| 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)
Cinchonan-9-ol, 6'-methoxy-, (8α,9R)-, sulfate (1:1) (salt)
EINECS 212-359-2
MFCD00078499
Quinine hydrogen sulfate
Quinine sulphate
chinidinesulfate
Quinine sulfate
|
| 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 |
[1]. Shilu Malakar，et al. Drug repurposing of quinine as antiviral against dengue virus infection. Virus Res. 2018 Aug 15;255:171-178. doi: 10.1016/j.virusres.2018.07.018. Epub 2018 Jul 25. [2]. Jhanwar, Deepika，et al. Chemoprevention of DMBA induced skin carcinogenesis in swiss albino mice by quinine sulfate.(2016): 2636-2640. [3]. Ebenezer O Farombi, et al. Quercetin protects against testicular toxicity induced by chronic administration of therapeutic dose of quinine sulfate in rats. J Basic Clin Physiol Pharmacol. 2012 Feb 27;23(1):39-44.
|
| 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 |
CHEMICAL IDENTIFICATION
-
RTECS NUMBER :
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VA8440000
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CHEMICAL NAME :
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Quinine, sulfate
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CAS REGISTRY NUMBER :
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804-63-7
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LAST UPDATED :
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199701
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DATA ITEMS CITED :
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17
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MOLECULAR FORMULA :
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C20-H24-N2-O2.1/2H2-O4-S
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MOLECULAR WEIGHT :
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420.52
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WISWESSER LINE NOTATION :
-
T66 BNJ HO1 EYQ- DT66 A B CNTJ A1U1 &WSQQ
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
-
45455 ug/kg
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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
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
-
6500 ug/kg
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TOXIC EFFECTS :
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Behavioral - muscle weakness Kidney, Ureter, Bladder - interstitial nephritis
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
-
130 mg/kg
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TOXIC EFFECTS :
-
Sense Organs and Special Senses (Ear) - change in acuity Behavioral - changes in motor activity (specific assay)
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - man
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DOSE/DURATION :
-
129 mg/kg
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TOXIC EFFECTS :
-
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation)
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
-
ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Human - man
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DOSE/DURATION :
-
27 mg/kg
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TOXIC EFFECTS :
-
Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Ear) - tinnitus Gastrointestinal - nausea or vomiting
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
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12 mg/kg/1D-I
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TOXIC EFFECTS :
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Liver - hepatitis, fibrous (cirrhosis, post-necrotic scarring)
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TYPE OF TEST :
-
LDLo - Lowest published lethal dose
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ROUTE OF EXPOSURE :
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Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
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220 mg/kg
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TOXIC EFFECTS :
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Cardiac - other changes Lungs, Thorax, or Respiration - acute pulmonary edema Blood - changes in spleen
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Oral
-
SPECIES OBSERVED :
-
Human
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DOSE/DURATION :
-
4300 ug/kg
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TOXIC EFFECTS :
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Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - agranulocytosis
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
-
80 mg/kg
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TOXIC EFFECTS :
-
Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Ear) - change in acuity Gastrointestinal - nausea or vomiting
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TYPE OF TEST :
-
LDLo - Lowest published lethal dose
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ROUTE OF EXPOSURE :
-
Oral
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SPECIES OBSERVED :
-
Human - woman
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DOSE/DURATION :
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126 mg/kg/3W-I
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TOXIC EFFECTS :
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Cardiac - cardiomyopathy including infarction Skin and Appendages - dermatitis, allergic (after systemic exposure)
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TYPE OF TEST :
-
LDLo - Lowest published lethal dose
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ROUTE OF EXPOSURE :
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Oral
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SPECIES OBSERVED :
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Rodent - mouse
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DOSE/DURATION :
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800 mg/kg
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TOXIC EFFECTS :
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Details of toxic effects not reported other than lethal dose value
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TYPE OF TEST :
-
TDLo - Lowest published toxic dose
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ROUTE OF EXPOSURE :
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Oral
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DOSE :
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1425 mg/kg
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SEX/DURATION :
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female 14 day(s) pre-mating - 21 day(s) post-birth
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TOXIC EFFECTS :
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Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical
MUTATION DATA
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TYPE OF TEST :
-
Phage inhibition capacity
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TEST SYSTEM :
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Bacteria - Escherichia coli
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DOSE/DURATION :
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100 ug/plate
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REFERENCE :
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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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| 危险品运输编码 |
UN 1544 |
| 包装等级 |
III |
| 危险类别 |
6.1(b) |
【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。
