Oxygenated heterocyclic metabolites with dual cyclooxygenase-2 and 5-lipoxygenase inhibitory potentials from Rhizophora annamalayana

Previously undescribed oxygenated heterocyclic metabolites were purified from the ethyl acetate fraction of natural mangrove hybrid Rhizophora annamalayana. The purified metabolites were characterized as 11-(tetrahydro-14α-hydroxy- 13β-methylfuran-12-yl)-10β-methylbutyl benzoate (1), 13-(tetrahydro-15β,16α-dimethyl-18-oxo-2H-pyran-14-yl)-10β- methylhept-12(E)-enyl benzoate (2), and dihydro-11-((7E)-2-hydroxy-8β-methyl-2H-chromen-9-yl)-13-methylpent-12(E)- enyl)-17β-methylfuran-19(3H)-one (3) by the combined spectroscopic experiments. These metabolites were assessed for their antioxidant and anti-inflammatory activities, and compared with the commercially available standards. The purified compound 3 exhibited greater antioxidant activities as deduced by 2, 2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid and 2, 2-diphenyl-1-picrylhydrazyl quenching properties (IC50 2.10 and 2.22 mM, respectively) compared to the positive control (α-tocopherol, IC50 1.46 and 1.69 mM, respectively). Consequently, the anti-inflammatory activity of compound 3 with regard to the inhibitory property towards pro-inflammatory 5-lipoxygenase was greater (IC50 2.16 mM) than that exhibited by the synthetic anti-inflammatory drug ibuprofen (IC50 4.51 mM). Electronic and hydrophobic parameters were deduced to find the target bioactivities of the studied compounds. These oxygenated heterocyclic metabolites could be used as potential therapeutic lead compounds in the pharmaceutical applications

Biogenic guaianolide-type sesquiterpene lactones with antioxidative and anti-inflammatory properties from natural mangrove hybrid Rhizophora annamalayana

Previously undescribed guaianolide-type sesquiterpene lactones were isolated from the chloroform fraction of the natural hybrid mangrove Rhizophora annamalayana, and were characterised as (Z)-3α,4,5,6-tetrahydro-5α-isobutyl-2β-(methoxymethyl)-7-methyl-3H-cyclohepta[b]carbolactone (1) and (7Z)-isopentyl 3α,4,5,6,7,8-hexahydro-2β-((E)-11-methylbut-10-enyl)-1-oxo-2H-cyclohepta[b]furan-6-carboxylate (2). Compound 2 displayed greater antioxidative activities {1, 1-diphenyl-2-picrylhydrazyl (DPPH) and 2, 2'-azino-bis-3 ethylbenzothiozoline-6-sulphonic acid diammonium salt (ABTS), IC50 0.65 and 0.62 mg/mL, respectively)} compared to 1 (IC50 0.83 and 1.14 mg/mL, respectively) (p < 0.05). Compound 2 recorded no significant difference in DPPH. scavenging activities (IC50 0.65 mg/mL) compared to α-tocopherol (IC50 0.63 mg/mL). Pro-inflammatory 5-lipoxygenase inhibitory activity of 2 was found to be comparable (IC50 0.98 mg/mL) to that displayed by synthetic anti-inflammatory drug ibuprofen (IC50 0.93 mg/mL). Compound 2 showed significantly greater selectivity index (anti-cyclooxygenase-1/anti-cyclooxygenase-2 = 2.15) than non-steroidal anti-inflammatory ibuprofen (<0.5) (p < 0.05), and therefore, might be used as selective cyclooxygenase-2 inhibitor. The hitherto undescribed guaianolide lactones might be used as potential anti-inflammatory and antioxidative pharmacophore leads

De regreso a la hemodiálisis tras el fracaso del trasplante renal.

Un número creciente de pacientes están retornando a diálisis después del fallo del trasplante renal. Tras su fracaso, estos pacientes presentan elevada morbimortalidad, sobre la cual influyen diversos factores. No está claro si la mortalidad aumenta entre estos pacientes en relación con aquellos en lista de espera que no han recibido un trasplante renal. Se describe la morbimortalidad y los factores que influyen sobre ella en pacientes de regreso a hemodiálisis tras el fracaso del injerto renal. Los pacientes trasplantados vuelven a diálisis en un porcentaje progresivamente creciente en relación con el mayor número de trasplantes que se realizan. Así, en los Estados Unidos, hasta un cuarto de los pacientes que ingresan en diálisis o en lista de espera han recibido un trasplante previo. La cuestión que se plantea es la de si la morbimortalidad es mayor después del fracaso del injerto que la de los pacientes que nunca han sido trasplantados. Las principales causas se relacionan con la enfermedad cardiovascular y los factores que a ello se vinculan son: causa de la pérdida del injerto, estado nutricional, inmunosupresión recibida, tiempo de permanencia en trasplante, precocidad con que haya comenzado el tratamiento sustitutivo, anemia, presencia de enfermedades infecciosas y oncoproliferativas, acceso vascular disponible, entre otros. En resumen se conoce el mal pronóstico después de la vuelta a diálisis, la morbimortalidad y sus factores de riesgo en relación con la mortalidad entre los pacientes que esperan un trasplante renal nos permitirá intervenir para reducirlos y mejorar su expectativa de vida.  Palabras clave: Hemodiálisis tras fracaso del trasplante renal, morbi-mortalidad, factores de riesgo

