Unsupervised Pattern Recognition Chemometrics for Distinguishing Different Egyptian Olive Varieties Using a New Integrated Densitometric Reversed-Phase High-Performance Thin-Layer Chromatography—Image Analysis Technique

JPC – Journal of Planar Chromatography – Modern TLC - The merits of chemometrics in categorizing different Egyptian olive chemovarieties based on their compositional integrity were...     

Microwave chemistry: Synthesis of purine and pyrimidine nucleosides using microwave radiation

Pyrimidine and purine nucleosides have a remarkable and comprehensive impact on medicinal chemistry and pharmaceutical industries. They become key parts of the growing interdisciplinary area of antimetabolites. The paramount importance of the nucleoside analogs triggered their broader use in treatment of critical diseases such as cancer, malignancies, microbial infection, and autoimmune diseases. Recent advances in their synthetic strategies through microwave-assisted organic synthesis (MAOS) have been reviewed.     

Electron Ionization Mass Spectra of Organophosphorus Compounds. Part III: Mass Spectrometric Fragmentation of Diethyl Spiro[Pyrimidino[5,3′][1,2]Oxazole] Phosphonate,Diethyl (Oxazolo[5,4-D]Pyrimidine-4,6-Dione)Phosphonate,and Diethyl (Pyrimidino[4,5-B][1,4]Oxazine)Phosphonate Derivatives

Abstract

Fragmentation pathways of 14 organophosphorus compounds derived from diethyl spiro[pyrimidino[5,3][1,2]oxazole] phosphonates, diethyl (oxazolo[5,4-d]pyrimidine-4,6-dione)phosphonates, and diethyl (pyrimidino[4,5-b][1,4] oxazine)phosphonates were investigated by electron impact mass spectrometry (EI-MS). The intensity of the recorded molecular ion peaks showed various values depending on the nature of the compounds. Characteristic fragment ions were formed by successive loss of simple functional groups followed by decomposition of heterocycles connected to pyrimidine rings.     

Regioselective Condensation of Alkylidenephosphoranes to N-Methoxy- and N-Anilino-1H isoindole-1,3-(2H)-diones

Treatment of 2-methoxyisoindoline-1,3-dione with resonance-stabilized alkylidenephosphoranes afforded the corresponding monoalkenes as the sole reaction product, in ～58–63% yields, whereas more than 80% yields of the same monoolefin products were obtained when the reactions were carried out under microwave conditions. Similarly, 2-(phenylamino)isoindoline-1,3-dione reacted under either thermal or microwave conditions to give only the corresponding monoalkene derivatives. The alkene products from both substrates were further reduced to the corresponding isoindoles using Zn-dust in EtOH. Prediction of the designed compounds and the in vivo anti-inflammation activity of the products in the rat adjuvant model were also studied. The work is the first demonstration of the anti-inflammatory activity of phthalimide derivatives.     

Synthesis and antiviral screening of 2-(propylthio)-7-substituted-thiazolo[5,4-d]pyrimidines as anti-bovine viral diarrhea virus agents

7-Chloro-2-(propylthio)thiazolo[5,4-d]pyrimidine 4 was prepared and used as a precursor for synthesizing new derivatives of thiazolo[5,4-d]pyrimidine through the nucleophilic displacement of the chlorine atom by different types of amino derivatives. Reaction of compound 4 with primary and secondary amines produced the corresponding substituted amino derivatives. Reaction of 4 with hydrazine hydrate then followed by condensation with aromatic aldehydes afforded hydrazone derivatives. Reaction of 4 with hydrazine hydrate then followed by reaction with isothiocyanates gave the disubstituted thiosemicarbazides. Finally, treatment of 4 with hydrazine derivatives afforded the novel disubstituted hydrazine derivatives. Preliminary antiviral screening on the bovine viral diarrhea virus (BVDV) was carried out, which was classified as a member of the same family of Hepatitis C virus. The results indicated that some of the tested compounds exhibited anti-BVDV activity which may be suitable for a new lead molecule to design more potent anti-BVDV agents.     

