Lycopene Improves Metabolic Disorders and Liver Injury Induced by a Hight-Fat Diet in Obese Rats

Epidemiological studies have shown that the consumption of a high-fat diet (HFD) is positively related to the development of obesity. Lycopene (LYC) can potentially combat HFD-induced obesity and metabolic disorders in rats. This study aimed to investigate the effect of LYC on metabolic syndrome and assess its anti-inflammatory and antioxidant effects on the liver and adipose tissue in rats fed an HFD. Thirty-six male Wistar albino rats were divided into three groups. Group Ι (the control group) was fed a normal diet, group ΙΙ (HFD) received an HFD for 16 weeks, and group ΙΙΙ (HFD + LYC) received an HFD for 12 weeks and then LYC (25 mg/kg b.wt) was administered for four weeks. Lipid peroxidation, antioxidants, lipid profile, liver function biomarkers, and inflammatory markers were determined. The results showed that long-term consumption of an HFD significantly increased weight gain, liver weight, and cholesterol and triglyceride levels. Rats on an HFD displayed higher levels of lipid peroxidation and inflammatory markers. Moreover, liver and white adipose tissue histopathological investigations showed that LYC treatment mended the damaged tissue. Overall, LYC supplementation successfully reversed HFD-induced changes and shifts through its antioxidant and anti-inflammatory activity. Therefore, LYC displayed a therapeutic potential to manage obesity and its associated pathologies.     

Comparative proteomic analysis using 2DE‐LC‐MS/MS reveals the mechanism of Fuzhuan brick tea extract against hepatic fat accumulation in rats with nonalcoholic fatty liver disease

Fuzhuan brick tea has received increasing attention in recent years owing to its benefits for nonalcoholic fatty liver disease (NAFLD) and associated metabolic syndrome. For exploring the ameliorative mechanism, the liver proteomes from three groups of rats fed either a normal control diet (NCD), a high fat diet (HFD), or a HFD supplemented with high‐dose Fuzhuan brick tea extract (FTE) (HFD + HFTE) were comprehensively compared by quantitative proteomics using 2DE‐LC‐MS/MS. This is the first study of the effects of tea aqueous extract on the liver proteome of rats suffering from metabolic syndrome. The results showed that 57 proteins displayed more than 1.5‐fold differences in at least one of two comparisons of HFD versus NCD and HFD versus HFD + HFTE due to HFD feeding and FTE treatment, respectively. Of them, over 75% of proteins exhibited a similar tendency of expression in the two comparisons, meaning FTE was able to correct HFD effects on rat livers. By function analyses, an extensive list of proteins was involved in sugar and lipid metabolism. Compared with HFD‐fed rats, the reduced lipogenesis and enhanced β‐oxidation, tricarboxylic acid cycle and respiratory chain in HFD + HFTE‐fed rats, which mainly contributed to ameliorate hepatic fat accumulation and associated NAFLD. Additionally, some putative drug targets were also revealed such as COX2, PGAM1, ACACB, FAS, and ECHS1.     

Gas chromatography-mass spectrometry and high-performance liquid chromatography-tandem mass spectrometry in quantifying fatty acids

This critical overview covers current analytical methods and future developments in quantitative determination of fatty acids (FAs), emphasizing sample extraction, derivatization and instrumental analysis with gas chromatography/mass spectrometry (GC/MS) and high-performance liquid chromatography/tandem mass spectrometry (HPLC/MS²). We compare the benefits and the drawbacks of these two analytical techniques.We consider the well-established GC/MS method with pre-derivatization to be a traditional technique in terms of highly standardized sample-preparation procedures, affordability and readily available library searching for compound identification. However, the complicated derivatization steps required prior to instrumental analysis with GC/MS take a long time, with loss and transformation of FAs, low recovery and poor reproducibility.HPLC/MS² without derivatization shows the benefits of simple, mild sample-processing conditions, satisfactory recovery, short running time and high selectivity and sensitivity, which may allow it to become a viable alternative to GC/MS for the analysis of FAs in the years ahead.     

Cytotoxic activity of alkyl benzoate and fatty acids from the red sea sponge Hyrtios erectus

The chemical investigation of the methylene chloride fraction of marine sponge Hyrtios erectus led to the isolation of the known oxysterol (2) along with a new alkyl benzoate compound identified by spectroscopic methods (NMR and MS) as 4′-methylheptyl benzoate (1), whilst the n-butanol fraction afforded the known indole 3-carbaldehyde and β-carboline derivatives. Moreover, the hexane fraction was analysed by GC–MS for their fatty acids (FAs). A total of 17 FAs with chain lengths between 14 and 25 carbons were identified. Methyl-branched FAs are predominated suggesting the presence of bacterial symbionts in the H. erectus sponge. Furthermore, compounds 1 and 2 displayed significant cytotoxicity against breast adenocarcinoma (MCF-7) with IC₅₀ values of 2.4 and 3.8 μM, respectively, since compound 2 was also shown to have potent cytotoxic effect against hepatocellular carcinoma cells (HepG 2) with IC₅₀ value of 1.3 μM.     

Fatty acids profiling of avocado seed and pulp using gas chromatography–mass spectrometry combined with multivariate chemometric techniques

In the present study, the profiling of 17 fatty acids (FAs) in avocado seed and pulp was investigated. The fatty acids were extracted with vortex-assisted extraction, methyl esterified and finally preconcentrated by dispersive liquid–liquid microextraction. The preconcentrated fatty acid methyl esters (FAMEs) were analyzed using gas chromatography–mass spectrometry (GC–MS) to obtain qualitative and quantitative information. The GC–MS data were analyzed using multivariate curve resolution-alternating least squares (MCR-ALS) method to overcome general chromatographic problems such as overlapped peaks, background interference and peak shifts. The calibration data were prepared using pure analytical information obtained by MCR-ALS. The linear dynamic ranges and regression coefficients (R ²) for FAMEs were in the range of 0.19–65 mg L^?1 and 0.990–0.999, respectively. The relative standard deviation (RSD%) for determination of FAs in avocado seed and pulp was 0.17–8.84 and 0.64–17.93, respectively. The main FAs in the avocado pulp were: oleic acid (74.25 g Kg^?1), linoleic acid (26.87 g Kg^?1), palmitic acid (26.02 g Kg^?1), palmitoleic acid (1.22 g Kg^?1) and stearic acid (0.05 g Kg^?1). And, the main FAs in the avocado seed were: linoleic acid (1.09 g Kg^?1), palmitic acid (0.47 g Kg^?1), oleic acid (0.33 g Kg^?1), linolenic acid (0.12 g Kg^?1), and palmitoleic acid (0.04 g Kg^?1).     

Characterization of fatty acid and triacylglycerol composition in animal fats using silver-ion and non-aqueous reversed-phase high-performance liquid chromatography/mass spectrometry and gas chromatography/flame ionization detection

Fatty acid (FA) and triacylglycerol (TG) composition of natural oils and fats intake in the diet has a strong influence on the human health and chronic diseases. In this work, non-aqueous reversed-phase (NARP) and silver-ion high-performance liquid chromatography with atmospheric pressure chemical ionization mass spectrometry detection and gas chromatography with flame-ionization detection (GC/FID) and mass spectrometry detection are used for the characterization of FA and TG composition in complex samples of animal fats from fallow deer, red deer, sheep, moufflon, wild boar, cock, duck and rabbit. The FA composition of samples is determined based on the GC/FID analysis of FA methyl esters. In total, 81 FAs of different acyl chain length, double bond (DB) number, branched/linear, cis-/trans- and DB positional isomers are identified. TGs in animal fats contain mainly monounsaturated and saturated FAs. High amounts of branched and trans-FAs are observed in the samples of ruminants. In NARP mode, individual TG species are separated including the separation of trans- and branched TGs. Silver-ion mode provides the separation of TG regioisomers, which enables the determination of their ratios. Great differences in the preference of unsaturated and saturated FAs in the sn-2 position on the glycerol skeleton are observed among individual animal fats. Unsaturated FAs are preferentially occupied in the sn-2 position in all animal samples except for wild boar with the strong preference of saturated FAs in the sn-2 position.     

Comparison of GC–MS and MEKC methods for caffeine determination in preworkout supplements

In this study, GC–MS‐ and MEKC‐based methods for determination of caffeine (CAF) in preworkout supplements were developed and validated. The proposed protocols utilized minimal sample preparation (simple dilution and syringe filtration). The developed methods achieved satisfactory validation parameters, i.e. good linearity (R² > 0.9988 and R² > 0.9985 for GC–MS‐ and MEKC‐based method, respectively), satisfactory intra‐ and interaccuracy (within 92.6–100.7% for method utilizing GC–MS and 92.1–110.3% for protocol based on MEKC) and precision (CV < 15.9% and CV < 6.3% for GC–MS‐ and MEKC‐based method, respectively) and recovery (within 100.1–100.8% for method utilizing GC–MS and 101.5–106.2% for protocol based on MEKC). The LOD was 0.03 and 3 μg/mL for method utilizing GC–MS and MEKC, respectively. The CAF concentrations determined by GC–MS‐ and MEKC‐based methods were found to be in the range of 8.53–11.23 and 8.20–11.61 μg/mL, respectively. Taking into consideration information on the labels, the investigated supplements were found to contain from 110.0 to 167.3% of the declared CAF content, which confirmed the literature reports on incompatibility of the declared product compositions with real ones. Nevertheless, the consumption of examined supplements as recommended by producers did not lead to exceeding the CAF safe limit of 400 mg per day. Additionally, the MEKC‐based method allowed for detection and identification of vitamin B3 and B6 in all of the investigated supplement samples, which demonstrated that MEKC‐based protocols may be an appropriate assays for simultaneous determination of CAF and vitamins.     

New cathinone‐derived designer drugs 3‐bromomethcathinone and 3‐fluoromethcathinone: studies on their metabolism in rat urine and human liver microsomes using GC–MS and LC–high‐resolution MS and their detectability in urine

3‐Bromomethcathinone (3‐BMC) and 3‐Fluoromethcathinone (3‐FMC) are two new designer drugs, which were seized in Israel during 2009 and had also appeared on the illicit drug market in Germany. These two compounds were sold via the Internet as so‐called “bath salts” or “plant feeders.” The aim of the present study was to identify for the first time the 3‐BMC and 3‐FMC Phase I and II metabolites in rat urine and human liver microsomes using GC–MS and LC–high‐resolution MS (HR‐MS) and to test for their detectability by established urine screening approaches using GC–MS or LC–MS. Furthermore, the human cytochrome‐P450 (CYP) isoenzymes responsible for the main metabolic steps were studied to highlight possible risks of consumption due to drug–drug interaction or genetic variations. For the first aim, rat urine samples were extracted after and without enzymatic cleavage of conjugates. The metabolites were separated and identified by GC–MS and by LC–HR‐MS. The main metabolic steps were N‐demethylation, reduction of the keto group to the corresponding alcohol, hydroxylation of the aromatic system and combinations of these steps. The elemental composition of the metabolites identified by GC–MS could be confirmed by LC–HR‐MS. Furthermore, corresponding Phase II metabolites were identified using the LC–HR‐MS approach. For both compounds, detection in rat urine was possible within the authors' systematic toxicological analysis using both GC–MS and LC–MSⁿ after a suspected recreational users dose. Following CYP enzyme kinetic studies, CYP2B6 was the most relevant enzyme for both the N‐demethylation of 3‐BMC and 3‐FMC after in vitro–in vivo extrapolation. Copyright © 2012 John Wiley & Sons, Ltd.     

Effects of Fermented Citrus Peel on Ameliorating Obesity in Rats Fed with High-Fat Diet

Although citrus peel is a waste material, it contains a variety of bioactive components. As our preliminary findings showed that citrus peels fermented with Saccharomyces cerevisiae T1 contained increased levels of anti-obesity flavonoids, the objective of this study was to prepare fermented citrus peel and to investigate its effect on ameliorating obesity in Sprague Dawley (SD) rats fed with a high-fat diet (HFD). After fermentation, the amounts of limonene, nobiletin and 3-methoxynobiletin in citrus peel were markedly increased. SD rats were fed with an HFD for 10 weeks, followed by fermented citrus peel-containing HFD (0.3% or 0.9% w/w) for 6 weeks. Compared with those fed with an HFD alone, lower levels of body weight, visceral fat, body fat percentage, blood triglyceride, total cholesterol, low-density lipoprotein, malondialdehyde and hepatic adipose accumulation were observed in rats fed with fermented citrus peel. In parallel, hepatic levels of acetyl-CoA carboxylase and fatty acid synthase were diminished, and the level of hormone sensitivity lipase in visceral fat was elevated. These results reveal fermented citrus peel is a promising natural product with beneficial effects of alleviating HFD-induced obesity.     

Oleuropein prevents the progression of steatohepatitis to hepatic fibrosis induced by a high-fat diet in mice

Nonalcoholic steatohepatitis (NASH) is characterized by hepatocyte injury and inflammatory cell infiltration, which has been linked to peripheral insulin resistance and increased levels of triglycerides in the liver. The purposes of this study were to establish a mouse model of NASH by feeding mice a 60% high-fat diet (HFD) and to demonstrate the anti-fibrotic effects of oleuropein, which has been shown to have anti-oxidant and anti-inflammatory properties, in this HFD-induced mouse model of NASH. C57BL/6 mice were divided into three groups: a regular diet group (Chow), a HFD group and an oleuropein-supplemented HFD group (OSD), which was fed a 0.05% OSD for 6 months. The effects of oleuropein in this model were evaluated using biochemical, histological and molecular markers. The expression levels of alpha-smooth muscle actin (α-SMA)and collagen type I in the HFD and OSD groups were evaluated using real-time PCR and western blotting. The body weight, biochemical marker levels, nonalcoholic fatty liver disease activity score, homeostasis model of assessment-insulin resistance (HOMA-IR) and leptin levels observed in the HFD group at 9 and 12 months were higher than those observed in the Chow group. The HOMA-IR and leptin levels in the OSD group were decreased compared with the HFD group. In addition, α-SMA and collagen type I expression were decreased by oleuropein treatment. We established a NASH model induced by HFD and demonstrated that this model exhibits the histopathological features of NASH progressing to fibrosis. Our results suggest that oleuropein may be pharmacologically useful in preventing the progression of steatohepatitis and fibrosis and may be a promising agent for the treatment of NASH in humans.     

β-Caryophyllene: A Therapeutic Alternative for Intestinal Barrier Dysfunction Caused by Obesity

Obesity is an excessive accumulation of fat that exacerbates the metabolic and inflammatory processes. Studies associate these processes with conditions and dysregulation in the intestinal tract, increased concentrations of lipopolysaccharides (LPSs) in the blood, differences in the abundance of intestinal microbiota, and the production of secondary metabolites such as short-chain fatty acids. β-Caryophyllene (BCP) is a natural sesquiterpene with anti-inflammatory properties and with the potential purpose of fighting metabolic diseases. A diet-induced obesity model was performed in 16-week-old C57BL/6 mice administered with BCP [50 mg/kg]. A reduction in the expression of Claudin-1 was observed in the group with a high-fat diet (HFD), which was caused by the administration of BCP; besides BCP, the phyla Akkermansia and Bacteroidetes decreased between the groups with a standard diet (STD) vs. HFD. Nevertheless, the use of BCP in the STD increased the expression of these phyla with respect to fatty acids; a similar effect was observed, in the HFD group that had a decreasing concentration that was restored with the use of BCP. The levels of endotoxemia and serum leptin increased in the HFD group, while in the HFD + BCP group, similar values were found to those of the STD group, attributing the ability to reduce these in conditions of obesity.     

Direct infusion electrospray ionization–ion mobility–mass spectrometry for comparative profiling of fatty acids based on stable isotope labeling

A rapid method for fatty acids (FAs) comparative profiling based on carboxyl-specific stable isotope labeling (SIL) and direct infusion electrospray ionization–ion mobility–mass spectrometry (ESI–IM–MS) is established. The design of the method takes advantage of the three-dimensional characteristics of IM–MS including drift time, m/z and ion intensity, for comparison of d0-/d6-2,4-dimethoxy-6-piperazin-1-yl pyrimidine (DMPP)-labeled FAs. In particular, without chromatographic separation, the method allowed direct FAs profiling in complex samples due to the advantageous priority of DMPP in signal enhancement as well as the extra resolution that IM–MS offered. Additionally, the d0-/d6-DMPP-labeled FAs showed expected features, including very similar drift times, 6 Da mass deviations, specific reporter ions, similar MS responses, and adherence to the drift time rule regarding the influence of carbon chain length and unsaturation on relative drift times. Therefore, the introduction of isotope analogs minimized the matrix effect and variations in quantification and ensured accurate identification of non-targeted FAs by those typical features. Peak intensity ratios between d0-/d6-DMPP-labeled ions were subsequently used in relative quantification for the detected FAs. The established strategy has been applied successfully in the rapid profiling of trace free FAs between normal and cancerous human thyroid tissues. Sixteen free FAs were found with the increased level with a statistically significant difference (p < 0.05) compared to the normal tissue samples. The integrated SIL technique and ESI–IM–MS are expected to serve as an alternative tool for high-throughput analysis of FAs in complex samples.     

Comparison of different mass spectrometry techniques in the measurement of L‐[ring‐13C6]phenylalanine incorporation into mixed muscle proteins

Precise measurement of low enrichment of stable isotope labeled amino‐acid tracers in tissue samples is a prerequisite in measuring tissue protein synthesis rates. The challenge of this analysis is augmented when small sample size is a critical factor. Muscle samples from human participants following an 8 h intravenous infusion of L‐[ring‐¹³C₆]phenylalanine and a bolus dose of L‐[ring‐¹³C₆]phenylalanine in a mouse were utilized. Liquid chromatography tandem mass spectrometry (LC/MS/MS), gas chromatography (GC) MS/MS and GC/MS were compared to the GC‐combustion‐isotope ratio MS (GC/C/IRMS), to measure mixed muscle protein enrichment of [ring‐¹³C₆]phenylalanine enrichment. The sample isotope enrichment ranged from 0.0091 to 0.1312 molar percent excess. As compared with GC/C/IRMS, LC/MS/MS, GC/MS/MS and GC/MS showed coefficients of determination of R² = 0.9962 and R² = 0.9942, and 0.9217 respectively. However, the precision of measurements (coefficients of variation) for intra‐assay are 13.0%, 1.7%, 6.3% and 13.5% and for inter‐assay are 9.2%, 3.2%, 10.2% and 25% for GC/C/IRMS, LC/MS/MS, GC/MS/MS and GC/MS, respectively. The muscle sample sizes required to obtain these results were 8 µg, 0.8 µg, 3 µg and 3 µg for GC/C/IRMS, LC/MS/MS, GC/MS/MS and GC/MS, respectively. We conclude that LC/MS/MS is optimally suited for precise measurements of L‐[ring‐¹³C₆]phenylalanine tracer enrichment in low abundance and in small quantity samples. Copyright © 2013 John Wiley & Sons, Ltd.     

Physico-chemical properties of Tecoma stans Linn. seed oil: a new crop for vegetable oil

Tecoma stans Linn. is known to have various medicinal and therapeutic properties. However, to our knowledge, no information is available regarding their seed oils. In this study, the fatty acid (FA) compositions, physico-chemical properties and antioxidant capacities of T. stans seed oils (TSOs) were investigated. The oil content of the seeds was 15%. The FAs of the TSOs were analysed by GC–MS. α-Linolenic (45.47%), oleic (23.56%), linoleic (11.48%), palmitic (6.09%) and stearic (4.12%) acids were the major detected FAs. γ-Linolenic acid and stearidonic acid, unusually FAs, were also present (1.04% and 6.65%, respectively). The total tocol content in the TSOs was found to be 266.06 mg/100 g. The main component was γ-tocopherol (78.93%). The total phenolic content (168.69 mg GAE/100 g oil) and total flavonoid content (5.54 mg CE/g oil) were also determined in the TSOs.     

Gas chromatography/tandem mass spectrometry analysis of alkylresorcinols in red blood cells

Erythrocyte alkylresorcinols (5‐alkyl‐1,3‐dihydroxybenzenes) are potential biomarkers of wholegrain wheat and rye intake. However, their high‐throughput quantitative analysis by gas chromatography/mass spectrometry (GC/MS) is hindered by the time‐consuming sample preparation and, more importantly, by interfering compounds that still remain after sample cleanup. In the present work we describe a gas chromatography/tandem mass spectrometry (GC/MS/MS) method for the rapid and reliable quantification of alkylresorcinols in erythrocyte samples. The performance of the GC/MS/MS method is compared with that of GC/MS. The main characteristics of the method are: lower limits of detection: 2–10 µg/L standard solution; lower limits of quantification: 6–30 µg/L standard solution; linearity coefficients: 0.9611–0.9888; linear ranges: 2–20 µg/L in erythrocytes; and intra‐day precisions (n = 6): 4–13% at endogenous analyte levels in non‐spiked erythrocytes. Tandem mass spectrometry showed greatly improved selectivity over single‐stage mass spectrometry in the case of erythrocyte samples, eliminating all interferences detectable in single‐stage MS and enabling simple peak integration for quantification. Moreover, increased selectivity resulted in GC separation speeded up by a factor of two, allowing the duplicate analysis of over 40 samples per day. This GC/MS/MS method is suggested as an improved alternative to GC/MS for the quantification of alkylresorcinols in erythrocytes for assessing wholegrain wheat and rye intake. Copyright © 2008 John Wiley & Sons, Ltd.     

Antioxidant and chemical properties of Inula helenium root extracts

The objective of the paper was to investigate the chemical composition of Inula helenium roots extracts and to evaluate the antioxidant potential conferred by the chemical constituents. GC/MS and HPLC/MS techniques were used to characterize two extracts separated from Inula helenium roots by extraction with chloroform and ethyl acetate, respectively. Volatile compounds have been identified by GC from their mass spectra and retention time values, while HPLC identification of phenolic compounds was realized by comparing their retention times, UV and MS spectra with those of standards or literature data. Measurements of antioxidant activity of Inula helenium root extracts showed a variation between them, which can be correlated with the flavonoid and total phenolic contents. Both Inula helenium root extracts contain phenolic acids (caffeic, chlorogenic, dicaffeoyl quinic, hydroxibenzoic), terpenes (alantolactone) and different flavonoids (epicatechin, catechin gallate, ferulic acid-4-O-glucoside, dihydroquercetin pentosyl rutinoside, kaempherol-7-O-dipentoside, quercetin-3-O-β-glucopyranoside). In addition, the study provides preliminary data on the anti-inflammatory activity of Inula helenium root extracts, this being evaluated using the fresh egg albumin as phlogistic agent, and aspirin as reference compound. Root extracts of I. helenium did not exert any significant anti-inflammatory effect on egg albumin-induced rat paw edema.      

Determination of human muscle protein fractional synthesis rate: an evaluation of different mass spectrometry techniques and considerations for tracer choice

In the present study, different MS methods for the determination of human muscle protein fractional synthesis rate (FSR) using [ring‐¹³C₆]phenylalanine as a tracer were evaluated. Because the turnover rate of human skeletal muscle is slow, only minute quantities of the stable isotopically labeled amino acid will be incorporated within the few hours of a typical laboratory experiment. GC combustion isotope ratio MS (GC‐C‐IRMS) has thus far been considered the ‘gold’ standard for the precise measurements of these low enrichment levels. However, advances in liquid chromatography‐tandem MS (LC‐MS/MS) and GC‐tandem MS (GC‐MS/MS) have made these techniques an option for human muscle FSR measurements. Human muscle biopsies were freeze dried, cleaned, and hydrolyzed, and the amino acids derivatized using either N‐acetyl‐n‐propyl, phenylisothiocyanate, or N‐methyl‐N‐(tert‐butyldimethylsilyl)trifluoroacetamide (MTBSTFA) for GC‐C‐IRMS, LC‐MS/MS, and GC‐MS/MS analysis, respectively. A second derivative, heptafluorobutyric acid (HFBA), was also used for GC‐MS/MS analysis as an alternative for MTBSTFA. The machine reproducibility or the coefficients of variation for delta tracer‐tracee‐ratio measurements (delta tracer‐tracee‐ratio values around 0.0002) were 2.6%, 4.1%, and 10.9% for GC‐C‐IRMS, LC‐MS/MS, and GC‐MS/MS (MTBSTFA), respectively. FSR determined with LC‐MS/MS compared well with GC‐C‐IRMS and so did the GC‐MS/MS when using the HFBA derivative (linear fit Y = 1.08 ± 0.10, X + 0.0049 ± 0.0061, r = 0.89 ± 0.01, P < 0.0001). In conclusion, (1) IRMS still offers the most precise measurement of human muscle FSR, (2) LC‐MS/MS comes quite close and is a good alternative when tissue quantities are too small for GC‐C‐IRMS, and (3) If GC‐MS/MS is to be used, then the HFBA derivative should be used instead of MTBSTFA, which gave unacceptably high variability. Copyright © 2014 John Wiley & Sons, Ltd.     

Novel CBG Derivatives Can Reduce Inflammation,Pain and Obesity

Interest in CBG (cannabigerol) has been growing in the past few years, due to its anti-inflammatory properties and other therapeutic benefits. Here we report the synthesis of three new CBG derivatives (HUM-223, HUM-233 and HUM-234) and show them to possess anti-inflammatory and analgesic properties. In addition, unlike CBG, HUM-234 also prevents obesity in mice fed a high-fat diet (HFD). The metabolic state of the treated mice on HFD is significantly better than that of vehicle-treated mice, and their liver slices show significantly less steatosis than untreated HFD or CBG-treated ones from HFD mice. We believe that HUM-223, HUM-233 and HUM-234 have the potential for development as novel drug candidates for the treatment of inflammatory conditions, and in the case of HUM-234, potentially for obesity where there is a huge unmet need.     

Standard equivalent chain length values of monoenic and polyenic (methylene interrupted) fatty acids

The equivalent chain length (ECL) values of the methyl esters of 83 defined fatty acids (FAs) have been determined by gas chromatog-raphy (GC) on three fused silica DB-WAX and three DB-1 columns. ECL values of further 46 FAs were calculated by different methods. Conditions of chromatography, methods of ECL values calculation and differences between ECL values on individual columns and between trans- and cis-isomers of corresponding FAs are also discussed.     

Fast Heroin and Cocaine Analysis by GC–MS with Cold EI: The Important Role of Flow Programming

A fast GC–MS method was developed based on the use of GC–MS with Cold EI. This new method was applied for the analysis of the street drugs heroin and cocaine and it enabled 2 min chromatography time and 3 min full analysis cycle time. GC–MS with cold EI provides mass spectra with enhanced molecular ions that are library compatible (with increased identification probabilities) and allows the use of short, 5 m 0.25 mm ID columns, which facilitates fast GC–MS. A central ingredient of our unique cold EI-based fast GC–MS analysis method is the use of column flow programming from 1 up to 32 ml min^?1 column flow rate. Column flow programming can reduce the analysis time by about a factor of two and unlike temperature programs of GC ovens the carrier gas flow rate can be raised and lowered very quickly (in a few seconds). The fast GC–MS with Cold EI method is demonstrated by the analysis of heroin in its street drug powder and cocaine on paper money and it can be applied for other drugs of abuse as a general fast drugs analysis method.