High-Throughput Preparation of Antibacterial Polymers from Natural Product Derivatives via the Hantzsch Reaction

2019 ◽  
Author(s):  
Guoqiang Liu ◽  
Qiang Zhang ◽  
Yongsan Li ◽  
Xing Wang ◽  
Haibo Wu ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
Hantzsch Reaction ◽  
Antibacterial Polymers

scholarly journals High-Throughput Preparation of Antibacterial Polymers from Natural Product Derivatives via the Hantzsch Reaction

iScience ◽  
2020 ◽  
Vol 23 (1) ◽  
pp. 100754 ◽  
Author(s):  
Guoqiang Liu ◽  
Qiang Zhang ◽  
Yongsan Li ◽  
Xing Wang ◽  
Haibo Wu ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
Hantzsch Reaction ◽  
Antibacterial Polymers

New Antileishmanial Drug Leads from a Library of Natural Product Fractions Prepared by a High Throughput Fractionation Paradigm*

Planta Medica ◽  
2012 ◽  
Vol 78 (05) ◽  
Author(s):  
SK Jain ◽  
R Sahu ◽  
J Zhang ◽  
MR Jacob ◽  
XC Li ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
Antileishmanial Drug ◽  
Drug Leads

High throughput huaman pancreactic lipase screening of natural product library for lipase inhibition activity

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
P Jiao ◽  
J Zhao ◽  
J Yeop Lee ◽  
J Tseng-Crank ◽  
B Corneliusen ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
Inhibition Activity ◽  
Natural Product Library ◽  
Lipase Screening ◽  
Lipase Inhibition

The Search for Novel Human Pancreatic α-Amylase Inhibitors: High-Throughput Screening of Terrestrial and Marine Natural Product Extracts

ChemBioChem ◽  
2008 ◽  
Vol 9 (3) ◽  
pp. 433-438 ◽  
Author(s):  
Chris A. Tarling ◽  
Kate Woods ◽  
Ran Zhang ◽  
Harry C. Brastianos ◽  
Gary D. Brayer ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Marine Natural Product ◽  
Amylase Inhibitors

scholarly journals Development of a Robust Cytopathic Effect-Based High-Throughput Screening Assay To Identify Novel Inhibitors of Dengue Virus

2012 ◽  
Vol 56 (6) ◽  
pp. 3399-3401 ◽  
Author(s):  
Kevin D. McCormick ◽  
Shufeng Liu ◽  
Jana L. Jacobs ◽  
Ernesto T. A. Marques ◽  
Nicolas Sluis-Cremer ◽  
...  
Keyword(s):  
Dengue Virus ◽  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Cytopathic Effect ◽  
Complex Molecule ◽  
Denv Infection ◽  
Screening Assay ◽  
High Throughput Screening Assay ◽  
Natural Product Library

ABSTRACTWe have developed a robust cytopathic effect-based high-throughput screening assay to identify inhibitors of dengue virus (DENV) infection. Screening of a small natural product library yielded 11 hits. Four of these were found to be potent inhibitors of DENV, although serotype differences were noted. Taken together, these data suggest that screening of larger and more complex molecule libraries may result in the identification of more potent and specific DENV inhibitors.

Logistic Considerations to Deliver Natural Product Libraries for High-­Throughput Screening

2015 ◽  
pp. 91-104
Author(s):  
Ngoc Pham ◽  
Stephen Toms ◽  
David Camp ◽  
Ronald Quinn
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening

High-Throughput, Microarray-Based Synthesis of Natural Product Analogues via in Vitro Metabolic Pathway Construction

2007 ◽  
Vol 2 (6) ◽  
pp. 419-425 ◽  
Author(s):  
Seok Joon Kwon ◽  
Moo-Yeal Lee ◽  
Bosung Ku ◽  
David H. Sherman ◽  
Jonathan S. Dordick
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
Metabolic Pathway

scholarly journals High-Throughput Screening Platform for Natural Product–Based Drug Discovery Against 3 Neglected Tropical Diseases

2014 ◽  
Vol 20 (1) ◽  
pp. 82-91 ◽  
Author(s):  
F. Annang ◽  
G. Pérez-Moreno ◽  
R. García-Hernández ◽  
C. Cordon-Obras ◽  
J. Martín ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Neglected Tropical Diseases ◽  
Chemical Diversity ◽  
Tropical Diseases ◽  
Isolation And Characterization ◽  
Microbial Extracts

African trypanosomiasis, leishmaniasis, and Chagas disease are 3 neglected tropical diseases for which current therapeutic interventions are inadequate or toxic. There is an urgent need to find new lead compounds against these diseases. Most drug discovery strategies rely on high-throughput screening (HTS) of synthetic chemical libraries using phenotypic and target-based approaches. Combinatorial chemistry libraries contain hundreds of thousands of compounds; however, they lack the structural diversity required to find entirely novel chemotypes. Natural products, in contrast, are a highly underexplored pool of unique chemical diversity that can serve as excellent templates for the synthesis of novel, biologically active molecules. We report here a validated HTS platform for the screening of microbial extracts against the 3 diseases. We have used this platform in a pilot project to screen a subset (5976) of microbial extracts from the MEDINA Natural Products library. Tandem liquid chromatography–mass spectrometry showed that 48 extracts contain potentially new compounds that are currently undergoing de-replication for future isolation and characterization. Known active components included actinomycin D, bafilomycin B1, chromomycin A3, echinomycin, hygrolidin, and nonactins, among others. The report here is, to our knowledge, the first HTS of microbial natural product extracts against the above-mentioned kinetoplastid parasites.

scholarly journals A High-Throughput Cell-Based Assay to Identify Specific Inhibitors of Transcription Factor AP-1

2006 ◽  
Vol 12 (1) ◽  
pp. 133-139 ◽  
Author(s):  
Katie M. Ruocco ◽  
Ekaterina I. Goncharova ◽  
Matthew R. Young ◽  
Nancy H. Colburn ◽  
James B. McMahon ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Natural Products ◽  
Natural Product ◽  
High Throughput ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Nordihydroguaiaretic Acid ◽  
Activator Protein 1 ◽  
Taxonomic Groups ◽  
High Throughput Assay

The oncogenic transcription factor AP-1 (activator protein–1) is required for tumor promotion and progression. Identification of novel and specific AP-1 inhibitors would be beneficial for cancer prevention and therapy. The authors have developed a high-throughput assay to screen synthetic and natural product libraries for noncytotoxic inhibitors of mitogen-activated AP-1 activity. The cell-based high-throughput screen is conducted in a 384-well format using a fluorescent resonance energy transfer (FRET) substrate to quantify the activity of a β-lactamase reporter under the control of an AP-1-dependent promoter. The ratiometric FRET readout makes this assay extremely robust and reproducible, particularly for use with natural product extracts. To eliminate false positives due to cell killing, a cytotoxicity assay was incorporated. The AP-1 β-lactamase reporter was validated with inhibitors of kinases located upstream of AP-1 and with known natural product inhibitors of AP-1 (nordihydroguaiaretic acid and curcumin). The assay was able to identify other known AP-1 inhibitors and protein kinase C modulators, as well as a number of chemically diverse compounds with unknown mechanisms of action from natural products libraries. Application to natural product extracts identified hits from a range of taxonomic groups. Screening of synthetic compounds and natural products should identify novel AP-1 inhibitors that may be useful in the prevention and treatment of cancers.

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