阿昔洛韦钠

阿昔洛韦钠用途

阿昔洛韦钠是一种有效的口服抗病毒药物。阿昔洛韦钠具有抗疱疹活性,对HSV-1和HSV-2的IC50值分别为0.85μM和0.86μM。阿昔洛韦钠诱导细胞周期紊乱和凋亡。阿昔洛韦钠预防急性白血病诱导治疗期间的细菌感染[1][2][3][4]。

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阿昔洛韦钠名称

[ CAS 号 ]:
69657-51-8

[ 中文名 ]:
阿昔洛韦钠

[ 英文名 ]:
Aciclovir sodium

[中文别名 ]:

[英文别名 ]:

Aciclovir sodium

阿昔洛韦钠生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 抗感染 >> HSV

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

HSV-1:0.85 μM (IC50)

HSV-2:0.86 μM (IC50)

[体外研究]

阿昔洛韦钠(3-100µM；24-72小时；Jurkat、U937和K562白血病细胞)以剂量和时间依赖性降低细胞存活率[1]。阿昔洛韦钠(10-100µM；24-72小时；Jurkat细胞)阻断DNA合成,从而阻止细胞周期进入G2/M和S期,并以剂量依赖性方式增加亚G1亚二倍体峰[1]。阿昔洛韦钠(10-100µM；24-72小时；Jurkat细胞)通过激活caspase-3和存在核DNA碎片诱导凋亡[1]。细胞存活率测定[1]细胞系：Jurkat、U937和K562白血病细胞浓度：3、10、30和100µM孵育时间：24、48和72小时结果：细胞存活率呈剂量和时间依赖性降低。凋亡分析[1]细胞系：Jurkat细胞浓度：10和100µM孵育时间：24、48和72小时结果：caspase-3活性增加并切割核间体DNA。细胞周期分析[1]细胞系：Jurkat细胞浓度：10和100µM孵育时间：24、48和72小时结果：24和48小时后,细胞在S期呈剂量依赖性聚集。72小时后,亚G1亚二倍体峰呈剂量依赖增加。

[体内研究]

阿昔洛韦钠(20 mg/kg；p.o.；每日三次；持续10天；BALB/c小鼠)抑制皮肤损伤的发展,并导致DTH反应和抗体产生之间的分离[3]动物模型：感染HSV-1的特异性无病原体BALB/c小鼠(7周龄)[3]剂量：20 mg/千克给药：口服给药；每日三次；10天结果：抑制皮肤损伤的发展,导致DTH反应和抗体产生之间的分离。

[参考文献]

[1]. Benedetti S, et, al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity. Life Sci. 2018 Dec 15;215:80-85.

[2]. Suzuki M, et, al. Synergistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61.

[3]. Li Z, et, al. Acyclovir treatment of skin lesions results in immune deviation in mice infected cutaneously with herpes simplex virus. Antivir Chem Chemother. 1999 Sep;10(5):251-7.

[4]. Lönnqvist B, et, al. Oral acyclovir as prophylaxis for bacterial infections during induction therapy for acute leukaemia in adults. The Leukemia Group of Middle Sweden. Support Care Cancer. 1993 May;1(3):139-44.

阿昔洛韦钠物理化学性质

[ 沸点 ]:
613.1ºC at 760 mmHg

[ 分子式 ]:
C₈H₁₀N₅NaO₃

[ 分子量 ]:
247.18600

[ 精确质量 ]:
247.06800

[ PSA ]:
122.14000

[ LogP ]:
0.09990

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

阿昔洛韦钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UP0791500

CHEMICAL NAME :: 6H-Purin-6-one, 1,9-dihydro-2-amino-9-((2-hydroxyethoxy)methyl)-, monosodium salt

CAS REGISTRY NUMBER :: 69657-51-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C8-H10-N5-O3.Na

MOLECULAR WEIGHT :: 247.22

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 107 mg/kg/5D-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 248 mg/kg/80H-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >20 gm/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1210 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 650 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >600 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 999 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 405 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1550 mg/kg/31D-I

TOXIC EFFECTS :: Gastrointestinal - other changes Kidney, Ureter, Bladder - urine volume decreased Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 300 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 300 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 300 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - delayed effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 100 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - endocrine system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 1995 umol/kg/24H (Intermittent)

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 369,65,1996

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阿昔洛韦钠安全信息

[ 危害码 (欧洲) ]:
C

[ 海关编码 ]:
2933990090

阿昔洛韦钠海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%