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1.
Food Chem ; 339: 127902, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-32920304

RESUMO

A protoberberine alkaloid, (-)-tetrahydroberberrubine∙acetate (THBA) was assessed for its antioxidant potential and ability to inhibit the growth of a food hazard bacterium Bacillus cereus in vitro and in situ. THBA displayed significant and dose-dependent cellular antioxidant potential against hydrogen peroxide-induced oxidative stress in NIH 3T3 fibroblast cells and decreased the ROS levels as well as increased the expression levels of SOD1 and SOD2 enzymes. The inhibitory spectrum of THBA confirmed its mechanistic role in the disruption of the membrane integrity of B. cereus as evidenced by the results of time-inactivation, cell membrane integrity, NPN membrane uptake, membrane potential, and electron microscopy analyses. Moreover, THBA inhibited biofilm formation by B. cereus and disrupted pre-established biofilms on a glass surface. Furthermore, THBA was also able to inhibit B. cereus in raw rice with a significant amount of reduction in CFU counts, suggesting its potential role as a natural antioxidant and antimicrobial agent.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/metabolismo , Berberina/análogos & derivados , Biofilmes/efeitos dos fármacos , Oryza/microbiologia , Alcaloides/química , Animais , Anti-Infecciosos/química , Antioxidantes/farmacologia , Bacillus cereus/fisiologia , Bacillus cereus/efeitos da radiação , Berberina/química , Berberina/farmacologia , Biofilmes/efeitos da radiação , Sobrevivência Celular/efeitos dos fármacos , Microbiologia de Alimentos , Camundongos , Células NIH 3T3 , Espécies Reativas de Oxigênio/metabolismo , Superóxido Dismutase-1/metabolismo , Raios Ultravioleta
2.
Pest Manag Sci ; 77(1): 208-216, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32677739

RESUMO

BACKGROUND: Camptothecin (CPT) and matrine (MAT) have potential as botanical pesticides against several pest species. However, the mechanisms of metabolic and physiological changes in pests induced by CPT and MAT are unknown. In this study, a toxicological test, an NMR-based metabolomic study, an enzymatic test, and an RT quantitative PCR (RT-qPCR) experiment were all conducted to examine the effect of CPT and MAT on Spodoptera litura. RESULTS: CPT (0.5-1%) exerted high toxicity against larvae of S. litura and caused growth stagnation and high mortality of larvae. A variety of metabolites were significantly influenced by 0.5% CPT, including several energy-related metabolites such as trehalose, lactate, succinate, citrate, malate, and fumarate. In contrast, MAT showed low toxicity against larvae and induced almost no changes in hemolymph metabolites of S. litura. Enzymatic tests showed that trehalase activity was significantly decreased in larvae after feeding with 0.5% CPT. RT-qPCR showed that the transcription levels of alanine aminotransferase, malate dehydrogenase, and isocitrate dehydrogenase were decreased while lactate dehydrogenase was increased in the 0.5% CPT-treated group. CONCLUSIONS: These data indicate that one of the important mechanisms of CPT against S. litura larvae is via the inhibition of trehalose hydrolysis and glycolysis. Our findings also suggest that CPT exhibits a stronger toxicological effect than MAT against S. litura, which provides basic information for the application of CPT in the control of S. litura or other lepidoptera pests.


Assuntos
Praguicidas , Alcaloides , Animais , Camptotecina/toxicidade , Larva , Quinolizinas , Spodoptera
3.
Food Chem ; 336: 127701, 2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-32781354

RESUMO

This study presents innovative research for comparison of the effect of the different dehydration techniques and methods of extraction on the antioxidant potential and bioactive compounds of Conilon and Arabica coffee flowers. The compounds were analyzed by high performance liquid chromatography and the antioxidant capacity evaluated by the 2,2'-azinobis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide assays. Among the compounds evaluated, trigonelline, gallic acid, chlorogenic acid, and caffeine were identified, with trigonelline and caffeine being those with the highest concentration. The investigated factors significantly influenced the profile of the bioactive compounds identified, and the antioxidant capacity. The 92 °C infusion of freeze-dried Conilon coffee flowers, in general, showed greater antioxidant capacity by ABTS and DPPH assays, as well as total phenolic content. Lyophilization had a positive influence on maintaining the content of phenolic compounds and antioxidant capacity of the samples. Coffee flowers proved to be a potential raw material for making tea-like drinks.


