Pharmacology Of Drugs Research Articles

Aspects of improving metrological characteristics of a sensor based on palladium nanoparticles for methionine determination

Relevance. The need to accurately determine the concentration of methionine in various biogeochemical samples. This amino acid serves as a precursor for the biosynthesis of proteins and peptides, as well as a donor of methyl groups, making it an essential participant in numerous biochemical processes, including cysteine synthesis. Additionally, methionine can be found in certain proteins, such as casein. Methionine is a widely used pharmacological drug that has a lipotropic effect and a positive impact on liver function. It enhances the synthesis of phospholipids, choline, and lecithin, as well as having an antidepressant effect due to its s-adenosylmethionine content. It is also a radioprotector and can be used in cancer diagnosis. Methionine is commonly used as an amino acid supplement in poultry and cattle feed, as well as in sports nutrition and medicine. Aim. To investigate the dependence of the metrological characteristics of electrochemical sensors for methionine on the morphological properties of palladium nanoparticles and the composition of the low-molecular reducing agents used for their synthesis. Methods. Transmission electron microscopy, cyclic voltammetry. Results and conclusions. The paper considers the effect of the reducing agent nature on the morphological characteristics of palladium nanoparticles and the composition of their micelles. Sodium borohydride, sodium citrate, and a mixture of borohydride and sodium citrate were used as reducing agents. All the synthesized nanoparticles have a cubic face-centered crystal cell. The composition of the micelles depends on the reducing properties of the reagents used. The reasons for the improved metrological characteristics of methionine determination on an electrochemical sensor based on palladium nanoparticles obtained using sodium citrate are associated with the growth of a shell on the nanoparticle core material, forming a heterostructure.

From Diversity to Standardization: Unveiling Key Parameters in Chick Ileum Bioassays for Enhanced Pharmacology Education and Research

Background As traditional laboratory animal use faces ethical and logistical constraints, the chick ileum has been experimented with as an alternate tissue for bioassays, which is crucial for drug discovery and pharmacology education. However, the absence of uniform bioassay protocols for chick ileum presents a significant challenge, impacting the accuracy and reliability of results in pharmacological studies. Purpose The objective of this review was to compile existing data on chick ileum bioassays from published sources, aiming to enhance future experiments and contribute to the establishment of standardized methods for conducting these bioassays. Methods We conducted a systematic literature review, utilizing keywords like “Chick ileum,” “Bioassay,” “Acetylcholine,” and “Histamine” across databases such as PubMed, Google Scholar, and ScienceDirect. The study selection adhered to specified inclusion and exclusion criteria, focusing on chick ileum research. Data extraction and subsequent analysis were performed to retrieve data for the experiment. Results Eleven articles were selected after applying strict inclusion criteria. Studies ranged from 1967 to 2019, with diverse physiological salt solutions and varied responses to essential chemicals like acetylcholine and histamine. Assay methods varied, but three-point assays were common. Commonly employed tissue lengths and temperatures were identified, and additional factors like organ bath volume and aeration were crucial for consistent results. Conclusion The review highlights the feasibility and ethical advantages of using chick ileum for bioassays. Despite challenges like variable tissue responses and methodological diversity, the review suggests these can be navigated with careful optimization, making chick ileum a valuable model for pharmacological research and education.

Synthesis and Pharmacology of Clinical Drugs Containing Isoindoline Heterocycle Core

Heterocyclic compounds are the cornerstone for active pharmaceutical ingredients. Among heterocycles, isoindoline core occupies a special place, as ten commercial bioactive compounds/drugs contain this skeleton decorated with several functional groups required for optimal receptor binding. These drugs are employed for indications such as multiple myeloma, leukemia, inflammation, hypertension, edema, obesity, and insect control. This review presents the pharmacological activities, mechanisms of action, and chemical syntheses of these commercial bioactive molecules/drugs.

Nateglinide: A comprehensive profile.

