ABSTRACT
This study aimed to explore the characteristics of Pickering emulsions stabilized by tea water-insoluble protein nanoparticles (TWIPNs) at different pH values. The characteristics of TWIPNs at different pH values were analysed first. The average hydrodynamic diameter of TWIPNs in the suspension was smaller than 400 nm at pH 7-11. TWIPNs at pH 3 could not be used to stabilize Pickering emulsions. The flocculation index (FI) of fresh TWIPN-stabilized Pickering emulsions (TWIPNPEs) at pH 5 was higher than those of TWIPNPEs at pH 7-11 (FI < 5%), indicating that bridging flocculation led to the aggregation of small emulsion droplets. The zeta potential of TWIPNPEs at pH 7-11 did not change after 7 d. In addition, the TWIPNPEs showed gel-like properties under neutral and alkaline conditions. These results will be helpful for broadening the application of TWIPNPEs at different pH values.
Subject(s)
Nanoparticles , Water , Emulsions , Hydrogen-Ion Concentration , Particle Size , TeaABSTRACT
Resveratrol exists widely in plant species and has a variety of anti-oxidant, anti-inflammatory, and immunomodulatory properties. However, there have been few reports regarding its anti-food allergic activity. In this study, we demonstrated that resveratrol (isolated from Abies georgei) could decrease the release of ß-hexosaminidase and histamine in rat basophilic leukemia-2H3 cells. Resveratrol was not only found to suppress the development of diarrhea, up-regulate the rectal temperature of ovalbumin-allergic mice, and decrease the serum level of specific immunoglobulin E, mouse mast cell protease-1 and histamine, but also found to decrease the population of dendritic cells, B cells and mast cells of ovalbumin -allergic mice in the spleen or mesenteric lymph node. Furthermore, resveratrol inhibited the release of ß-hexosaminidase and histamine in bone marrow-derived cells and alleviated mast cell-mediated passive cutaneous anaphylaxis reactions. These findings indicated that resveratrol isolated from Abies georgei might have the potential to alleviate food hypersensitivity or allergic disease.
Subject(s)
Abies/chemistry , Anti-Allergic Agents/administration & dosage , Food Hypersensitivity/drug therapy , Mast Cells/drug effects , Plant Extracts/administration & dosage , Resveratrol/administration & dosage , Animals , B-Lymphocytes/drug effects , B-Lymphocytes/immunology , Cell Line , Disease Models, Animal , Female , Food Hypersensitivity/etiology , Food Hypersensitivity/immunology , Histamine/immunology , Humans , Immunoglobulin E/immunology , Mast Cells/immunology , Mice , Mice, Inbred BALB C , Ovalbumin/adverse effects , Passive Cutaneous Anaphylaxis/drug effects , Peptide Hydrolases/immunology , Rats , beta-N-Acetylhexosaminidases/immunologyABSTRACT
Although dietary polyphenols are known to be beneficial to vision, the protective distinctions among different types of polyphenols are unclear. In this work, the visual benefits of various blueberry polyphenols were evaluated using an in vitro model of visible light-lipid-induced injury of retinal pigment epithelial cells. Results showed that, at 10.0 µg/mL, the phenolic acid-rich fraction was superior in inhibiting cell death (93.6% ± 2.8% of cell viability). Anthocyanin- and flavonoid-rich fractions shared similar advantages in preventing the expression of senescence-associated ß-galactosidase (34.8% ± 11.1% and 32.2% ± 9.7% of aged cells, respectively) and overexpression of vascular endothelial growth factor (51.8 ± 3.5 and 54.1 ± 6.5 pg/mL, respectively). The flavonoid-rich fraction also showed high activity in ameliorating phagocytosis (70.3% ± 12.6%) and cellular oxidative stress. These results were further confirmed by using the corresponding polyphenol standards. Improved inhibitory effects of polyphenol mixture on cell death and senescence-associated ß-galactosidase expression were also observed. Therefore, various polyphenols play diverse roles and exert synergistic effects in nourishing the retina.
