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1.
Food Funct ; 12(20): 10023-10039, 2021 Oct 19.
Article in English | MEDLINE | ID: mdl-34523644

ABSTRACT

Brassica rapa L. is one of the most popular traditional foods with a variety of biological activities. In this study, the petroleum ether extract of B. rapa was separated by silica gel column chromatography, and named BRPS, which was identified by LC-MS. The effects and pharmacological mechanisms of BRPS on the treatment of lung cancer were investigated both in vitro and in vivo. The results showed that BRPS significantly inhibited the proliferation of both human lung cancer A549 and mouse lung cancer LLC cells, while its toxicity to normal cells was lower than that of cancer cells. BRPS induced cell cycle arrest at the G2/M phase and significantly reduced the levels of CDK1 and CyclinB1 in A549 cells. Moreover, BRPS induced apoptosis in a dose-dependent manner, and increased the Bax/Bcl-2 ratio, while it decreased mitochondrial membrane potential, promoted the release of cytochrome c, activated caspase 9 and 3, and enhanced the degradation of PARP in A549 cells. Furthermore, the levels of reactive oxygen species (ROS) were also upregulated by BRPS and ROS inhibitor reversed BRPS-induced apoptosis. Importantly, BRPS significantly suppressed the growth of LLC cells in vivo without any obvious side effect on body weight and organs of mice, and increased the proportion of B cells, CD4+ T cells, CD8+ T cells and CD44+CD8+ T cells in the spleen. These results revealed that BRPS inhibited the growth of lung cancer cells through inducing cell cycle arrest, mitochondria-dependent apoptosis, and activating immunity of mice, and BRPS might be a potential anti-tumor functional food and promising agent for the treatment of lung cancer.


Subject(s)
Adenocarcinoma of Lung/drug therapy , Alkanes/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Brassica rapa/chemistry , Lung Neoplasms/drug therapy , A549 Cells , Adenocarcinoma of Lung/metabolism , Animals , Caspases/metabolism , Cell Cycle Checkpoints/drug effects , Cell Proliferation/drug effects , Female , Humans , Lung Neoplasms/metabolism , Membrane Potential, Mitochondrial/drug effects , Mice , Mice, Inbred C57BL , Mitochondria/drug effects , Plant Extracts/pharmacology , Reactive Oxygen Species/metabolism
2.
Eur J Pharmacol ; 902: 174110, 2021 Jul 05.
Article in English | MEDLINE | ID: mdl-33901457

ABSTRACT

There is an almost unlimited interest in searching and developing new drugs, especially when we are in an era that are witnessing more and more emerging pathogens. Natural products from traditional medicines represent a large library for searching lead compounds with novel bioactivities. Sodium houttuyfonate is such one bioactive compound derived from Houttuynia cordata Thunb which has been employed in traditional medicine for treating infectious and inflammatory diseases. Sodium houttuyfonate has demonstrated multiple kinds of pharmacological effects, including antifungal, antibacterial, anti-inflammatory, and cardiovascular protective activities, which are discussed here to provide insights into our understanding of the pharmacological effects of SH and the underlying mechanisms.


Subject(s)
Alkanes/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antifungal Agents/pharmacology , Cardiotonic Agents/pharmacology , Sulfites/pharmacology , Alkanes/adverse effects , Alkanes/chemistry , Alkanes/therapeutic use , Animals , Anti-Bacterial Agents/adverse effects , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/therapeutic use , Anti-Inflammatory Agents/adverse effects , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/therapeutic use , Antifungal Agents/adverse effects , Antifungal Agents/chemistry , Antifungal Agents/therapeutic use , Cardiotonic Agents/adverse effects , Cardiotonic Agents/chemistry , Cardiotonic Agents/therapeutic use , Houttuynia/chemistry , Humans , Sulfites/adverse effects , Sulfites/chemistry , Sulfites/therapeutic use
3.
J Leukoc Biol ; 110(5): 927-937, 2021 11.
Article in English | MEDLINE | ID: mdl-33682190

