Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 47
Filtrar
1.
Phytopathology ; 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38916927

RESUMO

Valsa pyri, the causal agent of pear canker disease, typically induces cankers on the bark of infected trees and even leads to tree mortality. Secondary metabolites (SMs) produced by pathogenic fungi play a crucial role in the pathogenic process. In this study, secondary metabolic regulator VpLaeA was identified in V. pyri. VpLaeA was found to strongly affect the pathogenicity, fruiting body formation and toxicity of SMs of V. pyri. Additionally, VpLaeA was also found to be required for the response of V. pyri to some abiotic stresses. Transcriptome data analysis revealed that many of differentially expressed genes were involved in the secondary metabolite biosynthesis (SMB). Among them, about one third of SMB core genes were regulated by VpLaeA at different periods. Seven differentially expressed SMB core genes (VpPKS9, VpPKS10, VpPKS33, VpNRPS6, VpNRPS7, VpNRPS16, and VpNRPS17) were selected for knockout. Two modular polyketide synthase (PKS) genes (VpPKS10 and VpPKS33), which were closely related to the virulence of V. pyri from the above seven genes were identified. Notably, VpPKS10 and VpPKS33 also affected the production of fruiting body of V. pyri, but didn't participate in the resistance of V. pyri to abiotic stresses. Overall, this study demonstrates the multifaceted biological functions of VpLaeA in V. pyri, and identifies two toxicity-associated PKS genes in Valsa species fungi for the first time.

2.
J Nat Prod ; 86(7): 1855-1861, 2023 07 28.
Artigo em Inglês | MEDLINE | ID: mdl-37368408

RESUMO

Two new caulamidines C (2) and D (4) and three isocaulamidines B, C, and D (1, 3, and 5) along with the known compound caulamidine B (6) were isolated from the marine ascidian Polyandrocarpa sp. Their structures were elucidated by analysis of nuclear magnetic resonance (NMR) and electronic circular dichroism (ECD) data. Isocaulamidines have an altered pattern of N-methyl substitution (N-15 vs N-13 in the caulamidines) with a concomitant double-bond rearrangement to provide a new C-14/N-13 imine functionality. Caulamidine C (2) and isocaulamidine C (3) are the first members of this alkaloid family with two chlorine substituents in the core 6H-2,6-naphthyridine ring system.


Assuntos
Alcaloides , Antineoplásicos , Urocordados , Animais , Urocordados/química , Alcaloides/farmacologia , Alcaloides/química , Espectroscopia de Ressonância Magnética , Imageamento por Ressonância Magnética , Estrutura Molecular
3.
J Nat Prod ; 85(5): 1419-1427, 2022 05 27.
Artigo em Inglês | MEDLINE | ID: mdl-35465663

RESUMO

Chemical investigation of the marine hydroid Dentitheca habereri led to the identification of eight new diacylated zoanthoxanthin alkaloids, named dentithecamides A-H (1-8), along with three previously reported analogues, zoamides B-D (9-11). The structures of compounds 1-11 were elucidated by spectroscopic and spectrometric analyses, including IR, HRESIMS, and NMR experiments, and by comparison with literature data. Compounds 1-11 are the first zoanthoxanthin alkaloids to be reported from a hydroid. Dentithecamides A (1) and B (2) along with zoamides B-D (9-11), which all share a conformationally mobile cycloheptadiene core, inhibited PAX3-FOXO1 regulated transcriptional activity and thus provided a structural framework for the potential development of more potent PAX3-FOXO1 inhibitors.


Assuntos
Alcaloides , Imidazóis , Alcaloides/química
4.
Plant Dis ; 106(9): 2462-2469, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35196100

