scholarly journals 3,5-Bis((E)-4-methoxybenzylidene)-1-(2-morpholinoethyl)piperidin-4-one

Molbank ◽  
10.3390/m1159 ◽  
2020 ◽  
Vol 2020 (4) ◽  
pp. M1159
Author(s):  
Tyas Kuswardani ◽  
Noval Herfindo ◽  
Neni Frimayanti ◽  
Rudi Hendra ◽  
Adel Zamri
Keyword(s):  
Mass Spectrometry ◽  
Inhibitory Activity ◽  
Title Compound ◽  
Chemical Structure ◽  
Ns3 Protease

The 3,5-bis((E)-4-methoxybenzylidene)-1-(2-morpholinoethyl)piperidin-4-one (3) compound was synthesized by a two-step reaction with 92% yield. The chemical structure of compound 3 was confirmed by IR, NMR, and mass spectrometry. The title compound was screened for its anti-dengue activity against DENV2 NS2B-NS3 protease and showed 39.09% inhibitory activity at 200 µg/mL.

scholarly journals Mass Spectrometry versus Conventional Techniques of Protein Detection: Zika Virus NS3 Protease Activity towards Cellular Proteins

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3732
Author(s):  
Agnieszka Dabrowska ◽  
Aleksandra Milewska ◽  
Joanna Ner-Kluza ◽  
Piotr Suder ◽  
Krzysztof Pyrc
Keyword(s):  
Mass Spectrometry ◽  
Zika Virus ◽  
Viral Infections ◽  
Protein Detection ◽  
Extensive Discussion ◽  
Protein Targets ◽  
Highly Sensitive ◽  
Infected Cells ◽  
Ns3 Protease ◽  
To Receive

Mass spectrometry (MS) used in proteomic approaches is able to detect hundreds of proteins in a single assay. Although undeniable high analytical power of MS, data acquired sometimes lead to confusing results, especially during a search of very selective, unique interactions in complex biological matrices. Here, we would like to show an example of such confusing data, providing an extensive discussion on the observed phenomenon. Our investigations focus on the interaction between the Zika virus NS3 protease, which is essential for virus replication. This enzyme is known for helping to remodel the microenvironment of the infected cells. Several reports show that this protease can process cellular substrates and thereby modify cellular pathways that are important for the virus. Herein, we explored some of the targets of NS3, clearly shown by proteomic techniques, as processed during infection. Unfortunately, we could not confirm the biological relevance of protein targets for viral infections detected by MS. Thus, although mass spectrometry is highly sensitive and useful in many instances, also being able to show directions where cell/virus interaction occurs, we believe that deep recognition of their biological role is essential to receive complete insight into the investigated process.

Omphaloprenol A: A new bioactive polyisoprenepolyol isolated from the mycelium of poisonous mushroom Omphalotus japonicus

2021 ◽  
Author(s):  
Satoki Aoki ◽  
Takako Aboshi ◽  
Takumu Onodera ◽  
Ken-ichi Kimura ◽  
Daisuke Arai ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Nuclear Magnetic Resonance ◽  
Magnetic Resonance ◽  
Secondary Metabolites ◽  
Bioactive Compounds ◽  
Chemical Structure ◽  
Lettuce Seeds ◽  
Illudin S ◽  
Poisonous Mushroom ◽  
Growth Promoting

Abstract Mushrooms of the Omphalotus genus are known to be rich in secondary metabolites. In the quest for new bioactive compounds, we analyzed the compounds isolated from the mycelium of the poisonous mushroom Omphalotus japonicus. As a result, a new polyisoprenepolyol, which was named omphaloprenol A, was identified, along with known substances such as hypsiziprenol A10 and A11, illudin S, and ergosterol. The chemical structure of omphaloprenol A was elucidated by nuclear magnetic resonance and infrared spectroscopies and mass spectrometry, and its bioactivity was investigated. Omphaloprenol A showed growth promoting activity against the root of lettuce seeds and cytotoxicity against HL60 cells. To the best of our knowledge, this is the first report on the isolation of a polyisoprenepolyol compound from Omphalotaceae mushrooms.

scholarly journals 2α-Acetoxy-15-acetylartemisiifolin, a new Anti-trypanosomal Sesquiterpene Lactone from Mikania guaco

2017 ◽  
Vol 12 (5) ◽  
pp. 1934578X1701200
Author(s):  
Ahmed A. Hussein ◽  
Luz Romero ◽  
Jose Luis López-Pérez ◽  
Mahabir P. Gupta
Keyword(s):  
Mass Spectrometry ◽  
Trypanosoma Cruzi ◽  
Sesquiterpene Lactone ◽  
Chemical Structure ◽  
Methanol Extract ◽  
Amastigote Form ◽  
Bioassay Guided Fractionation ◽  
Nmr Techniques

Mikania guaco Bonpl. methanol extract showed an interesting activity against Trypanosoma cruzi with an IC50 of 4 μg/mL. Bioassay-guided fractionation of the methanol extract resulted in the isolation of a new sesquiterpene lactone, 2α-acetoxy, 15-acetylartemisiifolin (1), which was shown to be active (IC50 = 25 μM) against the amastigote form of T. cruzi,. The chemical structure of 1 was elucidated using 2-D NMR techniques and mass spectrometry.

scholarly journals Ubiquitin-Proteasome Modulating Dolabellanes and Secosteroids from Soft Coral Clavularia flava

Marine Drugs ◽  
2020 ◽  
Vol 18 (1) ◽  
pp. 39
Author(s):  
Che-Yen Chiu ◽  
Xue-Hua Ling ◽  
Shang-Kwei Wang ◽  
Chang-Yih Duh
Keyword(s):  
Inhibitory Activity ◽  
Structure Elucidation ◽  
Chemical Structure ◽  
Soft Coral ◽  
Proteasome Inhibitors ◽  
Proteasome Inhibition ◽  
Structural Elucidation ◽  
Bioactive Molecules ◽  
High Content Screening ◽  
Ubiquitin Proteasome

We performed a high-content screening (HCS) assay aiming to discover bioactive molecules with proteasome inhibitory activity. By structural elucidation, we identified six compounds purified from soft coral Clavularia flava, which potentiates proteasome inhibition. Chemical structure elucidation revealed they are dolabellane- and secosteroid-based compounds including a new dolabellane, clavinflol C (1), three known dolabellanes, stolonidiol (2), stolonidiol-17-acetate (3), and clavinflol B (4) as well as two new secosteroids, 3β,11-dihydroxy-24-methyl-9,11-secocholest-5-en-9,23-dione (5) and 3β,11-dihydroxy-24-methylene-9,11-secocholest-5-en-9,23-dione (6). All six compounds show less cytotoxicity than those of known proteasome inhibitors, bortezomib and MG132. In summary, the high-content measurements of control inhibitors, bortezomib and MG132, manifest the highest ratio >2 in high-content measurement. Of the isolated compounds, 2 and 5 showed higher activity, followed by 3 and 6, and then 1 and 4 exhibited moderate inhibition.

scholarly journals Reducing-End Functionalization of 2,5-Anhydro-d-mannofuranose-Linked Chitooligosaccharides by Dioxyamine: Synthesis and Characterization

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1143 ◽  
Author(s):  
Maxence Coudurier ◽  
Jimmy Faivre ◽  
Agnès Crépet ◽  
Catherine Ladavière ◽  
Thierry Delair ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
13C Nmr ◽  
Nitrous Acid ◽  
Chemical Structure ◽  
Chemical Method ◽  
Reductive Amination ◽  
High Mass ◽  
Synthesis And Characterization ◽  
1H And 13C Nmr ◽  
Chitosan Oligosaccharides

The nitrous acid depolymerization of chitosan enables the synthesis of singular chitosan oligosaccharides (COS) since their reducing-end unit is composed of 2,5-anhydro-d-mannofuranose (amf). In the present study, we describe a chemical method for the reducing-end conjugation of COS-amf by the commercially available dioxyamine O,O′-1,3-propanediylbishydroxylamine in high mass yields. The chemical structure of resulting dioxyamine-linked COS-amf synthesized by both oximation and reductive amination ways were fully characterized by 1H- and 13C-NMR spectroscopies and MALDI-TOF mass spectrometry. The coupling of chemically attractive linkers such as dioxyamines at the reducing end of COS-amf forms a relevant strategy for the development of advanced functional COS-based conjugates.

scholarly journals Characterization of platinum(II) complexes exhibiting inhibitory activity against the 20S proteasome

2020 ◽  
Vol 7 (8) ◽  
pp. 200545
Author(s):  
Tatsuto Kiwada ◽  
Hiromu Katakasu ◽  
Serina Okumura ◽  
Akira Odani
Keyword(s):  
Inhibitory Activity ◽  
Chemical Structure ◽  
Competitive Inhibition ◽  
Proteasome Inhibitors ◽  
Platinum Complex ◽  
Platinum Complexes ◽  
Binding Mode ◽  
Structure Activity Relationships ◽  
Structure Activity

Proteasome inhibitors are useful for biochemical research and clinical treatment. In our previous study, we reported that the 4N-coordinated platinum complexes with anthracenyl ring and heterocycle exhibited proteasome-inhibitory activity. In the present study, the structure–activity relationships and characterization of these complexes were determined for the elucidation of the role of aromatic ligands. Lineweaver–Burk analysis revealed that the chemical structure of heterocycles affects the binding mode of platinum complexes. Platinum complexes with anthracenyl ring and pyridine showed competitive inhibition, although platinum complexes with anthracenyl ring and phenanthroline showed non-competitive inhibition. The structure–activity relationships demonstrated that anthracenyl moiety plays a crucial role in proteasome-inhibitory activity. The platinum complexes with naphthyl or phenyl rings exhibited lower inhibitory activities than the platinum complex with anthracenyl ring. The reactivity with N-acetylcysteine varied according to the chemical structure of complexes.

GC-MS Investigation and Acetylcholinesterase Inhibitory Activity of Galanthus rizehensis

2013 ◽  
Vol 68 (3-4) ◽  
pp. 118-124 ◽  
Author(s):  
Buket Bozkurt Sarikaya ◽  
Nehir Unver Somer ◽  
Gulen Irem Kaya ◽  
Mustafa Ali Onur ◽  
Jaume Bastida ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Gas Chromatography ◽  
Inhibitory Activity ◽  
Gas Chromatography Mass Spectrometry ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
Chromatography Mass Spectrometry ◽  
Inhibitory Activities ◽  
Alkaloid Extracts ◽  
Potent Inhibitory Activity

GC-MS (gas chromatography-mass spectrometry) analyses of alkaloids in the aerial parts and bulbs of Galanthus rizehensis Stern (Amaryllidaceae), collected during two different vegetation periods, was performed. Twenty three alkaloids were identified in four different alkaloid extracts. Acetylcholinesterase (AChE) inhibitory activities of the alkaloid extracts were tested. Both the highest alkaloid diversity and the most potent inhibitory activity (IC50 12.94 μg/ml) were obtained in extracts from the bulbs of G. rizehensis collected during the fruiting period.

Chemical Ionization Mass Spectrometry of Organophosphorus Insecticides

1974 ◽  
Vol 57 (5) ◽  
pp. 1050-1055 ◽  
Author(s):  
Roy L Holmstead ◽  
John E Casida
Keyword(s):  
Mass Spectrometry ◽  
Electron Impact ◽  
Mass Spectra ◽  
Chemical Structure ◽  
Chemical Ionization ◽  
Ionization Mass Spectrometry ◽  
Chemical Ionization Mass Spectrometry ◽  
Ionization Mass ◽  
Organophosphorus Insecticides ◽  
Fragmentation Patterns

Abstract The chemical ionization (CI) mass spectra of 15 important organophosphorus insecticides and 14 of their major metabolites are discussed in relation to the effect of chemical structure on fragmentation patterns. The fragments obtained with CI are sometimes quite different from those formed on electron impact and, in general, simpler spectra are obtained with CI.

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