Month: October 2022

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

Jiang, Qingjian; Wei, Nan; Huo, Yishen; Kang, Xi; Chen, Gang; Wen, Lu published the artcile< Secondary Metabolites of the Endophytic Fungus Cladosporium sp. CYC38>, Reference of 2873-36-1, the main research area is cerevisterol beta sitosterol Cyclosorus Cladosporium Salmonella.

This study of Cyclosorus parasiticus plant affected by Cladoporium fungi organism. Fungi secondary metabolites of cerevisterol, cyclo-gly-phe. these compounds are act as a antibacterial activity. Cyclo-pro–N-MePhe-Val-Ala-Leu is against microorganism like Salmonella sp, Escherichia coli, staphylococcus.

Chemistry of Natural Compounds published new progress about Cladosporium. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Reference of 2873-36-1.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Meng, Lili; Sun, Changli; Zhang, Chunyan; Song, Shihao; Sun, Xiuyun; Ju, Jianhua; Deng, Yinyue published the artcile< Efficacy of compounds isolated from Streptomyces olivaceus against the morphogenesis and virulence of Candida albicans>, Computed Properties of 2873-36-1, the main research area is Streptomyces Candida morphogenesis virulence; Candida albicans; Streptomyces olivaceus; hypha formation; virulence.

Candida albicans is a type of commensal fungi which causes serious infections in immunocompromised patients and contributes to high mortality. In the present study, we identified that the extract from Streptomyces olivaceus SCSIO T05 inhibited hypha and biofilm formation of C. albicans. Seven compounds were isolated and evaluated for their effects on the biol. functions and virulence of C. albicans. Two leading compounds, compound 1 (sorbicillin) and compound 2 (3-methyl-N-(2′-phenethyl)-butyrylamide) were identified as exhibiting strong activity against C. albicans morphol. transition, adhesion activity, cytotoxicity, and adhesion to human cells, in a dose-dependent manner. Notably, compound 2 inhibited C. albicans infection in mouse oral mucosal models. Transcriptomic anal. and real-time PCR results revealed that compound 2 most likely inhibited the biol. functions of C. albicans cells by regulating the expression levels of HWP1, TEC1, ALS1, IFD6, and CSH1, which are associated with filament formation and cell adhesion. Our results suggest that the candidate compounds present excellent efficacy against C. albicans pathogenicity and that they can be developed as potential options for the clin. treatment of candidiasis.

Marine Drugs published new progress about Agglutinin-like protein 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Leyte-Lugo, Martha; Richomme, Pascal; Poupard, Pascal; Pena-Rodriguez, Luis M. published the artcile< Identification and quantification of a phytotoxic metabolite from Alternaria dauci>, Reference of 2873-36-1, the main research area is Daucus carota Alternaria dauci phytotoxic metabolite quantification; Alternaria leaf blight; Daucus carota; p-hydroxybenzoic acid; phytotoxins; α-acetylorcinol.

Alternaria dauci is the causal agent of Alternaria leaf blight (ALB) in carrot (Daucus carota) crops around the world. However, to date, A. dauci has received limited attention in its production of phytotoxic metabolites. In this investigation, the bioassay-guided isolation of the extract from liquid cultures of A. dauci resulted in the isolation of two metabolites identified as α-acetylorcinol (1) and p-hydroxybenzoic acid (2), based on their spectroscopic data and results from chem. correlation reactions. Testing of both metabolites in different assays showed an important phytotoxic activity for p-hydroxybenzoic acid (2) when tested in the leaf-spot assay on parsley (Petroselinum crispum), in the leaf infiltration assay on tobacco (Nicotiana alata) and marigold (Tagetes erecta), and in the immersion assay on parsley and parsnip (Pastinaca sativa) leaves. Quantification of the two metabolites in the crude extract of A. dauci kept at different times showed that p-hydroxybenzoic acid (2) is one of the first metabolites to be synthesized by the pathogen, suggesting that this salicylic acid derivative could play an important role in the pathogenicity of the fungus.

Molecules published new progress about Alternaria dauci. 2873-36-1 belongs to class pyrazines, and the molecular formula is C11H18N2O2, Reference of 2873-36-1.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem