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Analysis of an antimicrobial extract prepared from culture broth of the marine-derived actinomycete Streptomyces sp. G278 led to the isolation of ten compounds, 1-10. Two compounds, 2,5-Bis(5-tert-butyl-2-benzoxazolyl)thiophene (1), and 3-hydroxyl-2-methylpyridine (2) were isolated from a natural source for the first time. The structures of the isolated compounds were established by their spectral data analysis, including mass spectrometry, 1D-NMR, 2D-NMR, and X-ray crystallographic analysis in case of compound 3. All isolated compounds were evaluated for their antimicrobial activity against a panel of clinically significant microorganisms. Compounds 1 and 3 selectively inhibited Enterococcus faecalis (MIC: 256 mug/mL). Compound 2 was found to have antibacterial and antifungal activity against Escherichia coli (MIC: 64 mug/mL), Salmonella enterica (MIC: 256 mug/mL), Staphylococcus aureus (MIC: 256 mug/mL), Enterococcus faecalis (MIC: 256 mug/mL), and Candida albicans (MIC: 64 mug/mL). Except for compounds 9 and 10, the other known metabolites (4-8) also exhibited antimicrobial activity.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Copper-catalyzed oxoazidation and alkoxyazidation of indoles has been developed. The dearomatization reaction which leads to versatile 3-azido indolenine and oxindole derivatives in moderate to good yields could be used in a further transformation.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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To investigate whether melatonin has a direct action on the cardiovascular system, putative melatonin receptors were studied in quail heart membrane preparations using the specific melatonin agonist 2-[125I]iodomelatonin ([125I]Mel) as the radioligand. The [125I]Mel binding demonstrated in the mature quail heart was saturable, highly specific and reversible, of picomolar affinity and femtomolar density (Kd = 35.2 ± 5.2 pM; Bmax = 1.32 ±: 0.25 fmol/mg protein; n = 8). The linear Scatchard plots and the close to unity Hill coefficient indicated a single class of binding sites. The pharmacological profile was in the affinity order of 2-iodomelatonin = 2-phenylmelatonin > melatonin > 6-chloromelatonin >> 6-hydroxymelatonin > 6-sulphatoxymelatonin >> N-acetylserotonin >>> 5-hydroxytryptamine. Guanosine 5′-triphosphate and guanosine 5′-O-(3-thiotriphosphate) (GTPgammaS) dose dependently inhibited the binding. Ten muM GTPgammaS lowered the binding affinity by 50% in saturation studies. The order of potency of inhibition by cations was: Ca2+ > Mg2+ > Li+ > Na+ > K+ > choline chloride. Contrary to most other melatonin binding sites, millimolar concentrations of Ca2+ and Mg2+ did not promote binding in the quail heart membranes. In vitro autoradiography indicated homogeneous labeling in the heart. Our results demonstrated [125I]Mel binding sites in the quail heart. That guanine nucleotides and Na+ inhibited the binding indicated that these putative melatonin receptors are coupled to guanine nucleotide-binding proteins (G-proteins).

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Stichworte: alpha-Amylase-Assay * Chemoenzymatische Synthesen * Enzyme * Fluoreszenz * Oligosaccharide

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Hepatocellular carcinoma (HCC) accounts for most cases of liver cancer worldwide; contraction of hepatitis C (HCV) is considered a major risk factor for liver cancer even when individuals have not developed formal cirrhosis. Global, untargeted metabolic profiling methods were applied to serum samples from patients with either HCV alone or HCC (with underlying HCV). The main objective of the study was to identify metabolite based biomarkers associated with cancer risk, with the long term goal of ultimately improving early detection and prognosis. Serum global metabolite profiles from patients with HCC (n= 37) and HCV (n= 21) were obtained using high performance liquid chromatography-mass spectrometry (HPLC-MS) methods. The selection of statistically significant metabolites for partial least-squares discriminant analysis (PLS-DA) model creation based on biological and statistical significance was contrasted to that of a traditional approach utilizing p-values alone. A PLS-DA model created using the former approach resulted in a model with 92% sensitivity, 95% specificity, and an AUROC of 0.93. A series of PLS-DA models iteratively utilizing three to seven metabolites that were altered significantly (p<. 0.05) and sufficiently (FC. ?. 0.7 or FC. ?. 1.3) showed good performance using p-values alone ; the best of these PLS-DA models was capable of generating 73% sensitivity, 95% specificity, and an AUROC of 0.92. Metabolic profiles derived from LC-MS readily distinguish patients with HCC and HCV from those with HCV only. Differences in the metabolic profiles between high-risk individuals and HCC indicate the possibility of identifying the early development of liver cancer in at risk patients. The use of biological significance as a selection process prior to PLS-DA modeling may offer improved probabilities for translation of newly discovered biomarkers to clinical application. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 526-55-6, help many people in the next few years.Quality Control of: 3-Indoleethanol

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Quorum sensing is the response-regulation system of genes expression in accordance with the variation of cell population density. In this communication system, the response-regulation system induces group behaviors via signal molecules, which enabling cell acts actively to external environmental fluctuation. From practical point of view, these group behaviors ubiquitously occurred in a myriad of environments threatening human health and causing unrecoverable deterioration of manufacturing processes. Therefore, the mechanism of quorum sensing involves producing, releasing, detecting, and responding to small hormone-like chemical compounds called as autoinducers. For intraspecies communications, Gram-negative bacteria representatively utilize acyl-homoserine lactones, and Gram-positive bacteria typically use modified peptides as autoinducer. In case of a eukaryote, fungi generate a variety of autoinducers, such as farnesol, tyrosol, and aromatic alcohols. The intraspecies quorum sensing allows bacteria themselves to recognize the same species in the mixed culture system, but it could not use to detect the presence of other species and identify and act on their proportions in the overall environmental system. Thus, bacteria produce furanone-based signal molecules to build an interspecies communication and maintain a balance in the entire ecosystem. This type of bacterial Esperanto, called autoinducer-2, is synthesized by LuxS protein and its associated genes have been found in over 70 different microorganisms to date. Meanwhile, recent studies also identified that interkingdom quorum sensing between eukaryote and prokaryote, such as a bacteria-to-fungi, bacteria-to-plant, and bacteria-to-mammalian cell. This chapter focuses on the history of quorum sensing and the signal molecules chemistry; how response-regulation system in bacteria is developed; how the definition of quorum sensing is determined; how the signal molecule is generated; and the recent studies related to the exploration of new quorum sensing systems.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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The invention belongs to organic chemical and technical field of pharmaceutical chemistry, and in particular relates to a process for preparing 3 – substituted oxidation indole and its derivative. The invention relates to 3 – substituted indole derivatives as raw materials, to four-butyl halide/sodium chloride/sodium iodide knob/potassium iodide in one or several kinds of additive, then adding dichloromethane/1, 2 – dichloroethane/tetrahydrofuran/toluene/1, 4 – dioxane/ethyl acetate/methanol of one or several as solvent; control the reaction temperature, then adding [double-(trifluoroacetic acyloxy) iodo] benzene/acetate in the oxygenated esters of one or several kinds as the oxidizing agent, produced by the reaction of 3 – substituted oxidation of indole derivatives. The invention mild reaction conditions, the operation is simple, short reaction time, high yield; and has not used the metal catalyst, environment-friendly. (by machine translation)

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Paenibacillus polymyxa is a common bacterium, belonging to Plant Growth Promoting Rhizobacteria (PGPR). It is found in soils, roots and rhizosphere of various crop plants especially wheat. This bacterium has a great biotechnological potential in sustainable agriculture. Indeed, in the rhizosphere, P. polymyxa is involved in nitrogen fixation, production of phytohormones, exoplysaccharides, hydrolytic enzymes and antibiotics, in the enhancement of soil porosity and in soil phosphorus solubilization. In this study, we have identified GOL 0202 strain as Paenibacillus polymyxa, isolated from durum wheat (Triticum durum Desf.) rhizosphere collected from arid region soil of Southern. This genomic identification was performed by 16S rRNA gene sequencing. It was shown that this strain possesses an interesting phosphate solubilization activity on NBRIP (National Botanical Research Institute Phosphorus) medium containing tricalcium phosphate (Ca3 (PO4)2). This activity, was recorded over five days, it was negatively correlated with pH medium whose decline was due probably to the release of organic acids. In addition to other activities associated with P. polymyxa, this availability of soluble phosphate has allowed the improvement of durum wheat seedlings growth estimated through dry weight, chlorophylls and proteins contents. Hence, P. polymyxa GOL 0202 could be used for their targeted application as bioinoculant.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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A ruthenium complex of Xantphos has been shown to be a good catalyst for the alkylation of active methylene compounds with a range of alcohols.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Quorum sensing is a well-described mechanism of intercellular signalling among bacteria, which involves cell-density-dependent chemical signal molecules. The concentration of these quorum-sensing molecules increases in proportion to cell density until a threshold value is exceeded, which triggers a community-wide response. In this review, we propose that intercellular signalling mechanisms can be associated with a corresponding ecological interaction type based on similarities between how the interaction affects the signal receiver and producer. Thus, we do not confine quorum sensing, a specific form of intercellular signalling, to only cooperative behaviours. Instead, we define it as cell-density-dependent responses that occur at a critical concentration of signal molecules and through a specific signalling pathway. For fungal species, the medically important yeast Candida albicans has a well-described quorum sensing system, while this system is not well described in Saccharomyces cerevisiae, which is involved in food and beverage fermentations. The more precise definition for quorum sensing proposed in this review is based on the studies suggesting that S. cerevisiae may undergo intercellular signalling through quorum sensing. Through this lens, we conclude that there is a lack of evidence to support a specific signalling mechanism and a critical signal concentration of these behaviours in S. cerevisiae, and, thus, these features require further investigation.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles