Reinvestigation of the Reaction of Phenacy lMalononitrile with Hydrazines under Solvent Conditions

Phenacylmalononitrile 3 reacts with hydrazine hydrate in refluxing dioxan to afford the iminopyridazine derivative 6 and the pyrazolo[3,4-c]pyridazine derivative 7.Compound 3 reacts also with phenylhydrazine in refluxing ethanol to afford the iminopyridazine derivative 11 along with the phenylhydrazone derivative 12. Compound 12 could be cyclized into the pyrazolo[3,4-c]pyridazine derivative 13 upon reflux with sodium ethoxide

A prospective, randomized therapeutic trial for schistosomal specific nephropathy

A prospective, randomized therapeutic trial for schistosomal specific nephropathy. In this work 26 patients with schistosomal specific nephropathy were randomly distributed among three groups. Group I cases were given anti-schistosomal drugs (oxamniquine and praziquantel), group II cases were given anti-schistosomal drugs plus prednisolone, and group III cases were given anti-schistosomal drugs plus cyclosporine. The schistosomal specificity of kidney lesions was assessed by detecting the schistosomal specific antigens (CAA and CCA) and antibodies deposited in the renal glomeruli of these patients. Patients who had another etiologic cause which may explain their kidney disease were not admitted to this study. After initiation of the treatment, patients were followed up every other week in the outpatient clinic for 12 months. Follow-up showed complete remission of proteinuria in two cases in group II (duration of remission was 4 and 8 months) and in one case in group III (duration of remission was 6 months) but in none in group I. Partial remission was observed in one case in group I, in three cases in group II and in one case in group HI. During the observation period, improvement in kidney function was observed in two cases in group II but deterioration in kidney function was observed in one case in group I and in one other case in group III. We conclude that in patients with schistosomal nephropathy, none of the tried therapeutic regimens produce regression of the disease if given to patients with established disease

Biofunctional molecules from Citrullus colocynthis: An HPLC/MS analysis in correlation to antimicrobial and anticancer activities

Background: Citrullus colocynthis belongs to Family Cucurbitaceae. It grows widely in Egypt and Sudan and it has been used in folk medicine of Sudan and many other African countries as anti inflammatory, anti diabetic, and antioxidant agent. Objectives: To evaluate the antibacterial, antifungal, antiviral, anticancer activities of ethanolic crude extracts of the fruits, leaves, seeds and roots of this plant, as well as identifying them HPLC/MS. Materials and Methods: Dried fruits, seeds, leaves and roots of C. colocynthis were powdered and passed through a 40- mesh, then, the powders were extracted with 95% ethanol in a soxhlet apparatus. The residues were dried under reduced pressure in rotary evaporator. Crude extract from different plant parts were evaluated biologically and phytochemically. Results: All extracts showed good antifungal activities with inhibition zone ranges between 15.1 ± 0.32 to 25.6 ± 0.16 mm. In terms of plant organ, fruits were the most active. In term of fungal strain Aspergillus fumigatus and Geotricum candidum were the most sensitive. Against tested Gram +ve, all extracts showed good activities except roots, while antibacterial activity against Gram –ve showed that the fruits extract have good activity as it was the sole extract with activity against Pseudomonas aeruginosa. Test for antiviral activities showed moderate to weak inhibitions of cytopathic effect (CPE). Anticancer activities of different crude extracts showed that fruits had significant antitumor activities against all tested cell lines, the IC50 values were 24.6, 16, 18.5 and 19.7 µg /ml for HCT-116, MCF-7, Hep-G2 and Caco-2 respectively. Seeds extract was only active on HCT-116 and Hep G2 with IC50 =21.2 µg/ml for HCT-116 and 22.4 µg/ml for Hep G2. Leaves extract was only active against Hep G2 cancer cell line with IC50 19.7 µg/ml. Roots extract show weak antitumor activity on tested cell lines (IC50 values > 30µg/ml). HPLC/MS qualitative and quantitative analysis of different organs extracts revealed the presence of 21 compounds identified as fourteen cucurbitacins, three flavonoids, three tannins, and one sterol. The presence of cucurbitacins can explain most of the biological activities. Conclusion: The biological activities of colocynth different parts are due to the presence of secondary metabolites mainly cucurbitacins in addition to flavonoids and tannins.  These activities prove the use of this plant in folk medicine and deserve much more future exploration targeting their discovery in unexplored sources and their derivatives for improving their anticancer and antimicrobial abilities. Keywords: Citrullus colocynthis, crude extracts, antifungal, antibacterial, antiviral, anticancer, HPLC/M

