青蒿素

青蒿素用途

青蒿用作抗疟药，临床应用证明，青蒿素及其衍生物对间疟及恶性疟疾有特效，特别是青蒿甲(Artemtherin)，它比其他青蒿素类药物的杀减疟原虫细胞内无性体的作用更强。具有高效、速效、低毒和与氯喹无交叉抗性等优点，不仅可用于治疗，还可用于急救。适用于各种疟疾，如恶性疟、间日疟、抗氯喹疟及脑型疟等。包括凶险型。最引人注目的是双氢青蒿素及其片剂。该药比青蒿素抗疟疗效提高10倍，复发率只有1.95%。因此被评为1992年中国十大科技成就。青蒿素及其衍生物不单是一种优良的抗疟药物，在其他疾病的治疗中也潜在诱人的前景。动物实验发现，青蒿素类治疗小鼠华支睾吸虫，灭虫率可达100%；治疗动物血吸虫，灭虫率达33.8-99.3%。以青蒿素治疗盘形红斑狼疮，总有效率达90%。治疗登革热，疗效显著优于吗啉双胍等西药。免疫学家在研究中还发现，青蒿素能显著提高淋巴细胞转化率，增强抗体的免疫功能。未发现本品对心、肝、肾有毒性作用。临床均未有任何明显的副作用。

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青蒿素名称

[ CAS 号 ]:
63968-64-9

[ 中文名 ]:
青蒿素

[ 英文名 ]:
Artemisinin

[中文别名 ]:

[英文别名 ]:

artemisininum
qinghausu
Artemisinin
UNII-9RMU91N5K2
ARTEANUIN
Quinghaosu
qinghaosu
QINGHAOSA
artemisinine
(+)-artemisinin

青蒿素生物活性

[ 描述 ]:

Artemisinin是从青蒿 (Artemisia annua L.) 植物的地上部分分离的抗疟疾药物。

[ 相关类别 ]:

信号通路 >> 抗感染 >> HCV

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

天然产物 >> 萜类化合物和糖苷

[体外研究]

青蒿素(3.125-100μM)浓度依赖性地抑制Aβ25-35在PC12细胞中诱导的细胞毒性。青蒿素(25μM)抑制Aβ25-35诱导的LDH释放,细胞凋亡和ROS产生,减弱Aβ诱导的线粒体膜电位损失和caspase 3/7活性增加,并在时间和浓度下刺激ERK1/2的磷酸化。依赖于PC12细胞的方式。 ERK 1/2途径介导青蒿素对PC12细胞的保护作用[1]。青蒿素在MCF-7/Dox细胞系中显示细胞毒活性,处理24小时后IC50为3.7±0.4μg/ mL。此外,青蒿素处理MCF-7细胞,对Dox和DDP敏感和抗性,导致蛋白质如LF,FTH1和HEP的表达降低。由于抑制VEGF表达和细胞迁移,青蒿素激活p38 MAPK激酶级联,而不管氧化应激[2]。青蒿素(50,100或200 mg)显着抑制异氟醚诱导的海马神经元丢失,降低caspase-3阳性细胞计数,并切割caspase-3表达,并调节凋亡途径蛋白的表达。青蒿素调节JNK/ERK 1/2信号传导和组蛋白乙酰化[3]。青蒿素以剂量依赖性方式抑制HCV复制,EC50值为167±38μM。青蒿素及其最有效的类似物通过诱导活性氧(ROS)部分抑制HCV的体外复制[4]。青蒿素以剂量依赖的方式显着抑制VSMC增殖。青蒿素(1 mM)72 h显着降低增殖细胞核抗原信使RNA的表达[5]。

[体内研究]

青蒿素(50,100或200mg/kg b.wt /天,po)防止异氟醚诱导的工作记忆损伤,如在T迷宫测试中观察到的。青蒿素增强暴露于异氟醚的大鼠的空间导航和记忆。与单独使用异氟醚的大鼠相比,青蒿素处理的大鼠表现出明显更好的表现[3]。

[激酶实验]

