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Special Issue "Selected papers from 2nd International Symposium on Phytochemicals in Medicine and Food (2-ISPMF, Fuzhou, 2017)"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (15 February 2017)

Special Issue Editors

Guest Editor
Prof. Dr. Pinarosa Avato

Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari Aldo Moro Via Orabona 4, 70125 Bari, Italy
E-Mail
Phone: +390805442785
Fax: +390805442230
Interests: phytochemicals; natural products; plant biodiversity; medicinal plants; food plants; bioactivity; polyphenols; glucosinolates; biocides
Guest Editor
Prof. Dr. Baodong Zheng

College of Food Science, Fujian Agriculture and Forestry University, Fuzhou, Fujian, 350002, China
E-Mail
Interests: polysaccharides; natural products; antioxidants; starch; food process; function foods
Guest Editor
Prof. Dr. Jianbo Xiao

Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau; College of Food Science, Fujian Agriculture and Forestry University, Fuzhou 350002, China
E-Mail
Interests: phytochemicals; polyphenols; diabetes; function food; natural products; glycosylation; biological activity; flavonoids; stilbenoids; pharmacokinetics; nutrition and metabolism; polyphenol-protein interaction

Special Issue Information

Dear Colleagues,

This Special Issue is related to 2nd International Symposium on Phytochemicals in Medicine and Food (2-ISPMF), which will be held at Fujian Agriculture and Forestry University, 7–10 April, 2017. 2-ISPMF is sponsored by the Phytochemical Society of Europe (PSE), and the International Society for Chinese Medicine (ISCM).

This Special Issue seeks updated and new knowledge on the phytochemicals in medicine and food. Evidence from epidemiological investigations show that natural phytochemicals have received increased attention due to their considerable benefits in the prevention and management of modern diseases, such as cancers, diabetes, and cardiovascular diseases. This Special Issue will shape the future research direction for this important phytomedicine source. Our purpose is to feature high-quality, advanced research and knowledge, contributed by various research groups working on phytochemicals. We invite researchers to contribute reviews and reports of their recent work on the chemistry, biology, and biotechnology of phytochemicals.

The Special Issue will focus on phytochemicals in medicine and food, including following aspects:

  1. Natural products for the prevention and therapy of modern diseases.
  2. Mechanism of phytochemicals for the therapy and chemoprevention of modern diseases.
  3. Importance of natural phytochemicals in medicine and food
  4. Quantitative structure–activity relationship (QSAR) and modeling for natural drugs design
  5. Natural antioxidants and human health
  6. New strategy of using natural products for managing diseases
  7. Pharmacokinetics and biotransformation of phytochemicals
  8. Food-medicine/phytochemicals interaction
  9. Nutrition and metabolism of phytochemicals

Prof. Dr. Pinarosa Avato
Prof. Dr. Baodong Zheng
Dr. Jianbo Xiao
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Phytochemicals
  • Medicinal plants
  • Natural products
  • Food chemistry
  • Phytomedicine
  • Metabolism
  • Prevention
  • Chemoprevention
  • Function food
  • Pharmacokinetics
  • Biotransformation

Published Papers (18 papers)

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Research

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Open AccessArticle Metronomic Cordycepin Therapy Prolongs Survival of Oral Cancer-Bearing Mice and Inhibits Epithelial-Mesenchymal Transition
Molecules 2017, 22(4), 629; doi:10.3390/molecules22040629
Received: 14 February 2017 / Revised: 6 April 2017 / Accepted: 10 April 2017 / Published: 13 April 2017
Cited by 1 | PDF Full-text (3486 KB) | HTML Full-text | XML Full-text
Abstract
Cordycepin (3′-deoxyadenosine) is a natural compound abundantly found in Cordyceps sinesis in natural and fermented sources. In this study, we examined the effects of cordycepin in a human oral squamous cell carcinoma (OSCC) xenograft model. Cordycepin was administered in a regular, low-dose and
[...] Read more.
Cordycepin (3′-deoxyadenosine) is a natural compound abundantly found in Cordyceps sinesis in natural and fermented sources. In this study, we examined the effects of cordycepin in a human oral squamous cell carcinoma (OSCC) xenograft model. Cordycepin was administered in a regular, low-dose and prolonged schedule metronomic therapy. Two doses of cordycepin (25 mg/kg, 50 mg/kg) were administrated five days a week for eight consecutive weeks. The tumor volumes were reduced and survival time was significantly prolonged from 30.3 ± 0.9 days (control group) to 56 days (50 mg/kg group, the day of tumor-bearing mice were sacrificed for welfare consideration). The weights of mice did not change and liver, renal, and hematologic functions were not compromised. Cordycepin inhibited the OSCC cell viability in vitro (IC50 122.4–125.2 μM). Furthermore, morphological characteristics of apoptosis, increased caspase-3 activity and G2/M cell cycle arrest were observed. In wound healing assay, cordycepin restrained the OSCC cell migration. Cordycepin upregulated E-cadherin and downregulated N-cadherin protein expression, implying inhibition of epithelial-mesenchymal transition (EMT). The immunohistochemical staining of xenograft tumor with E-cadherin and vimentin validated in vitro results. In conclusion, metronomic cordycepin therapy showed effective tumor control, prolonged survival and low toxicities. Cytotoxicity against cancer cells with apoptotic features and EMT inhibition were observed. Full article
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Open AccessArticle A Specific Peptide with Calcium-Binding Capacity from Defatted Schizochytrium sp. Protein Hydrolysates and the Molecular Properties
Molecules 2017, 22(4), 544; doi:10.3390/molecules22040544
Received: 15 February 2017 / Revised: 19 March 2017 / Accepted: 23 March 2017 / Published: 29 March 2017
PDF Full-text (2011 KB) | HTML Full-text | XML Full-text
Abstract
Marine microorganisms have been proposed as a new kind of protein source. Efforts are needed in order to transform the protein-rich biological wastes left after lipid extraction into value-added bio-products. Thus, the utilization of protein recovered from defatted Schizochytrium sp. by-products presents an
[...] Read more.
Marine microorganisms have been proposed as a new kind of protein source. Efforts are needed in order to transform the protein-rich biological wastes left after lipid extraction into value-added bio-products. Thus, the utilization of protein recovered from defatted Schizochytrium sp. by-products presents an opportunity. A specific peptide Tyr-Leu (YL) with calcium-binding capacity was purified from defatted Schizochytrium sp. protein hydrolysates through gel filtration chromatography and RP-HPLC. The calcium-binding activity of YL reached 126.34 ± 3.40 μg/mg. The calcium-binding mechanism was investigated through ultraviolet, fluorescence and infrared spectroscopy. The results showed that calcium ions could form dative bonds with carboxyl oxygen atoms and amino nitrogen atoms as well as the nitrogen and oxygen atoms of amide bonds. YL-Ca exhibited excellent thermal stability and solubility, which was beneficial for its absorption and transport in the basic intestinal tract of the human body. Moreover, the cellular uptake of calcium in Caco-2 cells showed that YL-Ca could enhance calcium uptake efficiency and protect calcium ions against precipitation caused by dietary inhibitors such as tannic acid, oxalate, phytate and metal ions. The findings indicate that the by-product of Schizochytrium sp. is a promising source for making peptide-calcium bio-products as algae-based functional supplements for human beings. Full article
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Open AccessArticle In Vitro Antioxidant Activity and In Vivo Anti-Fatigue Effect of Sea Horse (Hippocampus) Peptides
Molecules 2017, 22(3), 482; doi:10.3390/molecules22030482
Received: 10 February 2017 / Revised: 13 March 2017 / Accepted: 15 March 2017 / Published: 18 March 2017
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Abstract
This study investigated changes the in vitro antioxidant activity of Hippocampus polypeptides during enzymatic hydrolysis, including the effects of enzyme species, enzyme concentration, material–liquid ratio, hydrolysis time, pH, and temperature of the reaction system. Its in vivo anti-fatigue activity was also studied. Hippocampus
[...] Read more.
This study investigated changes the in vitro antioxidant activity of Hippocampus polypeptides during enzymatic hydrolysis, including the effects of enzyme species, enzyme concentration, material–liquid ratio, hydrolysis time, pH, and temperature of the reaction system. Its in vivo anti-fatigue activity was also studied. Hippocampus peptide prepared by papain digestion exhibited the highest 1,1-diphenyl-2-picryl-hydrazyl free radical scavenging rate (71.89% ± 1.50%) and strong hydroxyl radical scavenging rate (75.53% ± 0.98%), compared to those prepared by five other commonly used enzymes (i.e., trypsin, neutral protease, compound protease, flavorzyme, and alkaline protease). Additionally, maximum antioxidant activity of Hippocampus polypeptide prepared by papain digestion was reached after hydrolysis for 40 min at pH 6.0 and 60 °C of the reaction system by using 2000 U/g enzyme and a material–liquid ratio of 1:15. Moreover, compared with the control group, Hippocampus peptide prolonged the swimming time by 33%–40%, stabilized the blood glucose concentration, increased liver glycogen levels, and decreased blood lactate levels and blood urea nitrogen levels in mice (p < 0.01). In conclusion, these results indicated that Hippocampus polypeptide prepared by papain digestion under optimal conditions exhibited high degrees of antioxidant and anti-fatigue activity. Full article
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Open AccessCommunication Comparison of Free Total Amino Acid Compositions and Their Functional Classifications in 13 Wild Edible Mushrooms
Molecules 2017, 22(3), 350; doi:10.3390/molecules22030350
Received: 5 February 2017 / Revised: 18 February 2017 / Accepted: 19 February 2017 / Published: 24 February 2017
Cited by 2 | PDF Full-text (1421 KB) | HTML Full-text | XML Full-text
Abstract
Thirteen popular wild edible mushroom species in Yunnan Province, Boletus bicolor, Boletus speciosus, Boletus sinicus, Boletus craspedius, Boletus griseus, Boletus ornatipes, Xerocomus, Suillus placidus, Boletinus pinetorus, Tricholoma terreum, Tricholomopsis lividipileata, Termitomyces microcarpus
[...] Read more.
Thirteen popular wild edible mushroom species in Yunnan Province, Boletus bicolor, Boletus speciosus, Boletus sinicus, Boletus craspedius, Boletus griseus, Boletus ornatipes, Xerocomus, Suillus placidus, Boletinus pinetorus, Tricholoma terreum, Tricholomopsis lividipileata, Termitomyces microcarpus, and Amanita hemibapha, were analyzed for their free amino acid compositions by online pre-column derivazation reversed phase high-performance liquid chromatography (RP-HPLC) analysis. Twenty free amino acids, aspartic acid, glutamic acid, serine, glycine, alanine, praline, cysteine, valine, methionine, phenylalanine, isoleucine, leucine, lysine, histidine, threonine, asparagines, glutamine, arginine, tyrosine, and tryptophan, were determined. The total free amino acid (TAA) contents ranged from 1462.6 mg/100 g in B. craspedius to 13,106.2 mg/100 g in T. microcarpus. The different species showed distinct free amino acid profiles. The ratio of total essential amino acids (EAA) to TAA was 0.13–0.41. All of the analyzed species showed high contents of hydrophobic amino acids, at 33%–54% of TAA. Alanine, cysteine, glutamine, and glutamic acid were among the most abundant amino acids present in all species. The results showed that the analyzed mushrooms possessed significant free amino acid contents, which may be important compounds contributing to the typical mushroom taste, nutritional value, and potent antioxidant properties of these wild edible mushrooms. Furthermore, the principal component analysis (PCA) showed that the accumulative variance contribution rate of the first four principal components reached 94.39%. Cluster analysis revealed EAA composition and content might be an important parameter to separate the mushroom species, and T. microcarpus and A. hemibapha showed remarkable EAA content among the 13 species. Full article
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Open AccessArticle Purification and Characterization of Antioxidant Peptides of Pseudosciaena crocea Protein Hydrolysates
Molecules 2017, 22(1), 57; doi:10.3390/molecules22010057
Received: 12 November 2016 / Revised: 28 December 2016 / Accepted: 29 December 2016 / Published: 30 December 2016
Cited by 1 | PDF Full-text (1835 KB) | HTML Full-text | XML Full-text
Abstract
Two peptides with antioxidant activity were isolated from Pseudosciaena crocea proteins. Pseudosciaena crocea muscle was hydrolyzed with neutral protease to obtain Pseudosciaena crocea protein hydrolysates (PCPH). After ultrafiltration through molecular weight cut-off membranes of 10, 5 and 3 kDa and assessment of free
[...] Read more.
Two peptides with antioxidant activity were isolated from Pseudosciaena crocea proteins. Pseudosciaena crocea muscle was hydrolyzed with neutral protease to obtain Pseudosciaena crocea protein hydrolysates (PCPH). After ultrafiltration through molecular weight cut-off membranes of 10, 5 and 3 kDa and assessment of free radical scavenging ability, the fraction (PCPH-IV) with the highest antioxidant activity was obtained. Several purification steps, i.e., ion exchange chromatography, gel filtration chromatography and reversed phase high performance liquid chromatography, were applied to further purify PCPH-IV. Two antioxidant peptides with the amino acid sequences Ser-Arg-Cys-His-Val and Pro-Glu-His-Trp were finally identified by LC-MS/MS. Full article
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Open AccessArticle Chemical Basis of the Fungicidal Activity of Tobacco Extracts against Valsa mali
Molecules 2016, 21(12), 1743; doi:10.3390/molecules21121743
Received: 14 November 2016 / Revised: 8 December 2016 / Accepted: 13 December 2016 / Published: 18 December 2016
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Abstract
Under pressure from social criticism and an unclear future, tobacco researchers have begun to seek alternative uses for the product. Here, we present our study on isolating tobacco compounds with fungicidal activity, which could be used as plant-derived pesticides. Using
Valsa mali as
[...] Read more.
Under pressure from social criticism and an unclear future, tobacco researchers have begun to seek alternative uses for the product. Here, we present our study on isolating tobacco compounds with fungicidal activity, which could be used as plant-derived pesticides. Using
Valsa mali as the target fungus, agar plate tests were conducted to evaluate the fungicidal activity of various tobacco extracts, including tobacco leaves extracts prepared with different solvents, extracts of different tobacco cultivars, and samples from different tobacco organs. Fungal growth morphology was used as the criterion to evaluate the fungicidal activity of tobacco extracts. Correlation analyses between the fungicidal activities and the chemical components of tobacco extracts indicated the major chemical constituents with fungicidal activity. Then, the active compounds were isolated and their effects on the ultra-microstructures of V. mali was analyzed using scanning- and transmission-electron microscopy. The results suggested that tobacco extracts prepared with solvents of weaker polarity had higher fungicidal activity, and the inhibitory activity of tobacco extracts against V. mali was also cultivar dependent. Furthermore, the fungicidal effects of tobacco flower extracts were higher than those of the leaf extracts. Chemical analysis indicated that cembranoids were the main fungicidal substances, which act by destroying the endometrial structure of the fungus. Tobacco cembranoids at 80 μg/mL could completely inhibit the growth of V. mali, with an EC50 value of 13.18 μg/mL. Our study therefore suggests that tobacco leaves and inflorescences are excellent plant resources for the biological control of V. mali. Full article
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Open AccessArticle The Traditional Chinese Medicine DangguiBuxue Tang Sensitizes Colorectal Cancer Cells to Chemoradiotherapy
Molecules 2016, 21(12), 1677; doi:10.3390/molecules21121677
Received: 30 September 2016 / Revised: 23 November 2016 / Accepted: 30 November 2016 / Published: 6 December 2016
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Abstract
Chemotherapy is an important treatment modality for colon cancer, and concurrent chemoradiation therapy (CCRT) is the preferred treatment route for patients with stage II and III rectal cancer. We examined whether DangguiBuxue Tang (DBT), a traditional Chinese herbal extract, sensitizes colorectal cancer cells
[...] Read more.
Chemotherapy is an important treatment modality for colon cancer, and concurrent chemoradiation therapy (CCRT) is the preferred treatment route for patients with stage II and III rectal cancer. We examined whether DangguiBuxue Tang (DBT), a traditional Chinese herbal extract, sensitizes colorectal cancer cells to anticancer treatments. The polysaccharide-depleted fraction of DBT (DBT-PD) contains greater amounts of astragaloside IV (312.626 µg/g) and ferulic acid (1.404 µg/g) than does the original formula. Treatment of the murine colon carcinoma cell line (CT26) with DBT-PD inhibits growth, whereas treatment with comparable amounts of purified astragaloside IV and ferulic acid showed no significant effect. Concurrent treatment with DBT-PD increases the growth inhibitory effect of 5-fluorouracil up to 4.39-fold. DBT-PD enhances the effect of radiation therapy (RT) with a sensitizer enhancement ratio (SER) of up to 1.3. It also increases the therapeutic effect of CCRT on CT26 cells. Cells treated with DBP-PD showed ultrastructural changes characteristic of autophagy, including multiple cytoplasmic vacuoles with double-layered membranes, vacuoles containing remnants of degraded organelles, marked swelling and vacuolization of mitochondria, and autolysosome-like vacuoles. We conclude that DBT-PD induces autophagy-associated cell death in CT26 cells, and may have potential as a chemotherapy or radiotherapy sensitizer in colorectal cancer treatment. Full article
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Open AccessArticle Pathway Analysis and Metabolites Identification by Metabolomics of Etiolation Substrate from Fresh-Cut Chinese Water Chestnut (Eleocharis tuberosa)
Molecules 2016, 21(12), 1648; doi:10.3390/molecules21121648
Received: 9 October 2016 / Revised: 20 November 2016 / Accepted: 21 November 2016 / Published: 1 December 2016
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Abstract
Fresh-cut Chinese water chestnuts (CWC) turn yellow after being peeled, reducing their shelf life and commercial value. Metabolomics, the systematic study of the full complement of small molecular metabolites, was useful for clarifying the mechanism of fresh-cut CWC etiolation and developing methods to
[...] Read more.
Fresh-cut Chinese water chestnuts (CWC) turn yellow after being peeled, reducing their shelf life and commercial value. Metabolomics, the systematic study of the full complement of small molecular metabolites, was useful for clarifying the mechanism of fresh-cut CWC etiolation and developing methods to inhibit yellowing. In this study, metabolic alterations associated with etiolation at different growth stages (0 day, 2 days, 3 days, 4 days, 5 days) from fresh-cut CWC were investigated using LC–MS and analyzed by pattern recognition methods (principal component analysis (PCA), partial least squares-discriminant analysis (PLS-DA), and orthogonal projection to latent structures-discriminant analysis (OPLS-DA)). The metabolic pathways of the etiolation molecules were elucidated. The main metabolic pathway appears to be the conversion of phenylalanine to p-coumaroyl-CoA, followed by conversion to naringenin chalcone, to naringenin, and naringenin then following different pathways. Firstly, it can transform into apigenin and its derivatives; secondly, it can produce eriodictyol and its derivatives; and thirdly it can produce dihydrokaempferol, quercetin, and myricetin. The eriodictyol can be further transformed to luteolin, cyanidin, dihydroquercetin, dihydrotricetin, and others. This is the first reported use of metabolomics to study the metabolic pathways of the etiolation of fresh-cut CWC. Full article
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Open AccessArticle Organ- and Growing Stage-Specific Expression of Solanesol Biosynthesis Genes in Nicotiana tabacum Reveals Their Association with Solanesol Content
Molecules 2016, 21(11), 1536; doi:10.3390/molecules21111536
Received: 9 September 2016 / Revised: 11 November 2016 / Accepted: 11 November 2016 / Published: 15 November 2016
Cited by 1 | PDF Full-text (2250 KB) | HTML Full-text | XML Full-text
Abstract
Solanesol is a noncyclic terpene alcohol that is composed of nine isoprene units and mainly accumulates in solanaceous plants, especially tobacco (Nicotiana tabacum L.). In the present study, RNA-seq analyses of tobacco leaves, stems, and roots were used to identify putative solanesol
[...] Read more.
Solanesol is a noncyclic terpene alcohol that is composed of nine isoprene units and mainly accumulates in solanaceous plants, especially tobacco (Nicotiana tabacum L.). In the present study, RNA-seq analyses of tobacco leaves, stems, and roots were used to identify putative solanesol biosynthesis genes. Six 1-deoxy-d-xylulose 5-phosphate synthase (DXS), two 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), two 2-C-methyl-d-erythritol 4-phosphate cytidylyltransferase (IspD), four 4-diphosphocytidyl-2-C-methyl-d-erythritol kinase (IspE), two 2-C-methyl-d-erythritol 2,4-cyclo-diphosphate synthase (IspF), four 1-hydroxy-2-methyl-2-(E)-butenyl 4-diphosphate synthase (IspG), two 1-hydroxy-2-methyl-2-(E)-butenyl 4-diphosphate reductase (IspH), six isopentenyl diphosphate isomerase (IPI), and two solanesyl diphosphate synthase (SPS) candidate genes were identified in the solanesol biosynthetic pathway. Furthermore, the two N. tabacum SPS proteins (NtSPS1 and NtSPS2), which possessed two conserved aspartate-rich DDxxD domains, were highly homologous with SPS enzymes from other solanaceous plant species. In addition, the solanesol contents of three organs and of leaves from four growing stages of tobacco plants corresponded with the distribution of chlorophyll. Our findings provide a comprehensive evaluation of the correlation between the expression of different biosynthesis genes and the accumulation of solanesol, thus providing valuable insight into the regulation of solanesol biosynthesis in tobacco. Full article
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Open AccessArticle Medium Optimization and Fermentation Kinetics for κ-Carrageenase Production by Thalassospira sp. Fjfst-332
Molecules 2016, 21(11), 1479; doi:10.3390/molecules21111479
Received: 11 August 2016 / Revised: 17 October 2016 / Accepted: 31 October 2016 / Published: 5 November 2016
Cited by 2 | PDF Full-text (8440 KB) | HTML Full-text | XML Full-text
Abstract
Effective degradation of κ-carrageenan by isolated Thalassospira sp. fjfst-332 is reported for the first time in this paper. It was identified by 16S rDNA sequencing and morphological observation using Transmission Electron Microscopy (TEM). Based on a Plackett–Burman design for significant variables, Box–Behnken experimental
[...] Read more.
Effective degradation of κ-carrageenan by isolated Thalassospira sp. fjfst-332 is reported for the first time in this paper. It was identified by 16S rDNA sequencing and morphological observation using Transmission Electron Microscopy (TEM). Based on a Plackett–Burman design for significant variables, Box–Behnken experimental design and response surface methodology were used to optimize the culture conditions. Through statistical optimization, the optimum medium components were determined as follows: 2.0 g/L κ-carrageenan, 1.0 g/L yeast extract, 1.0 g/L FOS, 20.0 g/L NaCl, 2.0 g/L NaNO3, 0.5 g/L MgSO4·7H2O, 0.1 g/L K2HPO4, and 0.1 g/L CaCl2. The highest activity exhibited by Thalassospira sp. fjfst-332 was 267 U/mL, which makes it the most vigorous wild bacterium for κ-carrageenan production. In order to guide scaled-up production, two empirical models—the logistic equation and Luedeking–Piretequation—were proposed to predict the strain growth and enzyme production, respectively. Furthermore, we report the fermentation kinetics and every empirical equation of the coefficients (α, β, X0, Xm and μm) for the two models, which could be used to design and optimize industrial processes. Full article
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Open AccessArticle Cytotoxic, Antitumor and Immunomodulatory Effects of the Water-Soluble Polysaccharides from Lotus (Nelumbo nucifera Gaertn.) Seeds
Molecules 2016, 21(11), 1465; doi:10.3390/molecules21111465
Received: 10 October 2016 / Revised: 25 October 2016 / Accepted: 28 October 2016 / Published: 2 November 2016
Cited by 3 | PDF Full-text (4601 KB) | HTML Full-text | XML Full-text
Abstract
Lotus is an edible and medicinal plant, and the extracts from its different parts exhibit various bioactivities. In the present study, the hot water–soluble polysaccharides from lotus seeds (LSPS) were evaluated for their cancer cell cytotoxicity, immunomodulatory and antitumor activities. LSPS showed significant
[...] Read more.