RESUMO

Valsa mali, the causal agent of apple Valsa canker, produces several phytotoxic metabolites to promote infection. Bioassay and 1H nuclear magnetic resonance (NMR)-guided isolation from the culture filtrate of V. mali strain 03-8 led to the identification of seven compounds including three unreported ones, ethyl phloretate (1), ethyl p-coumarate (2), and 1-p-hydroxybenzoyl glycerol (3). Compounds 1 and 2 produced significant phytotoxicity, with average lesion areas of 6.22 and 3.74 mm2, along with 2.96 and 3.47 mm2 at 1 mg/ml on mature and tissue-cultured apple leaves, respectively, whereas compound 3 did not cause any symptoms on host plants. The necrotic lesion area of compounds 1 and 2 on tobacco leaves was 52.65 and 48.28 mm2, respectively, compared with the negative control (0.46 mm2) at 1 mg/ml. At the same concentration, compounds 1 and 2 showed no significant influence on the germination rate of lettuce seeds while significantly decreasing the root length of lettuce seedlings to 6.74 and 4.67 mm, respectively, compared with that treated with sterile distilled water (22.01 mm). The discovery indicated that compounds 1 and 2 could be considered as non-host-specific toxins. Furthermore, compounds 1 and 2 could cause cell shrinkage, organelle damage, plasmolysis, and eventually ruptured protoplasmic membranes with cell death for their phytotoxicity in the host plants under optical microscopy and transmission electron microscopy. The results shed light on the mechanism for toxins 1 and 2 in V. mali-infected plants at the macroscopic and cellular levels.


Assuntos
Ascomicetos , Malus , Ascomicetos/metabolismo , Germinação , Doenças das Plantas
5.
Pestic Biochem Physiol ; 171: 104697, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33357538

RESUMO

Glycoprotein (GP)-1 is a glycoprotein elicitor with antiviral activity found in Streptomyces kanasensis zx01. GP-1 can induce programmed cell death (PCD) in vitro; however, the underlying mechanism is unclear. In the present study, we demonstrated that GP-1 induced PCD in tobacco suspension cells, which was modulated by hydrogen peroxide (H2O2). GP-1 participated in and modulated biologically relevant signaling in plant cells. GP-1 induced tobacco cell death in a dose- and time-dependent manner; affected the expression of BRI1-associated receptor kinase 1 (BAK1) and the accumulation of salicylic acid (SA), which are related to PCD; and enzymatic activities and mitochondrial functions. In conclusion, GP-1-induced PCD in tobacco may be mediated by H2O2 which alters BAK1 and SA levels, as well as mitochondrial and gene function. This cell signal cascade played an important role in the process of GP-1 induced plant disease resistance.


Assuntos
Peróxido de Hidrogênio , Nicotiana , Apoptose , Glicoproteínas , Streptomyces
6.
Mar Drugs ; 15(4)2017 Apr 13.
Artigo em Inglês | MEDLINE | ID: mdl-28406457

RESUMO

A new sterol, (23R)-methoxycholest-5,24-dien-3ß-ol (1), two new ceramides, (2S,3R,4E,8E)-2-(tetradecanoylamino)-4,8-octadecadien-l,3-diol (6) and (2S,3R,2'R,4E,8E)-2-(tetradecanoylamino)-4,8-octadecadien-l,3,2'-triol (7), together with three known sterols (2-4), a lactone (5) and two ceramides (8,9), were isolated from the marine bryozoan Cryptosula pallasiana, collected at Huang Island of China. The structures of the new compounds were elucidated by extensive spectroscopic analyses, chemical methods and quantum electronic circular dichroism (ECD) calculations. Among the isolated compounds, sterol 1 possessed a rare side chain with a methoxy group at C-23, and a double bond between C-24 and C-25. Ceramides 6 and 7 possessed 14 carbons in their long-chain fatty acid base (FAB), which were different from the normal ceramides with 16 carbons in the FAB. Moreover, compounds 5 and 8 were isolated for the first time from marine bryozoans. Compounds 1-9 were evaluated for their cytotoxicity against human tumor cell lines HL-60, Hep-G2 and SGC-7901. The results showed that lactone 5 appears to have strong cytotoxicity against the test tumor cell lines, with IC50 values from 4.12 µM to 7.32 µM, and sterol 1 displayed moderate cytotoxicity with IC50 values between 12.34 µM and 18.37 µM, while ceramides 6-9 showed weak cytotoxicity with IC50 ranging from 21.13 µM to 58.15 µM.


