2-PMAP Ameliorates Cerebral Vasospasm and Brain Injury after Subarachnoid Hemorrhage by Regulating Neuro-Inflammation in Rats

A subarachnoid hemorrhage (SAH), leading to severe disability and high fatality in survivors, is a devastating disease. Neuro-inflammation, a critical mechanism of cerebral vasospasm and brain injury from SAH, is tightly related to prognoses. Interestingly, studies indicate that 2-[(pyridine-2-ylmethyl)-amino]-phenol (2-PMAP) crosses the blood–brain barrier easily. Here, we investigated whether the vasodilatory and neuroprotective roles of 2-PMAP were observed in SAH rats. Rats were assigned to three groups: sham, SAH and SAH+2-PMAP. SAHs were induced by a cisterna magna injection. In the SAH+2-PMAP group, 5 mg/kg 2-PMAP was injected into the subarachnoid space before SAH induction. The administration of 2-PMAP markedly ameliorated cerebral vasospasm and decreased endothelial apoptosis 48 h after SAH. Meanwhile, 2-PMAP decreased the severity of neurological impairments and neuronal apoptosis after SAH. Furthermore, 2-PMAP decreased the activation of microglia and astrocytes, expressions of TLR-4 and p-NF-κB, inflammatory markers (TNF-α, IL-1β and IL-6) and reactive oxygen species. This study is the first to confirm that 2-PMAP has vasodilatory and neuroprotective effects in a rat model of SAH. Taken together, the experimental results indicate that 2-PMAP treatment attenuates neuro-inflammation, oxidative stress and cerebral vasospasm, in addition to ameliorating neurological deficits, and that these attenuating and ameliorating effects are conferred through the TLR-4/NF-κB pathway.

Green Synthesis of Surfactant Capped CTAB@Ag Nanoparticles and Study of Its Catalytic Activity

In the present study, ginger extract, which is widely available as a medicinal herb, is used to develop a facile method for green synthesis of bare Ag and surfactant capped CTAB@Ag nanoparticles via Hydrothermal route. The as-prepared Ag nanoparticles were characterized by UV-Vis spectroscopy, photoluminescence (PL), X-ray Diffraction (XRD), Infrared spectroscopy (IR), and Scanning electron microscopy (SEM). The catalytic properties of as prepared bare and surfactant capped CTAB@Ag nanoparticles were also investigated in reductive degradation of Methyl Orange (MO) dye and 4-Nitrophenol (4-NP). Surfactant-capped CTAB@Ag nanoparticles exhibit superior catalytic properties in the degradation of MO and conversion of 4-nitro phenol to 4-amino phenol when compared to bare silver nanoparticles.

Optimization of 4-Anilinoquinolines as Dengue Virus Inhibitors

Emerging viral infections, including those caused by dengue virus (DENV) and Venezuelan Equine Encephalitis virus (VEEV), pose a significant global health challenge. Here, we report the preparation and screening of a series of 4-anilinoquinoline libraries targeting DENV and VEEV. This effort generated a series of lead compounds, each occupying a distinct chemical space, including 3-((6-bromoquinolin-4-yl)amino)phenol (12), 6-bromo-N-(5-fluoro-1H-indazol-6-yl)quinolin-4-amine (50) and 6-((6-bromoquinolin-4-yl)amino)isoindolin-1-one (52), with EC50 values of 0.63–0.69 µM for DENV infection. These compound libraries demonstrated very limited toxicity with CC50 values greater than 10 µM in almost all cases. Additionally, the lead compounds were screened for activity against VEEV and demonstrated activity in the low single-digit micromolar range, with 50 and 52 demonstrating EC50s of 2.3 µM and 3.6 µM, respectively. The promising results presented here highlight the potential to further refine this series in order to develop a clinical compound against DENV, VEEV, and potentially other emerging viral threats.

Evaluation of the Anticancer and DNA-Binding Characteristics of Dichloro(diimine)zinc(II) Complexes

Several metal diimine complexes have been reported to possess anticancer properties. To evaluate the anticancer properties of tetrahedral zinc(II) diimine complexes, six complexes were synthesized with the general formula M(N^N)Cl2 {where M = Zn, Pt and N^N = 2,2’-biquinoline (1), 2,2’-dipyridylketone (2) and 4-((pyridine-2-ylmethylene)amino)phenol (3)}. In general, the intrinsic DNA-binding constants for the different compounds exhibited values within close proximity; the changes in the viscosity of the CT-DNA upon binding to the compounds suggest intercalation-binding mode. Molecular docking study predicted that complexes containing the highly planar ligand 2,2’-biquinoline are capable to establish π–π interactions with nucleobases of the DNA; the other four complexes engaged in donor–acceptor interactions with DNA nucleobases. The six complexes and two reference drugs (cisplatin and sunitinib) were tested against two cancer cell lines (COLO 205 and RCC-PR) and one normal cell line (LLC-MK2), highlighting the better performance of the zinc(II) complexes compared to their platinum(II) analogues. Moreover, zinc(II) complexes have higher selectivity index values than the reference drugs, with promising anticancer properties.

