Role of Shirodhara and Abhyanga on serum cortisol in Anxiety - A case report.

Chittodvega, classified as a Mano-Vikara (psychological disorder) in Ayurveda, can be correlated with general anxiety disorder. The disturbance of Vata Dosha plays a critical role in its manifestation. Ayurvedic treatments such as Abhyanga (oleation) and Shirodhara (dripping of medicated oil or other suitable liquid on forehead) are known to pacify Vata.

Inoculants of Arbuscular Mycorrhizal Fungi Influence Growth and Biomass of under Amendment and Anamendment Entisol.

Entisol soil is hard and compact in nature, rendering it high in bulk density, which influences root penetration adversely and thereby poor plant growth. In this experiment, used seven treatments in different combination in normal soil, were used as growth media for the seedling. T3 (60% entisol) found the best as it gave the highest biomass in the species regardless of arbuscular mycorrhizal fungi (AMF) treatment.

-Alkyl Carbamoylimidazoles as Versatile Synthons for the Synthesis of Urea-Based PSMA Inhibitors.

We describe -alkyl carbamoylimidazoles as readily available and highly versatile synthons for synthesizing urea-based prostate-specific membrane antigen (PSMA) inhibitors. Urea formation proceeded in high yields (>80%) at room temperature under aqueous conditions. All novel compounds were tested for their PSMA inhibitory potency in a cell-based radiometric binding assay.

Elucidating Residue-Level Determinants Affecting Dimerization of Ebola Virus Matrix Protein Using High-Throughput Site Saturation Mutagenesis and Biophysical Approaches.

The Ebola virus (EBOV) is a filamentous virus that acquires its lipid envelope from the plasma membrane of the host cell it infects. EBOV assembly and budding from the host cell plasma membrane are mediated by a peripheral protein, known as the matrix protein VP40. VP40 is a 326 amino acid protein with two domains that are loosely linked.

[F]ONO-8430506: A novel radioligand for PET imaging of autotaxin (ATX).

We have prepared and tested radioligand [F]ONO-8430506 ([F]8) as a novel ATX PET imaging agent derived from highly potent ATX inhibitor ONO-8430506. Radioligand [F]8 could be prepared in good and reproducible radiochemical yields of 35 ± 5% (n = 6) using late-stage radiofluorination chemistry. ATX binding analysis showed that 9-benzyl tetrahydro-b-carboline 8 has about five times better inhibitory potency than clinical candidate GLPG1690 and somewhat less inhibitory potency than ATX inhibitor PRIMATX.

Targeting the chromatin effector Pygo2 promotes cytotoxic T cell responses and overcomes immunotherapy resistance in prostate cancer.

The noninflamed microenvironment in prostate cancer represents a barrier to immunotherapy. Genetic alterations underlying cancer cell-intrinsic oncogenic signaling are increasingly appreciated for their role in shaping the immune landscape. Recently, we identified Pygopus 2 () as the driver oncogene for the amplicon at 1q21.

Fluorine-18 Labelled Radioligands for PET Imaging of Cyclooxygenase-2.

Molecular imaging probes enable the early and accurate detection of disease-specific biomarkers and facilitate personalized treatment of many chronic diseases, including cancer. Among current clinically used functional imaging modalities, positron emission tomography (PET) plays a significant role in cancer detection and in monitoring the response to therapeutic interventions. Several preclinical and clinical studies have demonstrated the crucial involvement of cyclooxygenase-2 (COX-2) isozyme in cancer development and progression, making COX-2 a promising cancer biomarker.

A Narrative Review on Current Diagnostic Imaging Tools for Dentomaxillofacial Abnormalities in Children.

The current review narrates the findings and discusses the available diagnostic tools for detecting structural abnormalities. The review discusses several diagnostic tools, such as magnetic resonance imaging, cone beam computed tomography, multi detector row CT and positron emission tomography. The vital findings and comparative analysis of different diagnostic tools are presented in this review.

Synthesis and Preclinical Evaluation of [F]SiFA-PSMA Inhibitors in a Prostate Cancer Model.

