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Screening for Natural Inhibitors of Topoisomerases I from Rhamnus davurica by Affinity Ultrafiltration and High-Performance Liquid Chromatography–Mass Spectrometry

Overview of attention for article published in Frontiers in Plant Science, September 2017
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Title
Screening for Natural Inhibitors of Topoisomerases I from Rhamnus davurica by Affinity Ultrafiltration and High-Performance Liquid Chromatography–Mass Spectrometry
Published in
Frontiers in Plant Science, September 2017
DOI 10.3389/fpls.2017.01521
Pubmed ID
Authors

Guilin Chen, Mingquan Guo

Abstract

Topoisomerase I (Topo I) catalyzes topological interconversion of duplex DNA during DNA replication and transcription, and has been deemed as important antineoplastic targets. In this study, the fraction R.d-60 from ethyl acetate extracts of Rhamnus davurica showed higher inhibitory rates against SGC-7901 and HT-29 compared with the R.d-30 fraction in vitro. However, the specific active components of R.d-60 fraction remain elusive. To this end, a method based on bio-affinity ultrafiltration and high performance liquid chromatography/electrospray mass spectrometry (HPLC- ESI-MS/MS) was developed to rapidly screen and identify the Topo I inhibitors in this fraction. The enrichment factors (EFs) were calculated to evaluate the binding affinities between the bioactive constituents and Topo I. As a result, eight ligands were identified and six of which with higher EFs showed more potential antitumor activity. Furthermore, antiproliferative assays in vitro (IC50 values) with two representative candidates (apigenin, quercetin) against SGC-7901, HT-29 and Hep G2 cells were conducted and further validated. Finally, the structure-activity relationships revealed that flavones contain a C2-C3 double bond of C ring exhibited higher bio-affinities to Topo I than those without it. This integrated method combining Topo I ultrafiltration with HPLC-MS/MS proved to be very efficient in rapid screening and identification of potential Topo I inhibitors from the complex extracts of medicinal plants, and could be further explored as a valuable high-throughput screening platform in the early drug discovery stage.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 14 100%

Demographic breakdown

Readers by professional status Count As %
Student > Bachelor 3 21%
Student > Doctoral Student 1 7%
Professor 1 7%
Student > Ph. D. Student 1 7%
Researcher 1 7%
Other 1 7%
Unknown 6 43%
Readers by discipline Count As %
Chemistry 3 21%
Environmental Science 1 7%
Biochemistry, Genetics and Molecular Biology 1 7%
Pharmacology, Toxicology and Pharmaceutical Science 1 7%
Economics, Econometrics and Finance 1 7%
Other 1 7%
Unknown 6 43%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 07 October 2017.
All research outputs
#18,572,036
of 23,002,898 outputs
Outputs from Frontiers in Plant Science
#13,963
of 20,497 outputs
Outputs of similar age
#242,414
of 316,299 outputs
Outputs of similar age from Frontiers in Plant Science
#360
of 485 outputs
Altmetric has tracked 23,002,898 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 20,497 research outputs from this source. They receive a mean Attention Score of 4.0. This one is in the 20th percentile – i.e., 20% of its peers scored the same or lower than it.
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We're also able to compare this research output to 485 others from the same source and published within six weeks on either side of this one. This one is in the 14th percentile – i.e., 14% of its contemporaries scored the same or lower than it.