Dorzolamide intermediates with potential anti-inflammatory activity.

Dorzolamide (DZD), a Carbonic anhydrase (CA) inhibitor clinically used to lower intraocular pressure, exhibits anti-inflammatory effects owing to the drug's ability to inhibit the TIR domain-containing adaptor protein (TIRAP)-mediated signalling in macrophages. Here, we investigated whether DZD intermediates also demonstrate any anti-inflammatory property like DZD but with a reduced inhibition of CA. We found that several intermediates of DZD show increased binding to TIRAP at the common interface of kinases, such as Protein kinase C-delta (PKCδ) and Bruton's tyrosine kinase (BTK).

Multicomponent Synthesis of 2,4,5-Trisubstituted Thiazoles Using a Sustainable Carbonaceous Catalyst and Assessment of Its Herbicidal and Antibacterial Potential.

Herein, a novel, biocatalyzed, and on-water microwave-assisted multicomponent methodology have been developed for the synthesis of trisubstituted thiazoles (-). The reaction was catalyzed using a sulfonated peanut shell residue-derived carbonaceous catalyst (). The developed catalyst was characterized using Fourier transform infrared (FTIR), a Brunauer-Emmett-Teller (BET) surface area analyzer, a field emission scanning electron microscope (FE-SEM), energy-dispersive X-ray (EDX), and a particle size analyzer (PSA).

Correlation of distance walked in audio signal-modified shuttle walk test with six-minute walk test.

The literature review suggested that the audio signal-modified shuttle walk test (SWTSR) was equally reliable and valid when compared to the conventional shuttle walk test. A comparison of SWTSR with the six-minute walk test (6MWT), which is considered the gold standard in walk tests, allowed us to evaluate the SWTSR and determine its validity and reliability as an alternative or supplement to the 6MWT. The objective of this study was to determine the correlation between the distances walked during a SWTSR and the 6MWT in healthy, normal adults.

Mortality in chronic pulmonary aspergillosis: a systematic review and individual patient data meta-analysis.

Background: Despite antifungal treatment, chronic pulmonary aspergillosis (CPA) is associated with substantial morbidity and mortality. We conducted a systematic review and meta-analysis to evaluate rates of mortality and its predictors in CPA.

Methods: A systematic literature search was conducted across MEDLINE (PubMed), Scopus, Embase, and Web of Science to identify studies in English, reporting mortality in CPA, from database inception to Aug 15, 2023.

Beyond digestion: Exploring how the gut microbiota modulates human social behaviors.

For a long time, traditional medicine has acknowledged the gut's impact on general health. Contemporary science substantiates this association through investigations of the gut microbiota, the extensive community of microorganisms inhabiting our gastrointestinal system. These microscopic residents considerably improve digestive processes, nutritional absorption, immunological function, and pathogen defense.

Therapeutic role of naringin in cancer: molecular pathways, synergy with other agents, and nanocarrier innovations.

Naringin, a flavanone glycoside found abundantly in citrus fruits, is well-known for its various pharmacological properties, particularly its significant anticancer effects. Research, both in vitro and in vivo, has shown that naringin is effective against several types of cancer, including liver, breast, thyroid, prostate, colon, bladder, cervical, lung, ovarian, brain, melanoma, and leukemia. Its anticancer properties are mediated through multiple mechanisms, such as apoptosis induction, inhibition of cell proliferation, cell cycle arrest, and suppression of angiogenesis, metastasis, and invasion, all while exhibiting minimal toxicity and adverse effects.

Modulation of the ubiquitin-proteasome system by curcumin: Therapeutic implications in cancer.

By the ubiquitin-proteasomes, cellular proteins are structurally degraded and turnover. Many essential functions and regulations of cells are regulated and controlled by these proteins. Recent studies indicated that many cancer types have been associated with aberrations in the ubiquitination pathway, which involves three enzymatic steps.

Smart polymers: key to targeted therapeutic interventions.

Smart polymers represent a class of advanced materials that undergo reversible changes in their physical or chemical form and are known as responsive polymers. These polymers show transitions when external stimuli, such as temperature and pH, come into play. Smart polymers are being increasingly applied in various fields, such as drug delivery to a targeted site and gene therapy.

Ethnopharmacological Perspective for Treatment of Epilepsy: An Updated Review.

Plants have been used as healing agents since humanity began. This review presents the plant profiles inhabiting the world regarding their traditional usage by various tribes/ethnic groups for the treatment of epilepsy. The bibliographic investigation was carried out by analyzing standard reference textbooks, Science Direct, Google Scholar, Scopus, Medline, Web of Science, and PubMed databases.

CTX-1 and TRACP-5b as biomarkers for osteoporosis risk in type 2 diabetes mellitus: a cross-sectional study.

Objective: Type 2 diabetes mellitus (T2DM) demonstrates a higher risk of fractures compared to the healthy population. Therefore, the aim of our study is to assess the risk of osteoporosis in T2DM patients.

Methodology: A cross-sectional observational study was conducted in T2DM patients.

Role of miRNAs in breast cancer development and progression: Current research.

Breast cancer, a complex and heterogeneous ailment impacting numerous women worldwide, persists as a prominent cause of cancer-related fatalities. MicroRNAs (miRNAs), small non-coding RNAs, have garnered significant attention for their involvement in breast cancer's progression. These molecules post-transcriptionally regulate gene expression, influencing crucial cellular processes including proliferation, differentiation, and apoptosis.

Medicinal chemistry-based perspectives on thiophene and its derivatives: exploring structural insights to discover plausible druggable leads.

Thiophene is a privileged pharmacophore in medicinal chemistry owing to its diversified biological attributes. The thiophene moiety has been ranked 4th in the US FDA drug approval of small drug molecules, with around 7 drug approvals over the last decade. The present review covers USFDA-approved drugs possessing a thiophene ring system.

The Therapeutic Management of Chemical and Herbal Medications on Uric Acid Levels and Gout: Modern and Traditional Wisdom.

Gout is a chronic inflammatory condition characterized by elevated uric acid levels in the blood, which can precipitate acute gout attacks in individuals with genetic susceptibility, existing medical conditions, and dietary influences. Genetic predispositions, comorbid medical conditions, nutritional choices, and environmental factors increasingly recognize the multifactorial etiology of the disease. Recent research has highlighted the potential of phytochemicals, particularly flavonoids, saponins, and alkaloids, to manage hyperuricemia (HUA) and its associated complications.

L. (Butterfly Pea) Flower Against Endometrial Pain: Integrating Preliminary In Vivo and In Vitro Experimentations Supported by Network Pharmacology, Molecular Docking, and Molecular Dynamics Simulation Studies.

L. (CT) is a perennial herbaceous plant with deep blue flowers native to tropical Asia. This work explores the endometrial pain (EP) regulation of CT flower through a multifaceted approach.

Development, Analysis, and Determination of Pharmacokinetic Properties of a Solid SMEDDS of Voriconazole for Enhanced Antifungal Therapy.

Background: Voriconazole is an antifungal drug, which is classified under Bio-Classification System-II and has low water solubility (0.71 mg/mL) and high permeability. Hardly any endeavors have been made to increase the bioavailability of voriconazole.

Rosiridin Protects Against Aluminum Chloride-Induced Memory Impairment via Modulation of BDNF/NFκB/PI3K/Akt Pathway in Rats.

Rosiridin is a monoterpene with outstanding monoamine inhibitory activity that is useful to treat depressive episodes and rapid-onset dementia. The current investigation aims to evaluate the neurologically protective impact of rosiridin, which opposes aluminum chloride (AlCl) and causes memory dysfunction in rats. Memory impairment was developed in Wistar rats by administering AlCl (100 mg/kg p.

Measles-Rubella Microarray Patches Phase III Clinical Trial Framework: Proposal and Considerations.

: The Measles-Rubella Microarray Patch (MR-MAP) is an important technology that is expected to reduce coverage and equity gaps for measles-containing vaccines (MCVs), reach zero-dose children, and contribute to elimination of measles and rubella. MR-MAPs are anticipated to be easier to deploy programmatically and could be delivered by lesser-trained health workers, thereby increasing immunization coverage. The most advanced MR-MAP has reached clinical proof-of-concept through a Phase I/II trial in the target population of infants and young children.

Nano-enabled pharmacogenomics: revolutionizing personalized drug therapy.

The combination of pharmacogenomics and nanotechnology science of pharmacogenomics into a highly advanced single entity has given birth to personalized medicine known as nano-enabled pharmacogenomics. This review article covers all aspects starting from pharmacogenomics to gene editing tools, how these have evolved or are likely to be evolved for pharmacogenomic application, and how these can be delivered using nanoparticle delivery systems. In this prior work, we explore the evolution of pharmacogenomics over the years, as well as new achievements in the field of genomic sciences, the challenges in drug creation, and application of the strategy of personalized medicine.

Enhanced cell survival in prepubertal testicular tissue cryopreserved with membrane lipids and antioxidants rich cryopreservation medium.

The present study explores the advantages of enriching the freezing medium with membrane lipids and antioxidants in improving the outcome of prepubertal testicular tissue cryopreservation. For the study, testicular tissue from Swiss albino mice of prepubertal age group (2 weeks) was cryopreserved by slow freezing method either in control freezing medium (CFM; containing DMSO and FBS in DMEM/F12) or test freezing medium (TFM; containing soy lecithin, phosphatidylserine, phosphatidylethanolamine, cholesterol, vitamin C, sodium selenite, DMSO and FBS in DMEM/F12 medium) and stored in liquid nitrogen for at least one week. The tissues were thawed and enzymatically digested to assess viability, DNA damage, and oxidative stress in the testicular cells.

Targeting cancer-associated fibroblasts with pirfenidone: A novel approach for cancer therapy.

Cancer-associated fibroblasts (CAFs) are a heterogeneous cell population within the tumor that have recently come into the spotlight. By extracellular matrix (ECM) remodeling and robust cross-talk with cancer cells via different secretions such as cytokines, chemokines, and growth factors, CAFs contribute to cancer progression and poorer prognoses in patients. Novel candidates have been developed to inhibit CAFs; however, due to safety and efficacy issues, none have successfully passed clinical trials.

Nondestructive techniques for pharmaceutical drug product characterization.

Pharmaceutical product development involves multiple steps; therefore product quality must be assessed to ensure robustness and acceptability. Raw components, production methods, and ambient conditions yield highly variable end products with low batch-to-batch consistency. Although end testing is performed to ensure product quality, intermediate quality checks are limited.