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Molecules, Volume 20, Issue 12 (December 2015)

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Open AccessCommunication Guignardones P–S, New Meroterpenoids from the Endophytic Fungus Guignardia mangiferae A348 Derived from the Medicinal Plant Smilax glabra
Molecules 2015, 20(12), 22900-22907; https://doi.org/10.3390/molecules201219890
Received: 23 November 2015 / Revised: 15 December 2015 / Accepted: 17 December 2015 / Published: 21 December 2015
Cited by 10 | PDF Full-text (3618 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Four new meroterpenoids, guignardones P–S (14), and three known analogues (57) were isolated from the endophytic fungal strain Guignardia mangiferae A348. Their structures were elucidated on the basis of spectroscopic analysis and single crystal X-ray
[...] Read more.
Four new meroterpenoids, guignardones P–S (14), and three known analogues (57) were isolated from the endophytic fungal strain Guignardia mangiferae A348. Their structures were elucidated on the basis of spectroscopic analysis and single crystal X-ray diffraction. All the isolated compounds were evaluated for their inhibitory effects on SF-268, MCF-7, and NCI-H460 human cancer cell lines. Compounds 2 and 4 exhibited weak inhibitions of cell proliferation against MCF-7 cell line. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Cross-Coupling Synthesis of Methylallyl Alkenes: Scope Extension and Mechanistic Study
Molecules 2015, 20(12), 22890-22899; https://doi.org/10.3390/molecules201219886
Received: 20 November 2015 / Revised: 9 December 2015 / Accepted: 14 December 2015 / Published: 21 December 2015
Cited by 4 | PDF Full-text (5257 KB) | HTML Full-text | XML Full-text
Abstract
Cross-coupling reactions between 2-methyl-2-propen-1-ol and various boronic acids are used to obtain aromatic-(2-methylallyl) derivatives. However, deboronation or isomerization side reactions may occur for several boronic acids. We describe herein the synthesis of original alkenes with good yields under mild reaction conditions that decrease
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Cross-coupling reactions between 2-methyl-2-propen-1-ol and various boronic acids are used to obtain aromatic-(2-methylallyl) derivatives. However, deboronation or isomerization side reactions may occur for several boronic acids. We describe herein the synthesis of original alkenes with good yields under mild reaction conditions that decrease these side reactions. The scope of this environmentally benign reaction is thereby extended to a wide variety of boronic acids. A mechanistic study was conducted and suggested a plausible catalytic cycle mechanism, pointing to the importance of the Lewis acidity of the boronic acid used. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle The Sensitivity of Endodontic Enterococcus spp. Strains to Geranium Essential Oil
Molecules 2015, 20(12), 22881-22889; https://doi.org/10.3390/molecules201219888
Received: 18 September 2015 / Revised: 7 December 2015 / Accepted: 14 December 2015 / Published: 21 December 2015
Cited by 1 | PDF Full-text (199 KB) | HTML Full-text | XML Full-text
Abstract
Enterococci are able to survive endodontic procedures and contribute to the failure of endodontic therapy. Thus, it is essential to identify novel ways of eradicating them from infected root canals. One such approach may be the use of antimicrobials such as plant essential
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Enterococci are able to survive endodontic procedures and contribute to the failure of endodontic therapy. Thus, it is essential to identify novel ways of eradicating them from infected root canals. One such approach may be the use of antimicrobials such as plant essential oils. Enterococcal strains were isolated from endodontically treated teeth by standard microbiological methods. Susceptibility to antibiotics was evaluated by the disc-diffusion method. The minimal inhibitory concentration (MIC) of geranium essential oil was investigated by microdilution in 96-well microplates in Mueller Hinton Broth