RESUMO
BACKGROUND: Benign prostatic hyperplasia (BPH) is a prevalent disease affecting elderly men, with chronic inflammation being a critical factor in its development. Omentin-1, also known as intelectin-1 (ITLN-1), is an anti-inflammatory protein primarily found in the epithelial cells of the small intestine. This study aimed to investigate the potential of ITLN-1 in mitigating BPH by modulating local inflammation in the prostate gland. METHODS: Our investigation involved two in vivo experimental models. Firstly, ITLN-1 knockout mice (Itln-1-/-) were used to study the absence of ITLN-1 in BPH development. Secondly, a testosterone propionate (TP)-induced BPH mouse model was treated with an ITLN-1 overexpressing adenovirus. We assessed BPH severity using prostate weight index and histological analysis, including H&E staining, immunohistochemistry, and enzyme-linked immunosorbent assay. In vitro, the impact of ITLN-1 on BPH-1 cell proliferation and inflammatory response was evaluated using cell proliferation assays and enzyme-linked immunosorbent assay. RESULTS: In vivo, Itln-1-/- mice exhibited elevated prostate weight index, enlarged lumen area, and higher TNF-α levels compared to wild-type littermates. In contrast, ITLN-1 overexpression in TP-induced BPH mice resulted in reduced prostate weight index, lumen area, and TNF-α levels. In vitro studies indicated that ITLN-1 suppressed the proliferation of prostate epithelial cells and reduced TNF-α production in macrophages, suggesting a mechanism involving the inhibition of macrophage-mediated inflammation. CONCLUSION: The study demonstrates that ITLN-1 plays a significant role in inhibiting the development of BPH by reducing local inflammation in the prostate gland. These findings highlight the potential of ITLN-1 as a therapeutic target in the management of BPH.
Assuntos
Proteínas Ligadas por GPI , Lectinas , Hiperplasia Prostática , Animais , Masculino , Camundongos , Citocinas/genética , Citocinas/metabolismo , Proteínas Ligadas por GPI/genética , Proteínas Ligadas por GPI/metabolismo , Inflamação/patologia , Lectinas/genética , Lectinas/metabolismo , Extratos Vegetais/farmacologia , Próstata/metabolismo , Próstata/patologia , Hiperplasia Prostática/genética , Hiperplasia Prostática/tratamento farmacológico , Hiperplasia Prostática/metabolismo , Fator de Necrose Tumoral alfaRESUMO
Perillaldehyde is a monoterpene compound mainly from the medicinal plant Perilla frutescens (L.) Britt., which has hypolipidemic, antioxidant, antibacterial and anti-inflammatory functions. In this investigation, we discovered that Perillaldehyde had powerful antimicrobial activity against Acinetobacter baumannii 5F1, and its minimum inhibitory concentration was 287.08 µg/mL. A. baumannii is a conditionally pathogenic bacterium with a high clinical resistance rate and is a major source of hospital infections, especially in intensive care units, which is one of the main causes of pneumonia. Inflammatory immune response is characteristic of pneumonia caused by A. baumannii infection. The results of our in vitro experiments indicate that Perillaldehyde disrupts the cell membrane of A. baumannii 5F1 and inhibits its quorum sensing to inhibit biofilm formation, among other effects. With an experimental model of murine pneumonia, we investigated that Perillaldehyde decreased NLRP3 inflammasome activation and TNF-α expression in lung tissues by inhibiting the NF-κB pathway, and also impacted MAPKs protein signaling pathway through the activation of TLR4. Notably, the use of high doses of Perillaldehyde for the treatment of pneumonia caused by A. baumannii 5F1 infection resulted in a survival rate of up to 80 % in mice. In summary, we demonstrated that Perillaldehyde is promising as a new drug for the treatment of pneumonia caused by A. baumannii 5F1 infection.
