bipolar disorder are closely associated with dysregulation of key neurotransmitters, including serotonin, dopamine, norepinephrine, gamma-aminobutyric acid (GABA), glutamate, and acetylcholine. This comprehensive review explores the neurobiological roles of these neurotransmitters, highlighting their mechanistic involvement in psychiatric pathophysiology and the pharmacological interventions used to correct these imbalances.

The review begins by detailing the physiological and pathological significance of neurotransmitters, followed by in-depth analyses of pharmacotherapies, including selective serotonin reuptake inhibitors (SSRIs), atypical antipsychotics, mood stabilizers, and novel agents like ketamine and psychedelics. Further, it examines treatment resistance, delayed onset of action, and adverse effect profiles associated with monotherapy. Recent advances such as neuroplasticity-enhancing agents, pharmacogenomics, neuromodulation (e.g., rTMS, DBS), and gut-brain axis interventions are also discussed.

The review emphasizes the growing necessity for integrated and personalized treatment strategies that combine pharmacological, psychological, lifestyle, and digital interventions. It concludes by proposing a roadmap for future psychiatric care—grounded in neuroscience, data-driven precision medicine, and holistic patient-centered approaches. This article serves as a critical resource for clinicians, researchers, and policy-makers aiming to advance pharmacological psychiatry toward more effective, individualized, and ethically sound treatment paradigms.

Keywords: Psychiatric disorders; neurotransmitters; serotonin; dopamine; GABA; glutamate; antipsychotics; antidepressants; pharmacological interventions; treatment resistance; neuroplasticity; pharmacogenomics; neuromodulation; integrative psychiatry; personalized medicine.

Formulation and evaluation of transdermal patch containing essential oils

2025-07-10T12:33:54+00:00

This study investigates the formulation and evaluation of a herbal essential oil-based transdermal drug delivery system (TDDS) with potential anti-inflammatory and analgesic properties. The oils selected—Capsicum oleoresin, Wintergreen oil (methyl salicylate), Mentha oil (menthol), and Thymol oil—are well-known for their therapeutic activities. These oils were incorporated into transdermal patches using suitable polymers and evaluated for physicochemical parameters, and in vitro drug release. Results demonstrated that the herbal essential oil-based TDDS offers a promising alternative for pain and inflammation management with controlled drug delivery and enhanced patient compliance.

Keywords: Transdermal drug delivery system, Essential oils, Capsicum oleoresin, Wintergreen oil, Mentha oil, Thymol, Anti-inflammatory, Analgesic.

Managing responsibility for cybersecurity risks in new technologies

2025-07-25T02:09:25+00:00

In modern times, it is essential for companies to effectively manage cyber security threats linked to emerging technology. This article offers a comprehensive overview of cybersecurity across several technologies. It illustrates the difficulties that organizations have while addressing these risks. The field of cybersecurity has challenges that must be addressed. Technical challenges include the protection of communication networks and the defence of data and systems against intruders. Moreover, it is important to ensure the trustworthiness and credibility of emerging technologies. Organizational challenges include the preparation and training of personnel, with the development of effective strategies to address the unique cybersecurity issues associated with evolving technologies. Regulatory challenges arise from changing compliance mandates in a global environment marked by diverse cybersecurity laws across countries. To effectively manage cyber security risks, it is crucial to follow established risk management standards, including the systematic identification and evaluation of threats. However, there are shortcomings in research and practices that need improvement. The highlighted inadequacies include the lack of frameworks for conducting cost-benefit analyses, a limited understanding of the impact of mistakes in cybersecurity incidents, and the need for comprehensive strategies to tackle the constantly evolving landscape of cybersecurity threats. Addressing these deficiencies requires study and the development of viable solutions to improve cybersecurity in emerging technologies.

Keywords: Cyber security Risks, Risk Management Strategies, Technical Challenges

Revolutionizing Lung Cancer Therapy with Nano-Fiber -Based Drug Delivery System

2025-07-25T02:18:37+00:00

Lung most cancers continues to pose giant challenges to clinicians and sufferers alike, with conventional treatment modalities regularly falling brief in phrases of efficacy and safety. In latest years, nanotechnology used for revolutionizing lung cancer therapy. Among the numerous nano-materials being explored, nano-fiber-primarily based drug shipping structures have garnered sizeable attention due to their particular homes and capability for targeted and controlled drug delivery. This complete evaluate presents a top-level view of the modern-day brand new in nanofiber-based totally drug transport systems for lung most cancers remedy, highlighting their blessings, challenges, and future possibilities. Chemotherapy including general anticancer medicines is linked to serious adverse effects because of the large dosage required. Researchers have lessened the environmental impact of nanofiber manufacturing by using water as an efficient solvent in place of hazardous chemicals. The environmentally benign properties of this green method of creating nanofibers make it a promising tool for regenerative medicine, including cancer treatment. However, a wealth of research studies on the use of nanofibers are accessible. This review article focuses just on using nanofibers for cancer treatment.

Keywords: Lung cancer therapy, nanofibers, drug delivery system, electrospinning, targeted drug delivery, nanotechnology, controlled release, biocompatible polymers, cancer nanomedicine, tumor targeting, pulmonary drug delivery, biodegradable nanofibers, smart drug carriers

Formulation and in-vitro evaluation Rutin Phytosomes

2025-07-28T06:37:06+00:00

Rutin, a naturally occurring bioflavonoid with potent antioxidant and therapeutic properties, suffers from poor water solubility and limited bioavailability, restricting its clinical applications. To overcome these limitations, the present study aimed to develop and evaluate rutin-loaded phytosomes using a lyophilization technique. Rutin phytosomes were formulated using different molar ratios of rutin and soy phosphatidylcholine (SPC) and characterized for particle size, polydispersity index (PDI), zeta potential, drug content, and in-vitro drug release. The optimized phytosomal complex showed improved particle uniformity, stability, and high drug entrapment efficiency. Characterization techniques such as FTIR, DSC, XRD, SEM, TEM, AFM, and [1] H-NMR were employed to confirm the formation and morphological properties of the complex. The in-vitro release study demonstrated a sustained and enhanced release profile of rutin from the phytosomal system compared to pure rutin. These results suggest that rutin phytosomes may serve as an effective delivery system for improving the solubility, stability, and therapeutic efficacy of rutin.

Keywords: Rutin, Phytosomes, Bioavailability, Drug delivery, Soy phosphatidylcholine

Evaluation of in-vivo anti-inflammatory activity of Tridax procumbens Linn extract

2025-07-28T06:59:25+00:00

The present study investigates the in-vivo anti-inflammatory potential of various extracts of Tridax procumbens Linn, a medicinal herb traditionally used in Indian folklore for treating inflammation and wounds. The anti-inflammatory activity was evaluated using standard biochemical markers including alanine transaminase (ALT), aspartate transaminase (AST), lipid peroxidase (MDA), and alkaline phosphatase (ALP) in experimental animal models. Different solvent extracts—ethanolic (TP-EtOHE), aqueous (TP-AqE), chloroform (TP-CHCl₃E), and petroleum ether (TP-PEE)—were administered at a dose of 200 mg/kg body weight, while a standardized ethanol extract (TPEE-S) was tested at 30 mg/kg. Diclofenac (50 mg/kg) served as the standard drug. Results indicated that the TPEE-S and TP-EtOHE extracts significantly reduced inflammatory biomarkers, with values comparable to the standard drug, suggesting potent anti-inflammatory properties. The aqueous, chloroform, and petroleum ether extracts also demonstrated moderate activity. These findings support the traditional use of Tridax procumbens in inflammation and warrant further studies to isolate and characterize its active constituents.

Keywords: Tridax procumbens, Anti-inflammatory, In-vivo study, Phytochemicals, Ethanolic extract, Lipid peroxidation, Liver enzymes, Herbal medicine

Green Synthesis of Nanoparticles and their Antibacterial Activity Against Pathogenic Bacteria

2025-07-28T07:03:01+00:00

This work examined the phytochemical characterization of the primary bioactive ingredients of Punica granatum peels in its aqueous extract, green production of silver nanoparticles, and their antibacterial efficacy. Flavonoids, phenol, tannins, carbohydrates, glycosides, etc. were abundant in peel extract. UV-Visible spectroscopy verified silver nanoparticle production and characterization. UV-Visible spectroscopy of silver nanoparticle-containing reaction media shows maximal absorbance peaks at 430nm (1%), 373nm (3%), and 379nm (5%). The disc diffusion technique was used to assess the green production of silver nanoparticles against bacterial cultures. The silver nanoparticles killed E. coli (MTCC-40), Staphylococcus aureus (MTCC-7443), and Proteus vulgaris (MTCC-*1771). Punica granatum peel extract rapidly lowers Ag+ to Ago and aids silver nanoparticle formation with antimicrobial properties.

Evaluation of in-vitro cytotoxicity studies of Sida rhombifolia leaves extract

2025-08-04T13:57:58+00:00

Recent research into medicinal plants has led to the identification of numerous bioactive compounds with anticancer potential. Sida rhombifolia, a traditionally used medicinal herb, was evaluated in this study for its in vitro cytotoxic activity against Dalton’s Ascitic Lymphoma (DAL) cell lines using the MTT assay. Various extracts of the leaves—including ethyl acetate, aqueous, and others—were tested to determine their ability to inhibit cell viability. Among them, the ethyl acetate and aqueous extracts exhibited the most significant cytotoxic effects, indicating their potential as sources of natural anticancer compounds. These findings support further investigation into the phytochemical constituents of Sida rhombifolia and their mechanism of action in cancer therapy.

Keywords: Sida rhombifolia, MTT assay, Invitro cytotoxicity, DAL cell lines, Medicinal plants.