Assuntos
Antioxidantes/farmacologia , Coffea/química , Flores/química , Alcaloides/análise , Antioxidantes/química , Cafeína/análise , Ácido Clorogênico/análise , Cromatografia Líquida de Alta Pressão , Liofilização , Fenóis/análise , Extratos Vegetais/química
4.
Food Chem ; 334: 127552, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-32795786

RESUMO

Extracts of Opuntia stricta var. dillenii fruits were fractionated by semi-preparative high-performance countercurrent chromatography (HPCCC) to study the secondary metabolite formation, whereby HPCCC showed a superior separation capacity to fractionate minor metabolites compared to HPLC. A family of new peptides was detected in semi-polar fractions when monitoring the HPCCC separation by off-line injections of fractions to ESI-MS/MS. Planar structures of the major compounds, two 14-ring-membered cyclopeptide alkaloids, which were named opuntisines A and B, were elucidated by 1D- and 2D-NMR spectroscopy and HR-ESI-MS/MS spectrometry, while a combination of chemical derivatisation and degradation revealed the stereo-configurations. Specifically, the methods of Marfey and Mosher indicated l-Glu, l-Ile, l-Phe and 1S-configurations, respectively; ROESY correlations revealed 8S, 9S. The novel opuntisine A showed moderate activity against the Gram-negative bacterium Escherichia coli, but no further antibacterial, antifungal nor cytotoxic effects. This bioactive natural product class is reported for the first time in the plant family Cactaceae.


Assuntos
Alcaloides/análise , Cromatografia Líquida de Alta Pressão/métodos , Opuntia/química , Peptídeos Cíclicos/química , Alcaloides/química , Alcaloides/farmacologia , Distribuição Contracorrente , Escherichia coli/efeitos dos fármacos , Frutas/química , Frutas/metabolismo , Espectroscopia de Ressonância Magnética , Conformação Molecular , Opuntia/metabolismo , Extratos Vegetais/química , Espectrometria de Massas em Tandem
5.
Food Chem ; 339: 127864, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-32858385

RESUMO

Flavoalkaloids have been found from tea. However, there is limited information about their content in different teas. Herein, 51 tea samples were screened for flavoalkaloid content. Twelve teas with relatively higher contents of flavoalkaloids were further quantified by UPLC-TOF-MS/MS. The cultivars Yiwu and Bulangshan had the highest levels, with total flavoalkaloid contents of 3063 and 2727 µg g-1, respectively. Each of the six flavoalkaloids were at levels > 198 µg g-1 in these cultivars. Of the flavoalkaloids, etc-pyrrolidinone A had the highest content in the teas, reaching 835 µg g-1 in Yiwu. The content of the flavoalkaloids varied among tea cultivars and with processing procedures, particularly heating. The potential of using flavoalkaloids to discriminate grades of Keemun black tea was studied and discussed. The teas identified in this work with high levels of flavoalkaloids can be used in the future to study the mechanisms by which flavoalkaloids are synthesized in tea.


Assuntos
Alcaloides/análise , Alcaloides/química , Camellia sinensis/química , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas em Tandem , Manipulação de Alimentos
6.
Food Chem ; 339: 128110, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33152887

RESUMO

Piperine, as the most abundant alkaloid in pepper, gained a lot of attention for possible antioxidant and therapeutic properties. Electrochemical techniques were applied to widely evaluate the redox behavior of piperine by comparison to that of well-known antioxidants: ascorbic acid, protocatechuic acid, syringic acid, tyrosine and capsaicin used as controls. Also, electrochemistry was involved in an innovative way to investigate the potential antioxidant properties of piperine combined with different in vitro peroxidation and reducing assays: (i) 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH) scavenging; (ii) 2,2,6,6-tetramethylpiperidinyl-1-oxy (TEMPO) scavenging; (iii) ferric ions (Fe3+) reducing power; (iv) hydrogen peroxide (H2O2) scavenging. Results show that piperine readily reacts with highly oxidizing radicals and bind redox-active metal ions in a similar manner as antioxidants used as model.


Assuntos
Alcaloides/química , Antioxidantes/química , Benzodioxóis/química , Piperidinas/química , Alcamidas Poli-Insaturadas/química , Ácido Ascórbico/química , Compostos de Bifenilo/química , Óxidos N-Cíclicos/química , Técnicas Eletroquímicas , Depuradores de Radicais Livres/química , Radicais Livres/metabolismo , Peróxido de Hidrogênio/química , Ferro/química , Oxirredução , Picratos/química
7.
Pest Manag Sci ; 77(1): 510-517, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32815231

RESUMO

BACKGROUND: Plant viral diseases are difficult to control and have caused serious damage to the agricultural industry. Recently, botanical biopesticides characterized by environment friendly, safe to non-target organism and not as susceptible to produce drug resistance, have exhibited great potential to be developed as antiviral agents. To screen the natural products with antiviral effect, three alkaloids possessed anti-tobacco mosaic virus (TMV) activity were isolated from Chelidonium majus and the modes of action were investigated. RESULT: The anti-TMV effect of crude extracts at 10 mg mL-1 was 51.73%. Bioassay-guided fractionation and isolation of the compounds with anti-TMV activity were performed on the methanol extract of C. majus yielding three bioactive alkaloids namely: chelerythrine (1), chelidonine (2), and sanguinarine (3). The results of bioassay showed that chelerythrine exhibited great inactivation, proliferation inhibition and protection effects against TMV at 0.5 mg mL-1 with the efficiency of 72.67%, 77.52% and 59.34%, respectively. Chelidonine at 0.1 mg mL-1 can provide 54.90% and 64.45% inhibitions on TMV through inducing resistance in two kinds of tobacco. Sanguinarine showed a weaker protection for resisting TMV in comparison to chelerythrine and chelidonine. CONCLUSION: Chelerythrine and chelidonine displayed significant inhibitions on TMV with different modes of action. These results provided important evidence that the extracts in C. majus might be a potential source of new drugs in controlling virus disease agriculturally.


