Anticandidal activity of the extract and compounds isolated from Cyperus conglomertus Rottb

The phytochemical screening of Cyperus conglomeratus showed that carbohydrates and/or glycosides, flavonoids, tannins, sterols and/or triterpenes, and proteins and/or amino acids are present. The fatty acid profile comprised major; palmitic, oleic, heptadecanoic, linoleic and minor; arachidonic, lignoceric, stearic, and myristic acid. Two compounds; namely, α-amyrin and β-sitosterol were isolated by the fractionation of unsaponifiable matter.The acute toxicity study showed that the reported after oral administration of the alcohol extract (TAE) showed that the plant was highly safe as the LD₅₀ was more than 4000?mg/kg. These results were well supported by the sub-chronic toxicity, as the TAE administrated to rats for 15 consecutive days at dose 1000?mg/kg showed no alteration in the liver and kidney functions. Moreover, the extract of the plant exhibited anti-candidal activity against different Candida species. The most potent activity, (23.1?±?2.1, 0.98?µg/ml) and (22.3?±?0.53, 0.98?µg/ml), was obtained by the chloroform and total extract, respectively against Candida albicans.     

Analysis of lipophilic compounds of tea coated on the surface of clay teapots

The surface of a clay teapot tends to be coated with a waterproof film after constant use for tea preparation. The waterproof films of two kinds of teapots (zisha and zhuni) used for preparing oolong tea and old oolong tea were extracted and subjected to gas chromatography–mass spectrometry analysis. The results showed that comparable constituents were detected in these films; they were primarily fatty acids and linear hydrocarbons that were particularly rich in palmitic acid and stearic acid. To explore the source of these two abundant fatty acids, the fatty acid compositions of fresh tea leaves, granules, infusion, and vapor of infusion were analyzed by gas chromatography. Fresh tea leaves were rich in palmitic acid (C-16:0), unsaturated linolenic acid (C-18:3), linoleic acid (C-18:2), and oleic acid (C-18:1), which were presumably from the phospholipid membrane. During the process of manufacturing oolong tea, the three unsaturated fatty acids may be substantially degraded or oxidized to stearic acid (C-18:0), which was enriched with palmitic acid in the tea granules and in the infusion. The vapor of the tea infusion is primarily composed of palmitic acid and stearic acid. Thus, the coated films of teapots mostly originated from the lipophilic compounds of the tea infusions.     

Further insights into chemical characterization through GC–MS and evaluation for anticancer potential of Dracaena draco leaf and fruit extracts

The present study reports for the first time the amino acid and fatty acid compositions and the antitumoral activity of aqueous extracts obtained from Dracaena draco L. leaf and fruit. Metabolite profiles were determined by gas chromatography-ion trap-mass spectrometry (GC–IT-MS), with several amino acids, palmitic, linolenic and stearic acid being identified in the leaf extract, and only proline, oleic and stearic acid in the fruit extract. The in vitro antiproliferative activities of the extracts were tested against human colon (Caco-2), kidney (A-498), and liver (HepG2) cancer cell lines. In addition, primary cultures of normal and cancerous renal cells derived from kidney cancer patients were treated with D. draco extracts (0–400 μg/mL). Antiproliferative and cytotoxic effects were determined by the MTT assay. D. draco extracts inhibited proliferation of human colon and renal tumor cells in vitro, whereas no or weak effect was observed in HepG2 cells. Compared to the fruit extract, D. draco leaf extract exhibited stronger antiproliferative activity against all cancer cells. Our results indicate that D. draco, particularly the leaf, may be useful as a cancer chemopreventive and/or chemotherapeutic agent for colon and kidney cancers.     

Extraction of protein with protease inhibitor activity from Brazilwood (Caesalpinia echinata LAM.) seeds using choline-based ionic liquids

Proteolytic inhibitors are low molecular weight proteins that prevent protein hydrolysis and are used against moderate to high severity diseases. Some plants can produce these protease inhibitors, such as Brazilwood seeds (Caesalpinia echinata LAM.). This work aimed to optimise the extraction of proteins from Brazilwood seeds with proteolytic inhibitory activity, using choline-based ionic liquid. The seeds were characterised in terms of their dimensions (15 mm in length, 11 mm in width and 4.8 mm in thickness), centesimal composition (moisture - 9.21%, ash - 3.37%, lipids - 32.6%, total fibre - 0.80%, crude proteins - 17.2%, carbohydrates - 36.8%), energy (510 Kcal.100 g^-1) and major fatty acid (linoleic acid - 43%). Protein extraction was performed by maceration of the Brazilwood seeds using ionic liquids (choline bitartrate, choline chloride and choline dihydrogen citrate) and optimised using a factorial design of experiments, whose variables were the temperature and solvent concentration, with the total protein content as the response variable. The best extraction conditions were 25.42 °C, 5.42% (m/v) choline bitartrate, solid-liquid ratio 1:5, 500 rpm and pH 7.0 (1.74 mg mL^?1 theoretical and 1.88 mg mL^?1 experimental). The kinetic model best fitted to the experimental data was Peleg's, and the best extraction time was 15 min. Under optimised conditions, the protein extract of Brazilwood seeds provided a 60.8% inhibition of trypsin. According to the molecular docking results, the inhibition of bovine trypsin is driven by Caesalpinia echinata kallikrein inhibitor (CeKI) and the selected ionic liquid (choline bitartrate), promoting a synergistic inhibition effect.     

Concentration-dependent effects of fatty acids on warfarin binding to albumin

The interrelationships between fatty acid and warfarin binding to albumin were investigated. Various molar ratios of palmitic acid and oleic acid were added to defatted human albumin in the presence of warfarin, and the warfarin binding association constants, K_a, were calculated. Warfarin association constants increased from 0.84 × 10⁵ M ^?1 to 3.66 × 10⁵ M ^?1 as the oleic acid concentration increased from zero to three moles per mole of albumin and from 1.19 × 10⁵ M ^?1 to 3.13 × 10⁵ M ^?1 as the palmitic acid concentration increased from zero to two moles per mole of albumin. Larger amounts of either fatty acid progressively decreased the amount of warfarin bound in a noncompetitive fashion. In addition, two proteolytic fragments were utilized to define the location of the warfarin binding site on albumin. The warfarin site was located between loops 5 and 6 on the albumin molecule in close proximity to the secondary and tertiary binding sites of palmitic acid.     

Analysis of sterols and fatty acids in natural and cultured Cordyceps by one-step derivatization followed with gas chromatography–mass spectrometry

Ten free fatty acids namely lauric acid, myristic acid, pentadecanoic acid, palmitoleic acid, palmitic acid, linoleic acid, oleic acid, stearic acid, docosanoic acid and lignoceric acid and four free sterols including ergosterol, cholesterol, campesterol and β-sitosterol in natural (wild) Cordyceps sinensis, Cordyceps liangshanensis and Cordyceps gunnii, as well as cultured C. sinensis and Cordyceps militaris were first determined using pressurized liquid extraction (PLE), trimethylsilyl (TMS) derivatization and GC–MS analysis. The conditions such as the amount of reagent, temperature and time for TMS derivatization of analytes were optimized. Under the optimum conditions, all calibration curves showed good linearity within the tested ranges. The intra- and inter-day variations for 14 investigated compounds were less than 3.4% and 5.2%, respectively. The results showed that palmitic acid, linoleic acid, oleic acid, stearic acid and ergosterol are main components in natural and cultured Cordyceps which could be discriminated by hierarchical clustering analysis based on the contents of 14 investigated compounds or the 4 fatty acids, where the contents of palmitic acid and oleic acid in natural Cordyceps are significantly higher than those in the cultured ones.     

Effect of acute nitrogen dioxide exposure on the composition of fatty acids in lung and liver phospholipids

In order to examine the effects of NO₂ on the fatty acid content of the lung and liver phospholipids, the phospholipid fractions of rats exposed to 20 ppm NO₂ for 20 and 40 h were extracted and analyzed using gas chromatography. Among the fatty acid species in the lung, the relative amount of palmitic acid, palmitoleic acid and linoleic acid increased significantly, whereas myristic acid, stearic acid and oleic acid decreased significantly after exposure to NO₂. These changes in the composition of fatty acids are discussed in comparison with the results of acute, subacute and chronic exposure to NO₂ reported by other workers. In the case of the fatty acid species in the liver, a significant increase for stearic acid and arachidonic acid and a decrease in oleic acid were observed.     