Serum calprotectin as a diagnostic marker of late onset sepsis in full-term neonates

Background: Calprotectin, a complex of two calcium-binding proteins that belong to the S100 protein family, is abundant in the cytosolic fraction of neutrophils. A high level of calprotectin reportedly exists in extracellular fluid during various inflammatory conditions, but its role in neonatal sepsis was investigated only in one study as a marker of sepsis in very low birth weight neonates. Objective: This study aimed to measure the serum calprotectin level by ELISA in full-term neonates with late onset neonatal sepsis, its correlations with other laboratory markers of sepsis as interleukin-6, C-reactive protein (CRP), total leucocytic count and platelet count and its relation to the outcome of cases. Methods: This study comprised 48 full-term neonates with gestational ages of 37 to 42 weeks with manifestations of late onset neonatal sepsis admitted to the neonatal intensive care unit, Minia University Hospital during the period from February, 2011 to December, 2011 and 40 healthy neonates, age and sex matched as a control group. Serum levels of calprotectin, IL6 and CRP were measured for all neonates recruited in this study. Results: Serum calprotectin levels were significantly higher in term neonates with late onset neonatal sepsis than controls (3.77±1.85 μg/ml and 0.70±0.33 μg/ml respectively, P-value = 0.000). Cases with positive blood cultures and poor outcomes had the highest levels of calprotectin (5.8±0.61 μg/ml and 6.1±0.42 μg/ml respectively). Significant positive correlations were found between calprotectin levels and IL6 (P-value =0.000, r=0.92), C-reactive protein (p=0.000,r=0.95) and total leucocytic count (P-value =0.000, r=0.72), and negative correlations were found between its level and platelet count (P-value =0.000, r=-0.87), gestational age (P-value =0.014, r=-0.35) and body weight (P-value=0.018, r=-0.34). No significant differences were observed between males and females as regards calprotectin levels (3.96±2.10 μg/ml vs 3.55±1.52 μg/ml, P-value=0.444). Conclusions: Serum calprotectin levels are significantly higher in full-term neonates with late onset neonatal sepsis. Its levels correlated well with other laboratory markers of sepsis and neonatal mortality. It is a sensitive diagnostic marker for late onset neonatal sepsis.Keywords: Calprotectin, IL6, Full-term, Late-onset sepsisEgypt J Pediatr Allergy Immunol 2012;10(1):19-2

Induction of Biologically Active Flavonoids in Cell Cultures of Morus nigra and Testing their Hypoglycemic Efficacy

The antidiabetic activity of both leaves and MJ-treated cell cultures of Morus nigra was evaluated after their oral administration to streptozotocin-induced diabetic rats. The antidiabetic activity of extracts from leaves given to streptozotocin (STZ)-diabetic rats for 10 days increased with increasing doses of leaves extract up to 500 mg/kg/day. The administration of 500 mg/kg/day of leaves extract reduced the concentration of glucose from 370 ± 7.31 mg/dl (control) to 154 ± 6.27 mg/dl, and a significant increase in the insulin level from 11.3 ± 0.31 μU/ml (control) to 14.6 ± 0.43 μU/ml was recorded. Cell suspension cultures were established from the young leaves of Morus nigra cultivated on modified MS medium supplemented with 2.0 mg/l 1-naphthaleneacetic acid (NAA), 0.2 mg/l 6-(furfurylamino)purine (kinetin). The changes in cell weight and flavonoid content were monitored between day zero and 12. The linear increase in fresh weight was found to be parallel to flavonoids production. Cell cultures treated with 100 μM methyl jasmonate for 24 hours showed a noticeable increase in level of flavonoids and significant and more effective hypoglycemic activity than that for extract from leaves. The major flavonoids were isolated by TLC and HPLC and identified as rutin, quercetin, Morusin and cyclomorusin by co-chromatography and mass spectrometry in comparison to samples of authentic reference compounds

