Evaluation of HPLC Profile, Antioxidant, Quorum Sensing, Biofilm, Swarming Motility, and Enzyme Inhibition Activities of Conventional and Green Extracts of .

The current study aims to prepare a green extract using a new method in addition to conventional extraction methods including; methanolic and ultrasonic extraction of , to compare their phenolic composition utilizing high-performance liquid chromatograph equipped with a diode array detector (HPLC-DAD), anti-bacterial, anti-oxidant, and enzyme inhibition activities. The results of HPLC-DAD analysis showed that Rosmarinic acid was found the highest amount in the methanolic extract followed by ultrasonic and green extracts as 169.7 ± 0.

Evaluation of the Ameliorative Potential of 3,5-(2-hydroxyethyl)-1,3,5-thiadiazinane-2-thione against Scopolamine-Induced Alzheimer's Disease.

Alzheimer's disease (AD) is the most common neurodegenerative disorder, marked by cognitive impairment. Currently, the available treatment provides only symptomatic relief and there is a great need to design and formulate new drugs to stabilize AD. In the search for a new anti-Alzheimer's drug, 3,5-(2-hydroxyethyl)-1,3,5-thiadiazinane-2-thione (THTT), a tetrahydro-2H-1,3,5-thiadiazine-2-thione derivative, was investigated against a scopolamine-induced Alzheimer's model.

Identification of Novel Antileishmanial Chemotypes By High-Throughput Virtual and In Vitro Screening.

Background: Leishmaniasis is a deadly protozoan parasitic disease and a significant health problem in underdeveloped and developing countries. The global spread of the parasite, coupled with the emergence of drug resistance and severe side effects associated with existing treatments, has necessitated the identification of new and potential drugs.

Objective: This study aimed to identify promising compounds for the treatment of leishmaniasis by targeting two essential enzymes of Leishmania donovani: trypanothione reductase (Try-R) and trypanothione synthetase (Try-S).

Removal of hydrocarbon pollutants from refinery wastewater using N-hexadecylchitosan as an efficient adsorptive platform.

The negative impact of refinery wastewater is of great concern to the aquatic, terrestrial, and aerial environment. In this study, N-hexadecylchitosan (NHDC) was successfully synthesized to deal with low mechanical strength, poor adsorption capacity, and limited selectivity of native chitosan. The NHDC was characterized by fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and X-Ray diffraction analysis (XRD) to study its composition, morphology, and structural attributes.

Potent bioactive metabolites from .

Seven known (-) and one new compound () were isolated and identified from the stem of . The species has been recognised as a new source for six of the known metabolites (, , , , , and ). Based on detailed spectroscopic analyses, these compounds were identified as scopoletin (), 8-ketosetosterol (), (+)-cycloolivil (), (+)-africanal (), isovanilic acid (), hydroxytyrosol acetate (), vanillic acid (), and cycloolivil A ().

Comparative assessment of phenolic composition profile and biological activities of green extract and conventional extracts of Salvia sclarea.

In recent years, there have been an attempt to develop safe and environmental friendly solvents to replace conventional solvents, and use for extraction bioactive compounds from natural sources. A current investigation involved the preparation of green, methanolic, and ultrasonic extracts of S. sclarea, and compared their phenolic profiling using HPLC-DAD, antibacterial, antioxidant, and enzyme inhibition activities.

Blocking the major inflammatory pathways by newly synthesized thiadiazine derivatives via in-vivo, in-vitro and in-silico mechanism.

A series of new thiadiazine derivatives including 2-(5-alkyl/aryl-6-thioxo-1,3,5-thiadiazinan-3-yl) propanoic acids (a) and 4-methyl-2-(5-alkyl/aryl-6-thioxo-1,3,5-thiadiazinan-3-yl) pentanoic acids (b) were synthesized by reacting primary alkyl/aryl amines with CS, followed by reaction with formaldehyde and amino acids. The chemical structures of synthesized compounds were confirmed by C- NMR and H- NMR techniques. The inhibitory potential of major inflammatory enzymes, COX-2 and 5-LOX was examined.

Thiadiazine thione derivatives as anti-leishmanial agents: synthesis, biological evaluation, structure activity relationship, ADMET, molecular docking and molecular dynamics simulation studies.