Assuntos
Acinetobacter baumannii , Pneumonia , Camundongos , Animais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Monoterpenos/farmacologia , Monoterpenos/uso terapêuticoRESUMO
Objective. In the field of motor imagery (MI) electroencephalography (EEG)-based brain-computer interfaces, deep transfer learning (TL) has proven to be an effective tool for solving the problem of limited availability in subject-specific data for the training of robust deep learning (DL) models. Although considerable progress has been made in the cross-subject/session and cross-device scenarios, the more challenging problem of cross-task deep TL remains largely unexplored.Approach. We propose a novel explainable cross-task adaptive TL method for MI EEG decoding. Firstly, similarity analysis and data alignment are performed for EEG data of motor execution (ME) and MI tasks. Afterwards, the MI EEG decoding model is obtained via pre-training with extensive ME EEG data and fine-tuning with partial MI EEG data. Finally, expected gradient-based post-hoc explainability analysis is conducted for the visualization of important temporal-spatial features.Main results. Extensive experiments are conducted on one large ME EEG High-Gamma dataset and two large MI EEG datasets (openBMI and GIST). The best average classification accuracy of our method reaches 80.00% and 72.73% for OpenBMI and GIST respectively, which outperforms several state-of-the-art algorithms. In addition, the results of the explainability analysis further validate the correlation between ME and MI EEG data and the effectiveness of ME/MI cross-task adaptation.Significance. This paper confirms that the decoding of MI EEG can be well facilitated by pre-existing ME EEG data, which largely relaxes the constraint of training samples for MI EEG decoding and is important in a practical sense.
Assuntos
Interfaces Cérebro-Computador , Imaginação , Eletroencefalografia/métodos , Algoritmos , Aprendizado de MáquinaRESUMO
OBJECTIVE: To investigate the molecular mechanisms underlying the effect of baicalin on prostate cancer (PCa) progression both in vivo and in vitro. METHODS: The in situ PCa stem cells (PCSCs)-injected xenograft tumor models were established in BALB/c nude mice. Tumor volume and weight were respectively checked after baicalin (100 mg/kg) treatment. Hematoxylin-eosin (HE) staining was used to observe the growth arrest and cell necrosis. mRNA expression levels of acetaldehyde dehydrogenase 1 (ALDH1), CD44, CD133 and Notch1 were determined by reverse transcription-polymerase chain reaction. Protein expression levels of ALDH1, CD44, CD133, Notch1, nuclear factor κB (NF-κB) P65 and NF-κB p-P65 were detected by Western blot. Expression and subcellular location of ALDH1, CD44, CD133, Notch1 and NF-κB p65 were detected by immunofluorescence analysis. In vitro, cell cycle distribution and cell apoptosis of PC3 PCSCs was assessed by flow cytometry after baicalin (125 µmol/L) treatment. The migration and invasion abilities of PCSCs were assessed using Transwell assays. Transmission electron microscopy scanning was utilized to observe the structure and autophagosome formation of baicalin-treated PCSCs. In addition, PCSCs were infected with lentiviruses expressing human Notch1. RESULTS: Compared with the control group, the tumor volume and weight were notably reduced in mice treated with 100 mg/kg baicalin (P<0.05 or P<0.01). Histopathological analysis showed that baicalin treatment significantly inhibited cell proliferation and promoted cell apoptosis. Furthermore, baicalin treatment reduced mRNA and protein expression levels of CD44, CD133, ALDH1, and Notch1 as well as the protein expression of NF-κB p-P65 in the xenograft tumor (P<0.01). In vitro, the cell proliferation of PCSCs was significantly attenuated after treatment with 125 µmol/L baicalin for 72 h (P<0.01). The cell migration and invasion rates were decreased following treatment with baicalin for 48 and 72 h (P<0.01). Baicalin notably induced cell apoptosis and seriously damaged the structure of PCSCs. The mRNA and protein expressions of CD133, CD44, ALDH1 and Notch1 in PCSCs were significantly downregulated following baicalin treatment (P<0.01). Importantly, the inhibitory effects of baicalin on PCa progression and stemness were reversed by Notch1 overexpression (P<0.05 or P<0.01). CONCLUSION: Mechanistically, baicalin exhibited a potential therapeutic effect on PCa via inhibiting the Notch1/NF-κB signaling pathway and its mediated cancer stemness.