Assuntos
Alcaloides , Antivirais , Chelidonium , Vírus do Mosaico do Tabaco , Alcaloides/farmacologia , Antivirais/farmacologia , Extratos Vegetais/farmacologia
8.
Food Chem ; 340: 128132, 2021 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-33011468

RESUMO

Piperine (PIP) is an alkaloid which is potent as a therapeutic agent. However, its applications are restricted by its poor water solubility. Nanosponges (NS) derived from polymers are versatile carriers for poor water-soluble substances. The aim of this work was to synthesize ß-cyclodextrin NS, by microwave-assisted fusion, for the encapsulation of PIP. Different formulations of NS were synthesized by varying the molar ratio of ß-cyclodextrin:diphenyl carbonate (ß-CD:DPC; 1:2, 1:6 and 1:10). NS specimens derived from 1:2, 1:6 and 1:10 ß-CD:DPC molar ratios exhibited degree of substitution values of 0.345, 0.629 and 0.878, respectively. The crystallinity of NS was enhanced by increasing diphenyl carbonate concentration. A high degree of crosslinking in the NS increased the loading efficiency due to increased surface area available for bioactive inclusion. This study demonstrated the feasibility of synthesizing NS derived from ß-cyclodextrin of high crystallinity for the encapsulation of PIP at high loading capacity.


Assuntos
Alcaloides/química , Benzodioxóis/química , Nanoestruturas/química , Piperidinas/química , Alcamidas Poli-Insaturadas/química , beta-Ciclodextrinas/química , Composição de Medicamentos , Micro-Ondas , Piper nigrum/química , Piper nigrum/metabolismo , Solubilidade
9.
Trials ; 21(1): 1027, 2020 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-33334357

RESUMO

OBJECTIVES: This study aims to investigate the efficacy of curcumin-piperine co-supplementation on disease duration, severity and clinical symptoms, and inflammatory mediators in patients with coronavirus (COVID-19). TRIAL DESIGN: This is a randomized, placebo-controlled, double-blind, parallel arm clinical trial. PARTICIPANTS: All patients aged 20-75 years with the diagnosis of Covid-19 based on the PCR test. The exclusion criteria will include an age less than 20 and more than 75 years, current use of warfarin or other anticoagulant drugs, and the presence of sensitivity to herbal products such as turmeric and pepper. This study will be conducted in academic hospitals affiliated to Isfahan University of Medical Sciences, Isfahan, Iran. INTERVENTION AND COMPARATOR: Fifty outpatients will be randomly allocated in a ratio of 1:1 to receive a capsule of curcumin-piperine containing 500 mg curcumin plus 5 mg piperine or matching placebo containing 505 mg maltodextrin twice a daily, after lunch and dinner, over a period of 2 weeks. Similarly, 50 inpatients who are admitted to hospital wards excluding intensive care unit (ICU) will be randomly assigned in a ratio of 1:1 to receive a capsule curcumin-piperine or matching placebo (provided by the Sami Labs company) twice a daily, after lunch and dinner, over a period of 2 weeks. MAIN OUTCOMES: The main outcomes of this study are the efficacy of curcumin-piperine on coronavirus disease's clinical symptoms, duration, severity, and inflammatory mediators after 2 weeks of curcumin-piperine co-supplementation. RANDOMISATION: Randomization sequences will be generated with the use of a random-number table with a permuted block design (block size of 4) and stratification according to the gender variable (male vs. female). These sequences will be prepared by an independent statistician and will be kept in opaque, sealed, numbered envelopes which will be opened only at the time of enrollment. The allocation ratio in intervention and control groups is 1:1. Researchers and all patients will be unaware of the study-group assignment until the completion of data analyses. BLINDING (MASKING): This study is a double-blind clinical trial (participant, researcher). The curcumin-piperine and placebo supplements are packaged in similar numbered drug containers, and the researcher and all patients will be unaware of the study assignment until the end of the study. NUMBERS TO BE RANDOMISED (SAMPLE SIZE): The calculated total sample size is 100 patients, with 25 patients in each group. TRIAL STATUS: The protocol is Version 2.0, May 24, 2020. Recruitment began May 4, 2020, and is anticipated to be completed by April 19, 2021. TRIAL REGISTRATION: This trial has been registered by the title of "Effect of curcumin-piperine co-supplementation on disease duration, severity and clinical signs, and inflammatory factors in patients with coronavirus (COVID-19): A randomized, double-blind, placebo-controlled clinical trial study" in the Iranian Registry of Clinical Trials (IRCT) with code "IRCT20121216011763N46", https://www.irct.ir/trial/47529 . The registration date is May 4, 2020. FULL PROTOCOL: The full protocol is attached as an additional file, accessible from the Trials website (Additional file 1). In the interest in expediting dissemination of this material, the familiar formatting has been eliminated; this Letter serves as a summary of the key elements of the full protocol.


Assuntos
Alcaloides/administração & dosagem , Benzodioxóis/administração & dosagem , Curcumina/administração & dosagem , Suplementos Nutricionais , Piperidinas/administração & dosagem , Alcamidas Poli-Insaturadas/administração & dosagem , Método Duplo-Cego , Hospitalização , Humanos , Irã (Geográfico) , Ensaios Clínicos Controlados Aleatórios como Assunto , Fatores de Tempo , Resultado do Tratamento
10.
Antivir Chem Chemother ; 28: 2040206620984076, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33372806

RESUMO

Corona Virus Disease 2019 (COVID-19) is a pandemic caused by Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). Exploiting the potentials of phytocompounds is an integral component of the international response to this pandemic. In this study, a virtual screening through molecular docking analysis was used to screen a total of 226 bioactive compounds from African herbs and medicinal plants for direct interactions with SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). From these, 36 phytocompounds with binding affinities higher than the approved reference drugs (remdesivir and sobosivir), were further docked targeting the active sites of SARS-CoV-2, as well as SARS-CoV and HCV RdRp. A hit list of 7 compounds alongside two positive controls (remdesivir and sofosbuvir) and two negative controls (cinnamaldehyde and Thymoquinone) were further docked into the active site of 8 different conformations of SARS-CoV-2 RdRp gotten from molecular dynamics simulation (MDS) system equilibration. The top docked compounds were further subjected to predictive druglikeness and ADME/tox filtering analyses. Drugable alkaloids (10'-hydroxyusambarensine, cryptospirolepine, strychnopentamine) and flavonoids (usararotenoid A, and 12α-epi-millettosin), were reported to exhibit strong affinity binding and interactions with key amino acid residues in the catalytic site, the divalent-cation-binding site, and the NTP entry channel in the active region of the RdRp enzyme as the positive controls. These phytochemicals, in addition to other promising antivirals such as remdesivir and sofosbuvir, may be exploited towards the development of a cocktail of anti-coronavirus treatments in COVID-19. Experimental studies are recommended to validate these study.


Assuntos
Alcaloides/farmacologia , Antivirais/farmacologia , Flavonoides/farmacologia , /efeitos dos fármacos , África , Alcaloides/farmacocinética , Avaliação Pré-Clínica de Medicamentos , Flavonoides/farmacocinética , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Compostos Fitoquímicos/farmacologia , /enzimologia
11.
Zhongguo Zhong Yao Za Zhi ; 45(21): 5129-5142, 2020 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-33350228

RESUMO

Genus Veratrum plants contain a diversity of steroidal alkaloids, so far at least 184 steroidal alkaloids attributed to cevanine type(A-1~A-69), veratramine type(B-1~B-21), jervanine type(C-1~C-31), solanidine type(D-1~D-10) and verazine type(E-1~E-53), respectively, have been isolated and identified in the genus Veratrum. Their pharmacological activities mainly focused on decreasing blood pressure, anti-platelet aggregation and anti-thrombosis, anti-inflammatory and analgesic, and antitumor effect. This paper classified and summarized the 184 kind of steroidal alkaloids from the Veratrum plants and their major pharmalogical activities in order to provide the scientific basis for the further development and utilization of active alkaloids.


Assuntos
Alcaloides , Veratrum , Alcaloides/farmacologia , Analgésicos , Agregação Plaquetária , Esteroides/farmacologia
12.
Zhongguo Zhong Yao Za Zhi ; 45(21): 5238-5247, 2020 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-33350241

RESUMO

This article is to investigate the effect of piperine on the small intestine of mice with Parkinson's disease with dementia(PDD). Ninety-six C57 BL/6 mice of SPF grade were randomly divided into 8 groups(male, 12 in each group): normal group, model group, autophagy inhibitor group(6-amino-3-methylpurine, 3 MA, 30 mg·kg~(-1)), autophagy activator group(rapamycin, 1 mg·kg~(-1)), low, medium, and high dose piperine groups(10, 20, 40 mg·kg~(-1)), and medopar group(112.5 mg·kg~(-1)). Except for the normal group, mice in each group were injected subcutaneously with reserpine(0.1 mg·kg~(-1)) once every 48 hours for 40 days. In addition, on the 20 th day of administration, except for the normal group, the mice in the other groups were subjected to bilateral common carotid artery occlusion to finally prepare PDD models. At the same time, each group was given the corresponding drug treatment once a day for 40 days. After the last administration, the behavioral changes of mice were observed by autonomic activity experiment and hot plate experiment. The expression levels of α-synuclein(α-syn) and tyrosine hydroxylase(TH) in the small intestine were detected by immunohistochemistry. The expression levels of beclin-1, microtubule-associated protein 1 light chain 3 B(LC3 B) and p62 in the small intestine were detected by immunofluorescence assay. Hematoxylin-eosin staining was used to observe the pathological morphology of small intestine tissues in each group. Enzyme-linked immunosorbent assay was adopted for detection of ß-amyloid precursor protein(APP), p-tau, acetylcholine transferase(ChAT), interleukin-6(IL-6) and tumor necrosis factor-α(TNF-α) in small intestine. Real-time fluorescent quantitative polymerase chain reaction was used to detect the expression of α-syn, TH, beclin-1, microtubule-associated protein 1 light chain 3(LC3), and p62 mRNA and mmu-miR-99 a-5 p in the small intestine. The results of this study showed that, as compared with the model group, the number of activities, the expression levels of ChAT, TH, and p62 were significantly increased in the 3 MA group, the various piperine dose groups, and the medopar group(P<0.05), and their first foot licking time was shortened; APP, p-tau, IL-6, TNF-α, α-syn, beclin-1, LC3 B and mmu-miR-99 a-5 p expression levels were significantly reduced(P<0.05). However, as compared with the model group, the number of activities, ChAT, TH, and p62 expression levels in the rapamycin group were significantly reduced(P<0.05), and the APP, p-tau, IL-6, TNF-α, α-syn, beclin-1, LC3 B and mmu-miR-99 a-5 p expression levels were significantly increased(P<0.05). As compared with the 3 MA group, the number of activities, ChAT, TH, and p62 expression levels were significantly reduced in the low and medium dose piperine groups and rapamycin group(P<0.05); howe-ver, their first foot licking time was significantly prolonged, APP, p-tau, IL-6, TNF-α, α-syn, beclin-1, LC3 B and mmu-miR-99 a-5 p expression levels were increased significantly(P<0.05). As compared with the medopar group, the number of activities, ChAT, TH, and p62 expression levels were significantly reduced in low dose piperine group and rapamycin group(P<0.05), but their first foot licking time was significantly extended, and APP, p-tau, IL-6, TNF-α, α-syn, beclin-1, LC3 B and mmu-miR-99 a-5 p expression levels were significantly increased(P<0.05). In addition, as compared with the normal group, the small intestinal epithelial cells of the model group and the rapamycin group were shed off a lot, with severe damages of intestinal mucosa as well as edema and shedding of the small intestine villi. After administration of the therapeutic interventions, the small intestinal epithelial cells of the 3 MA group, each dose group of piperine, and the medopa group were slightly damaged and the villi were slightly shed off. In summary, piperine has a protective effect on the small intestine of PDD model mice, showing reduced expression of mmu-miR-99 a-5 p, pro-inflammatory factors and autophagy factors, and the mechanism of slowing PDD pathological symptoms may be related to the inhibition of autophagy.


Assuntos
Demência , Doença de Parkinson , Alcaloides , Animais , Autofagia , Benzodioxóis , Intestino Delgado , Masculino , Camundongos , Piperidinas , Alcamidas Poli-Insaturadas
13.
Zhongguo Zhong Yao Za Zhi ; 45(20): 4836-4845, 2020 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-33350254

RESUMO

Alcohol is considered to be one of the main causes for gastric injury, and alcoholic gastric injury has been becoming one of the global health problems, which seriously affects the quality of human life. Many studies suggest that the active components extracted from Chinese herbal medicine can effectively reduce the degree of alcohol-induced gastric injury. The active components and its mechanism of anti-alcoholic gastric injury of Chinese herbal medicine reported in recent five years were preliminarily summarized according to the classification of terpenoids, flavonoids, polyphenols, polysaccharides, volatile oils, phenylpropanoids and alkaloids in this paper. The terpenoids could improve oxidative stress and inflammatory response by regulating relevant signaling pathways. The flavonoids are mainly related to antioxidant and anti-inflammatory properties. The polyphenols mainly regulate the level of relevant factors involved in inflammatory pathway, oxidative stress and apoptosis pathway. The polysaccharides could enhance the ability of gastric mucosal defense factor by inhibiting oxidative stress injury and inflammatory response. Phenylpropanoids could enhance the gastric mucosal defense factor. The volatile oils mainly inhibit H~+/K~+-ATPase activity or inflammatory reaction. Alkaloids are closely related to the inhibition of inflammatory response and the improvement of antioxidant system. This paper aims to provide reference for further research and development of Chinese herbal medicine against alcoholic gastric injury.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Anti-Inflamatórios , Antioxidantes , Flavonoides , Humanos
14.
Artigo em Russo | MEDLINE | ID: mdl-33244961

RESUMO

OBJECTIVE: To identify polymorphisms in the genes of dopaminergic and serotonergic systems associated with the risk of suicidal behavior in individuals with dependence on synthetic cathinones. MATERIAL AND METHODS: One hundred and eighty-two men with the diagnosis of Substance dependence (ICD-10 F15) tested positive for metabolites of synthetic cathinones (a-PVP, MDPV) in the urine were studied. Genotyping was performed for rs1800497 DRD2, rs4646984 DRD4, VNTR 40 b.p. SLC6A3, rs27072 SLC6A3, rs6313 HTR2A and rs6296 HTR1B using PCR and RFLP technique. RESULTS AND CONCLUSION: It was found that the genes of the serotonergic system HTR2A and HTR1B are predictors of the development of some endophenotypes of suicidal behavior in individuals with dependence on synthetic cathinones.


Assuntos
Alcaloides , Transtornos Relacionados ao Uso de Substâncias , Suicídio , Proteínas da Membrana Plasmática de Transporte de Dopamina , Endofenótipos , Humanos , Masculino , Polimorfismo Genético , Receptor 5-HT1B de Serotonina/genética , Receptor 5-HT2A de Serotonina/genética , Transtornos Relacionados ao Uso de Substâncias/genética
15.
Sheng Wu Gong Cheng Xue Bao ; 36(10): 2001-2016, 2020 Oct 25.
Artigo em Chinês | MEDLINE | ID: mdl-33169566

RESUMO

Pictet-Spenglerases (P-Sases) catalyze the Pictet-Spengler (P-S) reactions and exhibit high stereoselectivity and regioselectivity under mild conditions. The typical P-S reaction refers to the condensation and recyclization of ß-arylethylamine with aldehyde or ketone under acidic conditions to form tetrahydroisoquinoline and ß-carboline alkaloid derivatives. The related enzymatic products of P-Sases are the backbones of various bioactive compounds, including clinical drugs: morphine, noscapine, quinine, berberine, ajmaline, morphine. Furthermore, the activity of P-Sases in stereoselective and regioselective catalysis is also valuable for chemoenzymatic synthesis. Therefore, this review summarizes the research progress in the discovery, functional identification, biological characteristics and catalytic applications of P-Sases, which provide the useful theoretical reference in future P-Sases research and development.


Assuntos
Alcaloides , Enzimas , Pesquisa , Tetra-Hidroisoquinolinas , Alcaloides/química , Catálise , Enzimas/metabolismo , Pesquisa/tendências , Tetra-Hidroisoquinolinas/química
16.
Zhongguo Zhong Yao Za Zhi ; 45(19): 4617-4624, 2020 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-33164425

RESUMO

With matrine(MAT) as the model drug, to prepare nano graphene oxide(NGO)-based MAT in situ gel(MAT-NGO-gel), a kind of drug for tumor treatment in combination with phototheraphy, and investigate the physicochemical properties and anti-tumor effects in vivo of MAT-NGO-gel. First, HPLC method was established to measure the content of MAT in the gel. The ultrasonic method was used to load MAT onto the surface of NGO, and then poloxamer 188 and poloxamer 407 were chosen as the main materials to prepare MAT-NGO-gel. The optimum prescription was selected with the gelation temperature as the index. Finally, the drug loading rate, micromorphology, phototherrmal conversion characteristics and drug release in vitro of MAT-NGO-gel were characterized. In the optimized prescription, the concentration of poloxamer 188 and poloxamer 407 was 2% and 20% respectively, and the mass ratio of NGO and MAT was 1∶1. The gelation temperature and drug loading rate of MAT-NGO-gel prepared by the optimal prescription process was 37.5 ℃ and 16.7%. Under 808 nm laser irradiation, MAT-NGO-gel showed obvious concentration-and time-dependent photothermal conversion characteristics. In vitro release experiments showed that MAT-NGO-gel had temperature-dependent release characteristics. The pharmacodynamics of MAT solution, NGO-gel and MAT-NGO-gel were studied by using S180 tumor-bearing mice and 808 nm laser. The relative tumor volume and body weight of the tumor-bearing mice were plotted over time. After the experiment, the tumor tissues of each group were taken and the histopathological changes were observed by HE staining. The results of pharmacodynamic studies demonstrated that when compared with NS group and NGO-gel group, the body weights of mice in MAT-NGO-gel group and MAT-NGO-gel + laser group were higher, and the relative tumor volume growth was slower. The results of HE stained pathological sections showed that the tumor cells count for the mice in MAT-NGO-gel group and MAT-NGO-gel + laser group was significantly reduced, with obvious nuclear fragmentation and nucleolysis in these two groups. These results suggested that MAT-NGO-gel, especially combined with 808 nm laser, had stronger anti-tumor activity in vivo. The prescription process of MAT-NGO-gel in this experiment was stable and feasible. As compared with MAT solution, MAT-NGO-gel showed obvious sustained and temperature-dependent drug release characteristics. MAT-NGO-gel had much more obvious anti-tumor activity in vivo when combined with 808 nm laser irradiation. This study could provide certain theoretical basis for the therapy of malignant tumor with multiple mechanisms.


Assuntos
Alcaloides , Óxidos , Animais , Liberação Controlada de Fármacos , Camundongos , Quinolizinas
17.
Lancet Glob Health ; 8(11): e1408-e1417, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-33069301

RESUMO

BACKGROUND: Smoking cessation is important in patients with tuberculosis because it can reduce the high rates of treatment failure and mortality. We aimed to assess the effectiveness and safety of cystine as a smoking cessation aid in patients with tuberculosis in Bangladesh and Pakistan. METHODS: We did a randomised, double-blind, placebo-controlled, trial at 32 health centres in Bangladesh and Pakistan. Eligible patients were adults (aged >18 years in Bangladesh; aged >15 years in Pakistan) with pulmonary tuberculosis diagnosed in the previous 4 weeks, who smoked tobacco on a daily basis and were willing to stop smoking. Patients were randomly assigned (1:1) to receive behavioural support plus either oral cytisine (9 mg on day 0, which was gradually reduced to 1·5 mg by day 25) or placebo for 25 days. Randomisation was done using pregenerated block randomisation lists, stratified by trial sites. Investigators, clinicians, and patients were masked to treatment allocation. The primary outcome was continuous abstinence at 6 months, defined as self-report (of not having used more than five cigarettes, bidis, a water pipe, or smokeless tobacco products since the quit date), confirmed biochemically by a breath carbon monoxide reading of less than 10 parts per million. Primary and safety analysis were done in the intention-to-treat population. This trial is registered with the International Standard Randomised Clinical Trial Registry, ISRCTN43811467, and enrolment is complete. FINDINGS: Between June 6, 2017, and April 30, 2018, 2472 patients (1527 patients from Bangladesh; 945 patients from Pakistan) were enrolled and randomly assigned to receive cytisine (n=1239) or placebo (n=1233). At 6 months, 401 (32·4%) participants in the cytisine group and 366 (29·7%) participants in the placebo group had achieved continuous abstinence (risk difference 2·68%, 95% CI -0·96 to 6·33; relative risk 1·09, 95% CI 0·97 to 1·23, p=0·114). 53 (4·3%) of 1239 participants in the cytisine group and 46 (3·7%) of 1233 participants in the placebo group reported serious adverse events (94 events in the cytisine group and 90 events in the placebo group), which included 91 deaths (49 in the cytisine group and 42 in the placebo group). None of the adverse events were attributed to the study medication. INTERPRETATION: Our findings do not support the addition of cytisine to brief behavioural support for the treatment of tobacco dependence in patients with tuberculosis. FUNDING: European Union Horizon 2020 and Health Data Research UK. TRANSLATIONS: For the Bengali and Urdu translations of the abstract see Supplementary Materials section.


Assuntos
Alcaloides/uso terapêutico , Abandono do Hábito de Fumar/métodos , Tabagismo/terapia , Tuberculose/epidemiologia , Adulto , Azocinas/uso terapêutico , Bangladesh/epidemiologia , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Paquistão/epidemiologia , Psicoterapia Breve , Quinolizinas/uso terapêutico , Tabagismo/psicologia , Resultado do Tratamento
18.
PLoS One ; 15(10): e0239365, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33001998

RESUMO

The growth of filamentous fungi during the spontaneous cocoa bean fermentation leads to inferior cocoa bean quality and poses a health risk for consumers due to the potential accumulation of mycotoxins. We recently developed anti-fungal cultures with the capacity to inhibit the growth of mycotoxigenic filamentous fungi on cocoa beans. However, it is not clear how these anti-fungal cultures affect the fermentation process and cocoa bean quality. For that, the anti-fungal co-cultures, Lactobacillus fermentum M017-Saccharomyces cerevisiae H290 (A) and Lb. fermentum 223-S. cerevisiae H290 (B), were applied to 180-kg box fermentations in Honduras in three time-independent replications each including a spontaneous control fermentation. The comparison of inoculated and spontaneous fermentation processes revealed that the co-cultures only marginally affected the fermentation process and cocoa bean quality. Microorganisms reached maximal levels of 6.2-7.6 log CFU/g of yeasts and acetic acid bacteria and 7.9-9.5 log CFU/g of lactic acid bacteria during all fermentations and led to maximal metabolite concentrations in bean cotyledons of 4-12 mg/g ethanol, 2-6 mg/g lactic acid and 6-14 mg/g acetic acid. The fermentation and drying processes resulted in 38-90 mg epicatechin equivalents/g in the cotyledons of dried beans. However, the co-cultures led to up to ten times higher mannitol levels in cotyledons of inoculated beans compared to beans during spontaneous fermentation, and caused a slower fermentation process, detectable as up to 8-12 °C lower temperatures in the centre of the fermenting pulp-bean mass and up to 22% lower proportions of well-fermented beans after drying. Co-culture B-with Lb. fermentum 223 -led to improved cocoa bean quality compared to co-culture A-with Lb. fermentum M017 -, i.e. cocoa beans with 0.5-1.9 mg/g less acetic acid, 4-17% higher shares of well-fermented beans and, on a scale from 0 to 10, to 0.2-0.6 units lower astringency, up to 1.1 units lower off-flavours, and 0.2-0.9 units higher cocoa notes. Therefore, the anti-fungal co-culture B is recommended for future applications and its capacity to limit fungal growth and mycotoxin production during industrial-scale cocoa bean fermentation should be investigated in further studies.


