Anti-alcoholic effects of honeys from different floral origins and their correlation with honey chemical compositions.

The effects of honeys from different floral origins on alcohol metabolism were compared, and the correlation between their chemical compositions and antialcholic effects was analyzed. The results demonstrated that the five types of investigated honeys from different floral origins had different effects on alcohol metabolism, and the blood alcohol removal rate by these honeys ranged from 18.01% to 49.17%. Ziziphus jujuba honey exhibited the best blood alcohol removal effect, and meanwhile significantly enhanced the activity of alcohol-metabolizing enzymes including alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH). Chemical composition analysis also showed that honeys from different floral origins were considerably different in the contents of sugars, minerals, ascorbic acid and phenolics. Ziziphus jujuba honey had the highest fructose/glucose ratio, ascorbic acid and phenolics contents, and higher contents of minerals, especially K, Ca, Mg, Fe, Cu, Zn and Mn. This chemical composition might contribute to its better anti-alcoholic effect.

Red mulberry fruit aqueous extract and silk proteins accelerate acute ethanol metabolism and promote the anti­oxidant enzyme systems in rats.

Red mulberry (Morus alba) fruit is rich in anthocyanins, and mulberry leaves are used by silk worms to make silk protein. We determined that the water and ethanol extract of mulberry fruit and silk amino acids accelerated ethanol degradation and suppressed temporal cognitive dysfunction in acute alcohol administered rats. The mechanism was explored in rats with acute oral administration of silk protein and mulberry fruit extracts. Rats were given 0.3 g of dextrin (control) and water extract (WMB) and ethanol extract of mulberry (EMB), silk protein hydrolysates (SKA), and a commercial product (positive­control) based on body weight. After 30 min, rats were administered 3 g ethanol/kg body weight and serum ethanol and acetaldehyde levels were measured. After 3 h movements were measured with a video tracking system and at 5 h cognitive function was measured by Y maze test. WMB contain much higher rutin, luteolin and quercetins than EMB. In SKA rats, serum alcohol concentrations slowly increased until 60 min, but were markedly elevated until 120 min. However, WMB rats exhibited rapidly increased serum alcohol levels until 60 min and showed the lowest peak of serum alcohol levels, indicating the highest degradation of alcohol. The patterns of serum acetaldehyde levels were similar to those of serum ethanol levels but WMB was more effective for reducing serum acetaldehyde levels than serum ethanol levels. WMB was most effective for increasing mRNA expression of alcohol dehydrogenase and acetaldehyde dehydrogenase. WMB and SKA decreased lipid peroxides by increasing activities of SOD and GSH­Px in the liver and they also reduced pro­inflammatory cytokines such as tumor necrosis factor­α and interleukin­6. WMB and SKA exerted better anti­oxidant effects than the positive­control. WMB containing higher flavonoids reduced pro­inflammatory cytokines better than SKA. In conclusions, both WMB and SKA might reduce acute alcohol­induced hangover and liver and brain damage by lowering serum alcohol and acetaldehyde levels.

ß-Caryophyllene protects against alcoholic steatohepatitis by attenuating inflammation and metabolic dysregulation in mice.

