Author: Jessica.F

Sun, Xiaowen; Zhang, Run; Ding, Meijuan; Liu, Yongxuan; Li, Lin published the artcile< Biocontrol of the root-knot nematode Meloidogyne incognita by a nematicidal bacterium Pseudomonas simiae MB751 with cyclic dipeptide>, SDS of cas: 2873-36-1, the main research area is cyclic dipeptide biocontrol root Pseudomonas Meloidogyne infection; Meloidogyne incognita; Pseudomonas simiae; cyclic dipeptide; nematicidal activity; root-knot nematode.

Root-knot nematodes (RKNs) are harmful plant-parasitic nematodes that cause serious damage to plant hosts. In the long-term practice of RKN management, bacterial nematicides have attracted increasing attention as an effective biocontrol means. Here we determined the active substances against Meloidogyne incognita from a nematicidal bacterium, developed a biocontrol agent (BCA) based on optimized culture processes. The effects of the BCA on RKN control and plant growth-promotion were evaluated in tomato pot trials. Pseudomonas simiae strain MB751 exhibiting significant nematicidal activity against M. incognita second-stage juveniles (J2) with approx. 80% mortality (with culture supernatant, 96% volume percentage) was isolated from a vineyard. A set of purification and identification experiments was performed to determine the main nematicidal component in MB751. A cyclic dipeptide Cyclo(L-Pro-L-Leu) was identified with a lethal concentration necessary to kill 50% of the population (LC50) of 65.3μg mL-1 against M. incognita J2. Following optimization trials on culture medium/fermentation conditions, such as the single factor test, Plackett-Burman test, steepest ascent, and response surface methodol. experiments, the MB751 fermentation broth was then prepared as a BCA via a cold-air drying process. The BCA and was evaluated in tomato pot experiments for effectiveness in suppressing M. incognita. Significant effects on M. incognita suppression and plant-growth promotion as well as induced systemic resistance to M. incognita of tomato, were observed The cyclic dipeptide-producing bacterium P. simiae MB751 exhibited high nematicidal activity and performance. Further development of this BCA should be pursued for the management of M. incognita in agriculture.

Pest Management Science published new progress about Biological pest control. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, SDS of cas: 2873-36-1.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Xiang, Wen-Xin; Liu, Qing; Li, Xiao-Man; Lu, Chun-Hua; Shen, Yue-Mao published the artcile< Four pairs of proline-containing cyclic dipeptides from Nocardiopsis sp. HT88, an endophytic bacterium of Mallotus nudiflorus L>, Application of C11H18N2O2, the main research area is cyclic dipeptide isolation structure activity Nocardiopsis; Mallotus nudiflorus (L.) Kulju & Welzen; Nocardiopsis sp. HT88; dd-diketopiperazines; proline (or hydroxyproline)-containing cyclic dipeptides.

Strain HT88 was isolated from the fresh stems of Mallotus nudiflorus, and it was identified as Nocardiopsis sp. by analyzing its morphol. and the 16S rRNA sequence. The extracts of fermented HT88 showed potent antimicrobial activities. Bioassay guided separation of extracts led to 8 proline (or hydroxyproline, Hyp)-containing cyclic dipeptides. Their structures were determined by 1D and 2D NMR spectroscopy and ESI mass spectrometry and further comparison with existing 1H and 13C NMR, m.ps. and sp. rotation data. The 8 2,5-diketopiperazines (DKPs) were identified as cyclo(L-Pro-L-Leu), cyclo(Pro-Leu), cyclo(L-trans-Hyp-L-Leu), cyclo(D-trans-Hyp-D-Leu), and cyclo(D-Pro-L-Phe), cyclo(L-Pro-L-Phe) and cyclo(D-cis-Hyp-L-Phe), cyclo(L-trans-Hyp-L-Phe). Up to date, this is the 1st isolation of 4 pairs of proline-based DKPs from Nocardiopsis sp.

Natural Product Research published new progress about Antibacterial agents. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Application of C11H18N2O2.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Georgousaki, Katerina; Tsafantakis, Nikolaos; Gumeni, Sentiljana; Gonzalez, Ignacio; MacKenzie, Thomas Andrew; Reyes, Fernando; Lambert, Carole; Trougakos, Ioannis P.; Genilloud, Olga; Fokialakis, Nikolas published the artcile< Screening for tyrosinase inhibitors from actinomycetes; identification of trichostatin derivatives from Streptomyces sp. CA-129531 and scale up production in bioreactor>, Formula: C11H18N2O2, the main research area is Streptomyces trichostatin derivative tyrosinase inhibitors fermentation; Bioreactor; Enzyme kinetics studies; Secondary metabolites, Streptomyces sp.; Trichostatin derivatives; Tyrosinase inhibitors.

In the course of a primary screening of 614 microbial actinomycete extracts for the discovery of tyrosinase inhibitors, the EtOAc extract of the fermentation broth of the strain Streptomyces sp. CA-129531 isolated from a Martinique sample, exhibited in cell free and cell-based assays the most promising activity (IC50 value of 63 μg/mL). Scaled-up production in a bioreactor led to the isolation of one new trichostatic acid analog, namely trichostatic acid B (1), along with six known trichostatin derivatives (2-7), four diketopiperazines (8-11), two butyrolactones (12-13) and one hydroxamic acid siderophore (14). Among them, trichostatin A (4) showed a Ki value of 6.1 μM and six times stronger anti-tyrosinase activity (IC50 2.18 μΜ) than kojic acid (IC50 14.07 μΜ) used as a pos. control. Deoxytrichostatin A (6) displayed also strong inhibitory activity against tyrosinase (IC50 19.18 μΜ). Trichostatin A production in bioreactor started together with the exponential phase of growth (day 4) and the maximum concentration was reached at day 9 (2.67 ± 0.13 μg/mL). Despite the cytotoxicity of some individual components, the EtOAc extract showed no cytotoxic effect on HepG2, A2058, A549, MCF-7 and MIA PaCa-2 cell lines, (IC50 >2.84 mg/mL) and against BG fibroblasts at the concentrations where the whitening effect was exerted, reassuring its safety and great tyrosinase inhibitory potential.

Bioorganic & Medicinal Chemistry Letters published new progress about Fermentation. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Formula: C11H18N2O2.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Gonzalez-Dominguez, Raul; Urpi-Sarda, Mireia; Jauregui, Olga; Needs, Paul W.; Kroon, Paul A.; Andres-Lacueva, Cristina published the artcile< Quantitative Dietary Fingerprinting (QDF)-A Novel Tool for Comprehensive Dietary Assessment Based on Urinary Nutrimetabolomics>, Recommanded Product: (3S,8aS)-3-Isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione, the main research area is quant dietary fingerprinting urine nutrimetabolomics; dietary assessment; quantitative dietary fingerprinting (QDF); targeted metabolomics; ultra-high-performance liquid chromatography−tandem mass spectrometry; urine.

Accurate dietary assessment is a challenge in nutritional research, needing powerful and robust tools for reliable measurement of food intake biomarkers. In this work, we have developed a novel quant. dietary fingerprinting (QDF) approach, which enables for the first time the simultaneous quantitation of about 350 urinary food-derived metabolites, including (poly)phenolic aglycons, phase II metabolites, and microbial-transformed compounds, as well as other compounds (e.g., glucosinolates, amino acid derivatives, methylxanthines, alkaloids, and markers of alc. and tobacco consumption). This method was fully validated for 220 metabolites, yielding good linearity, high sensitivity and precision, accurate recovery rates, and negligible matrix effects. Furthermore, 127 addnl. phase II metabolites were also included in this method after identification in urines collected from acute dietary interventions with various foods. Thus, this metabolomic approach represents one-step further toward precision nutrition and the objective of improving the accurateness and comprehensiveness in the assessment of dietary patterns and lifestyles.

Journal of Agricultural and Food Chemistry published new progress about Apple. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Recommanded Product: (3S,8aS)-3-Isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Kgk, Deepak; Kumari, Seema; G, Shailender; Malla, Rama Rao published the artcile< Marine natural compound cyclo(L-leucyl-L-prolyl) peptide inhibits migration of triple negative breast cancer cells by disrupting interaction of CD151 and EGFR signaling>, Name: (3S,8aS)-3-Isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione, the main research area is cycloleucyl prolyl peptide EGFR signaling breast cancer antitumor agent; Antiproliferative; Apoptosis; Cell cycle; Cytotoxicity; Migration and TNBC.

Cyclo (L-Leucyl-L-Prolyl) peptide/CLP is a marine natural metabolite and well recognized as an antimicrobial and antioxidant agent with limited studies on anticancer activity. The current study aims to determine the effect of CLP on migration and growth of triple neg. breast cancer cell lines. The anti-growth potential was evaluated by MTT, BrdU and TUNEL assays; DNA damage by γH2AX and Dead green assays; antimigration activity by Boyden chamber invasion and wound healing assays. Interaction of CLP with CD151 was resolved by PatchDock. Effect of CLP on the expression of transmembrane CD151 was evaluated by cell-based ELISA assay. The interaction between CD151 and EGFR was predicted by using FireDoc Web server. Impact of CLP on the interaction of CD151 with EGFR was evaluated by co-immunoprecipitation assay. The effect of CLP on the cell cycle and its controlling proteins was determined by Western blotting. CLP reduced the viability of MDA-MB-231 and MDA-MB-468 TNBC cell lines but not human breast healthy epithelial cell line (MCF-12A) similar to eribulin, standard CLP also inhibited proliferation; cell cycle and migration. It induced DNA strand breaks, DNA damage, and cell death. It showed the most favorable interactions with CD151 in in silico docking and significantly reduced the expression of membrane-bound CD151 proteins. FireDoc Web study predicted the association between CD151 and EGFR with -29.13 kcal/mol of binding energy. CLP reduced the interaction of CD151 with EGFR along with the expression of cyclin D, CDK4, PAK, RAC1, and P27kiP1. This study concludes that CLP suppresses growth and migration by attenuating cell cycle of TNBC cell lines via EGFR and CD151 signaling. Thus, exploring the EGFR and CD151 signaling pathway targeted by CLP may provide a new approach in the treatment of TNBC.

Chemico-Biological Interactions published new progress about Antitumor agents. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Name: (3S,8aS)-3-Isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Blair, Victoria L.; Blakemore, David C.; Hay, Duncan; Hevia, Eva; Pryde, David C. published the artcile< Alkali-metal mediated zincation of N-heterocyclic substrates using the lithium zincate complex, (THF)Li(TMP)Zn(tBu)2 and applications in in situ cross coupling reactions>, Computed Properties of 136866-30-3, the main research area is zincation nitrogen heterocycle reactant quench iodine reagent iodoheterocycle preparation; heteroarylzincate preparation palladium catalyzed Negishi cross coupling arylheterocycle preparation.

This study investigates the ability of the mixed-metal reagent [Li(TMP)Zn(tBu)2] (I) to promote direct Zn-H exchange reactions (zincations) of a wide range of N-heterocyclic mols. The generated metalated intermediates from these reactions are intercepted with I2 to yield iodoheterocycles, e.g. 3-iodo-2-methoxypyridine, and some of them are also employed as precursors in Pd-catalyzed Negishi cross-coupling applications yielding arylated N-heterocycles, e.g. 4-(4-chlorophenyl)-2-methoxypyridine. A comparison with recent precedents in metalation chem. reveals that for some of these heterocycles, I allows improved conversions, under milder conditions and in certain cases, even gives unique regioselectivities.

Tetrahedron Letters published new progress about Group 12 element compounds, zincates Role: FMU (Formation, Unclassified), RCT (Reactant), FORM (Formation, Nonpreparative), RACT (Reactant or Reagent). 136866-30-3 belongs to class pyrazines, and the molecular formula is C4HCl2IN2, Computed Properties of 136866-30-3.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Huang, Ying; Zhang, Jeff; Yu, Zhengtian; Zhang, Hailong; Wang, Youzhen; Lingel, Andreas; Qi, Wei; Gu, Justin; Zhao, Kehao; Shultz, Michael D.; Wang, Long; Fu, Xingnian; Sun, Yongfeng; Zhang, Qiong; Jiang, Xiangqing; Zhang, Jiangwei; Zhang, Chunye; Li, Ling; Zeng, Jue; Feng, Lijian; Zhang, Chao; Liu, Yueqin; Zhang, Man; Zhang, Lijun; Zhao, Mengxi; Gao, Zhenting; Liu, Xianghui; Fang, Douglas; Guo, Haibing; Mi, Yuan; Gabriel, Tobias; Dillon, Michael P.; Atadja, Peter; Oyang, Counde published the artcile< Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy>, Application In Synthesis of 136866-30-3, the main research area is EED226 preparation polycomb repressive complex PRC2 EED inhibitor bioavailability.

Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit Polycomb repressive complex 2 (PRC2), are associated with several tumor types. EZH2 inhibitor, EPZ-6438 (Tazemetostat), demonstrated clin. efficacy in patients with acceptable safety profile as monotherapy. EED, another subunit of PRC2 complex, is essential for its histone methyltransferase activity through direct binding to trimethylated lysine 27 on histone 3 (H3K27Me3). Herein the authors disclose the discovery of a first-in-class potent, selective and orally bioavailable EED inhibitor EED226 (compound 43). Guided by x-ray crystallog., compound 43 discovered by fragmentation and regrowth of Compound (I), a PRC2 HTS hit that directly binds EED. Scaffold hopping followed by ensuing multi-parameter optimization led to the discovery compound 43. Compound 43 induces robust and sustained tumor regression in EZH2MUT pre-clin. DLBCL model. For the first time specific and direct inhibition of EED can be effective as an anti-cancer strategy.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 136866-30-3 belongs to class pyrazines, and the molecular formula is C4HCl2IN2, Application In Synthesis of 136866-30-3.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Yeoh, Chiann Ying; Rosandy, Andi Rifki; Khalid, Rozida Mohd; Cheah, Yoke Kqueen published the artcile< Barrientosiimonas humi ethyl acetate extract exerts cytotoxicity against MCF-7 and MDA-MB-231 cells via induction of apoptosis and cell cycle arrest>, Formula: C11H18N2O2, the main research area is Barrientosiimonas ethyl acetate extract anticancer apoptosis cell cycle arrest.

To elucidate the cytotoxic effect of the secondary metabolites of Barrientosiimonas humi (B. humi) on MCF-7 and MDA-MB-231 human breast cancer cells and its underlying mechanisms of action. The extract was obtained from the fermentation of B. humi and fractionation of the crude extract was conducted via column chromatog. Cytotoxicity of the B. humi extract was determined by using MTT assay and real-time cellular anal. Morphol. changes, cell cycle profiles, mode of cell death, and caspase expressions of control and treated breast cancer cells were determined The Et acetate extract isolated from B. humi was cytotoxic against MCF-7 and MDA-MB-231 cell lines. One of the dichloromethane (DCM) fractions, designated as DCM-F2, exhibited the strongest activity among all the fractions and thereby was selected for further studies. DCM-F2 had selective cytotoxicity on target cells by inducing apoptosis, particularly in the early stage, and cell cycle arrest. Treated cells caused inhibition of cell cycle progression at 72 h leading to a significant increase (P < 0.05) in the G0/G1 population. DCM-F2 treated MDA-MB-231 cells showed caspase-dependent apoptosis, whereas DCM-F2 treated MCF-7 cells showed a caspase-independent apoptosis pathway. Five compounds were successfully isolated from B. humi. Cyclo (Pro-Tyr) was the most cytotoxic and selective compound against MCF-7 cells. B. humi Et acetate extract exhibits significant cytotoxicity against MCF-7 and MDA-MB-231 cells via induction of apoptosis and cell cycle arrest. Asian Pacific Journal of Tropical Biomedicine published new progress about Antitumor agents. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Formula: C11H18N2O2.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Zhao, Lijun; Duan, Feixia; Gong, Meng; Tian, Xue; Guo, Yan; Jia, Lirong; Deng, Sha published the artcile< (+)-Terpinen-4-ol Inhibits Bacillus cereus Biofilm Formation by Upregulating the Interspecies Quorum Sensing Signals Diketopiperazines and Diffusing Signaling Factors>, Related Products of 2873-36-1, the main research area is Bacillus biofilm formation terpinenol quorum sensing diketopiperazine; Bacillus cereus; EPS synthesis; biofilm inhibition; diffusing signaling factor; diketopiperazine; monocyclic monoterpenoids; quorum sensing; rpfB.

Bacillus cereus is a Gram-pos. endospore-forming foodborne pathogen that causes lethal food poisoning and significant economic losses, usually through biofilm- and endospore-induced recurrent cross- and postprocessing contamination. Due to the lack of critical inhibitory targets and control strategies, B. cereus biofilm contamination is a problem that urgently needs a solution In this study, the antibacterial and antibiofilm activities of several natural potential bacterial quorum sensing (QS) interferers, a group of spice-originated monoterpenoids, were screened, and terpinen-4-ol effectively inhibited B. cereus growth and biofilm and spore germination with min. growth inhibition and 50% biofilm inhibitory concentrations of 8 and 2μmol/mL, resp. FESEM/CLSM and phenotypic research illustrated that in addition to a decrease in the number of attached B. cereus cells, (+)-terpinen-4-ol also obviously reduced extracellular matrix synthesis, especially exopolysaccharides, and inhibited the swarming motility and protease activity of B. cereus. (+)-Terpinen-4-ol did not exert a significant effect on AI-2 signals in B. cereus. Accordingly, the B. cereus-produced interspecies QS signals diffusing signal factors (DSFs, C8-C15) and diketopiperazines (DKPs) were detected and identified here, which suppressed B. cereus biofilm formation in a concentration-dependent manner. (+)-Terpinen-4-ol significantly increased the levels of specific DSF and DKP signals in B. cereus and down-regulated the gene expression of some rpfB homologues in transcription level. Moreover, both DKPs and DSFs inhibited swarming motility and protease activity in B. cereus, while just the DSF signals 2-dodecenoic acid and 11-methyl-2-dodecenoic acid inhibited exopolysaccharide synthesis like (+)-terpinen-4-ol. In summary, B. cereus strains were found to produce nine DSF- and six DKP-type QS signaling mols., which repressed B. cereus biofilm formation. (+)-Terpinen-4-ol was confirmed to be a promising antibacterial and antibiofilm agent against B. cereus upregulating DSFs and DKPs levels, and it could target the critical genes rpfB for DSFs turnover.

Journal of Agricultural and Food Chemistry published new progress about Antibacterial agents. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Related Products of 2873-36-1.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ma, Haoran; Wang, Fuqian; Jin, Xiaoqi; Jiang, Jie; Hu, Song; Cheng, Lu; Zhang, Geng published the artcile< A new diketopiperazine from an endophytic fungus Aspergillus aculeatus F027>, Computed Properties of 2873-36-1, the main research area is diketopiperazine isolation structure Aspergillus; Aspergillus aculeatus ; diketopiperazine; endophytic fungus.

A new diketopiperazine cyclo-(L-Phe-N-ethyl-L-Glu), along with 2 known diketopiperazines cyclo-(L-Pro-L-Leu) and cyclo-(L-Pro-L-Phe) were isolated from the cultures of an endophytic fungus Aspergillus aculeatus F027. The structures of these compounds were elucidated based on spectroscopic data. The configurations of these compounds were determined by advanced Marfey’s anal. Antibacterial activity of the diketopiperazines against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa were also evaluated.

Natural Product Research published new progress about Aspergillus aculeatus. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Computed Properties of 2873-36-1.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem