Evidence map›Paper›PMID 25982031›Full record

ArticleExperimental parasitology2015

A non-cytotoxic N-dehydroabietylamine derivative with potent antimalarial activity.

Maralinganadoddi P Sadashiva, Raghavendra Gowda, Xianzhu Wu, Gajanan S Inamdar, Omer F Kuzu, Kanchugarakoppal S Rangappa, Gavin P Robertson, D Channe Gowda

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Experimental parasitology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Nanoliposomal delivery of cytosolic phospholipase ANanomedicine : nanotechnology, biology, and medicine · 2018
    Article
  4. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Maralinganadoddi P SadashivaDepartment of Biochemistry and Molecular Biology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA; Department of Chemistry, University of Mysore, Manasagangothri, Mysore, 570 006, India. Electronic address: mpsadashiva@gmail.com.
Raghavendra GowdaDepartment of Pharmacology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
Xianzhu WuDepartment of Biochemistry and Molecular Biology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
Gajanan S InamdarDepartment of Pharmacology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
Omer F KuzuDepartment of Pharmacology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
Kanchugarakoppal S RangappaDepartment of Chemistry, University of Mysore, Manasagangothri, Mysore, 570 006, India.
Gavin P RobertsonDepartment of Pharmacology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
D Channe GowdaDepartment of Biochemistry and Molecular Biology, The Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA. Electronic address: gowda@psu.edu.

Funding

Innate Immune Responses to Malaria ParasitesR01AI041139 · NIAID · PENNSYLVANIA STATE UNIV HERSHEY MED CTR · PI GOWDA, CHANNE D · 1998 to 2017
$5.8M
Therapeutic targeting of malarial placental cytoadherenceR01AI104844 · NIAID · PENNSYLVANIA STATE UNIV HERSHEY MED CTR · PI GOWDA, CHANNE D · 2015 to 2019
$2.4M
Akt3 Signaling as a Therapeutic TargetR01CA127892 · NCI · PENNSYLVANIA STATE UNIV HERSHEY MED CTR · PI ROBERTSON, GAVIN P. · 2008 to 2012
$1.5M
NCI NIH HHS CA127892-01ANCI NIH HHS R01 CA127892NIAID NIH HHS AI 41139NIAID NIH HHS R01 AI041139
6 · The paper itself

Abstract

Malaria caused by the Plasmodium parasites continues to be an enormous global health problem owing to wide spread drug resistance of parasites to many of the available antimalarial drugs. Therefore, development of new classes of antimalarial agents is essential to effectively treat malaria. In this study, the efficacy of naturally occurring diterpenoids, dehydroabietylamine and abietic acid, and their synthetic derivatives was assessed for antimalarial activity. Dehydroabietylamine and its N-trifluoroacetyl, N-tribromoacetyl, N-benzoyl, and N-benzyl derivatives showed excellent activity against P. falciparum parasites with IC50 values of 0.36 to 2.6 µM. Interestingly, N-dehydroabietylbenzamide showed potent antimalarial activity (IC50 0.36), and negligible cytotoxicity (IC50 >100 µM) to mammalian cells; thus, this compound can be an important antimalarial drug. In contrast, abietic acid was only marginally effective, exhibiting an IC50 value of ~82 µM. Several carboxylic group-derivatives of abietic acid were moderately active with IC50 values of ~8.2 to ~13.3 µM. These results suggest that a detailed understanding of the structure-activity relationship of abietane diterpenoids might provide strategies to exploit this class of compounds for malaria treatment.

Indexed as

AbietanesAntimalarialsBenzamidesBenzothiazolesCell LineCell Line, TumorDiaminesDose-Response Relationship, DrugErythrocytesFibroblastsFluorescent DyesHumansInhibitory Concentration 50Organic ChemicalsPlasmodium falciparumQuinolinesAbietanesabietic acidAntimalarialsBenzamidesBenzothiazolesdehydroabietylamineDiaminesFluorescent DyesN-dehydroabietylbenzamideOrganic ChemicalsQuinolinesSYBR Green IAbietane diterpenoidsAbietic acid derivativesAntimalarial activityDehydroabietylamine derivatives

Identifiers

PMID25982031
PMCPMC4480188

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Registered trials

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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.