Inhibitory activity on HIV‐1 reverse transcriptase and integrase of a carmalol derivative from a brown Alga, Ishige okamurae

Abstract

The bioassay-directed isolation of a marine brown alga, Ishige okamurae, afforded a carmalol derivative, diphlorethohydroxycarmalol. This compound exhibited inhibitory effects on HIV-1 reverse transcriptase and integrase with IC(50) values of 9.1 microM and 25.2 microM, respectively. However, diphlorethohydroxycarmalol did not show an inhibitory activity against HIV-1 protease. Moreover, diphlorethohydroxycarmalol nonaacetate obtained by acetylation and fucosterol failed to show any inhibitory activity against these viral enzymes.

Synergistic antivirus effect of combined administration of Combivir with Angelica polysaccharide sulfate

“…The primary mode of action for lamivudine and zidovudine is the termination of the DNA chain after incorporation into the viral genome. While as for sulfated polysaccharides, several researches reveal that its antivirus mechanism was mainly due to: (1) block viral entry into host cells by interfering with the attachment of virus to the cell-surface receptors [15,16]; (2) inhibit reverse transcriptase [17]; and (3) improve the immune function [18].…”

Potential Anti-HIV Agents from Marine Resources: An Overview

“…[25] showed that Ishige okamurae Yendo-derived diphlorethohydroxycarmalol also has an inhibitory effect on HIV-1. This compound exhibited inhibitory effects on the HIV-1 reverse transcriptase and integrase with IC 50 values of 9.1 μM and 25.2 μM, respectively.…”

Phlorotannins from Ishige okamurae and their acetyl- and butyrylcholinesterase inhibitory effects

“…It is found throughout the upper and middle intertidal zones on rough open coast in Korea (Cho et al, 2008). I. okamurae and its phlorotannins have been reported to have many useful bioactivities including anticoagulative, antioxidant, and HIV-1 reverse transcriptase and bacterial phospholipase A 2 inhibitory activities (Heo et al, 2008;Zou et al, 2008;Ahn et al, 2006;Cho et al, 2008).…”