Influence of Fatty Acids on the Binding of Warfarin and Phenprocoumon to Human Serum Albumin with Relation to Anticoagulant Therapy

Warfarin and phenprocoumon binding to human serum albumin was studied by equilibrium dialysis. The first stoichiometric binding constant was 1.89 × 10⁵ M^?1 for warfarin and 2.40 × 10⁵ M^?1 for phenprocoumon. The affinity of warfarin was markedly increased on addition of up to 3 mol mol^?1 albumin of palmitic, stearic, oleic or linoleic acids with energetic couplings for co-binding of one molecule of each of the fatty acids and one molecule of warfarin of 0.9, 1.1, 0.7 and 0.6 kJ mol^?1, respectively. The affinity of phenprocoumon was only increased slightly on addition of palmitate with an energetic coupling of 0.3 kJ mol^?1. Six consecutive serum samples were obtained from each of 14 patients undergoing surgery. The serum affinity of the drugs varied considerably corresponding to free drug concentrations between 0.7 and 2.7% for warfarin and between 0.8 and 4.9% for phenprocoumon. The affinity of warfarin but not of phenprocoumon was correlated to the increasing plasma fatty acid concentration. Anticoagulant therapy with phenprocoumon may thus be less sensitive than warfarin to changes in the fatty acid concentration of plasma.     

Cold-pressed raspberry seeds oil ameliorates high-fat diet triggered non-alcoholic fatty liver disease

Non-alcoholic fatty liver disease (NAFLD) is considered one of the most serious public health problems affecting liver. The reported beneficial impact of raspberries on obesity and associated metabolic disorder makes it a suitable candidate against NAFLD. In the current study, the chemical profile of raspberry seed oil (RO) was characterized by analysis of fatty acid and tocopherol contents using high-performance liquid chromatography (HPLC) in addition to the determination of total phenolic and flavonoids. High levels of unsaturated fatty acids, linoleic acid (49.9%), α-linolenic acid (25.98%), and oleic acid (17.6%), along with high total tocopherol content (184 mg/100 gm) were detected in oil. The total phenolic and flavonoid contents in RO were estimated to be 22.40 ± 0.25 mg gallic acid equivalent (GAE)/100 mg oil and 1.34 ± 0.15 mg quercetin (QU)/100 mg, respectively. Anti-NAFLD efficacy of RO at different doses (0.4 and 0.8 mL) in a model of a high-fat diet (HFD) fed rats was assessed by estimating lipid profile, liver enzyme activity, glucose and insulin levels as well as adipokines and inflammatory marker. Peroxisome proliferator-activated receptor γ (PPARγ), which is a molecular target for NAFLD was also tested. Liver histopathology was carried out and its homogenate was used to estimate oxidative stress markers. Consumption of RO significantly improved lipid parameters and hepatic enzyme activities, reduced insulin resistance and glucose levels, significantly ameliorated inflammatory and oxidative stress markers. Furthermore, RO treatment significantly modulated adipokines activities and elevated PPARγ levels. Raspberry seed oil administration significantly improved these HFD induced histopathological alterations. Moreover, a molecular docking study was performed on the identified fatty acids and tocopherols. Among the identified compounds, oleic acid, α-linolenic acid and γ-tocopherol exhibited the highest docking score as PPARγ activator posing them as a potential anti-NAFLD drug leads. Study findings suggest RO as an effective therapeutic candidate for ameliorating NAFLD.     

Omega-3 fatty acids induce Ca2+ mobilization responses in human colon epithelial cell lines endogenously expressing FFA4

Aim:

Free fatty acid receptor 4 (FFA4; formerly known as GPR120) is the G protein-coupled receptor (GPCR) for omega-3 polyunsaturated fatty acids. FFA4 has been found to express in the small intestines and colons of mice and humans. In this study we investigate the effects of omega-3 polyunsaturated fatty acids on FFA4 in human colon epithelial cells in vitro.

Methods:

HCT116 and HT-29 human colon epithelial cell lines endogenously expressing FFA4 were used. Intracellular Ca²⁺ concentration ([Ca²⁺]_i) was measured in fura 2-AM-loaded cells with fluorescence spectrophotometry. RT-PCR and immunohistochemistry were used to detect FFA4.

