GLQ223: an inhibitor of human immunodeficiency virus replication in acutely and chronically infected cells of lymphocyte and mononuclear phagocyte lineage.

Abstract

GLQ223 is a highly purified, formulated preparation of trichosanthin, a 26-kDa plant-derived ribosome-inactivating protein with potent inhibitory activity against human immunodeficiency virus (HIV) in vitro. The compound produced concentration-dependent inhibition of HIV replication in acutely infected cultures of T-lymphoblastoid cells (VB cell line). Treatment with GLQ223 selectively reduced levels of detectable viral proteins compared to total cellular protein synthesis and produced a selective decrease in levels of viral RNA relative to total cellular RNA in acutely infected cells. Substantial inhibition of viral replication was observed at concentrations of GLQ223 that showed little inhibition of parallel uninfected cultures. Selective anti-HIV activity was also observed in cultures of primary monocyte/macrophages chronically infected with HIV in vitro. When freshly drawn blood samples from HIV-infected patients were treated with a single 3-hr exposure to GLQ223. HIV replication was blocked for at least 5 days in subsequently cultured monocyte/macrophages, without further treatment. The anti-HIV activity of GLQ223 in both acutely and chronically infected cells and its activity in cells of both lymphoid and mononuclear phagocytic lineage make it an interesting candidate as a potential therapeutic agent in HIV infection and AIDS.

Influence of Intercrop Population and Applied Poultry Manure Rates on Component Crops Productivity Responses in a Snake Tomato/Celosia Cropping System

“…These natural antioxidants have been strongly associated with reduced risk of chronic diseases, and age-related functional decline in addition to other health benefits [4] [5]. The medicinal importance of the plant also includes uses as a therapeutic agent for AIDS [6], as a tonic and in curing coughs while the seeds are used as purgative, anthelmintic and in the treatment of syphilis [7].…”

Mapping the antigenic determinants and reducing the immunogenicity of trichosanthin by site-directed mutagenesis

“…In the late 1980s, TCS was the first RIP found to possess anti-HIV activity. It preferentially inhibited the replication of HIV-1 in both acutely infected T-lymphoblastoid cells and chronically infected macrophages in vitro [16]. Therefore, it is also a potential therapeutic agent for AIDS.…”

Trichosanthin Induces Leakage and Membrane Fusion of Liposome

“…Clinically, it is used in China to terminate early and midtrimester pregnancies (8) and to treat trophoblastic tumors (9). In the late 1980s, studies showed TCS to be a potential therapeutic agent against HIV infection (10,11). In the early 1990s, TCS was used in the treatment of patients with AIDS or AIDS-related complex in phase I and II studies (12 -15).…”