Parasites

B. gibsoni

Preparation method

The solubility of this compound in DMSO is >17.03mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

0 ~ 3.2 μM

Applications

The ΣFICs against WT B. gibsoni were 0.93, 0.82, 0.83 and 0.96 for Atovaquone and Proguanil at a ratio of 4:1, 3:2, 2:3 and 1:4, respectively. The ΣFICs against Atovaquone-resistant B. gibsoni were 0.88, 0.60, 0.77 and 0.88 at each ratio. The results implied that Atovaquone synergized the effects of Proguanil on WT and Atovaquone-resistant B. gibsoni.

Animal models

Dogs infected with B. gibsoni

Dosage form

17 ~ 25 mg/kg; p.o.

Applications

In B. gibsoni-infected dogs, the combination of Atovaquone and Proguanil alleviated parasitemia. However, all dogs showed relapse of parasitic infection. In addition, some side effects were also observed. Self-limiting vomiting occurred in 2 dogs and hyperphosphatasia occurred in another dog. Mild increases in the alanine aminotransferase levels were confirmed in 2 dogs.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Atovaquone is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.Target: AntiparasiticAtovaquone (atavaquone) is a chemical compound that belongs to the class of naphthalenes. Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone, with antipneumocystic activity [1]. Atovaquone is an anti-protozoal mitochondrial electron transport inhibitor; Antimalarial; Antipneumocystic, and has also been used to treat toxoplasmosis. It acts by inhibiting the cytochrome bc(1) complex via interactions with the Rieske iron-sulfur protein and cytochrome b in the ubiquinol oxidation pocket [2]. Atovaquone is a unique naphthoquinone with broad-spectrum antiprotozoal activity. It is effective for the treatment and prevention of Pneumocystis carinii pneumonia (PCP), it is effective in combination with proguanil for the treatment and prevention of malaria, and it is effective in combination with azithromycin for the treatment of babesiosis [3].

References:
[1]. Looareesuwan, S., et al., Clinical studies of atovaquone, alone or in combination with other antimalarial drugs, for treatment of acute uncomplicated malaria in Thailand. Am J Trop Med Hyg, 1996. 54(1): p. 62-6.
[2]. Kessl, J.J., et al., Molecular basis for atovaquone binding to the cytochrome bc1 complex. J Biol Chem, 2003. 278(33): p. 31312-8.
[3]. Baggish, A.L. and D.R. Hill, Antiparasitic agent atovaquone. Antimicrobial agents and chemotherapy, 2002. 46(5): p. 1163-1173.