Buparvaquone是与parvaquone和atovaquone有关的一种羟基萘醌类抗原虫药。

Buparvaquone is a hydroxynaphthoquinone antiprotozoal drug related to atovaquone and parvaquone.

Buparvaquone is significantly selective against L. (L.) infantum chagasi intracellular amastigotes, with an IC50 value of 1.5 μM. In 4-day proliferation assays, buparvaquone efficiently inhibits N.?caninum tachyzoite replication(IC50=4.9?nM; IC100=100?nM). Other cutaneous species are also susceptible to buparvaquone, with IC50 values in the range 1-4 μM.

Both a hydrous gel and water-in-oil emulsion of buparvaquone significantly reduce cutaneous parasite burden and lesion size than the untreated control. Treatment of N. caninum infected mice with buparvaquone (100 mg/kg) either by intraperitoneal injection or gavage prevents neosporosis symptoms in 4 out of 6 mice in the intraperitoneally treated group, and in 6 out of 7 mice in the group receiving oral treatment.

To study whether pretreatment of host cells prior to invasion had any effect on parasite proliferation, confluent HFF grown in 6-well plates are treated with 1?μM buparvaquone in medium for 1?h or 5?h, and controls are exposed to the corresponding amounts of DMSO. Subsequently, the drug-containing medium is removed and monolayers are ished 4 times with Hank's Balanced Salt Solution, and are infected with Nc-Liv tachyzoites in 5?mL medium without any drug or solvent. After 2 days, cells are collected with a cell scraper, centrifuged, ished once more in PBS, and the pellet is stored at ?20?°C prior to quantification of N.?caninum proliferation by N.?caninum-specific real time PCR as outlined below.

Mice: On day 0, all mice are infected by intraperitoneal (i.p.) injection of freshly purified N.?caninum tachyzoites. After 48?h, mice receive BPQ (100?mg/kg) as suspension in corn oil either by i.p. injection of a volume of 100?μl or by oral application of 100?μl by gavage. The control groups obtained the corresponding amount of the solvent only, either i.p. or orally. The treatments are performed 5 times on a daily basis. If not indicated otherwise, mice are inspected twice daily for clinical signs (ruffled coat, apathy, hind limb paralysis) until day 21 post infection (p.i.), at which time they are euthanized.

88426-33-9

C21H26O3

326.436

布帕伐醌;Butalex;BW 720C

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years