Next Article in Journal
A Tropical Marine Microbial Natural Products Geobibliography as an Example of Desktop Exploration of Current Research Using Web Visualisation Tools
Previous Article in Journal
Anticancer Alkaloid Lamellarins Inhibit Protein Kinases
Mar. Drugs 2008, 6(4), 528-549; doi:10.3390/md20080027

Characterizing the Anti-HIV Activity of Papuamide A

, 2
 and 1,*
Received: 22 July 2008 / Revised: 8 September 2008 / Accepted: 2 October 2008 / Published: 8 October 2008
View Full-Text   |   Download PDF [540 KB, uploaded 24 February 2015]   |   Browse Figures
Abstract: Papuamide A is representative of a class of marine derived cyclic depsipeptides, reported to have cytoprotective activity against HIV-1 in vitro. We show here that papuamide A acts as an entry inhibitor, preventing human immunodeficiency virus infection of host cells and that this inhibition is not specific to R5 or X4 tropic virus. This inhibition of viral entry was determined to not be due to papuamide A binding to CD4 or HIV gp120, the two proteins involved in the cell-virus recognition and binding. Furthermore, papuamide A was able to inhibit HIV pseudotype viruses expressing envelope glycoproteins from vesicular stomatitis virus or amphotropic murine leukemia virus indicating the mechanism of viral entry inhibition is not HIV-1 envelope glycoprotein specific. Time delayed addition studies with the pseudotyped viruses show that papuamide A inhibits viral infection only at the initial stage of the viral life cycle. Additionally, pretreatment studies revealed that the virus, and not the cell, is the target of papuamide A’s action. Together, these results suggest a direct virucidal mechanism of HIV-1 inhibition by papuamide A. We also demonstrate here that the other papuamides (B-D) are able to inhibit viral entry indicating that the free amino moiety of 2,3-diaminobutanoic acid residue is not required for the virucidal activity.
Keywords: HIV; papuamide A; cyclic depsipeptide; entry inhibitor; marine metabolite HIV; papuamide A; cyclic depsipeptide; entry inhibitor; marine metabolite
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |

MDPI and ACS Style

Andjelic, C.D.; Planelles, V.; Barrows, L.R. Characterizing the Anti-HIV Activity of Papuamide A. Mar. Drugs 2008, 6, 528-549.

AMA Style

Andjelic CD, Planelles V, Barrows LR. Characterizing the Anti-HIV Activity of Papuamide A. Marine Drugs. 2008; 6(4):528-549.

Chicago/Turabian Style

Andjelic, Cynthia D.; Planelles, Vicente; Barrows, Louis R. 2008. "Characterizing the Anti-HIV Activity of Papuamide A." Mar. Drugs 6, no. 4: 528-549.

Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert