硫酸奎宁
硫酸奎宁用途
硫酸奎宁(2:1)(奎拉喹)是一种从金鸡纳树皮中提取的口服活性生物碱,可用于抗疟疾研究。硫酸奎宁(2:1)是一种钾通道抑制剂,可抑制WT小鼠Slo3(KCa5.1)通道电流,该电流由+100的电压脉冲引起 mV,IC50为169μM[1][2]。
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硫酸奎宁名称
[ CAS 号 ]:
804-63-7
[ 中文名 ]:
硫酸奎宁
[ 英文名 ]:
Quinine sulfate
[英文别名 ]:
- quinine hydrogen sulphate
- (8α,9R)-6'-Methoxycinchonan-9-ol sulfate (1:1)
- EINECS 212-359-2
- MFCD00078499
- Quinine hydrogen sulfate
- Quinine sulphate
- chinidinesulfate
- Quinine sulfate
硫酸奎宁生物活性
[ 描述 ]:
硫酸奎宁(2:1)(奎拉喹)是一种从金鸡纳树皮中提取的口服活性生物碱,可用于抗疟疾研究。硫酸奎宁(2:1)是一种钾通道抑制剂,可抑制WT小鼠Slo3(KCa5.1)通道电流,该电流由+100的电压脉冲引起 mV,IC50为169μM[1][2]。
[ 相关类别 ]:
[体外研究]
硫酸奎宁(150μM,30分钟)抑制人肝癌HepG2细胞系中登革热病毒的增殖和细胞抑制作用[1]。硫酸奎宁(37.5-150μM,24小时)以剂量依赖性方式显著降低人肝癌HepG2细胞系中的病毒DENV RNA和蛋白质水平[1]。细胞增殖试验[1]细胞系:人肝癌细胞系(HepG2)浓度:150μM孵育时间:30分钟结果:与未处理相比,抑制DENV病毒复制,产率为19%。以剂量依赖性方式将DENV阳性细胞从23.28%减少到12.05%。
[体内研究]
硫酸奎宁(口服灌胃,12或15 mg/kg,每周,16周)对瑞士白化小鼠的皮肤癌有一定的抑制作用[2]。硫酸奎宁(口服,10 mg/kg,每日,8周)导致雄性成年白化大鼠睾丸组织抗氧化防御系统(如SOD、CAT和GSH酶活性)降低[3]。动物模型:7-8周(体重24g)的瑞士白化小鼠[2]剂量:12mg/kg,15mg/kg给药:口服灌胃;每周;16周结果:在12mg/kg剂量下,肿瘤大小和重量显著减少,而在15mg/kg更高剂量下,影响很小。
[参考文献]
硫酸奎宁物理化学性质
[ 沸点 ]:
911.6ºC at 760 mmHg
[ 分子式 ]:
C20H26N2O6S
[ 分子量 ]:
422.495
[ 闪点 ]:
505.1ºC
[ 精确质量 ]:
422.151154
[ PSA ]:
128.57000
[ LogP ]:
3.53910
硫酸奎宁毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- VA8440000
- CHEMICAL NAME :
- Quinine, sulfate
- CAS REGISTRY NUMBER :
- 804-63-7
- LAST UPDATED :
- 199701
- DATA ITEMS CITED :
- 17
- MOLECULAR FORMULA :
- C20-H24-N2-O2.1/2H2-O4-S
- MOLECULAR WEIGHT :
- 420.52
- WISWESSER LINE NOTATION :
- T66 BNJ HO1 EYQ- DT66 A B CNTJ A1U1 &WSQQ
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 45455 ug/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Kidney, Ureter, Bladder - renal function tests depressed
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 6500 ug/kg
- TOXIC EFFECTS :
- Behavioral - muscle weakness Kidney, Ureter, Bladder - interstitial nephritis
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 130 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Ear) - change in acuity Behavioral - changes in motor activity (specific assay)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 129 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 27 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Ear) - tinnitus Gastrointestinal - nausea or vomiting
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 12 mg/kg/1D-I
- TOXIC EFFECTS :
- Liver - hepatitis, fibrous (cirrhosis, post-necrotic scarring)
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 220 mg/kg
- TOXIC EFFECTS :
- Cardiac - other changes Lungs, Thorax, or Respiration - acute pulmonary edema Blood - changes in spleen
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 4300 ug/kg
- TOXIC EFFECTS :
- Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - agranulocytosis
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 80 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Ear) - change in acuity Gastrointestinal - nausea or vomiting
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 126 mg/kg/3W-I
- TOXIC EFFECTS :
- Cardiac - cardiomyopathy including infarction Skin and Appendages - dermatitis, allergic (after systemic exposure)
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 800 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 1425 mg/kg
- SEX/DURATION :
- female 14 day(s) pre-mating - 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical
MUTATION DATA
- TYPE OF TEST :
- Phage inhibition capacity
- TEST SYSTEM :
- Bacteria - Escherichia coli
- DOSE/DURATION :
- 100 ug/plate
- REFERENCE :
- CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,2819,1983 *** REVIEWS *** TOXICOLOGY REVIEW PHJOAV Pharmaceutical Journal. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London, SE1 7JN, UK) V.131- 1933- Volume(issue)/page/year: 213,159,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80205 No. of Facilities: 92 (estimated) No. of Industries: 3 No. of Occupations: 4 No. of Employees: 460 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80205 No. of Facilities: 82 (estimated) No. of Industries: 2 No. of Occupations: 3 No. of Employees: 1305 (estimated) No. of Female Employees: 678 (estimated)
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硫酸奎宁安全信息
[ 危险品运输编码 ]:
UN 1544
[ 包装等级 ]:
III
[ 危险类别 ]:
6.1(b)
硫酸奎宁制备
【方法一】
由金鸡纳属树(chinchona succirubra)等的树皮提取所得奎宁经硫酸化而成。
【方法二】
该品系由苯草植物金鸡钠树皮中提取的生物碱。较重要的有四种、即奎宁、奎尼丁、辛可宁和辛可尼丁。它们者有抗疟作用,作以硅宁最强。金鸡纲树皮主要产于印尼、印度,我国台湾、海南岛和去南等地也有出产。取干燥的金鸡钠树皮粉碎,用消石和烧碱水溶液湿润,然后用乙醇浸泡提取。乙醇提取液加硫酸调pH至6-6.5,减压蒸发浓缩,同时回收乙醇。浓缩液经硫酸、烧碱处理,活性炭脱色,结晶得到粗品,再经精制而得成品。对干燥金鸡纲树皮计,总收率为2%。奎宁也可由化学合成。
由金鸡纳属树(chinchona succirubra)等的树皮提取所得奎宁经硫酸化而成。
【方法二】
该品系由苯草植物金鸡钠树皮中提取的生物碱。较重要的有四种、即奎宁、奎尼丁、辛可宁和辛可尼丁。它们者有抗疟作用,作以硅宁最强。金鸡纲树皮主要产于印尼、印度,我国台湾、海南岛和去南等地也有出产。取干燥的金鸡钠树皮粉碎,用消石和烧碱水溶液湿润,然后用乙醇浸泡提取。乙醇提取液加硫酸调pH至6-6.5,减压蒸发浓缩,同时回收乙醇。浓缩液经硫酸、烧碱处理,活性炭脱色,结晶得到粗品,再经精制而得成品。对干燥金鸡纲树皮计,总收率为2%。奎宁也可由化学合成。
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