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  • 1
    Publikationsdatum: 2018
    Beschreibung: The people of the Bayangi tribe (Manyu Division) of Cameroon have used the leaves of Pseudopanax arboreus (Araliaceae) traditionally for decades as an aphrodisiac. In order to scientifically investigate this folk claim, we evaluated the effects of the leaf-aqueous extract of P. arboreus on the sexual behavior of normal male rats. The present study was designed to assess the effects of the leaf-methanolic extract of P. arboreus on amitriptyline-induced sexual dysfunction in male rats. Sexually impaired male rats were randomly divided into 4 groups of 8 rats each. Group 1 received 10 ml/kg distilled water, while group 2 was given 6 mg/kg Viagra. Groups 3 and 4 received 46.5 and 93 mg/kg of the leaf-methanolic extract, respectively. Female rats were made receptive by ovariectomy and subsequent hormonal treatment. Sexual behavior parameters were monitored on days 1, 7, 14, and 21 by pairing each male to a receptive female. The extract-treated rats registered significant decrease in mount latency (ML) and intromission latency (IL); nonsignificant increase in mount frequency (MF), intromission frequency (IF), and penile licking (PL); significant decrease in postejaculatory interval (PEI); contrasting effects in ejaculation latency (EL); and mean intromission interval (MII). Both doses of the extract also provoked a significant increase in relative weight of testes, but had no significant effect on the plasma hormonal profile. These findings are similar to those obtained with normal male rats and show that the leaf-methanolic extract of P. arboreus could constitute a potential solution to male sexual impairment.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 2
    Publikationsdatum: 2018
    Beschreibung: Modeling studies using 3D-QSAR and molecular docking methods were performed on a set of 34 hybrids of 4-aminoquinoline derivatives previously studied as effective antimalarial agents of wild type and quadruple mutant Plasmodium falciparum dihydrofolate reductase (DHFR). So, the famous mathematical method multiple linear regression (MLR) was explored to build the QSAR model. The DFT-B3LYP method with the basis set 6-31G was used to calculate the quantum chemical descriptors, chosen to represent the electronic descriptors of molecular structures. On the contrary, the MM2 method was used to calculate lipophilic, geometrical, physicochemical, and steric descriptors. The QSAR model tested with artificial neural network (ANN) method shows high performance towards its predictability. The predicted model was confirmed by three validation methods: leave-one-out (LOO) cross validation, Y-randomization, and validation external. The molecular docking study of three compounds 9, 11, and 26 on both wild and quadruple mutant types of pf-DHFR-TS as the protein target helps to understand more and then predict the binding modes with the binding sites.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 3
    Publikationsdatum: 2018
    Beschreibung: Type 2 diabetes mellitus (T2DM) is emerging as a metabolic epidemic worldwide. Pathologically, dysregulation of many biological pathways precedes hyperglycemia and the clinical diagnosis of T2DM. Changing trajectories along the process of T2DM development necessitates frequent measurement of biomarkers for early identification of at-risk individuals and successful prevention. Increase in circulating inflammatory adipokines has been suggested as predictive of T2DM. Human saliva is an easily accessible biospecimen amenable for painless frequent collection and possesses nearly 50% of serum proteome. In this study, we measured the adipokines resistin, visfatin, TNF-α, and ghrelin as markers for T2DM in unstimulated whole saliva (UWS) using specific assay kits. Resistin and visfatin concentrations were significantly higher in T2DM saliva. Although the concentration of acylated or unacylated ghrelin was lower in diabetic saliva, the decrease was not significant. Since resistin and visfatin are biomarkers integral to T2DM pathology, their salivary assessments may receive clinical acceptance.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 4
    Publikationsdatum: 2018
    Beschreibung: The increasing prevalence of diabetes continues to be a major health issue worldwide. Alteration of mitochondrial electron transport chain is a recognized hallmark of the diabetic-associated decline in liver bioenergetics; however, the molecular events involved are only poorly understood. Moringa oleifera is used for the treatment of diabetes. However, its role on mitochondrial functionality is not yet established. This study was aimed to evaluate the effect of M. oleifera extract on supercomplex formation, ATPase activity, ROS production, GSH levels, lipid peroxidation, and protein carbonylation. The levels of lipid peroxidation and protein carbonylation were increased in diabetic group. However, the levels were decreased in Moringa-treated diabetic rats. Analysis of in-gel activity showed an increase in all complex activities in the diabetic group, but spectrophotometric determinations of complex II and IV activities were unaffected in this treatment. However, we found an oxygen consumption abolition through complex I-III-IV pathway in the diabetic group treated with Moringa. While respiration with succinate feeding into complex II-III-IV was increased in the diabetic group. These findings suggest that hyperglycemia modifies oxygen consumption, supercomplexes formation, and increases ROS levels in mitochondria from the liver of STZ-diabetic rats, whereas M. oleifera may have a protective role against some alterations.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 5
    Publikationsdatum: 2018
    Beschreibung: This work investigated the content of total polyphenolic compounds and flavonoids as well as their toxicity and larvicidal and acetylcholinesterase inhibitory activities. The antioxidant activities of two medicinal Senna species extracts (Senna cana and Senna pendula) were also investigated. The ethanol extract of the leaves of S. cana and the ethanol extract of the branches of S. pendula presented the best performance in the DPPH/FRAP and ABTS/ORAC assays, respectively. For the inhibition of acetylcholinesterase, the hexane extract of the flowers of S. pendula presented the lowest IC50 value among the ethanol extracts of the leaves of S. cana and showed the best performance in some assays. The hexane extract of the leaves of S. pendula and the hexane extract of the branches of S. cana were moderate to Artemia salina Leach. In the quantification of phenols and flavonoids, the ethanol extract of the leaves of S. cana presented the best results. The ethanol extracts of the leaves of S. cana were found to be rich in antioxidants, phenolic compounds, and flavonoids. These results indicate the antioxidant potential of the extracts of Senna species and can be responsible for some of the therapeutic uses of these plants.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 6
    Publikationsdatum: 2018
    Beschreibung: Med6 protein (Med6p) is a hallmark component of evolutionarily conserved Mediator complexes, and the genuine role of Med6p in Mediator functions remains elusive. For the functional analysis of Saccharomyces cerevisiae Med6p (scMed6p), we generated a series of scMed6p mutants harboring a small internal deletion. Genetic analysis of these mutants revealed that three regions (amino acids 33–42 (Δ2), 125–134 (Δ5), and 157–166 (Δ6)) of scMed6p are required for cell viability and are located at highly conserved regions of Med6 homologs. Notably, the Med6p-Δ2 mutant was barely detectable in whole-cell extracts and purified Mediator, suggesting a loss of Mediator association and concurrent rapid degradation. Consistent with this, the recombinant forms of Med6p having these mutations partially (Δ2) restore or fail (Δ5 and Δ6) to restore in vitro transcriptional defects caused by temperature-sensitive med6 mutation. In an artificial recruitment assay, Mediator containing a LexA-fused wild-type Med6p or Med6p-Δ5 was recruited to the lexA operator region with TBP and activated reporter gene expression. However, the recruitment of Mediator containing LexA-Med6p-Δ6 to lexA operator region resulted in neither TBP recruitment nor reporter gene expression. This result demonstrates a pivotal role of Med6p in the postrecruitment function of Mediator, which is essential for transcriptional activation by Mediator.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 7
    Publikationsdatum: 2018
    Beschreibung: Heart diseases, especially acute coronary syndrome (ACS), are among the most severe illnesses that often lead to death. Despite significant advances in the prevention and treatment of ACS, the incidence of the disease and its complications are very serious. The imbalance between pro- and antioxidant systems, the formation of active carbonyl compounds, and the end products of glycation in the blood and tissues are the key moments in the development of heart and neurological disorders leading to a change of behavioral responses. So, the search for antioxidants with cardio- and neuroprotective effects is an urgent task. This study was aimed at evaluating the effects of Corvitin and 2-oxoglutarate on physiological parameters, heart histology, and markers of carbonyl/oxidative stress of rats with pituitrin-isoproterenol-induced myocardial damage (PIMD). Increased sweating, tachycardia, significantly decreased locomotor and exploratory activity, changes of ECG, heart histology, and biochemical changes were observed in the PIMD-group. The administration of Corvitin or 2-OG led to the recovery of locomotor and cognitive activities of the rats, improvement in heart histology, a decrease in the levels of thiobarbituric acid reactive substances, advanced glycated end products, and various changes in the activity of the antioxidant enzymes, 6 days after PIMD. So, Corvitin and exogenous 2-OG show cardio- and neuroprotective effects through the decrease of carbonyl/oxidative stress and regulation of the activity of the antioxidant system.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 8