Assuntos
NF-kappa B , Neoplasias da Próstata , Masculino , Humanos , Camundongos , Animais , NF-kappa B/metabolismo , Camundongos Nus , Linhagem Celular Tumoral , Transdução de Sinais , Neoplasias da Próstata/tratamento farmacológico , RNA MensageiroRESUMO
Breast cancer is a high-risk disease with a high mortality rate among women. Chemotherapy plays an important role in the treatment of breast cancer. However, chemotherapy eventually results in tumours that are resistant to drugs. In recent years, many studies have revealed that the activation of Wnt/ß-catenin signalling is crucial for the emergence and growth of breast tumours as well as the development of drug resistance. Additionally, drugs that target this pathway can reverse drug resistance in breast cancer therapy. Traditional Chinese medicine has the properties of multi-target and tenderness. Therefore, integrating traditional Chinese medicine and modern medicine into chemotherapy provides a new strategy for reversing the drug resistance of breast tumours. This paper mainly reviews the possible mechanism of Wnt/ß-catenin in promoting the process of breast tumour drug resistance, and the progress of alkaloids extracted from traditional Chinese medicine in the targeting of this pathway in order to reverse the drug resistance of breast cancer.
Assuntos
Alcaloides , Neoplasias da Mama , Via de Sinalização Wnt , Feminino , Humanos , Alcaloides/farmacologia , Alcaloides/uso terapêutico , beta Catenina/metabolismo , beta Catenina/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Proliferação de Células , Resistência a Medicamentos , Medicina Tradicional ChinesaRESUMO
Long-term stored oolong tea has recently attracted considerable attention concerning its salutary effect. In this study, the anti-obesity effect of different years' oolong tea on high-fat diet-fed mice was compared. Wuyi rock tea of 2001, 2011, and 2020 were chosen to be the representative samples of oolong tea. The results showed that eight-week administration of 2001 Wuyi rock tea (WRT01), 2011 Wuyi rock tea (WRT11), and 2020 Wuyi rock tea (WRT20) extracts (400 mg per kg per d) significantly decreased the body weight and attenuated the obesity in high-fat diet-fed mice. 2001 and 2011 Wuyi rock teas reduced obesity mainly through regulating lipid metabolism and activating the AMPK/SREBP-1 pathway, downregulating the expression of SREBP-1, FAS, and ACC and upregulating CPT-1a expression; while the 2011 and 2020 Wuyi rock teas by moderating the gut microbiota dysbiosis, reshaping the gut microbiota, and promoting the growth of beneficial bacteria, especially Akkermansia. 2011 Wuyi rock tea was proven to be more effective in reducing body weight gain and liver oxidative stress than the others. Collectively, all three Wuyi rock teas of different years alleviated high-fat diet-induced obesity by regulating lipid metabolism and modulating gut microbiota, whereas the emphasis of their internal mechanism is different with different storage ages.
Assuntos
Dieta Hiperlipídica , Microbioma Gastrointestinal , Camundongos , Animais , Dieta Hiperlipídica/efeitos adversos , Proteína de Ligação a Elemento Regulador de Esterol 1/genética , Proteína de Ligação a Elemento Regulador de Esterol 1/metabolismo , Metabolismo dos Lipídeos , Chá/metabolismo , Obesidade/metabolismo , Peso Corporal , Camundongos Endogâmicos C57BLRESUMO
Quorum sensing (QS) plays an important role in the production of virulence factors and pathogenicity in pathogenic bacteria and is, therefore, a hopeful target to fight against bacterial infections. During our search for natural QS inhibitors, two new xanthonolignoids (1 and 2), each existing as a racemic mixture, one new simple oxygenated xanthone (7), and eight known analogs (3-6, 8-11) were isolated from Hypericum scabrum Linn. Chiral separation of 1 yielded a pair of enantiomers 1a and 1b. The structures of these compounds were elucidated by spectroscopic analysis and ECD (electrostatic circular dichroism) calculations. All isolates were evaluated for their QS inhibitory activity against Chromobacterium violaceum. Both 9 and 10 exhibited the most potent QS inhibitory effects with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 31.25 and 62.5 µM, respectively. Crystal violet staining was used to further evaluate the biofilm inhibition potential of compounds 7, 9 and 10, and the formation of biofilms increased with decreasing drug concentration in a classic dose-dependent manner. The results of a cytotoxicity assay revealed that compounds 7, 9 and 10 exhibited no cytotoxic activity on PC-12 cells at the tested concentration.
