Disease relevance of AIDS060352

• Treatment of hamsters infected with L. donovani with intraperitoneal administration of licochalcone A at a dose of 20 mg/kg of body weight per day for 6 consecutive days resulted in a > 96% reduction of parasite load in the liver and the spleen compared with values for untreated control animals [1].
• Licochalcone A showed effects against all gram-positive bacteria tested and especially was effective against all Bacillus spp. tested, with MICs of 2 to 3 micrograms/ml, but was not effective against gram-negative bacteria or eukaryotes at 50 micrograms/ml [2].
• These data clearly demonstrate that licochalcone A is a promising lead for the development of a new drug against leishmaniases [1].
• The vegetative cell growth of Bacillus subtilis was inhibited in a licochalcone A concentration-dependent manner and was completely prevented by 3 micrograms of licochalcone A/ml [2].
• Anti-tumour promoting action of licochalcone A was also observed in vivo for mouse skin papilloma initiated by dimethylbenz[a]anthracene (DMBA) and promoted by TPA [3].

High impact information on AIDS060352

• The antiparasitic compound licochalcone a is a potent echinocytogenic agent that modifies the erythrocyte membrane in the concentration range where antiplasmodial activity is observed [4].
• The well-known antiparasitic compound licochalcone A is a potent membrane-active agent that transforms normal erythrocytes into echinocytes in parallel with the inhibition of growth of Plasmodium falciparum cultures, the in vitro antiplasmodial effect apparently being an indirect effect on the host cell [4].
• The data show that licochalcone A inhibited the activity of fumarate reductase (FRD) in the permeabilized Leishmania major promastigote and in the parasite mitochondria, and it also inhibited solubilized FRD and a purified FRD from L. donovani [5].
• The IC(50) of licochalcone A for SDH and NDH in human peripheral blood mononuclear cells were at least 70 times higher than that for FRD [5].
• Electron microscopic studies showed that licochalcone A altered the ultrastructure of Leishmania major promastigote and amastigote mitochondria in a concentration-dependent manner without damaging the organelles of macrophages or the phagocytic function of these cells [6].

Chemical compound and disease context of AIDS060352

• Among the chemical constituents of the plant, glabridin and glabrene (components of Glycyrrhiza glabra), licochalcone A (G. inflata), licoricidin and licoisoflavone B (G. uralensis) exhibited inhibitory activity against the growth of Helicobacter pylori in vitro [7].

Biological context of AIDS060352

• Licochalcone A: an inducer of cell differentiation and cytotoxic agent from Pogostemon cablin [8].
• Parasite Mitochondria as a Target of Chemotherapy: Inhibitory Effect of Licochalcone A on the Plasmodium falciparum Respiratory Chain [9].

Anatomical context of AIDS060352

• Studies on the function of the parasite mitochondria showed that licochalcone A inhibited the respiration of the parasite by the parasites [6].
• Results of studies on the site of action of licochalcone A indicate that the target organelle appears to be the parasite mitochondria [10].
• At a concentration of 0.5 microgram/ml, licochalcone A markedly reduced the infection rate of human peripheral blood monocyte-derived macrophages and U937 cells with L. major promastigotes and exhibited a strong intracellular killing of the parasite [10].
• A competitive interaction of licochalcone A with the TPA-receptors in the cell membrane has been suggested [3].
• In this study, we examined the effect of licochalcone A on the production of chemical mediators such as prostaglandin (PG)E2 and cytokines by interleukin (IL)-1beta in human skin fibroblasts [11].

Associations of AIDS060352 with other chemical compounds

• Although licochalcone A inhibited the activities of succinate dehydrogenase (SDH), NADH dehydrogenase (NDH), and succinate- and NADH-cytochrome c reductases in the parasite mitochondria, the 50% inhibitory concentrations (IC(50)) of licochalcone A for these enzymes were at least 20 times higher than that for FRD [5].
• Licochalcone-A (LA) is one flavonoid extracted from licorice root with antiparasitic and anti-tumor activity, but the effect on the human estrogen receptor and mechanism of anti-tumor activity is unknown [12].

Gene context of AIDS060352

• However, licochalcone A (1 microM) had no effect on increased levels of cyclooxygenase (COX)-2 mRNA and protein in cells [11].

Analytical, diagnostic and therapeutic context of AIDS060352

• Oral administration of licochalcone A at concentrations of 5 to 150 mg/kg of body weight per day for 6 consecutive days resulted in > 65 and 85% reductions of L. donovani parasite loads in the liver and the spleen, respectively, compared with those of untreated control hamsters [1].
• The structure of the licochalcone A was established by mass and nuclear magnetic resonance spectroscopies and by synthesis, and its purity was verified by high-pressure liquid chromatography [10].
• Skin tolerance, efficacy, and quality of life of patients with red facial skin using a skin care regimen containing Licochalcone A [13].

References