Lotus is an edible and medicinal plant, and the extracts from its different parts exhibit various bioactivities. In the present study, the hot water–soluble polysaccharides from lotus seeds (LSPS) were evaluated for their cancer cell cytotoxicity, immunomodulatory and antitumor activities. LSPS showed significant inhibitory effects on the mouse gastric cancer MFC cells, human liver cancer HuH-7 cells and mouse hepatocarcinoma H22 cells. The animal studies showed that LSPS inhibited tumor growth in H22 tumor-bearing mice with the highest inhibition rate of 45.36%, which is comparable to that induced by cyclophosphamide (30 mg/kg) treatment (50.79%). The concentrations of white blood cells were significantly reduced in cyclophosphamide-treated groups (p < 0.01), while LSPS showed much fewer side effects according to the hematology analysis. LSPS improved the immune response in H22 tumor-bearing mice by enhancing the spleen and thymus indexes, and increasing the levels of serum cytokines including tumor necrosis factor-α and interleukin-2. Moreover, LSPS also showed in vivo antioxidant activity by increasing superoxide dismutase activity, thus reducing the malondialdehyde level in the liver tissue. These results suggested that LSPS can be used as an antitumor and immunomodulatory agent. Full article
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Open AccessArticle In Vitro Study on Anti-Hepatitis C Virus Activity of Spatholobus suberectus Dunn
Molecules 2016, 21(10), 1367; doi:10.3390/molecules21101367
Received: 27 August 2016 / Revised: 7 October 2016 / Accepted: 9 October 2016 / Published: 15 October 2016
Cited by 2 | PDF Full-text (3443 KB) | HTML Full-text | XML Full-text
Abstract
Hepatitis C virus (HCV) infects 200 million people worldwide, and 75% of HCV cases progress into chronic infections, which consequently cause cirrhosis and hepatocellular carcinoma. HCV infection is treated with currently considered standard drugs, including direct anti-viral agents (DAAs), alone or in combination
[...] Read more.
Hepatitis C virus (HCV) infects 200 million people worldwide, and 75% of HCV cases progress into chronic infections, which consequently cause cirrhosis and hepatocellular carcinoma. HCV infection is treated with currently considered standard drugs, including direct anti-viral agents (DAAs), alone or in combination with peginterferon-α plus ribavirin. However, sustained viral responses vary in different cohorts, and high costs limit the broad use of DAAs. In this study, the ethanol and water extracts of 12 herbs from Lingnan in China were examined in terms of their inhibitory effect on HCV replication. Among the examined extracts, Spatholobus suberectus ethanol extracts suppressed HCV replication. By comparison, Extracts from Fructus lycii, Radix astragali (root), Rubus chingii Hu (fruit), Flos chrysanthemi Indici (flower), Cassia obtusifolia (seed), Lonicera japonica Thunb (flower), Forsythia suspense Thunb (fruit), Poria cocos (sclerotia), Carthamus tinctorius L. (flower), Crataegus pinnatifida Bge. (fruit), and Leonurus japonicas Houtt. (leaf) extracts failed to show a similar activity. Active S. suberectus fractions containing tannins as the major component also inhibited the in vitro translation of HCV RNA. The combination treatments of single compounds, such as epigallocatechin gallate and epicatechin gallate, were not as potent as crude S. suberectus fractions; therefore, crude S. suberectus extract may be a potential alternative treatment against HCV either alone or in combination with other agents. Full article
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Open AccessArticle Nujiangexathone A, a Novel Compound Derived from Garcinia nujiangensis, Induces Caspase-Dependent Apoptosis in Cervical Cancer through the ROS/JNK Pathway
Molecules 2016, 21(10), 1360; doi:10.3390/molecules21101360
Received: 19 August 2016 / Revised: 20 September 2016 / Accepted: 29 September 2016 / Published: 12 October 2016
PDF Full-text (5264 KB) | HTML Full-text | XML Full-text
Abstract
Nujiangexathone A (NJXA), a novel compound derived from Garcinia nujiangensis, has been demonstrated to inhibit the proliferation of several human cancer cell lines. This study is the first to demonstrate the apoptosis inductive activities of NJXA and the possible underlying mechanisms. Our
[...] Read more.
Nujiangexathone A (NJXA), a novel compound derived from Garcinia nujiangensis, has been demonstrated to inhibit the proliferation of several human cancer cell lines. This study is the first to demonstrate the apoptosis inductive activities of NJXA and the possible underlying mechanisms. Our results demonstrated that NJXA inhibited colony formation by HeLa and SiHa cells in a dose-dependent manner. An Annexin V-FITC/PI staining assay showed that NJXA strongly triggered apoptosis in a dose-dependent manner. Western blotting analyses showed that NJXA induced the caspase-dependent apoptosis of HeLa and SiHa cells by triggering a series of events, including changes in the levels of Bcl-2 family proteins, cytochrome c release, caspase-3 activation, and chromosome fragmentation. Furthermore, we demonstrated that NJXA induced cell apoptosis by activating the reactive oxygen species (ROS)-mediated JNK signaling pathway. Consistent with this finding, a ROS scavenger, N-acetyl-l-cysteine (NAC, 10 mM), hindered NJXA-induced apoptosis and attenuated the sensitivity of HeLa and SiHa cells to NJXA. In vivo results further confirmed that the tumor inhibitory effect of NJXA was partially through the induction of apoptosis. Taken together, our results demonstrated that NJXA induced the apoptosis of HeLa and SiHa cells through the ROS/JNK signaling pathway, indicating that NJXA could be important candidate for the clinical treatment of cervical cancer. Full article
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Open AccessArticle Isolation of α-Amylase Inhibitors from Kadsura longipedunculata Using a High-Speed Counter-Current Chromatography Target Guided by Centrifugal Ultrafiltration with LC-MS
Molecules 2016, 21(9), 1190; doi:10.3390/molecules21091190
Received: 9 August 2016 / Revised: 5 September 2016 / Accepted: 5 September 2016 / Published: 7 September 2016
PDF Full-text (1702 KB) | HTML Full-text | XML Full-text
Abstract
In this study, a high-speed counter-current chromatography (HSCCC) separation method target guided by centrifugal ultrafiltration with high-performance liquid chromatography-mass spectrometry (CU-LC-MS) was proposed. This method was used to analyze α-amylase inhibitors from Kadsura longipedunculata extract. According to previous screening with CU-LC-MS, two screened
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In this study, a high-speed counter-current chromatography (HSCCC) separation method target guided by centrifugal ultrafiltration with high-performance liquid chromatography-mass spectrometry (CU-LC-MS) was proposed. This method was used to analyze α-amylase inhibitors from Kadsura longipedunculata extract. According to previous screening with CU-LC-MS, two screened potential α-amylase inhibitors was successfully isolated from Kadsura longipedunculata extract using HSCCC under the optimized experimental conditions. The isolated two target compounds (with purities of 92.3% and 94.6%) were, respectively, identified as quercetin-3-O-rhamnoside (1) and protocatechuic acid (2) based on the MS, UV, and 1H-NMR spectrometry data. To verify the inhibition of screened compounds, the inhibitory activities of quercetin-3-O-rhamnoside (1) and protocatechuic acid (2) on α-amylase were tested, and it demonstrated that the experimental IC50 values of quercetin-3-O-rhamnoside (1) and protocatechuic acid (2) were 28.8 and 12.5 μmol/L. These results proved that the hyphenated technique using CU-LC-MS and HSCCC was a rapid, competent, and reproductive method to screen and separate potential active compounds, like enzyme inhibitors from the extract of herbal medicines. Full article
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Open AccessArticle Molecular Encapsulation of Histamine H2-Receptor Antagonists by Cucurbit[7]Uril: An Experimental and Computational Study
Molecules 2016, 21(9), 1178; doi:10.3390/molecules21091178
Received: 17 July 2016 / Revised: 31 August 2016 / Accepted: 1 September 2016 / Published: 6 September 2016
Cited by 3 | PDF Full-text (2762 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The histamine H2-receptor antagonists cimetidine, famotidine and nizatidine are individually encapsulated by macrocyclic cucurbit[7]uril (CB[7]), with binding affinities of 6.57 (±0.19) × 103 M−1, 1.30 (±0.27) × 104 M−1 and 1.05 (±0.33) × 105 M
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The histamine H2-receptor antagonists cimetidine, famotidine and nizatidine are individually encapsulated by macrocyclic cucurbit[7]uril (CB[7]), with binding affinities of 6.57 (±0.19) × 103 M−1, 1.30 (±0.27) × 104 M−1 and 1.05 (±0.33) × 105 M−1, respectively. These 1:1 host-guest inclusion complexes have been experimentally examined by 1H-NMR, UV-visible spectroscopic titrations (including Job plots), electrospray ionization mass spectrometry (ESI-MS), and isothermal titration calorimetry (ITC), as well as theoretically by molecular dynamics (MD) computation. This study may provide important insights on the supramolecular formulation of H2-receptor antagonist drugs for potentially enhanced stability and controlled release based on different binding strengths of these host-guest complexes. Full article
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Open AccessArticle Characterization and Prebiotic Effect of the Resistant Starch from Purple Sweet Potato
Molecules 2016, 21(7), 932; doi:10.3390/molecules21070932
Received: 18 June 2016 / Revised: 9 July 2016 / Accepted: 12 July 2016 / Published: 19 July 2016
Cited by 5 | PDF Full-text (1377 KB) | HTML Full-text | XML Full-text
Abstract
Purple sweet potato starch is a potential resource for resistant starch production. The effects of heat-moisture treatment (HMT) and enzyme debranching combined heat-moisture treatment (EHMT) on the morphological, crystallinity and thermal properties of PSP starches were investigated. The results indicated that, after HMT
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Purple sweet potato starch is a potential resource for resistant starch production. The effects of heat-moisture treatment (HMT) and enzyme debranching combined heat-moisture treatment (EHMT) on the morphological, crystallinity and thermal properties of PSP starches were investigated. The results indicated that, after HMT or EHMT treatments, native starch granules with smooth surface was destroyed to form a more compact, irregular and sheet-like structure. The crystalline pattern was transformed from C-type to B-type with decreasing relative crystallinity. Due to stronger crystallites formed in modified starches, the swelling power and solubility of HMT and EHMT starch were decreased, while the transition temperatures and gelatinization enthalpy were significantly increased. In addition, HMT and EHMT exhibited greater effects on the proliferation of bifidobacteria compared with either glucose or high amylose maize starch. Full article
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Review

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Open AccessReview An Overview of Plant Phenolic Compounds and Their Importance in Human Nutrition and Management of Type 2 Diabetes
Molecules 2016, 21(10), 1374; doi:10.3390/molecules21101374
Received: 8 September 2016 / Revised: 10 October 2016 / Accepted: 12 October 2016 / Published: 15 October 2016
Cited by 14 | PDF Full-text (1357 KB) | HTML Full-text | XML Full-text
Abstract
In this paper, the biosynthesis process of phenolic compounds in plants is summarized, which includes the shikimate, pentose phosphate and phenylpropanoid pathways. Plant phenolic compounds can act as antioxidants, structural polymers (lignin), attractants (flavonoids and carotenoids), UV screens (flavonoids), signal compounds (salicylic acid
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In this paper, the biosynthesis process of phenolic compounds in plants is summarized, which includes the shikimate, pentose phosphate and phenylpropanoid pathways. Plant phenolic compounds can act as antioxidants, structural polymers (lignin), attractants (flavonoids and carotenoids), UV screens (flavonoids), signal compounds (salicylic acid and flavonoids) and defense response chemicals (tannins and phytoalexins). From a human physiological standpoint, phenolic compounds are vital in defense responses, such as anti-aging, anti-inflammatory, antioxidant and anti-proliferative activities. Therefore, it is beneficial to eat such plant foods that have a high antioxidant compound content, which will cut down the incidence of certain chronic diseases, for instance diabetes, cancers and cardiovascular diseases, through the management of oxidative stress. Furthermore, berries and other fruits with low-amylase and high-glucosidase inhibitory activities could be regarded as candidate food items in the control of the early stages of hyperglycemia associated with type 2 diabetes. Full article
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Open AccessReview Saponins from Chinese Medicines as Anticancer Agents
Molecules 2016, 21(10), 1326; doi:10.3390/molecules21101326
Received: 15 August 2016 / Accepted: 30 September 2016 / Published: 5 October 2016
Cited by 3 | PDF Full-text (667 KB) | HTML Full-text | XML Full-text
Abstract
Saponins are glycosides with triterpenoid or spirostane aglycones that demonstrate various pharmacological effects against mammalian diseases. To promote the research and development of anticancer agents from saponins, this review focuses on the anticancer properties of several typical naturally derived triterpenoid saponins (ginsenosides and
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Saponins are glycosides with triterpenoid or spirostane aglycones that demonstrate various pharmacological effects against mammalian diseases. To promote the research and development of anticancer agents from saponins, this review focuses on the anticancer properties of several typical naturally derived triterpenoid saponins (ginsenosides and saikosaponins) and steroid saponins (dioscin, polyphyllin, and timosaponin) isolated from Chinese medicines. These saponins exhibit in vitro and in vivo anticancer effects, such as anti-proliferation, anti-metastasis, anti-angiogenesis, anti-multidrug resistance, and autophagy regulation actions. In addition, related signaling pathways and target proteins involved in the anticancer effects of saponins are also summarized in this work. Full article
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