RESUMEN
Ion channels are a type of protein channel that play a vital role in numerous physiological functions by facilitating the passage of ions through cell membranes, thereby enabling ion and electrical signal transmission. As a crucial target for drug action, ion channels have been implicated in various diseases. Many natural products from marine organisms, such as fungi, algae, sponges, and sea cucumber, etc. have been found to have activities related to ion channels for decades. These interesting natural product molecules undoubtedly bring good news for the treatment of neurological and cardiovascular diseases. In this review, 92 marine natural products and their synthetic derivatives with ion channel-related activities that were identified during the period 2000-2024 were systematically reviewed. The synthesis and mechanisms of action of selected compounds were also discussed, aiming to offer insights for the development of drugs targeting ion channels.
Asunto(s)
Organismos Acuáticos , Productos Biológicos , Canales Iónicos , Productos Biológicos/farmacología , Productos Biológicos/química , Productos Biológicos/síntesis química , Canales Iónicos/metabolismo , Canales Iónicos/antagonistas & inhibidores , Canales Iónicos/efectos de los fármacos , Animales , Humanos , Estructura MolecularRESUMEN
Methicillin-resistant Staphylococcus aureus (MRSA) can easily form biofilms on food surfaces, thus leading to cross-contamination, which is difficult to remove. Therefore, there is an urgent need to find alternatives with good antibacterial and antibiofilm effects. In this study, two indole sesquiterpene compounds, xiamycin (1) and chlorinated metabolite chloroxiamycin (2), were isolated from the fermentation liquid of marine Streptomyces sp. NBU3429 for the first time. The chemical structures of the two compounds were characterized by spectroscopic data interpretation, including 1D NMR and HRESIMS analysis. Antimicrobial test showed that chloroxiamycin (2) (minimum inhibitory concentration, MIC = 16 µg/mL) exhibited superior antibacterial activity than xiamycin (1) (MIC = 32 µg/mL) against MRSA ATCC43300. Moreover, compound (2) decreased the biofilm formation rate of MRSA ATCC43300 by 12.7%-84.6% in the concentration range of 32-512 µg/mL, which is relatively stronger than xiamycin (1) (4.1%-49.9%) as well. Antibacterial/antibiofilm mechanism investigation indicated that chloroxiamycin (2) could disrupt the cell wall and membrane of MRSA, inhibiting the production of biofilm extracellular polysaccharides. All these results illustrated that chloroxiamycin (2) is an effective antibacterial/antibiofilm agent, which makes it an attractive candidate for food preservatives.
Asunto(s)
Antibacterianos , Biopelículas , Indoles , Staphylococcus aureus Resistente a Meticilina , Pruebas de Sensibilidad Microbiana , Sesquiterpenos , Streptomyces , Biopelículas/efectos de los fármacos , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Antibacterianos/farmacología , Sesquiterpenos/farmacología , Indoles/farmacología , Streptomyces/químicaRESUMEN
Actinomycetes have long been recognized as important sources of clinical antibiotics. However, the exploration of rare actinomycetes, despite their potential for producing bioactive molecules, has remained relatively limited compared to the extensively studied Streptomyces genus. The extensive investigation of Streptomyces species and their natural products has led to a diminished probability of discovering novel bioactive compounds from this group. Consequently, our research focus has shifted towards less explored actinomycetes, beyond Streptomyces, with particular emphasis on Kitasatospora setae (K. setae). The genome of K. setae was annotated and analyzed through whole-genome sequencing using multiple bio-informatics tools, revealing an 8.6 Mbp genome with a 74.42% G + C content. AntiSMASH analysis identified 40 putative biosynthetic gene clusters (BGCs), approximately half of which were recessive and unknown. Additionally, metabolomic mining utilizing mass spectrometry demonstrated the potential for this rare actinomycete to generate numerous bioactive compounds such as glycosides and macrolides, with bafilomycin being the major compound produced. Collectively, genomics- and metabolomics-based techniques confirmed K. setae's potential as a bioactive secondary metabolite producer that is worthy of further exploration.
RESUMEN
A Gram-negative, rod-shaped, non-motile and strictly aerobic strain, designated NBU2979T, was isolated from a coastal mudflat located on Meishan Island in the East China Sea. Strain NBU2979T grew optimally at 32â°C, with 2.0â% NaCl (w/v) and at pH 7.0-7.5. The predominant fatty acid (>10â%) was iso-C15â:â0. The major polar lipids included phosphatidylglycerol, phosphatidylethanolamine, diphosphatidylglycerol, phosphatidyldimethylethanolamine, phosphatidylcholine, an unidentified glycolipid, two unidentified aminophospholipids, an unidentified phospholipid and an unidentified lipid. The only respiratory quinone was ubiquinone-8. Comparative analysis of 16S rRNA gene sequences showed that strain NBU2979T exhibited highest similarity to Marinicella sediminis F2T (98.0â%), Marinicella marina S1101T (97.5â%), Marinicella litoralis KMM 3900T (96.6â%), Marinicella rhabdoformis 3539T (95.5â%), Marinicella pacifica sw153T (95.2â%) and Marinicella gelatinilytica S6413T (94.9â%). Phylogenetic analyses indicated that strain NBU2979T clustered with the genus Marinicella and was closely related to strain M. sediminis F2T. The average nucleotide identity and digital DNA-DNA hybridization values between strain NBU2979T and related species of genus Marinicella were well below the threshold limit for prokaryotic species delineation. The DNA G+C content of strain NBU2979T was 51.6âmol%. Based on its phenotypic, chemotaxonomic and genotypic data, strain NBU2979T (=KCTC 82911T=MCCC 1K06402T) is considered to be a representative of a novel species in the genus Marinicella, for which the name Marinicella meishanensis sp. nov. is proposed.
Asunto(s)
Técnicas de Tipificación Bacteriana , Composición de Base , ADN Bacteriano , Ácidos Grasos , Sedimentos Geológicos , Hibridación de Ácido Nucleico , Fosfolípidos , Filogenia , ARN Ribosómico 16S , Agua de Mar , Análisis de Secuencia de ADN , Ubiquinona , China , ARN Ribosómico 16S/genética , Ácidos Grasos/química , Sedimentos Geológicos/microbiología , ADN Bacteriano/genética , Agua de Mar/microbiología , Ubiquinona/análogos & derivados , Fosfolípidos/química , Islas , Datos de Secuencia MolecularRESUMEN
Citrus canker, caused by Xanthomonas citri subsp. citri (Xcc), is a severe citrus disease. Currently, copper-containing pesticides are widely used to manage this disease, posing high risks to the environment and human health. This study reports the discovery of naturally occurring anti-Xcc compounds from a deep-sea fungus, Aspergillus terreus SCSIO 41202, and the possible mode of action. The ethyl acetate extract of A. terreus was subjected to bioassay-guided isolation, resulting in the discovery of eight anti-Xcc compounds (1-8) with minimum inhibitory concentrations (MICs) ranging from 0.078 to 0.625 mg/mL. The chemical structures of these eight metabolites were determined by integrative analysis of various spectroscopic data. Among these compounds, Asperporonin A (1) and Asperporonin B (2) were identified as novel compounds with a very unusual structural skeleton. The electronic circular dichroism was used to determine the absolute configurations of 1 and 2 through quantum chemical calculation. A bioconversion pathway involving pinacol rearrangement was proposed to produce the unusual compounds (1-2). Compound 6 exhibited an excellent anti-Xcc effect with a MIC value of 0.078 mg/mL, which was significantly more potent than the positive control CuSO4 (MIC = 0.3125 mg/mL). Compound 6 inhibited cell growth by disrupting biofilm formation, destroying the cell membrane, and inducing the accumulation of reactive oxygen species. In vivo tests indicated that compound 6 is highly effective in controlling citrus canker disease. These results indicate that compounds 1-8, especially 6, have the potential as lead compounds for the development of new, environmentally friendly, and efficient anti-Xcc pesticides.
Asunto(s)
Antibacterianos , Aspergillus , Pruebas de Sensibilidad Microbiana , Enfermedades de las Plantas , Xanthomonas , Xanthomonas/efectos de los fármacos , Aspergillus/efectos de los fármacos , Aspergillus/química , Aspergillus/metabolismo , Enfermedades de las Plantas/microbiología , Antibacterianos/farmacología , Antibacterianos/química , Citrus/química , Citrus/microbiología , Estructura MolecularRESUMEN
Antimicrobial peptides are potent food additive candidates, but most of them are sensitive to proteases, which limits their application. Therefore, we substituted arginine for lysine and introduced a lysine isopeptide bond to peptide IDR-1018 in order to improve its enzymatic stability. Subsequently, the protease stability and antimicrobial/antibiofilm activity of the novel peptides (1018K2-1018KI11) were investigated. The data revealed that the antienzymatic potential of 1018KI11 to bromelain and papain increased by 2-8 folds and 16 folds, respectively. The minimum inhibitory concentration (MIC) of 1018KI11 against methicillin-resistant Staphylococcus aureus (MRSA) ATCC43300 and Escherichia coli (E. coli) ATCC25922 was reduced 2-fold compared to 1018K11. Mechanism exploration suggested that 1018KI11 was more effective than 1018K11 in disrupting the cell barrier and damaging genomic DNA. Additionally, 1018KI11 at certain concentration conditions (2-64 µg/mL) reduced biofilm development of MRSA ATCC43300 by 4.9-85.9%. These data indicated that novel peptide 1018KI11 is a potential food preservative candidate.
Asunto(s)
Antiinfecciosos , Staphylococcus aureus Resistente a Meticilina , Conservantes de Alimentos/farmacología , Lisina/farmacología , Escherichia coli , Pruebas de Sensibilidad Microbiana , Antiinfecciosos/farmacología , Antibacterianos/farmacología , BiopelículasRESUMEN
Chemical investigation of Irpex sp. NBUF088, associated with an Ircinia sp. sponge located at an 84 m deep mesophotic zone, led to the discovery of two new heptaketides, named irpetones A (1) and B (2). Their structures were identified by analysis of spectroscopic data and quantum-chemical calculations. Compound 1 exhibited inhibition against the receptor activator of NF-κB ligand-induced osteoclastogenesis in bone marrow monocytes with an IC50 of 6.3 ± 0.2 µM, causing no notable cytotoxicity. It was also determined that 1 inhibited the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and the nuclear translocation of NF-κB, consequently suppressing the activation of MAPK and NF-κB signaling pathways induced by the NF-κB ligand.
Asunto(s)
Osteoclastos , Poríferos , Animales , Poríferos/microbiología , Estructura Molecular , Osteoclastos/efectos de los fármacos , FN-kappa B/metabolismo , Ratones , Osteogénesis/efectos de los fármacosRESUMEN
A facultative anaerobic, Gram-strain-negative, rod-shaped bacterium (strain NBU2970T) was isolated by using modified ichip in situ cultivation from a marine sediment sample collected from Meishan Island in the East China Sea. Strain NBU2970T grew optimally at 37â°C, with a NaCl concentration of 2.0â% (w/v) and at pH 7.0. The 16S rRNA gene sequence analyses revealed that strain NBU2970T represents a novel species with the genus Muricauda, sharing highest sequence identities with Muricauda beolgyonensis BB-My12T (96.1â%), Muricauda alvinocaridis SCR12T (96.0â%), Muricauda taeanensis 105T (96.0â%) and Muricauda ruestringensis B1T (95.6â%). Phylogenetic analyses also indicated that strain NBU2970T clustered with the genus Muricauda and was closely related to M. beolgyonensis BB-My12T and M. ruestringensis B1T. The draft genome sequence of strain NBU2970T was composed of six contigs with a size of 3.2 Mbp, containing 3045 protein-coding genes and 38 RNA genes. The DNA G+C content was 43.8âmol%. The average nucleotide identity and digital DNA-DNA hybridization values between strain NBU2970T and related species of the genus Muricauda were well below the threshold limit for prokaryotic species delineation. The major cellular fatty acids were iso-C15â:â0, iso-C15â:â1 G and iso-C17â:â0 3-OH. The only respiratory quinone was MK-6. The major polar lipid was phosphatidylethanolamine. Based on its phenotypic, chemotaxonomic and genotypic data, strain NBU2970T is considered to be a representative of a novel species in the genus Muricauda, for which the name Muricauda meishanensis sp. nov. is proposed. The type strain is NBU2970T (=KCTC 82915T=MCCC 1K06394T).
Asunto(s)
Flavobacteriaceae , Agua de Mar , Agua de Mar/microbiología , Filogenia , Composición de Base , Ácidos Grasos/química , ARN Ribosómico 16S/genética , Anaerobiosis , ADN Bacteriano/genética , Análisis de Secuencia de ADN , Técnicas de Tipificación Bacteriana , Sedimentos Geológicos/microbiología , ChinaRESUMEN
Two oxygenated ergostane-type steroids including one new compound, 3ß-hydroxy-5α,6ß-methoxyergosta-7,22-dien-15-one (1) along with a known analogue ergosta-6,22-dien-3ß,5α,8α-triol (2) were isolated from the crude extracts of the marine sponge-derived fungus Aspergillus sp. Their structures were elucidated on the basis of combined NMR and MS spectroscopic methods. Compound 1 was a marine ergostane-type steroid with two methoxy groups at C-5 and C-6, respectively. These oxygenated ergostane-type steroids were evaluated for their antibacterial activities against human or aquatic pathogens. Among them, compound 1 exhibited antibacterial activity against Staphylococcus aureus.
RESUMEN
Two pink-pigmented bacterial strains, designated NBU2971T and NBU2972T, were isolated from the pit mud of a Chinese liquor. Phylogenetic analyses based on 16S rRNA gene sequences suggested that strains NBU2971T and NBU2972T formed a distinct lineage within the family Hymenobacteraceae and were closely related to members of the genus Pontibacter. 16S rRNA gene sequences revealed that strain NBU2971T showed highest similarity of 97.9â% to Pontibacter arcticus 2b14T, and strain NBU2972T showed the highest similarity of 96.9â% to Pontibacter deserti JC215T. The 16S rRNA gene sequence similarity, average nucleotide identity (ANI) and digital DNA-DNA hybridization (dDDH) values between the two novel strains were 95.2, 73.8 and 19.6â%, respectively, suggesting that they represent different species. The ANI and dDDH values between two novel strains and related species of genus Pontibacter were well below the threshold limit for prokaryotic species delineation. The genomic DNA G+C contents of strains NBU2971T and NBU2972T were 51.3 and 44.5âmol%, respectively. The major cellular fatty acids of the two novel strains were iso-C15â:â0 and summed feature 4 (iso-C17â:â1 I and/or anteiso-C17â:â1 B). The major polar lipid of both novel strains was phosphatidylethanolamine. The only respiratory quinone was MK-7. Combining results of phenotypic, chemotaxonomic and genotypic data, strains NBU2971T and NBU2972T are considered to be two representatives in the genus Pontibacter, which the name Pontibacter liquoris sp. nov. and Pontibacter vulgaris sp. nov. are proposed. The type strains of the new species are NBU2971T (=KCTC 82916T=MCCC 1K06395T) and NBU2972T (=KCTC 82917T=MCCC 1K06396T), respectively.
Asunto(s)
Bebidas Alcohólicas , Cytophagaceae , ADN Bacteriano , Microbiología del Suelo , Técnicas de Tipificación Bacteriana , Composición de Base , Cytophagaceae/genética , Cytophagaceae/aislamiento & purificación , ADN Bacteriano/genética , ADN Bacteriano/aislamiento & purificación , Ácidos Grasos/química , Filogenia , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN , Vitamina K 2 , China , Bebidas Alcohólicas/microbiología , Microbiología del AguaRESUMEN
Under the guidance of MS/MS-based molecular networking, eight odoriferous sesquiterpenes including two undescribed geosmin-type sesquiterpenoid degradations, odoripenoid A (1) and odoripenoid B (2), and two undescribed germacrane-type sesquiterpenoids, odoripenoid C (3) and odoripenoid (4), together with four known related compounds (5-8) were isolated from the EtOAc extract of the marine mesophotic zone sponge-associated Streptomyces sp. NBU3428. All chemical structures including absolute configurations of these compounds were elucidated by means of HRESIMS, NMR, ECD calculations and single-crystal X-ray diffraction experiments. Compounds 1 and 2 represent the rarely geosmin-related metabolites directly as natural products from actinomycetes. The isolated compounds (1-8) were assayed in a range of biological activities. Compounds 1 and 2 showed anti-Candida albicans activity with MIC values of 16 and 32 µg/mL, respectively, representing potential antifungal agents.
Asunto(s)
Sesquiterpenos , Streptomyces , Antifúngicos , Streptomyces/química , Streptomyces/metabolismo , Espectrometría de Masas en Tándem , Sesquiterpenos/química , Estructura MolecularRESUMEN
Pan-histone deacetylase (HDAC) inhibitors often have some toxic side effects. In this study, three series of novel polysubstituted N-alkyl acridone analogous were designed and synthesised as HDAC isoform-selective inhibitors. Among them, 11b and 11c exhibited selective inhibition of HDAC1, HDAC3, and HDAC10, with IC50 values ranging from 87 nM to 418 nM. However, these compounds showed no inhibitory effect against HDAC6 and HDAC8. Moreover, 11b and 11c displayed potent antiproliferative activity against leukaemia HL-60 cells and colon cancer HCT-116 cells, with IC50 values ranging from 0.56 µM to 4.21 µM. Molecular docking and energy scoring functions further analysed the differences in the binding modes of 11c with HDAC1/6. In vitro anticancer studies revealed that the hit compounds 11b and 11c effectively induced histone H3 acetylation, S-phase cell cycle arrest, and apoptosis in HL-60 cells in a concentration-dependent manner.
Asunto(s)
Antineoplásicos , Neoplasias , Humanos , Inhibidores de Histona Desacetilasas/farmacología , Inhibidores de Histona Desacetilasas/química , Estructura Molecular , Relación Estructura-Actividad , Línea Celular Tumoral , Simulación del Acoplamiento Molecular , Histona Desacetilasas/metabolismo , Isoformas de Proteínas/metabolismo , Proliferación Celular , Antineoplásicos/farmacología , Antineoplásicos/química , Histona Desacetilasa 1/metabolismo , Histona Desacetilasa 1/farmacología , Proteínas Represoras/metabolismo , Proteínas Represoras/farmacologíaRESUMEN
This article addresses the problem of fast fixed-time tracking control for robotic manipulator systems subject to model uncertainties and disturbances. First, on the basis of a newly constructed fixed-time stable system, a novel faster nonsingular fixed-time sliding mode (FNFTSM) surface is developed to ensure a faster convergence rate, and the settling time of the proposed surface is independent of initial values of system states. Subsequently, an extreme learning machine (ELM) algorithm is utilized to suppress the negative influence of system uncertainties and disturbances. By incorporating fixed-time stable theory and the ELM learning technique, an adaptive fixed-time sliding mode control scheme without knowing any information of system parameters is synthesized, which can circumvent chattering phenomenon and ensure that the tracking errors converge to a small region in fixed time. Finally, the superior of the proposed control strategy is substantiated with comparison simulation results.
RESUMEN
Breast cancer (BC) is a kind of malignant cancer in women, and it has become the most diagnosed cancer worldwide since 2020. Histone methylation is a common biological epigenetic modification mediating varieties of physiological and pathological processes. Lysine-specific demethylase 1 (LSD1), a first identified histone demethylase, mediates the removal of methyl groups from histones H3K4me1/2 and H3K9me1/2 and plays a crucial role in varieties of cancer progression. It is also specifically amplified in breast cancer and contributes to BC tumorigenesis and drug resistance via both demethylase and non-demethylase manners. This review will provide insight into the overview structure of LSD1, summarize its action mechanisms in BC, describe the therapeutic potential of LSD1 inhibitors in BC, and prospect the current opportunities and challenges of targeting LSD1 for BC therapy.
RESUMEN
A modified in situ cultivation technique was developed and applied to resource mining of uncultured microbes from marine sediments of Meishan Island in the East China Sea. Two novel strains NBU2968T and NBU2984T were isolated by this method but not standard Petri dish, which indicated the modified technique was more effective compared to conventional approaches for isolating uncultured microbes and could be popularized and applied to other aquatic environments. The two novel strains were identified by the polyphasic taxonomic approach. Cells of both strains were observed to be Gram-staining-negative, rod-shaped, nonmotile, aerobic, and yellow-pigmented. Catalase and oxidase activities and hydrolysis of Tweens 40, 60, and 80 of two novel strains were positive. Methyl red reaction, H2S production, and hydrolysis of Tween 20 were negative. According to 16S rRNA gene sequence analysis, two novel strains shared the highest similarities (96.4-97.7%) to the species with a validated name in the genus Hanstruepera, while shared lower sequence similarities (<95.6%) to all other genera. Phylogenetic analysis revealed that strains NBU2968T and NBU2984T were affiliated with the genus Hanstruepera. ANI and dDDH values between the two novel strains and Hanstruepera species were 77.4-78.3% and 20.4-20.9%, respectively, which were below the thresholds for species delineation. The 16S rRNA gene sequence similarity, ANI, and dDDH values between the two novel strains were 99.3, 88.9, and 36.3%, respectively, indicating that the two strains represent different species. The genomes of NBU2968T and NBU2984T were 3.28 Mbp with a G+C content of 34.2% and 3.09 Mbp with a G+C content of 34.4%, respectively. The only respiratory quinone was menaquinone-6 (MK-6). The major cellular fatty acids were iso-C15:0, iso-C15:1G, and iso-C17:0 3-OH. The major polar lipids of the two strains were phosphatidylethanolamine, unidentified amino lipids, and unidentified lipids. Based on the above polyphasic characteristics, strains NBU2968T and NBU2984T represent two novel species within the genus Hanstruepera, for which the names Hanstruepera marina sp. nov. and Hanstruepera flava sp. nov. are proposed. The type strains are NBU2968T (= MCCC 1K06392T= KCTC 82913T) and NBU2984T (= MCCC 1K07472T= KCTC 92511T), respectively.
RESUMEN
Biofilm is a complex microbial consortium that are embedded in a membrane structure of the extracellular polymeric substances (EPS). As a major form of microorganisms in nature, biofilm has evolved complex and diverse resistance mechanisms to numerous known antibiotics, posing a major threat to human health. The biofilm formation of pathogens including Pseudomonas aeruginosa, Staphylococcus aureus and Candida albicans, etc. has become the most commonly reasons for clinically chronic and incurable infectious diseases, which urges the development of effective antibiofilm agents. The adaptation of marine organisms and microorganisms to their unique habitats has led to the formation of natural products with charming chemical diversity and biological activity, providing a rich reservoir for the development of antibiofilm agents. According to chemical classification, 129 marine-derived natural products and their synthetic analogs with antibiofilm activity were systematically reviewed, and the related mechanisms and efficacy were discussed as well, aiming to find and develop new and effective antibiofilm agents.
Asunto(s)
Antibacterianos , Productos Biológicos , Antibacterianos/química , Antibacterianos/farmacología , Biopelículas , Productos Biológicos/farmacología , Humanos , Pruebas de Sensibilidad Microbiana , Pseudomonas aeruginosaRESUMEN
Phytopathogenic fungi could affect the growth of agricultural products and result in serious economic losses. To develop novel and potent fungicides, secondary metabolites of an oceanic mesophotic zone Streptomyces sp. NBU3104 was isolated by metabolomics and genomics, which led to the discovery of eight novel antimycins I-P (1-8), including antimycin I (1), six rare acetylated actimycins J-N (2-6), P (8), and an unusual deformylated antimycin O (7). The chemical structures of these metabolites were identified using nuclear magnetic resonance (NMR) spectroscopic analysis, high-resolution electrospray ionization mass spectrometry (HRESIMS) data, and the known reported metabolites in the literature. Their absolute configurations were elucidated by comparison of coupling constant and experimental electronic circular dichroism (ECD) spectra. Among them, compound 1 exhibited excellent inhibitory activities against phytopathogenic fungi, such as Candida albicans, Penicillium expansum, Penicillium citrinum, and Botrytis cinerea. Furthermore, compound 1 could effectively control gray mold of apple in vivo (minimum inhibitory concentration (MIC) = 8 µg/mL). The structure-activity relations of antimycins I-P (1-8) suggested that the aldehyde group in 3-formamidosalicylate unit moiety should be the key factor in their antifungal activities.
Asunto(s)
Actinobacteria , Streptomyces , Antifúngicos/química , Antimicina A/análogos & derivados , Candida albicans , Streptomyces/química , Streptomyces/genéticaRESUMEN
Guignardones Y-Z (1-2), two new meroterpenoids, and six known metabolites involving guignardones A-H (3-4), gyorgy-isoflavone (5), daidzein (6), blumenol A (7) and guignardianone A (8) were isolated from the fungus Penicillium sp. NBUF154, which was obtained from a 60â m deep Crella sponge. Their structures including absolute configurations were unambiguously elucidated by exhaustive spectroscopic analysis and ECD calculations. A putative biosynthetic pathway toward guignardones (1-4) is here proposed. Biological evaluation of compounds 1-8 showed that 1 and 7 exert potent inhibitory effects towards human enterovirus 71 (EV71).
