13,415 results match your criteria Bioorganic & medicinal chemistry letters[Journal]


Cytotoxic polyphenolic compounds from Lespedeza bicolor stem bark.

Fitoterapia 2019 Apr 17. Epub 2019 Apr 17.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch, Russian Academy of Sciences, Prospect 100-let Vladivostoku 159, Vladivostok, 690022, Russia.

Four new pterocarpans (6aR,11aR)-6a,11a-dihydrolespedezol A (2), (6aR,11aR)-2-isoprenyl-6a,11a-dihydrolespedezol A (3), (6aR,11aR,3'R)-6a,11a-dihydrolespedezol A (4), (6aR,11aR,3'S)-6a,11a-dihydrolespedezol A (5) and one new stilbenoid with 1,2-diketone fragment named bicoloketone (6) along with one previously known pterocarpen lespedezol A (1) have been isolated from Lespedeza bicolor stem bark using multistage column chromatography on polyamide and silica gel. The structures of the isolated polyphenolic compounds were determined by spectroscopic methods. The absolute configurations of 4 and 5 were determined by comparison of their electronic circular dichroism (ECD) spectra obtained experimentally and the spectra calculated using time-dependent density functional theory (TDDFT). Read More

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http://dx.doi.org/10.1016/j.fitote.2019.04.003DOI Listing

Dual DNA topoisomerase 1 and tyrosyl-DNA phosphodiesterase 1 inhibition for improved anticancer activity.

Med Res Rev 2019 Apr 19. Epub 2019 Apr 19.

Laboratory of Bioorganic Chemistry of Enzymes, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, Novosibirsk, Russian Federation.

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a DNA repair enzyme that catalyzes the hydrolysis of the phosphodiester bond in the DNA-topoisomerase 1 (Top1) covalent complex and repairs some other 3'-end DNA adducts. Currently, Tdp1 functions as an important target in cancer drug design owing to its ability to break down various DNA adducts induced by chemotherapeutics. Tdp1 inhibitors may sensitize tumor cells to the action of Top1 poisons, thereby potentiating their effects. Read More

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http://dx.doi.org/10.1002/med.21587DOI Listing

Immobilization of recombinant Escherichia coli whole cells harboring xylose reductase and glucose dehydrogenase for xylitol production from xylose mother liquor.

Bioresour Technol 2019 Apr 13;285:121344. Epub 2019 Apr 13.

Key Laboratory of Bioorganic Synthesis of Zhejiang Province, College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, PR China; Engineering Research Center of Bioconversion and Biopurification of Ministry of Education, Zhejiang University of Technology, Hangzhou 310014, PR China.

In this study, recombinant E. coli BL21(DE3)/pCDFDuet-1-XR-GDH harboring xylose reductase (XR) and glucose dehydrogenase (GDH) were immobilized and applied for the production of xylitol from xylose mother liquor (XML). Various immobilization methods were screened and the cross-linking approach with diatomite and polyetherimide as the raw materials and glutaraldehyde as the cross-linking agent was the optimal one, and the recovery activity reached of 80. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09608524193056
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http://dx.doi.org/10.1016/j.biortech.2019.121344DOI Listing
April 2019
2 Reads

Matrix attachment regions as a tool to influence plant transgene expression.

3 Biotech 2019 May 12;9(5):176. Epub 2019 Apr 12.

Biotron, Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry, Puschino, Russia.

The inclusion of special regulatory sequences known as matrix attachment regions (MARs) in transgene constructs has been suggested as a possible approach to stabilise the expression of foreign heterological genes. The present review provides a brief summary regarding the MARs that have been used in investigations studying their influence on plant transgene expression in different plants with different promoters and reporter genes, and the comparison of these investigations. Read More

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http://dx.doi.org/10.1007/s13205-019-1709-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6461602PMC

Durable liquid-crystalline vitrimer actuators.

Chem Sci 2019 Mar 23;10(10):3025-3030. Epub 2019 Jan 23.

MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology , Department of Chemistry , Tsinghua University , Beijing 100084 , China . Email:

Vitrimer-based liquid-crystalline elastomers (LCEs) exhibit great advantages over the traditional LCEs due to their inherent processability to realize monodomain alignment and construction of LCE actuators with complex 3D structures in a robust way. Though exciting progress has been made, how to achieve a proper balance between processability and actuation durability/stability remains a big challenge. Here, we report a strategy to mitigate the conflict between processability and actuation stability by reducing the catalyst content in an epoxy/acid LCE vitrimer system. Read More

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http://xlink.rsc.org/?DOI=C8SC05358H
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http://dx.doi.org/10.1039/c8sc05358hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427948PMC
March 2019
2 Reads

Direct Functionalization of White Phosphorus to Cyclotetraphosphanes: Selective Formation of Four P-C Bonds.

J Am Chem Soc 2019 Apr 18. Epub 2019 Apr 18.

Beijing National Laboratory for Molecular Sciences (BNLMS), Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry , Peking University , Beijing 100871 , China.

Converting elemental white phosphorus directly into organophosphorus or polyphosphorus is meaningful, challenging and attractive. The ate-complexes of aluminacyclopentadienes 1a,b react with P to afford selectively the cyclotetraphosphanes 2a,b featuring four newly formed P-C bonds and a planar square cyclo-P ring. Density functional theory calculations show that the conversion of tetrahedral P to planar cyclo-P moiety undergoes through an unexpected 1,1- P-insertion/Diels-Alder reaction/isomerization cascade process. Read More

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http://pubs.acs.org/doi/10.1021/jacs.9b02628
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http://dx.doi.org/10.1021/jacs.9b02628DOI Listing
April 2019
1 Read

Domain Diversity and Polarization Switching in Amino Acid β-Glycine.

Materials (Basel) 2019 Apr 15;12(8). Epub 2019 Apr 15.

School of Natural Sciences and Mathematics, Ural Federal University, Ekaterinburg 620000, Russia.

Piezoelectric materials based on lead zirconate titanate are widely used in sensors and actuators. However, their application is limited because of high processing temperature, brittleness, lack of conformal deposition and, more importantly, intrinsic incompatibility with biological environments. Recent studies on bioorganic piezoelectrics have demonstrated their potential in these applications, essentially due to using the same building blocks as those used by nature. Read More

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https://www.mdpi.com/1996-1944/12/8/1223
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http://dx.doi.org/10.3390/ma12081223DOI Listing
April 2019
1 Read

Identification of novel imidazole flavonoids as potent and selective inhibitors of protein tyrosine phosphatase.

Bioorg Chem 2019 Apr 9;88:102900. Epub 2019 Apr 9.

Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, People's Republic of China.

A series of imidazole flavonoids as new type of protein tyrosine phosphatase inhibitors were synthesized and characterized. Most of them gave potent protein phosphatase 1B (PTP1B) inhibitory activities. Especially, compound 11a could effectively inhibit PTP1B with an IC value of 0. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.074DOI Listing

Stereoselective Pd-Catalyzed Decarboxylative Allylation: Assembly of Highly Functionalized Allylic Amines Bearing a Quaternary Center.

Org Lett 2019 Apr 16. Epub 2019 Apr 16.

State Key Laboratory of Chemical Oncogenomics, Key Laboratory of Chemical Genomics , Peking University Shenzhen Graduate School , Shenzhen 518055 , China.

Here, we report a practical and reliable methodology to direct construction of tri- and tetrasubstituted olefins bearing an allylic amine, with the concomitant construction of the sterically congested quaternary stereocenter through stereoselective palladium-catalyzed cascade decarboxylation of vinyloxazolidinones. Read More

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http://pubs.acs.org/doi/10.1021/acs.orglett.9b00673
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http://dx.doi.org/10.1021/acs.orglett.9b00673DOI Listing
April 2019
1 Read

Direct intramolecular carbon(sp)-nitrogen(sp) reductive elimination from gold(iii).

Dalton Trans 2019 Apr 16. Epub 2019 Apr 16.

Department of Chemistry, University of Kentucky, 505 Rose Street, Lexington, Kentucky 40506, USA.

The reactivity of bidentate AuIII-Cl species, [(C^N)AuCl2], with a bisphosphine or carbon donor ligands results in reductive elimination. Combined experimental and computational investigations lead to the first evidence of a direct intramolecular C(sp2)-N(sp2) bond formation from a monomeric [(C^N)AuCl2] gold(iii) complex. We show that bidentate ligated Au(iii) systems bypass transmetallation to form C(sp2)-N(sp2) species and NHC-Au-Cl. Read More

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http://xlink.rsc.org/?DOI=C8DT05155K
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http://dx.doi.org/10.1039/c8dt05155kDOI Listing
April 2019
1 Read

Magnetically Hollow Pt Nanocages with Ultrathin Walls as a Highly Integrated Nanoreactor for Catalytic Transfer Hydrogenation Reaction.

Adv Sci (Weinh) 2019 Apr 7;6(7):1802132. Epub 2019 Feb 7.

Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education) Beijing Key Lab of Microanalytical Methods & Instrumentation Department of Chemistry Center for Synthetic and Systems Biology Tsinghua University Beijing 100084 P. R. China.

Fabricating efficient and stable nanocatalysts for chemoselective hydrogenation of nitroaromatics is highly desirable because the amines hold tremendous promise for the synthesis of nitrogen containing chemicals. Here, a highly reactive and stable porous carbon nitride encapsulated magnetically hollow platinum nanocage is developed with subnanometer thick walls (FeO@Pt@PCN) for this transformation. This well-controlled nanoreactor is prepared via the following procedures: the preparation of core template, the deposition of platinum nanocage with subnanometer thick walls, oxidative etching, and calcination. Read More

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http://dx.doi.org/10.1002/advs.201802132DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6446610PMC

Nickel-catalysed selective migratory hydrothiolation of alkenes and alkynes with thiols.

Nat Commun 2019 Apr 15;10(1):1752. Epub 2019 Apr 15.

State Key Laboratory of Coordination Chemistry, Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing University, 210093, Nanjing, China.

Direct (utilize easily available and abundant precursors) and selective (both chemo- and regio-) aliphatic C-H functionalization is an attractive mean with which to streamline chemical synthesis. With many possible sites of reaction, traditional methods often need an adjacent polar directing group nearby to achieve high regio- and chemoselectivity and are often restricted to a single site of functionalization. Here we report a remote aliphatic C-H thiolation process with predictable and switchable regioselectivity through NiH-catalysed migratory hydrothiolation of two feedstock chemicals (alkenes/alkynes and thiols). Read More

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http://dx.doi.org/10.1038/s41467-019-09783-wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6465347PMC

Microwave-assisted synthesis and in vitro stability of N-benzylamide non-steroidal anti-inflammatory drug conjugates for CNS delivery.

Bioorg Med Chem Lett 2019 Apr 8. Epub 2019 Apr 8.

Department of Chemistry, Muhlenberg College, 2400 Chew Street, Allentown, PA 18104, United States. Electronic address:

More effective delivery of non-steroidal anti-inflammatory drugs (NSAIDs) to the brain could treat the underlying inflammatory pathology of a range of CNS diseases and conditions. Use of a blood-brain barrier shuttle such as the N-benzylamide moiety, which has been largely unexplored for this purpose, could improve the brain bioavailabilities of NSAIDs. A series of novel N-benzylamide NSAID conjugates was synthesized via a three-step process with a microwave-assisted bimolecular nucleophilic substitution as the final step. Read More

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http://dx.doi.org/10.1016/j.bmcl.2019.04.016DOI Listing

Marine Bacterium V sp. CB1-14 Produces Guanidine Alkaloid 6--Monanchorin, Previously Isolated from Marine Polychaete and Sponges.

Mar Drugs 2019 Apr 4;17(4). Epub 2019 Apr 4.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry (PIBOC), Russian Academy of Sciences,Prospect 100 let Vladivostoku, 159, Vladivostok 690022, Russia.

Twenty-three bacterial strains were isolated from the secreted mucus trapping net of themarine polychaete Chaetopterus variopedatus (phylum Annelida) and twenty strains were identifiedusing 16S rRNA gene analysis. Strain CB1-14 was recognized as a new species of the genus Vibriousing the eight-gene multilocus sequence analysis (MLSA) and genome sequences of nineteen typeVibrio strains. This Vibrio sp. Read More

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http://dx.doi.org/10.3390/md17040213DOI Listing

Serial Femtosecond X-Ray Diffraction of HIV-1 Gag MA-IP6 Microcrystals at Ambient Temperature.

Int J Mol Sci 2019 Apr 3;20(7). Epub 2019 Apr 3.

Stanford PULSE Institute, SLAC National Accelerator Laboratory, Menlo Park, CA 94025, USA.

The Human immunodeficiency virus-1 (HIV-1) matrix (MA) domain is involved in the highly regulated assembly process of the virus particles that occur at the host cell's plasma membrane. High-resolution structures of the MA domain determined using cryo X-ray crystallography have provided initial insights into the possible steps in the viral assembly process. However, these structural studies have relied on large and frozen crystals in order to reduce radiation damage caused by the intense X-rays. Read More

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https://www.mdpi.com/1422-0067/20/7/1675
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http://dx.doi.org/10.3390/ijms20071675DOI Listing
April 2019
2 Reads

Derivatives of the β-Crinane Amaryllidaceae Alkaloid Haemanthamine as Multi-Target Directed Ligands for Alzheimer's Disease.

Molecules 2019 Apr 3;24(7). Epub 2019 Apr 3.

ADINACO Research Group, Department of Pharmaceutical Botany, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.

Twelve derivatives - of the β-crinane-type alkaloid haemanthamine were developed. All the semisynthetic derivatives were studied for their inhibitory potential against both acetylcholinesterase and butyrylcholinesterase. In addition, glycogen synthase kinase 3β (GSK-3β) inhibition potency was evaluated in the active derivatives. Read More

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http://dx.doi.org/10.3390/molecules24071307DOI Listing
April 2019
1 Read

Anti-trypanosomal activity of doubly modified salinomycin derivatives.

Eur J Med Chem 2019 Apr 3;173:90-98. Epub 2019 Apr 3.

Department of Bioorganic Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61‒614, Poznań, Poland.

As a group of biologically active compounds, polyether antibiotics (ionophores) show a broad spectrum of interesting pharmacological properties, ranging from anti-bacterial to anti-cancer activities. There is increasing evidence that ionophores, including salinomycin (SAL), and their semi-synthetic analogues are promising candidates for the development of drugs against parasitic diseases. Our previous studies have shown that esterification and amidation of the C1 carboxylate moiety of SAL provides compounds with potent activity against Trypanosoma brucei, protozoan parasites responsible for African trypanosomiasis. Read More

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http://dx.doi.org/10.1016/j.ejmech.2019.03.061DOI Listing
April 2019
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Preclinical Study of Biofunctional Polymer-Coated Upconversion Nanoparticles.

Toxicol Sci 2019 Apr 15. Epub 2019 Apr 15.

Nizhny Novgorod State University, Nizhny Novgorod, Russia.

