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At least 685 records · Page 38Linked to original sources
PubMed2003

Microbial transformation of xanthohumol.

Microbial transformation of xanthohumol using the culture broth of Pichia membranifaciens afforded three metabolites, (E)-2"-(2"'-hydroxyisopropyl)-dihydrofurano[2",3":4',3']-2', 4-dihydroxy-6'-methoxychalcone, (2S)-2"-(2"'-hydroxyisopropyl)-dihydrofurano[2",3":7,8]-4'-hydroxy-5-methoxyflavanone and (E)-2"-(2"'-hydroxyisopropyl)-dihydrofurano[2",3":2',3']-4'-hydroxy-5-methoxychalcone.

Biotransformation↗
PubMed1997

Xanthohumols, diacylglycerol acyltransferase inhibitors, from Humulus lupulus.

A methanol extract of hops of Humulus lupulus (L.) showed inhibitory activity against rat liver diacylglycerol acyltransferase (DGAT). From DGAT inhibitory activity-guided fractionation, two chalcones were isolated. One was identified as xanthohumol and the other was found to be a new product designated xanthohumol B. The structure of xanthohumol B was shown to be 6-[3,4-dihydro-3,5-dihydroxy-7-methoxy-2,2-dimethyl-2H-benzo[b]pyrano ]- 3-(4-hydroxyphynyl)-2-propen-l-one by spectroscopic studies including various NMR measurements. Xanthohumol and xanthohumol B inhibited DGAT activity with IC50 values of 50.3 and 194 microM in rat liver microsomes, respectively. They showed preferential inhibition of triacylglycerol formation in intact Raji cells, indicating that they inhibit DGAT activity preferentially in living cells.

Acyltransferases↗
PubMed2002

Central stimulants as discriminative stimuli. Asymmetric generalization between (-)ephedrine and S(+)methamphetamine.

Central stimulants readily serve as training stimuli in drug discrimination studies and typically substitute for one another in tests of stimulus generalization regardless of which is used as training drug. We have previously found that, although substitution occurs between (+)amphetamine and (-)ephedrine, substitution did not occur upon administration of S(+)methamphetamine to (-)ephedrine-trained animals. In the present investigation, rats were trained to discriminate S(+)methamphetamine (1 mg/kg) from saline vehicle and tests of stimulus generalization were performed with several stimulants, including (-)ephedrine. The S(+)methamphetamine stimulus (ED(50)=0.06 mg/kg) generalized to R(-)methamphetamine (ED(50)=1.61 mg/kg), S(+)amphetamine (ED(50)=0.28 mg/kg), S(-)methcathinone (ED(50)=0.21 mg/kg), methylphenidate (ED(50)=0.28 mg/kg), cocaine (ED(50)=3.68 mg/kg) and (-)ephedrine (ED(50)=13.1 mg/kg). Hence, stimulus generalization between S(+)methamphetamine and (-)ephedrine is apparently asymmetrical. In a companion study, R(-)methamphetamine was administered to rats trained to discriminate (-)ephedrine (4 mg/kg); substitution occurred and R(-)methamphetamine (ED(50)=0.92 mg/kg) was found to be nearly equipotent with (-)ephedrine (ED(50)=0.8 mg/kg). Although the exact basis for the observed results are unclear, they are discussed in terms of the different effects of (-)ephedrine and the methamphetamine optical isomers on neurotransmitter release and reuptake.

Animals↗
PubMed1997

Drug-drug discrimination: stimulus properties of drugs of abuse upon a serotonergic-dopaminergic continuum.

Ten male N/Nih rats were trained to discriminate between the interoceptive cues produced by the purportedly dopaminergically-mediated drug d-amphetamine at 0.4 mg/kg intraperitoneally administered 20 min prior to training and those produced by the purportedly serotonergically-active agent norfenfluramine at 0.7 mg/kg. Once this discrimination was successfully acquired, the rats were tested with saline and with both drugs administered simultaneously and these manipulations were seen to produce random responding; indicating roughly equivalent cueing strength. Subsequently, various drugs thought to act upon serotonergic neurons, i.e., LSD and MDMA, were tested and shown to generalize in a dose-responsive manner to the norfenfluramine-appropriate lever. In contrast, the dopaminergically-active agent methcathinone and the D3 agonist 7-OH-DPAT produced generalization on the amphetamine-appropriate lever. Results are discussed in light of the increased specificity of behavioral testing available in a drug vs. drug discriminative paradigm using two drugs with different mechanisms of action.

Amphetamine↗
PubMed1997

Discriminative characteristics of high and low cocaine administration: effect of other psychostimulants.

