Evidence map›Paper›PMID 31601218›Full record

ArticleMalaria journal2019

Enhanced uptake, high selective and microtubule disrupting activity of carbohydrate fused pyrano-pyranones derived from natural coumarins attributes to its anti-malarial potential.

Sonal Gupta, Juveria Khan, Priti Kumari, Chintam Narayana, R Ayana, Malabika Chakrabarti, Ram Sagar, Shailja Singh

Erratum issuedOpen access · goldAbstract read
In one paragraph

Article in Malaria journal, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.7field-weighted citation impact, top 34% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 16 citations in OpenAlex.

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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

8 authors at 3 institutions in 1 country.

Sonal GuptaSpecial Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi, 110067, India.
Juveria KhanSchool of Biotechnology, Jawaharlal Nehru University, New Delhi, 110067, India.
Priti KumariDepartment of Chemistry, Shiv Nadar University, NH-91 Dadri, GB Nagar, Greater Noida, UP, 201314, India.
Chintam NarayanaDepartment of Chemistry, Shiv Nadar University, NH-91 Dadri, GB Nagar, Greater Noida, UP, 201314, India.
R AyanaDepartment of Life Sciences, School of Natural Sciences, Shiv Nadar University, Greater Noida, India.
Malabika ChakrabartiSpecial Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi, 110067, India.
Ram SagarDepartment of Chemistry, Institute of Science, Banaras Hindu University, Varanasi, 221005, India. ram.sagar@bhu.ac.in.
Shailja SinghSpecial Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi, 110067, India. shailja.jnu@gmail.com.
Jawaharlal Nehru University · INShiv Nadar University · INBanaras Hindu University · IN

Funding

Department of Science and Technology, Ministry of Science and Technology P/569/2016-1/TDTScience and Engineering Research Board EMR/2016/005644
6 · The paper itself

Abstract

backgroundMalaria is one of the deadliest infectious diseases caused by protozoan parasite of Plasmodium spp. Increasing resistance to anti-malarials has become global threat in control of the disease and demands for novel anti-malarial interventions. Naturally-occurring coumarins, which belong to a class of benzo-α-pyrones, found in higher plants and some essential oils, exhibit therapeutic potential against various diseases. However, their limited uptake and non-specificity has restricted their wide spread use as potential drug candidates.

methodsTwo series of carbohydrate fused pyrano[3,2-c]pyranone carbohybrids which were synthesized by combination of 2-C-formyl galactal and 2-C-formyl glucal, with various freshly prepared 4-hydroxycoumarins were screened against Plasmodium falciparum. The anti-malarial activity of these carbohybrids was determined by growth inhibition assay on P. falciparum 3D7 strain using SYBR green based fluorescence assay. Haemolytic activity of carbohybrid 12, which showed maximal anti-malarial activity, was determined by haemocompatibility assay. The uptake of the carbohybrid 12 by parasitized erythrocytes was determined using confocal microscopy. Growth progression assays were performed to determine the stage specific effect of carbohybrid 12 treatment on Pf3D7. In silico studies were conducted to explore the mechanism of action of carbohybrid 12 on parasite microtubule dynamics. These findings were further validated by immunofluorescence assay and drug combination assay.

results2-C-formyl galactal fused pyrano[3,2-c]pyranone carbohybrid 12 exhibited maximum growth inhibitory potential against Plasmodium with IC

conclusionThese findings show carbohydrate group fusion to 4-hydroxycoumarin precursor resulted in pyrano-pyranones derivatives with better solubility, enhanced uptake and improved selectivity. This data confirms that, carbohydrate fused pyrano[3,2-c]pyranones carbohybrids are effective candidates for anti-malarial interventions against P. falciparum.

Indexed as

AntimalarialsComputer SimulationCoumarinsFluorescent Antibody TechniqueMicrotubulesPlasmodium falciparumAntimalarialsCoumarinsCarbohybridsCarbohydrate-fused pyranopyroneCoumarinsMalariaMicrotubulePlasmodium falciparum 3D7

Identifiers

PMID31601218
PMCPMC6788091
OpenAlexW4240611094

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.