Disease relevance of BW 720C

• In addition, 4b easily released the parent drug in human skin homogenate and, therefore, is a promising prodrug candidate to deliver buparvaquone through the skin for the treatment of cutaneous leishmaniasis [1].
• Water-soluble phosphate prodrugs of buparvaquone (1), containing a hydroxynaphthoquinone structure, were synthesized and evaluated in vitro for improved topical and oral drug delivery against cutaneous and visceral leishmaniasis [1].
• As a result of a theileriosis problem at about day 60 after inoculation in 2 cattle given 10(-2) dilution of stabilate and buparvaquone treatment on day 0, an additional 5 cattle were given 10(-2) dilution of stabilate and developed a good immunity after buparaquone treatment [2].
• Groups of 3 cattle infected with 1 ml inocula at 10(0), 10(-1) and 10(-2) dilutions were treated with 2.5 mg/kg body weight of buparvaquone on day 0 and similar groups were left untreated to act as controls [2].
• When administered at the rate of 5 mg/kg of body weight, IV, 4 times at 48-hour intervals, buparvaquone prompted rapid abatement of parasitemia [3].

High impact information on BW 720C

• A significant correlation was obtained between the rapid inhibition of luminescence with parasite proliferation and the dissipation of changes in mitochondrial membrane potential (DeltaPsi(m)) produced by buparvaquone or plumbagin, two leishmanicidal inhibitors of oxidative phosphorylation [4].
• These gammadelta T cells were found to respond to TpL infected with several different parasite stocks and failed to recognize TpL after elimination of the parasite by the theilericidal drug BW 720C [5].
• In a BALB/c mouse model, treatment with 100 mg/kg/day for five days with buparvaquone, 250C80 and 566C80 (atovaquone) reduced liver amastigote numbers by 60%, 22% and 30.5%, respectively [6].
• The hydroxynaphthoquinones, buparvaquone, 250C80 and 56W82, showed high activity in vitro against Leishmania donovani amastigotes in mouse peritoneal macrophages, with ED50 values of 0.05, 2.95 and 13.82 microM, respectively [6].
• In this study we found that elimination of the parasite by buparvaquone induces apoptosis of transformed B and CD8(+) T-lymphocytes [7].

Chemical compound and disease context of BW 720C

• Treatment of East Coast fever: a comparison of parvaquone and buparvaquone [8].
• It is suggested that the most economical way to control theileriosis in India would be to immunise calves by infection with sporozoite stabilate and simultaneous treatment with tetracycline, and to reserve buparvaquone for the treatment of clinical cases, in cattle of all ages [9].

Biological context of BW 720C

• The infection rate in the adult ticks, fed as nymphs during the febrile reaction, was high (62%), dropped to zero for 1 day in tick batches that engorged after treatment with Butalex and increased to 30% 2 days later and 38% of the ticks acquired the infection after feeding as nymphs during a carrier state piroplasm parasitaemia of less than 0.1% [10].
• The rectal body temperature of 90.5% of buparvaquone-treated cattle dropped to normal values (37.5-39.5 degrees C) by day 7 of treatment, and by day 15 of treatment 96.8% of treated cattle showed normal values [11].
• Parvaquone and buparvaquone: HPLC analysis and comparative pharmacokinetics in cattle [12].
• The effect of buparvaquone treatment on the levels of some antioxidant vitamins, lipid peroxidation and glutathione peroxidase in cattle with theileriosis [13].

Anatomical context of BW 720C

• Immunization of cattle using varying infective doses of Theileria parva lawrencei sporozoites derived from an African buffalo (Syncerus caffer) and treatment with buparvaquone [2].
• Although buparvaquone-oxime (1a) has been shown to undergo a cytochrome P450-catalysed oxidation in liver microsomes to the parent buparvaquone and behave as a novel bioreversible prodrug, its usefulness is limited in oral drug delivery due to its poor aqueous solubility, like buparvaquone itself [14].
• The in vitro data showed a significant decrease in the incorporation of 3H-hypoxanthine by infected red blood cells treated with buparvaquone when compared to that seen with imidocarb and chloroquine treatment [15].
• The influence of Buparvaquone on the morphology, proliferation, and stimulation with T and B cell mitogens of Theileria annulata-infected cells was studied [16].
• In addition, the stimulatory capacity of the infected cells before and after treatment with Buparvaquone or cyclosporin A (CsA) was also examined and compared to that of ConA-stimulated bovine peripheral blood cells (PBL) [16].

Associations of BW 720C with other chemical compounds

• 4. The prodrugs 2b, 3b and 5b rapidly released (t1/2 = 7 min) the corresponding oximes of buparvaquone (1a and 1b), and prodrug 4b at a moderate rate (t1/2 = 22.5 min) in alkaline phosphatase solution in vitro [14].
• Elimination of Theileria buffeli infections from cattle by concurrent treatment with buparvaquone and primaquine phosphate [17].

Gene context of BW 720C

• Therefore, it is possible that buparvaquone interferes with the expression of the beta chain of the IL-2R [18].
• Effect of buparvaquone on the expression of interleukin 2 receptors in Theileria annulata-infected cells [18].

Analytical, diagnostic and therapeutic context of BW 720C

• The aerosolization characteristics of two buparvaquone nanosuspensions were determined with commercial jet and ultrasonic nebulizer devices [19].
• Chemotherapy of Theileria annulata infection with buparvaquone [20].
• Chemoprophylaxis of Theileria annulata and Theileria parva infections of calves with buparvaquone [21].
• Furthermore, Buparvaquone but not CsA inhibits the generation of mixed lymphocyte reaction (MLR) [16].

References