BACKGROUND AND AIMS: ß-Caryophyllene (BCP) is a plant-derived FDA approved food additive with anti-inflammatory properties. Some of its beneficial effects in vivo are reported to involve activation of cannabinoid CB2 receptors that are predominantly expressed in immune cells. Here, we evaluated the translational potential of BCP using a well-established model of chronic and binge alcohol-induced liver injury. METHODS: In this study, we investigated the effects of BCP on liver injury induced by chronic plus binge alcohol feeding in mice in vivo by using biochemical assays, real-time PCR and histology analyses. Serum and hepatic BCP levels were also determined by GC/MS. RESULTS: Chronic treatment with BCP alleviated the chronic and binge alcohol-induced liver injury and inflammation by attenuating the pro-inflammatory phenotypic `M1` switch of Kupffer cells and by decreasing the expression of vascular adhesion molecules intercellular adhesion molecule 1, E-Selectin and P-Selectin, as well as the neutrophil infiltration. It also beneficially influenced hepatic metabolic dysregulation (steatosis, protein hyperacetylation and PPAR-α signalling). These protective effects of BCP against alcohol-induced liver injury were attenuated in CB2 receptor knockout mice, indicating that the beneficial effects of this natural product in liver injury involve activation of these receptors. Following acute or chronic administration, BCP was detectable both in the serum and liver tissue homogenates but not in the brain. CONCLUSIONS: Given the safety of BCP in humans, this food additive has a high translational potential in treating or preventing hepatic injury associated with oxidative stress, inflammation and steatosis. LINKED ARTICLES: This article is part of a themed section on Inventing New Therapies Without Reinventing the Wheel: The Power of Drug Repurposing. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.2/issuetoc.

Evolution of matrinic ethanol derivatives as anti-HCV agents from matrine skeleton.

Twenty-two novel 12N-substituted matrinic ethanol derivatives were synthesized and evaluated for their antiviral activities against HCV taking compound 1 as the lead. The SAR study indicated that the shortening of the 11-butyl chain to ethyl chain did not affect the activity significantly. Out of the target compounds, matrinic ethanol 6a demonstrated a potential anti-HCV effect with an EC50 value of 3.2µM and a SI value of 96.6. The free hydroxyl arm in 6a made it possible as a parent structure to prepare pro-drug for the potential application in HCV treatment. This study provided powerful information on further strategic optimization and development of this kind of compounds into a novel family of anti-HCV agents.

Effects of antrosterol from Antrodia camphorata submerged whole broth on lipid homeostasis, antioxidation, alcohol clearance, and anti-inflammation in livers of chronic-alcohol fed mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Antrodia camphorata is a functional fungus in Taiwan and owns several pharmacological functions. Antrosterol, a bioactive constitute of sterols in edible Antrodia camphorata submerged whole broth, can protect liver from CCl4 damage via enhancing antioxidant and anti-inflammatory capacities. AIM OF THE STUDY: The aim of this study was to investigate the hepatoprotection of antrosterol (named as EK100) against alcohol consumption. MATERIALS AND METHODS: A Lieber-DeCarli regular EtOH diet (EtOH liquid diet, 5% (v/v) alcohol) was applied to induce alcoholic liver damage. Mice were randomly divided into 5 groups: (1) Control: control liquid diet; (2) EtOH: EtOH liquid diet; (3) EK100_1X: EtOH liquid diet and 1mg EK100 (Antrosterol)/Kg body weight (bw); (4) EK100_5X: EtOH liquid diet and 5mg EK100/Kg bw; (5) EK100_10X: EtOH liquid diet and 10mg EK100/Kg bw. At the end of experiment, the livers were collected for histo-pathological analyses, RNA and protein extraction, and enzymatic activities. RESULTS: Antrosterol reduced serum/liver lipids of alcohol-diet fed mice which highly related to upregulated fatty acid ß-oxidation and downregulated lipogenesis, and increased fecal lipid/bile-acid outputs. Antrosterol enhanced hepatic antioxidant capabilities in alcohol-diet fed mice while it also lowered serum alcohol level, as well as increased alcohol dehydrogenase (ADH) and catalase (CAT) activities and decreased CYP2E1 protein expression in livers of alcohol-diet fed mice. Besides, antrosterol lowered hepatic inflammation and fibrosis related gene expressions, as well as serum AST/ALT values and TNF-α/IL-1ß contents in alcohol-diet fed mice. CONCLUSION: Based on the results, hepatoprotection of antrosterol is mostly attributed to its regulations of lipid homeostasis, antioxidant capability, alcohol metabolism, and anti-inflammation.

Dietary Fisetin Supplementation Protects Against Alcohol-Induced Liver Injury in Mice.