Positron emission tomography (PET) imaging of prostate-specific membrane antigen (PSMA) with gallium-68 (Ga) and fluorine-18 (F) radiotracers has aroused tremendous interest over the past few years. The use of organosilicon-[F]fluoride acceptors (SiFA) conjugated to urea-based peptidomimetic PSMA inhibitors provides a "kit-like" multidose synthesis technology. Nine novel F-labeled SiFA-bearing PSMA inhibitors with different linker moieties were synthesized and analyzed for their binding against [I]I-TAAG-PSMA in LNCaP cells.

Synthesis, Binding Affinity Analysis, and F Radiosynthesis of Small-Molecular-Weight HIF-1α-Binding Compounds.

Eleven small-molecular-weight compounds and three cyclic peptides were synthesized and evaluated for binding to hypoxia-inducible factor-1α (HIF-1α). Microscale thermophoresis analysis identified peptide [ F]SFB-link-c-(Ppg)LLFVY 3 and small-molecule inhibitor 5 as potent HIF-1α binding compounds with K values of 0.46±0.

Production of Proteins of the SARS-CoV-2 Proteome for Drug Discovery.

The severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is the causative agent of the coronavirus disease of 2019 (COVID-19). Its genome encodes two open reading frames for two large proteins, PP1a and PP1ab. Within the two polypeptide stretches, there are two proteases that process the large proteins into 15 discrete proteins essential for the assembly of the virion during its replication.

Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.

Recent experimental evidence demonstrated an aberrant overexpression of cyclooxygenase-1 (COX-1) in various cancers, which has stimulated the development of COX-1-selective inhibitors as promising anticancer drugs and cancer imaging agents. Herein we describe the synthesis and validation of 3-(furan-2-yl)--aryl 5-amino-pyrazoles as a novel class of COX-1 inhibitors, including molecular docking studies. Among all tested compounds, 4-(5-azido-3-(furan-2-yl)-1-pyrazol-1-yl)benzoic displayed a favorable COX-1 inhibition and selectivity profile (COX-1 IC = 0.

Genetically Encoded Fragment-Based Discovery from Phage-Displayed Macrocyclic Libraries with Genetically Encoded Unnatural Pharmacophores.

Genetically encoded macrocyclic peptide libraries with unnatural pharmacophores are valuable sources for the discovery of ligands for many targets of interest. Traditionally, generation of such libraries employs "early stage" incorporation of unnatural building blocks into the chemically or translationally produced macrocycles. Here, we describe a divergent late-stage approach to such libraries starting from readily available starting material: genetically encoded libraries of peptides.

Design, Synthesis, and Evaluation of a Luminescent Cholesterol Mimic.

The development of new chemical tools with improved properties is essential to chemical and cell biology. Of particular interest is the development of mimics of small molecules with important cellular function that allow the direct observation of their trafficking in a cell. To this end, a novel 15-azasterol has been designed and synthesized as a luminescent cholesterol mimic for the monitoring of cholesterol trafficking.

Optimization of Acetazolamide-Based Scaffold as Potent Inhibitors of Vancomycin-Resistant .

Vancomycin-resistant enterococci (VRE) are the second leading cause of hospital-acquired infections (HAIs) attributed to a drug-resistant bacterium in the United States, and resistance to the frontline treatments is well documented. To combat VRE, we have repurposed the FDA-approved carbonic anhydrase drug acetazolamide to design potent antienterococcal agents. Through structure-activity relationship optimization we have arrived at two leads possessing improved potency against clinical VRE strains from MIC = 2 μg/mL (acetazolamide) to MIC = 0.

In Cellulo Generation of Fluorescent Probes for Live-Cell Imaging of Cylooxygenase-2.

Live-cell imaging with fluorescent probes is an essential tool in chemical biology to visualize the dynamics of biological processes in real-time. Intracellular disease biomarker imaging remains a formidable challenge due to the intrinsic limitations of conventional fluorescent probes and the complex nature of cells. This work reports the in cellulo assembly of a fluorescent probe to image cyclooxygenase-2 (COX-2).

Assessment of correlation of periodontitis in teeth adjacent to implant and peri- implantitis.

Aims: The present study was conducted to determine correlation between peri-implantitis and periodontitis in adjacent teeth.

Materials And Methods: The present study was conducted on 58 patients with 84 dental implants. They were divided into two groups, group I (50) was with peri-implantitis and group II (34) was without it.

The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor.

AT13387 is an orally bioavailable clinical candidate developed to inhibit theheat shock protein 90 (Hsp90). This article describes a modified synthetic route for the multi-gram production of AT13387 in 46% overall yield. The modified synthetic route is short, avoids stringent reaction conditions and difficult purifications, which led to increase in an overall yield.

Analysis of chain length, substitution patterns, and unsaturation of AM-404 derivatives as 20S proteasome stimulators.

Proteasome-mediated degradation of proteins is a vital cellular process and is performed by the ubiquitin-dependent proteasome system (UPS) and the ubiquitin-independent proteasome system (UIPS). While both systems are necessary to maintain healthy cell function, many disease states are characterized by reduced activity of the UPS, and the UIPS cannot by itself maintain proper protein levels. It has been suggested that the 20S core particle (20S CP), the isoform of the proteasome in the UIPS that can degrade proteins without a ubiquitin tag, can be stimulated with a small molecule to assist the 20S CP to accept and hydrolyze substrates more rapidly.

Glutathione S-Transferase π-Activatable O-(Sulfonylethyl Derived) Diazeniumdiolates Potently Suppress Melanoma in Vitro and in Vivo.

A group of glutathione S-transferase π (GSTπ) activatable O-(sulfonylethyl derived) diazeniumdiolates 5-12 were designed and synthesized. These compounds could be activated by GSTπ to initiate the β-elimination reaction, liberating an active vinyl sulfone-based GSH derivative and a diazeniumdiolate anion which subsequently releases NO in situ. The most active compound 6 released relatively high levels of NO and inhibited proliferation of melanoma B16 cells, superior to a diazeniumdiolate-based anticancer agent JS-K (1).

Assessment of Root Resorption and Root Shape by Periapical and Panoramic Radiographs: A Comparative Study.

Introduction: One of the common findings encountered by the clinician at the end of orthodontic treatment is the apical root resorption. Root resorption occurs to various degrees. A severe form of root resorption is characterized by shortening of root for more than 4 mm or more than one-third of the total tooth length.

Denture identification using individual national identification number of Saudi Arabia: An innovative inclusion method of casted metal.

Context: Forensic odontology is one of the branches of dentistry, which played a very important role in identification of individuals in accident, natural and mass disaster, and civil unrest and in genocide crimes. In the absence of natural teeth, marking or labeling of denture plays a vital role in the personal identification.

Background: Various types of marking or labeling methods are reported.

The Evolution of Computer-Assisted Total Hip Arthroplasty and Relevant Applications.

In total hip arthroplasty (THA), the accurate positioning of implants is the key to achieve a good clinical outcome. Computer-assisted orthopaedic surgery (CAOS) has been developed for more accurate positioning of implants during the THA. There are passive, semi-active, and active systems in CAOS for THA.

In situ click chemistry generation of cyclooxygenase-2 inhibitors.

Cyclooxygenase-2 isozyme is a promising anti-inflammatory drug target, and overexpression of this enzyme is also associated with several cancers and neurodegenerative diseases. The amino-acid sequence and structural similarity between inducible cyclooxygenase-2 and housekeeping cyclooxygenase-1 isoforms present a significant challenge to design selective cyclooxygenase-2 inhibitors. Herein, we describe the use of the cyclooxygenase-2 active site as a reaction vessel for the in situ generation of its own highly specific inhibitors.

Assessment of Various Nutritional Parameters in Geriatric Patients Who underwent Different Prosthodontic Treatments.

Background: Some relation exists between oral and general health with progressive aging. Certain risk factors are common between oral and systemic diseases. Absence of teeth also affects the oral health by altering the quality of life.