Mckenziemohr2464
To further elucidate the active components of leaves of C. paliurus, the 70% ethanol eluate fraction was characterized by UPLC-MS/MS analysis, and 10 compounds were identified. This study provides a valuable reference for further research and development of hypoglycemic active components of C. paliurus.Borneol (Bingpian), a monoterpenoid pharmaceutical ingredient, is commonly used as a main composition in traditional Chinese medicine preparations such as compound Danshen dropping pills (CDDP) and has also been approved by the U.S. Food and Drug Administration as a flavoring substance or adjuvant in food. Borneol plays a regulating and guiding role as a messenger drug in CDDP. However, the effect of borneol on the pharmacokinetics of the components of CDDP in human plasma is unclear. In this study, we investigate the effects of borneol on the pharmacokinetics of ginsenoside Rb1 (Rb1 ), ginsenoside Rg1 (Rg1 ), and notoginsenoside R1 (NR1 ) in CDDP. We used a double-cycle crossover-administration model in 12 healthy male volunteers, administered CDDP with borneol (drug T) and without borneol (drug R). The selective response monitoring mode was used for MS quantification in the positive mode. As a result, we found that borneol could significantly affect the pharmacokinetic parameters of notoginsenosides and increase the absorption and systemic exposure of Rb1 , Rg1 , and NR1 in human plasma by ~1.85-3.71 times.Our study explores the combined effect of polyacrylic acid and vitamin E as prophylactic and curative agent against ethylene glycol (EG) induced calcium oxalate stone formation in Wistar rats. Male Wistar rats (54) were divided into nine groups, including control. The experimental groups were equally segregated into two for preventive study (4) and curative study (4). Urolithiasis was induced with 0.75% (v/v) EG in drinking water. Polyacrylic acid (10 mg/kg) and vitamin E (300 IU/day) were supplemented from day 1 for preventive and day 30 for curative studies. Restoration of urinary lithogenic factors (calcium, oxalate, phosphate, citrate and magnesium) and renal function (urea and creatinine in serum) by intervening agents were accomplished compared to urolithic rats (P less then .001). Abnormal localization and increased expression of Tamm-Horsfall Protein, osteopontin and transferrin were observed in the kidneys of urolithic rats (P less then .001) from immunohistochemistry and immunoblotting analysis. Polyacrylic acid and vitamin E supplementation have regulated the expression of the urinary macromolecules. Pro-inflammatory cytokines in kidney were significantly reduced (P less then .001) by the intervening agents compared to urolithic rats. Therefore, polyacrylic acid and vitamin E in combination could be a potential formulation for better management of urolithiasis.Tropical forests are important to the regulation of climate and the maintenance of biodiversity on Earth. However, these ecosystems are threatened by climate change, as temperatures rise and droughts' frequency and duration increase. Xylem anatomical traits are an essential component in understanding and predicting forest responses to changes in water availability. We calculated the community-weighted means and variances of xylem anatomical traits of hydraulic and structural importance (plot-level trait values weighted by species abundance) to assess their linkages to local adaptation and community assembly in response to varying soil water conditions in an environmentally diverse Brazilian Atlantic Forest habitat. Scaling approaches revealed community-level tradeoffs in xylem traits not observed at the species level. Towards drier sites, xylem structural reinforcement and integration balanced against hydraulic efficiency and capacitance xylem traits, leading to changes in plant community diversity. We show how general community assembly rules are reflected in persistent fiber-parenchyma and xylem hydraulic tradeoffs. Trait variation across a moisture gradient is larger between species than within species and is realized mainly through changes in species composition and abundance, suggesting habitat specialization. Modeling efforts to predict tropical forest diversity and drought sensitivity may benefit from adding hydraulic architecture traits into the analysis.An HPLC method has been described in the European Pharmacopoeia and United States Pharmacopeia for the determination of nine organic impurities (imp A-I) in fingolimod hydrochloride, a synthetic sphingosine-1-phosphate receptor modulator. The manufacturing process of fingolimod hydrochloride consists of multistep chemical synthesis wherein controls of precursors, intermediates and process steps should be performed to assure the final quality of the drug substance. We synthesized and isolated eight process-related impurities (FINI imp A-H) of fingolimod, which were different from the pharmacopoeial impurities. One unknown process-related impurity was found as a key intermediate (FINI) and was identified by LC-MS. Characterization of all of the impurities were done using spectroscopic techniques (1 H and 13 C NMR, FTIR, MS), and the mechanistic pathways to the formation of these impurities were also discussed. Two of these impurities were evaluated as potential genotoxic impurities owing to their alerting structures and alkylating properties (alkyl sulfonates and alkyl halides, class 3, ICH M7). We also developed and validated an RP-UPLC method in line with ICH Q2 guidelines for control these impurities (FINI imp A-H) and to assure the pharmacopoeial quality drug substance.Obesity is a predisposing factor to diseases such as diabetes mellitus, hypertension, and coronary artery disease. Lemongrass essential oil (LEO), from Cymbopogon flexuosus, possesses numerous therapeutic properties including modulation of obesity in vivo. This experiment investigated