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  • Article  (15)
  • American Chemical Society (CrossRef)  (15)
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  • Article  (15)
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  • 11
    Language: English
    In: Journal of natural products, July 2008, Vol.71(7), pp.1237-41
    Description: The minor hop ( Humulus lupulus) chalcones 3'-geranylchalconaringenin (3), 5'-prenylxanthohumol (4), flavokawin (5), xanthohumol H (8), xanthohumol C (9), and 1'',2''-dihydroxanthohumol C (10) were synthesized. The non-natural chalcones 3'-geranyl-6'-O-methylchalconaringenin (2), 3'-methylflavokawin (6), and 2'-O-methyl-3'-prenylchalconaringenin (7) were also synthesized. Cytotoxicity was investigated in HeLa cells, and these compounds all had IC 50 values comparable to xanthohumol (8.2-19.2 microM). The ORAC-fluorescein assay revealed potent antioxidative activity for 7 and 8 with 5.2 and 4.8 Trolox equivalents, respectively.
    Keywords: Antioxidants -- Chemical Synthesis ; Chalcones -- Chemical Synthesis ; Humulus -- Chemistry ; Propiophenones -- Pharmacology
    ISSN: 01633864
    E-ISSN: 1520-6025
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  • 12
    Language: English
    In: Molecular pharmaceutics, 2009, Vol.6(2), pp.407-15
    Description: Some Pluronics, particularly F127, are known to stabilize nanospheres and prolong their circulation time in vivo. However, these copolymers of poly(ethylene glycol) (PEG) and poly(propylene glycol) are not biodegradable, and despite the long history, there is no approved commercial product using F127 for parenteral administration until now. Meanwhile, hydroxyethyl starch (HES) is a biodegradable polymer that is currently investigated as a substitute for PEG. In order to produce a fully biodegradable amphiphilic polymer, we esterified different molar masses of HES with lauric acid to get different molar substitutions. These polymers, as well as Pluronic F68 and F127, were used to stabilize poly(lactic-co-glycolic acid) (PLGA) nanospheres prepared by nanoprecipitation. For physicochemical characterization, the particle size, zeta potential, and the thickness of the adsorbed polymer layer were measured. The ability of the polymer coating to prevent the adsorption of human serum albumin (HSA) and fibrinogen (FBG) was evaluated. Finally, the phagocytosis of the stabilized nanospheres by a monocyte macrophage cell line (J774.2) was assessed. Results show that the PLGA nanospheres had an average particle size of 110-140 nm. The thickness of the adsorbed polymer layer increases with the increase in molar mass, and is generally higher for HES laurates than the studied Pluronics. Pluronic F68, F127 as well as the HES laurates with low molar substitution prevented the adsorption of HSA. HES laurates with low molar substitution and F127, but not F68, prevented the adsorption of FBG. The phagocytosis experiments showed that the HES laurates, particularly the one with the highest molar mass, could reduce the uptake of the nanospheres better than F68 and comparable to F127. Finally, these results warrant in vivo experiments to evaluate how the HES laurates can affect the pharmacokinetics and fate of the nanospheres.
    Keywords: Nanospheres ; Glycolates -- Chemistry ; Hydroxyethyl Starch Derivatives -- Chemistry ; Poloxamer -- Chemistry ; Polymers -- Chemistry
    ISSN: 1543-8384
    E-ISSN: 15438392
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  • 13
    Language: English
    In: Journal of natural products, October 2009, Vol.72(10), pp.1741-7
    Description: Therapeutic effects of dietary flavonoids have been attributed mainly to their antioxidant capacity. Xanthohumol (1), a prominent flavonoid of the hop plant, Humulus lupulus, was investigated for its antioxidant potential and for its effect on NF-kappaB activation. To examine the biological relevance of 1, a hepatic ischemia/reperfusion model was chosen as a widely accepted model of oxidative stress generation. The impact of 1 on endogenous antioxidant systems, on the NF-kappaB signal transduction pathway as well as on apoptotic parameters, and on hepatic tissue damage was evaluated. Compound 1 markedly decreased the level of reactive oxygen species in vitro. Furthermore, levels of enzymatic and nonenzymatic antioxidants were restored after pretreatment in postischemic hepatic tissue, and lipid peroxidation was attenuated. NF-kappaB activity was reduced in vitro as well as in hepatic tissue after ischemia/reperfusion upon pretreatment with 1. In addition, the phosphorylation of Akt was markedly inhibited. Surprisingly, 1 decreased the expression of the antiapoptotic protein Bcl-X and increased caspase-3 like-activity, a proapoptotic parameter. Moreover, hepatic tissue damage as well as TNF-alpha levels increased in xanthohumol-pretreated liver tissue after ischemia/reperfusion. In summary, xanthohumol did not protect against ischemia/reperfusion injury in rat liver, despite its antioxidant and NF-kappaB inhibitory properties.
    Keywords: Antioxidants -- Pharmacology ; Flavonoids -- Pharmacology ; Liver -- Drug Effects ; Propiophenones -- Pharmacology ; Reperfusion Injury -- Metabolism
    ISSN: 01633864
    E-ISSN: 1520-6025
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  • 14
    Language: English
    In: Journal of Chemical & Engineering Data, 01/2006, Vol.51(1), pp.136-144
    Description: The viscosity of gaseous ethane was measured using a vibrating-wire viscometer at subcritical temperatures of 290 and 300 K up to 88% of the saturated vapour pressure and at supercritical temperatures of 310, 320, 340, 400 and 430 K at pressures up to a maximum of 30 MPa. The measured data were tabulated and evaluated using the Bucker and Wagner equation of state. The reproducibility and uncertainty were estimated. The viscosity values from the isotherms were correlated as a function of reduced density using a power series expansion and compared with literature data.
    Keywords: Gaseous Status ; Ethane ; Hydrocarbon ; Viscosity ; Isotherm ; Engineering ; Chemistry;
    ISSN: 0021-9568
    E-ISSN: 1520-5134
    Source: American Chemical Society (via CrossRef)
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  • 15
    Language: English
    In: Journal of Chemical & Engineering Data, 05/2005, Vol.50(3), pp.896-906
    ISSN: 0021-9568
    E-ISSN: 1520-5134
    Source: American Chemical Society (via CrossRef)
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