简言之，将PC12细胞在裂解缓冲液中裂解并以12,500×g离心5分钟。将15mL细胞裂解物与50mL 2X底物工作溶液在室温下在96孔板中孵育30分钟。然后通过Infinite M200 PRO多模微孔板在490nm的激发波长和520nm的发射下测定荧光强度。将每个样品的荧光强度标准化为样品的蛋白质浓度。将％caspase 3/7活性的所有值标准化为对照组。

[细胞实验]

为此目的，将细胞在补充有胰岛素的DMEM中的96孔板中培养。将青蒿素，Dox和DDP以不同浓度添加到培养基中，并将细胞培养24或48小时。为此目的，青蒿素在培养基中的0.01％DMSO中稀释。此后，向细胞中加入10μLMTT染料溶液（在磷酸盐缓冲盐水中5mg / mL）;将细胞在相同条件下孵育3小时。离心（1500rpm，5分钟）后，除去上清液。向每个孔中加入100μL二甲基亚砜，以溶解甲..使用多孔分光光度计在540nm的波长下测量吸收。

[动物实验]

通过口服强饲法每天从P2到P21给予单独的一组大鼠幼仔（总大鼠幼崽80;每组n = 16）青蒿素（50,100或200mg / kg体重）。在P7上，幼崽在温度控制室中暴露于异氟烷（0.75％在30％氧气或空气中）6小时。未暴露于麻醉但未给予青蒿素的动物作为对照组，而单独接受异氟醚的大鼠被归类为麻醉对照。

[参考文献]

[1]. Zeng Z, et al. Artemisinin protects PC12 cells against β-amyloid-induced apoptosis through activation of the ERK1/2 signaling pathway. Redox Biol. 2017 Apr 4;12:625-633.

[2]. Chekhun VF, et al. Artemisinin modulating effect on human breast cancer cell lines with different sensitivity to cytostatics. Exp Oncol. 2017 Mar;39(1):25-29.

[3]. Xu G, et al. Neuroprotective effects of artemisinin against isoflurane-induced cognitive impairments and neuronal cell death involve JNK/ERK1/2 signalling and improved hippocampal histone acetylation in neonatal rats. J Pharm Pharmacol. 2017 Mar 12.

[4]. Obeid S, et al. Artemisinin analogues as potent inhibitors of in vitro hepatitis C virus replication. PLoS One. 2013 Dec 11;8(12):e81783.

[5]. Wang HY, et al. The effects of artemisinin on the proliferation and apoptosis of vascular smooth muscle cells of rats. Cell Biochem Funct. 2013 Sep 17.

[相关活性小分子]

青蒿素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
389.9±42.0 °C at 760 mmHg

[ 熔点 ]:
156-157ºC

[ 分子式 ]:
C₁₅H₂₂O₅

[ 分子量 ]:
282.332

[ 闪点 ]:
172.0±27.9 °C

[ 精确质量 ]:
282.146729

[ PSA ]:
53.99000

[ LogP ]:
2.27

[ 外观性状 ]:
结晶固体

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.533

[ 储存条件 ]:
通风低温干燥

[ 水溶解性 ]:
可溶于：甲醇

青蒿素MSDS

详细MSDS(安全技术说明书)

青蒿素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KD4170000

CHEMICAL NAME :: 3,12-Epoxy-12H-pyranol(4,3-j)-1,2-benzodioxepin-10(3H )-one, octahydro-3,6,9-trimethyl-, (3- alpha,5a-beta,6-beta,8a-beta,9-alpha,12-beta,12aR*)-( +)-

CAS REGISTRY NUMBER :: 63968-64-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C15-H22-O5

MOLECULAR WEIGHT :: 282.37

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 :: 5576 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - ataxia

REFERENCE :: JTCMEC Journal of Traditional Chinese Medicine (English Edition). (All-China Assoc. of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine) V.1- 1981- Volume(issue)/page/year: 2,31,1982

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2571 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - ataxia

REFERENCE :: JTCMEC Journal of Traditional Chinese Medicine (English Edition). (All-China Assoc. of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine) V.1- 1981- Volume(issue)/page/year: 2,31,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4228 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - ataxia