ABSTRACT

Inflammatory bowel disease (IBD) including Crohn's disease and ulcerative colitis is a chronic intestinal disease most likely associated with gut dysbiosis. Candida related mycobiota has been demonstrated to play a role in IBD progression. Traditional Chinese herbal medicines (TCHMs) with antifungal activity have a potential in prevention and treatment of fungi-related IBD. Sodium houttuyfonate (SH) is a promising anti-Candida TCHMs. In this study, a dextran sulfate sodium induced colitis model with Candida albicans precolonization is established. SH gavage can significantly decrease the fungal burdens in feces and colon tissues, reduce disease activity index score, elongate colon length, and attenuate colonic damages. Moreover, SH markedly inhibits the levels of anti-Saccharomyces cerevisiae antibodies, ß-glucan, and proinflammatory cytokine (IL-1ß, IL-6, IL-8, TNF-α), and increases anti-inflammatory factor IL-10 level in serum and colon tissue. Further experiments demonstrate that SH could induce ß-glucan exposure, priming intestinal macrophages to get rid of colonized C. albicans through the collaboration of Dectin-1 and TLR2/4. With the decreased fungal burden, the protein levels of Dectin-1, TLR2, TLR4, and NF-κBp65 are fallen back, indicating the primed macrophages calm down and the colitis is alleviated. Collectively, these results manifest that SH can attenuate C. albicans associated colitis via ß-glucan exposure, deepening our understanding of TCHMs in the prevention and treatment of fungi associated IBD.


Subject(s)
Alkanes/pharmacology , Candida albicans/drug effects , Colitis/microbiology , Gastrointestinal Microbiome/drug effects , Sulfites/pharmacology , Animals , Colitis/chemically induced , Dextran Sulfate/toxicity , Dysbiosis/microbiology , Mice , beta-Glucans
4.
Biofouling ; 36(3): 319-331, 2020 03.
Article in English | MEDLINE | ID: mdl-32410461

ABSTRACT

Traditional herbal monomers (THMs) are widely distributed in many traditional Chinese formulas (TCFs) and decoctions (TCDs) and are frequently used for the prevention and treatment of fungal infections. The antifungal activities of five common THMs, including sodium houttuyfonate (SH), berberine (BER), palmatine (PAL), jatrorrhizine (JAT) and cinnamaldehyde (CIN), and their potential for inducing cell wall remodeling (CWR), were evaluated against Candida albicans SC5314 and Candida auris 12372. SH/CIN plus BER/PAL/JAT showed synergistic antifungal activity against both Candida isolates. Furthermore, SH-associated combinations (SH plus BER/PAL/JAT) induced stronger exposure of ß-glucan and chitin than their counterparts, while CIN triggered more marked exposure compared with CIN-associated combinations (CIN plus BER/PAL/JAT). Collectively, this study demonstrated the anti-Candida effect and the CWR induction potential of the five THMs and their associated combinations, providing a possibility of their in vivo application against fungal-associated infections.


Subject(s)
Antifungal Agents/pharmacology , Candida albicans/drug effects , Candida/drug effects , Cell Wall/drug effects , Drugs, Chinese Herbal/pharmacology , Acrolein/analogs & derivatives , Acrolein/pharmacology , Alkanes/pharmacology , Berberine/analogs & derivatives , Berberine/pharmacology , Berberine Alkaloids/pharmacology , Humans , Microbial Sensitivity Tests , Sulfites/pharmacology
5.
Mol Biol Rep ; 46(1): 471-477, 2019 Feb.
Article in English | MEDLINE | ID: mdl-30511304

ABSTRACT

Biofilm dispersion is the last step in the development of biofilms, and allows bacteria to spawn novel biofilms in new locales. In the previous studies, we found that sodium houttuyfonate (SH) is effective at inhibiting biofilm formation and motility of Pseudomonas aeruginosa. Here, we investigated the effect of SH against the biofilm dispersion of P. aeruginosa by an in vitro model. The results show that the plant derivative, SH, could effectively inhibit both biofilm dispersion of P. aeruginosa, and gene and protein expression of the key biofilm regulator BdlA in a dose-dependent manner. Furthermore, our presented results suggest that SH can penetrate into the biofilm of P. aeruginosa to repress the biofilm life cycle. Therefore, these results indicate that the antimicrobial activity of SH may be partially due to its ability to disrupt biofilm dispersion in P. aeruginosa.


Subject(s)
Alkanes/pharmacology , Biofilms/drug effects , Pseudomonas aeruginosa/drug effects , Sulfites/pharmacology , Alkanes/metabolism , Anti-Bacterial Agents/pharmacology , Bacterial Proteins/genetics , Pseudomonas aeruginosa/metabolism , Sulfites/metabolism
6.
Zhongguo Zhong Yao Za Zhi ; 42(11): 2131-2138, 2017 Jun.
Article in Chinese | MEDLINE | ID: mdl-28822159

