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Molecules, Volume 21, Issue 4 (April 2016)

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Cover Story (view full-size image) With its epidemic proportion and an attrition rate approaching 100%, Alzheimer’s disease (AD) is an [...] Read more.
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Open AccessCorrection Correction: Popp, J., et al. Biofuels and Their Co-Products as Livestock Feed: Global Economic and Environmental Implications. Molecules 2016, 21, 285.
Molecules 2016, 21(4), 546; https://doi.org/10.3390/molecules21040546
Received: 15 April 2016 / Revised: 15 April 2016 / Accepted: 21 April 2016 / Published: 23 April 2016
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Abstract
The authors wish to make the following correction to their paper[1].[...] Full article
(This article belongs to the Section Green Chemistry)
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Open AccessReview Selenium in Cattle: A Review
Molecules 2016, 21(4), 545; https://doi.org/10.3390/molecules21040545
Received: 2 March 2016 / Revised: 8 April 2016 / Accepted: 19 April 2016 / Published: 23 April 2016
Cited by 12 | PDF Full-text (242 KB) | HTML Full-text | XML Full-text
Abstract
This review article examines the role of selenium (Se) and the effects of Se supplementation especially in the bovine species. Selenium is an important trace element in cattle. Some of its roles include the participation in the antioxidant defense the cattle farms. The
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This review article examines the role of selenium (Se) and the effects of Se supplementation especially in the bovine species. Selenium is an important trace element in cattle. Some of its roles include the participation in the antioxidant defense the cattle farms. The nutritional requirements of Se in cattle are estimated at 100 μg/kg DM (dry matter) for beef cattle and at 300 μg/kg DM for dairy cows. The rations high in fermentable carbohydrates, nitrates, sulfates, calcium or hydrogen cyanide negatively influence the organism’s use of the selenium contained in the diet. The Se supplementation may reduce the incidence of metritis and ovarian cysts during the postpartum period. The increase in fertility when adding Se is attributed to the reduction of the embryonic death during the first month of gestation. A use of organic Se in feed would provide a better transfer of Se in calves relative to mineral Se supplementation. The addition of Se yeasts in the foodstuffs of cows significantly increases the Se content and the percentage of polyunsaturated fatty acids (PUFA) in milk compared to the addition of sodium selenite. The enzyme 5-iodothyronine deiodinase is a seleno-dependent selenoprotein. It is one of the last proteins to be affected in the event of Se deficiency. This delay in response could explain the fact that several studies did not show the effect of Se supplementation on growth and weight gain of calves. Enrichment of Se in the diet did not significantly affect the slaughter weight and carcass yield of bulls. The impact and results of Se supplementation in cattle depend on physiological stage, Se status of animals, type and content of Se and types of Se administration. Further studies in Se supplementation should investigate the speciation of Se in food and yeasts, as well as understanding their metabolism and absorption. This constitute a path to exploit in order to explain certain different effects of Se. Full article
(This article belongs to the Section Molecular Diversity)
Open AccessArticle Crystallization of Esomeprazole Magnesium Water/Butanol Solvate
Molecules 2016, 21(4), 544; https://doi.org/10.3390/molecules21040544
Received: 15 March 2016 / Revised: 8 April 2016 / Accepted: 21 April 2016 / Published: 23 April 2016
Cited by 1 | PDF Full-text (3082 KB) | HTML Full-text | XML Full-text
Abstract
The molecular structure of esomeprazole magnesium derivative in the solid-state is reported for the first time, along with a simplified crystallization pathway. The structure was determined using the single crystal X-ray diffraction technique to reveal the bonding relationships between esomeprazole heteroatoms and magnesium.
[...] Read more.