Assuntos
Hypericum , Xantonas , Antibacterianos/farmacologia , Biofilmes , Chromobacterium , Pseudomonas aeruginosa , Percepção de Quorum , Xantonas/farmacologiaRESUMO
Two new C21 steroidal glycosides, brapreguanes A and B (1-2) were isolated from 75 % aqueous ethanol extract of Selaginella braunii Baker. Their structures were established by spectroscopic analyses (1D/2D NMR spectra and HR-ESI-MS). The absolute configurations of sugar were elucidated by enzymatic hydrolysis and GCMS analysis. In addition, all compounds were evaluated for the anti-proliferative activities against various human cancer cells inâ vitro. Compounds exhibited no inhibition to various human cancer cells.
Assuntos
Selaginellaceae , Humanos , Selaginellaceae/química , Estrutura Molecular , Glicosídeos/farmacologia , Glicosídeos/química , Açúcares , Etanol , Extratos VegetaisRESUMO
Candida albicans is an opportunistic pathogen that causes biofilm-associated infections. C. albicans biofilms are known to display reduced susceptibility to antimicrobials and high rates of acquired antibiotic resistance, and biofilm forming in C. albicans further hampers treatment options and highlights the need for new antibiofilm strategies. Identifying active components from desert actinomycetes strains to inhibit the formation of C. albicans biofilms represents an effective treatment strategy. In this study, actinomycetes that can inhibit C. albicans biofilm formation were isolated from the Taklimakan Desert, and the underlying mechanisms were explored. After screening the anti-C.albicans biofilm activities of culture supernatants from 170 Actinomycete strains, six strains showed significant inhibition of C. albicans biofilm formation. Microscopic examination showed a reduction in biofilm formation of C. albicans treated with supernatants from actinomycetes. Scanning electron microscopy showed that the morphological changes in biofilm cells were caused by cell membrane rupture and cell material leakage. Then, C.albicans biofilms were destroyed by changing the content of extracellular polysaccharides or degrading extracellular DNA. Finally, a preliminary study on active substances extracted from a new species (TRM43335) showed that the substances that inhibited the formation of biofilms might be peptides. This study provides preliminary evidence that desert actinomyces strains have inhibitory effects on the biofilm development of C. albicans.
Assuntos
Anti-Infecciosos , Streptomyces , Anti-Infecciosos/farmacologia , Antifúngicos/farmacologia , Biofilmes , Candida albicans , Extratos Vegetais/farmacologiaRESUMO
Gnaphalium hypoleucum DC. was first recorded in the Chinese National Pharmacopoeia "Yi Plant Medicine". There is no detailed report on its main components' activity in suppressing the quorum sensing activity (QS) of bacteria. Our study aimed to screen the main components in extracts of G. hypoleucum DC. in order to measure their effects on bacterial QS activity and to explore specific quorum sensing mechanisms that are affected by G. hypoleucum DC. extracts. Crude extracts of G. hypoleucum DC. contained significant amounts of two compounds shown to inhibit bacterial QS activity, namely apigenin and luteolin. Apigenin and luteolin in crude extracts of G. hypoleucum DC. showed substantial inhibition of pigment formation, biofilm production, and motility in Chromobacterium violaceum ATCC 12472 compared to the effects of other phytochemicals from G. hypoleucum DC. Apigenin and luteolin exhibited a strong QS inhibitory effect on C. violaceum, interfering with the violacein pigment biosynthesis by downregulating the vioB, vioC, and vioD genes. In the presence of signal molecules, the QS effect is prevented, and the selected compounds can still inhibit the production of the characteristic purple pigment in C. violaceum. Based on qualitative and quantitative research using genomics and bioinformatics, we concluded that apigenin and luteolin in crude extracts of G. hypoleucum DC can interfere with the generation of QS in C. violaceum by downregulating the vioB, vioC, and vioD genes. Indeed, G. hypoleucum DC. is used for the treatment of bacterial infections, and this research provides new ideas and potential alternative uses for medicinal plants.
