Isolation and Characterization of New Anti-HIV and Cytotoxic Leads from Plants, Marine, and Microbial Organisms

Abstract

New cytotoxic isomalabaricane triterpenes have been isolated from a sponge Stelletta sp. (1-7); anti-HIV pterocarpans (8 and 9) and isoflavanoids (12-16 and 18) were elucidated from two tropical plants in the genus Erythrina; and anti-HIV enniatins (20 and 22-23) were characterized from fungi in the genera Fusarium and Alternaria. The enniatins were evaluated for in vivo anti-HIV activity in the hollow fiber assay.

Effect of acute treatment with a water-alcohol extract of Erythrina mulungu on anxiety-related responses in rats

“…Erythrina species are known to produce alkaloids, flavonoids and terpenes (1,2). Pharmacological assays performed with the alkaloids of Erythrina americana have shown anticonvulsant, hypnotic and analgesic effects (3).…”

“…Pharmacological assays performed with the alkaloids of Erythrina americana have shown anticonvulsant, hypnotic and analgesic effects (3). The species Erythrina glauca and Erythrina lysistemon have been reported to possess antiviral and antibacterial activity (1,4). Furthermore, analgesic and anti-inflammatory effects were observed for an aqueous extract of the stem bark of Erythrina senegalensis (5).…”

Beauvericin and enniatins H, I and MK1688 are new potent inhibitors of human immunodeficiency virus type-1 integrase

“…6,16,17 Mixtures of ENs B, EN B 1 and A previously showed anti-HIV-1 activity by protecting human lymphoblastoid cells against HIV-1-induced cell death with an in vitro therapeutic index of approximately 200. 5 Our group has copurified BEA, and ENs H, I and MK1688 from culture broth of F. oxysporum, and the production of these cyclic hexadepsipeptides were further characterized during fermentation (Figure 2). The growth and production of BEA and ENs H, I and MK1688 by F. oxysporum strain KFCC 11363P in FDM are shown in Figure 2.…”

“…4 Various classes of the compounds, including natural products and synthetic compounds, have been suggested. Enniatins (ENs) B, B 1 and A 1 produced by Fusarium species reportedly exhibit anti-HIV-1 activity, 5 but the mechanism for EN inhibition of viral replication remains ambiguous. Our group has recently reported the successful copurification of beauvericin (BEA) and ENs H, I, and MK1688 from culture broth of Fusarium oxysporum isolated from soil samples collected in Korea.…”

“…Our group has recently reported the successful copurification of beauvericin (BEA) and ENs H, I, and MK1688 from culture broth of Fusarium oxysporum isolated from soil samples collected in Korea. [6][7][8] As ENs B, B 1 and A 1 have been shown to protect human lymphoblastoid cells in HIV-1-induced cell death, 5 we decided to test the antiviral activity of BEA and these ENs, H, I and MK1688, by studying whether or not they inhibit viral enzymes such as reverse transcriptase and integrase in vitro. In our assay, BEA, EN I and EN MK1688 were found to strongly inhibit the 3¢-processing activity of HIV-1 integrase.…”