REFERENCE :: JTCMEC Journal of Traditional Chinese Medicine (English Edition). (All-China Assoc. of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine) V.1- 1981- Volume(issue)/page/year: 2,31,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1558 mg/kg

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

REFERENCE :: CMJODS Chinese Medical Journal (Beijing, English Edition). (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1975- Adopted vol. no. 92 in 1979. Volume(issue)/page/year: 92,811,1979

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2800 mg/kg

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

REFERENCE :: CMJODS Chinese Medical Journal (Beijing, English Edition). (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1975- Adopted vol. no. 92 in 1979. Volume(issue)/page/year: 92,811,1979

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 37,1108,1993

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >800 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: JTCMEC Journal of Traditional Chinese Medicine (English Edition). (All-China Assoc. of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine) V.1- 1981- Volume(issue)/page/year: 2,31,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3200 mg/kg/4D-I

TOXIC EFFECTS :: Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: CTYAD8 Zhongcaoyao. Chinese Traditional and Herbal Medicine. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.11- 1980- Volume(issue)/page/year: 21,134,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 1344 mg/kg/14D-I

TOXIC EFFECTS :: Cardiac - other changes Blood - changes in bone marrow (not otherwise specified) Blood - other changes

REFERENCE :: JTCMEC Journal of Traditional Chinese Medicine (English Edition). (All-China Assoc. of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine) V.1- 1981- Volume(issue)/page/year: 2,31,1982

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青蒿素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 安全声明 (欧洲) ]:
22-24/25

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

[ WGK德国 ]:
2

[ RTECS号 ]:
KD4170000

[ 海关编码 ]:
2932999099

青蒿素合成路线

详细合成路线

青蒿素上下游产品

青蒿素上游产品

青蒿素下游产品

青蒿素制备

1.取黄花蒿叶粉以5倍量乙醚冷浸3次，提取液浓缩至小体积；再用2% NaOH溶液除去酸性成分，蒸去乙醚，得中性醚提取物(得率为2%～3%)；将此中性醚提取物，拌以聚酰胺粉，以47%乙醇渗漉，渗漉液浓缩至小体积；再以乙醚提取，合并乙醚液浓缩后用硅胶柱层析，以石油醚-10%乙酸乙酯洗脱，将10%乙酸乙酯石油醚洗脱液浓缩后结晶，即得青蒿素(得率0.2%)。

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青蒿素海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧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

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

青蒿素文献

Anti-inflammatory, Antioxidant and Antimicrobial Effects of Artemisinin Extracts from Artemisia annua L.

Korean J. Physiol. Pharmacol. 19(1) , 21-7, (2015)

The anti-inflammatory, antioxidant, and antimicrobial properties of artemisinin derived from water, methanol, ethanol, or acetone extracts of Artemisia annua L. were evaluated. All 4 artemisinin-conta...

Artemisinin nanoformulation suitable for intravenous injection: Preparation, characterization and antimalarial activities.

Int. J. Pharm. 495 , 671-9, (2015)

More than 40 years after its discovery, artemisinin has become the most promising antimalarial agent. However, no intravenous formulation is available due to its poor aqueous solubility. Here, we repo...

Self-assembled biotransesterified cyclodextrins as potential Artemisinin nanocarriers. II: In vitro behavior toward the immune system and in vivo biodistribution assessment of unloaded nanoparticles.

Eur. J. Pharm. Biopharm. 88(3) , 683-94, (2014)

In a previous study, we reported on the formulation of Artemisinin-loaded surface-decorated nanoparticles (nanospheres and nanoreservoirs) by co-nanoprecipitation of PEG derivatives (PEG1500 and PEG40...

更多文献

青蒿素

青蒿素用途

青蒿素名称

青蒿素生物活性

青蒿素物理化学性质

青蒿素MSDS

详细MSDS(安全技术说明书)

青蒿素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

青蒿素安全信息

青蒿素合成路线

详细合成路线

青蒿素上下游产品

青蒿素上游产品

青蒿素下游产品

青蒿素制备

青蒿素海关

青蒿素文献

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