    Publikationsdatum: 2018
    Beschreibung: Oldenlandia diffusa has been used to treat various cancers. Cytochrome P450, a drug metabolic enzyme, might be influenced by herbal medicine. Currently, the problem that remains is the effective treatment in drug-drug interaction situation. Potential influences of Oldenlandia diffusa were elucidated on the CYP450 activities in rats using a cocktail method. Blood samples were precipitated by acetonitrile. Quantitative determination of target test object was done by ultra-performance liquid chromatography tandem mass spectrometry detection. Influences of oldenlandia diffusa on the activities of five CYP450 subtypes in rats were evaluated by five specific probe drugs (phenacetin for CYP1A2, omeprazole for CYP2C19, tolbutamide for CYP2C9, metoprolol for CYP2D6, and midazolam for CYP3A4) according to the pharmacokinetic parameters changes. No statistically significant difference () in pharmacokinetic behaviors can be observed in the five probe drugs. There is a potential guidance on clinical drug combination with Oldenlandia diffusa. Oldenlandia diffusa in compound preparation showed well security.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 9
    Publikationsdatum: 2018
    Beschreibung: The increasing prevalence of diabetes continues to be a major health issue worldwide. Alteration of mitochondrial electron transport chain is a recognized hallmark of the diabetic-associated decline in liver bioenergetics; however, the molecular events involved are only poorly understood. Moringa oleifera is used for the treatment of diabetes. However, its role on mitochondrial functionality is not yet established. This study was aimed to evaluate the effect of M. oleifera extract on supercomplex formation, ATPase activity, ROS production, GSH levels, lipid peroxidation, and protein carbonylation. The levels of lipid peroxidation and protein carbonylation were increased in diabetic group. However, the levels were decreased in Moringa-treated diabetic rats. Analysis of in-gel activity showed an increase in all complex activities in the diabetic group, but spectrophotometric determinations of complex II and IV activities were unaffected in this treatment. However, we found an oxygen consumption abolition through complex I-III-IV pathway in the diabetic group treated with Moringa. While respiration with succinate feeding into complex II-III-IV was increased in the diabetic group. These findings suggest that hyperglycemia modifies oxygen consumption, supercomplexes formation, and increases ROS levels in mitochondria from the liver of STZ-diabetic rats, whereas M. oleifera may have a protective role against some alterations.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 10
    Publikationsdatum: 2018
    Beschreibung: Med6 protein (Med6p) is a hallmark component of evolutionarily conserved Mediator complexes, and the genuine role of Med6p in Mediator functions remains elusive. For the functional analysis of Saccharomyces cerevisiae Med6p (scMed6p), we generated a series of scMed6p mutants harboring a small internal deletion. Genetic analysis of these mutants revealed that three regions (amino acids 33–42 (Δ2), 125–134 (Δ5), and 157–166 (Δ6)) of scMed6p are required for cell viability and are located at highly conserved regions of Med6 homologs. Notably, the Med6p-Δ2 mutant was barely detectable in whole-cell extracts and purified Mediator, suggesting a loss of Mediator association and concurrent rapid degradation. Consistent with this, the recombinant forms of Med6p having these mutations partially (Δ2) restore or fail (Δ5 and Δ6) to restore in vitro transcriptional defects caused by temperature-sensitive med6 mutation. In an artificial recruitment assay, Mediator containing a LexA-fused wild-type Med6p or Med6p-Δ5 was recruited to the lexA operator region with TBP and activated reporter gene expression. However, the recruitment of Mediator containing LexA-Med6p-Δ6 to lexA operator region resulted in neither TBP recruitment nor reporter gene expression. This result demonstrates a pivotal role of Med6p in the postrecruitment function of Mediator, which is essential for transcriptional activation by Mediator.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 11
    Publikationsdatum: 2018
    Beschreibung: Type 2 diabetes mellitus (T2DM) is emerging as a metabolic epidemic worldwide. Pathologically, dysregulation of many biological pathways precedes hyperglycemia and the clinical diagnosis of T2DM. Changing trajectories along the process of T2DM development necessitates frequent measurement of biomarkers for early identification of at-risk individuals and successful prevention. Increase in circulating inflammatory adipokines has been suggested as predictive of T2DM. Human saliva is an easily accessible biospecimen amenable for painless frequent collection and possesses nearly 50% of serum proteome. In this study, we measured the adipokines resistin, visfatin, TNF-α, and ghrelin as markers for T2DM in unstimulated whole saliva (UWS) using specific assay kits. Resistin and visfatin concentrations were significantly higher in T2DM saliva. Although the concentration of acylated or unacylated ghrelin was lower in diabetic saliva, the decrease was not significant. Since resistin and visfatin are biomarkers integral to T2DM pathology, their salivary assessments may receive clinical acceptance.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 12
    Publikationsdatum: 2018
    Beschreibung: Heart diseases, especially acute coronary syndrome (ACS), are among the most severe illnesses that often lead to death. Despite significant advances in the prevention and treatment of ACS, the incidence of the disease and its complications are very serious. The imbalance between pro- and antioxidant systems, the formation of active carbonyl compounds, and the end products of glycation in the blood and tissues are the key moments in the development of heart and neurological disorders leading to a change of behavioral responses. So, the search for antioxidants with cardio- and neuroprotective effects is an urgent task. This study was aimed at evaluating the effects of Corvitin and 2-oxoglutarate on physiological parameters, heart histology, and markers of carbonyl/oxidative stress of rats with pituitrin-isoproterenol-induced myocardial damage (PIMD). Increased sweating, tachycardia, significantly decreased locomotor and exploratory activity, changes of ECG, heart histology, and biochemical changes were observed in the PIMD-group. The administration of Corvitin or 2-OG led to the recovery of locomotor and cognitive activities of the rats, improvement in heart histology, a decrease in the levels of thiobarbituric acid reactive substances, advanced glycated end products, and various changes in the activity of the antioxidant enzymes, 6 days after PIMD. So, Corvitin and exogenous 2-OG show cardio- and neuroprotective effects through the decrease of carbonyl/oxidative stress and regulation of the activity of the antioxidant system.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 13
    Publikationsdatum: 2018
    Beschreibung: This work investigated the content of total polyphenolic compounds and flavonoids as well as their toxicity and larvicidal and acetylcholinesterase inhibitory activities. The antioxidant activities of two medicinal Senna species extracts (Senna cana and Senna pendula) were also investigated. The ethanol extract of the leaves of S. cana and the ethanol extract of the branches of S. pendula presented the best performance in the DPPH/FRAP and ABTS/ORAC assays, respectively. For the inhibition of acetylcholinesterase, the hexane extract of the flowers of S. pendula presented the lowest IC50 value among the ethanol extracts of the leaves of S. cana and showed the best performance in some assays. The hexane extract of the leaves of S. pendula and the hexane extract of the branches of S. cana were moderate to Artemia salina Leach. In the quantification of phenols and flavonoids, the ethanol extract of the leaves of S. cana presented the best results. The ethanol extracts of the leaves of S. cana were found to be rich in antioxidants, phenolic compounds, and flavonoids. These results indicate the antioxidant potential of the extracts of Senna species and can be responsible for some of the therapeutic uses of these plants.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 14
    Publikationsdatum: 2018
    Beschreibung: The people of the Bayangi tribe (Manyu Division) of Cameroon have used the leaves of Pseudopanax arboreus (Araliaceae) traditionally for decades as an aphrodisiac. In order to scientifically investigate this folk claim, we evaluated the effects of the leaf-aqueous extract of P. arboreus on the sexual behavior of normal male rats. The present study was designed to assess the effects of the leaf-methanolic extract of P. arboreus on amitriptyline-induced sexual dysfunction in male rats. Sexually impaired male rats were randomly divided into 4 groups of 8 rats each. Group 1 received 10 ml/kg distilled water, while group 2 was given 6 mg/kg Viagra. Groups 3 and 4 received 46.5 and 93 mg/kg of the leaf-methanolic extract, respectively. Female rats were made receptive by ovariectomy and subsequent hormonal treatment. Sexual behavior parameters were monitored on days 1, 7, 14, and 21 by pairing each male to a receptive female. The extract-treated rats registered significant decrease in mount latency (ML) and intromission latency (IL); nonsignificant increase in mount frequency (MF), intromission frequency (IF), and penile licking (PL); significant decrease in postejaculatory interval (PEI); contrasting effects in ejaculation latency (EL); and mean intromission interval (MII). Both doses of the extract also provoked a significant increase in relative weight of testes, but had no significant effect on the plasma hormonal profile. These findings are similar to those obtained with normal male rats and show that the leaf-methanolic extract of P. arboreus could constitute a potential solution to male sexual impairment.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 15
    Publikationsdatum: 2018
    Beschreibung: Oldenlandia diffusa has been used to treat various cancers. Cytochrome P450, a drug metabolic enzyme, might be influenced by herbal medicine. Currently, the problem that remains is the effective treatment in drug-drug interaction situation. Potential influences of Oldenlandia diffusa were elucidated on the CYP450 activities in rats using a cocktail method. Blood samples were precipitated by acetonitrile. Quantitative determination of target test object was done by ultra-performance liquid chromatography tandem mass spectrometry detection. Influences of oldenlandia diffusa on the activities of five CYP450 subtypes in rats were evaluated by five specific probe drugs (phenacetin for CYP1A2, omeprazole for CYP2C19, tolbutamide for CYP2C9, metoprolol for CYP2D6, and midazolam for CYP3A4) according to the pharmacokinetic parameters changes. No statistically significant difference () in pharmacokinetic behaviors can be observed in the five probe drugs. There is a potential guidance on clinical drug combination with Oldenlandia diffusa. Oldenlandia diffusa in compound preparation showed well security.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 16
    Publikationsdatum: 2018
    Beschreibung: Modeling studies using 3D-QSAR and molecular docking methods were performed on a set of 34 hybrids of 4-aminoquinoline derivatives previously studied as effective antimalarial agents of wild type and quadruple mutant Plasmodium falciparum dihydrofolate reductase (DHFR). So, the famous mathematical method multiple linear regression (MLR) was explored to build the QSAR model. The DFT-B3LYP method with the basis set 6-31G was used to calculate the quantum chemical descriptors, chosen to represent the electronic descriptors of molecular structures. On the contrary, the MM2 method was used to calculate lipophilic, geometrical, physicochemical, and steric descriptors. The QSAR model tested with artificial neural network (ANN) method shows high performance towards its predictability. The predicted model was confirmed by three validation methods: leave-one-out (LOO) cross validation, Y-randomization, and validation external. The molecular docking study of three compounds 9, 11, and 26 on both wild and quadruple mutant types of pf-DHFR-TS as the protein target helps to understand more and then predict the binding modes with the binding sites.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 17
    Publikationsdatum: 2018-09-03
    Beschreibung: Heart diseases, especially acute coronary syndrome (ACS), are among the most severe illnesses that often lead to death. Despite significant advances in the prevention and treatment of ACS, the incidence of the disease and its complications are very serious. The imbalance between pro- and antioxidant systems, the formation of active carbonyl compounds, and the end products of glycation in the blood and tissues are the key moments in the development of heart and neurological disorders leading to a change of behavioral responses. So, the search for antioxidants with cardio- and neuroprotective effects is an urgent task. This study was aimed at evaluating the effects of Corvitin and 2-oxoglutarate on physiological parameters, heart histology, and markers of carbonyl/oxidative stress of rats with pituitrin-isoproterenol-induced myocardial damage (PIMD). Increased sweating, tachycardia, significantly decreased locomotor and exploratory activity, changes of ECG, heart histology, and biochemical changes were observed in the PIMD-group. The administration of Corvitin or 2-OG led to the recovery of locomotor and cognitive activities of the rats, improvement in heart histology, a decrease in the levels of thiobarbituric acid reactive substances, advanced glycated end products, and various changes in the activity of the antioxidant enzymes, 6 days after PIMD. So, Corvitin and exogenous 2-OG show cardio- and neuroprotective effects through the decrease of carbonyl/oxidative stress and regulation of the activity of the antioxidant system.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 18
    Publikationsdatum: 2018-01-01
    Beschreibung: Oldenlandia diffusa has been used to treat various cancers. Cytochrome P450, a drug metabolic enzyme, might be influenced by herbal medicine. Currently, the problem that remains is the effective treatment in drug-drug interaction situation. Potential influences of Oldenlandia diffusa were elucidated on the CYP450 activities in rats using a cocktail method. Blood samples were precipitated by acetonitrile. Quantitative determination of target test object was done by ultra-performance liquid chromatography tandem mass spectrometry detection. Influences of oldenlandia diffusa on the activities of five CYP450 subtypes in rats were evaluated by five specific probe drugs (phenacetin for CYP1A2, omeprazole for CYP2C19, tolbutamide for CYP2C9, metoprolol for CYP2D6, and midazolam for CYP3A4) according to the pharmacokinetic parameters changes. No statistically significant difference (P〉0.05) in pharmacokinetic behaviors can be observed in the five probe drugs. There is a potential guidance on clinical drug combination with Oldenlandia diffusa. Oldenlandia diffusa in compound preparation showed well security.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 19
    Publikationsdatum: 2018-11-15
    Beschreibung: The people of the Bayangi tribe (Manyu Division) of Cameroon have used the leaves of Pseudopanax arboreus (Araliaceae) traditionally for decades as an aphrodisiac. In order to scientifically investigate this folk claim, we evaluated the effects of the leaf-aqueous extract of P. arboreus on the sexual behavior of normal male rats. The present study was designed to assess the effects of the leaf-methanolic extract of P. arboreus on amitriptyline-induced sexual dysfunction in male rats. Sexually impaired male rats were randomly divided into 4 groups of 8 rats each. Group 1 received 10 ml/kg distilled water, while group 2 was given 6 mg/kg Viagra. Groups 3 and 4 received 46.5 and 93 mg/kg of the leaf-methanolic extract, respectively. Female rats were made receptive by ovariectomy and subsequent hormonal treatment. Sexual behavior parameters were monitored on days 1, 7, 14, and 21 by pairing each male to a receptive female. The extract-treated rats registered significant decrease in mount latency (ML) and intromission latency (IL); nonsignificant increase in mount frequency (MF), intromission frequency (IF), and penile licking (PL); significant decrease in postejaculatory interval (PEI); contrasting effects in ejaculation latency (EL); and mean intromission interval (MII). Both doses of the extract also provoked a significant increase in relative weight of testes, but had no significant effect on the plasma hormonal profile. These findings are similar to those obtained with normal male rats and show that the leaf-methanolic extract of P. arboreus could constitute a potential solution to male sexual impairment.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 20
    Publikationsdatum: 2018-01-01
    Beschreibung: This work investigated the content of total polyphenolic compounds and flavonoids as well as their toxicity and larvicidal and acetylcholinesterase inhibitory activities. The antioxidant activities of two medicinal Senna species extracts (Senna cana and Senna pendula) were also investigated. The ethanol extract of the leaves of S. cana and the ethanol extract of the branches of S. pendula presented the best performance in the DPPH/FRAP and ABTS/ORAC assays, respectively. For the inhibition of acetylcholinesterase, the hexane extract of the flowers of S. pendula presented the lowest IC50 value among the ethanol extracts of the leaves of S. cana and showed the best performance in some assays. The hexane extract of the leaves of S. pendula and the hexane extract of the branches of S. cana were moderate to Artemia salina Leach. In the quantification of phenols and flavonoids, the ethanol extract of the leaves of S. cana presented the best results. The ethanol extracts of the leaves of S. cana were found to be rich in antioxidants, phenolic compounds, and flavonoids. These results indicate the antioxidant potential of the extracts of Senna species and can be responsible for some of the therapeutic uses of these plants.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
    BibTip Andere fanden auch interessant ...
