Dizajniranje i sinteza novih derivata tiofenkarbohidrazida, tienopirazola i tienopirimidina s antioksidativnim i antitumorskim djelovanjem

2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3a), 1-(5-amino-4-(4-chloro-3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3b), 1-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) pyrazolidine-3,5-dione (4), (Z)-N\u27-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl) formohydrazonic acid (5a), (Z)-ethyl-N\u27-(4-methyl-2-amino-5-acetylthiophene-3-carbonylformo hydrazonate (5b), 6-acetyl-3-amino-2,5-dimethylthieno2,3-dpyrimidin-4(3H)-one (8), 5-methyl-3-amino-2-mercapto-6-acetylthieno2,3-dpyrimidin-4(3H)-one (10) and 5-methyl-6-acetyl-2-thioxo-2,3-dihydrothieno2,3-dpyrimidin-4(1H)-one (12) as potential antioxidant and antitumor agents. Pharmacological results showed that compounds 6a, 6b, 8, 10 and 12 exhibited promising antitumor and antioxidant activity.Etilni ester 2-amino-5-acetil-4-metil-tiofen-3-karboksilne kiseline (1) i 5-acetil-2-amino-4-metiltiofen-3-karbohidrazid (2) sintetizirani su i upotrebljeni kao reaktanti u sintezi novih spojeva 1-(5-amino-4-(3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3a), 1-(5-amino-4-(4-klor-3,5-dimetil-1H-pirazol-1-karbonil)-3-metiltiofen-2-il) etanona (3b), 1-(4-metil-2-amino-5-acetiltiofen-3-karbonil) pirazolidin-3,5-diona (4), (Z)-N\u27-(4-metil-2-amino-5-acetiltiofen-3-karbonil) formohidrazonske kiseline (5a), (Z)-etil-N\u27-(4-metil-2-amino-5-acetiltiofen-3-karbonilformo hidrazonata (5b), 6-acetil-3-amino-2,5-dimetiltieno2,3-dpirimidin-4(3H)-one (8), 5-metil-3-amino-2-merkapto-6-acetiltieno2,3-dpirimidin-4(3H)-ona (10) i 5-metil-6-acetil-2-tiokso-2,3-dihidrotieno2,3-dpirimidin-4(1H)-ona (12) kao potencijalnih antioksidansa i citostatika. Farmakološka ispitivanja ukazuju na to da spojevi 6a, 6b, 8, 10 i 12 imaju značajno antitumorsko i antioksidativno djelovanje

Zingiber officinale acts as a nutraceutical agent against liver fibrosis

<p>Abstract</p> <p>Background/objective</p> <p><it>Zingiber officinale </it>Roscoe (ginger) (<it>Zingiberaceae</it>) has been cultivated for thousands of years both as a spice and for medicinal purposes. Ginger rhizomes successive extracts (petroleum ether, chloroform and ethanol) were examined against liver fibrosis induced by carbon tetrachloride in rats.</p> <p>Results</p> <p>The evaluation was done through measuring antioxidant parameters; glutathione (GSH), total superoxide dismutase (SOD) and malondialdehyde (MDA). Liver marker enzymes; succinate and lactate dehydrogenases (SDH and LDH), glucose-6-phosphatase (G-6-Pase), acid phosphatase (AP), 5'- nucleotidase (5'NT) and liver function enzymes; aspartate and alanine aminotransferases (AST and ALT) as well as cholestatic markers; alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), total bilirubin were estimated. Liver histopathological analysis and collagen content were also evaluated. Treatments with the selected extracts significantly increased GSH, SOD, SDH, LDH, G-6-Pase, AP and 5'NT. However, MDA, AST, ALT ALP, GGT and total bilirubin were significantly decreased.</p> <p>Conclusions</p> <p>Extracts of ginger, particularly the ethanol one resulted in an attractive candidate for the treatment of liver fibrosis induced by CCl₄. Further studies are required in order to identify the molecules responsible of the pharmacological activity.</p

Channel equalization for indoor lighting communications networks

We consider indoors communications networks using modulated LEDs to transmit the information packets. A generic indoor channel equalization formulation is proposed assuming the existence of both line of sight and diffuse emitters. The proposed approach is of relevance to emergent indoors distributed sensing modalities for which various lighting based network communications protocols are considered

Acquired air-filled lung cysts in childhood: pathogenesis of cysts of diverse etiologies; nuances of management

Background Air-filled pulmonary parenchymal cysts (pneumatoceles/PCs) – a pathological condition – involving the lung parenchyma may be congenital or acquired. In children, acquired cases are often caused by staphylococcal pneumonias, but other etiologies may also cause PCs and lead to diagnostic confusion.Objectives The aim of this study was to examine the natural history and clinicopathologic features of noncongenital, nonstaphylococcal PCs in children.Patients and methods Four children with nonstaphylococcal PCs were included in this study. A full history, clinical examination, relevant radiological and pathological findings, surgical intervention where relevant, and follow-up were analyzed.Results The cases described represent acquired PCs: one occurred after infarction following cardiac surgery, another was a subpleural pulmonary bleb of inflammatory origin, and the remaining two were post-traumatic pseudocysts. The inflammatory-process bleb and the postinfarction cysts presented with pneumothorax. The postinfarction and post-traumatic PCs responded to observation. The pulmonary bleb was excised.Conclusion Our understanding of the clinicopathologic features and pathogenesis of many types of acquired PCs is incomplete. We propose that PC formation has a basis in destruction of the distal airways of the lung. Damaged tissue may act as a valve, and cause air-trapping, which leads to PC formation. Cysts arising after infarction or after trauma usually resolve on observation. Subpleural blebs may require excision because of nonresolution and recurrence of pneumothorax

The Psychometric Properties of a Self-Administered, Open-Source Module for Valuing Metastatic Epidural Spinal Cord Compression Utilities.

INTRODUCTION: Web surveys are often used for utility valuation. Typically, custom utility valuation tools that have not undergone psychometric evaluation are used. OBJECTIVES: This study aimed to determine the psychometric properties of a metastatic epidural spinal cord compression (MESCC) module run on a customizable open-source, internet-based, self-directed utility valuation platform (Self-directed Online Assessment of Preferences [SOAP]). METHODS: Individuals accompanying patients to the emergency department waiting room in Ottawa, Canada, were recruited. Participants made SOAP MESCC health state valuations in the waiting room and 48 h later at home. Validity, agreement reliability, and responsiveness were measured by logical consistency of responses, smallest detectable change, the interclass correlation coefficient, and Guyatt\u27s responsiveness index, respectively. RESULTS: Of 285 participants who completed utility valuations, only 113 (39.6%) completed the re-test. Of these 113 participants, 92 (81.4%) provided valid responses on the first test and 75 (66.4%) provided valid responses on the test and re-test. Agreement for all groups of health states was adequate, since their smallest detectable change was less than the minimal clinically important difference. The mean interclass correlation coefficients for all health states were \u3e 0.8, indicating at least substantial reliability. Guyatt\u27s responsiveness indices all exceeded 0.80, indicating a high level of responsiveness. CONCLUSIONS: To our knowledge, this is the first validated open-source, web-based, self-directed utility valuation module. We have demonstrated the SOAP MESCC module is valid, reproducible, and responsive for obtaining ex ante utilities. Considering the successful psychometric validation of the SOAP MESCC module, other investigators can consider developing modules for other diseases where direct utility valuation is needed

Irrigation Requirements for Grape Crop under Climate Changes Conditions in Egypt

The present work is mainly directed to discuss sensitivity of climate changes upon the irrigation demand for grape crop in Egypt.The Penman Monteith equation was used to calculate reference Evapotranspiration (ETo) under current and future climate for the two locations(El Menya and El Beheira). The historical climate data for ten years from (2000 – 2010) was used as current climate to calculate irrigationrequirement for grape crop under Egyptian conditions. Two climate changes scenarios have been applied as changes in temperature. The firstscenario supposed that increasing in temperature of 1.5°C would happen, and the second scenario supposed that increasing of 3.5°C wouldhappen to calculate reference Evapotranspiration and irrigation requirement for future climate. The results showed that the evapotranspirationand irrigation requirement for grape crop at El Menya location higher than El Beheira location. Irrigation demand for grape plant under twoclimate changes scenario will increase in El Menya and El Beheira locations. El Menya location will take the highest irrigation demand underclimate changes. Therefore, possible adaptation countermeasures should be developed to mitigate the negative effects of climate changes forthe sustainable development of agro-ecosystems in Egypt

Irrigation Requirements for Grape Crop under Climate Changes Conditions in Egypt

The present work is mainly directed to discuss sensitivity of climate changes upon the irrigation demand for grape crop in Egypt. The Penman Monteith equation was used to calculate reference Evapotranspiration (ETo) under current and future climate for the two locations (El Menya and El Beheira). The historical climate data for ten years from (2000 – 2010) was used as current climate to calculate irrigation requirement for grape crop under Egyptian conditions. Two climate changes scenarios have been applied as changes in temperature. The first scenario supposed that increasing in temperature of 1.5°C would happen, and the second scenario supposed that increasing of 3.5°C would happen to calculate reference Evapotranspiration and irrigation requirement for future climate. The results showed that the evapotranspiration and irrigation requirement for grape crop at El Menya location higher than El Beheira location. Irrigation demand for grape plant under two climate changes scenario will increase in El Menya and El Beheira locations. El Menya location will take the highest irrigation demand under climate changes. Therefore, possible adaptation countermeasures should be developed to mitigate the negative effects of climate changes for the sustainable development of agro-ecosystems in Egypt