Assuntos
Organismos Aquáticos/metabolismo , Briozoários/metabolismo , Esteróis/metabolismo , Esteróis/farmacologia , Animais , Linhagem Celular Tumoral , Ceramidas/metabolismo , China , Ácidos Graxos/metabolismo , Células HL-60 , Células Hep G2 , Humanos , Estrutura Molecular
7.
Int J Syst Evol Microbiol ; 65(Pt 5): 1561-1566, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25713049

RESUMO

A novel Gram-stain-positive, motile, catalase- and oxidase-positive, endospore-forming, facultatively anaerobic rod, designated strain JSM 100118(T), was isolated from an oyster (Crassostrea hongkongensis) collected from the tidal flat of Naozhou Island in the South China Sea. Strain JSM 100118(T) was able to grow with 0-13% (w/v) NaCl (optimum 2-5%), at pH 5.5-10.0 (optimum pH 7.5) and at 5-50 °C (optimum 30-35 °C). The cell-wall peptidoglycan contained meso-diaminopimelic acid as the diagnostic diamino acid. The predominant respiratory quinone was menaquinone-7 and the major cellular fatty acids were anteiso-C15 : 0, iso-C15 : 0, C16 : 0 and C16 : 1ω11c. The polar lipids consisted of diphosphatidylglycerol, phosphatidylethanolamine, phosphatidylglycerol, an unknown glycolipid and an unknown phospholipid. The genomic DNA G+C content was 35.9 mol%. Phylogenetic analysis based on 16S rRNA gene sequences indicated that strain JSM 100118(T) belonged to the genus Bacillus , and was most closely related to Bacillus litoralis SW-211(T) (98.9% 16S rRNA gene sequence similarity), Bacillus halosaccharovorans E33(T) (98.3%), Bacillus niabensis 4T19(T) (97.8%) and Bacillus herbersteinensis D-1,5a(T) (97.1%). The combination of results from the phylogenetic analysis, DNA-DNA hybridization, and phenotypic and chemotaxonomic characterization supported the conclusion that strain JSM 100118(T) represents a novel species of the genus Bacillus , for which the name Bacillus crassostreae sp. nov. is proposed. The type strain is JSM 100118(T) ( = CTCC AB 2010452(T) =DSM 24486(T) =JCM 17523(T)).


Assuntos
Bacillus/classificação , Crassostrea/microbiologia , Filogenia , Animais , Bacillus/genética , Bacillus/isolamento & purificação , Composição de Bases , China , DNA Bacteriano/genética , Ácido Diaminopimélico/química , Ácidos Graxos/química , Dados de Sequência Molecular , Hibridização de Ácido Nucleico , Peptidoglicano/química , Fosfolipídeos/química , RNA Ribossômico 16S/genética , Análise de Sequência de DNA , Vitamina K 2/análogos & derivados , Vitamina K 2/química
8.
Zhong Yao Cai ; 38(12): 2483-6, 2015 Dec.
Artigo em Zh | MEDLINE | ID: mdl-27352528

RESUMO

OBJECTIVE: To study the impact of climatic factors on the major medical component in Smilax china, and to supply a scientific and standard operation protocol on the introduction and cultivation. METHODS: Detect the content of major medical components, such as baicalin and astibin, in Smilax china from eight counties of Xiangxi Autonomous Prefecture. And establish their relationship with annual average temperature, Jan average temp, Jul average temp, valid accumulative temp (≥ 10 degress C), annual maximum temp, annual minimum temp, annual precipitation, annual sunshine amount, non-frost period and relative humidity by using the methods of partial least squares regression analysis (PLS). RESULTS: Relative humidity, annual minimum temp and annual precipitation are the dominant factors. Annual minimum temp, annual average temp and valid accumulative temp were significantly correlated to the content of major medical components, thus, relative humidity, annual precipitation and non-frost period were negatively related to them. CONCLUSION: This study provides a scientific basis for resources protection,introduction and cultivation of Smilax china.


