Evaluation of Analgesic Efficacy of Dexmedetomidine as an Adjuvant to Local Anaesthesia in Maxillofacial Soft Tissue Injuries: A Prospective Randomised Clinical Trial.

Aims And Objectives: Dexmedetomidine is a relatively new, potent, and highly selective α2-adrenergic receptor agonist used for perioperative sympatholytic, analgesia, and sedation. We conducted this study to evaluate the effects of dexmedetomidine as an adjunct to local anaesthesia for maxillofacial soft tissue injuries as day care in the emergency department on patient hemodynamics and analgesic efficacy.

Materials And Methods: Eighty patients gave informed consent to participate in the study.

Pharmacological Evaluation of Bakuchiol From Psoralea corylifolia L. as Potent Antimicrobial Agent Against Staphylococcus aureus.

The surge in multidrug resistance in Staphylococcus aureus is the pressing need to identify novel alternatives to combat antimicrobial resistance effectively. Bakuchiol is a bioactive prenylated phenolic meroterpene largely abundant in the seeds of Psoralea corylifolia. In this study, we present the biological assessment of bakuchiol derived from P.

Prioritization before dereplication, an effective strategy to target new metabolites in whole extracts: ghosalin from root.

Re-discovery of known metabolites is a common challenge in natural product-based drug discovery, and to avoid re-discovery, dereplication has been proposed for identifying known metabolites at the early stage of isolation. A majority of methods use LCMS to profile the extract and ignore the known mass. LC-HRMS profiling may generate a long mass list of metabolites.

An Optimized Method for LC-MS-Based Quantification of Endogenous Organic Acids: Metabolic Perturbations in Pancreatic Cancer.

Accurate and reliable quantification of organic acids with carboxylic acid functional groups in complex biological samples remains a major analytical challenge in clinical chemistry. Issues such as spontaneous decarboxylation during ionization, poor chromatographic resolution, and retention on a reverse-phase column hinder sensitivity, specificity, and reproducibility in multiple-reaction monitoring (MRM)-based LC-MS assays. We report a targeted metabolomics method using phenylenediamine derivatization for quantifying carboxylic acid-containing metabolites (CCMs).

Exploring the cytotoxic potential of biflavones of Araucaria cunninghamii: Precise identification combined by LC-HRMS-metabolomics and database mining, targeted isolation, network pharmacology, in vitro cytotoxicity, and docking studies.

The leaves of Araucaria cunninghamii are known to be nonedible and toxic. Previous studies have identified biflavones in various Araucaria species. This study aimed to investigate the in vitro cytotoxicity of the isolated compounds from Araucaria cunninghamii after metabolomics and network pharmacological analysis.

Penning micro-trap for quantum computing.

Trapped ions in radio-frequency traps are among the leading approaches for realizing quantum computers, because of high-fidelity quantum gates and long coherence times. However, the use of radio-frequencies presents several challenges to scaling, including requiring compatibility of chips with high voltages, managing power dissipation and restricting transport and placement of ions. Here we realize a micro-fabricated Penning ion trap that removes these restrictions by replacing the radio-frequency field with a 3 T magnetic field.

New ring-A modified cycloartane triterpenoids from Dysoxylum malabaricum bark: Isolation, structure elucidation and their cytotoxicity.

The Genus Dysoxylum (Meliaceae) consists of approximately 80 species that are abundant in structurally diverse triterpenoids. The present study focused on isolating new triterpenoids from the bark of Dysoxylum malabaricum, one of the predominant species of Dysoxylum present in India. The methanol-dichloromethane bark extract was subjected to LCMS profiling followed by silica gel column chromatography and HPLC analysis to target new compounds.

Identifying inflammation-related targets of natural lactones using network pharmacology, molecular modeling and approaches.

Natural lactones have been used in traditional and folklore medicine for centuries owing to their anti-inflammatory properties. The study uses a multifaceted approach to identify lead anti-inflammatory lactones from the SISTEMATX natural products database. The study analyzed the natural lactone database, revealing 18 lactones linked to inflammation targets.

Unveiling the healing properties of 2,3-dehydrosilychristin: a potential silymarin-derived flavonolignan from .

The compound 2,3-dehydrosilychristin, a flavonolignan linked to silychristin and silymarin, remains intriguing due to its challenging isolation from silymarin. While silymarin has been the exclusive source of flavonolignans - silybin, silychristin and silydianin - 2,3-dehydrosilychristin is reported in this study from Linn. leaves.

Isolation, Cytotoxicity, and In-silico Screening of Coumarins from Psoralea corylifolia Linn.

Psoralea corylifolia (syn. Cullen corylifolium), commonly called bawachi, is a medicinal plant extensively used for skin conditions like leukoderma, vitiligo, and psoriasis. It is notably rich in valuable bioactive compounds, particularly coumarins and furanocoumarins.

Mahamanalactone A, a new triterpenoid from bark: a case study for rapid identification of new metabolites via LC-HRMS profiling and database mining strategy.

In this recent investigation, the focus centred on exploring the potential phytoconstituents within the bark of . A profiling strategy employing LC-HRMS (Liquid Chromatography-High Resolution Mass Spectrometry) was implemented for the rapid identification of compounds from the bark extract. The crude extract underwent fractionation, resulting in the isolation of four previously known compounds () and a novel cycloartane triterpenoid named Mahamanalactone A ().

analysis, isolation, and cytotoxicity evaluation of the coumestans from (L.) Medik.

is well known for diverse phytoconstituents that possess multifaceted pharmacology, and one such less explored class is coumestans, which have not been well explored for their anticancer activities. One of the popular cancer targets is the Epidermal Growth Factor Receptor, a tyrosine kinase involved in various cancers, especially breast and lung cancer hence, a crucial cancer target. This work is focussed on molecular docking and molecular simulation studies on coumestans against EGFR.

New cycloartane triterpenoids from Dysoxylum malabaricum and their cytotoxic evaluation.

The cytotoxic dichloromethane-methanol bark extract of Dysoxylum malabaricum was subjected to bioassay-guided fractionation, followed by systematic dereplication to focus on the identification of new compounds. From the bark of Dysoxylum malabaricum, two new cycloartane-type triterpenoids were isolated in addition to two previously known triterpenoids. The structures and absolute configurations of the isolated compounds were elucidated unambiguously via NMR, HRESIMS data, and electronic circular dichroism calculations.

Phytochemical and Pharmacological Aspects of Psoralen - A Bioactive Furanocoumarin from Psoralea corylifolia Linn.

Since long ago, medicinal plants have played a vital role in drug discovery. Being blessed and rich in chemovars with diverse scaffolds, they have unique characteristics of evolving based on the need. The World Health Organization also mentions that medicinal plants remain at the center for meeting primary healthcare needs as the population relies on them.

Synthesis of amides directly from carboxylic acids and hydrazines.

The method for amide bond synthesis described here utilizes carboxylic acids and hydrazines in the presence of a catalytic amount of ZnCl. This is the first report that highlights the use of hydrazine as an amine partner for amide synthesis directly with carboxylic acids. Ammonia (gas) is the only by-product in this method.

Indole derivatives targeting colchicine binding site as potential anticancer agents.

Microtubules are appealing as intracellular targets for anticancer activity due to their importance in cell division. Three important binding sites are present on the tubulin protein: taxane, vinca, and colchicine binding sites (CBS). Many USFDA-approved drugs such as paclitaxel, ixabepilone, vinblastine, and combretastatin act by altering the dynamics of the microtubules.

Rottlerin renders a selective and highly potent CYP2C8 inhibition to impede EET formation for implication in cancer therapy.

CYP2C8 is a crucial CYP isoform responsible for the metabolism of xenobiotics and endogenous molecules. CYP2C8 converts arachidonic acid to epoxyeicosatrienoic acids (EETs) that cause cancer progression. Rottlerin possess significant anticancer actions.

A machine learning-based KNIME workflow to predict VEGFR-2 inhibitors.

Vascular endothelial growth factors (VEGFs) are specific cytokines involved in angiogenesis and do so via binding to vascular endothelial growth factor receptors (VEGFRs), a type of receptor tyrosine kinase. VEGFs are reported to facilitate angiogenesis in physiological (embryogenesis) and pathological (tumor) conditions. The overexpression of VEGFs and consequently VEGFRs is reported in tumorigenic conditions.

The genus Leucas: A review on phytochemistry and pharmacological activities.

Genus Leucas (family Lamiaceae) has been used as the traditional medicine for the treatment of a variety of disorders like skin diseases, diabetes, rheumatic pain, wounds, snake bites, etc. Several species of genus Leucas have been explored for their pharmacological activities and found to possess diverse properties like antimicrobial, antioxidant, anti-inflammatory, cytotoxic and anticancer, antinociceptive, antidiabetic, antitussive, wound healing, phytotoxic, etc. Phytochemical investigations of the different plant parts of Genus Leucas have revealed the presence of phytochemicals including terpenoids, flavonoids, lignans, phenolic glycosides, sterols, and essential oils.

Isolation of a new cytotoxic colchinoid from roots.

A new colchinoid compound, identified as -deacetyl--formylcornigerine (), named glorigerine was isolated from the roots of , along with two known compounds. The structures of isolated compounds were elucidated by 1 D and 2 D NMR and HRMS experiments. Glorigerine () differed from cornigerine () by the presence of an -formyl group instead of the -acetyl group.

LCMS-DNP based dereplication of Mudie gum-resin: identification of new cytotoxic labdane diterpene.

As a part of natural defense, plants initiate the secretion of gum containing numerous pharmacologically active essential metabolites. A fraction of such gum-resin from Mudie, when screened against human cancer cell lines, was found to be active. Further, it was subjected to an LCMS-DNP (Dictionary of Natural Products) based dereplication study followed by a detailed phytochemical investigation to obtain pure metabolites.

Natural products as a source of cytotoxic warheads in antibody-drug conjugates.

Antibody-drug conjugates (ADCs) are one of the most rapidly expanding classes of oncology therapeutics. Till now, 11 ADCs have been approved by USFDA, with the first ADC approval of gemtuzumab ozogamicin (Mylotarg) in 2000. A large number of ADCs are being evaluated in different stages of clinical trials and pre-clinical studies.

Correction: Chrysomycins A-C, antileukemic naphthocoumarins from .

[This corrects the article DOI: 10.1039/C3RA42884B.].