  • 21
    Publikationsdatum: 2018-06-24
    Beschreibung: Modeling studies using 3D-QSAR and molecular docking methods were performed on a set of 34 hybrids of 4-aminoquinoline derivatives previously studied as effective antimalarial agents of wild type and quadruple mutant Plasmodium falciparum dihydrofolate reductase (DHFR). So, the famous mathematical method multiple linear regression (MLR) was explored to build the QSAR model. The DFT-B3LYP method with the basis set 6-31G was used to calculate the quantum chemical descriptors, chosen to represent the electronic descriptors of molecular structures. On the contrary, the MM2 method was used to calculate lipophilic, geometrical, physicochemical, and steric descriptors. The QSAR model tested with artificial neural network (ANN) method shows high performance towards its predictability. The predicted model was confirmed by three validation methods: leave-one-out (LOO) cross validation, Y-randomization, and validation external. The molecular docking study of three compounds 9, 11, and 26 on both wild and quadruple mutant types of pf-DHFR-TS as the protein target helps to understand more and then predict the binding modes with the binding sites.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
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  • 22
    Publikationsdatum: 2018-01-01
    Beschreibung: Med6 protein (Med6p) is a hallmark component of evolutionarily conserved Mediator complexes, and the genuine role of Med6p in Mediator functions remains elusive. For the functional analysis ofSaccharomyces cerevisiaeMed6p (scMed6p), we generated a series of scMed6p mutants harboring a small internal deletion. Genetic analysis of these mutants revealed that three regions (amino acids 33–42 (Δ2), 125–134 (Δ5), and 157–166 (Δ6)) of scMed6p are required for cell viability and are located at highly conserved regions of Med6 homologs. Notably, the Med6p-Δ2 mutant was barely detectable in whole-cell extracts and purified Mediator, suggesting a loss of Mediator association and concurrent rapid degradation. Consistent with this, the recombinant forms of Med6p having these mutations partially (Δ2) restore or fail (Δ5 and Δ6) to restore in vitro transcriptional defects caused by temperature-sensitivemed6mutation. In an artificial recruitment assay, Mediator containing a LexA-fused wild-type Med6p or Med6p-Δ5 was recruited to thelexAoperator region with TBP and activated reporter gene expression. However, the recruitment of Mediator containing LexA-Med6p-Δ6 tolexAoperator region resulted in neither TBP recruitment nor reporter gene expression. This result demonstrates a pivotal role of Med6p in the postrecruitment function of Mediator, which is essential for transcriptional activation by Mediator.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
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  • 23
    Publikationsdatum: 2018-01-01
    Beschreibung: The increasing prevalence of diabetes continues to be a major health issue worldwide. Alteration of mitochondrial electron transport chain is a recognized hallmark of the diabetic-associated decline in liver bioenergetics; however, the molecular events involved are only poorly understood. Moringa oleifera is used for the treatment of diabetes. However, its role on mitochondrial functionality is not yet established. This study was aimed to evaluate the effect of M. oleifera extract on supercomplex formation, ATPase activity, ROS production, GSH levels, lipid peroxidation, and protein carbonylation. The levels of lipid peroxidation and protein carbonylation were increased in diabetic group. However, the levels were decreased in Moringa-treated diabetic rats. Analysis of in-gel activity showed an increase in all complex activities in the diabetic group, but spectrophotometric determinations of complex II and IV activities were unaffected in this treatment. However, we found an oxygen consumption abolition through complex I-III-IV pathway in the diabetic group treated with Moringa. While respiration with succinate feeding into complex II-III-IV was increased in the diabetic group. These findings suggest that hyperglycemia modifies oxygen consumption, supercomplexes formation, and increases ROS levels in mitochondria from the liver of STZ-diabetic rats, whereas M. oleifera may have a protective role against some alterations.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
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  • 24
    Publikationsdatum: 2018-01-01
    Beschreibung: Type 2 diabetes mellitus (T2DM) is emerging as a metabolic epidemic worldwide. Pathologically, dysregulation of many biological pathways precedes hyperglycemia and the clinical diagnosis of T2DM. Changing trajectories along the process of T2DM development necessitates frequent measurement of biomarkers for early identification of at-risk individuals and successful prevention. Increase in circulating inflammatory adipokines has been suggested as predictive of T2DM. Human saliva is an easily accessible biospecimen amenable for painless frequent collection and possesses nearly 50% of serum proteome. In this study, we measured the adipokines resistin, visfatin, TNF-α, and ghrelin as markers for T2DM in unstimulated whole saliva (UWS) using specific assay kits. Resistin and visfatin concentrations were significantly higher in T2DM saliva. Although the concentration of acylated or unacylated ghrelin was lower in diabetic saliva, the decrease was not significant. Since resistin and visfatin are biomarkers integral to T2DM pathology, their salivary assessments may receive clinical acceptance.
    Print ISSN: 2090-2247
    Digitale ISSN: 2090-2255
    Thema: Biologie , Chemie und Pharmazie
    Publiziert von Hindawi
    Standort Signatur Erwartet Verfügbarkeit
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