Assuntos
Asteraceae , Gnaphalium , Antibacterianos/química , Antibacterianos/farmacologia , Apigenina/farmacologia , Biofilmes , Chromobacterium , Luteolina/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Percepção de QuorumRESUMO
Eighteen polycyclic polyprenylated acylphloroglucinols were isolated from the whole plant of Hypericum scabrum Linn., including six new compounds (1-6). Their structures were elucidated by comprehensive spectroscopic analyses. The evaluation of their cytotoxic activities was carried out against SMMC-7721 and MGC-803 cell lines. We found that most tested compounds exhibited moderate cytotoxic activities against SMMC-7721 cell line except for 11 and 12, while compounds 1, 5-7, 13 and 16 also showed cytotoxic activities on MGC-803 cells. Besides, Bacillus subtilis, MRSA and MDPRA were also used to test inhibitory activity of these compounds. Our results showed that only compounds 12 and 13 presented weak inhibitory activity against Bacillus subtilis, while compounds 7, 13 and 14 also inhibited MRSA weakly.
Assuntos
Hypericum , Linhagem Celular , Hypericum/química , Estrutura Molecular , Floroglucinol/química , Floroglucinol/farmacologiaRESUMO
Chronical hyperuricemia, a severe metabolic disease characterized by increased serum uric acid, urea nitrogen, and creatinine, has a positive correlation with the risks of gouty arthritis, diabetes, hypertension, and kidney damage. Abnormal purine metabolism and reduced uric acid excretion are the major causes of hyperuricemia, which, thus, points to a potential strategy of preventing from or delaying the progress of hyperuricemia-related diseases and its complications by effectively controlling the serum uric acid level. Increasing evidence has revealed that Chinese medicines alleviate hyperuricemia through regulating intestinal flora, which plays a pivotal role in regulating metabolites, including uric acid level. The disease treatment with traditional Chinese medicine is based on syndrome differentiation, and Chinese medicines often have multiple effects and a wide range of targets. In this review, we summarized the anti-hyperuricemia effects and mechanisms of active compounds in Chinese medicines, single Chinese medicinal herbs, and Chinese medicinal prescriptions in regulating the uric acid level via intestinal flora and metabolites, which will be helpful for further study and application of Chinese medicines in hyperuricemia treatment.
Assuntos
Artrite Gotosa , Microbioma Gastrointestinal , Hiperuricemia , China , Humanos , Hiperuricemia/tratamento farmacológico , Ácido ÚricoRESUMO
In our study, the anti-quorum sensing (QS) activity of fermentation broth from TRM B-02, a bacterium isolated from Taklimakan desert, was investigated using the biosensor bioassay on Chromobacterium violaceum ATCC12472. TRM B-02 was 100% similar to Bacillus subtilis subsp. Inaquosorum KCTC 13429(T) by genotypic and phenotypic analyses. Based on anti-QS activity tracking, six known amicoumacins, named as AI-77-H (1), AI-77-F (2), amicoumacin B (3), amicoumacin C (4), AI-77-C (5) and bacilosarcins D (6), were isolated and identified. Among them, compounds 1-3 exhibited a better inhibitory effect on C. violaceum ATCC12472. Further research suggested that compounds 1-3 could significantly down-regulate the expressions of violacein operon A (vioA), vioB, vioD and vioE and up-regulate vioC. Docking experiments indicated that compounds 1-3 may act as an inhibitor of violacein biosynthetic pathway competitively inhibiting the binding of flavin adenine dinucleotide (FAD) with the vioD enzyme.[Figure: see text].
