Of 30 Indonesian plant extracts tested for their human immunodeficiency virus type-1 (HIV-1) inhibitory activities, six were shown to be effective by assays using HIV-1-infected MT-4 cells: a methanol extract of mahoni (bark of Swietenia rnahagoni) and water extracts of benalu teh (stems and branches of Loranthus parasiticus), kiules (fruit of Helicteres isora), supratul (fruits of Sindoru surnalranu), sambiloto (leaves of Andrographis paniculata) and temu ireng (rhizoma of Curcurna aeruginosa). Their EDs values ranged from 4.2 to 175 pg1mL. The samples also suppressed the formation of syncytia in co-cultures of MOLT-4 and MOLT41HIV-1 cells. The most potent inhibitor was a methanol extract of mahoni, which also showed a significant inhibition of HIV-1 protease.
An antimicrobial peptide, tachyplesin I, isolated from hemocytes of the Japanese horseshoe crab (Tachypleus tridentatus) was examined for its inhibitory effects on human immunodeficiency virus (HIV) infection in vitro. At a concentration of 7.5 μg/ml, tachyplesin I suppressed the development of cytopathic effects (CPE) by more than 70% in MT-4 cells infected with HIV (lymphadenopathy-associated virus). This inhibitory effect was observed only when the drug was added during the adsorption period of the virus to the cells. In cocultures of MOLT-4 and persistently HIV-infected cells (MOLT-4/HIV), tachyplesin I at the same concentration completely inhibited multinucleated giant cell formation. Infectivity of HIV was reduced by 10––2.5 in medium free from fetal calf serum containing tachyplesin I at a concentration of 200 μg/ml. Tachyplesin I did not show any inhibitory effect on reverse transcriptase activity of HIV at concentrations of 9–80 μg/ml at which tachyplesin I inhibited HIV infection. These results suggest that the anti-HIV action of tachyplesin I was due to the inhibition of virus adsorption.
The polyether-macrolide antibiotic, boromycin, was isolated as a potent anti-human immunodeficiency virus (HIV) antibiotic from a fermentation broth of Streptomyces sp. A-3376. Boromycin was found to strongly inhibit the replication of the clinically isolated HIV-1 strain as well as the cultured strain in in vitro laboratory experiments. The mechanism for the anti-HIV activity of boromycin is suggested to involve blocking the later stage of HIV infection, and probably the maturity step for replication of the HIV molecule.
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