Assuntos
Plantas Medicinais/química , Smilax/química , Luz Solar , Temperatura , China , Umidade
9.
Mar Drugs ; 12(4): 1987-2003, 2014 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-24699114

RESUMO

Five new ceramides, neritinaceramides A (1), B (2), C (3), D (4) and E (5), together with six known ceramides (6-11), two known alkyl glycerylethers (12 and 13) and a known nucleoside (14), were isolated from marine bryozoan Bugula neritina, which inhabits the South China Sea. The structures of the new compounds were elucidated as (2S,3R,3'S,4E,8E,10E)-2-(hexadecanoylamino)-4,8,10-octadecatriene-l,3,3'-triol (1), (2S,3R,2'R,4E,8E,10E)-2-(hexadecanoylamino)-4,8,10-octadecatriene-l,3,2'-triol (2), (2S,3R,2'R,4E,8E,10E)-2-(octadecanoylamino)-4,8,10-octadecatriene-l,3,2'-triol (3), (2S,3R,3'S,4E,8E)-2-(hexadecanoylamino)-4,8-octadecadiene-l,3,3'-triol (4) and (2S,3R,3'S,4E)-2-(hexadecanoylamino)-4-octadecene-l,3,3'-triol (5) on the basis of extensive spectral analysis and chemical evidences. The characteristic C-3'S hydroxyl group in the fatty acid moiety in compounds 1, 4 and 5, was a novel structural feature of ceramides. The rare 4E,8E,10E-triene structure in the sphingoid base of compounds 1-3, was found from marine bryozoans for the first time. The new ceramides 1-5 were evaluated for their cytotoxicity against HepG2, NCI-H460 and SGC7901 tumor cell lines, and all of them exhibited selective cytotoxicity against HepG2 and SGC7901 cells with a range of IC50 values from 47.3 µM to 58.1 µM. These chemical and cytotoxic studies on the new neritinaceramides A-E (1-5) added to the chemical diversity of B. neritina and expanded our knowledge of the chemical modifications and biological activity of ceramides.


Assuntos
Antineoplásicos/farmacologia , Briozoários/metabolismo , Ceramidas/farmacologia , Animais , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Ceramidas/química , Ceramidas/isolamento & purificação , China , Células Hep G2 , Humanos , Concentração Inibidora 50 , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Oceanos e Mares
10.
J Agric Food Chem ; 72(14): 7919-7932, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38554092

RESUMO

Nine caffeoyl derivatives (1-9), including two new dicaffeoyl glycosides, brevicaudatosides A and B (1 and 2), and six flavonoids (10-15), were identified from overground Clematis brevicaudata DC. Compounds 1 and 13 exhibited significant oral toxicities against Acyrthosiphon pisum Harris with LC50 (half-lethal concentration) values of 0.12 and 0.28 mM, respectively. Meanwhile, compounds 1, 8, 10, 13, and 15 showed remarkable repellent effects against A. pisum with the repellent indexes valued at 1.00 under 50-200 µg/mL at 24 h. Compounds 1 and 8 also displayed moderate antifeedant activities against Plutella xylostella L. The shrunken bodies, especially for wizened cauda, and the ultrastructural damages of microvilli, mitochondrion, nucleus, and endoplasmic reticulum in midgut were toxic symptoms of A. pisum caused by 1 and 13. The inhibition of Chitinase was the main reason for their potent insecticidal activities. This study provided valuable pieces of evidence for the high value-added application of caffeoyl and flavonoid derivatives from C. brevicaudata as novel plant-origin biopesticides for crop protection.


Assuntos
Produtos Biológicos , Clematis , Inseticidas , Mariposas , Animais , Inseticidas/farmacologia , Inseticidas/química , Clematis/química , Flavonoides/farmacologia , Produtos Biológicos/farmacologia , Proteção de Cultivos
11.
ACS Appl Bio Mater ; 7(1): 297-305, 2024 01 15.
Artigo em Inglês | MEDLINE | ID: mdl-38103174

RESUMO

Iron oxide nanoparticles (Fe3O4 NPs) have been reported to be a promising agent for cancer therapy due to their outstanding ability in catalyzing the Fenton reaction and causing peroxidation. Generally, particles with size of hundreds of nanometers exhibit enhanced accumulation in tumor due to the enhanced permeation and retention effect. However, the large size hinders penetration within the dense collagen matrix. Here, we propose a multistage system to realize pH-responsive size switch for efficient drug delivery. In this system, ultrasmall Fe3O4 (∼4 nm) NPs are simultaneously modified with hydrophilic mPEG and hydrophobic N,N-dibutylethylenediamine (DBE) to form pH-responsive self-assembled iron oxide aggregations (SIOA). In the acidic tumor microenvironment, the protonation of DBE makes it transit from the hydrophobic to hydrophilic state, causing the disassembly of the SIOA and the release of loaded doxorubicin. The multistage Fe3O4 NPs demonstrate enhanced accumulation and efficient diffusion within the tumor, holding a promise for drug delivery and cancer therapy.