The molecular structure of esomeprazole magnesium derivative in the solid-state is reported for the first time, along with a simplified crystallization pathway. The structure was determined using the single crystal X-ray diffraction technique to reveal the bonding relationships between esomeprazole heteroatoms and magnesium. The esomeprazole crystallization process was carried out in 1-butanol and water was utilized as anti-solvent. The product proved to be esomeprazole magnesium tetrahydrate with two 1-butanol molecules that crystallized in P63 space group, in a hexagonal unit cell. Complete characterization of a sample after drying was conducted by the use of powder X-ray diffraction (PXRD), 1H-nuclear magnetic resonance (NMR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), infrared spectroscopy (IR), and dynamic vapor sorption (DVS). Investigation by 1H-NMR and TGA has shown that the solvent content in the dried sample consists of two water molecules and 0.3 butanol molecules per esomeprazole magnesium molecule. This is different from the single crystal X-ray diffraction results and can be attributed to the loss of some water and 1-butanol molecules stabilized by intermolecular interactions. The title compound, after drying, is a true solvate in terms of water; conversely, 1-butanol fills the voids of the crystal lattice in non-stoichiometric amounts. Full article
(This article belongs to the Special Issue Crystallization of Pharmaceuticals)
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Open AccessArticle Highly Efficient Reproducible Perovskite Solar Cells Prepared by Low-Temperature Processing
Molecules 2016, 21(4), 542; https://doi.org/10.3390/molecules21040542
Received: 4 April 2016 / Revised: 19 April 2016 / Accepted: 21 April 2016 / Published: 23 April 2016
Cited by 9 | PDF Full-text (2036 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
In this work, we describe the role of the different layers in perovskite solar cells to achieve reproducible, ~16% efficient perovskite solar cells. We used a planar device architecture with PEDOT:PSS on the bottom, followed by the perovskite layer and an evaporated C
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In this work, we describe the role of the different layers in perovskite solar cells to achieve reproducible, ~16% efficient perovskite solar cells. We used a planar device architecture with PEDOT:PSS on the bottom, followed by the perovskite layer and an evaporated C60 layer before deposition of the top electrode. No high temperature annealing step is needed, which also allows processing on flexible plastic substrates. Only the optimization of all of these layers leads to highly efficient and reproducible results. In this work, we describe the effects of different processing conditions, especially the influence of the C60 top layer on the device performance. Full article
(This article belongs to the Special Issue Perovskite Solar Cells)
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Open AccessArticle 3,5,6,7,8,3′,4′-Heptamethoxyflavone, a Citrus Flavonoid, Ameliorates Corticosterone-Induced Depression-like Behavior and Restores Brain-Derived Neurotrophic Factor Expression, Neurogenesis, and Neuroplasticity in the Hippocampus
Molecules 2016, 21(4), 541; https://doi.org/10.3390/molecules21040541
Received: 2 March 2016 / Revised: 20 April 2016 / Accepted: 21 April 2016 / Published: 23 April 2016
Cited by 13 | PDF Full-text (2275 KB) | HTML Full-text | XML Full-text
Abstract
We previously reported that the citrus flavonoid 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF) increased the expression of brain-derived neurotrophic factor (BDNF) in the hippocampus of a transient global ischemia mouse model. Since the BDNF hypothesis of depression postulates that a reduction in BDNF is directly involved in
[...] Read more.
We previously reported that the citrus flavonoid 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF) increased the expression of brain-derived neurotrophic factor (BDNF) in the hippocampus of a transient global ischemia mouse model. Since the BDNF hypothesis of depression postulates that a reduction in BDNF is directly involved in the pathophysiology of depression, we evaluated the anti-depressive effects of HMF in mice with subcutaneously administered corticosterone at a dose of 20 mg/kg/day for 25 days. We demonstrated that the HMF treatment ameliorated (1) corticosterone-induced body weight loss, (2) corticosterone-induced depression-like behavior, and (3) corticosterone-induced reductions in BDNF production in the hippocampus. We also showed that the HMF treatment restored (4) corticosterone-induced reductions in neurogenesis in the dentate gyrus subgranular zone and (5) corticosterone-induced reductions in the expression levels of phosphorylated calcium-calmodulin-dependent protein kinase II and extracellular signal-regulated kinase1/2. These results suggest that HMF exerts its effects as an anti-depressant drug by inducing the expression of BDNF. Full article
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Open AccessReview Bifunctional Phosphorus Dendrimers and Their Properties
Molecules 2016, 21(4), 538; https://doi.org/10.3390/molecules21040538
Received: 23 March 2016 / Revised: 15 April 2016 / Accepted: 19 April 2016 / Published: 23 April 2016
Cited by 10 | PDF Full-text (4082 KB) | HTML Full-text | XML Full-text
Abstract
Dendrimers are hyperbranched and monodisperse macromolecules, generally considered as a special class of polymers, but synthesized step-by-step. Most dendrimers have a uniform structure, with a single type of terminal function. However, it is often desirable to have at least two different functional groups.
[...] Read more.
Dendrimers are hyperbranched and monodisperse macromolecules, generally considered as a special class of polymers, but synthesized step-by-step. Most dendrimers have a uniform structure, with a single type of terminal function. However, it is often desirable to have at least two different functional groups. This review will discuss the case of bifunctional phosphorus-containing dendrimers, and the consequences for their properties. Besides the terminal functions, dendritic structures may have also a function at the core, or linked off-center to the core, or at the core of dendrons (dendritic wedges). Association of two dendrons having different terminal functions leads to Janus dendrimers (two faces). The internal structure can also possess functional groups on one layer, or linked to one layer, or on several layers. Finally, there are several ways to have two types of terminal functions, besides the case of Janus dendrimers: either each terminal function bears two functions sequentially, or two different functions are linked to each terminal branching point. Examples of each type of structure will be given in this review, as well as practical uses of such sophisticated structures in the fields of fluorescence, catalysis, nanomaterials and biology. Full article
(This article belongs to the Special Issue Functional Dendrimers)
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Open AccessArticle Breast Cancer Stem Cell Culture and Enrichment Using Poly(ε-Caprolactone) Scaffolds
Molecules 2016, 21(4), 537; https://doi.org/10.3390/molecules21040537
Received: 14 March 2016 / Revised: 20 April 2016 / Accepted: 20 April 2016 / Published: 23 April 2016
Cited by 8 | PDF Full-text (5708 KB) | HTML Full-text | XML Full-text
Abstract
The cancer stem cell (CSC) population displays self-renewal capabilities, resistance to conventional therapies, and a tendency to post-treatment recurrence. Increasing knowledge about CSCs’ phenotype and functions is needed to investigate new therapeutic strategies against the CSC population. Here, poly(ε-caprolactone) (PCL), a biocompatible polymer
[...] Read more.
The cancer stem cell (CSC) population displays self-renewal capabilities, resistance to conventional therapies, and a tendency to post-treatment recurrence. Increasing knowledge about CSCs’ phenotype and functions is needed to investigate new therapeutic strategies against the CSC population. Here, poly(ε-caprolactone) (PCL), a biocompatible polymer free of toxic dye, has been used to fabricate scaffolds, solid structures suitable for 3D cancer cell culture. It has been reported that scaffold cell culture enhances the CSCs population. A RepRap BCN3D+ printer and 3 mm PCL wire were used to fabricate circular scaffolds. PCL design and fabrication parameters were first determined and then optimized considering several measurable variables of the resulting scaffolds. MCF7 breast carcinoma cell line was used to assess scaffolds adequacy for 3D cell culture. To evaluate CSC enrichment, the Mammosphere Forming Index (MFI) was performed in 2D and 3D MCF7 cultures. Results showed that the 60° scaffolds were more suitable for 3D culture than the 45° and 90° ones. Moreover, 3D culture experiments, in adherent and non-adherent conditions, showed a significant increase in MFI compared to 2D cultures (control). Thus, 3D cell culture with PCL scaffolds could be useful to improve cancer cell culture and enrich the CSCs population. Full article
(This article belongs to the Special Issue Biomaterials and Bioprinting)
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Open AccessEditorial Special Issue: Chemoinformatics
Molecules 2016, 21(4), 535; https://doi.org/10.3390/molecules21040535
Received: 19 April 2016 / Accepted: 20 April 2016 / Published: 22 April 2016
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Abstract
Chemoinformatics techniques were originally developed for the construction and searching of large archives of chemical structures but they were soon applied to problems in drug discovery and are now playing an increasingly important role in many additional areas of chemistry. This Special Issue
[...] Read more.
Chemoinformatics techniques were originally developed for the construction and searching of large archives of chemical structures but they were soon applied to problems in drug discovery and are now playing an increasingly important role in many additional areas of chemistry. This Special Issue contains seven original research articles and four review articles that provide an introduction to several aspects of this rapidly developing field. Full article
(This article belongs to the Special Issue Chemoinformatics)
Open AccessArticle Peruvoside, a Cardiac Glycoside, Induces Primitive Myeloid Leukemia Cell Death
Molecules 2016, 21(4), 534; https://doi.org/10.3390/molecules21040534
Received: 24 February 2016 / Revised: 15 April 2016 / Accepted: 20 April 2016 / Published: 22 April 2016
Cited by 3 | PDF Full-text (2694 KB) | HTML Full-text | XML Full-text
Abstract
Despite the available chemotherapy and treatment, leukemia remains a difficult disease to cure due to frequent relapses after treatment. Among the heterogeneous leukemic cells, a rare population referred as the leukemic stem cell (LSC), is thought to be responsible for relapses and drug
[...] Read more.
