[Re]Re- and [Tc]Tc-Tricarbonyl Metal Complexes with 1,4,7-Triazacyclononane-Based Chelators Bearing Amide, Alcohol, or Ketone Pendent Groups.

1,4,7-Triazacyclononane (TACN)-based chelators, such as NOTA and NODAGA, have shown great promise as bifunctional chelators for [M(CO)] cores (M = Tc and Re) in radiopharmaceutical development. Previous investigations of TACN-based chelators bearing pendent acid and ester arms demonstrated the important role the pendent arms have in successful coordination of the [M(CO)] core with the TACN backbone nitrogens. In this work, we introduce three TACN-based bifunctional chelators bearing amide, alcohol, and ketone pendent arms and evaluate their (radio)labeling efficiency with the [M(CO)] core as well as the stability and hydrophilicity of the resulting radiometal complexes.

Self-actuating inflammation responsive hydrogel microsphere formulation for controlled drug release in rheumatoid arthritis (RA): Animal trials and study in human fibroblast like synoviocytes (hFLS) of RA patients.

Patients with rheumatoid arthritis (RA) often have one or more painfuljoints despite adequate medicine. Local drug delivery to the synovial cavity bids for high drug concentration with minimal systemic adverse effects. However, anti-RA drugs show short half-lives in inflamed joints after intra-articular delivery.

Edible Vaccines: A Patent-Driven Exploration of Immunization Technologies.

Vaccines are biological preparations that improve immunity to particular diseases. Particularly for poor developing nations, edible vaccines show significant potential as a financially advantageous, simple to administer, straightforward to store, fail-safe, and socially and culturally acceptable vaccine delivery system. A vaccine incorporates the gene-encoding bacterial or viral disease-causing agent in plants without losing its immunogenic property.

Exploring the Therapeutic Potential of Phytoconstituents for Addressing Neurodegenerative Disorders.

Neurodegenerative disorder is a serious condition that is caused by abnormal or no neurological function. Neurodegenerative disease is a major growing cause of mortality and morbidity worldwide, especially in the elderly. After World War Ⅱ, eugenics term was exterminated from medicines.

Investigate the efficacy of size exclusion chromatography for the isolation of extracellular vesicles from C. elegans.

Isolation of Extracellular Vesicles (EVs) has been done extensively in the past using ultracentrifugation, a recent shift has been observed towards precipitation, and exosome isolation kits. These methods often co-elute contaminants of similar size and density which makes their detection and downstream applications quite challenging. As well as the EV yield is also compromised in some methodologies due to aggregate formation.

Emerging Treatment Options of Pluronic in Designing Colloidal Nano and Microcarriers Carriers for Various Therapies.

Poloxamers, commonly known as Pluronics, are a special family of synthetic tri-block copolymers with a core structure made of hydrophobic poly (propylene oxide) chains sandwiched by two hydrophilic poly (ethylene oxide) chains. It is possible to modify the mechanical, bioactive, and microstructural characteristics of Pluronics to simulate the behavior of different types of tissues. Additionally, they are auspicious drug carriers with the capacity to increase therapeutic agent availability and to design nano-drug formulations for various ailments.

Deciphering the Therapeutic Applications of Nanomedicine in Ovarian Cancer Therapy: An Overview.

The majority of deadly cancers that afflict the female reproductive system occur in the ovary. Around 1,40,000 women worldwide die from ovarian cancer each year, making it the sixth most common cancer-associated deceases among females in the United States. Modern, cutting-edge treatments like chemotherapy and surgery frequently produce full remissions, but the recurrence rate is still very high.

Biomass-Derived Core-Shell Carbon Dots with Embedded Tripodal Receptors for the Selective Recognition of Mefenamic Acid in Pharmaceutical Formulations and Urine.

A tripodal amine (TPA) with -OH, N, and S donors is synthesized to functionalize a core-shell carbon dot composite (FCDs@SiO-TPA) for sensing application. The TPA is characterized by spectroscopic and spectrometric techniques, and the composite is characterized by Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), Brunauer-Emmett-Teller (BET), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and energy-dispersive X-ray spectra (EDS) techniques. The composite has the ability to recognize mefenamic acid (MFA) selectively even in the presence of other drugs like ibuprofen sodium, acetylsalicylic acid, naproxen sodium, diclofenac sodium, and ketoprofen.

iTRAQ based proteomic analysis of rice lines having single or stacked blast resistance genes: / during incompatible interaction with .

Unlabelled: Deployment of single or multiple blast resistance () genes in rice plant is considered to be the most promising approach to enhance resistance against blast disease caused by fungus . At the proteome level, relatively little information about gene mediated defence mechanisms for single and stacking resistance characteristics is available. The overall objective of this study is to look at the proteomics of rice plants that have genes; and stacked  +  in response to rice blast infection.

Discovery of LNP1892: A Precision Calcimimetic for the Treatment of Secondary Hyperparathyroidism.

The calcium sensing receptor (CaSR) plays an important role in maintaining calcium homeostasis. The use of calcimimetic cinacalcet has been established to activate CaSR and normalize hypercalcemia. However, cinacalcet has limitations due to its high cLogP and p.

Synthesis of a trinuclear zinc(II) cluster composed of [4.4.3.0]tridecane cages: a rapid detection and degradation probe for the chemical warfare agent simulant diethyl cyanophosphonate in protein-rich food products.