During last decades, 3,5-disubstituted-tetrahydro--thiadiazine-2-thione scaffold remains the center of interest due to their ease of preparation, diverse range substituents at N-3 and N-5 positions, and profound biological activities. In the current study, a series of 3,5-disubstituted-tetrahydro--thiadiazine-2-thiones were synthesized in good to excellent yield, and the structure of the compounds were confirmed by various spectroscopic techniques such as FTIR, H-NMR, C-NMR and Mass spectrometry, and finally evaluated against . Whereas, all the evaluated compounds (1-33), demonstrate potential leishmanicidal activities with IC values in the range of (1.

Involvement of the Opioidergic Mechanism in the Analgesic Potential of a Novel Indazolone Derivative: Efficacy in the Management of Pain, Neuropathy, and Inflammation Using and Approaches.

Indazolones possess interesting pharmacological activities. The search for indazole and indazolone-containing nuclei as drugs is an important research area of medicinal chemistry. The current work aims to evaluate a novel indazolone derivative against and targets of pain, neuropathy, and inflammation.

Thiadiazine-thione derivatives ameliorate STZ-induced diabetic neuropathy by regulating insulin and neuroinflammatory signaling.

Diabetes Mellitus is accompanied by chronic hyperglycemia, inflammation, and related molecular processes, which leads to diabetic neuropathy. In this work, we tested Thiadiazine-thione (TDT) synthetic derivatives TDT1 and TDT2 against streptozotocin (STZ)-induced diabetic neuropathy. Sprague Dawley's rats, SH-SY5Y neuronal and BV2 microglial cells were employed in this work, followed by behavioral, biochemical, and morphological studies utilizing RT-qPCR, ELISA, Immunoblotting, immunohistochemistry, Immunofluorescence, and in silico analyses.

One pot domino synthesis of new 3,5-disubstituted-tetrahydro-2H-1,3,5-thiadiazine-2-thiones (THTTs) as anti-inflammatory and antinociceptive candidates: A proof from in-vivo to in-vitro and in-silico mechanistic studies.

A series of alkyl/aryl/aralkylamines or amino acids appended tetrahydro-2H-1,3,5-thiadiazine-2-thiones (4a-i, 5a-g, 6 and 7) were synthesized via one pot domino synthesis. The synthesis involved reacting alkyl/aryl/aralkylamines or amino acids with carbon disulfide employing basic aqueous medium and further cyclization with formaldehyde and alkyl/aryl/aralkylamines or amino acids. In addition, the carboxy-functionalized 1,3,5-thiadiazine-2-thione 6 was further subjected to esterification.

Analagesic and Anti-Inflammatory Potentials of a Less Ulcerogenic Thiadiazinethione Derivative in Animal Models: Biochemical and Histochemical Correlates.

Purpose: Gastric ulcer induced by NSAIDs is the major medical concern and researchers are utilizing several approaches to combat this medical issue. In the current study, we investigated the efficacy of thiadiazinethione derivative (2,2'(2-thioxo-1,3,5-thiadiazinane-3,5-diyl) diacetic acid, as new less ulcerogenic compound.

Methods: 2,2'(2-thioxo-1,3,5-thiadiazinane-3,5-diyl) diacetic acid was evaluated using standard animal models including hot plate, writhing test and formalin induced nociceptive models.

Antiproliferative activity of 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine thione (THTT) derivatives and evaluation as potential prodrug.

Four series of tetrahydro-2H-1,3,5-thiadiazine thione derivatives were screened for their in vitro antiproliferative activities against two human cancerous PC3 and HeLa cell lines. The cytotoxicity of all the compounds (series A-D) was also determined on mammalian mouse fibroblast 3T3 cells. Most of the compounds showed significant anticancer potential against both cancer cell lines within the range of IC = 6.

Isolation, Biological Evaluation, and Molecular Docking Studies of Compounds from (Royle) Graham Ex Baker.

The is one of the best anti-inflammatory, antioxidant, and anticancerous plant; therefore, the isolated chemical constituents, that is, scopoletin (), pinitol (), 2-propenoic acid, 3-(3,4-dihydroxyphenyl)-octacosyl ester (), betulin (), and β-sitosterol glucoside () were tested for these folklores. The structures of the isolated compounds were confirmed by H NMR, C NMR, 2D-NMR, and mass spectral data. The anti-inflammatory, anticancer, antiglycation, and antioxidant activities of compounds were evaluated using different assays.

Toxicological Evaluation of Novel Cyclohexenone Derivative in an Animal Model through Histopathological and Biochemical Techniques.

Toxicity studies were conducted to provide safety data of potential drug candidates by determining lethal and toxic doses. This study was designed for pre-clinical evaluation of novel cyclohexenone derivative with respect to the acute and sub-acute toxicity along with the diabetogenic potential. Acute and sub-acute toxicity were assessed after intraperitoneal (i.

Mechanistic evaluation of a novel cyclohexenone derivative's functionality against nociception and inflammation: An in-vitro, in-vivo and in-silico approach.

The synthesis of a novel cyclohexanone derivative (CHD; Ethyl 6-(4-metohxyphenyl)-2-oxo-4-phenylcyclohexe-3-enecarboxylate) was described and the subsequent aim was to perform an in vitro, in vivo and in silico pharmacological evaluation as a putative anti-nociceptive and anti-inflammatory agent in mice. Initial in vitro studies revealed that CHD inhibited both cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) enzymes and it also reduced mRNA expression of COX-2 and the pro-inflammatory cytokines TNF-α and IL-1β. It was then shown that CHD dose dependently inhibited chemically induced tonic nociception in the abdominal constriction assay and also phasic thermal nociception (i.

Synthesis of AgNPs coated with secondary metabolites of Acacia nilotica: An efficient antimicrobial and detoxification agent for environmental toxic organic pollutants.

This study concentrates on biosynthesis of Silver Nanoparticles (AgNPs) from stem extract of Acacia nilotica (A. nilotica). The reaction was completed at a temperature ~40-45 °C and time duration of 5 h.

Attenuation of vincristine-induced neuropathy by synthetic cyclohexenone-functionalized derivative in mice model.

Vincristine (VCR) is a well-known anticancer drug which frequently induced painful neuropathy and impairs the quality of life of patients. The present study was designed to investigate the alleviative potential of a novel cyclohexenone derivative (CHD), i.e.

Antileishmanial, insecticidal and phytotoxic potential of leaves and stems of Rumex nervosus Vahl.

Biological assays including; phytotoxicity, brine shrimp lethality, antileishmanial and insecticidal activities were carried out on crude methanolic extracts of stems and leaves of R. nervosus and their fraction namely; n-Hexane, CHCl3, EtOAc, and MeOH fractions. The highest significant phytotoxicty activity showed by chloroform, n-hexane fractions and crude extract of leaves, the growth regulation were (95%, 90% and 90%) respectively against Lemna minor, while ethyl acetate fraction and n-hexane fractions of stems displayed significant phytotoxicty (100% and 90%) respectively against Lemna minor at high dose (1000μg/ml).

3-D segmentation of lung nodules using hybrid level sets.

Lung nodule segmentation in CT images and its subsequent volume analysis can help determine the malignancy status of a lung nodule. While several efficient segmentation schemes have been proposed, only a few studies evaluated the segmentation's performance for large nodules. In this research, we contribute a semi-automatic system which is capable of performing robust 3-D segmentations on both small and large nodules with good accuracy.

Chemical composition and anticancer, antimicrobial and antioxidant activities of essential oil and methanol extract from .

Chemical composition, antioxidant, anticancer, and antimacrobial activities of essential oil obtained from leaves of has been evaluated here for the first time. GC/MS analysis reveals the presence of Palmitoleic Acid (28.35%) and Palmitic acid, (25.

Effects of temperature and storage on the antioxidant potential, polyphenols and Vitamin-C contents of azadirachta indica leave aqueous extract.

The aim of the study was to investigate the effects of effects of storage and temperature on the antioxidant potential, vitamin-C contents, total as well as selected individual phenolic acids and flavonoids of fresh aqueous leaves extract of Azadirachta Indica. The antioxidant activity of Azadirachta Indica leaves aqueous extract was determined by scavenging of DPPH free radical, while the phenolic compounds and vitamin-C contents by HPLC method. The analyses were carried out on crude extract of fresh leaves and after storage time of 1, 2 and 3 month at temperature of 20, 30 and 50°C.