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In this investigation, the chemical composition of the hydro-distilled essential oil (HD-EO), obtained from the fresh aerial parts (inflorescence heads (Inf), leaves (L), and stems (St)) of Conyza canadensis growing wild in Jordan was determined by GC/MS. Additionally, the methanolic extract obtained from the whole aerial parts of C. canadensis (CCM) was examined for its total phenolic content (TPC), total flavonoids content (TFC), DPPH radical scavenging activity, iron chelating activity and was then analyzed with LC-MS/MS for the presence of certain selected phenolic compounds and flavonoids. The GC/MS analysis of CCHD-EOs obtained from the different aerial parts revealed the presence of (2E, 8Z)-matricaria ester as the main component, amounting to 15.4% (Inf), 60.7% (L), and 31.6% (St) of the total content. Oxygenated monoterpenes were the main class of volatile compounds detected in the Inf-CCHD-EO. However, oils obtained from the leaves and stems were rich in polyacetylene derivatives. The evaluation of the CCM extract showed a richness in phenolic content (95.59 ± 0.40 mg GAE/g extract), flavonoids contents (467.0 ± 10.5 mg QE/ g extract), moderate DPPH radical scavenging power (IC50 of 23.75 ± 0.86 µg/mL) and low iron chelating activity (IC50 = 5396.07 ± 15.05 µg/mL). The LC-MS/MS profiling of the CCM extract allowed for the detection of twenty-five phenolic compounds and flavonoids. Results revealed that the CCM extract contained high concentration levels of rosmarinic acid (1441.1 mg/kg plant), in addition to caffeic acid phenethyl ester (231.8 mg/kg plant). An antimicrobial activity assessment of the CCM extract against a set of Gram-positive and Gram-negative bacteria, in addition to two other fungal species including Candida and Cryptococcus, showed significant antibacterial activity of the extract against S. aureus with MIC value of 3.125 µg/mL. The current study is the first phytochemical screening for the essential oil and methanolic extract composition of C. canadensis growing in Jordan, its antioxidant and antimicrobial activity. [ABSTRACT FROM AUTHOR]

Perampanel, a novel α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist, is registered for the adjunctive treatment of patients (aged ≥ 12 years) with refractory partial-onset seizures. A simple high-performance liquid chromatographic method fluorescence detection (HPLC-FLD) was developed to analyze perampanel in rats' plasma and validated for bioanalytical purposes. Rats' plasma (50 µL) was processed by microextraction packed sorbent (MEPS). The analytes were separated using a Hypersil Gold octadecyl silane column (250 × 4.6 mm internal diameter, 5 μm particle size) with isocratic elution. A mobile phase consisting of acetonitrile–methanol–water (275:275:450, v/v/v; containing 50 µL triethylamine and pH adjusted to 3.25 with orthophosphoric acid) was used in this analysis. The flow rate was 1.25 mL/min. Analytes were monitored at an excitation wavelength of 285 nm and an emission wavelength of 430 nm. The linearity range for this validated method was from 3.75 to 300 ng/mL. No endogenous peaks were found in the elution of analytes in drug-free rats' plasma. Intra- and inter-batch reproducibility studies demonstrated accuracy and precision within the acceptance criteria. The results indicate that the present method is simple, selective, reproducible, and suitable for the analysis of perampanel in small volume samples. The robustness of the method was accessed using MODDE® design of experiments software version 12.5. [ABSTRACT FROM AUTHOR]

Cancer is the second leading cause of the death worldwide. As per the reports published by WHO, the cases of cancer in the world will increase to 22 million by 2030. Many resources are investigated all around the world for developing preventive, diagnostic and therapeutic strategies for cancer. Malignant cells display metabolic changes because of genetic and epigenetic alterations as compared to normal cell. Heterocycles are the key structural feature of many anti-cancer drugs present in the market. Between 2010 to 2015, FDA approved anticancer drugs also contain heterocyclic rings in their structures. Their presence in anti-cancer drugs can be credited to their being extremely common in nature, with enormous cellular processes and mechanisms. This review throws light on several heterocyclic compounds containing nitrogen, sulphur and oxygen in their rings, possessing anticancer activity on different cell lines. A compiled data of heterocyclic rings will help in providing a new way towards future development of new compound for treatment of cancer. [ABSTRACT FROM AUTHOR]

The beneficial application of silver nanoparticles and biostimulants to increase crop yield and quality is a long-term strategy to achieve desired agricultural productions that are resilient to various biotic and abiotic challenges. This project aimed to evaluate the individual effects of silver nanoparticles (AgNPs), Ascophyllum nodosum (SEW), and Spirulina platensis (SP) on the growth and physiological responses of Santolina chamaecyparissus. S. chamaecyparissus plants were exposed to AgNPs (20, 40, and 60 mg L−1), SWE (0.5% and 1%), and SP (1%, 2%, and 3%). The finding indicates that the light-harvesting efficiency and plant photochemical capacity are not affected by most treatments except for 60 mg L−1 AgNPs. Furthermore, the pattern of H2O2 levels in leaves was significantly higher after AgNP, SP, and SEW treatments. In parallel, total phenolic production was at least accompanied by a burst in H2O2 levels. However, higher antioxidant activity compared to the control, is shown by the higher free-DPPH-radical inhibition that goes completely smoothly with lower H2O2 levels. Thus, the results of the present study showed that biostimulants overall improved the antioxidant activity of S. chamaecyparissus and induced variable detectable amounts of phenolic compounds in response to the concentrations of each biostimulant. [ABSTRACT FROM AUTHOR]

A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran- 3-yl)-2-(substituted)-acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg-1 body mass during 0.5-4 h, indicating their ability to prevent seizure spread at low doses. Relative to phenytoin, [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(cyclohexyl( methyl) amino)-acetamide] (5i) and [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4-methylpiperidin-1- yl)-acetamide] (5c) demonstrated comparable relative anticonvulsant potency of 0.74 and 0.72, respectively, whereas [(N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4-(furan-2-carbonyl)-piperazin-1-yl)-acetamide] (5f) exhibited the lowest relative potency of 0.16. The ALD50 of tested compounds ranged from 1.604 to 1.675 mmol kg-1 body mass. The ED50 of synthesized compounds ranged from 0.055 to 0.259 mmol kg-1 (~23.4 to 127.6 mg kg-1) body mass. The pharmacophore mapping of the examined compounds on standard drugs (phenobarbital, phenytoin, ralitolin and carbamazepine) strongly suggests that these compounds may exert their anticonvulsant activity via the same established mechanism as that of known drugs.