Assuntos
Cacau/metabolismo , Cacau/microbiologia , Técnicas de Cocultura , Fermentação , Qualidade dos Alimentos , Lactobacillus fermentum/fisiologia , Saccharomyces cerevisiae/fisiologia , Alcaloides/análise , Cacau/química , Concentração de Íons de Hidrogênio , Lactobacillus fermentum/crescimento & desenvolvimento , Polifenóis/análise , Saccharomyces cerevisiae/crescimento & desenvolvimento , Temperatura , Fatores de Tempo
19.
Nat Commun ; 11(1): 5314, 2020 10 20.
Artigo em Inglês | MEDLINE | ID: mdl-33082332

RESUMO

The powerful insecticidal and multi-drug-resistance-reversing activities displayed by the stemofoline group of alkaloids render them promising lead structures for further development as commercial agents in agriculture and medicine. However, concise, enantioselective total syntheses of stemofoline alkaloids remain a formidable challenge due to their structural complexity. We disclose herein the enantioselective total syntheses of four stemofoline alkaloids, including (+)-stemofoline, (+)-isostemofoline, (+)-stemoburkilline, and (+)-(11S,12R)-dihydrostemofoline, in just 19 steps. Our strategy relies on a biogenetic hypothesis, which postulates that stemoburkilline and dihydrostemofolines are biogenetic precursors of stemofoline and isostemofoline. Other highlights of our approach are the use of Horner-Wadsworth-Emmons reaction to connect the two segments of the molecule, an improved protocol allowing gram-scale access to the tetracyclic cage-type core, and a Cu-catalyzed direct and versatile nucleophilic alkylation reaction on an anti-Bredt iminium ion. The synthetic techniques that we developed could also be extended to the preparation of other Stemona alkaloids.


Assuntos
Compostos Heterocíclicos de 4 ou mais Anéis/síntese química , Inseticidas/síntese química , Stemonaceae/química , Alcaloides/síntese química , Alcaloides/química , Compostos Heterocíclicos de 4 ou mais Anéis/química , Inseticidas/química , Estrutura Molecular , Extratos Vegetais/síntese química , Extratos Vegetais/química , Estereoisomerismo
20.
Toxicon ; 188: 134-141, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33091389

RESUMO

The prolonged consumption of Ipomoea carnea produces neurologic symptoms in animals and a typical histological lesion, cytoplasmic vacuolization, especially in neurons. The toxic principles of I. carnea are the alkaloids swainsonine and calystegines B1, B2, B3 and C1. In this study, primary brain cultures from newborn mouse containing mixed glial cells were utilized. These cells were exposed to Ipomoea extracts containing between 0 and 250 µM swainsonine for 48 h. Morphological changes were investigated through Phase Contrast microscopy and Rosenfeld's staining. The extract induced cytoplasmic vacuolization in astrocytes and microglia in a dose dependent manner, being more evident when cultures were exposed to 250 µM of swainsonine. In addition, acridine orange staining evidenced an increase in the number of lysosomes in both microglia and astrocytes cells. Consistent with this, scanning electron microscopy also showed that both types of cells presented morphological characteristics of cell activation. Ultrastructurally, cells showed vacuoles filled with amorphous material and surrounded by a single membrane and also multilayer membranes. Taken together, these findings suggest that swainsonine along with calystegines, are probably responsible for the activation of glial cells due to a possible lysosomal dysfunction and therefore intracellular storage. Our results demonstrate that this in vitro glial cell model is a very good alternative to in vivo studies that require several weeks of animal intoxication to observe similar neurotoxic effects.


Assuntos
Ipomoea , Extratos Vegetais/toxicidade , Alcaloides , Animais , Cabras , Lisossomos , Camundongos , Microscopia Eletrônica de Varredura , Neuroglia , Nortropanos , Alcaloides de Solanáceas , Swainsonina , Tropanos
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