scholarly journals A new perspective on fungal metabolites: identification of bioactive compounds from fungi using zebrafish embryogenesis as read-out

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Jelmer Hoeksma ◽  
Tim Misset ◽  
Christie Wever ◽  
Johan Kemmink ◽  
John Kruijtzer ◽  
...  
Keyword(s):  
Biological Activity ◽  
Secondary Metabolites ◽  
High Resolution Mass Spectrometry ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Therapeutic Drug ◽  
Preparative Hplc ◽  
Active Compounds ◽  
Vis Spectroscopy ◽  
Therapeutic Compounds

AbstractThere is a constant need for new therapeutic compounds. Fungi have proven to be an excellent, but underexplored source for biologically active compounds with therapeutic potential. Here, we combine mycology, embryology and chemistry by testing secondary metabolites from more than 10,000 species of fungi for biological activity using developing zebrafish (Danio rerio) embryos. Zebrafish development is an excellent model for high-throughput screening. Development is rapid, multiple cell types are assessed simultaneously and embryos are available in high numbers. We found that 1,526 fungal strains produced secondary metabolites with biological activity in the zebrafish bioassay. The active compounds from 39 selected fungi were purified by liquid-liquid extraction and preparative HPLC. 34 compounds were identified by a combination of chemical analyses, including LCMS, UV-Vis spectroscopy/ spectrophotometry, high resolution mass spectrometry and NMR. Our results demonstrate that fungi express a wide variety of biologically active compounds, consisting of both known therapeutic compounds as well as relatively unexplored compounds. Understanding their biological activity in zebrafish may provide insight into underlying biological processes as well as mode of action. Together, this information may provide the first step towards lead compound development for therapeutic drug development.

scholarly journals Modular synthesis of α-fluorinated arylmethanes via desulfonylative cross-coupling

2019 ◽  
Vol 10 (1) ◽  
Author(s):  
Masakazu Nambo ◽  
Jacky C.-H. Yim ◽  
Luiza B. O. Freitas ◽  
Yasuyo Tahara ◽  
Zachary T. Ariki ◽  
...  
Keyword(s):  
Biological Activity ◽  
Late Stage ◽  
Recent Progress ◽  
Cross Coupling ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Arylboronic Acids ◽  
Modular Synthesis ◽  
Synthetic Routes

Abstract α-Fluoromethylarenes are common substructures in pharmaceuticals and agrochemicals, with the introduction of fluorine often resulting in improved biological activity and stability. Despite recent progress, synthetic routes to α-fluorinated diarylmethanes are still rare. Herein we describe the Pd-catalyzed Suzuki-Miyaura cross-coupling of α-fluorinated benzylic triflones with arylboronic acids affording structurally diverse α-fluorinated diarylmethanes. The ease of synthesis of fluorinated triflones as the key starting materials enables powerful late-stage transformations of known biologically active compounds into fluorinated analogs.

scholarly journals Monoterpenes as a renewable source of biologically active compounds

2017 ◽  
Vol 89 (8) ◽  
pp. 1105-1117 ◽  
Author(s):  
Nariman F. Salakhutdinov ◽  
Konstantin P. Volcho ◽  
Olga I. Yarovaya
Keyword(s):  
Biological Activity ◽  
Absolute Configuration ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Great Promise ◽  
Active Compounds ◽  
Renewable Source ◽  
The Creation ◽  
Anti Inflammatory

AbstractMonoterpenes and their derivatives play an important role in the creation of new biologically active compounds including drugs. The review focuses on the data on various types of biological activity exhibited by monoterpenes and their derivatives, including analgesic, anti-inflammatory, anticonvulsant, antidepressant, anti-Alzheimer, anti-Parkinsonian, antiviral, and antibacterial (anti-tuberculosis) effects. Searching for novel potential drugs among monoterpene derivatives shows great promise for treating various pathologies. Special attention is paid to the effect of absolute configuration of monoterpenes and monoterpenoids on their activity.

The Use of Cinnamic Acid and Cinnamaldehyde, as Bio-Based Molecules, in Organic Synthesis and Preparation of Biologically Active Compounds

2020 ◽  
Vol 17 ◽  
Author(s):  
Anna S. Zalivatskaya ◽  
Dmitriy N. Zakusilo ◽  
Aleksander V. Vasilyev
Keyword(s):  
Biological Activity ◽  
Double Bond ◽  
Carbonyl Group ◽  
Organic Compounds ◽  
Organic Synthesis ◽  
Cinnamic Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Platform Chemicals

: Cinnamic acid and cinnamaldehyde may be obtained from renewable plant bio-mass, Cinnamon plants, therefore these compounds should be considered as bio-based platform chemicals for synthesis of novel substances. This review describes recent achievements in organic synthesis based on transformations of cinnamaldehyde, cinnamic acid and its derivatives, focusing, mainly, on the preparation of biologically active compounds. Reactions of these cinnamic derivatives may proceed both onto carbon-carbon double bond and carbonyl group that allows obtaining a wide variety of organic compounds having high synthetic importance and different practically valuable properties, including biological activity.

scholarly journals Skeletocutins M–Q: biologically active compounds from the fruiting bodies of the basidiomycete Skeletocutis sp. collected in Africa

2019 ◽  
Vol 15 ◽  
pp. 2782-2789 ◽  
Author(s):  
Tian Cheng ◽  
Clara Chepkirui ◽  
Cony Decock ◽  
Josphat C Matasyoh ◽  
Marc Stadler
Keyword(s):  
Staphylococcus Aureus ◽  
Secondary Metabolites ◽  
Biofilm Formation ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Fruiting Bodies ◽  
Inhibition Assay ◽  
Active Compounds ◽  
New Compounds ◽  
New Metabolites

During the course of screening for new metabolites from basidiomycetes, we isolated and characterized five previously undescribed secondary metabolites, skeletocutins M–Q (1–5), along with the known metabolite tyromycin A (6) from the fruiting bodies of the polypore Skeletocutis sp. The new compounds did not exhibit any antimicrobial, cytotoxic, or nematicidal activities. However, compound 3 moderately inhibited the biofilm formation of Staphylococcus aureus (S. aureus), while compounds 3 and 4 performed moderately in the ʟ-leucine-7-amido-4-methylcoumarin (ʟ-Leu-AMC) inhibition assay. These compounds represent the first secondary metabolites reported to occur in the fruiting bodies by Skeletocutis. Interestingly, tyromycin A (6) was found to be the only common metabolite in fruiting bodies and mycelial cultures of the fungus, and none of the recently reported skeletocutins from the culture of the same strain were detected in the basidiomes.

Piperazine derivatives of boronic acids – potential bifunctional biologically active compounds

2015 ◽  
Vol 39 (6) ◽  
pp. 4308-4315 ◽  
Author(s):  
Agnieszka Adamczyk-Woźniak ◽  
Karolina Czerwińska ◽  
Izabela D. Madura ◽  
Alicja Matuszewska ◽  
Andrzej Sporzyński ◽  
...  
Keyword(s):  
Biological Activity ◽  
Boronic Acids ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Piperazine Derivatives ◽  
Derivatives Of

The combination of a piperazine and boronic groups within one molecule can result in a totally novel biological activity.

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