Nateglinide belongs to the meglitinide class of insulin secretagogues. It is used as an oral hypoglycemic agent for the treatment of type 2 diabetes mellitus. Nateglinide is an amino acid derivative of D-phenylalanine that binds to the ATP-sensitive potassium channels in pancreatic beta cells and stimulates the secretion of insulin. In this chapter, various aspects of Nateglinide are discussed. This includes methods used for its synthesis, physicochemical properties, and different techniques employed to determine its structure, such as elemental analysis, IR, UV, (1H and 13C) NMR, MS, and XRD. Additionally, the chapter covers a literature review of various methods of analysis of Nateglinide, such as X-ray powder diffraction pattern analysis, differential scanning calorimetry, spectrophotometric, chromatographic, capillary electrophoresis and immunoassay methods. Moreover, the pharmacology of the title drug including pharmacokinetics, pharmacodynamics, mechanism of action, drug-drug and drug-food interactions are also reviewed.

Production and Cryopreservation of 3d Cultures

Three-dimensional (3D) culture systems, which include spheroids (SPs), provide a unique platform for studying complex biological processes in vivo and for enhancing the capabilities of in vitro test systems. Their uniqueness lies in the 3D organization of cells and in the reproduction of complex intercellular interactions, similar to those in native tissues and organs. These "mini-organs" can be used for fundamental research, tissue-engineering constructs, development of preclinical models for testing pharmacological drugs, etc. Important and current issues regarding SPs involve improving methods for their production and cryopreservation. Solving these issues will expand the range and effectiveness of their use in tissue engineering. Here, we describe the authors' research and experience on factors influencing the formation of SPs, which can enhance the understanding of their correct application and standardization. A crucial aspect of this review is the information on applying theoretical approaches based on physico-mathematical calculations to improve the quality of existing cryopreservation protocols for SPs.

Sulfur Derivatives of 1,2,4-Triazole: Recently Developed Compounds, Structure Activity Relationship, and Biological Activity: Review article

The term of heterocyclic chemistry focuses only on heterocyclic compounds, which consider as a percentage of organic chemistry, they equal to greater than sixty-five. These compounds are widely founded in nature and most of them are important to life. In the past few years, scientist fused on 1,2,4-triazoles and their condensed heterocyclic ring due to their medicinal significance, 1,2,4-triazole containing Sulphur atom is one of the important heterocyclic moieties due to its broad range of biological activities also their derivatives can accommodate one of the alternatives as electronic effect as exchanges of the electronic density (electron donating or withdrawing) groups ; for all what mentioned above they are consider as a core molecule in development of large number of medicinal compounds. 1,2,4-Triazole have wide range of pharmacological motivating drug possibility such as analgesic, anti-microbial, anti-inflammatory, anti-convulsant, antioxidant, anti-septic, anti-cancer, diuretics, anti-diabetic, anti-urease, and anti-migraine agents. This review focus on 1,2,4-triazole Sulfur based compounds about their different biological activities and the relationship with their chemistry.

Date palm (Phoenix dactylifera) bioactive constituents and their applications as natural multifunctional ingredients in health-promoting foods and nutraceuticals: A comprehensive review.

Foods that support human health and longevity are becoming increasingly relevant as substitutes for or adjuncts to pharmacological drugs, either through direct consumption or incorporation into designer foods fortified with health-promoting ingredients. Date palm (Phoenix dactylifera L.) fruits, seeds, and pollen are a cornerstone of diverse food and medicine traditions. Their reported metabolic activities include anti-inflammatory, antioxidant, antihypertensive, antihyperlipidemic, antidiabetic, antitumor, antianemia, hepatoprotective, antibacterial, and antiviral effects. Beneficial effects on gut health and vascular health, as well as effectiveness in alleviating certain dysfunctions of the reproductive system, have also been noted. The genomic diversity of this versatile tree and the diverse agroecological conditions in which it grows lead to appreciable variations in the occurrence of protective nutrients and other high-value bioactive phytochemicals, including flavonoid and non-flavonoid phenolics, carotenoids, phytosterols, and oxylipins, whose potential remains underutilized in the food sector. As food ingredients, date fruits and their co-products can improve the sensory, nutritional, and nutraceutical qualities of a broad range of dietary items. Their high nutritional density can assist with the design of novel or improved products that meet the demand for healthier foods. This review summarizes the current state of evidence on the potentialities of date palm fruits and co-products in functional food development, focusing on the nutrients and extra-nutritional compounds of interest, their biofunctional activities, and factors that influence their abundance and bioactivity. Proofs of concept across food and beverage categories, new developments, and clinical evidence are discussed, followed by recommendations for addressing research gaps.

Analysis of the Incidence of Ocular Extraintestinal Manifestations in Inflammatory Bowel Disease Patients: A Systematic Review.

Background: Inflammatory bowel disease (IBD), which includes Crohn's disease and ulcerative colitis, primarily affects the gastrointestinal tract. Additionally, extraintestinal manifestations may occur in the liver, musculoskeletal system and eyes. Its etiology remains unknown, and further research is required in order to develop pharmacological drugs which achieve complete remission of the pathology. Objective: The aim of this study was to analyze the incidence of ocular extraintestinal manifestations in IBD patients. Methods: A total of six searches were carried out on the medical publication server "PubMed" in June and July 2024, using different keywords; a total of 323 results were obtained, of which 34 were finally selected for study. Results: Ocular extraintestinal manifestations in IBD patients are more common in the anterior pole of the eye, with uveitis, scleritis and episcleritis being the most usual ones. In the case of the posterior pole, the most common manifestations are posterior uveitis and optic neuritis. Conclusions: The incidence of ocular complications whose origin is inflammatory, such as uveitis, scleritis, episcleritis and neuritis, is higher than that of complications of non-inflammatory origin.

Pharmaceutical aspects of JAK inhibitors: a comparative review.

Janus kinase inhibitors (JAKIs) are a new class of drugs used in the treatment of a heterogeneous group of diseases, mainly inflammatory and autoimmune diseases. Janus kinase (JAK) is a family of non-receptor tyrosine kinases in cells that transduce cytokine-mediated signals. JAK, along with signal transducer and activator of transcription (STAT) protein, mediate important cellular processes such as immune response, carcinogenesis, cell differentiation, cell division, and cell death. Therefore, inhibitors of JAK-STAT signaling pathways could be useful in treating conditions mediated by the above-mentioned processes. JAK inhibitors mainly treat inflammatory and/or autoimmune diseases such as rheumatoid arthritis, psoriasis, and atopic dermatitis. In this review, we tried to focus on the discovery, pharmacology, and pharmaceutical aspects of JAK inhibitor drugs and their relative risks and benefits, especially focusing on the adverse effects of this class of drugs.

Bilosome as a potential carrier for improving poor oral drug bioavailability

Solid oral dosage forms are widely used in the management of chronic diseases. They are preferred due to their ease of administration, affordability, stability, and accuracy in dose measurement. However, there are challenges with oral delivery due to a number of physiological and metabolic barriers that may impair therapeutic efficacy. Difficulties such as limited water solubility and biological membrane translocation can have a major impact on how well a drug is absorbed. The complexity of developing an oral dosage form is further compounded by considerations such as the drug stability, the impact of gastrointestinal pH, and interactions with metabolic enzymes and biological efflux mechanisms. One of the most important pharmacokinetic indicators of a drug's ability to achieve systemic availability after absorption is bioavailability. It is controlled by how well the drug dissolves and how well it passes through physiological barriers. The purpose of bilosomes, vesicular carriers composed of bile salts and nonionic surfactants, is to improve the administration of vaccinations and drugs. The gastrointestinal tract (GIT) can efficiently transport a range of pharmacological drugs, such as those with antibacterial, antifungal, and antiparasitic capabilities, as well as vaccines and bioactive molecules that target infectious organisms, due to their stability and malleability. For oral medications, bilosomal formulations exhibit higher delivery efficacy due to the complex and hostile environment of the GIT. This research evaluates the potential of bilosomes as a delivery system and highlights how they could be used to administer medications for diseases and viruses that affect the GIT.

Rapid Identification of Chemical Constituents in New Compound Aloe Capsule Based on UPLC-Q-Orbitrap-MS.