Diethyl cyanophosphonate (DCNP), a simulant of Tabun, is a common pollutant in pharmaceutical waste and poses a high risk to living organisms. Herein, we demonstrate a compartmental ligand-derived trinuclear zinc(II) cluster [Zn(LH)(CHCOO)] as a probe for the selective detection and degradation of DCNP. It consists of two pentacoordinated Zn(II) [4.

Dual PI3Kδγ inhibition demonstrates potent anticancer effects in diffuse large B-cell lymphoma models: Discovery and preclinical characterization of LL-00084282.

Phosphoinositide 3-kinase (PI3K) pathway mediates key signaling events downstream to B-cell receptor (BCR) for survival of mature B-cells, and overexpression or overactivation of PI3Kδ is crucial for B-cell malignancies such as diffuse large B-cell lymphoma (DLBCL). Small molecule PI3Kδγ inhibitors, with a known potential to reduce activated B-cell (ABC)-DLBCL transformation, form an important class of therapeutics approved for follicular lymphoma (FL), chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL). In this study, we describe discovery of a potent, selective and efficacious dual PI3Kδγ inhibitor, LL-00084282, having a differentiated efficacy profile in human ABC- and germinal center B-cell (GCB)-DLBCL cell lines.

An Investigation on Self-Medication Practice During the COVID-19 Pandemic Among the Indian Population.

Background: Self-medication has both negative and beneficial effects on people's health, as the COVID-19 epidemic has demonstrated. The goal of the study is to look into the epidemiology of self-medicated medications used for respiratory symptoms, as a COVID-19 preventive, for its symptoms, or after a positive COVID-19 test, and to see how symptom relief is viewed in India, as well as what demographic factors encourage self-medication.

Methods: Using a trial version of Qualtrics Core XM software to prototype 24 surveys, a webbased questionnaire was built, tested, and disseminated in several Indian states.

Vomiting and risk of endotracheal intubation related to preoperative doxycycline use for dilation and evacuation.

Objective: To describe the rate of vomiting from oral doxycycline 200 mg given the night before second trimester dilation and evacuation (D&E), proportion of anesthesia modalities, and anesthetic complications.

Study Design: We conducted a single-institution retrospective cohort study of patients presenting for second trimester D&E (14-0/7 to 23-6/7 weeks gestation) July 1, 2019-June30, 2020 following their scheduled preoperative visit as identified by billing codes. We recorded vomiting within 30 minutes of ingestion, anesthetic modality, and anesthetic complications.

Discovery and pre-clinical characterization of a selective PI3Kδ inhibitor, LL-00071210 in rheumatoid arthritis.

PI3Kδ plays a critical role in adaptive immune cell activation and function. Suppression of PI3Kδ has been shown to counter excessive triggering of immune responses which has led to delineating the role of this isoform in the pathophysiology of autoimmune disorders. In the current study, we have described preclinical characterization of PI3Kδ specific inhibitor LL-00071210 in various rheumatoid arthritis models.

An Electronic Evaluation of Symptoms in People of India Post-COVID-19 Vaccination.

Background: Remarkable and groundbreaking performances of scientists all over the globe have led to the evolution of COVID-19 vaccines, which are extensively viewed as means to control the epidemic. The primary purpose of this research work was to discover the major side effects of the vaccines, mainly in Homo sapiens.

Methods: An online survey was conducted in various cities of Haryana, India, using a trial version of QualtricsCoreXM software to prototype 20 questionnaires.

Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro--(2'-methyl-3'-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1'-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization.

The role of calcium release-activated calcium (CRAC) channels is well characterized and is of particular importance in T-cell function. CRAC channels are involved in the pathogenesis of several autoimmune diseases, making it an attractive therapeutic target for treating inflammatory diseases, like rheumatoid arthritis (RA). A systematic structure-activity relationship study with the goal of optimizing lipophilicity successfully yielded two lead compounds, and .

The interaction between diet and neurobehavior in very low birth weight infants.

Background: Modulation of behavior and physiology by dietary perturbations early in life can provide clues to the pathogenesis of adult diseases. We tested the hypothesis that a period of early protein supplementation modulates sympathetic nervous system activity demonstrated indirectly by an increase in active sleep state distribution in very low birth weight (VLBW) infants.

Methods: VLBW infants (n = 71) were randomized to a total parenteral nutritional regimen providing 18% of the energy intake as amino acids (AA) or a conventional regimen providing 12.

Design and Optimization of Febuxostat-loaded Nano Lipid Carriers Using Full Factorial Design.

Objectives: This work aims to develop nanostructured lipid carriers (NLCs) to improve the oral bioavailability of febuxostat (FEB).

Materials And Methods: High shear homogenization, a well-known technique, followed by bath sonication with slight modifications was used to prepare FEB-loaded NLCs using oleic acid as liquid lipid and stearic acid as solid lipid. A total of 3² full factorial design was utilized to examine the effect of 2 independent variables, namely, X1 (liquid to solid lipid ratio) and X2 (surfactant concentration) on the Y1 (particle size) and Y2 (% entrapment efficiency) of the drug.

Molecular dynamics of hERG channel: insights into understanding the binding of small molecules for detuning cardiotoxicity.

Evaluation of cardiotoxicity potential of new chemical entities (NCEs) has lately become one of the stringent filters in the drug discovery and development process. Cardiotoxicity is caused mainly by the inhibition of human ether-a-go-go related gene (hERG) channel protein. Inhibition of the hERG channel leads to a life-threatening condition known as cardiac arrhythmia.