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毛钩藤碱

毛钩藤碱用途

Hirsutine,一种 Uncaria rhynchophylla 的吲哚生物碱,具有抗癌活性。Hirsutine 诱导细胞凋亡,并且是一种有效的 Dengue virus 抑制剂,具有低毒性。

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毛钩藤碱名称

[ CAS 号 ]:
7729-23-9

[ 中文名 ]:
毛钩藤碱

[ 英文名 ]:
Hirsutine

[中文别名 ]:

二氢柯楠因碱

[英文别名 ]:

Hirsutine

毛钩藤碱生物活性

[ 描述 ]:

Hirsutine,一种 Uncaria rhynchophylla 的吲哚生物碱,具有抗癌活性。Hirsutine 诱导细胞凋亡,并且是一种有效的 Dengue virus 抑制剂,具有低毒性。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

研究领域 >> 感染

[体外研究]

Hirsutine以时间和剂量依赖性方式显着降低MCF-7和MDA-MB-231细胞的活力,IC50值分别为447.79和179.06μM。在MDA-MB-231细胞中,Hirsutine诱导MMP的凋亡和去极化,从线粒体释放Cyt C,并激活半胱天冬酶9和半胱天冬酶3[2]。

[体内研究]

Hirsutine通过ROCK1/PTEN/PI3K/GSK3β途径诱导人肺癌细胞mPTP依赖性凋亡[3]。

[参考文献]

[1]. Hishiki T, et al. Hirsutine, an Indole Alkaloid of Uncaria rhynchophylla, Inhibits Late Step in Dengue Virus Lifecycle. Front Microbiol. 2017 Aug 30;8:1674.

[2]. Huang QW, et al. [Hirsutine induces apoptosis of human breast cancer MDA-MB-231 cells through mitochondrial pathway]. Sheng Li Xue Bao. 2018 Feb 25;70(1):40-46.

[3]. Zhang R, et al. Hirsutine induces mPTP-dependent apoptosis through ROCK1/PTEN/PI3K/GSK3β pathway in human lung cancer cells. Cell Death Dis. 2018 May 22;9(6):598.

毛钩藤碱物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
531.7±50.0 °C at 760 mmHg

[ 熔点 ]:
101℃

[ 分子式 ]:
C₂₂H₂₈N₂O₃

[ 分子量 ]:
368.469

[ 闪点 ]:
275.4±30.1 °C

[ 精确质量 ]:
368.209991

[ PSA ]:
54.56000

[ LogP ]:
3.96

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.613

[ 储存条件 ]:
室温

毛钩藤碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VS3660000

CHEMICAL NAME :: 17,18-Seco-3-beta-yohimban-16-carboxylic acid, 16,17-didehydro-17-methoxy-, methyl ester, (E)-

CAS REGISTRY NUMBER :: 7729-23-9

LAST UPDATED :: 198909

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C22-H28-N2-O3

MOLECULAR WEIGHT :: 368.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 110 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 94,17,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 94,17,1989