The chemical composition of the new compound aloe capsule (NCAC) has not been fully elucidated to date, which poses challenges for pharmacology, scientific, and rational drug use. In this study, a rapid and sensitive method was established to comprehensively study the constituents in the NCAC. The contents of the NCAC were analyzed by UPLC-Q-Orbitrap-MS and data postprocessing technology. Firstly, the extract was separated by UPLC system, and the fragment information was obtained under positive and negative ions and then compared with the characteristic fragments described in the literature, so as to achieve the purpose of rapid identification of the compound of NCAC. A total of 56 compounds including 21 chromones, 6 pyranones, 7 anthraquinones, 7 anthrone, 5 alkaloids, 4 amino acids, and 6 other components were detected in NCAC by comparing the retention time and mass spectrometry information and retrieving the reference literature. The UPLC-Q-Orbitrap-MS method was developed and utilized successfully to identify the major constituents in NCAC and would be helpful for improving the quality control standard of NCAC.

Exploring the Molecular Basis of Anticancer Activity in Various Moss Species Against Colorectal Cancer Cells

Background: Mushrooms are shown to protect against the side effects of cancer. Therefore, mushrooms with proven anticancer properties and active ingredients are fascinating in the search for new cancer drugs. Objective: In this study, the effects of extracts from Hericium coralloides (M1), Lactarius deliciosus (M2), Lepista nuda (M3), Pleurotus ostreatus (M4), and Suillus collitinus (M5) together on HCT116 were investigated. Mesenchymal stem cells (MSCs) were used to study the effect on healthy cells. Methods: MTT was used to determine cell viability. Dose-response curves were generated, the IC50 values of the compounds were calculated, and the effect of the extracts was compared using it. The FTIR was used to analyze the quantitative changes of the cellular components. Results and Discussion: The evaluation of the IC50 values of all fungal species showed that they reduced the cell viability of HCT116 cells. In contrast, no significant reduction in cell viability was observed in MSCs. Changes in the ratio of cell membrane lipids, proteins, and cell nucleic acids between control and fungal-treated HCT116 cells were detected by FTIR. Many of the chemotherapeutic agents are of plant origin, and many resources should still be explored to inhibit the side effects of cancer therapy. Conclusion: The data obtained through this experiment will serve as a reference for studies to be a new source of anticancer drugs in modern pharmacology.

Emitter-embedded metal–organic framework combined with molecularly-imprinted electrochemiluminescence microscopy for drug imaging detection

Drug imaging detection is of great significance for pharmacokinetic studies and for guiding clinical treatment. Electrochemiluminescence microscopy (ECLM) is an emerging technology for drug imaging. This study reports the embedding of tris(2,2′-bipyridyl)ruthenium (Ru-bpy) in a zinc-based metal–organic framework (Zn-MOF). Due to the excellent emission and repeatability of Zn-MOF@Ru, we used it for visual drug detection. To demonstrate this concept, we established a new drug imaging detection method using a smartphone-based ECLM (SECLM) to capture images. We used a molecularly-imprinted polymer to ensure the selectivity of the method using captopril (CTP) as a model compound. The concentration of CTP showed a linear relationship to the quenching efficiency within the range of 1–1 × 105 μmol/L, with a detection limit of 0.29 μmol/L. This method is expected to be widely used for pharmacokinetic research, drug molecular dynamics, drug mechanism research, and drug toxicology research. It provides a new strategy for promoting pharmacological research and drug screening.

INVESTIGATION OF CHANGES IN LENS THICKNESS DEPENDING ON INTRAVITREAL ADMINISTRATION OF ANGIOGENESIS INHIBITOR AND DEXAMETHASONE DEPOT

Currently, the frequency of intravitreal injections (IVV) has a steady upward trend. Antiangiogenic therapy is the predominant method of treating various retinal pathologies. Intravenous injections using pharmacological drugs against VEGF, as well as the intravitreal dexamethasone implant “Ozurdex” are widely used. Since the effect of these pharmacological drugs on cataractogenesis has not yet been sufficiently studied, research in this area is of paramount importance for understanding the morphological characteristics associated with cataract progression. Purpose: The purpose of this study is to study fluctuations in lens thickness during intravitreal administration of aflibercept and dexamethasone depot. Materials and methods. A total of 220 eyes were included in the study. Based on the administered pharmacological drug, the first group included 100 eyes that were intravenously injected with aflibercept, the second group received an intravitreal implant of dexamethasone Ozurdex, and the control (third) group included 100 eyes. Results: The dynamics of changes in lens thickness was documented in groups of patients treated with Ozurdex for 3-6 months (0.012), indicating a gradual increase in lens thickness in this group. Conclusion: no statistically significant changes in lens thickness were found in patients receiving aflibercept after 3 and 6 months. Conversely, the cohort receiving dexamethasone depot showed a statistically significant increase in lens thickness after both 3 and 6 months compared with the control group and the aflibercept cohort.

Atrial fibrillation – a comparative review of one of the most common arrhythmias in dogs and humans

Atrial fibrillation is the most prevalent arrythmia in dogs and humans and is characterised by chaotic depolarisation of the atria, resulting in damage to the atrial myocardium. It can lead to heart failure or worsen an existing condition and cause sudden death. Electrocardiographically, atrial fibrillation is characterised by the absence of P waves and an irregularly irregular rhythm, with narrow QRS complexes. Treatment of atrial fibrillation requires knowledge of pathophysiology and the pharmacology of antiarrhythmic drugs. In contrast to human medicine, the treatment of dogs revolves mainly around rate control strategies, although new studies propose the consideration of several rhythm strategies. Considering the complexity of atrial fibrillation, there is strong need for a consensus on classification, diagnosis and treatment in dogs.

The diverse functions of DYRK2 in response to cellular stress.

To maintain microenvironmental and cellular homeostasis, cells respond to multiple stresses by activating characteristic cellular mechanisms consisting of receptors, signal transducers, and effectors. Dysfunction of these mechanisms can trigger multiple human diseases as well as cancers. Dual-specificity tyrosine-regulated kinases (DYRKs) are members of the CMGC group and are evolutionarily conserved from yeast to mammals. Previous studies revealed that DYRK2 has important roles in the regulation of the cell cycle and survival in cancer cells. On the other hand, recent studies show that DYRK2 also exhibits significant functions in multiple cellular stress responses and in maintaining cellular homeostasis. Hence, the further elucidation of mechanisms underlying DYRK2's diverse responses to various stresses helps to promote the advancement of innovative clinical therapies and pharmacological drugs. This review summarizes the molecular mechanisms of DYRK2, particularly focusing on cellular stress responses.

A Comprehensive Overview of the Current Status and Advancements in Various Treatment Strategies against Epilepsy.

Epilepsy affects more than 70 million individuals of all ages worldwide and remains one of the most severe chronic noncommunicable neurological diseases globally. Several neurotransmitters, membrane protein channels, receptors, enzymes, and, more recently noted, various pathways, such as inflammatory and mTORC complexes, play significant roles in the initiation and propagation of seizures. Over the past two decades, significant developments have been made in the diagnosis and treatment of epilepsy. Various pharmacological drugs with diverse mechanisms of action and other treatment options have been developed to control seizures and treat epilepsy. These options include surgical treatment, nanomedicine, gene therapy, natural products, nervous stimulation, a ketogenic diet, gut microbiota, etc., which are in various developmental stages. Despite a plethora of drugs and other treatment options, one-third of affected individuals are resistant to current medications, while the majority of approved drugs have severe side effects, and significant changes can occur, such as pharmacoresistance, effects on cognition, long-term problems, drug interactions, risks of poor adherence, specific effects for certain medications, and psychological complications. Therefore, the development of new drugs and other treatment options that have no or minimal adverse effects is needed to combat this deadly disease. In this Review, we comprehensively summarize and explain all of the treatment options that have been approved or are in developmental stages for epilepsy as well as their status in clinical trials and advancements.