Design, synthesis and antitumor evaluation of novel pyrazolopyrimidines and pyrazoloquinazolines

A series of N-aryl-7-aryl-pyrazolo[1,5-a]pyrimidines 18a–u and N-aryl-pyrazolo[1,5-a] quinazolines 25a–c were designed and synthesized via the reaction of 5-aminopyrazoles 11a–c with enaminones 12a–g or 19, respectively. The new compounds were screened for their in vitro antitumor activity toward liver (HepG-2) and breast (MCF-7) human cancer cells using 3-[4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide MTT assay. From the results, it was found that all compounds showed dose-dependent cytotoxic activities against both HepG-2 and MCF-7 cells. Two compounds 18o and 18a were selected for further investigations. Cell cycle analysis of liver (HepG-2) cells treated with 18o and breast (MCF-7) cells treated with 18a showed cell cycle arrest at G2/M phase and pro-apoptotic activity as indicated by annexin V-FITC staining.publishedVersio

C–O isotope geochemistry of the Florida phosphate of Four Corners and Hardee County mines, USA: Implication for genesis and diagenesis

© 2017 Elsevier B.V. The study area located in Florida, USA and emphasized on low-grade phosphorites in Hardee County (HC) and Four Corners (FC) mining areas. The main purpose of this study is to apply a standard geochemical technique to understand the diagenetic history and paleo-environmental aspects of phosphates within one of the major phosphate deposits in the USA. The effect of diagenesis on the phosphate minerals was studied by isotope analysis of the phosphate bone fragments and phosphatized mudclasts and rods. The environmental conditions that prevailed during the life of organisms were assessed by isotope analysis of the shark teeth. In this paper, variation in stable isotope (δ18O and δ13C) signatures of structural carbonate in rocks and shark teeth were studied in Florida phosphate. The studied samples show negative values for both δ13C and δ18O isotopes of structural carbonate. The light mudclast samples shows higher oxygen ratios (− 1.6) than the dark mudclasts (− 2.3) in Hardee County, whereas those values were lower, − 2.3 and − 3, respectively, in Four Corners samples. The shark teeth found in the deposits show narrow variations in values of δ13C (− 3.4 to − 4.9%o) and δ18O (− 1.4 to 2.1%o) isotope. The bone fragments in the deposits are more similar to the light mudclasts regarding the isotope ratios and carbonate content. The alteration is evident in the Florida phosphorites where δ18O values of bulk teeth are higher than those of bones and mudclast. This alteration could be because of increasing crystallinity and decreasing carbonate content with increasing depth of burial

Calli Essential Oils Synergize with Lawsone against Multidrug Resistant Pathogens.

The fast development of multi-drug resistant (MDR) organisms increasingly threatens global health and well-being. Plant natural products have been known for centuries as alternative medicines that can possess pharmacological characteristics, including antimicrobial activities. The antimicrobial activities of essential oil (Calli oil) extracted from the Calligonum comosum plant by hydro-steam distillation was tested either alone or when combined with lawsone, a henna plant naphthoquinone, against MDR microbes. Lawsone showed significant antimicrobial activities against MDR pathogens in the range of 200-300 µg/mL. Furthermore, Calli oil showed significant antimicrobial activities against MDR bacteria in the range of 180-200 µg/mL, Candida at 220-240 µg/mL and spore-forming Rhizopus fungus at 250 µg/mL. Calli oil's inhibition effect on Rhizopus, the major cause of the lethal infection mucormycosis, stands for 72 h, followed by an extended irreversible white sporulation effect. The combination of Calli oil with lawsone enhanced the antimicrobial activities of each individual alone by at least three-fold, while incorporation of both natural products in a liposome reduced their toxicity by four- to eight-fold, while maintaining the augmented efficacy of the combination treatment. We map the antimicrobial activity of Calli oil to its major component, a benzaldehyde derivative. The findings from this study demonstrate that formulations containing essential oils have the potential in the future to overcome antimicrobial resistance