Asunto(s)
Penicillium , Poríferos , Animales , Antivirales/farmacología , Hongos , Humanos , Estructura Molecular , Penicillium/química , Terpenos/químicaRESUMEN
Hahella is one characteristic genus under the Hahellaceae family and shows a good potential for synthesizing new natural products. In this study, we examined the distribution of the secondary metabolite biosynthetic gene cluster (SMBGC) under Hahella with anti-SMASH. The results derived from five genomes released 70 SMBGCs. On average, each strain contains 12 gene clusters, and the most abundant ones (45.7%) are from the family of non-ribosomal peptide synthetase (NRPS) and non-ribosomal peptide synthetase hybrid with polyketide synthase (NRPS/PKS), indicating a great potential to find bioactive compounds. The comparison of SMBGC between H. chejuensis and other species showed that H. chejuensis contained two times more gene clusters than H. ganghwensis. One strain, designed as NBU794, was isolated from the mangrove soil of Dongzhai Port in Haikou (China) by iChip. The 16S rRNA gene of NBU794 exhibited 99% identity to H. chejuensis KCTC 2396 and clustered with the H. chejuensis clade on the phylogenetic trees. Genome mining on strain NBU794 released 17 SMBGCs and two groups of bioactive compounds, which are chejuenolide A-C and nine prodiginines derivatives. The prodiginines derivatives include the well-known lead compound prodigiosin and two new compounds, 2-methyl-3-pentyl-4-O-methyl-prodiginine and 2-methyl-3-octyl-prodiginine, which were identified through fragmentation analysis based on LC-MS/MS. The anti-microbial activity assay showed prodigiosin and 2-methyl-3-heptyl-prodiginine exhibited the best performance in inhibiting Escherichia coli, Salmonella paratyphi B, MASA Staphylococcus aureus, Bacillus subtilis, and Candida albicans. Moreover, the yield of prodigiosin in H. chejuensis NBU794 was also evaluated, which could reach 1.40 g/L under the non-optimized condition and increase to 5.83 g/L in the modified ISP4 medium with macroporous adsorption beads added, indicating that NBU794 is a promising source of prodigiosin.
Asunto(s)
Gammaproteobacteria , Prodigiosina , Cromatografía Liquida , Escherichia coli/metabolismo , Filogenia , Prodigiosina/farmacología , ARN Ribosómico 16S/genética , ARN Ribosómico 16S/metabolismo , Espectrometría de Masas en TándemRESUMEN
A Gram-stain-negative, rod-shaped, motile and aerobic marine bacterium, designated strain NBU2595T, was isolated from marine sediment sampled on Meishan Island, located in the East China Sea. Strain NBU2595T grew at 10-40 °C (optimum, 37 °C), at NaCl concentration of 0-10.0â% (w/v; optimum, 0.5â%) and at pH 6.0-8.0 (optimum, pH 7.0). Catalase and oxidase activities and H2S production were positive. Methyl red reaction and hydrolysis of casein, starch and Tweens 20, 40, 60 and 80 were negative. The major cellular fatty acids were summed feature 8 (C18â:â1 ω7c and/or C18â:â1 ω6c), C18â:â1 2-OH and C18â:â0 3-OH. The sole respiratory quinone was ubiquinone 10. The major polar lipids were phosphatidylglycerol, phosphatidylcholine, phosphatidylethanolamine and phosphatidylmonomethylethanolamine. Comparative analysis of 16S rRNA gene sequences showed highest similarity to Pelagibius litoralis CL-UU02T (97.9%), and low similarities (<92.9â%) to other species. Phylogenetic analyses indicated that strain NBU2595T clustered with the genus Pelagibius and was closely related to P. litoralis CL-UU02T. The average nucleotide identity and digital DNA-DNA hybridization values between strain NBU2595T and the related species of the genus Pelagibius were well below the thresholds for prokaryotic species delineation. The DNA G+C content was 66.5âmol%. Based on its phenotypic, chemotaxonomic and genotypic data, strain NBU2595T should be placed in the genus Pelagibius as representing a novel species, for which the name Pelagibius marinus sp. nov. is proposed. The type strain is NBU2595T (=MCCC 1K04773T=KCTC 82223T).