RESUMEN
Investigation of the effect of the Fe abiotic stress on the germination rate, iron accumulation, root and shoot elongation of wheat (Triticum aestivum) was carried out. The grains were exposed to different experimental concentrations of ferrous sulfate (FeSO4) (0-15 mM). The effect of the treatment on the shoot and root elongation of the seeds were reported. There is a linear relationship between the treatment and the inhibition of shoot elongation. The half-inhibition dose (ID50) of FeSO4 on inhibition of shoot elongation was 7.3 mM. Each treatment groups (3-15 mM) were used to fortify the wheat flour at 0.1 mg Fe/g. The effect of fortification on rheology (farinograph, extensograph, and amylograph), quality of pasta and iron bioavailability was studied. The pasta cooking properties, texture and sensory properties of 12 and 15 mM composite pasta were equally acceptable as wheat without fortification, or NaFeEDTA fortified pasta. The iron dialysability of 3-15 mM composite pasta was similar to the NaFeEDTA fortified pasta. The iron bioavailability (in vivo) of 15 mM group based pasta was evaluated in the anemic rats. The pasta at 4% (Fe 0.026 mg/g) in iron-deficient diet fed to anemic rats for 2 weeks showed percentage iron absorption (PIA) and hemoglobin regeneration efficiency (HRE) of 85.3% and 44.4% respectively which is higher than the NaFeEDTA. In conclusion, iron-fortified pasta is the promising food fortificant with more iron bioavailability in the prevention of iron deficiency anemia.
RESUMEN
OBJECTIVE: There are limited data on neuropsychological correlates of poor insight in obsessive-compulsive disorder (OCD). We hypothesize that poor insight may be associated with greater impairment in tasks of conflict resolution/response inhibition and possibly impairment in a task of verbal learning and memory. METHOD: Insight and neuropsychological functions were assessed in 150 subjects with DSM-IV OCD. The neuropsychological data of 177 healthy control subjects were used for comparison. RESULTS: Insight score correlated significantly with the Stroop Interference Test for conflict resolution/response inhibition (P = 0.002), and showed trends for significance with the Controlled Oral Word Association (COWA) average for verbal fluency (P = 0.021) and delayed recall on the Auditory Verbal Learning Test (AVLT) for verbal memory (P = 0.015). On regression analysis, the AVLT delayed recall, the COWA average, the Matrix score, the Yale-Brown Obsessive-Compulsive Scale total score, and current antipsychotic use emerged as significant predictors of poorer insight. CONCLUSION: Poor insight is associated with greater impairments in conflict resolution/response inhibition, verbal memory, and fluency. Individuals with poorer insight may have difficulty in appropriately processing conflicting information, updating their memory with corrective information, and then accessing this corrective information to modify their irrational beliefs.
Asunto(s)
Trastorno Obsesivo Compulsivo/psicología , Adulto , Aprendizaje por Asociación , Estudios de Casos y Controles , Comprensión , Conflicto Psicológico , Función Ejecutiva , Femenino , Humanos , Inhibición Psicológica , Masculino , Memoria , Pruebas Neuropsicológicas , Escalas de Valoración Psiquiátrica , Test de Stroop , Aprendizaje VerbalRESUMEN
1-Chloro-2-formyl indenes and tetralenes have been synthesized using Vilsmeier-Haack-Arnold reaction onto indanones and tetralones. Most of these analogues exhibited antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MICs ranging from 30 to 500 µg/mL. Analogue 13 was further modified to some derivatives. The most active analogue 23 showing MIC at 30 µg/mL was further evaluated for acute oral toxicity in Swiss albino mice and was found to be safe up to 300 mg/kg dose.
Asunto(s)
Antituberculosos/síntesis química , Antituberculosos/farmacología , Indenos/síntesis química , Indenos/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Animales , Antituberculosos/química , Indenos/química , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-ActividadRESUMEN
Phytol, a diterpene alcohol was modified to several semisynthetic analogues. Some of the modifications were done logically to enhance lipophilicity of the molecule. Analogues 14, 16 and 18 exhibited antitubercular activity (MIC 15.6-50microg/mL) better than phytol (100microg/mL). The most potent analogue 18 was evaluated for in vivo toxicity in Swiss albino mice and was well tolerated by the experimental animals up to 300mg/kg body weight as a single oral acute dose.
Asunto(s)
Antituberculosos/síntesis química , Oximas/síntesis química , Fitol/análogos & derivados , Animales , Antituberculosos/química , Antituberculosos/toxicidad , Ratones , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Oximas/química , Oximas/toxicidad , Fitol/síntesis química , Fitol/química , Fitol/toxicidadRESUMEN
Glabridin, an active constituent of Glycyrrhiza glabra roots, was found to be active against both yeast and filamentous fungi. Glabridin also showed resistance modifying activity against drug resistant mutants of Candida albicans at a minimum inhibitory concentration of 31.25-250 microg/mL. Although the compound was reported earlier to be active against Candida albicans, but this is the first report of its activity against drug resistant mutants.
Asunto(s)
Antifúngicos/farmacología , Candida albicans/efectos de los fármacos , Glycyrrhiza/química , Isoflavonas/farmacología , Fenoles/farmacología , Antifúngicos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Isoflavonas/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Fenoles/aislamiento & purificación , Extractos Vegetales/farmacologíaRESUMEN
Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds 10, 11, 12 and 14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (10, IC(50)=2.2 microM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100 microg/ml, 258 microM). While, indanones 11, 12 and 14 showed toxicities to erythrocytes at higher concentrations.
Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Química Farmacéutica/métodos , Ensayos de Selección de Medicamentos Antitumorales , Ácido Gálico/química , Indanos/síntesis química , Antioxidantes/farmacología , Línea Celular Tumoral , Diseño de Fármacos , Eritrocitos/efectos de los fármacos , Hemólisis , Humanos , Indanos/química , Concentración 50 Inhibidora , Modelos Químicos , Ósmosis , Sales de Tetrazolio/farmacología , Tiazoles/farmacologíaRESUMEN
The present study was aimed to investigate antimicrobial potential of Glycyrrhiza glabra roots. Antimycobacterial activity of Glycyrrhiza glabra was found at 500 microg/mL concentration. Bioactivity guided phytochemical analysis identified glabridin as potentially active against both Mycobacterium tuberculosis H(37)Ra and H(37)Rv strains at 29.16 microg/mL concentration. It exhibited antimicrobial activity against both Gram-positive and Gram-negative bacteria. Our results indicate potential use of licorice as antitubercular agent through systemic experiments and sophisticated anti-TB assay.
Asunto(s)
Antibacterianos/farmacología , Glycyrrhiza/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad MicrobianaRESUMEN
Medicinal plants have been traditionally used for treating liver diseases since centuries. Several leads from plant sources have been found as potential hepatoprotective agents with diverse chemical structures. Although, a big list of hepatoprotective phytomolecules was reported in the scientific literature, only a few were potent against various types of liver damages. Of which, silymarin, andrographolide, neoandrographolide, curcumin, picroside, kutkoside, phyllanthin, hypophyllanthin, and glycyrrhizin have largely attracted the scientific community. This review focuses discussion on the chemistry, biological activity, mode of action, toxicity, and future prospects of these leads.
Asunto(s)
Citocinas/metabolismo , Hepatopatías/tratamiento farmacológico , Hígado/efectos de los fármacos , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Animales , Cinamatos/química , Cinamatos/metabolismo , Cinamatos/farmacología , Cinamatos/toxicidad , Curcumina/química , Curcumina/metabolismo , Curcumina/farmacología , Curcumina/toxicidad , Diterpenos/química , Diterpenos/metabolismo , Diterpenos/farmacología , Diterpenos/toxicidad , Glucósidos/química , Glucósidos/metabolismo , Glucósidos/farmacología , Glucósidos/toxicidad , Ácido Glicirrínico/química , Ácido Glicirrínico/metabolismo , Ácido Glicirrínico/farmacología , Ácido Glicirrínico/toxicidad , Humanos , Lignanos/química , Lignanos/metabolismo , Lignanos/farmacología , Lignanos/toxicidad , Hígado/metabolismo , Hepatopatías/metabolismo , Fitoterapia , Extractos Vegetales/metabolismo , Extractos Vegetales/uso terapéutico , Extractos Vegetales/toxicidad , Plantas , Sustancias Protectoras/química , Sustancias Protectoras/metabolismo , Sustancias Protectoras/uso terapéutico , Sustancias Protectoras/toxicidad , Silimarina/química , Silimarina/metabolismo , Silimarina/farmacología , Silimarina/toxicidad , Tetrahidronaftalenos/química , Tetrahidronaftalenos/metabolismo , Tetrahidronaftalenos/farmacología , Tetrahidronaftalenos/toxicidadRESUMEN
Chalcone derivatives on estradiol framework have been synthesized. Some of the derivatives showed potent anticancer activity against some human cancer cell lines. Compounds 9 and 19 showed potent activity against MCF-7, a hormone dependent breast cancer cell line. Chalcone 7 was further modified to the corresponding indanone derivative (19) using the Nazarov reaction, which showed better activity than the parent compound against the MCF-7 breast cancer cell line. Active anticancer derivatives were also evaluated for osmotic hemolysis using the erythrocyte as a model system. It was observed that chalcone derivatives showing cytotoxicity against cancer cell lines did not affect the fragility of erythrocytes and hence may be considered as non-toxic to normal cells.
Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Chalcona/análogos & derivados , Estradiol/química , Antineoplásicos/síntesis química , Línea Celular Tumoral , HumanosRESUMEN
Several diverse analogues of Oenostacin, a naturally occurring potent antibacterial phenolic acid derivative, have been synthesized. A small library with more than forty analogues having different aromatic rings and varied side chains has been achieved through solution phase synthesis. Some of these analogues, that is, 22, 23 and 42, possessed potent antibacterial activities against Staphylococcus epidermidis and Staphylococcus aureus having EC(50) ranging from 0.49 to 0.67 microM as compared to Oenostacin (EC(50)=0.12 microM).
Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/farmacología , Hidroxibenzoatos/síntesis química , Hidroxibenzoatos/farmacología , Staphylococcus aureus/efectos de los fármacos , Staphylococcus epidermidis/efectos de los fármacos , Antibacterianos/química , Técnicas Químicas Combinatorias/métodos , Relación Dosis-Respuesta a Droga , Hidroxibenzoatos/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Estereoisomerismo , Relación Estructura-ActividadRESUMEN
Gallic acid, one of the most abundant plant phenolic acids, has been modified to cathepsin D protease inhibitors. The strategy of modification was proposed basing on some previously reported structure and activity relationship (SAR) studies. The synthesized naphthophenone fatty acid amide derivatives have been evaluated for in vitro cathepsin D inhibition activity. Two of them have shown significant inhibition activity with IC(50) values of 0.06 and 0.14 microM, respectively, as compared against pepstatin (0.0023 microM), the most potent inhibitor known so far. The study revealed that such attempts on gallic acid based pharmacophores might result in potent inhibitors of cathepsin D.
Asunto(s)
Amidas/química , Catepsina D/antagonistas & inhibidores , Catepsina D/metabolismo , Ácidos Grasos/química , Ácido Gálico/síntesis química , Ácido Gálico/farmacología , Cetonas/química , Naftalenos/química , Ácido Gálico/química , Estructura Molecular , Pepstatinas/antagonistas & inhibidores , Pepstatinas/metabolismo , Relación Estructura-ActividadRESUMEN
Vilsmeier reagent (DMF-POCl(3)) was used as an efficient formylating agent. Several sterols having sec-hydroxyl group at 3/17-position have been modified into respective formate esters. The method is simple, mild, chemoselective and provides sec-alcoholic protection in good yields.
Asunto(s)
Ésteres del Ácido Fórmico/síntesis química , Indicadores y Reactivos/química , Esteroles/síntesis química , Ésteres del Ácido Fórmico/química , Esteroles/químicaRESUMEN
3',4',5'-Trimethoxy benzoyl-naphthalene 2-O-acetic acid (5) underwent base catalysed intramolecular condensation to yield exclusively 1-(3',4',5'-trimethoxy) phenyl naphtho[2,1-b]furan 8. The cyclised product 8 has been characterised by spectroscopy. The product 8 showed significant anticancer activity against human cancer cell lines COLO320DM (colon), CaCO2 (colon) and WRL68 (liver) at 0.7, 0.65 and 0.50 microg/ml concentrations, respectively, in the in vitro MTT assay.
Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Furanos/síntesis química , Furanos/farmacología , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Furanos/química , Humanos , Técnicas In Vitro , Estructura Molecular , Relación Estructura-ActividadRESUMEN
A number of natural products, with diverse chemical structures, have been isolated as anticancer agents. Several potential lead molecules such as camptothecin, vincristine, vinblastine, taxol, podophyllotoxin, combretastatins, etc. have been isolated from plants and many of them have been modified to yield better analogues for activity, toxicity or solubility. Several successful molecules like topotecan, irinotecan, taxotere, etoposide, teniposide, etc. also have emerged as drugs upon modification of these natural leads and many more are yet to come. In this review, the authors have focused on four important anticancer leads, that is, camptothecin, taxol, combretastatin A-4 and podophyllotoxin. Their chemistry, structure and activity relationships, biological activities, modes of action, analogue synthesis and future prospects have been discussed.
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Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Animales , Camptotecina/química , Camptotecina/farmacología , Humanos , Paclitaxel/química , Paclitaxel/farmacología , Podofilotoxina/química , Podofilotoxina/farmacología , Estilbenos/química , Estilbenos/farmacologíaRESUMEN
Today, natural colourants are emerging globally, leaving synthetic colourants behind in the race, due to the realisation that are safer and ecofriendly in nature. In this context, a brief review of natural colourant sources, their classification, chemical constituents responsible for producing different colours, its activities and effect of different mordants on the hue is discussed.
Asunto(s)
Productos Biológicos/química , Colorantes/química , Colorantes de Alimentos/química , Animales , Colorantes/toxicidad , Contaminación Ambiental/prevención & control , Colorantes de Alimentos/toxicidad , Salud Holística , Humanos , Extractos Vegetales , Industria TextilRESUMEN
Vitellogenin (Vtg) plays vital roles as precursor to the yolk proteins and as carrier for lipids, carbohydrates, phosphates, metal ions, vitamins, and hormones into the oocytes during the massive deposition of yolk nutrients for subsequent nourishment of the developing embryos. Reproductive success is highly sensitive to the nutritional quality of the broodstock diet, which greatly affects the egg and larval viability. We present a novel strategy for genetically engineering a Pichia pastoris yeast strain that constitutively produces recombinant Vtg (rVtg), for application as an enriched feed. The tilapia Oreochromis aureus Vtg (OaVtg) cDNA (5.3 kb) was cloned into a nonsecretory pGAPZA vector. Clones containing up to 31 copies of glyceraldehyde-3-phosphate dehydrogenase (GAP)-promoter-driven Vtg expression cassettes were isolated. These clones expressed a membrane-associated intracellular rVtg protein of 194 kDa, constituting up to 1.16% of total protein. To facilitate future purification of rVtg, we explored the possibility of secreting rVtg using the native Vtg secretion signal and the alpha-factor secretion signal of Saccharomyces cerevisiae. However, neither signal promoted the secretion of rVtg. The clones maximally expressed rVtg at 23 degrees C, reaching a peak at 22 h in shake flasks and 16 h in a fermentor. The clones exhibited a significant increase in essential amino acids and long-chain polyunsaturated fatty acids, which are important for its application as a high-quality nutrient feed.
Asunto(s)
Gliceraldehído-3-Fosfato Deshidrogenasas/genética , Gliceraldehído-3-Fosfato Deshidrogenasas/metabolismo , Pichia/genética , Pichia/metabolismo , Ingeniería de Proteínas/métodos , Vitelogeninas/biosíntesis , Vitelogeninas/genética , Aminoácidos Esenciales/biosíntesis , Animales , Clonación Molecular/métodos , Ácidos Grasos Insaturados/biosíntesis , Regiones Promotoras Genéticas/genética , Proteínas Recombinantes/biosíntesis , Tilapia/genética , Tilapia/metabolismoRESUMEN
Microwave assisted condensation of asaronaldehyde (2) with malonic acid in piperidine-AcOH provides 2,4,5-trimethoxycinnamic acid (3) in 87% yield within 4 min, which upon further reduction with PdCl2- HCOOH-aq. NaOH gives 3-(2,4,5-trimethoxy)phenyl propionic acid (4) in 88% yield within 3 min. Esterification of 4 with MeOH-H+ gives methyl 2,4,5-trimethoxyphenylpropionate (1), a metabolite of Cordia alliodora, in 94% yield within 3 min (overall 69% yield).
Asunto(s)
Cordia/química , Fenilpropionatos/síntesis química , Aldehídos/química , Malonatos , MicroondasRESUMEN
Phytochemical investigation of the leaves of Bidens pilosa lead to the isolation and characterization of a new disubstituted acetylacetone (1) named as 3-Propyl-3-(2,4,5-trimethoxy)benzyloxy-pentan-2,4-dione.
Asunto(s)
Bidens/química , Pentanonas/aislamiento & purificación , Cromatografía en Capa Delgada , India , Resonancia Magnética Nuclear Biomolecular , Pentanonas/química , Hojas de la Planta/químicaRESUMEN
Gene 5 of bacteriophage T7 encodes a DNA polymerase essential for phage replication. A single point mutation in gene 5 confers temperature sensitivity for phage growth. The mutation results in an alanine to valine substitution at residue 73 in the exonuclease domain. Upon infection of Escherichia coli by the temperature-sensitive phage at 42 degrees C, there is no detectable T7 DNA synthesis in vivo. DNA polymerase activity in these phage-infected cell extracts is undetectable at assay temperatures of 30 degrees C or 42 degrees C. Upon infection at 30 degrees C, both DNA synthesis in vivo and DNA polymerase activity in cell extracts assayed at 30 degrees C or 42 degrees C approach levels observed using wild-type T7 phage. The amount of soluble gene 5 protein produced at 42 degrees C is comparable to that produced at 30 degrees C, indicating that the temperature-sensitive phenotype is not due to reduced expression, stability, or solubility. Thus the polymerase induced at elevated temperatures by the temperature-sensitive phage is functionally inactive. Consistent with this observation, biochemical properties and heat inactivation profiles of the genetically altered enzyme over-produced at 30 degrees C closely resemble that of wild-type T7 DNA polymerase. It is likely that the polymerase produced at elevated temperatures is a misfolded intermediate in its folding pathway.