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  • MDPI AG  (7)
  • Pharmacy  (7)
  • 1
    In: Marine Drugs, MDPI AG, Vol. 19, No. 8 ( 2021-07-29), p. 431-
    Abstract: The neoagaro-oligosaccharides, degraded from agarose by agarases, are important natural substances with many bioactivities. In this study, a novel agarase gene, agaW1540, from the genome of a deep-sea bacterium Shewanella sp. WPAGA9, was expressed, and the recombinant AgaW1540 (rAgaW1540) displayed the maximum activity under the optimal pH and temperature of 7.0 and 35 °C, respectively. rAgaW1540 retained 85.4% of its maximum activity at 0 °C and retained more than 92% of its maximum activity at the temperature range of 20–40 °C and the pH range of 4.0–9.0, respectively, indicating its extensive working temperature and pH values. The activity of rAgaW1540 was dramatically suppressed by Cu2+ and Zn2+, whereas Fe2+ displayed an intensification of enzymatic activity. The Km and Vmax of rAgaW1540 for agarose degradation were 15.7 mg/mL and 23.4 U/mg, respectively. rAgaW1540 retained 94.7%, 97.9%, and 42.4% of its maximum activity after incubation at 20 °C, 25 °C, and 30 °C for 60 min, respectively. Thin-layer chromatography and ion chromatography analyses verified that rAgaW1540 is an endo-acting β-agarase that degrades agarose into neoagarotetraose and neoagarohexaose as the main products. The wide variety of working conditions and stable activity at room temperatures make rAgaW1540an appropriate bio-tool for further industrial production of neoagaro-oligosaccharides.
    Type of Medium: Online Resource
    ISSN: 1660-3397
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
    detail.hit.zdb_id: 2175190-0
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  • 2
    In: Marine Drugs, MDPI AG, Vol. 20, No. 11 ( 2022-11-01), p. 692-
    Abstract: Up until now, the characterizations of GH50 agarases from Vibrio species have rarely been reported compared to GH16 agarases. In this study, a deep-sea strain, WPAGA4, was isolated and identified as Vibrio natriegens due to the maximum similarity of its 16S rRNA gene sequence, the values of its average nucleotide identity, and through digital DNA–DNA hybridization. Two circular chromosomes in V. natriegens WPAGA4 were assembled. A total of 4561 coding genes, 37 rRNA, 131 tRNA, and 59 other non-coding RNA genes were predicted in the genome of V. natriegens WPAGA4. An agarase gene belonging to the GH50 family was annotated in the genome sequence and expressed in E. coli cells. The optimum temperature and pH of the recombinant Aga3420 (rAga3420) were 40 °C and 7.0, respectively. Neoagarobiose (NA2) was the only product during the degradation process of agarose by rAga3420. rAga3420 had a favorable stability following incubation at 10–30 °C for 50 min. The Km, Vmax, and kcat values of rAga3420 were 2.8 mg/mL, 78.1 U/mg, and 376.9 s−1, respectively. rAga3420 displayed cold-adapted properties as 59.7% and 41.2% of the relative activity remained at 10 3 °C and 0 °C, respectively. This property ensured V. natriegens WPAGA4 could degrade and metabolize the agarose in cold deep-sea environments and enables rAga3420 to be an appropriate industrial enzyme for NA2 production, with industrial potential in medical and cosmetic fields.
    Type of Medium: Online Resource
    ISSN: 1660-3397
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2175190-0
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  • 3
    In: Pharmaceuticals, MDPI AG, Vol. 15, No. 10 ( 2022-10-21), p. 1303-
    Abstract: (1) Background: High-altitude hypoxia has been shown to affect the pharmacokinetic properties of drugs. Although there is a high incidence of cardiovascular disease among individuals living in high-altitude areas, studies on the effect of high-altitude hypoxia on the pharmacokinetic properties of cardiovascular drugs are limited. (2) Methods: The aim of this study was to evaluate the pharmacokinetics of nifedipine, bosentan, simvastatin, sildenafil, and their respective main metabolites, dehydronifedipine, hydroxybosentan, simvastatin hydroxy acid, and N-desmethyl sildenafil, in rats exposed to high-altitude hypoxia. Additionally, the protein and mRNA expression of cytochrome P450 3A1 (CYP3A1), a drug-metabolizing enzyme, were examined. (3) Results: There were significant changes in the pharmacokinetic properties of the drugs in rats exposed to high-altitude hypoxia, as evidenced by an increase in the area under the curve (AUC) and the half-life (t1/2z) and a decrease in total plasma clearance (CLz/F). However, most of these changes were reversed when the rats returned to a normoxic environment. Additionally, there was a significant decrease in CYP3A1 expression in rats exposed to high-altitude hypoxia at both the protein and mRNA levels. (4) Conclusions: High-altitude hypoxia suppressed the metabolism of the drugs, indicating that the pharmacokinetics of the drugs should be re-examined, and the optimal dose should be reassessed in patients living in high-altitude areas.