ABSTRACT

Quorum sensing of bacteria and its specific gene expression regulation have a very important role in bacterial biofilm formation. LuxS and agr are the key regulatory genes in quorum sensing of Staphylococcus epidermidis, and RNA Ⅲ is the effector molecule of agr system. In order to evaluate the effects of sodium houttuyfonate in combination with erythromycin on the transcription level of S. epidermidis, serial dilution method was used to determine the MIC of sodium houttuyfonate, erythromycin and vancomycin on S. epidermidis, and fluorescent quantitative PCR method was used to detect the transcription levels of luxS, agr/RNAⅢ in different time periods after treatment on S. epidermidis by sodium houttuyfonate in combination with erythromycin, vancomycin, and erythromycin alone. Our results showed that in treatment by 1/2MIC, 1/4MIC sodium houttuyfonate, 1/2MIC sodium houttuyfonate +1/2MIC erythromycin, 1/4MIC sodium houttuyfonate+1/4MIC erythromycin, and 1/8MIC sodium houttuyfonate+1/8MIC erythromycin for ATCC 35984, they could rapidly up-regulate the expression of luxS of S. epidermidis from the beginning as compared with negative control, with significant differences (P<0.05); furthermore, sodium houttuyfonate can still up-regulate the expression of luxS even after treatment for 6, 12 and 48 h. Sodium houttuyfonate in MIC and 1/2MIC concentration can significantly down-regulate the expression of agr (P<0.05); 1/2MIC sodium houttuyfonate+1/2MIC erythromycin, 1/4MIC sodium houttuyfonate+1/4MIC erythromycin, can also significantly down-regulate the expression of agr in 6 h, 12 h and 24 h(P<0.05). Sodium houttuyfonate in MIC, can significantly down-regulate the expression of RNA Ⅲ (P<0.05), and 1/2MIC sodium houttuyfonate+1/2MIC erythromycin can also significantly down-regulate the expression of RNAⅢ(P<0.05). Therefore, our presented results showed that sodium houttuyfonate in combination with erythromycin can rapidly up-regulate the transcription of luxS of S. epidermidis, and can down-regulate the expression of agr/RNA Ⅲ in certain concentrations, and suggested that sodium houttuyfonate in combination of erythromycin could inhibit mutual aggregation between S. epidermidis and biofilm bacteria, inhibit membrane nutrition and formation of water transport channels, prevent separation of bacterial cells in biofilm, and inhibit the formation of bacterial exotoxin of S. epidermidis.


Subject(s)
Alkanes/pharmacology , Erythromycin/pharmacology , Staphylococcus epidermidis/drug effects , Sulfites/pharmacology , Bacterial Proteins/metabolism , Biofilms , Carbon-Sulfur Lyases/metabolism , Microbial Sensitivity Tests , RNA, Bacterial/metabolism , Vancomycin/pharmacology
7.
Bull Entomol Res ; 107(3): 391-400, 2017 Jun.
Article in English | MEDLINE | ID: mdl-28132659

ABSTRACT

The importance of leaf surface wax compounds from the rice-field weed Ludwigia octovalvis (Jacq.) Raven (Onagraceae) was determined in the flea beetle Altica cyanea (Weber) (Coleoptera: Chrysomelidae). Extraction, thin layer chromatography and GC-MS and GC-FID analyses of surface waxes of young, mature and senescent leaves revealed 20, 19 and 19 n-alkanes between n-C15 and n-C35, respectively; whereas 14, 14 and 12 free fatty acids between C12:0 and C22:0 fatty acids were identified in young, mature and senescent leaves, respectively. Tricosane was predominant n-alkane in young and mature leaves, whilst eicosane predominated in senescent leaves. Heneicosanoic acid, palmitic acid and docosanoic acid were the most abundant free fatty acids in young, mature and senescent leaves, respectively. A. cyanea females showed attraction to 0.25 mature leaf equivalent surface waxes compared with young or senescent leaves in a short glass Y-tube olfactometer bioassay. The insects were attracted to a synthetic blend of 0.90, 1.86, 1.83, 1.95, 0.50 and 0.18 µg ml-1 petroleum ether of hexadecane, octadecane, eicosane, tricosane, palmitic acid and alpha-linolenic acid, respectively, comparable with the proportions as present in 0.25 mature leaf equivalent surface waxes. A. cyanea also laid eggs on a filter paper moistened with 0.25 mature leaf equivalent surface waxes or a synthetic blend of 0.90, 1.86, 1.83, 1.95, 0.50 and 0.18 µg ml-1 petroleum ether of hexadecane, octadecane, eicosane, tricosane, palmitic acid and alpha-linolenic acid, respectively. This finding could provide a basis for monitoring of the potential biocontrol agent in the field.