GC-MS Analysis of Bioactive Compounds in Lemongrass (Cymbopogon citratus) Powder

The bioactive components of lemongrass powder have been evaluated using GC-MS. The GC-MS analysis was performed on GC-MS comprising an automatic liquid sampler and agilent gas chromatograph interfaced to mass spectrometer (GC-MS). Interpretation of the mass spectrum GC-MS was conducted using the database of National Institute Standard and Technology (NIST). The compound bioactivity prediction is based on Dr. Duke’s phytochemical and ethnobotanical Database. GC/MS analysis of methanolic extract of lemongrass leaves revealed the existence of Pentane, 2,4-Dimethyl, Dodecanoic acid tert-butyl ester, 2,6 Bis (1,1-dimethylethyl)-4-[(4-chloro-6-(3,5, bis (1,1-dimethylethyl)-4- hydroxyanilino)-1,3,5-triazin-2-yl)amino]phenol and 3-Formyl-4,5-dimethyl-pyrrole. The presence of these compounds in the plant extract may at least be responsible for the pharmacological properties of Cymbopogon citratus and thus recommended as plant of phytopharmaceutical importance.

Design, Synthesis of a Novel Banana-Shaped Compounds via Esterification

Schiff's Bases were synthesized from the reaction of p-amino benzoic acid and alkoxybenzaldehyde in absolute ethanol and reacted with (E)-3-((4-hydroxybenzylidene) amino) phenol used DCC (N,N'-Dicyclocarbodiimide) and DAMP (4-(Dimethylamino) pyridine ) to 3-(((E)-4-((4-(((E)-4 alkoxy benzylidene) amino) benzoyl) oxy) benzylidene) amino) phenyl4- (E)- 4-alkoxy benzyli dene ) amino) benzoate. The structures of the products were confirmed by their melting points, FT-IR, 1HNMR spectra.

Studies on the Modification of Commercial Bisphenol-A-Based Epoxy Resin Using Different Multifunctional Epoxy Systems

The tensile fracture mechanics and thermo-mechanical properties of mixtures composed of two kinds of epoxy resins of different chemical structures and functional groups were studied. The base resin was a bi-functional epoxy resin based on diglycidyl ether of bisphenol-A (DGEBA) and the other resins were (a) distilled triglycidylether of meta-amino phenol (b) 1, 6–naphthalene di epoxy and (c) fluorene di epoxy. This research shows that a small number of multifunctional epoxy systems, both di- and tri-functional, can significantly increase tensile strength (14%) over neat DGEBA while having no negative impact on other mechanical properties including glass transition temperature and elastic modulus. In fact, when compared to unmodified DGEBA, the tri-functional epoxy shows a slight increase (5%) in glass transition temperature at 10 wt.% concentration. The enhanced crosslinking of DGEBA (90 wt.%)/distilled triglycidylether of meta-amino phenol (10 wt.%) blends may be the possible reason for the improved glass transition. Finally, the influence of strain rate, temperature and moisture were investigated for both the neat DGEBA and the best performing modified system. The neat DGEBA was steadily outperformed by its modified counterpart in every condition.

Condensation Product of 5-Bromosalicylaldehyde and Amino Phenol: Fluorescence Sensor for Ascorbic Acid and AND Logic Gate

Condensation product of 5-bromosalicylaldehyde and aminophenol (L) has been synthesised and characterised. Fluorescence of L enhances by 23 times on interaction with Ce3+ while it is quenched completely by Ce4+. Ascorbic acid (AA) is a well known strong reducing agent and this property has been used to act L:Ce4+ adduct as a fluorescence “on” sensor for AA. AA reduces Ce4+ into Ce3+ and thereby increasing fluorescence of L due to the formation of L:Ce3+ adduct. Molecules which generally coexist with AA viz. Cholesterol, Glucose, Sucrose and Dopamine found not to interfere. The interaction of L with Ce3+, Ce4+ and subsequently with AA has been verified with cyclic voltammetry.

Acute liver injury following acetaminophen administration does not activate atrophic pathways in the mouse diaphragm

N-acetyl-para-amino phenol (APAP, usually named paracetamol), which is commonly used for its analgesic and antipyretic properties may lead to hepatotoxicity and acute liver damage in case of overdoses. Released cytokines and oxidative stress following acute liver damage may affect other organs’ function notably the diaphragm, which is particularly sensitive to oxidative stress and circulating cytokines. We addressed this issue in a mouse model of acute liver injury induced by administration of APAP. C57BL/6J mice (each n = 8) were treated with N-acetyl-para-amino phenol (APAP) to induce acute drug caused liver injury and sacrificed 12 or 24 h afterwards. An untreated group served as controls. Key markers of inflammation, proteolysis, autophagy and oxidative stress were measured in diaphragm samples. In APAP treated animals, liver damage was proven by the enhanced serum levels of alanine aminotransferase and aspartate aminotransferase. In the diaphragm, besides a significant increase in IL 6 and lipid peroxidation, no changes were observed in key markers of the proteolytic, and autophagy signaling pathways, other inflammatory markers and fiber dimensions. The first 24 h of acute liver damage did not impair diaphragm atrophic pathways although it slightly enhanced IL-6 and lipid peroxidation. Whether longer exposure might affect the diaphragm needs to be addressed in future experiments.