BACKGROUND: Overproduction of reactive oxygen species is associated with the development of alcoholic liver disease (ALD). Plant polyphenols have been used as dietary interventions for multiple diseases including ALD. The objective of this study was to determine whether dietary supplementation with fisetin, a novel flavonoid, exerts beneficial effect on alcohol-induced liver injury. METHODS: C57BL/6J mice were pair-fed with the Lieber-DeCarli control or ethanol (EtOH) diet for 4 weeks with or without fisetin supplementation at 10 mg/kg/d. RESULTS: Alcohol feeding induced lipid accumulation in the liver and increased plasma alanine aminotransferase and aspartate aminotransferase activities, which were attenuated by fisetin supplementation. The EtOH concentrations in the plasma and liver were significantly elevated by alcohol exposure but were reduced by fisetin supplementation. Although fisetin did not affect the protein expression of alcohol metabolism enzymes, the aldehyde dehydrogenase activities were significantly increased by fisetin compared to the alcohol alone group. In addition, fisetin supplementation remarkably reduced hepatic NADPH oxidase 4 levels along with decreased plasma hydrogen peroxide and hepatic superoxide and 4-hydroxynonenal levels after alcohol exposure. Alcohol-induced apoptosis and up-regulation of Fas and cleaved caspase-3 in the liver were prevented by fisetin. Moreover, fisetin supplementation attenuated alcohol-induced hepatic steatosis through increasing plasma adiponectin levels and hepatic protein levels of p-AMPK, ACOX1, CYP4A, and MTTP. CONCLUSIONS: This study demonstrated that the protective effect of fisetin on ALD is achieved by accelerating EtOH clearance and inhibition of oxidative stress. The data suggest that fisetin has a therapeutical potential for treating ALD.

Measurement of Procedure-Specific Irrigation-Fluid Absorption in Transurethral Therapy of Lower Urinary Tract Syndrome, Using Ethanolic Saline and Breath Alcometry.

INTRODUCTION: Transurethral resection risks excessive absorption of irrigating fluid with potentially severe or life-threatening consequences. We determined the amount of absorbed saline irrigation fluid during photoselective vaporisation of the prostate (PVP) and bipolar transurethral resection of the prostate (bTURP). PATIENTS AND METHODS: Patients at our institution treated by one of these methods were monitored by the alcometric method: ethanol is added to the irrigation fluid and blood alcohol is measured with a breathalyser. Various possible correlations were investigated. RESULTS: Data from 71 patients (36 PVP, 35 bTURP) were analysed. Detection of any absorption was more frequent under bTURP (71% of patients) than under PVP (39%; p = 0.006). Absorption in the volume range 500-1,000 ml was conspicuously more frequent in the bTURP procedure than in PVP. CONCLUSIONS: Presence of absorption was more frequent under bTURP than under PVP. However, high-volume absorption was more frequent during bTURP than in PVP.

[Effect of the Chinese Herbal Medicinal Ingredients in Huoxiang Zhengqi Liquid on Alcohol Metabolism in Rats].

OBJECTIVES: To study the changes of alcohol content and pharmacokinetic parameter in rats after taking Huoxiang Zhengqi liquid. METHODS: The rats were randomly divided into three groups and given with white alcohol at the dose of 3.0 mL/kg, low-dose and high-dose Chinese medicine liquor, respectively. The blood was collected before administration and 5 min, 10 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 5 h, 6 h and 8 h after administration by cutting rats' tails. The concentrations of alcohol in blood were detected by headspace-gas chromatography method. The main pharmacokinetic parameters were calculated by DAS 2.0, and then analyzed by SPSS 17.0. RESULTS: The difference of maximum blood concentrations between high-dose Chinese medicine alcohol group and white alcohol group was statistically significant （P<0.05）. There was no significant difference in other pharmacokinetic parameters among three groups （P>0.05）. CONCLUSIONS: The Chinese herbal medicinal ingredients in the Huoxiang Zhengqi liquid has no effect on the metabolism and elimination of ethanol in rats. The research provides useful reference for the qualitative assessment and processing of traffic accident cases involved in Huoxiang Zhengqi liquid and the studies related to drug-interaction.