Subject(s)
Alkanes/pharmacology , Chemotaxis , Coleoptera/physiology , Fatty Acids/pharmacology , Onagraceae/chemistry , Oviposition/drug effects , Animals , Female , Olfactometry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Weed Control
8.
Chem Senses ; 42(3): 181-193, 2017 03 01.
Article in English | MEDLINE | ID: mdl-27916747

ABSTRACT

Key food odorants are the most relevant determinants by which we detect, recognize, and hedonically evaluate the aroma of foods and beverages. Odorants are detected by our chemical sense of olfaction, comprising a set of approximately 400 different odorant receptor types. However, the specific receptor activity patterns representing the aroma percepts of foods or beverages, as well as the key food odorant agonist profiles of single-odorant receptors, are largely unknown. We aimed to establish comprehensive key food odorant agonist profiles of 2 unrelated, broadly tuned receptors, OR1A1 and OR2W1, that had been associated thus far with mostly non-key food odorants and shared some of these agonists. By screening both receptors against 190 key food odorants in a cell-based luminescence assay, we identified 14 and 18 new key food odorant agonists for OR1A1 and OR2W1, respectively, with 3-methyl-2,4-nonanedione emerging as the most potent agonist for OR1A1 by 3 orders of magnitude, with a submicromolar half maximal effective concentration. 3-Methyl-2,4-nonanedione has been associated with a prune note in oxidized wine and is an aroma determinant in tea and apricots. Further screening against the entire set of 391 human odorant receptors revealed that 30 or 300 µmol/L 3-methyl-2,4-nonanedione activated only 1 receptor, OR1A1, suggesting a unique role of OR1A1 for the most sensitive detection of this key food odorant in wine, tea, and other food matrices.


Subject(s)
Alkanes/analysis , Diacetyl/analogs & derivatives , Odorants/analysis , Receptors, Odorant/metabolism , Tea/chemistry , Wine/analysis , Alkanes/pharmacology , Cells, Cultured , Diacetyl/analysis , Diacetyl/pharmacology , HEK293 Cells , Humans , Receptors, Odorant/agonists , Receptors, Odorant/genetics
9.
J Med Chem ; 59(10): 4831-48, 2016 05 26.
Article in English | MEDLINE | ID: mdl-27139780

ABSTRACT

Antivirulence strategies are now attracting interest for the inherent mechanism of action advantages. In our previous work, diapophytoene desaturase (CrtN) was identified to be an attractive and drugable target for fighting pigmented S. aureus infections. In this research, we developed a series of effective benzocycloalkane-derived CrtN inhibitors with submicromolar IC50. Analogue 8 blocked the pigment biosynthesis of three MRSA strains with a nanomolar IC50 value. Corresponding to its mode of action, 8 did not function as a bactericidal agent. 8 could sensitize S. aureus to immune clearance. In vivo, 8 was proven to be efficacious in an S. aureus Newman sepsis model and abscess formation model. For two typical MRSAs, USA400 MW2 and Mu50, 8 significantly decreased the staphylococcal loads in the liver and kidneys. Moreover, 8 showed minimal antifungal activity compared to that of NTF. In summary, 8 has the potential to be developed as a therapeutic drug, especially against intractable MRSA issues.


Subject(s)
Alkanes/pharmacology , Anti-Bacterial Agents/pharmacology , Drug Discovery , Enzyme Inhibitors/pharmacology , Methicillin-Resistant Staphylococcus aureus/drug effects , Oxidoreductases/antagonists & inhibitors , Staphylococcal Infections/drug therapy , Alkanes/chemical synthesis , Alkanes/chemistry , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Fungi/drug effects , Methicillin-Resistant Staphylococcus aureus/enzymology , Methicillin-Resistant Staphylococcus aureus/growth & development , Microbial Sensitivity Tests , Molecular Structure , Oxidoreductases/metabolism , Structure-Activity Relationship
10.
Bioorg Med Chem Lett ; 26(10): 2539-2543, 2016 05 15.
Article in English | MEDLINE | ID: mdl-27072909

ABSTRACT

A novel series of ferulic acid-memoquin hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). The in vitro studies showed that most of the compounds exhibited a significant ability to inhibit acetylcholinesterase (AChE) (IC50 of 3.2-34.7µM) and self-induced ß-amyloid (Aß1-42) aggregation (30.8-39.1%, 25µM), to act as potential antioxidants (ORAC-FL value of 0.9-1.3). In particular, compound 17d had the greatest ability to inhibit AChE (IC50=3.2µM), and Aß1-42 aggregation (30.8%) was also an excellent antioxidant and neuroprotectant. Moreover, it is capable of disaggregating self-induced Aß aggregation. Furthermore, 17d could cross the blood-brain barrier (BBB) in vitro. The results showed that compound 17d is a potential multifunctional agent for the treatment of AD.