Characterization of Human Melanoma Skin Cancer Models: A step towards Model-Based Melanoma Research

Advancing 3D in vitro human tissue models is crucial for biomedical research and drug development to address the ethical and biological limitations of animal testing. Recently, 3D skin models have proven to be effective for studying serious skin conditions, such as melanoma. For these advanced models to be applicable in preclinical studies, thorough characterization is essential to understand their applicability and limitations.In this study, we used bioimaging and RNA sequencing to assess the architecture and transcriptomic profiles of skin models, including models with melanoma. Our results indicated that these models closely mimicked skin morphology and gene expression patterns. The full-thickness (FT) model shows a superior resemblance to the human skin, particularly in basement membrane formation and cellular interactions.The integrity of the skin-like properties and gene expression signatures of both skin and melanoma cells were preserved upon the integration of melanoma cells, establishing these models as robust platforms for cancer research. The responsiveness of the FT melanoma models to vemurafenib treatment was successfully monitored, demonstrating their validity as a reliable, reproducible, and humane tool for pharmacological testing and drug development. Furthermore, the transcriptomic data showed that skin models with cancer spheroids had upregulated genes linked to aggressive and resilient cancer behavior compared to spheroids alone. This emphasizes the importance of the microenvironment in cancer progression and suggests that 3D skin models can serve to uncover mechanisms and therapeutic targets that are not detectable in simpler systems. Statement of SignificanceThis study introduces advanced, ethically sound skin and melanoma models as alternatives to animal testing in drug discovery. By thoroughly characterizing these models using bioimaging and RNA sequencing, we demonstrate their close resemblance to human skin, particularly in full-thickness models. These models not only replicate the complex cellular interactions and gene expression patterns of human tissue but also maintain robustness after melanoma integration. Our findings highlight the potential of these models in revealing cancer mechanisms and therapeutic targets, offering a significant impact on melanoma research and preclinical testing.

COMPREHENSIVE REVIEW OF POLYCYSTIC OVARIAN DISEASE: PATHOPHYSIOLOGY, DIAGNOSIS, AND EMERGING TREATMENT STRATEGIES

Polycystic Ovarian Infection (PCOD), consistently implied as Polycystic Ovary Condition (PCOS), is a confounding endocrine issue that influences conceptive created ladies all around the planet, adding to massive metabolic, regenerative, and mental difficulties. This survey gives an all out assessment of PCOD, zeroing in on its pathophysiology, interesting models, and current and arising treatment methodology. The pathophysiology of PCOD is multifactorial, including inborn, hormonal, and ordinary variables, close by advancing disclosures that feature the control of stomach dysbiosis, epigenetic changes, and possible safe structure parts. Finding keeps fixed on the Rotterdam standards, yet new interesting gadgets and biomarkers are being investigated to additionally foster accuracy and early disclosure. Current association ways of thinking feature way of life changes, pharmacological drugs like insulin sensitizers and enemies of androgens, and, in difficult cases, mindful mediations. Arising remedies, including nutraceuticals, engineered modulators, and huge level helped regenerative advances, give extra roads to changed and wide thought. Future heading in PCOD the bosses incorporate the limit of adjusted drug, preventive structures for high-risk people groups, and the need for went on with research on extraordinary biomarkers and steady systems. This study includes the significance of a perplexing, individualized treatment technique for overseeing work on clinical results and individual satisfaction for ladies impacted by PCOD.

Case Study : Observation of Reducing Heartburn Pain in Gastroesophageal Reflux Disease (Gerd) With Hypnotherapy

Hypnotherapy is a form of psychological treatment that utilizes hypnosis to assist in addressing specific mental and physical ailments. It can also be employed for altering habits. Hypnotherapy operates by inducing a hypnotic state in the subject, lowering brain waves to alpha-theta levels for relaxation and enhanced acceptance of suggestions in the subconscious. The aim is to improve psychological issues, emotions, and conduct. The study was carried out on two patients at the Lee Chen Thung Primary Clinic in Jakarta, Indonesia. Sampling was conducted by adhering to specific criteria for selection and administering the GERD-Q questionnaire. The patients included in the study had to have GERD-Q scores higher than 7 and frequently use PPIs for their stomach issues. Management of GERD can be done with drug therapy or pharmacology and non-pharmacology therapy. One of the non-pharmacology therapies that can be given is hypnotherapy. Patients who satisfied the criteria were provided with hypnotherapy in order to alleviate their heartburn symptoms. The process of hypnotherapy can help the body to stimulate the release of endorphins. Endorphins act as the body's innate pain relievers. Following hypnotherapy, patients underwent eval_uation for 1 week using numeric rating scale. Both patients experienced a decrease in pain levels following hypnotherapy.