Assuntos
Doxorrubicina , Compostos Férricos , Neoplasias , Humanos , Doxorrubicina/química , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Sistemas de Liberação de Medicamentos , Microambiente Tumoral
12.
Int J Biol Macromol ; 278(Pt 1): 134624, 2024 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-39134191

RESUMO

The molecular chaperone GroEL, commonly found in various bacterial species, exhibits heightened expression levels in response to high temperatures and increased levels of oxygen free radicals. Limited literature currently exists on the probiotic role of GroEL in invertebrates. This study sought to explore how the surface protein GroEL from Lactobacillus plantarum Ep-M17 impacts the intestinal barrier function of Penaeus vannamei. Through pull-down and immunofluorescence assays, the interaction between GroEL and Act1 in the gastrointestinal tract of P. vannamei was confirmed. Results from bacterial binding assays demonstrated that rGroEL can bind to pathogens like Vibrio parahaemolyticus E1 (V. p-E1). In vitro experiments revealed that the administration of rGroEL significantly decreased the levels of inflammatory cytokines induced by pathogens while preserving the integrity of tight junctions between intestinal epithelial cells and reducing bacteria-induced apoptosis. Additionally, rGroEL notably lessened the intestinal loading of V. p-E1 in P. vannamei, downregulated immune-related gene expression, and upregulated BCL/BAX expression in the intestines following V. p-E1 challenge. Mechanistic investigations further showed that rGroEL treatment effectively suppressed the expression and phosphorylation of proteins involved in the NF-κB and PI3K-AKT-mTOR signalling pathways in the intestines of bacteria-infected P. vannamei. Furthermore, GroEL reinforces protection against bacterial infections by enhancing the phagocytic and anti-apoptotic capabilities of P. vannamei hemocytes. These results suggest that GroEL may impede the interaction between pathogens and the intestinal mucosa through its competitive binding characteristics, ultimately reducing bacterial infections.

13.
J Agric Food Chem ; 72(9): 4596-4609, 2024 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-38385330

RESUMO

To discover new botanical products-based insecticide candidates, 14 triterpenoid saponins (1-14) including four new ones, obscurosides A-D (1-4), were isolated from Clematis obscura Maxim as potential agrochemicals against Acyrthosiphon pisum Harris and Plutella xylostella (L.). Compounds 1-3 were characterized by a rare ribose substitution at C-3, and 4 was a bidesmoside glycosylated at the rare C-23 and C-28 positions of the oleanane aglycone. Compounds 10 (median antifeeding concentration, AFC50 = 1.10 mg/mL; half-lethal concentration, LC50 = 1.21 mg/mL) and 13 (AFC50 = 1.09 mg/mL, LC50 = 1.37 mg/mL) showed significant insecticidal activities against third larvae of P. xylostella at 72 h. All saponins displayed antifeedant activities against A. pisum with the deterrence index of 0.20-1.00 at 400 µg/mL. Compound 8 showed optimal oral toxicity (LC50 = 50.09 µg/mL) against A. pisum, followed by compounds 1, 5-7, 9, and 14 (LC50 = 90.21-179.25 µg/mL) at 72 h. The shrinkage of the cuticle and the destruction of intestinal structures of microvilli, nucleus, endoplasmic reticulum, and mitochondria were toxic symptoms of 8-treated A. pisum. The significantly declined Chitinase activity in 8-treated A. pisum with an inhibition rate of 79.1% at LC70 (70% lethal concentration) could be the main reason for its significant oral toxicities. Molecular docking revealed favorable affinities of compounds 1 and 8 with group I Chitinase OfChtI (Group I Chitinase from Ostrinia furnacalis) through conventional hydrogen bonds and alkey/π-alkey interactions by different patterns. These results will provide valuable information for the development of novel botanical pesticides for the management of insect pests, especially against A. pisum.