Two groups of N/Nih male rats were trained to discriminate saline vehicle from either 2.0 mg/kg (n = 10) or 10.0 mg/kg (n = 10) cocaine in a food-motivated, two-lever operant paradigm. The rats trained at the low-dose cocaine took a significantly longer training period to reach criterion performance than did the high-dose cocaine group. In addition, the ED50 value for the 2.0 mg/kg cocaine-trained animals (0.465 mg/kg) was significantly lower than the ED50 value (2.105 mg/kg) for those animals trained at the 10.0 mg/kg dose of cocaine. This correlation of ED50 values for stimulus generalization decreasing with reduction in training dose was in contrast to the time-course of the two groups when tested from 15 to 240 min post-injection; this experimentation indicated that there was a non-significant difference in half-life for the 2.0 mg/kg (t1/2: 97.1 min) vs. that of the 10.0 mg/kg cocaine-trained group (t1/2: 83.4 min). Generalization tests with other purportedly dopaminergically-active drugs of abuse including 0.05-0.8 mg/kg d-amphetamine, 0.125-1.5 mg/kg methamphetamine and 0.125-1.0 mg/kg methcathinone indicated that the highest doses of each produced generalization and, with the exception of methcathinone, the ED50 values were significantly lower in the low-cocaine trained group. The stimulus properties of cocaine, as they generalize to amphetamine, methamphetamine and methcathinone, can be explained by effects upon central dopaminergic neurons and may be qualitatively different in low-and high-dose trained rats.

Amphetamine↗
PubMed2000

Functional discovery via a compendium of expression profiles.

Ascertaining the impact of uncharacterized perturbations on the cell is a fundamental problem in biology. Here, we describe how a single assay can be used to monitor hundreds of different cellular functions simultaneously. We constructed a reference database or "compendium" of expression profiles corresponding to 300 diverse mutations and chemical treatments in S. cerevisiae, and we show that the cellular pathways affected can be determined by pattern matching, even among very subtle profiles. The utility of this approach is validated by examining profiles caused by deletions of uncharacterized genes: we identify and experimentally confirm that eight uncharacterized open reading frames encode proteins required for sterol metabolism, cell wall function, mitochondrial respiration, or protein synthesis. We also show that the compendium can be used to characterize pharmacological perturbations by identifying a novel target of the commonly used drug dyclonine.

Cell Wall↗
PubMed2004

Antiviral activity of hop constituents against a series of DNA and RNA viruses.

We investigated whether crude hop extracts and purified hop components representing every major chemical class of hop compound have antiviral activity. These hop constituents were tested for antiviral activity against bovine viral diarrhea virus (BVDV) as a surrogate model of hepatitis C virus (HCV), human immunodeficiency virus (HIV), influenza A virus (FLU-A), influenza B virus (FLU-B), rhinovirus (Rhino), respiratory syncytial virus (RSV), yellow fever virus (YFV), cytomegalovirus (CMV), hepatitis B virus (HBV), and herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). The extracts all failed to prevent the replication of HIV, FLU-A, FLU-B, RSV and YFV. A xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Pure iso-alpha-acids demonstrated low to moderate antiviral activity against both BVDV (TI=9.1) and CMV (TI=4.2) with IC(50) values in the low microg/ml range. No antiviral activity was detected using beta-acids or a hop oil extract. Ultra-pure preparations (>99% pure) were used to show that xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 and HSV-2. Xanthohumol was found to be a more potent antiviral agent against these viruses than the isomer iso-xanthohumol. With Rhino, the opposite trend was observed with iso-xanthohumol showing superior antiviral activity to that observed with xanthohumol. Xanthohumol also showed antiviral activity against CMV, suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV. In summary, iso-alpha-acids and xanthohumol were shown to have a low-to-moderate antiviral activity against several viruses. These hop constituents might serve as interesting lead compounds from which more active anti-HCV, anti-Rhino and anti-herpesvirus antiviral agents could be synthesized.

Animals↗
PubMed1985

Allergic contact dermatitis to dyclonine hydrochloride simulating extensive herpes simplex labialis.

Two patients developed allergic contact dermatitis to 1% dyclonine hydrochloride gel, a nonprescription topical anesthetic widely marketed for the symptomatic treatment of herpes simplex labialis. Both patients mistakenly believed that the eruption was expanding herpes simplex labialis, which resulted in their more frequent application of the dyclonine hydrochloride and a delay in diagnosis. Dermatologists should recognize that 1% dyclonine hydrochloride gel can cause allergic contact dermatitis that can masquerade as widespread herpes simplex labialis.

Adult↗
PubMed1986

Efficacy of a sunscreen containing butyl methoxydibenzoylmethane against ultraviolet A radiation in photosensitized subjects.

Topical formulations containing a new chemical entity, the ultraviolet A absorber Parsol 1789 (butyl methoxydibenzoylmethane), were evaluated as agents for protecting human skin against ultraviolet A (UVA) radiation. Healthy subjects were photosensitized to UVA radiation by ingestion of 8-methoxypsoralen (0.6 mg/kg). After 90 minutes, five formulations (vehicle, vehicle + butyl methoxydibenzoylmethane, vehicle + butyl methoxydibenzoylmethane + padimate O, vehicle + padimate O, and a marketed sunscreen containing padimate O, oxybenzone, and octyl salicylate) were applied in a randomized, double-blind manner to areas on the lower part of the back. Thirty minutes later, sites in the five treated areas and in a sixth unprotected area were exposed to graduated doses of UVA radiation. Test sites were evaluated for erythema 48 and 72 hours after UVA exposure, and for melanogenesis approximately 2 weeks later. The combination of butyl methoxydibenzoylmethane + padimate O demonstrated significantly greater protection than the combination of padimate O, oxybenzone, and octyl salicylate.

4-Aminobenzoic Acid↗
PubMed1987

Comparison of methods for assessing photoprotection against ultraviolet A in vivo.

Photoprotection against ultraviolet A (UVA) by three sunscreens was evaluated in humans, with erythema and pigmentation used as end points in normal skin and in skin sensitized with 8-methoxypsoralen and anthracene. The test sunscreens were Parsol 1789 (2%), Eusolex 8020 (2%), and oxybenzone (3%). UVA was obtained from two filtered xenon-arc sources. UVA protection factors were found to be significantly higher in sensitized skin compared with normal skin. Both Parsol and Eusolex provided better and comparable photoprotection (approximately 3.0) than oxybenzone (approximately 2.0) in sensitized skin, regardless of whether 8-methoxypsoralen or anthracene was used. In normal unsensitized skin, Parsol 1789 and Eusolex 8020 were also comparable and provided slightly better photoprotection (approximately 1.8) than oxybenzone (approximately 1.4) when pigmentation was used as an end point. The three sunscreens, however, were similar in providing photoprotection against UVA-induced erythema. Protection factors obtained in artificially sensitized skin are probably not relevant to normal skin. It is concluded that pigmentation, either immediate or delayed, is a reproducible and useful end point for the routine assessment of photoprotection of normal skin against UVA.

Adolescent↗
PubMed1987

Indoor and outdoor efficacy testing of a broad-spectrum sunscreen against ultraviolet A radiation in psoralen-sensitized subjects.

The efficacy of a sunscreen containing an investigational drug, butyl methoxydibenzoylmethane in combination with padimate O against the erythemogenic effect of ultraviolet A (UVA) radiation was evaluated in two double-blind studies involving subjects sensitized with topical 8-methoxypsoralen. UVA radiation was supplied from either a filtered solar simulator (indoors) or filtered sunlight (outdoors). Five formulations were tested: 3% butyl methoxydibenzoylmethane and 7% padimate O, 7% padimate O, 5% octyl salicylate, and 3% oxybenzone, 3% butyl methoxydibenzoylmethane alone, 7% padimate O alone, and vehicle. Sunscreen protection against the erythemogenic effect of UVA radiation was expressed as phototoxic protection factors. The phototoxic protection factor for each sunscreen was derived from a ratio of the minimal phototoxic dose of UVA radiation that produced delayed erythema on sunscreen-protected and unprotected skin. The combination of 3% butyl methoxydibenzoylmethane and 7% padimate O provided significantly greater protection than the other sunscreen formulations, and for each sunscreen the phototoxic protection factors determined indoors and outdoors were comparable.

4-Aminobenzoic Acid↗
PubMed1993

Methcathinone: a Russian designer amphetamine infiltrates the rural midwest.

Four cases of methcathinone toxicity in the United States are presented and discussed. This drug is the latest in a series of "designer" amphetamines. Prominent findings of acute toxicity include hallucinations, fever, and tachycardia followed by periods of bradycardia and moderate hypotension as acute symptoms resolve. Chronic binge use may result in development of paranoid psychosis and brief periods of withdrawal tremors. Our current understanding of methcathinone effects and the Russian experience with it are discussed. Our recommendations for treatment of acute toxicity are based on well established guidelines for managing the toxicity of similar amphetamine-like drugs.

Adult↗