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PubMedDate not supplied

Production and secretion of 5-n-alkylresorcinols by Fusarium culmorum.

Fusarium culmorum F1 was found to produce and secrete into the culture medium several of 5-n-alkylresorcinols. The amount of resorcinolic lipids was 5.3 microg/g and 0.9 microg/l in mycelium and in post-culture liquid, respectively. First of all F. culmorum F1 produces saturated homologues with C15 to C25 side chains. The extract from the medium contained only homologues with shorter carbon chains (C13 to C17).

Culture Media↗
PubMedDate not supplied

Alkylresorcinols in barley (Hordeum vulgare L. distichon) grains.

This study was carried out to compare grains of barley (Hordeum vulgare L. distichon) regarding contents and compositions of 5-n-alkylresorcinols. Mixtures of resorcinol homologues were isolated from acetone extracts from five barley cultivars. These polyketide metabolites were identified by chromatographic and spectroscopic means. The content and homologue patterns among different varieties were similar. The predominant compounds were 1,3-dihydroxy-5-n-heneicosylbenzene (C21:0), 1,3-dihydroxy-5-n-nonadecylbenzene (C19:0) and 1,3-dihydroxy-5-n-pentacosylbenzene (C25:0). The alkylresorcinol concentrations, in contrast to their compositions, depended on environmental and agricultural factors.

Hordeum↗
PubMed2004

Calculation of cyclodextrin binding affinities: energy, entropy, and implications for drug design.

The second generation Mining Minima method yields binding affinities accurate to within 0.8 kcal/mol for the associations of alpha-, beta-, and gamma-cyclodextrin with benzene, resorcinol, flurbiprofen, naproxen, and nabumetone. These calculations require hours to a day on a commodity computer. The calculations also indicate that the changes in configurational entropy upon binding oppose association by as much as 24 kcal/mol and result primarily from a narrowing of energy wells in the bound versus the free state, rather than from a drop in the number of distinct low-energy conformations on binding. Also, the configurational entropy is found to vary substantially among the bound conformations of a given cyclodextrin-guest complex. This result suggests that the configurational entropy must be accounted for to reliably rank docked conformations in both host-guest and ligand-protein complexes. In close analogy with the common experimental observation of entropy-enthalpy compensation, the computed entropy changes show a near-linear relationship with the changes in mean potential plus solvation energy.

Algorithms↗
PubMed1996

Spontaneous comedones on the skin of hairless descendants of Mexican hairless dogs.

In the first experiment, the skin sebum and humidity, perspiration ability of sweat glands, and histology of spontaneous comedones were examined in hairless descendants of Mexican hairless dogs. The skin of females showed lower humidity than that of males. Some animals with a large number of comedones exhibited remarkably high skin sebum scores. The comedones were distributed throughout the dorsal skin, and a cluster of lesions was found mainly in the limbs and prepuces. The sweat glands showed no perspiration in the sudorific test. Histologically, both infant and adult animals had lesions of micro- and/or "blackhead" comedones. Plugged follicles containing abundant keratic substances associated well-developed sebaceous glands. Spontaneous comedones in the skin of hairless dogs were grossly and histologically similar to the acne vulgaris observed in human beings. The skin of some adult animals showed a large number of protrusive comedones which were solid cystic structures containing organized substances. In the second experiment, three kinds of antiacne agents (sulfur and camphor, sulfur and resorcinol, and ibuprofen piconol) were applied daily to the test sites for one month. These antiacne agents caused prominent extrusion of keratin plugs from follicular sites. The results suggest that the hairless dogs are a predictive model for evaluating the efficacy of antiacne agents proposed for acne treatment.

Acne Vulgaris↗
PubMed1999

Leptin enhances glycogen storage in hepatocytes by inhibition of phosphorylase and exerts an additive effect with insulin.

The effects of the adipocyte-derived hormone leptin on glucose metabolism in hepatocytes were investigated. Incubation of hepatocytes from Wistar rats with leptin for 16 h caused a dose-dependent increase in incorporation of [14C]glucose into glycogen, with a maximal effect at 30 nmol/l leptin. This effect of leptin was observed over a range of glucose concentrations (10-25 mmol/l) and was associated with stimulation of net glycogen deposition. It was not counteracted by mercaptopicolinate, an inhibitor of phosphoenolpyruvate carboxykinase, indicating that it is not due to increased gluconeogenic flux. Leptin also enhanced the short-term stimulation of glycogen synthesis by insulin. These effects of leptin were associated with inhibition of phosphorylase a, which occurred after 4 h of exposure to leptin. Culture with leptin for 16 h did not affect the activities of glucose-6-phosphatase or glucokinase or the activation state of glycogen synthase. Leptin did not affect glycolysis determined from the detritiation of [3-(3)H]glucose. The inhibitory effects of leptin on phosphorylase a were counteracted by short-term incubation with glucagon but were additive with the inhibitory effects of insulin and also with the inhibition caused by resorcinol (25 pmol/l), which inhibits phosphorylase kinase by a mechanism analogous to the antidiabetic drug proglycosyn. These results show that leptin has additive effects with insulin in inhibiting phosphorylase and stimulating glycogen storage in hepatocytes, indicating that these hormones act by separate but convergent mechanisms. It is concluded that the primary action of leptin in hepatocytes is to enhance glycogen storage. This may be an important compensatory mechanism for the inhibition of insulin secretion.

Animals↗
PubMed1985

Hydroxylation and conjugation of phenol by the frog Rana temporaria.

Frogs injected with phenol excrete 67-95% of dose in 15 h; 32-87% of dose are metabolites. Metabolites identified were phenyl sulphate (15-44% of dose), phenyl glucuronide (10-25% of dose), catechol sulphate (up to 7% of dose), quinol sulphate (1-25% of dose), resorcinol and catechol (traces).

Animals↗
PubMed1990

A sensitive method to quantitate gangliosides of the gangliotetraose series directly on chromatograms using peroxidase conjugated cholera toxin.

A method is described whereby ganglioside GM1 can be quantitated directly on thin-layer chromatograms using cholera toxin subunit B conjugated to horseradish peroxidase and visualized with chloronaphthol. Overlay and color development were performed after separating gangliosides on nano-TLC plates, and fixing with polyisobutylmethacrylate. Absolute quantitation was realized using a Shimadzu CS-9000 integrating spectrodensitometer, scanning at 580 nm. A correlation coefficient of 0.98 was obtained in a linear range of detection from 10(-11) to 10(-16) moles. Statistical analysis revealed good reproducibility and over 99% of the added gangliosides remained with the chromatogram during all overlay and washing procedures. By comparison, standard chemical visualization by resorcinol-HCl was linear in the nanomole range with a detection limit of only 10(-10) moles. Since the carbohydrate portion of gangliosides immobilized in this manner is susceptible to the action of enzymes including neuraminidase, this technique can be applied to all structures of the gangliotetraose series.

Animals↗
PubMed1988

Collagen based biomaterials: an ideal way of increasing their resistance to infection.

Collagen and gelatin containing biomaterials are relatively more susceptible to bacterial infection. Systemic administration or local delivery of antibiotics after implantation does not seem to solve the problem either effectively or easily. Antibiotics may be incorporated in the implant; but many, being water soluble, are quickly absorbed and not effective for adequate time periods. Resorcinol monoacetate (RMA) is a relatively water insoluble antibacterial agent which partially crosslinks collagen and has the potential to be an intrinsic antibiotic in collagenous bioprostheses. This study confirms the efficacy of RMA as a chemical that: (a) mildly crosslinks collagen at pH 3.5-4.5; (b) releases very slowly from the pretreated collagen sponge when washed in aqueous medium; (c) inhibits bacterial growth on the pretreated collagen sponges, at 2% (w/w) concentration, for at least 12 days; (d) remains biocompatible under treated conditions.

Animals↗
PubMed2004

Immunopathogenesis of experimental ulcerative colitis is mediated by eosinophil peroxidase.

The precise role that individual inflammatory cells and mediators play in the development of gastrointestinal (GI) dysfunction and extraintestinal clinical manifestations of ulcerative colitis (UC) is unknown. In this study, we have used a mouse model of UC to establish a central role for eotaxin and, in turn, eosinophils in the development of the immunopathogenesis of this disease. In this model the administration of dextran sodium sulfate (DSS) induces a prominent colonic eosinophilic inflammation and GI dysfunction (diarrhea with blood and shortening of the colon) that resembles UC in patients. GI dysfunction was associated with evidence of eosinophilic cytolytic degranulation and the release of eosinophil peroxidase (EPO) into the colon lumen. By using IL-5 or eotaxin-deficient mice, we show an important role for eotaxin in eosinophil recruitment into the colon during experimental UC. Furthermore, using EPO-deficient mice and an EPO inhibitor resorcinol we demonstrate that eosinophil-derived peroxidase is critical in the development of GI dysfunction in experimental UC. These findings provide direct evidence of a central role for eosinophils and EPO in GI dysfunction and potentially the immunopathogenesis of UC.

Animals↗
PubMed1975

Respiratory tract disease from thermosetting resins. Study of an outbreak in rubber tire workers.

An outbreak of upper and lower respiratory tract inflammatory disease and conjunctivitis among synthetic rubber tire workers occurred. The outbreak began after the introduction of a new thermosetting resin, containing resorcinol and a trimere of methylene aminoacetronitrile, into the rubber tire carcass stock formulation. Two hundred ten workers were affected. Characteristically, symptoms improved during periods of sick leave or vacation, recurring upon the workers' return to the plant. Chest radiograms disclosed pneumonic infiltrates in about one fourth of the cases. Pulmonary function studies detected abnormal airways dynamics as well as abnormal diffusing capacity in more than one third of the workers tested. Lung biopsy showed evidence of focal interstitial fibrosis and peribronchiolar and perivascular chronic inflammatory reaction. The illness was ascribed to volatile products released during the manufacture of synthetic rubber tires. The exact chemical nature of these products is unknown.

Adult↗
PubMed1999

The evolution of beta-agonists.

Inhaled beta-agonists have become the mainstay of bronchodilator therapy for reactive airway diseases, either alone or in conjunction with other medications. The history of the development of beta-agonists is a fascinating one that spans more than 5000 years. Scientific investigation for the past several hundred years has elucidated the physiology of bronchoconstriction and bronchodilation. In the past decade, a wealth of knowledge has come forth since the discovery of the beta-adrenoceptor which, along with advances in pharmacology, have helped answer the questions of how beta-agonists work. From these advancements, three classes of beta-agonists have been developed: catecholamines, resorcinols, and saligenins. The chemical structures of the more commonly used agents in each class, their interaction with the beta-adrenoceptor, and their beneficial and adverse effects are discussed. Review of the duration of action of these agents may suggest a new way of classifying them into ultrashort-acting, short-acting, intermediate-acting, and long-acting.

Adrenergic beta-Agonists↗
PubMed1999

Cyanoacrylate glue as an alternative to an additional suture line in the repair of type A aortic dissection.

We describe the use of cyanoacrylate glue in conjunction with gelatin-resorcinol-formalin glue for the treatment of type A aortic dissection. Instead of placing an additional suture line 2-3 cm from the edges of the aortic stumps to create a large pocket for gluing, we have been using a cyanoacrylate adhesive for approximating the walls of the true and false lumina without the risk of tearing them. Moreover, the simplicity and quickness of the procedure enables application of the cyanoacrylate glue even deeper into the aortic arch, creating a wider area for gluing the dissected layers.

Aortic Dissection↗
PubMed2000

Liposomal drug delivery, a novel approach: PLARosomes.

Almost from the time of their rediscovery in the 60's and the demonstration of their entrapment potential, liposomal vesicles have drawn attention of researchers as potential carriers of various bioactive molecules that could be used for therapeutic applications in humans and animals. Several commercial liposome-based drugs have already been discovered, registered and introduced with great success on the pharmaceutical market. However, further studies, focusing on the elaboration of more efficient and stable amphiphile-based vesicular (or non-viral) drug carriers are still under investigation. In this review we present the achievements of our group in this field. We have discovered that natural amphiphilic dihydroxyphenols and their semisynthetic derivatives are promising additives to liposomal lipid compositions. The presence of these compounds in lipid composition enhances liposomal drug encapsulation, reduces the amount of the lipid carrier necessary for efficient entrapment of anthracycline drugs by a factor of two, stabilizes liposomal formulation of the drug (both in suspension and in a lyophilized powder), does not influence liposomal fate in the blood circulation system and benefits from other biological activities of their resorcinolic lipid modifiers.

Anthracyclines↗
PubMedDate not supplied

[Polyphenolic antioxidants efficiently protect urease from inactivation by ultrasonic cavitation].

Inactivation of urease (25 nM) in aqueous solutions (pH 5.0-6.0) treated with low-frequency ultrasound (LFUS; 27 kHz, 60 Wt/cm2, 36-56 degrees C) or high-frequency ultrasound (HFUS; 2.64 MHz, 1 Wt/cm2, 36 or 56 degrees C) has been characterized quantitatively, using first-order rate constants: kin, aggregate inactivation; kin*, thermal inactivation; and kin* (US), ultrasonic inactivation. Within the range from 1 nM to 10 microM, propyl gallate (PG) decreases approximately threefold the rate of LFUS-induced inactivation of urease (56 degrees C), whereas resorcinol poly-2-disulfide prevents this process at 1 nM or higher concentrations. PG completely inhibits HFUS-induced inactivation of urease at 1 nM (36 degrees C) or 10 nM (56 degrees C). At 0.2-10 microM, human serum albumin (HSA) increases the resistance of urease (at 56 degrees C) treated with HFUS to temperature- and cavitation-induced inactivation. Complexes of gallic acid polydisulfide (GAPDS) with HSA (GAPDS-HSA), formed by conjugation of 1.0 nM PGDS with 0.33 nM HSA, prevent HFUS-induced urease inactivation (56 degrees C).

Antioxidants↗
PubMed2001

[Simultaneous determination of cobalt and nickel in catalyst by microwave digestion-dual wavelength equal absorption spectrophotometry].

Catalyst samples are digested in a microwave digestion system. The optimum parameters for microwave digestion are selected. Cobalt and nickel in the mixture of Co2+ and Ni2+ with 4-(2-pyridylazo) resorcinol (PAR) can be determined simultaneously by dual-wavelength equal absorption spectrophotometry. By means of the combination of two methods, Co2+ and Ni2+ in catalyst can be determined rapidly, accurately, and contamination problems avoided. The linear ranges are 0-30 micrograms.25 mL-1 for Co2+ and 0-25 micrograms.25 mL-1 for Ni2+. The recoveries of Co2+ and Ni2+ in synthetic samples are between 98.2%-103.6% and between 97.9%-103.7%, respectively. The relative standard deviations of analytical results in catalyst samples are less than 2.2% for Co2+ and less than 1.8% for Ni2+, and relative errors are less than +/- 2.5% for Co2+ and Ni2+.

Catalysis↗
PubMed2001

[Study on the energy transfer fluorescence quenching among combination of acridine yellow-PAR determination of trace iron].

An energy transfers technique between 4-(2-Pyridylazo) resorcinol(PAR) and acridine yellow is studied, and optimum experimental conditions of energy transfer is done as well. It is found that in the aqueous solution of sodium lauryl sulfate, NH3.H2O-NH4Cl buffer solution at pH = 9.2, the energy transfers from acridine yellow to iron(II)-PAR complexes. So a new method of fluorometric energy transfers determination of trace iron(II) by acridine yellow--PAR was described. The range of determination of iron is 0-10 micrograms.L-1. The detection limit for iron is 0.06 microgram.L-1. The method has been applied to the determination of iron in water sample and hair with satisfactory results.

Aminoacridines↗
PubMed1977

Nonenzymic spectrophotometric determination of potential poison ivy cross-reactors.

I describe an inexpensive, nonenzymic analytical system for prescreening substances that might cross-react as Rhus toxing (e.g., poison ivy, poison oak, and sumac allergens) on human skin. By spectrophotometric assay after incubation with an oxidizing mixture of Cu(II)ammine complex and ammonium persulfate, I could accurately and reproducibly determine o-quinoidal products of several potential synthetic cross-reactors and native poison ivy allergen, and could distinguish these from catecholamines, resorcinol, p-hydroquinone, and a closely related phenol. A good correlation was obtained between this nonenzymic technique and an enzymic assay. This Cu(II)ammine/persulfate oxidative assay, however, is inexpensive and obviates any spectral interference from enzymic proteins.

Allergens↗