Subject(s)
Alkanes/pharmacology , Alzheimer Disease/drug therapy , Cholinesterase Inhibitors/pharmacology , Coumaric Acids/pharmacology , Ethylamines/pharmacology , Neuroprotective Agents/pharmacology , Alkanes/chemistry , Amyloid beta-Peptides/metabolism , Animals , Antioxidants/chemistry , Antioxidants/pharmacology , Blood-Brain Barrier , Chemistry Techniques, Synthetic , Cholinesterase Inhibitors/chemistry , Coumaric Acids/chemistry , Drug Design , Drug Evaluation, Preclinical/methods , Ethylamines/chemistry , Humans , Hydrogen Peroxide/pharmacology , Neuroprotective Agents/chemistry , PC12 Cells , Rats
11.
Nat Prod Res ; 30(19): 2137-41, 2016 Oct.
Article in English | MEDLINE | ID: mdl-26828954

ABSTRACT

Wortmannolol (1), a new furanosteroid, along with five known compounds, wortmannolone (2), ergosterol (3), p-hydroxyphenyl ethanol (4), trans-6-dodecene (5), (2Z, 4E) -5-(8-hydroxy-1,5-dimethyl-3-oxo-6-oxabicyclo [3.2.1] octan-8-yl) -3-methylpenta-2,4-dienoic acid (6) were isolated from a fungal endophyte Talaromyces sp. lgt-4. Their structures were elucidated by IR, MS, 1D and 2D NMR spectra. Compound 1 show weak monoamine oxidase inhibitory activity.


Subject(s)
Talaromyces/chemistry , Alkanes/isolation & purification , Alkanes/pharmacology , Drug Evaluation, Preclinical/methods , Endophytes/chemistry , Ergosterol/isolation & purification , Ergosterol/pharmacology , Magnetic Resonance Spectroscopy , Molecular Structure , Monoamine Oxidase Inhibitors/chemistry , Monoamine Oxidase Inhibitors/pharmacology , Phenylethyl Alcohol/analogs & derivatives , Phenylethyl Alcohol/isolation & purification , Phenylethyl Alcohol/pharmacology , Sterols/isolation & purification , Sterols/pharmacology , Tripterygium/microbiology
12.
Nat Prod Commun ; 11(10): 1527-1530, 2016 Oct.
Article in English | MEDLINE | ID: mdl-30549614

ABSTRACT

The composition of the volatile fraction of Malva sylvestris var. mauritiana (L.) Boiss. (Malvaceae) was investigated. This plant species was cultivated in the southeastern Alps as an ingredient for herbal teas and infusions. Flowers and leaves were collected at the end of the summer season and separately steam- distilled to obtain two volatile oils, the yields of which were 0.019% for leaves and 0.012% for flowers. After GC-FID and GC-MS analyses, the two oils -revealed differences in the nature and especially in the proportion of their components, which were aldehydes, alcohols, phenolics, esters, hydrocarbons and acids. Eugenol was the single most abundant compound in the leaves, totalling 46.7% of the total oil, followed by phytol with 34.4%. Flowers showed a predominance of hydrocarbons, among which the anteiso branched-chain saturated hydrocarbon, 3-methyl tricosane, was the most abundant compound, accounting for 14.9% of the total volatiles. Eugenol ranked second with 10.3%, followed by the two linear-chain saturated hydrocarbons pentacosane and tricosane forming 8.2 and 7.7% of the total oil, respectively. The occurrence and the relative abundance of compounds from various chemical classes such as phenolics, hydrocarbons and aromatic aldehydes and alcohols are discussed, together with some of their ecological implications. The obtained volatile oils were than tested against two major honeybee (Apis mellifera) pathogens, namely Paenibacillus larvae and Melissococcus plutonius, the causative agents of the American and the European foulbrood, respectively.


Subject(s)
Anti-Infective Agents/pharmacology , Bees/microbiology , Flowers/chemistry , Malva/chemistry , Oils, Volatile/chemistry , Plant Leaves/chemistry , Alkanes/chemistry , Alkanes/pharmacology , Animals , Eugenol/chemistry , Eugenol/pharmacology , Microbial Sensitivity Tests , Oils, Volatile/pharmacology , Paenibacillus/drug effects
13.
J Cosmet Sci ; 67(2): 71-92, 2016.
Article in English | MEDLINE | ID: mdl-29394011

ABSTRACT

Natural peloids from sulfurous thermal springs are largely used in cosmetic and pelotherapy for the treatment of different dermatological conditions, including skin aging, dermatitis, and other eczemas. The beneficial effects are correlated to mineralogical and other thermal properties, as well as to the presence of natural substances with specific antioxidant activity. Few data are available for the comparison between natural peloids and synthetic (i.e., artificially maturated) muds. In this context, the natural substances and antioxidant activity of natural white mud (WM) and dark mud (DM) peloids from the sulfurous thermal spring pool Bagnaccio (Viterbo, Italy) have been studied in detail to evaluate possible relationships between physicochemical properties and therapeutic effect. A large panel of natural substances in WM and DM were characterized for the first time by ³¹P-nuclear magnetic resonance and gas chromatography associated to mass spectrometry analysis. Polar fractions of WM and DM peloids were characterized by the presence of several bioactive natural compounds, showing high antioxidant activity and DNA protective effect, as evaluated by 2,2-diphenyl-1-picrylhydrazyl assay, and hydrogen peroxide­induced DNA breakage in the alkaline comet assay. The antioxidant activity and DNA protective effect could be attributed to radical scavenging rather than a modulatory effect on the induced DNA repair, and are of order of intensity higher than that reported for synthetic muds.