Upconversion nanoparticles (UCNPs) are new-generation photoluminescent nanomaterials gaining considerable recognition in the life sciences due to their unique optical properties that allow high-contrast imaging in cells and tissues. UCNP applications in optical diagnosis, bioassays, therapeutics, photodynamic therapy, drug delivery, and light-controlled release of drugs are promising, demanding a comprehensive systematic study of their pharmacological properties. We report on production of biofunctional UCNP-based nanocomplexes suitable for optical microscopy and imaging of HER2-positive cells and tumors, as well as on the comprehensive evaluation of their pharmacokinetics, pharmacodynamics, and toxicological properties using cells and laboratory animals. Read More

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https://academic.oup.com/toxsci/advance-article/doi/10.1093/
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http://dx.doi.org/10.1093/toxsci/kfz086DOI Listing
April 2019
4 Reads

Organocatalytic enantioselective direct alkylation of phloroglucinol derivatives: asymmetric total synthesis of (+)-aflatoxin B.

Chem Commun (Camb) 2019 Apr 15. Epub 2019 Apr 15.

School of Pharmaceutical Sciences, Key Laboratory of Bioorganic Phosphorus, Chemistry & Chemical Biology (Ministry of Education), Beijing Frontier Research, Center for biological Structure, Tsinghua University, Beijing 100084, China.

The organocatalytic enantioselective Friedel-Crafts alkylation of phloroglucinol derivatives with enals is reported, providing general access to the benzylic chiral centers shown in a variety of phloroglucinol natural products. The synthetic utility is demonstrated by the very concise asymmetric total synthesis of aflatoxins B2. Read More

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http://dx.doi.org/10.1039/c9cc01833fDOI Listing

Properties of a cryptic lysyl oxidase from haloarchaeon .

PeerJ 2019 5;7:e6691. Epub 2019 Apr 5.

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Moscow, Russia.

Background: Lysyl oxidases (LOX) have been extensively studied in mammals, whereas properties and functions of recently found homologues in prokaryotic genomes remain enigmatic.

Methods: LOX open reading frame was cloned from in an expression vector. Recombinant lysyl oxidase (HTU-LOX) proteins were purified using metal affinity chromatography under denaturing conditions followed by refolding. Read More

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https://peerj.com/articles/6691
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http://dx.doi.org/10.7717/peerj.6691DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6452851PMC
April 2019
1 Read

Production of Marker-Free Apple Plants Expressing the Supersweet Protein Gene Driven by Plant Promoter.

Front Plant Sci 2019 29;10:388. Epub 2019 Mar 29.

Laboratory of Expression Systems and Modification of the Plant Genome "Biotron", Branch of the Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino, Russia.

The presence of antibiotic resistance and other marker genes in genetically modified plants causes concern in society because of perceived risks for the environment and human health. The creation of transgenic plants that do not contain foreign genetic material, especially that of bacterial and viral origin, largely alleviates the tension and makes the plants potentially more attractive for consumers. To produce marker-free transgenic apple plants, we used the pMF1 vector, which combines recombinaseR and a bifunctional selectable gene. Read More

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https://www.frontiersin.org/article/10.3389/fpls.2019.00388/
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http://dx.doi.org/10.3389/fpls.2019.00388DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6449483PMC
March 2019
2 Reads

Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development.

Front Cell Neurosci 2019 28;13:124. Epub 2019 Mar 28.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD, United States.

Adenosine receptors (ARs) function in the body's response to conditions of pathology and stress associated with a functional imbalance, such as in the supply and demand of energy/oxygen/nutrients. Extracellular adenosine concentrations vary widely to raise or lower the basal activation of four subtypes of ARs. Endogenous adenosine can correct an energy imbalance during hypoxia and other stress, for example, by slowing the heart rate by AAR activation or increasing the blood supply to heart muscle by the AAR. Read More

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http://dx.doi.org/10.3389/fncel.2019.00124DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6447611PMC
March 2019
1 Read

Growth inhibition of human breast and prostate cancer cells by cinnamic acid derivatives and their mechanism of action.

Biol Pharm Bull 2019 Apr 12. Epub 2019 Apr 12.

Laboratory of Physiological Chemistry, Institute of Medicinal Chemistry, Hoshi University.

Cancer is the leading cause of death and there is a particularly pressing need to develop effective treatments for breast and prostate cancer. In the current study, we show the inhibitory effects of cinnamic acid derivatives, including caffeic acid phenethyl ester (CAPE, 1), on the growth of breast and prostate cancer cells. Among the compounds examined, 3,4,5-trihydroxycinnamic acid decyl ester (6) showed the most potent inhibition of cancer cell growth by the induction of apoptosis. Read More

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http://dx.doi.org/10.1248/bpb.b18-01002DOI Listing

Seed germination, respiratory processes and phosphatidic acid accumulation in Arabidopsis diacylglycerol kinase knockouts - The effect of brassinosteroid, brassinazole and salinity.

Steroids 2019 Apr 11. Epub 2019 Apr 11.