the effect of LEO and its major components citral (3,7-dimethyl-2,6-octadienal), citral dimethyl acetal (1,1-dimethoxy-3,7-dimethylocta-2,6-diene), and citral diethyl acetal (1,1-diethoxy-3,7-dimethylocta-2,6-diene) in modulation of adipogenesis and genetic expression in adipocytes. Adipogenesis was induced from murine 3T3-L1 preadipocytes procured from ATCC and maintained in Dulbecco's modified Eagle's medium (DMEM) enriched with calf serum. Differentiation was conducted using DMEM enriched with 10% fetal bovine serum, Dexamethasone 0.25 µM, 3-isobutyl-methylxanthine 0.5 mM, and insulin 10 mg/ml for 2 days, followed by 5 days of insulin 10 mg/ml alone. Samples were subjected to experimental treatments at a concentration of 2.5 d effect.American ginseng berry (AGB) is a new medicinal source. Total saponins of American ginseng berry (TSAGB) are the main active ingredients. The effects and active saponins of TSAGB on myocardial ischemia (MI) rats were evaluated for the first time. First, there were 69 saponins identified or tentatively characterized by Ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS/MS) combined with UNIFI platform, among which, about 28 saponins were first identified in AGB. Second, MI model was established by ligating left coronary artery. It has been demonstrated that TSAGB could prevent the ST-segment elevation, reduce myocardial infarct size and levels of aspartate aminotransferase (AST), creatine kinase (CK), lactate dehydrogenase (LDH), malondialdehyde (MDA), and elevate the superoxide dismutase (SOD) level. Finally, network pharmacology combined with molecular docking to screen out four active saponins (ginsenoside Re, Rb3 , Rg3 , and PF11 ) and five key targets (SOD1, LDHA, CKB, GOT2, and ROS1) closely related to MI. PRACTICAL APPLICATIONS This study enriches the chemical composition of TSAGB, and provides a basis for clarifying the pharmacological substances for anti-myocardial ischemia. TSAGB might be a potential anti-myocardial ischemia agent. The effect might be related to alleviating oxidative stress.Hot water treatment (HWT) of tomato (Solanum lycopersicum L.) fruit reduces the symptoms of chilling injury (CI). see more The aim of this study was to identify metabolites associated with HWT-induced CI tolerance in tomato fruit cv. Imperial. Mature green tomatoes with HWT (42°C/5 min) and control were stored under chilling conditions (5°C/20 days) and then ripened (21°C/7 days). Methanol extracts from pericarp were analyzed for total phenolics (TP), antioxidant activity (AoxA), and metabolic profiling by UPLC-DAD-MS and GC-MS. After cold storage and ripening, HWT fruit showed less CI, higher TP, and AoxA than control. It also showed an increased accumulation of phenolics, sugars, and some alkaloids that may be mediated by azelaic acid, glutamine, and tryptophan. The levels of N-feruloyl putrescine, esculeoside AII, and hydroxy-α-tomatine II were reduced. The better metabolic performance of HWT fruit under cold storage was associated with a higher accumulation of several metabolites (e.g., antioxidants and osmolytes) in ripening fruit. PRACTICAL APPLICATION The identification of metabolites associated with the reduction of chilling injury (CI) symptoms in HWT tomato fruit extends the understanding of the mechanisms involved in CI tolerance. This information provides targets that could be used to develop strategies for preventing CI (e.g., genetic improvement of tomato, direct application of key metabolites). The application of such strategies will increase the economic value and decrease postharvest losses.Fucosterol is the main phytosterol in brown algae with various pharmacological effects such as cholesterol-lowering, anticancer, hepatoprotection and neuroprotection. Little is known about the pharmacokinetics and excretion characteristics of fucosterol. In this study, a GC-MS method was developed and validated for the determination of fucosterol in rat plasma, urine and feces. The method effectively avoids the interference of Δ5 -avenasterol, a cis-trans-isomer of fucosterol derived from feed, by using a TG-5 capillary column (a nonpolar column with 5% phenyl-methylpolysilicone as stationary phase material). The linearity ranges were fucosterol 0.300-18.0 μg/ml (R2 = 0.9960) for plasma, 0.0500-2.50 μg/ml for the urine sample (R2 = 0.9963) and 0.100-8.00 μg/mg (R2 = 0.9923) for the feces sample. With good extraction recoveries and stability, this rapid and sensitive method was successfully applied to the pharmacokinetic and excretion studies of fucosterol in Sprague-Dawley rats. Fucosterol from Sargassum fusiforme had poor absorption and slow elimination with an absolute oral bioavailability of 0.74%, and was mainly eliminated through fecal excretion.The present research aimed to investigate the attenuative effects of watermelon (Citrullus lanatus) leaf extract on biochemical and histological parameters in a high-fat diet combined with a low-dose streptozotocin (HFD/STZ)-induced type 2 diabetes mellitus. Forty male Sprague Dawley rats were divided into five groups, including three supplemented groups 10 mg metformin/kg BW (HFD/STZ +M), 200 mg watermelon leaf extract /kg BW (HFD/STZ + LD), and 400 mg watermelon leaf extract /kg BW (HFD/STZ + HD). The efficacy of the 6-week intervention was evaluated by measuring body weight, fasting blood sugar, serum insulin, lipid profile, superoxide dismutase, catalase, malondialdehyde, and serum liver markers. Kidneys and liver structure were defined by histopathological examination. Results revealed that intervention with watermelon leaf extract attenuated the biochemical parameters and the structural changes in kidneys and liver. In brief, the watermelon leaf extract treatment could effectively decrease complications associated with diabetes better than metformin, and that the treatment with 400 mg/kg BW is the most potent.