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Psicofuranine

Psicofuranine用途

Psicofuramine 是一种核苷抗生素,具有抑制黄嘌呤 5'-磷酸氨化酶的作用。Psicofuramine 还可以特异性抑制 GMP 合酶,并中断寄生虫的生长。Psicofuramine 对恶性疟原虫的生长具有剂量依赖性抑制作用。

Psicofuranine名称

[ CAS 号 ]:
1874-54-0

[ 中文名 ]:
二十烷呋喃酮

[ 英文名 ]:
Psicofuranine

[英文别名 ]:

Psicofuranine生物活性

[ 描述 ]:

Psicofuramine 是一种核苷抗生素,具有抑制黄嘌呤 5'-磷酸氨化酶的作用。Psicofuramine 还可以特异性抑制 GMP 合酶,并中断寄生虫的生长。Psicofuramine 对恶性疟原虫的生长具有剂量依赖性抑制作用。

[ 相关类别 ]:

研究领域 >> 感染
信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Xanthosine 5'-phosphate aminase[2] P. falciparum[1] E. coli[1]


[体外研究]

Psicofuranine特异性地抑制细菌GMP合酶,通过分离编码GMP合酶基因突变的抗Psicofuranine大肠杆菌突变体和抑制细菌生长证明了这一点。Psicofuranine对恶性疟原虫生长具有剂量依赖性抑制作用,IC50为0.3mm。Psicofuranine的抑制浓度与大肠杆菌相似[1]。

[参考文献]

[1]. cConkey GA. Plasmodium falciparum: isolation and characterisation of a gene encoding protozoan GMP synthase. Exp Parasitol. 2000 Jan;94(1):23-32.

[2]. UDAKA S, et al. INHIBITION OF PARENTAL AND MUTANT XANTHOSINE 5'-PHOSPHATE AMINASES BY PSICOFURANINE. J Biol Chem. 1963 Aug;238:2797-803.

Psicofuranine物理化学性质

[ 密度 ]:
2.02g/cm3

[ 沸点 ]:
720.1ºC at 760 mmHg

[ 分子式 ]:
C11H15N5O5

[ 分子量 ]:
297.26700

[ 闪点 ]:
389.3ºC

[ 精确质量 ]:
297.10700

[ PSA ]:
159.77000

[ 蒸汽压 ]:
9.24E-22mmHg at 25°C

[ 折射率 ]:
1.855

[ 储存条件 ]:
-20°C,密闭,干燥

Psicofuranine毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AU7100000
CHEMICAL NAME :
Adenine, 9-beta-D-psicofuranosyl-
CAS REGISTRY NUMBER :
1874-54-0
BEILSTEIN REFERENCE NO. :
0095142
LAST UPDATED :
199612
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C11-H15-N5-O5
MOLECULAR WEIGHT :
297.31
WISWESSER LINE NOTATION :
T56 BN DN FN HNJ IZ D- BT5OTJ B1Q CQ DQ E1Q

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 :
10 gm/kg
TOXIC EFFECTS :
Tumorigenic - active as anti-cancer agent
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 9,675,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
13 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85ERAY "Antibiotics: Origin, Nature, and Properties," Korzyoski, T., et al., eds., Washington, DC, American Soc. for Microbiology, 1978 Volume(issue)/page/year: 1,842,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1695 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
UPJOH* "Compounds Available for Fundamental Research, Volume II-6, Antibiotics, A Program of Upjohn Company Research Laboratory." (Kalamazoo, MI 49001) Volume(issue)/page/year: 2(6),-,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85ERAY "Antibiotics: Origin, Nature, and Properties," Korzyoski, T., et al., eds., Washington, DC, American Soc. for Microbiology, 1978 Volume(issue)/page/year: 1,842,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
UPJOH* "Compounds Available for Fundamental Research, Volume II-6, Antibiotics, A Program of Upjohn Company Research Laboratory." (Kalamazoo, MI 49001) Volume(issue)/page/year: 2(6),-,1971 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
9800 mg/kg/28D-I
TOXIC EFFECTS :
Liver - other changes Blood - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 9,675,1959 *** REVIEWS *** TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,159,1973

Psicofuranine合成路线

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