Department of the Molecular Mechanisms of Cell Metabolism Regulation, Kukhar Institute of Bioorganic Chemistry and Petrochemistry, The National Academy of Sciences of Ukraine, 02660, Murmanska str., 1, Kyiv, Ukraine. Electronic address:

Using Arabidopsis thaliana wild type (WT) plants and diacylglycerol kinase knockouts (single mutants - dgk3, dgk1, dgk6; double mutants - dgk3dgk7, dgk5dgk6, dgk1dgk2) we observed that the inhibitor of brassinosteroid (BR) biosynthesis, brassinazole (BRZ), drastically decreased germination of dgk mutants under salt stress, while BRZ co-administration with 24-epibrassinolide (EBL) partially improved germination rates. We also observed a statistically significant decrease in alternative and cytochrome respiratory pathways in response to BRZ treatment under salinity conditions. We showed that production of the lipid second messenger phosphatidic acid (PA) is impaired in dgk mutants in response to EBL treatment and inhibitor of diacylglycerol kinase (DGK) - R59022. Read More

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http://dx.doi.org/10.1016/j.steroids.2019.04.002DOI Listing

Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.

Bioorg Med Chem Lett 2019 Apr 6. Epub 2019 Apr 6.

Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1 E7HT, UK.

In this work, the synthesis and the pharmacological evaluation of diphenoxyadamantane alkylamines Ia-f and IIa-f is described. The new diphenoxy-substituted adamantanes share structural features present in trypanocidal and antitubercular agents. 1-Methylpiperazine derivative Ia is the most potent against T. Read More

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http://dx.doi.org/10.1016/j.bmcl.2019.04.010DOI Listing
April 2019
2.420 Impact Factor

Massive Cryptosporidium infections and chronic diarrhea in HIV-negative patients.

Parasitol Res 2019 Apr 12. Epub 2019 Apr 12.

Department and Clinic of Tropical and Parasitic Diseases, Poznań University of Medical Sciences, Przybyszewskiego Street, 60-355, Poznań, Poland.

Protozoa of the genus Cryptosporidium are common parasites of domestic and wild animals-mammals, birds, reptiles, and fishes. The invasive forms are thick-walled oocysts, which can be present in water supplies, on fruits, vegetables, or in the soil contaminated with feces. In this work, we describe three cases of middle-aged persons with massive Cryptosporidium hominis infection and chronic diarrhea with no immunological abnormalities and no history of previous travels to tropical countries. Read More

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http://dx.doi.org/10.1007/s00436-019-06302-0DOI Listing
April 2019
3 Reads

Potent and selective caspase-2 inhibitor prevents MDM-2 cleavage in reversine-treated colon cancer cells.

Cell Death Differ 2019 Apr 11. Epub 2019 Apr 11.

NCI Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, CA, 92037, USA.

Most caspases can be positioned unambiguously within the regulated cell death networks of apoptosis and pyroptosis, but the role of caspase-2, a highly conserved protease within the family, remains enigmatic. This is mainly due to lack of selective chemical and biochemical tools for the investigation of this protease. In this study, we used our hybrid combinatorial substrate library (HyCoSuL) approach to broadly profile caspase-2 substrate specificity using peptide scanning libraries. Read More

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http://dx.doi.org/10.1038/s41418-019-0329-2DOI Listing

Four N-(E)-cinnamoyl (cinnamamide) derivatives of aminoalkanols with promising anticonvulsant and analgesic activity.

Bioorg Med Chem Lett 2019 Apr 4. Epub 2019 Apr 4.

Department of Bioorganic Chemistry, Chair of Organic Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.

Epilepsy and neuropathic pain are frequent neurological disorders with pathomechanism based on abnormal neuronal discharges. Secondary tissue impairment observed after traumatic brain injury is also connected with neuronal dysfunction. Those three neurological disorders are ineffectively treated with currently available pharmacotherapy options so great effort is made in searching for new effective drugs. Read More

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http://dx.doi.org/10.1016/j.bmcl.2019.04.006DOI Listing

Immunoreactivity changes of human serum albumin and alpha-1-microglobulin induced by their interaction with dendrimers.

Colloids Surf B Biointerfaces 2019 Apr 4;179:226-232. Epub 2019 Apr 4.

Department of General Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, Lodz, Poland. Electronic address:

Dendrimers are hyperbranched polymers for delivery of therapeutic genetic material to cancer cells. The fine tuning chemical modifications of dendrimers allow for the modification of the composition. The architecture and the properties of dendrimers are key factors to improve their in vitro and in vivo properties such as biocompatibility with cells and tissues and their pharmacokinetic/pharmacodynamic behavior. Read More

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http://dx.doi.org/10.1016/j.colsurfb.2019.03.065DOI Listing
April 2019
1 Read

Hybrid design of isonicotinic acid hydrazide derivatives: machine learning studies, synthesis and biological evaluation of their anti-tuberculosis activity.

Curr Drug Discov Technol 2019 Apr 11. Epub 2019 Apr 11.

V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Science of Ukraine, 1 Murmanska Street, 02660, Kyiv. Ukraine.

Background: Tuberculosis (TB) is an infection disease caused by Mycobacterium tuberculosis (Mtb) bacteria. One of the main causes of mortality from TB is the problem of Mtb resistance to known drugs.

Objective: The goal of this work is to identify potent small molecule anti-TB agents by machine learning, synthesis and biological evaluation. Read More

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http://dx.doi.org/10.2174/1570163816666190411110331DOI Listing
April 2019
3 Reads

1,4-Disubstituted 1-1,2,3-Triazole Containing Peptidotriazolamers: A New Class of Peptidomimetics With Interesting Foldamer Properties.