Results:

Ten to 100 μmol/L of omega-3 polyunsaturated fatty acids α-linolenic acid (αLA) or eicosapentaenoic acid (EPA) induced dose-dependent [Ca²⁺]_i increase in HCT116 and HT-29 cells, whereas docosahexaenoic acid (DHA) had no effect. In addition, the omega-6 fatty acids linoleic acid and γ-linoleic acid also dose-dependently increase [Ca²⁺]_i, but the mono-unsaturated fatty acid oleic acid and saturated fatty acids such as stearic acid and palmitic acid had no effect. In HCT116 and HT-29 cells, the αLA-induced [Ca²⁺]_i increase was partially inhibited by pretreatment with EGTA, phospholipase C inhibitor edelfosine, cADPR inhibitors 8-bro-cADPR or DAB, and abolished by pretreatment with Ca²⁺ATPase inhibitor thapsigargin, but was not affected by G_i/o protein inhibitor PTX or IP₃R inhibitor 2-APB.

Conclusion:

Omega-3 and omega-6 long-chain polyunsaturated fatty acids (C18-20) induce Ca²⁺ mobilization responses in human colonic epithelial cells in vitro through activation of FFA4 and PTX-insensitive G_i/o protein, followed by Ca²⁺ release from thapsigargin-sensitive Ca²⁺ stores and Ca²⁺ influx across the plasma membrane.     

Extraction and quantification of polyphenols from kinnow (Citrus reticulate L.) peel using ultrasound and maceration techniques

An investigation was carried out to extract polyphenols from the peel of kinnow (Citrus reticulate L.) by maceration and ultrasound-assisted extraction (UAE) techniques. The antioxidant potential of these polyphenols was evaluated using ferric reducing antioxidant power (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and superoxide radical scavenging assays; and their antimicrobial activity was assessed against bacterial strains Staphyloccoccus aureus, Bacillus cereus, and Salmonella typhimurium. The highest extraction yield was obtained through the solvent ethanol at 80% concentration level, whereas UAE was a more efficient technique and yielded comparatively higher polyphenol contents than maceration. Maximum polyphenols were extracted with 80% methanol [32.48 mg gallic acid equivalent (GAE)/g extract] using UAE, whereas minimum phenolics (8.64 mg GAE/g extract) were obtained with 80% ethyl acetate through the maceration technique. Elevated antioxidant activity of kinnow peel extracts was exhibited in three antioxidant assays, where 80% methanolic extracts showed the highest antioxidant activity (27.67 ± 1.11mM/100 g for FRAP) and the highest scavenging activity, 72.83 ± 0.65% and 64.80 ± 0.91% for DPPH and superoxide anion radical assays, respectively. Strong correlations between total polyphenols and antioxidant activity were recorded. Eleven phenolic compounds—including five phenolic acids and six flavonoids—were identified and quantified by high performance liquid chromatography. Ferulic acid and hesperidin were the most abundant compounds whereas caffeic acid was the least abundant phenolic compound in kinnow peel extracts. Maximum inhibition zone was recorded against S. aureus (16.00 ± 0.58 mm) whereas minimum inhibition zone was noted against S. typhimurium (9.00 ± 1.16 mm). It was concluded that kinnow mandarin peels, being a potential source of phenolic compounds with antioxidant and antimicrobial properties, may be used as an ingredient for the preparation of functional foods.     

Malt and beer-related by-products as potential antioxidant skin-lightening agents for cosmetics

Malt and beer-related by-products, namely caramalt, aromatic malt, roasted malt, malt sprouts, dark beer spent grains, and wheat beer spent grains were extracted with water under moderate conditions to exploit the potential as sources of bioactive compounds. After characterizing the extracts in terms of carbohydrate, amino acid, and phenolic contents and composition, their antioxidant potential was assessed in vitro using keratinocyte cell cultures. Malt sprouts provided highest yields of glucose (50.1 mg g^-1) and fructose (38.4 mg g^-1), while the other materials gave up to 13.5 mg g^-1. Furthermore, malt sprouts gave a total amino acid content of 57.6 mg g^-1. Extracts of darker malts such as caramalt and roasted malt exhibited the highest yields of phenolic compounds of about 12.9 mg gallic acid equivalents (GAE) g^-1 and extracts from spent grains had the lowest total yield with 5.1 and 1.8 mg GAE g^-1 (dark beer and wheat beer spent grains), respectively. Phenolic compounds in caramalt extract inhibited the tyrosinase activity by 78% and 87%, when applying extract concentrations of 0.5% and 1%, respectively. Dark malt, roasted malt as well as the malt sprouts extracts achieved similar effects of 86% and 80% inhibition, when using a 1% extract. In contrast, extracts of spent grains showed low inhibitory effects. This study indicates the potential of malt and beer-related by-products as biological sources of ingredients for cosmeceutical products, for instance, in skin whitening.     

Biotransformation of pantoprazole by the fungus Cunninghamella blakesleeana

To investigate the biotransformation of pantoprazole, a proton-pump inhibitor, by filamentous fungus and further to compare the similarities between microbial transformation and mammalian metabolism of pantoprazole, four strains of Cunninghamella (C. blakesleeana AS 3.153, C. echinulata AS 3.2004, C. elegans AS 3.156, and AS 3.2028) were screened for the ability to catalyze the biotransformation of pantoprazole. Pantoprazole was partially metabolized by four strains of Cunninghamella, and C. blakesleeana AS 3.153 was selected for further investigation. Three metabolites produced by C. blakesleeana AS 3.153 were isolated using semi-preparative HPLC, and their structures were identified by a combination analysis of LC/MSⁿ and NMR spectra. Two further metabolites were confirmed with the aid of synthetic reference compounds. The structure of a glucoside was tentatively assigned by its chromatographic behavior and mass spectroscopic data. These six metabolites were separated and quantitatively assayed by liquid chromatography-ion trap mass spectrometry. After 96?h of incubation with C. blakesleeana AS 3.153, approximately 92.5% of pantoprazole was metabolized to six metabolites: pantoprazole sulfone (M1, 1.7%), pantoprazole thioether (M2, 12.4%), 6-hydroxy-pantoprazole thioether (M3, 1.3%), 4′-O-demethyl-pantoprazole thioether (M4, 48.1%), pantoprazole thioether-1-N-β-glucoside (M5, 20.6%), and a glucoside conjugate of pantoprazole thioether (M6, 8.4%). Among them, M5 and M6 are novel metabolites. Four phase I metabolites of pantoprazole produced by C. blakesleeana were essentially similar to those obtained in mammals. C. blakesleeana could be a useful tool for generating the mammalian phase I metabolites of pantoprazole.     

Preclinical evaluation and pilot clinical study of [18F]AlF-labeled FAPI-tracer for PET imaging of cancer associated fibroblasts

In recent years, fibroblast activation protein (FAP) has emerged as an attractive target for the diagnosis and radiotherapy of cancers using FAP-specific radioligands. Herein, we aimed to design a novel ¹⁸F-labeled FAP tracer ([¹⁸F]AlF-P-FAPI) for FAP imaging and evaluated its potential for clinical application. The [¹⁸F]AlF-P-FAPI novel tracer was prepared in an automated manner within 42 min with a non-decay corrected radiochemical yield of 32 ± 6% (n = 8). Among A549-FAP cells, [¹⁸F]AlF-P-FAPI demonstrated specific uptake, rapid internalization, and low cellular efflux. Compared to the patent tracer [¹⁸F]FAPI-42, [¹⁸F]AlF-P-FAPI exhibited lower levels of cellular efflux in the A549-FAP cells and higher stability in vivo. Micro-PET imaging in the A549-FAP tumor model indicated higher specific tumor uptake of [¹⁸F]AlF-P-FAPI (7.0 ± 1.0% ID/g) compared to patent tracers [¹⁸F]FAPI-42 (3.2 ± 0.6% ID/g) and [⁶⁸Ga]Ga-FAPI-04 (2.7 ± 0.5% ID/g). Furthermore, in an initial diagnostic application in a patient with nasopharyngeal cancer, [¹⁸F]AlF-P-FAPI and [¹⁸F]FDG PET/CT showed comparable results for both primary tumors and lymph node metastases. These results suggest that [¹⁸F]AlF-P-FAPI can be conveniently prepared, with promising characteristics in the preclinical evaluation. The feasibility of FAP imaging was demonstrated using PET studies.     

Pretreatment/fractionation and characterization of winery waste streams within an integrated biorefinery concept

The aim of this work was the characterization of the main winery wastes, e.g. vineyard prunings, grape stalks, grape pomace and wine lees, and the utilization of the hydrothermal pretreatment towards selective fractionation and recovery of hemicellulose (and related sugars, furans and acids), increased cellulose enzymatic hydrolysis, and isolation of “surface” and hydrothermal/acid hydrolysis lignin, discussing also the potential valorization of each stream into value-added chemicals. Two varieties from Greece were investigated, i.e. Grenache Rouge (Vitis vinifera L. cv. Grenache Rouge) and Malagouzia (Vitis vinifera L. cv. Malagouzia). Three hydrothermal pretreatment severities were applied, i.e. logRo 3.24, 4.32 and 4.71 (corresponding to 170^oC-15 min, 170^oC-180 min, and 220^oC-15 min), all leading to enhanced enzymatic hydrolysis of cellulose in the vine prunings to glucose. The composition of the recovered aqueous product contained mainly glucan and xylan, which were converted to monomeric sugars and eventually to furans (furfural, HMF) and organic acids (formic, lactic) at more intense conditions. The grape stalks and mainly the grape pomace which comprises of grape skins and seeds, contained less carbohydrates compared to vine prunings, but can be considered as an abundant source of lignin that can provide fast pyrolysis oils enriched in phenolic compounds. Similarly, the extracted surface lignin from the hydrothermally pretreated vine prunings may offer highly phenolic/aromatic bio-oils. The extractives of the parent lignocellulosic wastes (15–50 wt%) contain water soluble sugar monomers and oligo-saccharides and ethanol soluble fatty acids (palmitic, tridecanoic, a-linoleic, oleic, stearic acids). The wine lees can be considered as a source of value-added polyols and phenyl alcohols, such as glycerin (1,2,3-propanotriol), 2,3-butanediol and phenylethyl alcohol.     

Changes in the relative levels of fatty acids in blood and myocardium in the Prague breed of rats with hereditary hypercholesteremia after administration of slow calcium channel blockers]

The present paper describes the effect of six-week oral administration of verapamil and diltiazem (1 mg.kg-1 of weight two times daily in 12 hour intervals) on the content of fatty acids of the serum and myocardium of PHHC rats. A cholesterol diet changes the content of fatty acids of the serum and myocardium of PHHC rats in comparison with control rats without the cholesterol diet. A significant decrease in the content of palmitic acid, a decrease in the content of stearic acid, linoleic acid and arachidonic acid and a significant increase in the content of oleic acid were observed in the serum. Long-term administration of the slow calcium channel blockers produces another decrease in the content of the bound form of arachidonic acid. Changes in the representation of other fatty acids are not marked. Long-term administration of a cholesterol diet produces an increase in the content of palmitic acid and stearic acid and a decrease in the content of oleic acid, linoleic acid and arachidonic acid in the myocardium. Administration of verapamil results in a modification of the above-mentioned changes in all parameters excepting the content of arachidonic acid, the content of which was decreased in an even more marked manner. Administration of diltiazem produced an accumulation of both saturated and mono-unsaturated fatty acids (palmitic, stearic and oleic acids) and produced a significant decrease in the content of linoleic acid and mainly the bound form of arachidonic acid.(ABSTRACT TRUNCATED AT 250 WORDS)     

GC法同时测定鸦胆子油中4种脂肪酸的含量

目的建立同时测定鸦胆子油中棕榈酸、硬脂酸、油酸和亚油酸4种成分含量的方法。方法采用毛细管气相色谱法,甲酯化后测定鸦胆子油中棕榈酸、硬脂酸、油酸和亚油酸的含量。色谱柱:DB-17弹性石英毛细管柱(30 m×0.25 mm×0.25μm),检测器:氢火焰离子化检测器(FID),柱温恒温:200℃(保持11 min),进样口温度:250℃,检测器温度:250℃,流速:1.0 mL.min-1,分流比:20∶1,内标物:苯甲酸苯酯。结果棕榈酸、硬脂酸、油酸和亚油酸的线性分别为74～738 mg.L-1(r=0.999 6)、51～509 mg.L-1(r=0.999 1)、741～7 410 mg.L-1(r=0.999 1)和265～2 650 mg.L-1(r=0.999 1);各成分的平均回收率(n=9)分别为94.6%、94.2%、94.2%和95.3%。结论此方法可为鸦胆子油的质量评价提供依据。     

Effects of C18 Fatty Acids on Intracellular Ca2+ Mobilization and Histamine Release in RBL-2H3 Cells

To investigate the underlying mechanisms of C18 fatty acids (stearic acid, oleic acid, linoleic acid and α-linolenic acid) on mast cells, we measured the effect of C18 fatty acids on intracellular Ca²⁺ mobilization and histamine release in RBL-2H3 mast cells. Stearic acid rapidly increased initial peak of intracellular Ca²⁺ mobilization, whereas linoleic acid and α-linolenic acid gradually increased this mobilization. In the absence of extracellular Ca²⁺, stearic acid (100 µM) did not cause any increase of intracellular Ca²⁺ mobilization. Both linoleic acid and α-linolenic acid increased intracellular Ca²⁺ mobilization, but the increase was smaller than that in the presence of extracellular Ca²⁺. These results suggest that C18 fatty acid-induced intracellular Ca²⁺ mobilization is mainly dependent on extracellular Ca²⁺ influx. Verapamil dose-dependently inhibited stearic acid-induced intracellular Ca²⁺ mobilization, but did not affect both linoleic acid and α-linolenic acid-induced intracellular Ca²⁺ mobilization. These data suggest that the underlying mechanism of stearic acid, linoleic acid and α-linolenic acid on intracellular Ca²⁺ mobilization may differ. Linoleic acid and α-linolenic acid significantly increased histamine release. Linoleic acid (C18:2: ω-6)-induced intracellular Ca²⁺ mobilization and histamine release were more prominent than α-linolenic acid (C18:3: ω-3). These data support the view that the intake of more α-linolenic acid than linoleic acid is useful in preventing inflammation.     

Novel STING-targeted PET radiotracer for alert and therapeutic evaluation of acute lung injury

Acute lung injury(ALI),as a common clinical emergency,is pulmonary edema and diffuse lung infiltration caused by inflammation.The lack of non-invasive alert strategy,resulting in failure to carry out preventive treatment,means high mortality and poor prognosis.Stimulator of interferon genes(STING) is a key molecular biomarker of innate immunity in response to inflammation,but there is still a lack of STING-targeted strategy.In this study,a novel STING-targeted PET tracer,[¹⁸F]FBTA,was...     

Effects of dehydroepiandrosterone on oleic acid accumulation in rat liver

The purpose of the present study was to determine whether dehydroepiandrosterone (DHEA) affects de novo fatty acid synthesis, oleic acid formation, fatty acid oxidation, and very low density lipoprotein (VLDL) secretion, in relation to the accumulation of lipid containing oleic acid, in rat liver. The rates of hepatic de novo synthesis of both fatty acid and monounsaturated fatty acid, determined by incorporation of 3H from 3H(2)O into fatty acid, were increased markedly when rats were fed a diet containing 0.5% (w/w) DHEA for 14 days. The treatment of rats with DHEA also enhanced the conversion of [14C]stearic acid into oleic acid in the liver in vivo. DHEA did not suppress fatty acid degradation in the liver. Namely, mitochondrial palmitic acid oxidation in liver homogenates and isolated hepatocytes was increased approximately 1.9- and 5-fold, respectively, in DHEA-treated rats. Peroxisomal palmitic acid oxidation in isolated hepatocytes from rats treated with DHEA, however, was not significantly different from that of the control, despite the fact that peroxisomal degradation of palmitic acid in the liver homogenates was increased markedly. The rate of hepatic VLDL secretion in DHEA-treated rats was decreased markedly. These results indicate that the elevation of the hepatic fatty acid content, especially oleic acid, by DHEA feeding is due to an increase in both de novo fatty acid synthesis and the formation of oleic acid and to a decrease in the rate of hepatic VLDL secretion. Mitochondrial and peroxisomal fatty acid degradation does not appear to play a significant role in the accumulation of hepatic lipids.