Momordica charantia Extract Protects against Diabetes-Related Spermatogenic Dysfunction in Male Rats: Molecular and Biochemical Study

More than 90% of diabetic patients suffer from sexual dysfunction, including diminished sperm count, sperm motility, and sperm viability, and low testosterone levels. The effects of Momordica charantia (MC) were studied by estimating the blood levels of insulin, glucose, glycosylated hemoglobin (HbA1c), testosterone (TST), follicle-stimulating hormone (FSH), and luteinizing hormone (LH) in diabetic rats treated with 250 and 500 mg/kg b.w. of the total extract. Testicular antioxidants, epididymal sperm characteristics, testicular histopathology, and lesion scoring were also investigated. Testicular mRNA expression of apoptosis-related markers such as antiapoptotic B-cell lymphoma-2 (Bcl-2) and proapoptotic Bcl-2-associated X protein (Bax) were evaluated by real-time PCR. Furthermore, caspase-3 protein expression was evaluated by immunohistochemistry. MC administration resulted in a significant reduction in blood glucose and HbA1c and marked elevation of serum levels of insulin, TST, and gonadotropins in diabetic rats. It induced a significant recovery of testicular antioxidant enzymes, improved histopathological changes of the testes, and decreased spermatogenic and Sertoli cell apoptosis. MC effectively inhibited testicular apoptosis, as evidenced by upregulation of Bcl-2 and downregulation of Bax and caspase-3. Moreover, reduction in apoptotic potential in MC-treated groups was confirmed by reduction in the Bax/Bcl-2 mRNA expression ratio.     

Isoshamixanthone: a new pyrano xanthone from endophytic Aspergillus sp. ASCLA and absolute configuration of epiisoshamixanthone

Abstract

Isoshamixanthone (1), a new stereoisomeric pyrano xanthone together with the previously known fungal metabolites, epiisoshamixanthone (2), sterigmatocystin (3), arugosin C (4), norlichexanthone (5), diorcinol (6), ergosterol and methyllinoleate, were obtained from the endophytic fungal strain Aspergillus sp. ASCLA isolated from leaf tissues of the medicinal plant Callistemon subulatus. The chemical structure of the new xanthone (1) was elucidated by extensive 1D, 2D NMR, and ESI HR mass measurements, and by comparison with literature data. The constitutions and absolute configurations of 1 and epiisoshamixanthone (2) were additionally confirmed by X-ray crystallography. Compounds 1,2 were evaluated for their potential anticancer activity using the human cervix carcinoma cell line (KB-3-1). The antimicrobial activities of the fungal extract and compounds 1,2 were studied using a panel of pathogenic microorganisms as well.     

Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity

New furan-based derivatives have been, designed, synthesized, and evaluated for their cytotoxic and tubulin polymerization inhibitory activities. DNA flow cytometric study of pyridine carbohydrazide 4 and N-phenyl triazinone 7 demonstrated G₂/M phase cell cycle disruptions. Accumulation of cells in the pre-G1 phase and positive annexin V/PI staining, which may be caused by degeneration or fragmentation of the genetic components, suggested that cell death occurs via an apoptotic cascade. Furthermore, compounds 4 and 7 had a strong pro-apoptotic impact through inducing the intrinsic mitochondrial mechanism of apoptosis. This mechanistic route was verified by an ELISA experiment that indicated a considerable rise in the levels of p53 and Bax and a drop in the level of Bcl-2 when compared with the control.     

Promoting Effect of Soluble Polysaccharides Extracted from Ulva spp. on Zea mays L. Growth

Seaweeds can play a vital role in plant growth promotion. Two concentrations (5 and 10 mg/mL) of soluble polysaccharides extracted from the green macroalgae Ulva fasciata and Ulva lactuca were tested on Zea mays L. The carbohydrate and protein contents, and antioxidant activities (phenols, ascorbic, peroxidase, and catalase) were measured, as well as the protein banding patterns. The soluble polysaccharides at 5 mg/mL had the greatest effect on the base of all of the parameters. The highest effects of soluble polysaccharides on the Zea mays were 38.453, 96.76, 4, 835, 1.658, 7.462, and 38615.19, mg/mL for carbohydrates, proteins, phenol, µg ascorbic/mL, mg peroxidase/g dry tissue, and units/g tissue of catalase, respectively. The total number of protein bands (as determined by SDS PAGE) was not changed, but the density of the bands was correlated to the treatments. The highest band density and promoting effect were correlated to 5 mg/mL soluble polysaccharide treatments extracted from Ulva fasciata in Zea mays, which can be used as a biofertilizer.