Effect of the Chinese Herbal Medicinal Ingredients in Huoxiang Zhengqi Liquid on Alcohol Metabolism in Rats / 法医学杂志

OBJECTIVES@#To study the changes of alcohol content and pharmacokinetic parameter in rats after taking Huoxiang Zhengqi liquid.@*METHODS@#The rats were randomly divided into three groups and given with white alcohol at the dose of 3.0 mL/kg, low-dose and high-dose Chinese medicine liquor, respectively. The blood was collected before administration and 5 min, 10 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 5 h, 6 h and 8 h after administration by cutting rats' tails. The concentrations of alcohol in blood were detected by headspace-gas chromatography method. The main pharmacokinetic parameters were calculated by DAS 2.0, and then analyzed by SPSS 17.0.@*RESULTS@#The difference of maximum blood concentrations between high-dose Chinese medicine alcohol group and white alcohol group was statistically significant （P<0.05）. There was no significant difference in other pharmacokinetic parameters among three groups （P>0.05）.@*CONCLUSIONS@#The Chinese herbal medicinal ingredients in the Huoxiang Zhengqi liquid has no effect on the metabolism and elimination of ethanol in rats. The research provides useful reference for the qualitative assessment and processing of traffic accident cases involved in Huoxiang Zhengqi liquid and the studies related to drug-interaction.

A pilot study on the ability of clinoptilolite to absorb ethanol in vivo in healthy drinkers: effect of gender.

Zeolites are microscopic minerals of volcanic origin, and the zeolite most commonly used in medicine is clinoptilolite. Over the years, clinoptilolite has been tested in several ways: as an antioxidant, as an adjuvant in anticancer therapy due to its ability to capture chemotoxins, as an antidiarrhoeal agent and as a chelating agent for heavy metals. The aim of this study was to evaluate the ability of clinoptilolite to absorb ethanol in vivo in healthy drinkers. We enrolled 12 healthy drinkers in this study. The study was conducted as follows: phase 1: consumption of a hydroalcoholic solution containing 25 g of ethanol; phase 2: use of a 16.25 mL medical device containing clinoptilolite (2.5 g of clinoptilolite within a single-dose sachet) + consumption of a hydroalcoholic solution containing 25 g of ethanol; phase 3: use of a 32.5 mL medical device (5 g of clinoptilolite within a single-dose sachet) + consumption of a hydroalcoholic solution containing 25 g of ethanol. At the time of blood sampling, alcohol ingestion was also measured using an Alcolmeter instrument, and the results showed that the two methods overlapped. Reductions of 43%, 35%, 41% and 34% in blood ethanol at 30, 60, 90 and 120 minutes, respectively, were observed after the consumption of 5 g of clinoptilolite + 25 g of ethanol in both males and females, whereas the consumption of 2.5 g of clinoptilolite did not result in a statistically significant reduction in blood ethanol. In particular, the blood ethanol reduction was more significant in males. Our study highlights and confirms the ability of clinoptilolite to decrease the absorption of ingested ethanol by reducing blood alcohol levels. This effect was statistically significant at a dose of 5 g.

Is absorption of irrigation fluid a problem in Thulium laser vaporization of the prostate? A prospective investigation using the expired breath ethanol test.

BACKGROUND: Benign prostatic hyperplasia (BPH) is a prevalent entity in elderly men. If medical treatment fails, monopolar transurethral resection of the prostate (TUR-P) is still considered as the standard treatment. The proportion of high-risk patients with cardiac comorbidities increases and TUR-P goes along with a relevant perioperative risk. Especially large volume influx of irrigation fluid and transurethral resection syndrome (TUR syndrome) represent serious threats to these patients. Using isotonic saline as irrigation fluid like in transurethral laser vaporization (TUV-P), TUR syndrome can be prevented. However, no prospective trial has ever assessed occurrence or extent of irrigation fluid absorption in Thulium Laser TUV-P. METHODS/DESIGN: This is a single-center prospective trial, investigating, if absorption of irrigation fluid occurs during Thulium Laser TUV-P by expired breath ethanol test. The expired breath ethanol technique is an established method of investigating intraoperative absorption of irrigation fluid: A tracer amount of ethanol is added to the irrigation fluid and the absorption of irrigation fluid can be calculated by measuring the expiratory ethanol concentrations of the patient with an alcohol breathalyzer. Fifty consecutive patients undergoing TUV-P at our tertiary referral center are included into the trial. Absorption volume of irrigation fluid during Thulium Laser TUV-P is defined as primary endpoint. Pre- to postoperative changes in bladder diaries, biochemical and hematological laboratory findings, duration of operation and standardized questionnaires are assessed as secondary outcome measures. DISCUSSION: The aim of this study is to assess the safety of Thulium Laser TUV-P in regard to absorption of irrigation fluid.

Absorption of irrigation fluid occurs frequently during high power 532 nm laser vaporization of the prostate.

PURPOSE: Absorption of irrigation fluid was not detected during GreenLight™ laser vaporization of the prostate using the first generation 80 W laser. However, data are lacking on intraoperative irrigation fluid absorption using the second generation 120 W high power laser. We assessed whether fluid absorption occurs during high power laser vaporization of the prostate. MATERIALS AND METHODS: We performed this prospective investigation at a tertiary referral center in patients undergoing 120 W laser vaporization for prostatic bladder outlet obstruction. Normal saline containing 1% ethanol was used for intraoperative irrigation. The expired breath ethanol concentration was measured periodically during the operation using an alcometer. The volume of saline absorption was calculated from these concentrations. Intraoperative changes in hematological and biochemical blood parameters were also recorded. RESULTS: Of 50 investigated patients 22 (44%) had a positive breath ethanol test. Median absorption volume in the absorber group was 725 ml (range 138 to 3,452). Ten patients absorbed more than 1,000 ml. Absorbers had a smaller prostate, more capsular perforation, higher bleeding intensity and more laser energy applied during the operation. Three patients (13%) had symptoms potentially related to fluid absorption. Hemoglobin, hematocrit and serum chloride were the only blood parameters that changed significantly in the absorber group. The changes were significantly different than those in nonabsorbers. CONCLUSIONS: Fluid absorption occurs frequently during high power laser vaporization of the prostate. This should be considered in patients who present with cardiopulmonary or neurological symptoms during or after the procedure.

Protective effect of Flos puerariae extract following acute alcohol intoxication in mice.

BACKGROUND: The effect of Flos Puerariae extract (FPE) on alcohol metabolism, hepatic injury, and memory impairment was assessed following acute ethanol (EtOH) intoxication in mice. METHODS: The model of acute EtOH intoxication was established by intragastric administration with 8 g/kg EtOH in mice. FPE was orally administrated (gavage) once a day for 7 consecutive days. Mice were randomly divided into 4 groups: control group, model group, and FPE groups (100, 200 mg/kg). Alcohol tolerance and intoxication time, blood alcohol concentration, the activities of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) in liver, aspartate amino transferase (AST) and alanine amino transferase (ALT) in serum, superoxide dismutase (SOD), glutathione peroxidase (GSH-px), catalase and the formation of malondialdehyde (MDA) in both liver and brain, as well as memory ability were determined after acute alcohol exposure. RESULTS: Compared with model group, pretreatment with FPE significantly prolonged alcohol tolerance time and shortened intoxication time, which is accompanied by decreased blood alcohol concentration and elevated activities of ADH and ALDH in liver. Moreover, the index of hepatic injury, ALT, and AST activities in serum was markedly decreased by pretreatment with FPE. Additionally, decreased MDA level, enhanced GSH-px and catalase activities in liver, as well as enhanced SOD and catalase activities in brain were found in FPE pretreated mice after acute exposure to EtOH. Furthermore, FPE pretreated mice showed markedly relieved memory disruption following acute EtOH intoxication. CONCLUSIONS: This study suggests that FPE pretreatment could enhance alcohol metabolism, prevent hepatic injury, and relieve memory impairment after acute alcohol intoxication and that this effect is likely related to its modulation on the alcohol metabolizing and antioxidant enzymes.

Testing for drugs of abuse in children and adolescents.

Drug testing is often used as part of an assessment for substance use in children and adolescents. However, the indications for drug testing and guidance on how to use this procedure effectively are not clear. The complexity and invasiveness of the procedure and limitations to the information derived from drug testing all affect its utility. The objective of this clinical report is to provide guidance to pediatricians and other clinicians on the efficacy and efficient use of drug testing on the basis of a review of the nascent scientific literature, policy guidelines, and published clinical recommendations.

Effects of the serjania erecta and zeyheria montana ethanol extracts inexperimental pulpitis in rats: A histological study

Objectives: The aim of this study was to evaluate, by the semi-quantitative histological analysis, the anti-inflammatory activity of the ethanolic extracts of Serjania erecta e Zeyheria Montana, in experimental pulpits in rats. Study Design: In order to induce pulp inflammation, cavities were performed on the occlusal surface of the mandibular first molars of 45 male rats, without pulp exposure. The animals were distributed into 4 groups: GI, teeth without cavities; GII, single dose of saline solution via intraperitoneal (IP); GIII, single dose (IP) of 300mg/Kg ofethanolic extract of Zeyheria montana; GIV, single dose (IP) of 300mg/Kg of ethanolic extract of Serjania erecta. After 6, 12 and 24 hours, 5 animals of each group were killed by anesthetic overdose. The histological analyses of the pulp tissue were performed and the data analyzed by Dunn´s multiple test, at significance of 5%.Results: After 12 h, the GIII presented score statistically lower (p<0.05) than positive control group. After 24 h, GIII presented inflammatory index statistically lower than the positive control (p<0.01) and Serjania erecta (p<0.05) groups. Conclusion: The Zeyheria montana extract presented better anti-inflammatory activity than positive control group and Serjania erecta extract, which did not show anti-inflammatory effect in the analyzed periods (AU)

Antihyperglycemic, hypolipidemic and antioxidant activities of ethanolic extract of Commiphora mukul gum resin in fructose-fed male Wistar rats

High fructose feeding (66 % of fructose) induces type-2 diabetes in rats, which is associated with the insulin resistance, hyperinsulinemia, hypertriglyceridemia and oxidative stress. The present study was undertaken to evaluate the effect of ethanol extract of Commiphora mukul gum resin (CMEE) on blood glucose, plasma insulin, lipid profiles, reduced glutathione, lipid peroxidation, protein oxidation and enzymatic antioxidants like superoxide dismutase, catalase, glutathione reductase, glutathione peroxidase, glutathione-S-transferase in fructose-induced type-2 diabetic rats. A significant gain in body weight, hyperglycemia, hyperinsulinemia, increased lipid profiles, lipid peroxidation, protein oxidation and decreased reduced glutathione, activities of enzymatic antioxidants and insulin sensitivity (increased homeostasis assessment assay) were observed in high-fructose-induced diabetic rats. The administration of CMEE (200 mg/kg/day) daily for 60 days in high-fructose-induced diabetic rats reversed the above parameters significantly. CMEE has the ability to improve insulin sensitivity and delay the development of insulin resistance, aggravate antioxidant status in diabetic rats and may be used as an adjuvant therapy for patients with insulin resistance (AU)

Behavioral effects of taurine pretreatment in zebrafish acutely exposed to ethanol.

Taurine (TAU) is an amino sulfonic acid that plays protective roles against neurochemical impairments induced by ethanol (EtOH). Mounting evidence shows the applicability of zebrafish for evaluating locomotor parameters and anxiety-like behavioral phenotypes after EtOH exposure in a large scale manner. In this study, we assess the effects of TAU pretreatment on the behavior of zebrafish in the open tank after acute 1% EtOH (v/v) exposure (20 and 60 min of duration) and on brain alcohol contents. The exposure for 20 min exerted significant anxiolytic effects, which were prevented by 42, 150, and 400 mg/L TAU. Conversely, the 60-min condition induced depressant/sedative effects, in which the changes on vertical activity were associated to modifications on the exploratory profile. Although all TAU concentrations kept locomotor parameters at basal levels, 150 mg/L TAU, did not prevent the impairment on vertical activity of EtOH[60]. Despite the higher brain EtOH content detected in the 60-min exposure, 42, 150, and 400 mg/L TAU attenuated the increase of alcohol content in EtOH[60] group. In conclusion, our data suggest that both protocols of acute EtOH exposure induce significant changes in the spatio-temporal behavior of zebrafish and that TAU may exert a preventive role by antagonizing the effects induced by EtOH possibly due to its neuromodulatory role and also by decreasing brain EtOH levels. The hormetic dose-response of TAU on vertical exploration suggests a complex interaction between TAU and EtOH in the central nervous system.

[Preparation and transdermal diffusion of ursolic acid ethosomes].

OBJECTIVE: To prepare ursolic acid ethosomes and investigate the penetration characteristics of ursolic ethosomes as a transdermal vehicle. METHOD: Ursolic acid ethosomes were prepared by injection method, and the shape and particle size of the ethosomes were analyzed. Ursolic acid permeation tests in vitro through the skin of rats were performed in TP-3 diffusion cell. The accumulated permeation amounts of ursolic acid 10% isopropanol solution, ursolic acid liposomes, ursolic acid ethosomes were compared. RESULT: The average encapsulation percentage, particle size, and Zeta potential of the ethosomes were (95.83 +/- 0.86)%, (87.5 +/- 7.5) nm and - (38.4 +/- 3.6) mV, respectively. The accumulated permeation amount of the ethosomes in 12 h was 146.49 microg x cm(-2), and its transdermal permeability in 12 h was 12.17 microg x cm(-2) x h(-1). CONCLUSION: The encapsulation percentage of the ethosomes is good, and the stability of the ursolic acid ethosomes is fine. Ethosomes can significantly enhance the diffusion rate of ursolic acid through the skin of rats.

Effects of Antrodia camphorata on alcohol clearance and antifibrosis in livers of rats continuously fed alcohol.

Alcoholic fatty liver disease (AFLD) is the result of an excessive or chronic consumption of alcohol. Nine male Wistar rats per group were randomly assigned to one of the following drinking treatments: a 20% (w/w) alcohol solution (ALC); a 20% (w/w) alcohol solution cotreated with 0.25 g silymarin/kg BW/day; or a 20% (w/w) alcohol solution cotreated with 0.025 g Niuchangchih ( Antrodia camphorata )/kg BW/day for 4 weeks. Rats with cotreatments of silymarin or Niuchangchih had smaller (p < 0.05) relative liver size, less (p < 0.05) liver lipid accumulation, and lower (p < 0.05) liver damage indices [aspartate aminotransferase (AST) and alkaline phosphatase (ALP) values]. In the regulation of alcohol metabolism, the lower serum alcohol level was observed only in alcohol-fed rats supplemented with Niuchangchih. Meanwhile, cotreatment of silymarin or Niuchangchih increased (p < 0.05) CAT and ALDH activities but did not (p > 0.05) affect ADH and CYP2E1 expressions, which accelerate alcohol metabolism in the body. Additionally, neither silymarin nor Niuchangchih (p > 0.05) influenced serum/hepatic MMP-2 activities and NF-κB, AP1, and α-SMA gene expressions, but serum/hepatic MMP-9 activities and TNF-α, KLF-6, and TGF-ß1 gene expressions of alcohol-fed rats were down-regulated (p < 0.05) by silymarin or Niuchangchih, which also could explain the lower liver damage observed in rats chronically fed alcohol.