II. Biofilm eradication concentrations were checked in dentin tests. Geranium essential oil inhibited enterococcal strains at concentrations ranging from 1.8–4.5 mg/mL. No correlation was shown between resistance to antibiotics and the MICs of the test antimicrobials. The MICs of the test oil were lower than those found to show cytotoxic effects on the HMEC-1 cell line. Geranium essential oil eradicated enterococcal biofilm at concentrations of 150 mg/mL. Geranium essential oil inhibits the growth of endodontic enterococcal species at lower concentrations than those required to reach IC50 against the HMEC-1 cell line, and is effective against bacteria protected in biofilm at higher concentrations. In addition, bacteria do not develop resistance to essential oils. Hence, geranium essential oil represents a possible alternative to other antimicrobials during endodontic procedures. Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessCommunication Fatty Acid Profile and Biological Activities of Linseed and Rapeseed Oils
Molecules 2015, 20(12), 22872-22880; https://doi.org/10.3390/molecules201219887
Received: 2 November 2015 / Revised: 13 December 2015 / Accepted: 16 December 2015 / Published: 21 December 2015
Cited by 11 | PDF Full-text (907 KB) | HTML Full-text | XML Full-text
Abstract
It has been postulated that fatty acids found in edible oils may exert beneficial health effects by the modulation of signaling pathways regulating cell differentiation and proliferation, especially in the treatment of cardiovascular diseases. In the present study, the biological effects of selected
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It has been postulated that fatty acids found in edible oils may exert beneficial health effects by the modulation of signaling pathways regulating cell differentiation and proliferation, especially in the treatment of cardiovascular diseases. In the present study, the biological effects of selected edible oils—linseed (LO) and rapeseed (RO) oils—were tested in vitro on fibroblast cells. The fatty acid profile of the oils was determined using gas chromatography and FTIR spectroscopy. LO was found to be rich in α-linolenic acid (ALA), whereas oleic acid was the most abundant species in RO. Fatty acids were taken up by the cells and promoted cell proliferation. No oxidative stress-mediated cytotoxic or genotoxic effects were observed after oil stimulation. Oils ameliorated the process of wound healing as judged by improved migration of fibroblasts to the wounding area. As ALA-rich LO exhibited the most potent wound healing activity, ALA may be considered a candidate for promoting the observed effect. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Bioactive Properties of Tabebuia impetiginosa-Based Phytopreparations and Phytoformulations: A Comparison between Extracts and Dietary Supplements
Molecules 2015, 20(12), 22863-22871; https://doi.org/10.3390/molecules201219885
Received: 12 November 2015 / Revised: 15 December 2015 / Accepted: 17 December 2015 / Published: 21 December 2015
PDF Full-text (207 KB) | HTML Full-text | XML Full-text
Abstract
Tabebuia impetiginosa (Mart. ex DC.) Standl. has been used in traditional medicine for many centuries, being nowadays marketed as dried plant material (inner bark) for infusions, pills, and syrups. The main objective of the present work was to validate its popular use through
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Tabebuia impetiginosa (Mart. ex DC.) Standl. has been used in traditional medicine for many centuries, being nowadays marketed as dried plant material (inner bark) for infusions, pills, and syrups. The main objective of the present work was to validate its popular use through the bioactivity evaluation of the inner bark (methanolic extract and infusion) and of two different formulations (pills and syrup) also based on the same plant-material. The antioxidant activity was evaluated by in vitro assays testing free radical scavenging activity, reducing power and inhibition of lipid peroxidation in brain homogenates. The cytotoxicity was determined in four human tumor cell lines (MCF-7, NCI-H460, HeLa and HepG2, and also in non-tumor cells (porcine liver primary cells, PLP2)). Furthermore, the sample was chemically characterized regarding free sugars, organic acids, fatty acids, and tocopherols. Syrup and methanolic extract showed the highest antioxidant activity, related to their highest amount of phenolics and flavonoids. Methanolic extract was the only sample showing cytotoxic effects on the tested human tumor cell lines, but none of the samples showed toxicity in PLP2. Glucose and oxalic acid were, respectively, the most abundant sugar and organic acid in the sample. Unsaturated predominated over the saturated fatty acids, due to oleic, linoleic, and linolenic acids expression. α- and γ-Tocopherols were also identified and quantified. Overall, T. impetiginosa might be used in different phytoformulations, taking advantage of its interesting bioactive properties and chemical composition. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Ellagitannins and Flavan-3-ols from Raspberry Pomace Modulate Caecal Fermentation Processes and Plasma Lipid Parameters in Rats
Molecules 2015, 20(12), 22848-22862; https://doi.org/10.3390/molecules201219878
Received: 5 October 2015 / Revised: 25 November 2015 / Accepted: 14 December 2015 / Published: 21 December 2015
Cited by 5 | PDF Full-text (478 KB) | HTML Full-text | XML Full-text
Abstract
Raspberry pomace is a source of polyphenols, which nutritional and health promoting properties are not sufficiently known. The aim of this 8-weeks study was to scrutinize if raspberry extracts (REs) with different ellagitannins to flavan-3-ols ratios might favorably affect the caecal fermentation processes
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Raspberry pomace is a source of polyphenols, which nutritional and health promoting properties are not sufficiently known. The aim of this 8-weeks study was to scrutinize if raspberry extracts (REs) with different ellagitannins to flavan-3-ols ratios might favorably affect the caecal fermentation processes and blood lipid profile in rats. Forty male Wistar rats were fed with a standard diet or its modification with two types of REs (E1 and E2) characterized by different ratios of ellagitannins to flavan-3-ols (7.7 and 3.1 for E1 and E2, respectively) and added to a diet at two dosages of polyphenolic compounds (0.15 and 0.30% of a diet; L and H treatments, respectively). Irrespective of polyphenols dietary level, both REs reduced the activity of bacterial β-glucuronidase, increased production of butyric acid in the caecum and reduced triacylglycerols in blood plasma. The E1 treatment at both dosages caused more effective reduction in the concentration of ammonia and elevated acetate level in the caecal digesta than E2. On the other hand, only the E2 treatment lowered value of the atherogenic index when compared with control group. When comparing dosages of REs, a higher one was more potent to reduce the activity of bacterial β-glucosidase, β-, α-galactosidase and lowered value of the HDL profile in plasma. To conclude, REs may favorably modulate the activity of the caecal microbiota and blood lipid profile in rats; however, the intensity of these effects may be related to the dosages of dietary polyphenols and to their profile, e.g., ellagitannins to flavan-3-ols ratio. Full article
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Open AccessReview Properties and Applications of Polyvinyl Alcohol, Halloysite Nanotubes and Their Nanocomposites
Molecules 2015, 20(12), 22833-22847; https://doi.org/10.3390/molecules201219884
Received: 15 October 2015 / Revised: 27 November 2015 / Accepted: 11 December 2015 / Published: 19 December 2015
Cited by 47 | PDF Full-text (3289 KB) | HTML Full-text | XML Full-text
Abstract
The aim of this review was to analyze/investigate the synthesis, properties, and applications of polyvinyl alcohol–halloysite nanotubes (PVA–HNT), and their nanocomposites. Different polymers with versatile properties are attractive because of their introduction and potential uses in many fields. Synthetic polymers, such as PVA,
[...] Read more.
The aim of this review was to analyze/investigate the synthesis, properties, and applications of polyvinyl alcohol–halloysite nanotubes (PVA–HNT), and their nanocomposites. Different polymers with versatile properties are attractive because of their introduction and potential uses in many fields. Synthetic polymers, such as PVA, natural polymers like alginate, starch, chitosan, or any material with these components have prominent status as important and degradable materials with biocompatibility properties. These materials have been developed in the 1980s and are remarkable because of their recyclability and consideration of the natural continuation of their physical and chemical properties. The fabrication of PVA–HNT nanocomposites can be a potential way to address some of PVA’s limitations. Such nanocomposites have excellent mechanical properties and thermal stability. PVA–HNT nanocomposites have been reported earlier, but without proper HNT individualization and PVA modifications. The properties of PVA–HNT for medicinal and biomedical use are attracting an increasing amount of attention for medical applications, such as wound dressings, drug delivery, targeted-tissue transportation systems, and soft biomaterial implants. The demand for alternative polymeric medical devices has also increased substantially around the world. This paper reviews individualized HNT addition along with crosslinking of PVA for various biomedical applications that have been previously reported in literature, thereby showing the attainability, modification of characteristics, and goals underlying the blending process with PVA. Full article
(This article belongs to the Section Molecular Diversity)
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Open AccessFeature PaperReview Pharmacophore Models and Pharmacophore-Based Virtual Screening: Concepts and Applications Exemplified on Hydroxysteroid Dehydrogenases
Molecules 2015, 20(12), 22799-22832; https://doi.org/10.3390/molecules201219880
Received: 19 November 2015 / Revised: 3 December 2015 / Accepted: 9 December 2015 / Published: 19 December 2015
Cited by 20 | PDF Full-text (6349 KB) | HTML Full-text | XML Full-text
Abstract
Computational methods are well-established tools in the drug discovery process and can be employed for a variety of tasks. Common applications include lead identification and scaffold hopping, as well as lead optimization by structure-activity relationship analysis and selectivity profiling. In addition, compound-target interactions
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Computational methods are well-established tools in the drug discovery process and can be employed for a variety of tasks. Common applications include lead identification and scaffold hopping, as well as lead optimization by structure-activity relationship analysis and selectivity profiling. In addition, compound-target interactions associated with potentially harmful effects can be identified and investigated. This review focuses on pharmacophore-based virtual screening campaigns specifically addressing the target class of hydroxysteroid dehydrogenases. Many members of this enzyme family are associated with specific pathological conditions, and pharmacological modulation of their activity may represent promising therapeutic strategies. On the other hand, unintended interference with their biological functions, e.g., upon inhibition by xenobiotics, can disrupt steroid hormone-mediated effects, thereby contributing to the development and progression of major diseases. Besides a general introduction to pharmacophore modeling and pharmacophore-based virtual screening, exemplary case studies from the field of short-chain dehydrogenase/reductase (SDR) research are presented. These success stories highlight the suitability of pharmacophore modeling for the various application fields and suggest its application also in futures studies. Full article
(This article belongs to the Special Issue Chemoinformatics)
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Open AccessArticle Studies on Chromatographic Fingerprint and Fingerprinting Profile-Efficacy Relationship of Saxifraga stolonifera Meerb.
Molecules 2015, 20(12), 22781-22798; https://doi.org/10.3390/molecules201219882
Received: 28 September 2015 / Revised: 15 December 2015 / Accepted: 15 December 2015 / Published: 19 December 2015
Cited by 8 | PDF Full-text (1538 KB) | HTML Full-text | XML Full-text
Abstract
This work investigated the spectrum-effect relationships between high performance liquid chromatography (HPLC) fingerprints and the anti-benign prostatic hyperplasia activities of aqueous extracts from Saxifraga stolonifera. The fingerprints of S. stolonifera from various sources were established by HPLC and evaluated by similarity analysis
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This work investigated the spectrum-effect relationships between high performance liquid chromatography (HPLC) fingerprints and the anti-benign prostatic hyperplasia activities of aqueous extracts from Saxifraga stolonifera. The fingerprints of S. stolonifera from various sources were established by HPLC and evaluated by similarity analysis (SA), hierarchical clustering analysis (HCA) and principal component analysis (PCA). Nine samples were obtained from these 24 batches of different origins, according to the results of SA, HCA and the common chromatographic peaks area. A testosterone-induced mouse model of benign prostatic hyperplasia (BPH) was used to establish the anti-benign prostatic hyperplasia activities of these nine S. stolonifera samples. The model was evaluated by analyzing prostatic index (PI), serum acid phosphatase (ACP) activity, concentrations of serum dihydrotestosterone (DHT), prostatic acid phosphatase (PACP) and type II 5α-reductase (SRD5A2). The spectrum-effect relationships between HPLC fingerprints and anti-benign prostatic hyperplasia activities were investigated using Grey Correlation Analysis (GRA) and partial least squares regression (PLSR). The results showed that a close correlation existed between the fingerprints and anti-benign prostatic hyperplasia activities, and peak 14 (chlorogenic acid), peak 17 (quercetin 5-O-β-d-glucopyranoside) and peak 18 (quercetin 3-O-β-l-rhamno-pyranoside) in the HPLC fingerprints might be the main active components against anti-benign prostatic hyperplasia. This work provides a general model for the study of spectrum-effect relationships of S. stolonifera by combing HPLC fingerprints with a testosterone-induced mouse model of BPH, which can be employed to discover the principle components of anti-benign prostatic hyperplasia bioactivity. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Tissue- Specific Expression Analysis of Anthocyanin Biosynthetic Genes in White- and Red-Fleshed Grape Cultivars
Molecules 2015, 20(12), 22767-22780; https://doi.org/10.3390/molecules201219883
Received: 18 October 2015 / Revised: 11 December 2015 / Accepted: 15 December 2015 / Published: 19 December 2015
Cited by 9 | PDF Full-text (1858 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Yan73, a teinturier (dyer) grape variety in China, is one of the few Vitis vinifera cultivars with red-coloured berry flesh. To examine the tissue-specific expression of genes associated with berry colour in Yan73, we analysed the differential accumulation of anthocyanins in the skin
[...] Read more.
Yan73, a teinturier (dyer) grape variety in China, is one of the few Vitis vinifera cultivars with red-coloured berry flesh. To examine the tissue-specific expression of genes associated with berry colour in Yan73, we analysed the differential accumulation of anthocyanins in the skin and flesh tissues of two red-skinned grape varieties with either red (Yan73) or white flesh (Muscat Hamburg) based on HPLC-MS analysis, as well as the differential expression of 18 anthocyanin biosynthesis genes in both varieties by quantitative RT-PCR. The results revealed that the transcripts of GST, OMT, AM3, CHS3, UFGT, MYBA1, F3′5′H, F3H1 and LDOX were barely detectable in the white flesh of Muscat Hamburg. In particular, GST, OMT, AM3, CHS3 and F3H1 showed approximately 50-fold downregulation in the white flesh of Muscat Hamburg compared to the red flesh of Yan73. A correlation analysis between the accumulation of different types of anthocyanins and gene expression indicated that the cumulative expression of GST, F3′5′H, LDOX and MYBA1 was more closely associated with the acylated anthocyanins and the 3′5′-OH anthocyanins, while OMT and AM3 were more closely associated with the total anthocyanins and methoxylated anthocyanins. Therefore, the transcripts of OMT, AM3, GST, F3′5′H, LDOX and MYBA1 explained most of the variation in the amount and composition of anthocyanins in skin and flesh of Yan73. The data suggest that the specific localization of anthocyanins in the flesh tissue of Yan73 is most likely due to the tissue-specific expression of OMT, AM3, GST, F3′5′H, LDOX and MYBA1 in the flesh. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessFeature PaperArticle OSU-6: A Highly Efficient, Metal-Free, Heterogeneous Catalyst for the Click Synthesis of 5-Benzyl and 5-Aryl-1H-tetrazoles
Molecules 2015, 20(12), 22757-22766; https://doi.org/10.3390/molecules201219881
Received: 18 November 2015 / Revised: 7 December 2015 / Accepted: 11 December 2015 / Published: 19 December 2015
Cited by 6 | PDF Full-text (2132 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
OSU-6, an MCM-41 type hexagonal mesoporous silica with mild Brönsted acid properties, has been used as an efficient, metal-free, heterogeneous catalyst for the click synthesis of 5-benzyl and 5-aryl-1H-tetrazoles from nitriles in DMF at 90 °C. This catalyst offers advantages including
[...] Read more.
OSU-6, an MCM-41 type hexagonal mesoporous silica with mild Brönsted acid properties, has been used as an efficient, metal-free, heterogeneous catalyst for the click synthesis of 5-benzyl and 5-aryl-1H-tetrazoles from nitriles in DMF at 90 °C. This catalyst offers advantages including ease of operation, milder conditions, high yields, and reusability. Studies are presented that demonstrate the robust nature of the catalyst under the optimized reaction conditions. OSU-6 promotes the 1,3-dipolar addition of azides to nitriles without significant degradation or clogging of the nanoporous structure. The catalyst can be reused up to five times without a significant reduction in yield, and it does not require treatment with acid between reactions. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessReview Unfolded Protein Response and Macroautophagy in Alzheimer’s, Parkinson’s and Prion Diseases
Molecules 2015, 20(12), 22718-22756; https://doi.org/10.3390/molecules201219865
Received: 30 October 2015 / Revised: 30 November 2015 / Accepted: 9 December 2015 / Published: 18 December 2015
Cited by 14 | PDF Full-text (2421 KB) | HTML Full-text | XML Full-text
Abstract
Proteostasis are integrated biological pathways within cells that control synthesis, folding, trafficking and degradation of proteins. The absence of cell division makes brain proteostasis susceptible to age-related changes and neurodegeneration. Two key processes involved in sustaining normal brain proteostasis are the unfolded protein
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Proteostasis are integrated biological pathways within cells that control synthesis, folding, trafficking and degradation of proteins. The absence of cell division makes brain proteostasis susceptible to age-related changes and neurodegeneration. Two key processes involved in sustaining normal brain proteostasis are the unfolded protein response and autophagy. Alzheimer’s disease (AD), Parkinson’s disease (PD) and prion diseases (PrDs) have different clinical manifestations of neurodegeneration, however, all share an accumulation of misfolded pathological proteins associated with perturbations in unfolded protein response and macroautophagy. While both the unfolded protein response and macroautophagy play an important role in the prevention and attenuation of AD and PD progression, only macroautophagy seems to play an important role in the development of PrDs. Macroautophagy and unfolded protein response can be modulated by pharmacological interventions. However, further research is necessary to better understand the regulatory pathways of both processes in health and neurodegeneration to be able to develop new therapeutic interventions. Full article
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Open AccessArticle Phenolic Assesment of Uncaria tomentosa L. (Cat’s Claw): Leaves, Stem, Bark and Wood Extracts
Molecules 2015, 20(12), 22703-22717; https://doi.org/10.3390/molecules201219875
Received: 14 October 2015 / Revised: 7 December 2015 / Accepted: 10 December 2015 / Published: 18 December 2015
Cited by 13 | PDF Full-text (2451 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The phenolic composition of extracts from Uncaria tomentosa L. from different regions of Costa Rica was studied using advanced analytical techniques such as UPLC/TQ-ESI-MS and 13C-NMR. Samples from leaves, stems, bark and wood (n = 22) were subjected to extraction to
[...] Read more.
The phenolic composition of extracts from Uncaria tomentosa L. from different regions of Costa Rica was studied using advanced analytical techniques such as UPLC/TQ-ESI-MS and 13C-NMR. Samples from leaves, stems, bark and wood (n = 22) were subjected to extraction to obtain phenolic and alkaloid extracts, separately. Comparatively, higher values of total phenolic content were observed for leaves, stems and bark (225–494 gallic acid equivalents/g) than for wood extracts (40–167 gallic acid equivalents/g). A total of 32 non-flavonoid and flavonoid compounds were identified in the phenolic extracts: hydroxybenzoic acids (benzoic, salicylic, 4-hydroxybenzoic, prochatechuic, gallic, syringic and vanillic acids), hydroxycinnamic acids (p-coumaric, caffeic, ferulic and isoferulic acids), flavan-3-ols monomers [(+)-catechin and (−)-epicatechin)], procyanidin dimers (B1, B2, B3, B4, B5, B7 and two other of unknown structure) and trimers (C1, T2 and one of unknown structure), flavalignans (four unknown structures pertaining to the cinchonain family) and propelargonidin dimers (four unknown structures, reported for the first time in U. tomentosa). Additionally, alkaloid extracts obtained from the plant residue after phenolic extraction exhibited a content of tetracyclic and pentacyclic alkaloids ranging between 95 and 275 mg/100 g of dry material for bark extracts, and between 30 and 704 mg/100 g for leaves extracts. In addition, a minor alkaloid was isolated and characterized, namely 18,19-dehydrocorynoxinoic acid. Our results confirmed the feasibility of U. tomentosa as a suitable raw material for obtaining phenolic- and alkaloid-rich extracts of potential interest. Full article
(This article belongs to the Special Issue Recent Advances in Plant Phenolics)
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Open AccessArticle Solid-State Characterization and Biological Activity of Betulonic Acid Derivatives
Molecules 2015, 20(12), 22691-22702; https://doi.org/10.3390/molecules201219876
Received: 1 November 2015 / Revised: 4 December 2015 / Accepted: 7 December 2015 / Published: 18 December 2015
Cited by 2 | PDF Full-text (2263 KB) | HTML Full-text | XML Full-text
Abstract
Betulonic acid belongs to the pentacyclic triterpenic derivative class and can be obtained through the selective oxidation of betulin. In this study we set obtaining several functionalized derivatives of this compound by its condensation with several amino compounds such as aminoguanidine, hydroxylamine, n
[...] Read more.
Betulonic acid belongs to the pentacyclic triterpenic derivative class and can be obtained through the selective oxidation of betulin. In this study we set obtaining several functionalized derivatives of this compound by its condensation with several amino compounds such as aminoguanidine, hydroxylamine, n-butylamine and thiosemicarbazide as our goal. The functionalization of the parent compound led to several molecules with antiproliferative potential, the most promising being 3–2-carbamothioylhydrazonolup-20(29)-en-28-oic acid. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Short-Term and Sub-Chronic Dietary Exposure to Aspalathin-Enriched Green Rooibos (Aspalathus linearis) Extract Affects Rat Liver Function and Antioxidant Status
Molecules 2015, 20(12), 22674-22690; https://doi.org/10.3390/molecules201219868
Received: 9 November 2015 / Revised: 9 December 2015 / Accepted: 11 December 2015 / Published: 18 December 2015
Cited by 4 | PDF Full-text (1075 KB) | HTML Full-text | XML Full-text | Correction
Abstract
An aspalathin-enriched green rooibos (Aspalathus linearis) extract (GRE) was fed to male Fischer rats in two independent studies for 28 and 90 days. The average dietary total polyphenol (TP) intake was 756 and 627 mg Gallic acid equivalents (GAE)/kg body weight
[...] Read more.
An aspalathin-enriched green rooibos (Aspalathus linearis) extract (GRE) was fed to male Fischer rats in two independent studies for 28 and 90 days. The average dietary total polyphenol (TP) intake was 756 and 627 mg Gallic acid equivalents (GAE)/kg body weight (bw)/day over 28 and 90 days, respectively, equaling human equivalent doses (HEDs) of 123 and 102 GAE mg/kg bw/day. Aspalathin intake of 295 mg/kg bw/day represents a HED of 48 mg/kg bw/day (90 day study). Consumption of GRE increased feed intake significantly (p < 0.05) compared to the control after 90 days, but no effect on body and organ weight parameters was observed. GRE significantly (p < 0.05) reduced serum total cholesterol and iron levels, whilst significantly (p < 0.05) increasing alkaline phosphatase enzyme activity after 90 days. Endogenous antioxidant enzyme activity in the liver, i.e., catalase and superoxide dismutase activity, was not adversely affected. Glutathione reductase activity significantly (p < 0.05) increased after 28 days, while glutathione (GSH) content was decreased after 90 days, suggesting an altered glutathione redox cycle. Quantitative Real Time polymerase chain reaction (PCR) analysis showed altered expression of certain antioxidant defense and oxidative stress related genes, indicative, among others, of an underlying oxidative stress related to changes in the GSH redox pathway and possible biliary dysfunction. Full article
(This article belongs to the Special Issue Antioxidants—A Risk-Benefit Analysis for Health)
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