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A unique ring C-expanded angucyclinone, oxemycin A (1), and seven new ring-cleavage derivatives (2-5 and 9-11) were isolated from the marine actinomycete Streptomyces pratensis KCB-132, together with eight known analogues (6-8 and 12-16). Their structures were elucidated by spectroscopic analyses, single-crystal X-ray diffractions, and NMR and ECD calculations. Among these atypical angucyclinones, compound 1 represented the first seven-membered ketoester in the angucyclinone family, which sheds light on the origin of fragmented angucyclinones with C-ring cleavage at C-12/C-12a in the Baeyer-Villiger hypothesis, such as 2-4, while the related "nonoxidized" analogues 5-8 seem to originate from a diverse pathway within the Grob fragmentation hypothesis. Additionally, we have succeeded in the challenging separation of elmenols E and F (12) into their four stereoisomers, which remained stable in aprotic solvents but rapidly racemized under protic conditions. Furthermore, the absolute configurations of LS1924 and its isomers (14 and 15) were assigned by ECD calculations for the first time. Surprisingly, these two bicyclic acetals are susceptible to hydrolysis in solution, resulting in fragmented derivatives 17 and 18 with C-ring cleavage between C-6a and C-7. Compared with ring C-modified angucyclinones, ring A-cleaved 11 was more active to multiple resistant "ESKAPE" pathogens with MIC values ranging from 4.7 to 37.5 µg/mL.
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Actinobacteria , Streptomyces , Antraquinonas , AcetalesRESUMEN
Strepyrazinone (1), a tricyclic diketopiperazine derivative with a carbon skeleton unprecedented in natural products, was isolated from the marine-derived Streptomyces sp. B223. Its structure was elucidated by spectroscopic analyses and electronic circular dichroism calculation. Compound 1 showed cytotoxic activity against HCT-116 cancer cell lines with an IC50 value of 0.34 µM.
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Antineoplásicos , Streptomyces , Antineoplásicos/farmacología , Línea Celular Tumoral , Dicetopiperazinas/farmacología , Células HCT116 , Humanos , Estructura MolecularRESUMEN
(±)-Pratenone A (1), the first representative of natural 3-(1-naphthyl)-2-benzofuran-1(3H)-one polyketides, was isolated from a marine-derived Streptomyces pratensis strain KCB-132 together with three other new analogues (2-4). Its structure was assigned by spectroscopic analysis, and the absolute configurations of the two enantiomers separated by high-performance liquid chromatography were determined by single-crystal X-ray diffraction and electronic circular dichroism calculations. The solvent-induced racemization of 1 and a proposed biogenetic pathway to 1-4 from the co-isolated angucyclinone precursor, as well as their biological activity, are also discussed.
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Policétidos/química , Streptomyces/química , Antraquinonas/química , Antiinfecciosos/química , Antiinfecciosos/farmacología , Organismos Acuáticos , Benzofuranos/química , Cromatografía Líquida de Alta Presión , Dicroismo Circular , Cristalografía por Rayos X , Células HL-60 , Células Hep G2 , Humanos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Policétidos/aislamiento & purificación , Policétidos/farmacología , Policétidos/toxicidad , Staphylococcus aureus/efectos de los fármacos , Estereoisomerismo , Streptomyces/aislamiento & purificaciónRESUMEN
With the development and change of Uygur medicine, The sources,medicinal parts and producing area of some Uygur Medicine have changed. It is more important to master the classification, distribution and change of Uygur medicinal materials. These were more than 1 200 kinds Uygur medicine in history were resaerched by field investigation, philological research, and textual research, which main source of original plant were 140 families, 510 genera, 840 species; and source of original animal were 76 families, 107 genera, the original animal 141 species; 55 kinds of original mineral, which main producer were Xinjiang and Central Asia, West Asia, the Mediterranean, and North Africa, Southeast Asia and other provinces in China, there are individual medicinal materials from the Americas, Europe and other places. Through this study the classification, distribution, source and evolution of specific families and genera of Uygur medicine resources have mastered.It is hoped to provide theoretical basis for further research and development of Uygur medicinal materials.
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Plantas Medicinales , China , Europa (Continente)RESUMEN
OBJECTIVE: To investigate the effects of different processing methods on analgesic effect and toxicity of Strychni Semen, and to provide the scientific basis of milk-impregnated-processing-technology of traditional Uighur medicine for toxic medicines. METHODS: Three different methods, frying with sand of traditional Chinese medicine (1), cooled milk-impregnated-processing-technology of traditional Uighur medicine (2), and heated milk-impregnated-processing-technology of traditional Uighur medicine (3) were used to process raw Strychni Semen and the processed products were compared with those in the raw drug (4). Karber method was used to caculate the LD50. RESULTS: The LD50 of (4), (1), (2) and (3)were 273.0, 289.3, 289.3 and 339.2 mg/kg,successively. Low dose group of heated milk-impregnated-processing-technology, low and high dose groups of cooled milk-impregnated-processing-technology had significant inhibition on the acetic acid-induced writhing reaction in mice (P < 0.05). CONCLUSION: Strychni Semen processed by cooled and heated milk can enhance the analgesic effect in mice while improving the LD50 of mouse, which illustrates milk-impregnated-processing- technology's pharmacological mechanism on efficacy enhancing and toxicity reducing of Strychni Semen.
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Analgésicos/farmacología , Medicamentos Herbarios Chinos/farmacología , Medicina Tradicional China , Leche , Strychnos nux-vomica/química , Animales , Química Farmacéutica/métodos , Calor , Ratones , Semillas/químicaRESUMEN
OBJECTIVE: To study the chemical constituents of Sophora alopecuroides seeds. METHODS: Five compounds were isolated and purified from this plant by various chromatographic methods. Structures were elucidated on the basis of spectral analysis. RESULTS: The structures were identified as 5"-methoxy-6-C-beta-D-glucopyranosyl-6"-C-beta-D-xylopyranosyl cupressuflavone(1),5,6-dihydroxy-3,7, 3',4'-tetramethoxyflavone(2),butein(3),beta-daucosterol(4) and 3'-methoxyluteolin(5). CONCLUSION: Compounds 2,4 and 5 are isolated from Sophora alopecuroides for the first time.
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Chalconas/química , Flavonas/química , Semillas/química , Sophora/química , Chalconas/aislamiento & purificación , Flavonas/aislamiento & purificación , Flavonoides/química , Flavonoides/aislamiento & purificación , Espectroscopía de Resonancia MagnéticaRESUMEN
Agricultural by-products of sesame are promising bioresources in food processing. This study extracted lignin from the by-products of sesame oil production, namely, the capsules and straw of black and white sesame. Using acid, alkali, and ethanol methods, 12 distinct lignins were obtained to prepare biochar, aiming to investigate both the structural characteristics of lignin-based biochar (LBB) and its ability to remove benzo[a]pyrene (BaP) from sesame oil. The results showed that white sesame straw was the most suitable raw material for preparing biochar. In terms of the preparation method, acid-extracted lignin biochar was more effective in removing BaP than alkaline or ethanol methods. Notably, WS-1LB (white sesame straw acid-extracted lignin biochar) exhibited the highest BaP adsorption efficiency (91.44 %) and the maximum specific surface area (1065.8187 m2/g), characterized by porous structures. The pseudo 2nd and Freundlich models were found to be the best fit for the adsorption kinetics and isotherms of BaP on LBB, respectively, suggesting that a multilayer adsorption process was dominant. The high adsorption of LBB mainly resulted from pore filling. This study provides an economical and highly efficient biochar adsorbent for the removal of BaP in oil.
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Carbón Orgánico , Lignina , Aceite de Sésamo , Lignina/química , Carbón Orgánico/química , Adsorción , Aceite de Sésamo/química , Benzo(a)pireno/química , CinéticaRESUMEN
In this study, three activators and two activation methods were employed to activate sesame lignin-based biochar. The biochar samples were comprehensively characterized, their abilities to adsorb benzo[a]pyrene (BaP) from sesame oil were assessed, and the mechanism was analyzed. The results showed that the biochar obtained by one-step activation was more effective in removing BaP from sesame oil than the biochar produced by two-step activation. Among them, the biochar generated by one-step activation with ZnCl2 as the activator had the largest specific surface area (1068.8776 m3/g), and the richest mesoporous structure (0.7891 m3/g); it removed 90.53 % of BaP from sesame oil. BaP was mainly adsorbed by the mesopores of biochar. Mechanistically, pore-filling, π-π conjugations, hydrogen bonding, and n-π interactions were involved. The adsorption was spontaneous and heat-absorbing. In conclusion, the preparation of sesame lignin biochar using one-step activation with ZnCl2 as the activator was found to be the best for removing BaP from sesame oil. This biochar may be an economical adsorbent for the industrial removal of BaP from sesame oil.
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Benzo(a)pireno , Carbón Orgánico , Lignina , Aceite de Sésamo , Sesamum , Carbón Orgánico/química , Lignina/química , Benzo(a)pireno/química , Adsorción , Aceite de Sésamo/química , Sesamum/química , Compuestos de Zinc/química , Cloruros/químicaRESUMEN
OBJECTIVE: Written words demonstrated specific effects on biochemical measures and cell growth in cultured mammalian cells in previous study. We examined the protection and reparative effects of Chinese texts with positive meaning and the word "Buddha" on oxidative-damaged cells, with the goal of exploring the therapeutic effect of such characters. METHODS: The human embryonic kidney cell line HEK293T was utilized, with the oxidative- damaged cell model produced by hydrogen peroxide (H2O2). Double-blind experiments were set up to ensure all operators involved in the experiments did not know the contents of the texts in envelopes. Petri-dishes (9 plates) containing oxidative-damaged cells were selected randomly for three controls, three treatments by texts with positive meaning, and another three treatment by the word "Buddha". Cells were sub-sampled at 3 h and 24 h to examine growth and mitochondrial functions. All data are expressed relative to the controls. RESULTS: Compared with the control group, mitochondrial functions were enhanced as evidenced by increased adenosine triphosphate (ATP) levels, accompanied by the significant improvement in cell growth rate for the groups treated by positive texts and the word "Buddha". Reactive oxygen species (ROS) levels were decreased significantly in positive texts treatment, which suggested that the antioxidant capacity of cells was also improved. CONCLUSIONS: This study revealed that certain texts can potentially offer protection and accelerate the cellular repair for oxidative-damaged cells.
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Peróxido de Hidrógeno , Estrés Oxidativo , Animales , Humanos , Peróxido de Hidrógeno/metabolismo , Peróxido de Hidrógeno/farmacología , Células HEK293 , Especies Reactivas de Oxígeno/metabolismo , Especies Reactivas de Oxígeno/farmacología , Mitocondrias/metabolismo , Mamíferos/metabolismoRESUMEN
Purpose: Degeneration of retinal photoreceptors is frequently observed in diverse ciliopathy disorders, and photoreceptor cilium gates the molecular trafficking between the inner and the outer segment (OS). This study aims to generate a homozygous global Cep250 knockout (KO) mouse and study the resulting phenotype. Methods: We used Cep250 KO mice and untargeted metabolomics to uncover potential mechanisms underlying retinal degeneration. Long-term follow-up studies using optical coherence tomography (OCT) and electroretinography (ERG) were performed. Results: OCT and ERG results demonstrated gradual thinning of the outer nuclear layer (ONL) and progressive attenuation of the scotopic ERG responses in Cep250-/- mice. More TUNEL signal was observed in the ONL of these mice. Immunostaining of selected OS proteins revealed mislocalization of these proteins in the ONL of Cep250-/- mice. Interestingly, untargeted metabolomics analysis revealed arginine-related metabolic pathways were altered and enriched in Cep250-/- mice. Mis-localization of a key protein in the arginine metabolism pathway, arginase 1 (ARG1), in the ONL of KO mice further supports this model. Moreover, adeno-associated virus (AAV)-based retinal knockdown of Arg1 led to similar architectural and functional alterations in wild-type retinas. Conclusions: Altogether, these results suggest that dysregulated arginine metabolism contributes to retinal degeneration in Cep250-/- mice. Our findings provide novel insights that increase understanding of retinal degeneration in ciliopathy disorders.
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Ciliopatías , Degeneración Retiniana , Animales , Ratones , Arginina , Ratones Noqueados , RetinaRESUMEN
Background: Neurodegenerative retinal diseases such as retinitis pigmentosa are serious disorders that may cause irreversible visual impairment. Ferroptosis is a novel type of programmed cell death, and the involvement of ferroptosis in retinal degeneration is still unclear. This study aimed to investigate the related ferroptosis genes in a mice model of retinal degeneration induced by light damage. Methods: A public dataset of GSE10528 deriving from the Gene Expression Omnibus database was analyzed to identify the differentially expressed genes (DEGs). Gene set enrichment analysis between light damage and control group was conducted. The differentially expressed ferroptosis-related genes (DE-FRGs) were subsequently identified by intersecting the DEGs with a ferroptosis genes dataset retrieved from the FerrDb database. The Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) were further performed using the DE-FRGs. A protein-protein interaction (PPI) network was constructed to identify hub ferroptosis-related genes (HFRGs). The microRNAs (miRNAs)-HFRGs, transcription factors (TFs)-HFRGs networks as well as target drugs potentially interacting with HFRGs were analyzed utilizing bioinformatics algorithms. Results: A total of 932 DEGs were identified between the light damage and control group. Among these, 25 genes were associated with ferroptosis. GO and KEGG analyses revealed that these DE-FRGs were mainly enriched in apoptotic signaling pathway, response to oxidative stress and autophagy, ferroptosis, necroptosis and cytosolic DNA-sensing pathway. Through PPI network analysis, six hub ferroptosis-related genes (Jun, Stat3, Hmox1, Atf3, Hspa5 and Ripk1) were ultimately identified. All of them were upregulated in light damage retinas, as verified by the GSE146176 dataset. Bioinformatics analyses predicated that 116 miRNAs, 23 TFs and several potential therapeutic compounds might interact with the identified HFRGs. Conclusion: Our study may provide novel potential biomarkers, therapeutic targets and new insights into the ferroptosis landscape in retinal neurodegenerative diseases.
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Purpose: Abundant retinal microRNA-183 cluster (miR-183C) has been reported to be a key player in photoreceptor development and functionality in mice. However, whether there is a protagonist in this cluster remains unclear. Here, we used a mutant mouse model to study the role of miR-96, a member of miR-183C, in photoreceptor development and functionality. Methods: The mature miR-96 sequence was removed using the CRISPR/Cas9 genome-editing system. Electroretinogram (ERG) and optical coherence tomography (OCT) investigated the changes in structure and function in mouse retinas. Immunostaining determined the localization and morphology of the retinal cells. RNA sequencing was conducted to observe retinal transcription alterations. Results: The miR-96 mutant mice exhibited cone developmental delay, as occurs in miR-183/96 double knockout mice. Immunostaining of cone-specific marker genes revealed cone nucleus mislocalization and exiguous Opn1mw/Opn1sw in the mutant (MT) mouse outer segments at postnatal day 10. Interestingly, this phenomenon could be relieved in the adult stages. Transcriptome analysis revealed activation of microtubule-, actin filament-, and cilia-related pathways, further supporting the findings. Based on ERG and OCT results at different ages, the MT mice displayed developmental delay not only in cones but also in rods. In addition, a group of miR-96 potential direct and indirect target genes was summarized for interpretation and further studies of miR-96-related retinal developmental defects. Conclusions: Depletion of miR-96 delayed but did not arrest photoreceptor development in mice. This miRNA is indispensable for mouse photoreceptor maturation, especially for cones.
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MicroARNs , Células Fotorreceptoras Retinianas Conos , Animales , Electrorretinografía , Ratones , Ratones Noqueados , MicroARNs/metabolismo , Células Fotorreceptoras Retinianas Conos/metabolismo , Células Fotorreceptoras Retinianas Bastones/metabolismoRESUMEN
LncRNA play important roles in regulation of host immune and inflammation responses in defending bacterial infection. Clostridium perfringens (C. perfringens) type C is one of primary bacteria leading to piglet diarrhea and other intestinal inflammatory diseases. For the differences of host immune capacity, individuals usually show resistance and susceptibility to bacterial infection. However, whether and how lncRNAs involved in modulating host immune resistance have not been reported. We have investigated the expression patterns of ileum lncRNAs of 7-day-old piglets infected by C. perfringens type C through RNA sequencing. A total of 16 lncRNAs and 126 mRNAs were significantly differentially expressed in resistance (IR) and susceptibility (IS) groups. Many lncRNAs and mRNAs were identified to regulate resistance and susceptibility of piglets through immune related pathways. Five lncRNAs may have potential function on regulating the expressions of cytokines, these lncRNAs and cytokines work together to co-regulated piglet immune response to C. perfringens, affecting host resistance and susceptibility. These results provide valuable information for understanding the functions of lncRNA and mRNA in affecting piglet diarrhea resistance of defensing to C. perfringens type C, these lncRNAs and mRNAs may be used as the important biomarkers for decreasing C. perfringens spread and diseases in human and piglets.
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Infecciones por Clostridium/veterinaria , Íleon/inmunología , ARN Largo no Codificante/genética , ARN Mensajero/genética , Animales , Infecciones por Clostridium/inmunología , Clostridium perfringens/inmunología , Citocinas/genética , Citocinas/inmunología , Diarrea/microbiología , Diarrea/veterinaria , Perfilación de la Expresión Génica , Regulación de la Expresión Génica/genética , Regulación de la Expresión Génica/inmunología , Íleon/microbiología , Inflamación/genética , Inflamación/inmunología , Análisis de Secuencia de ARN , Porcinos , Enfermedades de los Porcinos/inmunología , Enfermedades de los Porcinos/microbiologíaRESUMEN
The complete mitochondrial genome sequence of the Qinghai Tibetan pig was first determined in this study. The total length of the mitogenome is 16,720 bp. Indicating the an A + T(60.5%)-rich feature, including 2 ribosomal RNA genes, 13 protein-coding genes. 22 transfer RNA genes and 1 non-coding control region. The NJ phylogenetic tree analysis showed that the phylogenetic relationship between Qinghai Tibetan pig and Yimenghei pig was the closest, and the relationship with Chinese northeas wildboar was farthest.
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Viola tianshanica Maxim, belonging to the Violaceae plant family, is traditionally used in Uighur medicine for treating pneumonia, headache, and fever. There is, however, a lack of basic understanding of its pharmacological activities. This study was designed to observe the effects of the ethanol extract (TSM) from Viola tianshanica Maxim on the inflammation response in acute lung injury (ALI) induced by LPS and the possible underlying mechanisms. We found that TSM (200 and 500 mg/kg) significantly decreased inflammatory cytokine production and the number of inflammatory cells, including macrophages and neutrophils, in bronchoalveolar lavage fluid. TSM also markedly inhibited the lung wet-to-dry ratio and alleviated pathological changes in lung tissues. In vitro, after TSM (12.5-100 µg/ml) treatment to RAW 264.7 cells for 1 h, LPS (1 µg/ml) was added and the cells were further incubated for 24 h. TSM dose-dependently inhibited the levels of proinflammatory cytokines, such as NO, PGE2, TNF-α, IL-6, and IL-1ß, and remarkably decreased the protein and mRNA expression of TNF-α and IL-6 in LPS-stimulated RAW 264.7 cells. TSM also suppressed protein expression of p-IκBa and p-ERK1/2 and blocked nuclear translocation of NF-κB p65. The results indicate that TSM exerts anti-inflammatory effects related with inhibition on NF-κB and MAPK (p-ERK1/2) signaling pathways. In conclusion, our data demonstrate that TSM might be a potential agent for the treatment of ALI.