Subject(s)
Alkaloids/pharmacology , Free Radical Scavengers/pharmacology , Hydrocarbons, Aromatic/pharmacology , Phenols/pharmacology , Terpenes/pharmacology , Alkaloids/chemistry , Alkaloids/isolation & purification , Alkanes/chemistry , Alkanes/isolation & purification , Alkanes/pharmacology , Alkenes/chemistry , Alkenes/isolation & purification , Alkenes/pharmacology , Animals , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , CHO Cells , Cell Line, Tumor , Cell Survival/drug effects , Comet Assay , Cricetulus , DNA/drug effects , Free Radical Scavengers/chemistry , Free Radical Scavengers/isolation & purification , Hot Springs , Humans , Hydrocarbons, Aromatic/chemistry , Hydrocarbons, Aromatic/isolation & purification , Hydrogen Peroxide/antagonists & inhibitors , Hydrogen Peroxide/chemistry , Italy , Magnetic Resonance Spectroscopy , Mice , Mud Therapy , Phenols/chemistry , Phenols/isolation & purification , Picrates/antagonists & inhibitors , Picrates/chemistry , Terpenes/chemistry , Terpenes/isolation & purification
14.
J Nat Med ; 70(1): 36-44, 2016 Jan.
Article in English | MEDLINE | ID: mdl-26382100

ABSTRACT

Ancient Chinese medicine treatises on Atractylodis Macrocephalae Rhizoma (AMR), the rhizome of Atractylodes macrocephala Koidz, indicated that it possessed an expectorant effect. However, in modern times, it is commonly used as a tocolytic agent. In this study, the components of AMR that are responsible for its expectorant and tocolytic effects were evaluated in order to clarify the differences in its application between ancient and modern times. A decoction of AMR was separated into five fractions, namely, volatile oil (VO), petroleum ether (PE), alcohol eluate from macroporous resin (AE), water eluate from macroporous resin (WE), and polysaccharides (PS), using various separation methods. The expectorant experiment indicated that the VO fraction, which mainly contains atractylone, produced an obvious expectorant effect. The experiment that assessed the irritability of uterine smooth muscle (USM) showed that the PE, which is mainly composed of atractylenolides, and the PS, which is mainly composed of inulin-type polysaccharides, were the active fractions for tocolysis, but the VO fraction had the opposite action. These data suggested that volatile oils are the key components responsible for the usage change of AMR in both ancient and current usage.


Subject(s)
Alkanes/pharmacology , Atractylodes/metabolism , Muscle, Smooth/drug effects , Oils, Volatile/pharmacology , Polysaccharides/pharmacology , Uterus/drug effects , Alcohols/pharmacology , Animals , Drugs, Chinese Herbal/therapeutic use , Expectorants/therapeutic use , Female , Humans , Mice , Pregnancy , Rhizome/metabolism , Solvents/pharmacology , Tocolytic Agents/therapeutic use
15.
J Parasitol ; 101(6): 701-5, 2015 Dec.
Article in English | MEDLINE | ID: mdl-26321352

ABSTRACT

Pentadecane is an organic compound that is made up of primarily carbon and hydrogen atoms. Pentadecane is a floral volatile found in many different plants and essential oils and also in crude extracts of some plants, and it shows antimicrobial activity. This study investigated in vitro effects of pentadecane in Leishmania infantum parasites and found that it decreases growth by 86 ± 2% both in promastigotes (half maximal inhibitory concentration [IC50] = 65.3 µM) and in amastigotes (IC50 = 60.5 µM), resulting in a reduction of macrophage infection; growth inhibition was 77% at 300 µM. Analysis of propidium iodide incorporation in L. infantum , treated with pentadecane at 48 hr, suggested that cells were arresting in the sub-G0/G1 and G1 phases of the cell cycle, whereas cytotoxicity assay of pentadecane in immortalized cells lines DH82 and U937 and in primary epithelial cells of Cercopiteco showed that it caused negligible cytotoxic effect. This study shows that pentadecane has antimicrobial activity against L. infantum parasites in in vitro culture.


Subject(s)
Alkanes/pharmacology , Leishmania infantum/drug effects , Plant Extracts/pharmacology , Alkanes/toxicity , Animals , Cell Line , Cercopithecus , Epithelial Cells/drug effects , Flowers/chemistry , G1 Phase/drug effects , Humans , Inhibitory Concentration 50 , Leishmania infantum/cytology , Leishmania infantum/growth & development , Macrophages/drug effects , Macrophages/parasitology , Plant Extracts/toxicity , Resting Phase, Cell Cycle/drug effects , U937 Cells
16.
Zhongguo Zhong Yao Za Zhi ; 40(8): 1585-8, 2015 Apr.
Article in Chinese | MEDLINE | ID: mdl-26281603

ABSTRACT

Sodium houttuyfonate (SH) is a derivative of effective component of a Chinese material medica, Houttuynia cordata, which is applied in anti-infection of microorganism. But, the antimicrobial mechanisms of SH still remain unclear. Here, we firstly discovered that SH effectively inhibits the three types of virulence related motility of.Pseudomonas aeruginosa, i.e., swimming, twitching and swarming. The plate assay results showed that the inhibitory action of SH against swimming and twitching in 24 h and swarming in 48 h is dose-dependent; and bacteria nearly lost all of the motile activities under the concentration of 1 x minimum inhibitory concentration (MIC) (512 mg x L(-1) same as azithromycin positive group (1 x MIC, 16 mg x L(-1)). Furthermore, we found that the expression of structural gene flgB and pilG is down-regulated by SH, which implies that inhibitory mechanism of SH against motility of P. aeruginosa may be due to the inhibition of flagella and pili bioformation of P. aeruginosa by SR Therefore, our presented results firstly demonstrate that SH effectively inhibits the motility activities of P. aeruginosa, and suggest that SH could be a promising antipseudomonas agents in clinic.


Subject(s)
Alkanes/pharmacology , Drugs, Chinese Herbal/pharmacology , Houttuynia/chemistry , Pseudomonas aeruginosa/cytology , Pseudomonas aeruginosa/drug effects , Sulfites/pharmacology , Anti-Bacterial Agents/pharmacology , Bacterial Proteins/genetics , Bacterial Proteins/metabolism , Biofilms/drug effects , Fimbriae, Bacterial/drug effects , Fimbriae, Bacterial/genetics , Fimbriae, Bacterial/metabolism , Pseudomonas aeruginosa/genetics , Pseudomonas aeruginosa/pathogenicity , Virulence/drug effects
17.
J Med Food ; 18(2): 259-63, 2015 Feb.
Article in English | MEDLINE | ID: mdl-25069066

ABSTRACT

Although the incidence of caries worldwide has declined in recent years, it is necessary to search for new means to overcome this disease and its microbiological agents. Phytochemistry can become an effective alternative to antibiotics, offering a promising strategy in the prevention and therapy of dental caries. This study aimed to evaluate in vitro the bactericide activity of a bioactive phytocomponent from Melia azedarach against Streptococcus mutans. The crude extract (CEx) from leaves and stem barks of M. azedarach in chloroform, petroleum ether, acetate ethyl, butanol, and aqueous fractions was evaluated using seven different concentrations. Disk diffusion and minimum inhibitory concentration assays were used to evaluate the antibacterial activity. 0.12% chlorhexidine was used as a positive control. The CEx and the petroleum ether fraction from M. azedarach showed significant antibacterial activity against S. mutans, confirming its antibiotic potential.


Subject(s)
Anti-Bacterial Agents/pharmacology , Melia azedarach/chemistry , Phytotherapy , Plant Bark/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Streptococcus mutans/drug effects , Acetates/pharmacology , Alkanes/pharmacology , Butanols/pharmacology , Chlorhexidine/pharmacology , Chloroform/pharmacology , Dental Caries/drug therapy , Dental Caries/prevention & control , Microbial Sensitivity Tests
18.
ScientificWorldJournal ; 2014: 715481, 2014.
Article in English | MEDLINE | ID: mdl-25436226

ABSTRACT

The acaricidal activity of the petroleum ether extract of leaves of Tetrastigma leucostaphylum (Dennst.) Alston (family: Vitaceae) against Rhipicephalus (Boophilus) annulatus was assessed using adult immersion test (AIT). The per cent of adult mortality, inhibition of fecundity, and blocking of hatching of eggs were studied at different concentrations. The extract at 10% concentration showed 88.96% inhibition of fecundity, 58.32% of adult tick mortality, and 50% inhibition of hatching. Peak mortality rate was observed after day 5 of treatment. Mortality of engorged female ticks, inhibition of fecundity, and hatching of eggs were concentration dependent. The LC50 value of the extract against R. (B.) annulatus was 10.46%. The HPTLC profiling of the petroleum ether extract revealed the presence of at least seven polyvalent components. In the petroleum ether extract, nicotine was identified as one of the components up to a concentration of 5.4%. However, nicotine did not reveal any acaricidal activity up to 20000 ppm (2%). Coconut oil, used as diluent for dissolving the extract, did not reveal any acaricidal effects. The results are indicative of the involvement of synergistic or additive action of the bioactive components in the tick mortality and inhibition of the oviposition.


Subject(s)
Acaricides/pharmacology , Alkanes/pharmacology , Plant Extracts/pharmacology , Rhipicephalus/drug effects , Vitaceae , Acaricides/isolation & purification , Alkanes/isolation & purification , Animals , Female , Plant Extracts/isolation & purification
19.
PLoS One ; 9(10): e109599, 2014.
Article in English | MEDLINE | ID: mdl-25302783

ABSTRACT

The chemical compositions and anti-tumor activities of the petroleum ether fraction (PE), from mushroom Pyropolyporus fomentarius, were studied. Upon gas chromatography-mass spectrometry (GC-MS) analysis, nine major constituents were identified in the fraction. In vitro, the PE showed cytotoxic activity against murine sarcoma S180 (S180) cells in a dose- and time-dependent manner, and the cytotoxic effects were associated with apoptosis. The mitochondrial membrane potential loss and the intracellular ROS generation were greatly increased in the Pyropolyporus fomentarius PE treated group, suggesting cell apoptosis, induced by the PE in S180 cells, might be mitochondria dependent and ROS mediated. Consistent with in vitro findings, the in vivo study showed that the Pyropolyporus fomentarius PE was also effective in inhibiting the tumor growth induced by S180 cells and had lower immune organ toxicity. We found that the Pyropolyporus fomentarius PE has significant anti-tumor activity and great potential in screening anti-tumor drugs.


Subject(s)
Agaricales , Alkanes/pharmacology , Apoptosis/drug effects , Phytotherapy , Plant Extracts/pharmacology , Sarcoma/drug therapy , Alkanes/therapeutic use , Animals , Cell Line, Tumor , Mice , Plant Extracts/therapeutic use , Reactive Oxygen Species/metabolism , Sarcoma/metabolism
20.
Biol Res ; 47: 12, 2014 Apr 01.
Article in English | MEDLINE | ID: mdl-25052892

ABSTRACT

BACKGROUND: Current study has been designed to evaluate the chemical composition of essential and fixed oils from stem and leaves of Perovskia abrotanoides and antioxidant and antimicrobial activities of these oils. RESULTS: GC-MS analysis of essential oil identified 19 compounds with (E)-9-dodecenal being the major component in stem and hexadecanoic acid in leaves. In contrast, GC-MS analysis of fixed oil showed 40 constituents with α-amyrin the major component in stem and α-copaene in leaves. The antioxidant activity showed the highest value of 76.7% in essential oil from leaves in comparison with fixed oil from stem (45.9%) through inhibition of peroxidation in linoleic acid system. The antimicrobial assay tested on different microorganisms (e.g. E. coli, S. aureus, B. cereus, Nitrospira, S. epidermis, A. niger, A. flavus and C. albicans) showed the higher inhibition zone at essential oil from leaves (15.2 mm on B. cereus) as compared to fixed oil from stem (8.34 mm on S. aureus) and leaves (11.2 mm on S. aureus). CONCLUSIONS: The present study revealed the fact that essential oil analyzed from Perovskia abrotanoides stem and leaves could be a promising source of natural products with potential antioxidant and antimicrobial activities, as compared to fixed oil.


Subject(s)
Anti-Infective Agents/chemistry , Antioxidants/chemistry , Lamiaceae/chemistry , Plant Leaves/chemistry , Plant Oils/pharmacology , Plant Stems/chemistry , Alkanes/analysis , Alkanes/pharmacology , Anti-Infective Agents/pharmacology , Antioxidants/pharmacology , Aspergillus/drug effects , Bacillus cereus/drug effects , Candida albicans/drug effects , Disk Diffusion Antimicrobial Tests , Escherichia coli/drug effects , Gas Chromatography-Mass Spectrometry , Lipid Peroxidation/drug effects , Methyl Ethers/analysis , Methyl Ethers/pharmacology , Microbial Sensitivity Tests , Oils, Volatile/chemistry , Oleanolic Acid/analogs & derivatives , Oleanolic Acid/analysis , Oleanolic Acid/pharmacology , Palmitic Acid/analysis , Palmitic Acid/pharmacology , Pentacyclic Triterpenes/analysis , Pentacyclic Triterpenes/pharmacology , Plant Oils/chemistry , Reducing Agents/analysis , Sesquiterpenes/analysis , Sesquiterpenes/pharmacology , Staphylococcus/drug effects , Stearic Acids/analysis , Stearic Acids/pharmacology
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