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布帕伐醌

布帕伐醌用途

Buparvaquone是一种与parvaquone和atovaquone有关的羟基萘醌类抗原虫药。

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布帕伐醌名称

[ CAS 号 ]:
88426-33-9

[ 中文名 ]:
布帕伐醌

[ 英文名 ]:
Buparvaquone

[中文别名 ]:

[英文别名 ]:

Butalex
UNII-0354RT7LG4
BW 720C
Buparvaquone
Buparvaquonum [Latin]
Buparvacuona [Spanish]
MFCD01712789

布帕伐醌生物活性

[ 描述 ]:

Buparvaquone是一种与parvaquone和atovaquone有关的羟基萘醌类抗原虫药。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[体外研究]

在4天的增殖试验中,buparvaquone有效抑制犬新孢子虫的速殖子复制(IC50 = 4.9 nM; IC100 = 100 nM)[1]。 Buparvaquone对L.(L.)infantum chagasi细胞内无鞭毛体具有显着选择性,IC50值为1.5μM。其他皮肤物种也对buparvaquone敏感,IC50值在1-4μM范围内[2]。

[体内研究]

用腹腔注射或强饲法治疗犬新型犬(100 mg/kg)对犬新孢子虫感染的小鼠,在腹腔注射治疗组的6只小鼠中有4只预防新孢子虫症状,在接受口服治疗的7只小鼠中有6只[ 1]。与未处理对照相比,buparvaquone的含水凝胶和油包水乳液均可显着降低皮肤寄生虫负荷和病变大小[3]。

[细胞实验]

为了研究入侵前宿主细胞的预处理是否对寄生虫增殖有任何影响，将6孔板中生长的融合HFF用1μMBuparvaquone在培养基中处理1小时或5小时，并将对照暴露于相应量的DMSO 。随后，除去含药物的培养基，用Hank's平衡盐溶液将单层细胞洗涤4次，并在5mL培养基中用Nc-Liv速殖子感染，不含任何药物或溶剂。 2天后，用细胞刮刀收集细胞，离心，再用PBS洗涤一次，然后将沉淀储存在-20℃，然后通过犬新孢子虫特异性实时PCR定量犬新孢子虫增殖，如下所述[1]。

[动物实验]

小鼠：在第0天，通过腹膜内（ip）注射新鲜纯化的犬新孢子虫速殖子感染所有小鼠。 48小时后，小鼠通过腹膜内注射100μl体积或通过管饲口服施用100μl，接受BPQ（100mg / kg）作为玉米油中的悬浮液。对照组仅ip或口服获得相应量的溶剂（参见表2）。治疗每天进行5次。如果没有另外说明，则每天两次检查小鼠的临床症状（皱褶外套，冷漠，后肢麻痹），直至感染后第21天（pi），此时将其安乐死[1]。

[参考文献]

[1]. Müller J, et al. Buparvaquone is active against Neospora caninum in vitro and in experimentally infected mice. Int J Parasitol Drugs Drug Resist. 2015 Feb 13;5(1):16-25.

[2]. Reimão JQ, et al. Effectiveness of liposomal buparvaquone in an experimental hamster model of Leishmania (L.) infantum chagasi. Exp Parasitol. 2012 Mar;130(3):195-9.

[3]. Garnier T, et al. In vivo studies on the antileishmanial activity of buparvaquone and its prodrugs. J Antimicrob Chemother. 2007 Oct;60(4):802-10.

[相关活性小分子]

布帕伐醌物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
460.7±45.0 °C at 760 mmHg

[ 熔点 ]:
178-184ºC

[ 分子式 ]:
C₂₁H₂₆O₃

[ 分子量 ]:
326.429

[ 闪点 ]:
246.5±25.2 °C

[ 精确质量 ]:
326.188202

[ PSA ]:
54.37000

[ LogP ]:
6.45

[ 外观性状 ]:
黄色结晶固体

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.574

[ 储存条件 ]:
Refrigerator

布帕伐醌毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QJ5766600

CHEMICAL NAME :: 1,4-Naphthalenedione, 2-((4-(1,1-dimethylethyl)cyclohexyl)methyl)-3-hydroxy -

CAS REGISTRY NUMBER :: 88426-33-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C21-H26-O3

MOLECULAR WEIGHT :: 326.47

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PARAAE Parasitology. (Cambridge University Press, The Edinburgh Bldg., Shaftesbury Rd., Cambridge, CB2 2RU, United Kingdom) V.1- 1908- Volume(issue)/page/year: 90,45,1985

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布帕伐醌安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
QJ5766600

布帕伐醌文献

Drug delivery systems for the topical treatment of cutaneous leishmaniasis.

Expert Opin. Drug Deliv. 9(9) , 1083-97, (2012)

The parenteral administration of pentavalent antimonials for the treatment of all forms of leishmaniasis, including cutaneous leishamniasis (CL), has several limitations. Therapy is long, requiring re...

In-vivo therapeutic efficacy trial with artemisinin derivative, buparvaquone and imidocarb dipropionate against Babesia equi infection in donkeys.

J. Vet. Med. Sci. 65(11) , 1171-7, (2003)

The therapeutic efficacy of imidocarb, artesunate, arteether, buparvaquone and arteether+buparvaquone combination was evaluated against Babesia equi of Indian origin in splenectomised donkeys with exp...

Design, synthesis and in vitro evaluation of novel water-soluble prodrugs of buparvaquone.

Eur. J. Pharm. Sci. 23(2) , 151-8, (2004)

Novel water-soluble phosphate prodrugs (2b-5b) of buparvaquone-oxime (1a) and buparvaquone-O-methyloxime (1b) were synthesized and evaluated in vitro as potential oral prodrugs against leishmaniasis. ...

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