Assuntos
Antibacterianos , Percepção de Quorum , Antibacterianos/farmacologia , Chromobacterium , Extratos Vegetais/farmacologiaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Siwu Paste (SWP) was recorded in the first national Pharmacopoeia of China, "Tai Ping Hui Min He Ji Ju Fang", it showed excellent effects in regulating all syndromes relevant to blood. AIM OF THE STUDY: This study aimed to investigate the protective effects of Siwu Paste (SWP) on bone marrow hematopoietic by using rats' model with blood deficiency syndrome induced by chemotherapy. MATERIALS AND METHODS: Animal model with blood deficiency syndrome was successfully established by evaluating their peripheral blood cell level and erythrocyte membrane energy metabolism enzyme activity. Serum hematopoietic cytokine levels were detected by using Enzyme-linked immunosorbent assay (ELISA). Hematoxylin-Eosin (HE) staining method was used to observe the pathological morphology of femur bone marrow, and the viability of BMSC was detected by Cell Counting Kit (CCK-8). Furthermore, the expression of toll-like receptor 4 (TLR4), nuclear transcription factor kB (NF-κB), and NOD-like receptor protein 3 (NLRP3) protein in femur bone marrow were detected by using Western-blotting and High-content cell imaging analysis system (HCA). RESULTS: Obtained results showed that SWP could significantly improve the status of anemia, regulate the expressions of serum hematopoietic cytokines, and protect bone marrow hematopoietic cells. Furthermore, the expressions of TLR4, NF-κB, and NLRP3 protein were inhibited in bone marrow hematopoietic cells. CONCLUSIONS: Siwu Paste (SWP) could recover the bone marrow hematopoietic functions in rats with blood deficiency syndrome. The therapeutic mechanism may be related to the regulation of serum hematopoietic cytokines, and inhibition of TLR4/NF-κB/NLRP3 signaling pathway.
Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Doenças Hematológicas/tratamento farmacológico , Hematopoese/efeitos dos fármacos , NF-kappa B/antagonistas & inibidores , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Receptor 4 Toll-Like/antagonistas & inibidores , Animais , Células da Medula Óssea/efeitos dos fármacos , Células da Medula Óssea/metabolismo , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Doenças Hematológicas/sangue , Hematopoese/fisiologia , Masculino , NF-kappa B/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Pomadas , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia , Receptor 4 Toll-Like/metabolismoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Coreopsis tinctoria Nutt has various medical and functional properties and its flower is widely used as health-care tea to decrease blood glucose and to lower blood lipids. However, the quorum sensing (QS) inhibition activity of Coreopsis tinctoria Nutt flower remains unclear. AIM OF THE STUDY: To assess inhibitory activity against quorum sensing by Chromobacterium violaceum, to identify the chemical composition of the extracts and to disclose the action mechanism of separated compound. MATERIAL AND METHODS: Violacein inhibition assays were performed in 96-wells microplates. The compounds extracted from Coreopsis tinctoria Nutt flower were separated and purified by various chromatography techniques. Respectively, thin layer chromatography (TLC, GF254), mass spectrometer (Agilent 1100 Series LC/MSD Trap SL), Medium-pressure automatic purification system (Buscisepacore C 620, Switzerland), High performance liquid chromatography (HPLC, Shimadzu LC-20AD, Japan), Liquid preparation Chromatography (Waters2545, USA). The chemical structures were identified by nuclear magnetic resonance (NMR, Bruker AV-500, Germany) technique. The inhibitory mechanism of okanin against C. violaceum quorum sensing was detected by quantitative real-time PCR (qRT-PCR). RESULTS: Quorum sensing regulates production of bacterial virulence factors, thereby making it an intriguing target for attenuating bacterial pathogenicity. In this study, anti-QS activity of Coreopsis tinctoria Nutt methanol fraction (CTM) was investigated against C. violaceum ATCC12472. CTM showed an inhibitory effect on the QS-mediated virulence factors production such as violacein in C. violaceum without effect on growth rate. Also, okanin was isolated from CTM and its potential of anti-QS was confirmed after observing a significant reduction of violacein production in C. violaceum. An attempt was made to assess the effect of okanin on vioABCDE expression in C. violaceum to disclose acting mechanisms. CONCLUSIONS: The results of this study contribute to validate an inhibitory effect of Coreopsis tinctoria Nutt flower on quorum sensing by Chromobacterium violaceum and to determine the compound responsible for inhibition. Also, the inhibitory effect was achieved in tandem with the down-regulation of vio operon.
Assuntos
Antibacterianos/farmacologia , Chalconas/farmacologia , Chromobacterium/efeitos dos fármacos , Coreopsis/química , Antibacterianos/isolamento & purificação , Chalconas/isolamento & purificação , Flores , Extratos Vegetais/farmacologia , Percepção de Quorum , Fatores de Virulência/análiseRESUMO
Candida albicans invasion is one of the most serious fungal infections in clinical history. In recent years, because of the widespread use of immunosuppressive drugs, chemotherapy drugs, glucocorticoids, and broad-spectrum antibiotics, serious drug resistance has been reported; therefore, a new type of antifungal drug needs to be developed. In this study, we found that Nerol (NEL) had strong antimicrobial activity and 0.77 µL/mL NEL was the minimum inhibitory concentration (MIC) effective against C. albicans. We determined the change of the growth curve of NEL for C. albicans, to identify the trend of NEL activity against C. albicans. Through the determination of the ergosterol content and glucose-induced extracellular fluid acidification of NEL on C. albicans, we found that NEL inhibits the growth of C. albicans by destroying cell membranes. This finding was also supported by the expression of SAP (secreted aspartyl proteinase) involved in cell membrane synthesis. Finally, demonstrations of phenotype investigation, colony-forming unit (CFU) counts, and PAS (periodic acid-Schiff) staining were conducted to prove that NEL had the ability to treated mouse oral C. albicans infection and vaginal C. albicans infection. This research may help us to investigate new antimicrobial agents for treating C. albicans infections. KEY POINTS: ⢠NEL can inhibit the growth of C. albicans. ⢠NEL destroys the cell membrane formation and permeability of C. albicans. ⢠NEL can treat vulvovaginal candidiasis and oropharyngeal candidiasis in mice. ⢠NEL could be used as a possible antifungal agent.
Assuntos
Monoterpenos Acíclicos/uso terapêutico , Antifúngicos/uso terapêutico , Candida albicans/efeitos dos fármacos , Candidíase Vulvovaginal/tratamento farmacológico , Doenças da Boca/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Ácido Aspártico Proteases/genética , Candida albicans/crescimento & desenvolvimento , Candidíase/tratamento farmacológico , Candidíase Vulvovaginal/microbiologia , Membrana Celular/efeitos dos fármacos , Ergosterol/análise , Feminino , Masculino , Camundongos Endogâmicos BALB C , Testes de Sensibilidade Microbiana , Boca/microbiologia , Doenças da Boca/microbiologiaRESUMO
Thirteen new grayanane diterpenoid glucosides, 3- epi-grayanoside B (1), micranthanosides A-E (2-6), 7α-hydroxygrayanoside C (7), micranthanoside F (8), 14ß-acetyoxymicranthanoside F (9), micranthanoside G (10), 14- O-acetylmicranthanoside G (11), 14ß-hydroxypieroside A (12), and micranthanoside H (13), and six known analogues (14-19) were isolated from the leaves of Rhododendron micranthum. The structures of 1-19 were elucidated based on spectroscopic analysis, comparison with literature, and chemical methods. The absolute configurations of 3- epi-grayanoside B (1) and micranthanosides A (2) and C (4) were defined by single-crystal X-ray diffraction analysis. This is the first report of the crystal structures of grayanane diterpenoid glucosides. 3- epi-Grayanoside B (1) represents the first example of a 3α-oxygrayanane diterpenoid glucoside, and micranthanosides A-D (2-5) are the first examples of 5α-hydroxy-1-ß H-grayanane diterpenoids. In addition, micranthanosides C-F (4-6 and 8) and 14ß-acetyoxymicranthanoside F (9) represent the first examples of grayanane glucosides with the glucosylation at C-16. All the grayanane diterpenoid glucosides 1-19 were assayed for their anti-inflammatory, antitumor, and PTP1B inhibitory activities, but did not show significant activities at 40 µM. Grayanane diterpenoid glucosides 1-18 were evaluated for their antinociceptive activity, and compounds 2, 3, 7-10, 12, 13, and 16 showed significant antinociceptive effects with percentage inhibitions in excess of 50%.