    Type of Medium: Online Resource
    ISSN: 1424-8247
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2193542-7
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  • 4
    In: Antioxidants, MDPI AG, Vol. 11, No. 7 ( 2022-07-08), p. 1340-
    Abstract: Yeast β-glucan is a natural antioxidant and has been reported to improve growth performance of piglets, but its application in improving pork quality is limited. This study investigated the effects of dietary yeast β-glucan supplementation on meat quality, antioxidant capacity and gut microbiota of finishing pigs. In a 40-day experiment, ninety finishing pigs (Duroc × Landrace × Yorkshire, 70.47 ± 0.04 kg) were randomly allocated into five treatments including a basal diet supplemented with 0, 50, 100, 200 and 400 mg/kg yeast β-glucan. Results showed that yeast β-glucan significantly increased pH45 min (linear and quadratic, p 〈 0.01) and a*45 min (linear, p 〈 0.05), and reduced cooking loss (linear, p 〈 0.05) and drip loss (quadratic, p 〈 0.05) of meat in finishing pigs. Importantly, the 200 mg/kg group exhibited the highest values of pH45 min (p 〈 0.01) and the lowest values of drip loss (p 〈 0.05), accompanied by a decreased lactate content (p 〈 0.05) and glycolytic potential (p 〈 0.05). Dietary supplementation of 200 mg/kg yeast β-glucan markedly increased catalase (CAT) (p 〈 0.05), superoxide dismutase (SOD) (p 〈 0.05) and total antioxidant capacity (T-AOC) (p 〈 0.01) activities in skeletal muscle. Moreover, WPS-2 abundance was decreased significantly in colonic digesta by 200 mg/kg yeast β-glucan and exhibited a positive association with muscle lactate content and drip loss. Together, dietary 200 mg/kg yeast β-glucan supplementation effectively improved pH value and the water-holding capacity of fresh meat through reducing muscle postmortem glycolysis, increasing antioxidant capacity and altering the gut microbiota composition of finishing pigs.
    Type of Medium: Online Resource
    ISSN: 2076-3921
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2704216-9
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  • 5
    In: Antioxidants, MDPI AG, Vol. 11, No. 12 ( 2022-12-01), p. 2383-
    Abstract: Acute liver injury has multiple causes and can result in liver failure. In this study, we evaluated the hepatoprotective ability of cyanidin (Cy) and investigated its associated mechanisms. Cy administration significantly and dose-dependently ameliorated acute liver injury induced by carbon tetrachloride (CCl4). High-dose Cy showed effects comparable to those achieved by the positive control (silymarin). Severe oxidative stress and inflammatory responses in the liver tissue induced by CCl4 were significantly mitigated by Cy supplementation. The total antioxidant capacity and the activity of superoxide dismutase, catalase, and glutathione peroxidase were increased and the content of malondialdehyde, lipid peroxide, tumor necrosis factor α, interleukin-1β, and interleukin-6 were decreased. Additionally, the Nrf2 and NF-κB signaling pathways, which regulate antioxidative and inflammatory responses, were analyzed using quantitative real-time polymerase chain reaction and western blot assay. Cy treatment not only increased Nrf2 transcription and expression but also decreased NF-κB signaling. Moreover, molecular docking simulation indicated that Cy had high affinity for Keap1 and NF-κB/p65, which may promote nuclear translocation of Nrf2 and inhibit that of NF-κB. In summary, Cy treatment exerted antioxidative and anti-inflammatory effects and ameliorated liver injury by increasing Nrf2 and inhibiting the NF-κB pathway, demonstrating the potential of Cy as a therapeutic agent in liver injury.
    Type of Medium: Online Resource
    ISSN: 2076-3921
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2704216-9
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  • 6
    In: Pharmaceuticals, MDPI AG, Vol. 16, No. 1 ( 2023-01-09), p. 99-
    Abstract: The objective of the present study was to develop a gentiopicroside-phospholipid complex (GTP-PC) and its self-nanoemulsion drug delivery system (GTP-PC-SNEDDS) to increase the oral bioavailability of gentiopicroside (GTP). The factors affecting the formation of GTP-PC were studied with the complexation efficiency and dissociation rate. The properties of the complex were investigated by means of differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared spectra (FT-IR), dissolution, etc. Then, GTP-PC was loaded into SNEDDS by investigating the effects of weight ratios of GTP-PC to blank SNEDDS, preparation technology, dilution media, and dilution multi, based on the screening results of oils, surfactants, and cosurfactants. In rats, GTP, GTP-PC, and GTP-PC-SNEDDS were orally administered at different times, and GTP concentrations were determined using RP-HPLC. The optimal GTP-PC was prepared with tetrahydrofuran as the reaction solvent, GTP:phospholipid = 1:2, and stirring for 4 h. The optimal prescription for GTP-PC-SNEDDS was as follows: Maisin 35-1:Miglycol = 30%, Labrasol:Cremophor EL = 1:4 = 40%, Transcutol P = 30%; Maisin 35-1:Miglycol = 12, and the ratio of GTP-PC to blank was 1:10—then the mixture was stirred at 37 °C for 1 d and then placed for 2 d to form stable GTP-PC-SNEDDS. After oral administration of GTP, GTP-PC and GTP-PC-SNEDDS, and mean plasma GTP concentration–time curves were all in accordance with the single-compartment model. The Cmax, AUC0–∞, and Fr of the three formulations were significantly higher than that of GTP, demonstrating that GTP was metabolized rapidly, and its higher bioavailability could be achieved by the formation of GTP-PC and GTP-PC-SNEDDS. Among the three formations, the bioavailability of GTP-PC-SNEDDS was highest, with approximately 2.6-fold and 1.3-fold of Fr value, compared with GTP-PC (suspension) and GTP-PC (oil solution), respectively. Compared with GTP, GTP-PC and GTP-PC-SNEDDS enhanced the bioavailability of GTP significantly. In the future, this study could serve as a reference for clinical trials using GTP-PC and GTP-PC-SNEDDS.
    Type of Medium: Online Resource
    ISSN: 1424-8247
    Language: English
    Publisher: MDPI AG
    Publication Date: 2023
    detail.hit.zdb_id: 2193542-7
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  • 7
    In: Antioxidants, MDPI AG, Vol. 11, No. 4 ( 2022-03-29), p. 657-
    Abstract: Mastitis (inflammation of the mammary gland) commonly occurs in dairy cattle during the periparturient period (transition period), in which dairy cattle experience physiological and hormonal changes and severe negative energy balance, followed by oxidative stress. To maintain successful lactation and combat negative energy balance (NEB), excessive fat mobilization occurs, leading to overproduction of reactive oxygen species (ROS). Excessive fat mobilization also increases the concentrations of nonesterified fatty acids (NEFA) and β-hydroxybutyric acid (BHB) during the periparturient period. In addition, the excessive utilization of oxygen by cellular respiration in the mammary causes abnormal production of oxidative stress (OS). OS impairs the immunity and anti-inflammatory efficiency of periparturient dairy cattle, increasing their susceptibility to mastitis. To alleviate oxidative stress and subsequent mastitis, antioxidants are supplemented to dairy cattle from an external source. Extensive studies have been conducted on the supplementation of selenium (Se) and vitamins E and B9 to mitigate mastitis during the transition period in dairy cattle. Altogether, in the current review, we discuss the research development on bovine mastitis and its major causes, with special emphasis on oxidative stress during the transition period. Moreover, we discuss the antioxidant, immunoregulatory, and anti-inflammatory properties of Se and vitamins E and B9 and their role in the control of bovine mastitis in periparturient dairy cattle.
    Type of Medium: Online Resource
    ISSN: 2076-3921
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2704216-9
    SSG: 15,3
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