NDLI: In Vitro Antimalarial Activity of Novel Semisynthetic Nocathiacin I Antibiotics

Content Provider	PubMed Central
Author	Sharma, Indu Sullivan, Margery Mccutchan, Thomas F.
Copyright Year	2015
Abstract	Presently, the arsenal of antimalarial drugs is limited and needs to be replenished. We evaluated the potential antimalarial activity of two water-soluble derivatives of nocathiacin (BMS461996 and BMS411886) against the asexual blood stages of Plasmodium falciparum. Nocathiacins are a thiazolyl peptide group of antibiotics, are structurally related to thiostrepton, have potent activity against a wide spectrum of multidrug-resistant Gram-positive bacteria, and inhibit protein synthesis. The in vitro growth inhibition assay was done using three laboratory strains of P. falciparum displaying various levels of chloroquine (CQ) susceptibility. Our results indicate that BMS461996 has potent antimalarial activity and inhibits parasite growth with mean 50% inhibitory concentrations (IC50s) of 51.55 nM for P. falciparum 3D7 (CQ susceptible), 85.67 nM for P. falciparum Dd2 (accelerated resistance to multiple drugs [ARMD]), and 99.44 nM for P. falciparum K1 (resistant to CQ, pyrimethamine, and sulfadoxine). Similar results at approximately 7-fold higher IC50s were obtained with BMS411886 than with BMS461996. We also tested the effect of BMS491996 on gametocytes; our results show that at a 20-fold excess of the mean IC50, gametocytes were deformed with a pyknotic nucleus and growth of stage I to IV gametocytes was arrested. This preliminary study shows a significant potential for nocathiacin analogues to be developed as antimalarial drug candidates and to warrant further investigation.
Related Links	http://dx.doi.org/10.1128/aac.04294-14
Ending Page	3179
Page Count	6
Starting Page	3174
File Format	PDF
ISSN	00664804
e-ISSN	10986596
Journal	Antimicrobial Agents and Chemotherapy
Issue Number	6
Volume Number	59
Language	English
Publisher	American Society for Microbiology
Publisher Date	2015-06-01
Access Restriction	Open
Rights Holder	American Society for Microbiology
Subject Keyword	Pharmacology (medical) Pharmacology Infectious Diseases Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Infectious Diseases Pharmacology Pharmacology (medical)

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Interactions of DB75, a Novel Antimalarial Agent, with Other Antimalarial Drugs In Vitro▿

Desbutyl-Benflumetol, a Novel Antimalarial Compound: In Vitro Activity in Fresh Isolates of Plasmodium falciparum from Thailand

In vitro activity of BRL 36650, a new semisynthetic penicillin.

In vitro activity of the semisynthetic glycopeptide amide MDL 63,246.

In vitro antibacterial activity of LY333328, a new semisynthetic glycopeptide.

In Vitro Comparison of Netilmicin, a Semisynthetic Derivative of Sisomicin, and Four Other Aminoglycoside Antibiotics

In Vitro Antimalarial Activity and Drug Interactions of Fenofibric Acid

In Vitro and In Vivo Activities of Novel, Semisynthetic Thiopeptide Inhibitors of Bacterial Elongation Factor Tu ▿

In vitro antibacterial activity of E-0702, a new semisynthetic cephalosporin.

In Vitro Antimalarial Activity of Novel Semisynthetic Nocathiacin I Antibiotics

Similar Documents

Interactions of DB75, a Novel Antimalarial Agent, with Other Antimalarial Drugs In Vitro▿

Desbutyl-Benflumetol, a Novel Antimalarial Compound: In Vitro Activity in Fresh Isolates of Plasmodium falciparum from Thailand

In vitro activity of BRL 36650, a new semisynthetic penicillin.

In vitro activity of the semisynthetic glycopeptide amide MDL 63,246.

In vitro antibacterial activity of LY333328, a new semisynthetic glycopeptide.

In Vitro Comparison of Netilmicin, a Semisynthetic Derivative of Sisomicin, and Four Other Aminoglycoside Antibiotics

In Vitro Antimalarial Activity and Drug Interactions of Fenofibric Acid

In Vitro and In Vivo Activities of Novel, Semisynthetic Thiopeptide Inhibitors of Bacterial Elongation Factor Tu ▿

In vitro antibacterial activity of E-0702, a new semisynthetic cephalosporin.

In Vitro Antimalarial Activity of Novel Semisynthetic Nocathiacin I Antibiotics