Despite the available chemotherapy and treatment, leukemia remains a difficult disease to cure due to frequent relapses after treatment. Among the heterogeneous leukemic cells, a rare population referred as the leukemic stem cell (LSC), is thought to be responsible for relapses and drug resistance. Cardiac glycosides (CGs) have been used in treating heart failure despite its toxicity. Recently, increasing evidence has demonstrated its new usage as a potential anti-cancer drug. Ouabain, one of the CGs, specifically targeted CD34+CD38 leukemic stem-like cells, but not the more mature CD34+CD38+ leukemic cells, making this type of compounds a potential treatment for leukemia. In search of other potential anti-leukemia CGs, we found that Peruvoside, a less studied CG, is more effective than Ouabain and Digitoxin at inducing cell death in primitive myeloid leukemia cells without obvious cytotoxicity on normal blood cells. Similar to Ouabain and Digitoxin, Peruvoside also caused cell cycle arrest at G2/M stage. It up-regulates CDKN1A expression and activated the cleavage of Caspase 3, 8 and PARP, resulting in apoptosis. Thus, Peruvoside showed potent anti-leukemia effect, which may serve as a new anti-leukemia agent in the future. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Repellent Activity of the Essential Oil from the Heartwood of Pilgerodendron uviferum (D. Don) Florin against Aegorhinus superciliosus (Coleoptera: Curculionidae)
Molecules 2016, 21(4), 533; https://doi.org/10.3390/molecules21040533
Received: 16 March 2016 / Revised: 14 April 2016 / Accepted: 20 April 2016 / Published: 22 April 2016
Cited by 2 | PDF Full-text (390 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The weevil Aegorhinus superciliosus Guérin (Coleoptera: Curculionidae), which is endemic to Central-Southern Chile and Argentina, is one of the major berry pests in Chile and the most important pest in the La Araucanía Region (38°44′9″S, 72°35′25″W). Due to the poor effectiveness and problems
[...] Read more.
The weevil Aegorhinus superciliosus Guérin (Coleoptera: Curculionidae), which is endemic to Central-Southern Chile and Argentina, is one of the major berry pests in Chile and the most important pest in the La Araucanía Region (38°44′9″S, 72°35′25″W). Due to the poor effectiveness and problems surrounding the implementation of the traditional control methods using organophosphate and carbamate insecticides, new strategies for controlling this pest are needed. In this communication, we evaluated the behavioral responses of male and female A. superciliosus to volatile compounds released from the essential oil (EO) obtained from the heartwood of Pilgerodendron uviferum (D. Don) Florin using olfactometric bioassays. The composition of the EO was analyzed using gas chromatography (GC) and gas chromatography/mass spectrometry (GC/MS). According to these analyses, δ-cadinol (24.16%), cubenol (22.64%), 15-copaenol (15.46%) and δ-cadinene (10.81%) were the principal components of the EO. The Pilgerodendron uviferum EO, which is almost exclusively composed of sesquiterpenes (99.5%), exhibited a repellent effect against A. superciliosus adults, regardless of the sex or concentration used (56.6 mg/cm3 and 1.58 × 10−2 mg/cm3). The EO has low volatility and greater persistence than the EOs composed of monoterpenes and is considered a good model in the search for raspberry weevil repellents. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Identification of Subnanometric Ag Species, Their Interaction with Supports and Role in Catalytic CO Oxidation
Molecules 2016, 21(4), 532; https://doi.org/10.3390/molecules21040532
Received: 6 February 2016 / Revised: 7 April 2016 / Accepted: 15 April 2016 / Published: 22 April 2016
Cited by 7 | PDF Full-text (4856 KB) | HTML Full-text | XML Full-text
Abstract
The nature and size of the real active species of nanoparticulated metal supported catalysts is still an unresolved question. The technique of choice to measure particle sizes at the nanoscale, HRTEM, has a practical limit of 1 nm. This work is aimed to