Proteína C reactiva elevada e hipoalbuminemia: síndrome/complejo alnutrición, microinflamación crónica, ateroesclerosis: significado pronostico en pacientes hemodializados

La mortalidad persiste muy alta en pacientes en hemodiálisis, su principal causa es la cardio-cerebro-vascular seguida de la infecciosa. Existe un estado micro-inflamatorio crónico evidenciado por la elevación de reactantes de fase aguda, entre ellos, la proteína C reactiva, la cual está asociada a la morbi-mortalidad de causa cardiovascular y general en estos enfermos. La hipoalbuminemia es un marcador de malnutrición y un fuerte predictor de todas las causas de morbilidad y mortalidad en hemodiálisis. El objetivo es determinar la posible influencia de la proteína C reactiva y la hipoalbuminemia sobre los resultados de morbimortalidad. Se realizó un estudio observacional analítico, prospectivo, con un seguimiento de 24 meses, cuyo resultado fue un promedio de edad de 46-60 años; el tiempo promedio en hemodiálisis era de 6-16 años. La prevalencia de cifras elevadas de PCR fue de 42,99 %, (IC 95%: 22,42-44,25).Existió una correlación inversa entre las cifras de PCR y la albúmina sérica (r=-0,30; p=0,01) y una correlación directa entre PCR y la edad (r=0,27; p=0,02). El tipo de acceso vascular, (PTFE y catéter), guarda relación con los títulos elevados de PCR (p=0,01). La mayorhospitalización (55,6 %), ocurrió en enfermos con PCR elevada (OR: 2,50, IC95%: 2,02-3,14). La hipoalbuminemia es un predictor independiente de la mortalidad general (OR: 2,44). La PCR constituyó un predictor independiente de mortalidad cardiovascular (OR: 2,76, IC 95%: 2,25-3,61). En conclusión se determina la influencia de la PCR y de la hipoalbuminemia sobre la morbimortalidad en enfermos en hemodiálisis.  Palabras clave: Proteína C-reactiva, hipoalbuminemia, malnutrición, hospitali-zación, mortalidad cardiovascular y no cardiovascular, hemodiálisis, enferme-dad renal crónica Ve insuficiencia renal crónica Terminal

Long chain n-3 polyunsaturated fatty acid enriched oil emulsion from sardine oil

Dietary fats are used to build every cell in the body and cell membranes are made of a variety of individual fatty acids which are carboxylic acids with long hydrocarbon chains (usually C12-22). The essential fatty acids from marine fish have protective mechanisms against coronary heart disease, which became apparent in the investigations of the health status of Greenland Eskimos who consumed diets very high in fat from seals,whales, fish etc, and yet had a low rate of coronary heart disease

Tunable emission properties of CdSe/CdS quantum dots by Ce doping

A facile one-step hydrothermal synthesis to prepare cerium (Ce3+) ion doped CdSe/CdS core/shell quantum dots (QDs) is introduced. The effect of Ce3+ ion doping on structural and optical properties of the CdSe/CdS core/shell QDs is comprehensively investigated. With increasing Ce doping concentration, a linear increase in the lattice parameter is observed, suggesting the successful coupling of Ce3+ ions to the CdSe/CdS QDs. X-ray photoelectron spectroscopy reveals strong peaks of the Ce3+ state, indicating that Ce is initially present mainly in the Ce3+ ion state. In addition, red-shift over the range 538–569 nm is observed in the photoluminescence (PL) spectra of Ce3+ ion doped CdSe/CdS QDs. Results clearly indicates that the PL peak positions of the CdSe/CdS QDs could be controlled by the Ce content. This study highlights a new approach to tune the emission of the QDs

Two rare antioxidant and anti-inflammatory oleanenes from loop root Asiatic mangrove Rhizophora mucronata

Two oleanenes, olean-18(19)-en-3b-yl-(3,6-dimethyl-3E,6Z-dienoate) and (13a)-27-frido-olean-14(15)- en-(17a)-furanyl-3b-ol representing a class of rare natural pentacyclic triterpenoids were isolated from the chloroform extract of Asiatic mangrove, Rhizophora mucronata Lam. (Family: Rhizophoraceae). The furanyl oleanene exhibited significantly greater antioxidative activities (IC50 0.73e0.76 mg/mL), than prenylated oleanene (IC50 0.84e0.96 mg/mL) (P < 0.05). No significant differences in anti-5-lipoxygenase activities of these compounds with the synthetic drug ibuprofen was discernable (IC50 0.8e0.9 mg/mL), whilst furanyl oleanene demonstrated significantly greater anti-cyclooxygenase-2 (IC50 0.84 mg/mL) and anti-5-lipoxygenase activities (IC50 0.78 mg/mL) over prenylated oleanene (IC50 > 0.90 mg/mL). These compounds exhibited lesser activity against cyclooxygenase-1 than cyclooxygenase-2 isoform, and therefore, their selectivity indices remained significantly greater (anti-cyclooxygenase-1IC50/anti-cyclooxygenase- 2IC50 > 1) than the aspirin (0.02) and ibuprofen (0.44). The lipophilic and steric molecular descriptors were found to occupy a prominent role in determining the bioactivities of the compounds. These previously undescribed oleanenes might serve as potential antioxidative and anti-inflammatory lead molecules in medicinal formulations and food industries

Not Available

Not AvailableTwo oleanenes, olean-18(19)-en-3b-yl-(3,6-dimethyl-3E,6Z-dienoate) and (13a)-27-frido-olean-14(15)- en-(17a)-furanyl-3b-ol representing a class of rare natural pentacyclic triterpenoids were isolated from the chloroform extract of Asiatic mangrove, Rhizophora mucronata Lam. (Family: Rhizophoraceae). The furanyl oleanene exhibited significantly greater antioxidative activities (IC50 0.73e0.76 mg/mL), than prenylated oleanene (IC50 0.84e0.96 mg/mL) (P < 0.05). No significant differences in anti-5-lipoxygenase activities of these compounds with the synthetic drug ibuprofen was discernable (IC50 0.8e0.9 mg/mL), whilst furanyl oleanene demonstrated significantly greater anti-cyclooxygenase-2 (IC50 0.84 mg/mL) and anti-5-lipoxygenase activities (IC50 0.78 mg/mL) over prenylated oleanene (IC50 > 0.90 mg/mL). These compounds exhibited lesser activity against cyclooxygenase-1 than cyclooxygenase-2 isoform, and therefore, their selectivity indices remained significantly greater (anti-cyclooxygenase-1IC50/anti-cyclooxygenase- 2IC50 > 1) than the aspirin (0.02) and ibuprofen (0.44). The lipophilic and steric molecular descriptors were found to occupy a prominent role in determining the bioactivities of the compounds. These previously undescribed oleanenes might serve as potential antioxidative and anti-inflammatory lead molecules in medicinal formulations and food industries.Not Availabl

Two rare antioxidative prenylated terpenoids from loop-root Asiatic mangrove Rhizophora mucronata (Family Rhizophoraceae) and their activity against pro-inflammatory cyclooxygenases and lipoxidase

Two new biogenic prenylated terpenoids were isolated from the methanol extract of Rhizophora mucronata. The extended C20 sesquiterpenoid with prenylated guaiane framework was characterised as (4E, 8Z)-3, 3a, 6, 7-tetrahydro-3, 9-dimethyl-5-(6-methylheptan-2-yl) cycloocta[b] furan-2-(9aH)-one (1). (35E)-1,2,3,5,6,6-icosahydro-4,4,8b,10,14,17,20,20- octamethylpicen-3-yl-34,35-dimethyloct-31-enoate (2) represents the first example of naturally occurring C40 prenylated oleanane-type triterpenoid, whereas one 4,5-dimethyloct-5-enoate side chain remains attached at C-3 position of the oleanane framework formed by the E-ring closure of C30 saccharide moiety. The structures of the compounds were elucidated using NMR and mass spectrometric analysis. Compound 1 was found to have significantly greater antioxidant activities (IC50 ~ 0.75 mg/ mL) compared to 2 (IC50 > 0.80 mg/mL). No significant differences in anti-cyclooxygenase-2 of these compounds were discernable (IC50 0.8 – 0.9 mg/mL), whilst compound 1 showed greater anti-5-lipoxidase activities (IC50 ~ 0.8 mg/mL) those that of 2 (IC50 0.96 mg/mL). Bioactivities of the prenylated terpenoids were inversely proportional to lipophilic and bulk descriptors