Anti-Aids Agents, 3. Inhibitory Effects of Colchicine Derivatives on HIV Replication in H9 Lymphocyte Cells

Abstract

A series of colchicine and isocolchicine derivatives were evaluated as inhibitors of HIV replication in H9 lymphocytes. Colchicine showed only very slight inhibition in the absence of toxicity, as measured by the therapeutic index (IC50/EC50). None of the derivatives inhibited HIV replication in the absence of toxicity.

Comparative Quantitative Structure−Activity Relationship Studies on Anti-HIV Drugs

“…Recently, Siddiqui et al 101b reported anti-HIV data for another series of aryl phosphoramidate (43b) 36). 102 For a series of cholchicines, anti-HIV data were reported by Tatematsue et al; 102 we observed that the ring substituents have a dominant electronic effect (eqs 49 and 50). Equation 49is for the potency of the compounds to inhibit the HIV-1 replication in H9 cells (IC 50 ) (Table 36a), and eq 50 is for their ability to protect the cells from the infection of HIV-1 replication (EC 50 ) (Table 36b).…”

“…(vi) IC 50 and EC 50 Activities of Cholchicines ( 44 ) against HIV Replication in H9 Lymphocytes (Table 36 ) . For a series of cholchicines, anti-HIV data were reported by Tatematsue et al; we observedthat the ring substituents have a dominant electronic effect (eqs 49 and 50).…”

Identification of ent-16β,17-Dihydroxykauran-19-oic Acid as an Anti-HIV Principle and Isolation of the New Diterpenoids Annosquamosins A and B from Annona squamosa

“…4 HIV Inhibition Assay. 15 The assay employed H9 lymphocytes (3.5 × 10 6 cells/mL) in the presence or absence of HIV-1 (IIIB strain, 0.01-0.1 TCID 50 /cell) for 1 h at 37 °C. Cells were washed thoroughly and resuspended at a final concentration of 2 × 10 5 cells/ mL in the presence or absence of compound.…”

Self-stabilized antisense oligodeoxynucleotide phosphorothioates: properties and anti-HIV activity

“…Oligonucleotides at various concentrations were added and the cells were cultured for three days. At the end of this time, supematants from infected cultures were collected and the levels of HIV-1 p24 expression were measured by a monoclonal antibody-based p24 antigen capture assay (17). The level of p24 expression was then compared with that of untreated infected cells.…”