Front Chem 2019 26;7:155. Epub 2019 Mar 26.

Organic and Bioorganic Chemistry, Department of Chemistry, Bielefeld University, Bielefeld, Germany.

Peptidotriazolamers are hybrid foldamers with features of peptides and triazolamers, containing alternation of amide bonds and 1,4-disubstituted 1-1,2,3-triazoles with conservation of the amino acid side chains. We report on the synthesis of a new class of peptidomimetics, containing 1,4-disubstituted 1-1,2,3-triazoles in alternation with amide bonds and the elucidation of their conformational properties in solution. Based on enantiomerically pure propargylamines bearing the stereogenic center in the propargylic position and α-azido esters, building blocks were obtained by copper-catalyzed azide-alkyne cycloaddition. Read More

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http://dx.doi.org/10.3389/fchem.2019.00155DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6443886PMC

An experimental assay of the interactions of amino acids from orthologous sequences shaping a complex fitness landscape.

PLoS Genet 2019 Apr 10;15(4):e1008079. Epub 2019 Apr 10.

Institute of Science and Technology Austria, Am Campus 1, Klosterneuburg, Austria.

Characterizing the fitness landscape, a representation of fitness for a large set of genotypes, is key to understanding how genetic information is interpreted to create functional organisms. Here we determined the evolutionarily-relevant segment of the fitness landscape of His3, a gene coding for an enzyme in the histidine synthesis pathway, focusing on combinations of amino acid states found at orthologous sites of extant species. Just 15% of amino acids found in yeast His3 orthologues were always neutral while the impact on fitness of the remaining 85% depended on the genetic background. Read More

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http://dx.doi.org/10.1371/journal.pgen.1008079DOI Listing

Comparison of tumor‑targeting properties of directly and indirectly radioiodinated designed ankyrin repeat protein (DARPin) G3 variants for molecular imaging of HER2.

Int J Oncol 2019 Feb 11. Epub 2019 Feb 11.

Department of Immunology, Genetics and Pathology, Uppsala University, SE 75185 Uppsala, Sweden.

Evaluation of human epidermal growth factor receptor 2 (HER2) expression levels in breast and gastroesophageal cancer is used for the stratification of patients for HER2‑targeting therapies. The use of radionuclide molecular imaging may facilitate such evaluation in a non‑invasive way. Designed ankyrin repeat proteins (DARPins) are engineered scaffold proteins with high potential as probes for radionuclide molecular imaging. Read More

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http://dx.doi.org/10.3892/ijo.2019.4712DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6411343PMC
February 2019
2 Reads
3.025 Impact Factor

Predicting queue wait time probabilities for multi-scale computing.

Philos Trans A Math Phys Eng Sci 2019 Apr;377(2142):20180151

2 Poznan Supercomputing and Networking Center , Institute of Bioorganic Chemistry of the Polish Academy of Sciences , ul Z. Noskowskiego 12/14 , 61-704 Poznan , Poland.

We describe a method for queue wait time prediction in supercomputing clusters. It was designed for use as a part of multi-criteria brokering mechanisms for resource selection in a multi-site High Performance Computing environment. The aim is to incorporate the time jobs stay queued in the scheduling system into the selection criteria. Read More

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http://dx.doi.org/10.1098/rsta.2018.0151DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6388012PMC
April 2019
2 Reads

Antifungal Paper Based on a Polyborneolacrylate Coating.

Polymers (Basel) 2018 Apr 17;10(4). Epub 2018 Apr 17.

Beijing Advanced Innovation Center for Soft Matter Science and Engineering, Beijing Laboratory of Biomedical Materials, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China.

Paper documents and products are very susceptible to microbial contamination and damage. Fungi are mainly responsible for those biodeterioration processes. Traditional microbicidal strategies constitute a serious health risk even when microbes are dead. Read More

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http://dx.doi.org/10.3390/polym10040448DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6415209PMC

Dammarane-type triterpenoids from the stem of Ziziphus glaziovii Warm. (Rhamnaceae).

Phytochemistry 2019 Apr 6;162:250-259. Epub 2019 Apr 6.

Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, D-06120 Halle (Saale), Germany. Electronic address:

Seven undescribed dammarane-type triterpenoids, together with ten known compounds, were isolated from the stems of Ziziphus glaziovii Warm (= Sarcomphalus glaziovii (Warm.) Hauenschild). The structures were fully assigned by means of uni- and bidimensional NMR and HR-ESI-MS experiments. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00319422183049
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http://dx.doi.org/10.1016/j.phytochem.2019.03.010DOI Listing
April 2019
1 Read

Photoinduced Proton Transfer of GFP-Inspired Fluorescent Superphotoacids: Principles and Design.

J Phys Chem B 2019 Apr 18. Epub 2019 Apr 18.

Department of Chemistry , Oregon State University , 153 Gilbert Hall , Corvallis , Oregon 97331 , United States.

Proton transfer remains one of the most fundamental processes in chemistry and biology. Superphotoacids provide an excellent platform to delineate the excited-state proton transfer (ESPT) mechanism on ultrafast time scales and enable one to precisely control photoacidity and other pertinent functionalities such as fluorescence. We modified the GFP core ( p-HBDI chromophore) into two series of highly fluorescent photoacids by fluorinating the phenolic ring and conformationally locking the backbone (i. Read More

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http://dx.doi.org/10.1021/acs.jpcb.9b03201DOI Listing
April 2019
2 Reads

Experimental Evidence of the Existence of Interleaflet Coupled Nanodomains: An MC-FRET Study.

J Phys Chem Lett 2019 Apr 11:2024-2030. Epub 2019 Apr 11.

Department of Biophysical Chemistry , J. Heyrovský Institute of Physical Chemistry of the Czech Academy of Sciences , 182 23 Prague , Czech Republic.

Plasma membranes of living cells are compartmentalized into small submicroscopic structures (nanodomains) having potentially relevant biological functions. Despite this, structural features of these nanodomains remain elusive, primarily due to the difficulties in characterizing such small dynamic entities. It is unclear whether nanodomains found in the upper bilayer leaflet are transversally registered with those found in the lower leaflet. Read More

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http://dx.doi.org/10.1021/acs.jpclett.9b00390DOI Listing

Droplet-Assisted Microfluidic Fabrication and Characterization of Multifunctional Polysaccharide Microgels Formed by Multicomponent Reactions.

Polymers (Basel) 2018 Sep 21;10(10). Epub 2018 Sep 21.

Institute of Physical Chemistry and Polymer Physics, Leibniz-Institut für Polymerforschung Dresden e.V., D-01069 Dresden, Germany.

Polysaccharide-based microgels have broad applications in multi-parametric cell cultures, cell-free biotechnology, and drug delivery. Multicomponent reactions like the Passerini three-component and the Ugi four-component reaction are shown in here to be versatile platforms for fabricating these polysaccharide microgels by droplet microfluidics with a narrow size distribution. While conventional microgel formation requires pre-modification of hydrogel building blocks to introduce certain functionality, in multicomponent reactions one building block can be simply exchanged by another to introduce and extend functionality in a library-like fashion. Read More

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http://dx.doi.org/10.3390/polym10101055DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6403549PMC
September 2018

Inorganic Polysulfides and Related Reactive Sulfur–Selenium Species from the Perspective of Chemistry.

Molecules 2019 04 6;24(7). Epub 2019 Apr 6.

Division of Bioorganic Chemistry, School of Pharmacy, University of Saarland, D-66123 Saarbruecken, Germany.

Polysulfides (H₂S) represent a class of reactive sulfur species (RSS) which includes molecules such as H₂S₂, H₂S₃, H₂S₄, and H₂S and whose presence and impact in biological systems, when compared to other sulfur compounds, has only recently attracted the wider attention of researchers. Studies in this field have revealed a facet-rich chemistry and biological activity associated with such chemically simple, still unusual inorganic molecules. Despite their chemical simplicity, these inorganic species, as reductants and oxidants, metal binders, surfactant-like "cork screws" for membranes, components of perthiol signalling and reservoirs for inorganic hydrogen sulfide (H₂S), are at the centre of complicated formation and transformation pathways which affect numerous cellular processes. Read More

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http://dx.doi.org/10.3390/molecules24071359DOI Listing
April 2019
1 Read

LC-MS/MS study of the degradation processes of nitisinone and its by-products.

J Pharm Biomed Anal 2019 Mar 30;171:15-21. Epub 2019 Mar 30.

Department of Inorganic Chemistry, Analytical Chemistry and Electrochemistry, Faculty of Chemistry, Silesian University of Technology, B. Krzywoustego 6 Str, 44-100 Gliwice, Poland.

Nitisinone (2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione, NTBC) was the first synthetically produced triketone herbicide. However, its unsatisfactory herbicidal properties, negative impact on the natural environment and the high cost of synthesis have hindered its commercialization as a plant protection agent. Nevertheless, NTBC has become the medical treatment of choice for a rare hereditary metabolic disease -hepatorenal tyrosinemia. Read More

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http://dx.doi.org/10.1016/j.jpba.2019.03.046DOI Listing

A Method for Bischler-Napieralski-Type Synthesis of 3,4-Dihydroisoquinolines.

Org Lett 2019 Apr 8;21(8):2574-2577. Epub 2019 Apr 8.

Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry , Tsinghua University , Beijing 100084 , P.R. China.

A new method for the Bischler-Napieralski-type synthesis of 3,4-dihydroisoquinolines was developed by a TfO-promoted tandem annulation from phenylethanols and nitriles. Its success was mainly due to the fact that a phenonium ion was formed in the process and practically functioned as a stable and reactive primary phenylethyl carbocation. Read More

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http://dx.doi.org/10.1021/acs.orglett.9b00534DOI Listing

Enantioselective Total Synthesis of (+)-Arboridinine.

J Am Chem Soc 2019 Apr 17. Epub 2019 Apr 17.

State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering , Lanzhou University , Lanzhou 730000 , China.

The enantioselective total synthesis of cage-shaped alkaloid (+)-arboridinine is reported. The synthesis takes advantage of the stereoselective double-Mannich reaction to rapidly construct the aza[3.3. Read More

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http://dx.doi.org/10.1021/jacs.9b02362DOI Listing

Lectin activity of Pseudomonas aeruginosa vaccine candidates PSE17-1, PSE41-5 and PSE54.

Biochem Biophys Res Commun 2019 Apr 3. Epub 2019 Apr 3.

Institute for Glycomics, Griffith University, Gold Coast, QLD, 4222, Australia. Electronic address:

Pseudomonas aeruginosa is an opportunistic pathogen that causes nosocomial infections most commonly in immunocompromised, cystic fibrosis (CF) and burns patients. The pilin and Pseudomonas lectins 1 (PA-IL) and 2 (PA-IIL) are known glycan-binding proteins of P. aeruginosa that are involved in adherence to host cells, particularly CF host airways. Read More

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http://dx.doi.org/10.1016/j.bbrc.2019.03.092DOI Listing
April 2019
3 Reads

Inhibition of pre-miRNA-136 processing by Dicer with small molecule BzDANP suggested the formation of ternary complex of pre-miR-136-BzDANP-Dicer.

Bioorg Med Chem 2019 Mar 18. Epub 2019 Mar 18.

Department of Regulatory Bioorganic Chemistry, The Institute of Scientific and Industrial Research, Osaka University, 8-1 Mihogaoka, Ibaraki, Osaka 567-0047, Japan. Electronic address:

Small-molecule modulators, along with antisense oligonucleotide, would be powerful tools and potential drug candidates for modulating miRNA-related gene expressions. The mechanism of the inhibitory effect of the C-bulge binding small molecule BzDANP for the Dicer processing reaction of pre-miR-136 was discussed on the data obtained by SPR, NMR, and kinetic analysis for Dicer processing. SPR and NMR analysis showed the preference of BzDANP binding to the C-bulge. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09680896183217
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http://dx.doi.org/10.1016/j.bmc.2019.03.031DOI Listing
March 2019
4 Reads

Integration of stable isotope labeling derivatization and magnetic dispersive solid phase extraction for measurement of neurosteroids by in vivo microdialysis and UHPLC-MS/MS.

Talanta 2019 Jul 10;199:97-106. Epub 2019 Feb 10.

Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Institute of Analytical Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.

In this work, a novel strategy of stable isotope labeling derivatization (SILD) combined with magnetic dispersive solid-phase extraction (MDSPE), has been proposed for simultaneous monitoring of neurosteroids changes linked to Parkinson's disease (PD) by in vivo microdialysis. The developed method was based on ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) detection using multiple-reaction monitoring (MRM) mode. In this study, a new pair of stable isotope labeling reagents d-/d-3-N-methyl-2'-carboxyl Rhodamine 6G (d-/d-MCR6G), were designed and synthesized for derivatizing neurosteroids in rat blood microdialysates and neurosteroid standards, respectively. Read More

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http://dx.doi.org/10.1016/j.talanta.2019.02.011DOI Listing
July 2019
3 Reads

Regio- and stereoselective C-H functionalization of brassinosteroids.

Steroids 2019 Apr 2;146:92-98. Epub 2019 Apr 2.

Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich St., 5/2, 220141 Minsk, Belarus.

Late stage CH functionalization is a powerful tool for modification of natural compounds. Herein we report that the rhodium-catalyzed reaction of brassinosteroids with aryloxysulfonamides proceeds regio- and stereoselectively at C15 position. The derivative obtained from 24-epibrassinolide was easily transformed to the conjugate with a BODIPY dye bearing unaffected functional groups of the native brassinosteroid. Read More

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http://dx.doi.org/10.1016/j.steroids.2019.03.010DOI Listing
April 2019
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In Situ Monitoring of Fluid Shear Stress Enhanced Adherence of Bacteria to Cancer Cells on Microfluidic Chip.

Anal Chem 2019 Apr 15. Epub 2019 Apr 15.

Department of Chemistry, Beijing Key Laboratory of Microanalytical Methods and Instrumentation, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology , Tsinghua University , Beijing 100084 , China.

Mechanosensing mechanisms for surface recognition by bacteria play an important role in inflammation and phagocytosis. Here, we describe a set of DNA probes for revealing microbe adherence to cancer cells under fluid shear stress. DNA probes modified with a biotin group, an azido group, and hexadecanoic acid were indiscriminately anchored to the cell surface, acting as indicators for the membrane proteins, cell-surface carbohydrate, and phospholipids. Read More

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http://dx.doi.org/10.1021/acs.analchem.9b00394DOI Listing
April 2019
1 Read

Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines in Vitro.

Anticancer Agents Med Chem 2019 Apr 5. Epub 2019 Apr 5.

Department of Biotechnology and Genetic Engineering, Medical University of Silesia, 8 Jedności Str., 41-200 Sosnowiec. Poland.

Background: Natural plant metabolites and their semisynthetic derivatives have been used for years in cancer therapy. Xanthones are oxygenated heterocyclic compounds produced as secondary metabolites by higher plants, fungi or lichens. Xanthone core may serve as a template in the synthesis of many derivatives that have broad biological activities. Read More

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http://dx.doi.org/10.2174/1871520619666190405113519DOI Listing
April 2019
3 Reads