Subject(s)
Blueberry Plants/chemistry , Lipids/adverse effects , Plant Extracts/pharmacology , Polyphenols/pharmacology , Retinal Pigment Epithelium/drug effects , Cell Line , Epithelial Cells/drug effects , Epithelial Cells/metabolism , Fruit/chemistry , Humans , Light/adverse effects , Oxidative Stress/drug effects , Retinal Pigment Epithelium/injuries , Retinal Pigment Epithelium/metabolism , Vascular Endothelial Growth Factor A/genetics , Vascular Endothelial Growth Factor A/metabolism , beta-Galactosidase/genetics , beta-Galactosidase/metabolismABSTRACT
BACKGROUND: Identifying targets of herbs is a primary step for investigating pharmacological mechanisms of herbal drugs in Traditional Chinese medicine (TCM). Experimental targets identification of herbs is a difficult and time-consuming work. Computational method for identifying herb targets is an efficient approach. However, how to make full use of heterogeneous network data about herbs and targets to improve the performance of herb targets prediction is still a dilemma. METHODS: In our study, a random walk algorithm on the heterogeneous herb-target network (named heNetRW) has been proposed to identify protein targets of herbs. By building a heterogeneous herb-target network involving herbs, targets and their interactions and simulating random walk algorithm on the network, the candidate targets of the given herb can be predicted. RESULTS: The experimental results on large-scale dataset showed that heNetRW had higher performance of targets prediction than PRINCE (improved F1-score by 0.08 and Hit@1 by 21.34% in one validation setting, and improved F1-score by 0.54 and Hit@1 by 69.08% in the other validation setting). Furthermore, we evaluated novel candidate targets of two herbs (rhizoma coptidis and turmeric), which showed our approach could generate potential targets that are valuable for further experimental investigations. CONCLUSIONS: Compared with PRINCE algorithm, heNetRW algorithm can fuse more known information (such as, known herb-target associations and pathway-based similarities of protein pairs) to improve prediction performance. Experimental results also indicated heNetRW had higher performance than PRINCE. The prediction results not only can be used to guide the selection of candidate targets of herbs, but also help to reveal the molecule mechanisms of herbal drugs.
Subject(s)
Algorithms , Drug Discovery , Drugs, Chinese Herbal , Medicine, Chinese Traditional , HumansABSTRACT
The chemical constituents from green peel of Juglans sigillata were isolated by column chomatographies over silica gel, Sephadex LH-20, and MCI. Four diarylheptanoids were isolated and their structures were characterized as dihydropterocarine(1), 3',4â³-epoxy-1-(4'-hydroxy-phenyl)-7-(3â³-methoxyl-phenyl)-heptan-3α-ol(2), pterocarine(3), and 1-(4'-hydroxy-phenyl)-7-(3â³-methoxy-4â³-hydroxyphenyl)-heptan-3α-ol(4). Compound 1 is a new compound, named as dihydropterocarine. Compounds 2-4 were isolated from the plant of J. sigillata for the first time.
Subject(s)
Diarylheptanoids/analysis , Fruit/chemistry , Juglans/chemistry , Phytochemicals/analysis , Plant ExtractsABSTRACT
Whether all dietary polyphenols nourish the eyes via oral supplementation is controversial. Given that passage of dietary polyphenols across the blood-retina barrier (BRB) is the precondition for polyphenols to exhibit ocular benefits, the BRB permeability of polyphenols was assessed in this study. Being common dietary polyphenols in fruits and vegetables, nonanthocyanin flavonoids, anthocyanins, and phenolic acids were investigated. BRB was simulated in vitro by using a differentiated retinal pigment epithelial cell monolayer cultivated on a Transwell culture system. Penetration rate was calculated by quantitatively analyzing the polyphenols in basolateral media. The BRB permeability of different polyphenols obviously (p < 0.05) differed, as follows: phenolic acids > nonanthocyanin flavonoids > anthocyanins. Glycosylation and methylation improved the BRB permeability of nonanthocyanin flavonoids and anthocyanins. However, instability and carbonylation at the C-4 position severely suppressed the BRB permeability of anthocyanins and nonanthocyanin flavonoids. Moreover, a new metabolite was discovered during penetration of anthocyanins into the BRB. However, hydrophilic phenolic acids exhibited better BRB permeability than hydrophobic ones. Data demonstrate that BRB permeability of polyphenols was determined based on structural characteristics, hydrophilicity, stability, and metabolic changes.
Subject(s)
Blood-Retinal Barrier/metabolism , Blueberry Plants/chemistry , Plant Extracts/pharmacokinetics , Polyphenols/pharmacokinetics , Retina/metabolism , Biological Transport , Cell Line , Humans , PermeabilityABSTRACT
In the present study, the anti-food allergy activity of Eucheuma cottonii sulfated oligosaccharide (ESO) was investigated. ESO was obtained by enzymatic degradation and purified by column chromatography. RBL-2H3 cells and BALB/c mouse model were used to test the anti-food allergy activity of ESO. The effects of ESO on the regulatory T (Treg) cells and bone marrow-derived mast cells (BMMCs) were investigated by flow cytometry. The results of in vivo assay showed that ESO decreased the levels of mast cell protease-1 and histamine and inhibited the levels of specific IgE by 77.7%. In addition, the production of interleukin (IL)-4 and IL-13 was diminished in the ESO groups compared to the non-ESO-treated group. Furthermore, ESO could up-regulate Treg cells by 22.2-97.1%. In conclusion, ESO decreased the allergy response in mice by reducing basophil degranulation, up-regulating Treg cells via Forkhead box protein 3 (Foxp3), and releasing IL-10. ESO may have preventive and therapeutic potential in allergic disease.
Subject(s)
Anti-Allergic Agents/administration & dosage , Food Hypersensitivity/drug therapy , Oligosaccharides/administration & dosage , Plant Extracts/administration & dosage , Rhodophyta/chemistry , Seaweed/chemistry , T-Lymphocytes, Regulatory/immunology , Animals , Anti-Allergic Agents/isolation & purification , Disease Models, Animal , Female , Food Hypersensitivity/immunology , Humans , Immunoglobulin E/immunology , Interleukin-13/immunology , Interleukin-4/immunology , Mast Cells/drug effects , Mast Cells/immunology , Mice , Mice, Inbred BALB C , Oligosaccharides/isolation & purification , Plant Extracts/isolation & purification , T-Lymphocytes, Regulatory/drug effects , Up-Regulation/drug effectsABSTRACT
Acute ischemic stroke (AIS) accounts for more than 80% of the approximately 610,000 new stroke cases worldwide every year. Both ischemia and reperfusion can cause death, damage, and functional changes of affected nerve cells, and these alterations can result in high rates of disability and mortality. Therefore, therapies aimed at increasing neuroprotection and neurorepair would make significant contributions to AIS management. However, with regard to AIS therapies, there is currently a large gap between experimental achievements and practical clinical solutions (EC-GAP-AIS). Here, by integrating curated disease-gene associations and interactome network known to be related to AIS, we investigated the molecular network mechanisms of multi-module structures underlying AIS, which might be relevant to the time frame subtypes of AIS. In addition, the EC-GAP-AIS phenomenon was confirmed and elucidated by the shortest path lengths and the inconsistencies in the molecular functionalities and overlapping pathways between AIS-related genes and drug targets. Furthermore, we identified 23 potential targets (e.g. ADORA3, which is involved in the regulation of cellular reprogramming and the extracellular matrix) and 46 candidate drugs (e.g. felbamate, methylphenobarbital and memantine) that may have value for the treatment of AIS.
Subject(s)
Disease/genetics , Drug Evaluation, Preclinical/methods , Gene Regulatory Networks , Medical Informatics/methods , Neuroprotective Agents/isolation & purification , Neuroprotective Agents/pharmacology , Stroke/drug therapy , Genetic Association Studies , HumansABSTRACT
Polysaccharides from Gracilaria lemaneiformis in particular possess various bioactive functions, but their antiallergic activity remains incompletely defined. Sulfated polysaccharide from Gracilaria lemaneiformis (GLSP) was obtained by water extraction and ethanol precipitation followed by column chromatography. BALB/c mice, RBL-2H3, and KU812 cells were used for verifying the anti food allergic activity of GLSP. According to the results of mice experiment, GLSP was able to alleviate allergy symptoms, to reduce TM-specific IgE and IgG1, to suppress Th2 cell polarization, and to promote the function of regulatory T (Treg) cells. In addition, GLSP had the ability to inhibit the function of RBL-2H3 cells. Furthermore, GLSP inhibited the activation of KU812 via suppression of p38 mitogen-activated protein kinase (MAPK). In conclusion, immunosuppression as well as the reduction in the level of p38 MAPK may contribute to GLSP's putative activity against food allergy. GLSP may be used as a functional food component for allergic patients.
Subject(s)
Anti-Allergic Agents/administration & dosage , Food Hypersensitivity/drug therapy , Gracilaria/chemistry , Plant Extracts/administration & dosage , Polysaccharides/administration & dosage , p38 Mitogen-Activated Protein Kinases/immunology , Animals , Anti-Allergic Agents/chemistry , Female , Food Hypersensitivity/genetics , Food Hypersensitivity/immunology , Humans , Immunosuppression Therapy , Mast Cells/drug effects , Mast Cells/immunology , Mice , Mice, Inbred BALB C , Plant Extracts/chemistry , Polysaccharides/chemistry , Rats , Seaweed/chemistry , Th2 Cells/drug effects , Th2 Cells/immunology , p38 Mitogen-Activated Protein Kinases/geneticsABSTRACT
With increasingly serious eye exposure to light stresses, such as light-emitting diodes, computers, and widescreen mobile phones, efficient natural compounds for preventing visible light-induced retinal damages are becoming compelling needs in the modern society. Fucoxanthin, as the main light absorption system in marine algae, may possess an outstanding bioactivity in vision protection because of its filtration of blue light and excellent antioxidative activity. In this work, both in vitro and in vivo simulated visible light-induced retinal damage models were employed. The in vitro results revealed that fucoxanthin exhibited better bioactivities than lutein, zeaxanthin, and blueberry anthocyanins in inhibiting overexpression of vascular endothelial growth factor, resisting senescence, improving phagocytic function, and clearing intracellular reactive oxygen species in retinal pigment epithelium cells. The in vivo experiment also confirmed the superiority of fucoxanthin than lutein in protecting retina against photoinduced damage. This excellent bioactivity may be attributed to its unique structural features, including allenic, epoxide, and acetyl groups. Fucoxanthin is expected to be an important ocular nutrient in the future.
Subject(s)
Laminaria/chemistry , Light/adverse effects , Plant Extracts/administration & dosage , Protective Agents/administration & dosage , Retina/radiation effects , Retinal Diseases/drug therapy , Vegetables/chemistry , Xanthophylls/administration & dosage , Animals , Cell Line , Humans , Oxidative Stress/drug effects , Oxidative Stress/radiation effects , Rabbits , Reactive Oxygen Species/metabolism , Retina/drug effects , Retina/injuries , Retina/metabolism , Retinal Diseases/metabolism , Vascular Endothelial Growth Factor A/metabolismABSTRACT
BACKGROUND: Lipid oxidation can occur in fish fillets during long-term frozen storage and cause quality and nutrition loss, which is a major concern in the seafood industry. Our previous study showed that chitosan combined with citric acid or licorice extract can have a preserving effect on fresh fish fillets stored at 4 °C. It is of interest to further study their antioxidant effects on fish fillets during frozen storage. RESULTS: Chitosan, chitosan and citric acid, chitosan and licorice extract can inhibit primary and secondary lipid oxidation, as indicated by lower peroxide value (PV) and thiobarbituric acid reactive substances (TBARS) values compared to the control samples. In addition, drip loss was decreased in the treatment samples. Both citric acid and licorice extract enhanced the antioxidant effects of chitosan. Among all the three treatments, chitosan and licorice extract showed the best antioxidant effects, reducing both PV and TBARS significantly at the end of storage. CONCLUSION: The combination of chitosan and citric acid or licorice extract showed significant antioxidant effects on ovate pompano fillets at -18 °C during 6 months of storage. They could be applied as natural antioxidant preservatives for use in seafood products or other meat products. © 2015 Society of Chemical Industry.
Subject(s)
Chitosan/pharmacology , Citric Acid/pharmacology , Food Storage/methods , Glycyrrhiza/chemistry , Lipid Peroxidation/drug effects , Perciformes , Seafood , Animals , Antioxidants/pharmacology , Food Preservation/methods , Plant Extracts/pharmacology , Thiobarbituric Acid Reactive Substances/analysisABSTRACT
The lipid peroxidation of unsaturated fatty acids (UFAs) in the retina not only threatens visual cells but also affects the physiological health of the retina. In this work, the potential damages caused by daily visible light exposure on retinal UFAs were evaluated via a simulated in vitro model. At the same time, the benefits of dietary supplementation of blueberries to the eyes were also assessed. After prolonged light exposure, lipid peroxidation occurred for both docosahexaenoic and arachidonic acids (DHA and AA, respectively). The oxidized UFAs presented obvious cytotoxicity and significantly inhibited cell growth in retinal pigment epithelium cells. Among the different blueberry polyphenol fractions, the flavonoid-rich fraction, in which quercetin was discovered as the main component, was considerably better in preventing visible light-induced DHA lipid peroxidation than the anthocyanin- and phenolic acid-rich fractions. Then the retinal protective activity of blueberry polyphenols against light-induced retinal injury was confirmed in vivo. On the basis of the above results, inhibiting lipid peroxidation of UFAs in the retina is proposed to be another important function mechanism for antioxidants to nourish eyes.
Subject(s)
Blueberry Plants/chemistry , Fatty Acids, Unsaturated/metabolism , Light/adverse effects , Plant Extracts/administration & dosage , Polyphenols/administration & dosage , Retinal Diseases/drug therapy , Animals , Dietary Supplements/analysis , Humans , Lipid Peroxidation/drug effects , Lipid Peroxidation/radiation effects , Rabbits , Retina/drug effects , Retina/metabolism , Retina/radiation effects , Retinal Diseases/etiology , Retinal Diseases/metabolismABSTRACT
OBJECTIVE: To study the anti-hepatic fibrosis effect of serum containing extracts of Periplaneta americana. METHODS: The serum contained extracts of Periplaneta americana was prepared with serologic pharmacological method. MTT method was used to observe the effect of serum containing extracts from periplaneta americana on hepatic stellate cells (HSC), and Elisa method was used to detect the contents of TGF-beta1 and collagen I in supernatant. RESULTS: Serum containing extracts I and II (15%) of Periplaneta americana had inhibitory effect on HCS (P < 0.05) after HSC were cultured with serum containing extracts of different concentration of Periolaneta americana for 24, 48 and 72 h. At 24 and 48 h, serum containing extracts I and II of Periplaneta americana decreased the content of collagen I in supernatant without significant difference (P < 0.05). Serum containing extracts I (15%, 9%, 5.4%) of Periplaneta americana could reduce generation of TGF-beta1 in supernatant for 24 h (P < 0.05). As for 48 h, only high concentration serum containing extracts I (15%) deceased the content of TGF-beta1 in supernatant. For 24 and 48 h,serum containing extracts II couldn't reduce the content of TGF-beta1 in supernatant (P < 0.05). CONCLUSION: It has definite effect on anti-hepatic fibrosis with serum containing extracts of Periplaneta americana in vitro. The mechanism may be related to inhibiting HSC propagation and reducing the production of TGF-beta1.
Subject(s)
Collagen Type I/metabolism , Hepatic Stellate Cells/metabolism , Liver Cirrhosis/pathology , Materia Medica/pharmacology , Periplaneta/chemistry , Transforming Growth Factor beta1/metabolism , Animals , Cell Line , Enzyme-Linked Immunosorbent Assay , Gene Expression Regulation/drug effects , Hepatic Stellate Cells/drug effects , Liver Cirrhosis/metabolism , Male , Materia Medica/isolation & purification , Random Allocation , Rats , Rats, Wistar , Serum/chemistryABSTRACT
The recent research progress of the utilization of natural drugs for the treatment of liver fibrosis in China and other countries was reviewed. Forty reported remedies were summarized and classified into 3 categories, that is, the single herbal drugs (rhizome, leaf, fruit, bark, peel, flower, whole plants, and oil), traditional Chinese medicine prescriptions and animal drugs. The future directions of the R&D of new natural drugs against liver fibrosis were discussed and some suggestions were provided.
Subject(s)
Biological Products/therapeutic use , Biomedical Research/methods , Liver Cirrhosis/drug therapy , Medicine, Chinese Traditional/methods , Animals , Biomedical Research/trends , China , Drugs, Chinese Herbal/therapeutic use , Humans , Medicine, Chinese Traditional/trends , PhytotherapyABSTRACT
The anti-HIV activities of a pine cone extract (YNS-PY-F) from Pinus yunnanensis have been evaluated, and its mechanisms of action were also explored. The pine cone extract, YNS-PY-F, potently inhibited HIV-1(IIIB), HIV-1(RF), HIV-1(A17), HIV-1(AO18) and HIV-2(ROD) and induced cytopathic effect in C8166 cells with EC50 values of 0.96 µg/mL, 1.53 µg/mL, 0.88 µg/mL, 7.20 µg/mL and 6.17 µg/mL, respectively. The quantification of a p24 production assay showed that YNS-PY-F significantly inhibited the acute replication of HIV-1(IIIB), HIV-1RF, HIV-1(A17) and HIV-1(AO18) in C8166 cells. An MTT assay showed that YNS-PY-F also significantly inhibited the HIV-1(IIIB) induced cytolysis in MT-4 cells with an EC50 value of 2.22 µg/mL. The mechanism assays showed that YNS-PY-F had potent inhibitory effects on the fusion between infected cells and uninfected cells, and the activity of HIV-1 reverse transcriptase, with EC50 values of 7.60 µg/mL and 4.60 µg/mL, respectively. Overall, these data suggest that the pine cone extract from Pinus yunnanensis has potent inhibitory activities against HIV-1(IIIB), HIV-1(RF), RT inhibitor-resistant strains HIV-1(A17) and HIV-1(AO18), and HIV-2(ROD), and its anti-HIV mechanisms include inhibition of HIV entry and inhibition of reverse transcriptase activity.
Subject(s)
Anti-HIV Agents/pharmacology , Pinus/chemistry , Plant Extracts/pharmacology , Anti-HIV Agents/chemistry , Anti-HIV Agents/toxicity , Cell Line , Cell Nucleus/metabolism , Chemokine CXCL12/metabolism , HIV Integrase/metabolism , HIV Reverse Transcriptase/antagonists & inhibitors , HIV-1/drug effects , Humans , Microbial Sensitivity Tests , Plant Extracts/chemistry , Plant Extracts/toxicity , Protein Transport , Receptors, CXCR4/metabolism , Virus Internalization/drug effectsABSTRACT
Twenty-nine phenolic compounds were isolated from the root bark of fresh (Yunnan) ginger and their structures fully characterized. Selected compounds were divided into structural categories and twelve compounds subjected to in-vitro assays including DPPH radical scavenging, xanthine-oxidase inhibition, monoamine oxidase inhibition, rat-brain homogenate lipid peroxidation, and rat pheochromocytoma PC12 cell and primary liver cell viability to determine their antioxidant and cytoprotective properties. Isolated compounds were also tested against nine human tumor cell lines to characterize anticancer potency. Several diarylheptanoids and epoxidic diarylheptanoids were effective DPPH radical scavengers and moderately effective at inhibiting xanthine oxidase. An enone-dione analog of 6-shogaol (compound 2) was isolated and identified to be most effective at protecting PC12 cells from H2O2-induced damage. Almost all tested compounds inhibited lipid peroxidation. Three compounds, 6-shogaol, 10-gingerol and an enone-diarylheptanoid analog of curcumin (compound 6) were identified to be cytotoxic in cell lines tested, with KB and HL60 cells most susceptible to 6-shogaol and the curcumin analog with IC50<10 µM. QSAR analysis revealed cytotoxicity was related to compound lipophilicity and chemical reactivity. In conclusion, we observed distinct compounds in fresh ginger to have biological activities relevant in diseases associated with reactive oxygen species.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/pharmacology , Catechols/pharmacology , Neoplasms/drug therapy , Phenols/pharmacology , Plant Extracts/pharmacology , Zingiber officinale/chemistry , Animals , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/therapeutic use , Antioxidants/isolation & purification , Antioxidants/therapeutic use , Biphenyl Compounds/metabolism , Catechols/isolation & purification , Catechols/therapeutic use , Curcumin/isolation & purification , Curcumin/pharmacology , Curcumin/therapeutic use , Cytoprotection , Fatty Alcohols/isolation & purification , Fatty Alcohols/pharmacology , Fatty Alcohols/therapeutic use , HL-60 Cells , Humans , Hydrogen Peroxide , Hydrophobic and Hydrophilic Interactions , KB Cells , Lipid Peroxidation/drug effects , PC12 Cells , Phenols/isolation & purification , Phenols/therapeutic use , Phytotherapy , Picrates/metabolism , Plant Bark , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Plant Roots , Rats , Xanthine Oxidase/metabolismABSTRACT
Two coriamyrtin-type sesquiterpenes, fengfangin A (1) and tutin (2), and six diarylheptanoids, namely alnusone (3), centrolobol (4), muricarpone B (5), 1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptan-3-one (6), (3S)-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptan-3-ol (7), and (3S)-1-(4-hydroxyphenyl)-7-(3,4-dihydroxyphenyl)heptan-3-ol (8), were isolated from the 95% EtOH extract of nidus vespae, the nest of Polistes species. Their structures were identified by spectroscopic methods. Compounds 1 and 8 are new products. The absolute configuration of 1 was determined by single-crystal X-ray diffraction analysis using Flack parameter. The biological tests showed that compounds 5, 6, and 8 could inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells with IC(50) values in the range of 13-17 µM, whereas the sesquiterpenes were inactive in this assay (>25 µM). In addition, the ecological significance of the presence of neurotoxic sesquiterpene lactones in nidus vespae is briefly discussed.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Diarylheptanoids/isolation & purification , Nitric Oxide/adverse effects , Sesquiterpenes/isolation & purification , Wasps/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Cell Line , Diarylheptanoids/chemistry , Diarylheptanoids/pharmacology , Macrophages/drug effects , Macrophages/metabolism , Medicine, Chinese Traditional , Mice , Models, Molecular , Molecular Structure , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , Wasps/growth & developmentABSTRACT
Three new triterpenoid glycosides, named puberosides C-E (1-3), were isolated from the water-soluble fraction of Glochidion puberum (Linn.) Hutch. Their structures were determined as 3α-[(O-ß-d-glucopyranosyl-(1 â 3)-O-α-l-arabinopyranosyl)oxy]-22α-trans-cinnamoyl-olean-12-ene-16α,28-diol, 3α-[(O-ß-d-glucopyranosyl-(1 â 3)-O-α-l-arabinopyranosyl)oxy]-22α-cis-cinnamoyl-olean-12-ene-16α,28-diol, and 3α-[(O-ß-d-glucopyranosyl-(1 â 3)-O-ß-d-glucopyranosyl)oxy]-22α-benzoyloxy-olean-12-ene-16α,28-diol by the combination of 1D, 2D NMR, and MS spectral analyses.
Subject(s)
Drugs, Chinese Herbal/isolation & purification , Euphorbiaceae/chemistry , Saponins/isolation & purification , Triterpenes/isolation & purification , Drugs, Chinese Herbal/chemistry , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Saponins/chemistry , Stereoisomerism , Triterpenes/chemistryABSTRACT
The organic extract of Periplaneta americana L. (Dictyoptera; Blattidae) has been traditionally used in southwestern China as an alternative medicine against disorders such as hepatitis, trauma, gastric ulcers, burns, and heart disease. The present study describes bioassay-guided purification and chemotherapeutic evaluation of the 60% ethanolic fraction of P americana organic extracts (PAE60). The most effective cytotoxic fraction was determined by way of repeated in vitro screenings against 12 distinct cultured human carcinoma cell lines: Eca 109, BGC823, HO8910, LS174T, CNE, HeLa, K562, PC-3, A549, BEL 7404, HL-60, and KB, followed by in vivo antitumor assays of the lead fraction (PAE60). The complexity of enriched active fraction was qualitatively evaluated using thin layer chromatography. Reconstituted PAE60 was effective at inhibiting HL-60, KB, CNE, and BGC823 cell growth with IC(50) values <20 µg mL-(1). PAE60 reduced tumor growth in S180-bearing immunocompetent mice by 72.62% after 10 days following oral doses of 500 mg kg d-(1) compared with 78.75% inhibition following 40 mg kg d-(1) of cyclophosphamide (CTX). Thymus and spleen indices of S180-bearing mice treated with PAE60 were significantly greater (P < .05) than CTX treatment groups, suggesting potential immunomodulation of antitumor host defenses by PAE60. Antiviral activity was also investigated and PAE60 inhibited herpes simplex type-2 replication (IC(50) = 4.11 ± 0.64 µg mL-(1)) with a selectivity index (CC(50) to IC(50) ratio) of 64.84 in Vero cells but was less effective on type-1 virus (IC(50) of 25.6 ± 3.16 µg mL-(1)). These results support future clinical trials on P. americana as an alternative or complementary medicinal agent.
Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Periplaneta/chemistry , Tissue Extracts/chemistry , Tissue Extracts/pharmacology , Animals , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Cell Line, Tumor , Chlorocebus aethiops , Cyclophosphamide/pharmacology , Drug Screening Assays, Antitumor , HL-60 Cells , HeLa Cells , Herpesvirus 1, Human/drug effects , Herpesvirus 2, Human/drug effects , Humans , K562 Cells , KB Cells , Male , Mice , Mice, Inbred BALB C , Mice, Inbred ICR , Random Allocation , Vero CellsABSTRACT
A rare type of phenolic compound, namely, planchol E (1), was isolated from the cones and seeds of Pinus yunnanensis together with 16 known abietane diterpenoids (2-17). The structure of planchol E was established on the basis of extensive spectroscopic analysis, and it was found that the new compound did not show cytotoxic activity against several cancer cell lines.