Assuntos
Diterpenos/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Glucosídeos/isolamento & purificação , Rhododendron/química , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Cristalografia por Raios X , Diterpenos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/farmacologia , Feminino , Glucosídeos/farmacologia , Humanos , Masculino , Camundongos , Estrutura Molecular , Folhas de Planta/químicaRESUMO
To investigate the effects of the introduction of Robinia pseudoacacia on the functional structure of plant communities, we selected paired-plots of R. pseudoacacia communities and native plant communities across different vegetation zones, i.e., steppe zone, forest-steppe zone, forest zone in hilly-gully region of Loess Plateau, China. We measured several functional characteristics and then compared the functional structures of R. pseudoacacia and native plant communities in different vegetation zones. The results showed that the variation of the functional traits across different vegetation zones were consistent in R. pseudoacacia community and native plant community, including leaf carbon concentration, leaf nitrogen concentration, leaf phosphorus concentration, specific leaf area, and leaf tissue density. The leaf carbon concentration, leaf nitrogen concentration, and specific leaf area of the R. pseudoacacia community were significantly higher than those of the native plant community. The trend of change that the functional diversity indices, i.e., FRic, FEve, FDiv, FDis, Rao of the R. pseudoacacia community and the native plant community with vegetation zones were different. The introduction of R. pseudoacacia enhanced the plant community functional diversity in the forest zone but reduced community functional diversity in the steppe zone.
Assuntos
Ecossistema , Espécies Introduzidas , Robinia , China , Florestas , Nitrogênio , SoloRESUMO
This manuscript elaborates on the establishment of a chemotaxonomic classification strategy for closely-related Citrus fruits in Traditional Chinese Medicines (TCMs). UPLC-Q-TOF-MS-based metabolomics was applied to depict the variable chemotaxonomic markers and elucidate the metabolic mechanism of Citrus TCMs from different species and at different ripening stages. Metabolomics can capture a comprehensive analysis of small molecule metabolites and can provide a powerful approach to establish metabolic profiling, creating a bridge between genotype and phenotype. To further investigate the different metabolites in four closely-related Citrus TCMs, non-targeted metabolite profiling analysis was employed as an efficient technique to profile the primary and secondary metabolites. The results presented in this manuscript indicate that primary metabolites enable the discrimination of species, whereas secondary metabolites are associated with species and the ripening process. In addition, analysis of the biosynthetic pathway highlighted that the syntheses of flavone and flavone glycosides are deeply affected in Citrus ripening stages. Ultimately, this work might provide a feasible strategy for the authentication of Citrus fruits from different species and ripening stages and facilitate a better understanding of their different medicinal uses.
Assuntos
Citrus/química , Frutas/química , Medicina Tradicional Chinesa , Metabolômica/classificação , Cromatografia Líquida , Citrus/classificação , Citrus/metabolismo , Frutas/classificação , Frutas/metabolismo , Genótipo , Glicosídeos/química , Glicosídeos/metabolismo , Humanos , FenótipoRESUMO
Electroencephalogram (EEG)-based motor imagery (MI) brain-computer interface (BCI) has shown its effectiveness for the control of rehabilitation devices designed for large body parts of the patients with neurologic impairments. In order to validate the feasibility of using EEG to decode the MI of a single index finger and constructing a BCI-enhanced finger rehabilitation system, we collected EEG data during right hand index finger MI and rest state for five healthy subjects and proposed a pattern recognition approach for classifying these two mental states. First, Fisher's linear discriminant criteria and power spectral density analysis were used to analyze the event-related desynchronization patterns. Second, both band power and approximate entropy were extracted as features. Third, aiming to eliminate the abnormal samples in the dictionary and improve the classification performance of the conventional sparse representation-based classification (SRC) method, we proposed a novel dictionary cleaned sparse representation-based classification (DCSRC) method for final classification. The experimental results show that the proposed DCSRC method gives better classification accuracies than SRC and an average classification accuracy of 81.32% is obtained for five subjects. Thus, it is demonstrated that single right hand index finger MI can be decoded from the sensorimotor rhythms, and the feature patterns of index finger MI and rest state can be well recognized for robotic exoskeleton initiation.