Assuntos
Afídeos , Quitinases , Clematis , Inseticidas , Mariposas , Saponinas , Animais , Inseticidas/química , Saponinas/química , Clematis/química , Pisum sativum , Simulação de Acoplamento Molecular , Larva
14.
J Agric Food Chem ; 72(5): 2624-2633, 2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38277222

RESUMO

Pseudomonas syringae pv. actinidiae (Psa) is a significant pathogenic bacterium affecting the kiwifruit industry. This study investigated the target sites of streptothricin-F (ST-F), produced by Streptomyces lavendulae gCLA4. The inhibition of ST-F on Psa was examined by the microscopic structural differences of Psa before and after treatment with ST-F, as well as the interaction between ST-F and cell division-related proteins. The results revealed filamentation of Psa after ST-F treatment, and fluorescence microscopy showed that ST-F inhibited the formation of the Z-ring composed of FtsZ protein. In vitro experiments and molecular docking demonstrated that ST-F can bind to FtsZ with a binding energy of 0.4 µM and inhibit FtsZ's GTP-dependent polymerization reaction. In addition, ST-F does not exert inhibitory effects on cell division in Psa strains overexpressing ftsZ. In conclusion, FtsZ is one of the target sites for ST-F inhibition of Psa, highlighting its potential as a therapeutic target for controlling Psa-induced kiwifruit bacterial canker.


Assuntos
Actinidia , Estreptotricinas , Estreptotricinas/farmacologia , Pseudomonas syringae , Simulação de Acoplamento Molecular , Doenças das Plantas/microbiologia , Actinidia/microbiologia
15.
Neurosignals ; 21(3-4): 272-84, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23796968

RESUMO

The Golgi apparatus (GA), an intermediate organelle of the cell inner membrane system, plays a key role in protein glycosylation and secretion. In recent years, this organelle has been found to act as a vital intracellular Ca(2+) store because different Ca (2+) regulators, such as the inositol-1,4,5-triphosphate receptor, sarco/endoplasmic reticulum Ca(2+) -ATPase and secretory pathway Ca 2+ -ATPase, were demonstrated to localize on their membrane. The mechanisms involved in Ca(2+) release and uptake in the GA have now been established.Here, based on careful backward looking on compartments and patterns in GA Ca (2+) regulation, we review neurological diseases related to GA calcium remodeling and propose a modified cytosolic Ca(2+) adjustment model, in which GA acts as part of the panel point.


Assuntos
Sinalização do Cálcio/fisiologia , Cálcio/metabolismo , Citosol/metabolismo , Complexo de Golgi/fisiologia , Animais , Canais de Cálcio/fisiologia , Proteínas de Ligação ao Cálcio/metabolismo , Transtornos Cerebrovasculares/metabolismo , Humanos , Doenças Neurodegenerativas/metabolismo , ATPases Transportadoras de Cálcio do Retículo Sarcoplasmático/fisiologia , Dermatopatias/metabolismo
16.
Planta Med ; 79(8): 673-9, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23670628

RESUMO

Four new triterpenoid saponins named clematangosides A-D (1-4) along with six known saponins (5-10) were isolated from the whole plants of Clematis tangutica. Their structures were determined by extensive spectral analysis and chemical evidences. All saponins were evaluated for their protective effects in hypoxia-induced myocardial injury model. Compounds 2-4, 6, and 10 exhibited anti-myocardial ischemia activities with ED50 values in the range of 75.77-127.22 µM.


Assuntos
Clematis/química , Isquemia Miocárdica/tratamento farmacológico , Saponinas/uso terapêutico , Triterpenos/uso terapêutico , Configuração de Carboidratos , Espectroscopia de Ressonância Magnética , Saponinas/química , Saponinas/isolamento & purificação , Espectrometria de Massas por Ionização por Electrospray , Triterpenos/química , Triterpenos/isolamento & purificação
17.
Pharmazie ; 68(4): 300-4, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23700798

RESUMO

Extracts of eleven traditional Chinese medicines (TCM) with a reputation of usefulness in treating diabetes mellitus were examined for alpha-glucosidase and alpha-amylase inhibitory activities in vitro. The extract with the highest activity was selected for further characterization. The extract of the root bark of Aralia taibaiensis (EAT) outperformed other extracts in the assays with IC50 values of 0.48 +/- 0.01 mg/mL (BSG), 0.41 +/- 0.02mg/mL (SCG), 0.61 +/- .03mg/mL (BLA) and 0.77 +/- 0.03mg/mL (PPA), respectively. To identify which constituents were responsible for the activities, thirteen triterpenoid saponins were isolated from EAT and examined for their inhibitory effects against alpha-glucosidase and alpha-amylase. The results revealed that saponins 2, 3, 4 (IC50: 0.83 +/- 0.05 microM for BSG and IC50: 0.72 +/- 0.03 microM for SCG), 5, 6, 7, 9, 10, 11 and 12 (IC50: 1.07 +/- 0.04 micro.M for BSG and IC50: 0.93 +/- 0.05 micro.M for SCG) showed alpha-glucosidase inhibitory activities, while 2, 3, 4 (IC50: 0.93 +/- 0.04 micro.M for PPA), 5, 6, 7, 9, 10, 11 and 12 (IC50: 1.02 +/- 0.03 micro.M for PPA) possessed significant alpha-amylase inhibitory activities. In addition, the structure-activity relationship of the thirteen saponins was discussed based on their structure features and diabetes mellitus related activities. It is suggested that the glucuronic acid unit at C-3 of the aglycone is the imperative functional group of the antidiabetic activities, and two characteristic structural features are responsible for the remarkable alpha-glucosidase and alpha-amylase inhibitory activities.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Inibidores Enzimáticos , Inibidores de Glicosídeo Hidrolases , Hipoglicemiantes/farmacologia , Saponinas/farmacologia , alfa-Amilases/antagonistas & inibidores , Aralia/química , Sequência de Carboidratos , Diabetes Mellitus/tratamento farmacológico , Medicamentos de Ervas Chinesas/química , Hipoglicemiantes/química , Medicina Tradicional Chinesa , Dados de Sequência Molecular , Pâncreas/enzimologia , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Saponinas/química , Triterpenos/farmacologia
18.
Zhong Yao Cai ; 36(3): 361-4, 2013 Mar.
Artigo em Zh | MEDLINE | ID: mdl-24010314

RESUMO

OBJECTIVE: To determine the content of huperzine A in the root, stem and leaf of Huperzia serrata from western Hunan, and analyze the relationship between the distribution of huperzine A and the expression of lysine decarboxylase gene in different parts of huperzia serrata. METHODS: The content of huperzine A in the root, stem and leaf of Huperzia serrata was determinated by HPLC, of which the chromatographic column was Diamonsil C18 (250 mm x 4.6 mm,5 microm), mobile phase was methanol-0.08 mol/L CH3COONH4 with flow rate at 1.0 mL/min, column temperature at 25 degrees C and detection wavelength at 308 nm. The expression of lysine decarboxylase gene in different parts of Huperzia serrata was analyzed by semi-quantitative RT-PCR, the beta-actin gene was used as internal reference. RESULTS: Huperzine A had good linear relationships within the range of 0.5 - 10.0 microg/mL, with the recovery rate of 102% and RSD 0.32%. The content of huperzine A in the root,stem and leaf of huperzia serrata was (118.35 +/- 0.77) microg/g and (411.09 +/- 2. 47) microg/g, (562.15 +/- 2.86) microg/g, respectively. Semi-quantitative RT-PCR results showed that lysine decarboxylase gene had nearly identical expression in the root, stem and leaf of Huperzia serrate. CONCLUSION: The content of huperzine A changes with different parts of Huperzia serrata, lysine decarboxylase might be not the key enzyme to regulate the biosynthesis of huperzine A.


