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Mendeley readers
Attention Score in Context
| Title |
Identification of natural inhibitors of Entamoeba histolytica cysteine synthase from microbial secondary metabolites
|
|---|---|
| Published in |
Frontiers in Microbiology, September 2015
|
| DOI | 10.3389/fmicb.2015.00962 |
| Pubmed ID | |
| Authors |
Mihoko Mori, Ghulam Jeelani, Yui Masuda, Kazunari Sakai, Kumiko Tsukui, Danang Waluyo, Tarwadi, Yoshio Watanabe, Kenichi Nonaka, Atsuko Matsumoto, Satoshi Ōmura, Tomoyoshi Nozaki, Kazuro Shiomi |
| Abstract |
Amebiasis is a common worldwide diarrheal disease, caused by the protozoan parasite, Entamoeba histolytica. Metronidazole has been a drug of choice against amebiasis for decades despite its known side effects and low efficacy against asymptomatic cyst carriers. E. histolytica is also capable of surviving sub-therapeutic levels of metronidazole in vitro. Novel drugs with different mode of action are therefore urgently needed. The sulfur assimilatory de novo L-cysteine biosynthetic pathway is essential for various cellular activities, including the proliferation and anti-oxidative defense of E. histolytica. Since the pathway, consisting of two reactions catalyzed by serine acetyltransferase (SAT) and cysteine synthase (CS, O-acetylserine sulfhydrylase), does not exist in humans, it is a rational drug target against amebiasis. To discover inhibitors against the CS of E. histolytica (EhCS), the compounds of Kitasato Natural Products Library were screened against two recombinant CS isozymes: EhCS1 and EhCS3. Nine compounds inhibited EhCS1 and EhCS3 with IC50 values of 0.31-490 μM. Of those, seven compounds share a naphthoquinone moiety, indicating the structural importance of the moiety for binding to the active site of EhCS1 and EhCS3. We further screened >9,000 microbial broths for CS inhibition and purified two compounds, xanthofulvin and exophillic acid from fungal broths. Xanthofulvin inhibited EhCS1 and EhCS3. Exophillic acid showed high selectivity against EhCS1, but exhibited no inhibition against EhCS3. In vitro anti-amebic activity of the 11 EhCS inhibitors was also examined. Deacetylkinamycin C and nanaomycin A showed more potent amebicidal activity with IC50 values of 18 and 0.8 μM, respectively, in the cysteine deprived conditions. The differential sensitivity of trophozoites against deacetylkinamycin C in the presence or absence of L-cysteine in the medium and the IC50 values against EhCS suggest the amebicidal effect of deacetylkinamycin C is due to CS inhibition. |
Mendeley readers
The data shown below were compiled from readership statistics for 37 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 37 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 9 | 24% |
| Student > Bachelor | 5 | 14% |
| Researcher | 3 | 8% |
| Professor > Associate Professor | 3 | 8% |
| Professor | 2 | 5% |
| Other | 7 | 19% |
| Unknown | 8 | 22% |
| Readers by discipline | Count | As % |
|---|---|---|
| Agricultural and Biological Sciences | 10 | 27% |
| Biochemistry, Genetics and Molecular Biology | 8 | 22% |
| Pharmacology, Toxicology and Pharmaceutical Science | 4 | 11% |
| Social Sciences | 2 | 5% |
| Medicine and Dentistry | 2 | 5% |
| Other | 2 | 5% |
| Unknown | 9 | 24% |
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 11 October 2016.
All research outputs
#15,387,502
of 22,893,031 outputs
Outputs from Frontiers in Microbiology
#15,233
of 24,938 outputs
Outputs of similar age
#157,408
of 268,690 outputs
Outputs of similar age from Frontiers in Microbiology
#241
of 420 outputs
Altmetric has tracked 22,893,031 research outputs across all sources so far. This one is in the 22nd percentile – i.e., 22% of other outputs scored the same or lower than it.
So far Altmetric has tracked 24,938 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.3. This one is in the 30th percentile – i.e., 30% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 268,690 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 32nd percentile – i.e., 32% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 420 others from the same source and published within six weeks on either side of this one. This one is in the 36th percentile – i.e., 36% of its contemporaries scored the same or lower than it.