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The nature and size of the real active species of nanoparticulated metal supported catalysts is still an unresolved question. The technique of choice to measure particle sizes at the nanoscale, HRTEM, has a practical limit of 1 nm. This work is aimed to identify the catalytic role of subnanometer species and methods to detect and characterize them. In this frame, we investigated the sensitivity to redox pretreatments of Ag/Fe/TiO2, Ag/Mg/TiO2 and Ag/Ce/TiO2 catalysts in CO oxidation. The joint application of HRTEM, SR-XRD, DRS, XPS, EXAFS and XANES methods indicated that most of the silver in all samples is in the form of Ag species with size <1 nm. The differences in catalytic properties and sensitivity to pretreatments, observed for the studied Ag catalysts, could not be explained taking into account only the Ag particles whose size distribution is measured by HRTEM, but may be explained by the presence of the subnanometer Ag species, undetectable by HRTEM, and their interaction with supports. This result highlights their role as active species and the need to take them into account to understand integrally the catalysis by supported nanometals. Full article
(This article belongs to the Special Issue Coinage Metal (Copper, Silver, and Gold) Catalysis)
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Open AccessArticle Volatile Organic Compounds Emissions from Luculia pinceana Flower and Its Changes at Different Stages of Flower Development
Molecules 2016, 21(4), 531; https://doi.org/10.3390/molecules21040531
Received: 22 February 2016 / Revised: 15 April 2016 / Accepted: 18 April 2016 / Published: 22 April 2016
Cited by 3 | PDF Full-text (1187 KB) | HTML Full-text | XML Full-text
Abstract
Luculia plants are famed ornamental plants with sweetly fragrant flowers, of which L. pinceana Hooker, found primarily in Yunnan Province, China, has the widest distribution. Solid phase microextraction-gas chromatography-mass spectrometry (SPME-GC-MS) was employed to identify the volatile organic compounds (VOCs) emitted from different
[...] Read more.
Luculia plants are famed ornamental plants with sweetly fragrant flowers, of which L. pinceana Hooker, found primarily in Yunnan Province, China, has the widest distribution. Solid phase microextraction-gas chromatography-mass spectrometry (SPME-GC-MS) was employed to identify the volatile organic compounds (VOCs) emitted from different flower development stages of L. pinceana for the evaluation of floral volatile polymorphism. Peak areas were normalized as percentages and used to determine the relative amounts of the volatiles. The results showed that a total of 39 compounds were identified at four different stages of L. pinceana flower development, including 26 at the bud stage, 26 at the initial-flowering stage, 32 at the full-flowering stage, and 32 at the end-flowering stage. The most abundant compound was paeonol (51%–83%) followed by (E,E)-α-farnesene, cyclosativene, and δ-cadinene. All these volatile compounds create the unique fragrance of L. pinceana flower. Floral scent emission offered tendency of ascending first and descending in succession, meeting its peak level at the initial-flowering stage. The richest diversity of floral volatile was detected at the third and later periods of flower development. Principal component analysis (PCA) indicated that the composition and its relative content of floral scent differed throughout the whole flower development. The result has important implications for future floral fragrance breeding of Luculia. L. pinceana would be adequate for a beneficial houseplant and has a promising prospect for development as essential oil besides for a fragrant ornamental owing to the main compounds of floral scent with many medicinal properties. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Enantioselective Separation of 4,8-DHT and Phytotoxicity of the Enantiomers on Various Plant Species
Molecules 2016, 21(4), 528; https://doi.org/10.3390/molecules21040528
Received: 23 March 2016 / Revised: 18 April 2016 / Accepted: 19 April 2016 / Published: 22 April 2016
Cited by 2 | PDF Full-text (2560 KB) | HTML Full-text | XML Full-text
Abstract
As a candidate for bioherbicide, 4,8-dihydroxy-1-tetralone (4,8-DHT) was isolated from Caryospora callicarpa epicarp and its two enantiomers, S-(+)-isosclerone and R-(−)-regiolone, were separated by chiral high-performance liquid chromatography (HPLC) on a Chiralcel OD column with chiral stationary phase (CSP)-coated cellulose-tris(3,5-dimethylphenylcarbamate). Then, the
[...] Read more.
As a candidate for bioherbicide, 4,8-dihydroxy-1-tetralone (4,8-DHT) was isolated from Caryospora callicarpa epicarp and its two enantiomers, S-(+)-isosclerone and R-(−)-regiolone, were separated by chiral high-performance liquid chromatography (HPLC) on a Chiralcel OD column with chiral stationary phase (CSP)-coated cellulose-tris(3,5-dimethylphenylcarbamate). Then, the phytotoxicity of 4,8-DHT and its enantiomers toward the seeds germination and seedling growth of the five tested plant species, including lettuce (Latuca sativa), radish (Raphanus sativus), cucumber (Cucumis sativus), onion (Allium cepa), and wheat (Triticum aestivum), were investigated and the results indicated a hormesis at low concentration of 4,8-DHT and its enantiomers, but a retardant effect at high concentration. Between the two enantiomers of 4,8-DHT, the S-(+)-isosclerone was more toxic to seeds germination and seedling growth of the five tested plant species than the R-(−)-regiolone, and also the phytotoxicity of S-(+)-isosclerone varied with different plants. For example, S-(+)-isosclerone was the most active to seedling growth of lettuce, indicating that S-(+)-isosclerone had specific effects on different organisms. Thus, all of the chirality and concentration of 4,8-DHT, as well as the affected plant species, need to be taken into consideration in the development and utilization of 4,8-DHT. Full article
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Open AccessArticle The Effects of Topical Application of Polycal (a 2:98 (g/g) Mixture of Polycan and Calcium Gluconate) on Experimental Periodontitis and Alveolar Bone Loss in Rats
Molecules 2016, 21(4), 527; https://doi.org/10.3390/molecules21040527
Received: 29 February 2016 / Revised: 8 April 2016 / Accepted: 18 April 2016 / Published: 22 April 2016
Cited by 3 | PDF Full-text (7781 KB) | HTML Full-text | XML Full-text
Abstract
The aim of this study was to observe whether Polycal has inhibitory activity on ligation-induced experimental periodontitis and related alveolar bone loss in rats following topical application to the gingival regions. One day after the ligation placements, Polycal (50, 25, and 12.5 mg/mL
[...] Read more.
The aim of this study was to observe whether Polycal has inhibitory activity on ligation-induced experimental periodontitis and related alveolar bone loss in rats following topical application to the gingival regions. One day after the ligation placements, Polycal (50, 25, and 12.5 mg/mL solutions at 200 μL/rat) was topically applied to the ligated gingival regions daily for 10 days. Changes in bodyweight, alveolar bone loss index, and total number of buccal gingival aerobic bacterial cells were monitored, and the anti-inflammatory effects were investigated via myeloperoxidase activity and levels of the pro-inflammatory cytokines IL-1β and TNF-α. The activities of inducible nitric oxide synthase (iNOS) and lipid peroxidation (MDA) were also evaluated. Bacterial proliferation, periodontitis, and alveolar bone loss induced by ligature placements were significantly inhibited after 10 days of continuous topical application of Polycal. These results indicate that topical application of Polycal has a significant inhibitory effect on periodontitis and related alveolar bone loss in rats mediated by antibacterial, anti-inflammatory, and anti-oxidative activities. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Glycyrrhetic Acid Ameliorates Dextran Sulfate Sodium-Induced Ulcerative Colitis in Vivo
Molecules 2016, 21(4), 523; https://doi.org/10.3390/molecules21040523
Received: 25 January 2016 / Revised: 13 April 2016 / Accepted: 14 April 2016 / Published: 22 April 2016
Cited by 1 | PDF Full-text (2467 KB) | HTML Full-text | XML Full-text
Abstract
Glycyrrhizae Radix (GR) is a Korean traditional herb medicine that is widely used in clinical health care. Glycyrrhetic acid (GA) is an aglycone saponin extracted from GR that has anti-inflammatory, anti-cancer, and anti-viral effects. However, the anti-inflammatory effects of GA in colitis have
[...] Read more.
Glycyrrhizae Radix (GR) is a Korean traditional herb medicine that is widely used in clinical health care. Glycyrrhetic acid (GA) is an aglycone saponin extracted from GR that has anti-inflammatory, anti-cancer, and anti-viral effects. However, the anti-inflammatory effects of GA in colitis have not been reported. This study investigated the role of GA on ulcerative colitis in a dextran sulfate sodium (DSS)-induced mouse colitis model. DSS-treated mice displayed weight loss and shortened colon length compared with control mice. Mice administered GA showed less weight loss and longer colon length than the DSS-treated group. Interleukin (IL)-6, IL-1β, and tumor necrosis factor-alpha were decreased by GA treatment. GA treatment also reduced DSS-induced microscopic damage to colon tissue. GA regulates the phosphorylation of transcription factors including nuclear factor-kappa B (NF-κB) and IκB alpha, and regulates the expression of cycloxygenase-2 and prostaglandin E2. GA thus showed beneficial effects in a mouse model of colitis, implicating GA might be a useful herb-derived medicine in the treatment of ulcerative colitis. Full article
(This article belongs to the Section Natural Products Chemistry)
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