Assuntos
Alcaloides/análise , Carboxiliases/metabolismo , Huperzia/química , Sesquiterpenos/análise , Carboxiliases/genética , China , Expressão Gênica , Huperzia/enzimologia , Huperzia/genética , Folhas de Planta/química , Raízes de Plantas/química , Caules de Planta/química , Reação em Cadeia da Polimerase Via Transcriptase Reversa
19.
Pest Manag Sci ; 79(1): 55-67, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36067067

RESUMO

BACKGROUND: Acyrthosiphon pisum Harris is the most destructive pest worldwide because of its ability to feed on plants directly and transmit plant viruses as a vector. This study aims to identify triterpenoid saponins from Oxytropis hirta Bunge as biopesticides to control aphids. RESULTS: Three new azukisapogenol triterpenoid saponins (1-3), a new pinoresinol lignan glycoside (8), and four known saponins (4-7) were identified from the root of O. hirta. Compounds 4-7 displayed significant aphicidal activities against A. pisum with oral toxicities (LC50  = 51.10-147.43 µg/mL, 72 h), deterrent effects (deterrence index = 1.00, 100-200 µg/mL, 24 h), and aphid reproduction inhibitory effects (inhibition rates = 75.91-86.73%, 400 µg/mL, 24 h), respectively. The carboxyl groups at C-3 GlcA and C-30 were functional groups for their aphicidal activities. The toxic symptoms caused by the optimal 5 involved insect body-color changes from light green to dark or gray-green, and then brown until death. The intestinal cavity, apical microvilli, nuclei, mitochondria, and electron dense granules in the midgut tissues of A. pisum were the target sites showing aphicidal activity. The suppression of pepsin and α-amylase, and the activation of lipase and trypsin could be the signs of organelle damage in the midgut tissues. CONCLUSION: Azukisapogenol triterpenoid saponins from O. hirta could be used as biopesticides to control aphids for their multiple efficacies, including oral toxicity, deterrent activity, and reproduction inhibitory activity. The toxic symptoms involved insect body-color changes. Midgut tissues and their related enzymes were the targets for saponins showing aphicidal activities. © 2022 Society of Chemical Industry.


Assuntos
Afídeos , Oxytropis , Saponinas , Animais , Afídeos/efeitos dos fármacos , Oxytropis/química , Triterpenos/química , Saponinas/química , Saponinas/farmacologia , Inseticidas/química , Inseticidas/farmacologia
20.
Aquat Toxicol ; 265: 106763, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37980848

RESUMO

Microcystins (MCs) are biologically active cyclic heptapeptide compounds released by cyanobacteria in water bodies, and MC-LR is one of the most widespread and toxic isoforms. It frequently poses a serious threat to Penaeus vannamei aquaculture. Our previous study revealed that the supplementation of Lactobacillus plantarum Ep-M17 has a probiotic effect on P. vannamei health and whether Ep-M17 can alleviate the stressful effects of MC-LR on shrimp remains unclear. Therefore, in the present work, shrimp were fed MC-LR alone or combined with Ep-M17 for six weeks, and then evaluated the effects on histology, enzyme activity, gene expression, and intestinal flora. The results showed that MC-LR stress lead to slow growth and reduced survival rates in shrimp. However, feeding Ep-M17 significantly increased both the growth rate and survival rate. Meanwhile, MC-LR stress caused severe tissue damage in the hepatopancreas and intestines of shrimp, but Ep-M17 significantly reduced the toxic effects and protected the integrity of these tissues. Additionally, Ep-M17 significantly enhanced the activities of antioxidant enzymes and digestive enzymes, and induced higher expression of immune-related genes, thereby promoting the digestive and immune responses in shrimp. Furthermore, MC-LR stress disrupted the intestinal flora in shrimp intestines, while the use of Ep-M17 significantly increased the abundance of immune- and metabolism-related bacteria and inhibited the growth of pathogenic bacteria to maintain intestinal flora balance and intestinal health. In conclusion, our results indicate that Ep-M17 can reduce the toxic effect of MC-LR on shrimp and has a positive function in the prevention and control of shrimp diseases caused by MC-LR.


Assuntos
Cianobactérias , Microbioma Gastrointestinal , Lactobacillus plantarum , Penaeidae , Poluentes Químicos da Água , Animais , Lactobacillus plantarum/metabolismo , Microcistinas/toxicidade , Microcistinas/metabolismo , Penaeidae/fisiologia , Poluentes Químicos da Água/toxicidade , Cianobactérias/metabolismo
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA