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一叶萩碱

一叶萩碱用途

(-)-Securinine 是一种植物来源的生物碱,也是一种 GABAA 受体拮抗剂。

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一叶萩碱名称

[ CAS 号 ]:
5610-40-2

[ 中文名 ]:
一叶秋碱

[ 英文名 ]:
Securinine

[中文别名 ]:

[英文别名 ]:

1,2,3,4,10,10a-Hexahydro-10-hydroxy
securinine
securinin
Securinan-11-one (9CI)
Securan one
SECURAN-11-ONE
Securinan-11-one
Securinan-11-on
(-)-Securinine

一叶萩碱生物活性

[ 描述 ]:

(-)-Securinine 是一种植物来源的生物碱,也是一种 GABAA 受体拮抗剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

信号通路 >> 神经信号通路 >> GABA受体

天然产物 >> 生物碱

研究领域 >> 神经疾病

[ 靶点 ]

GABAA receptor[1]

[体外研究]

(-)-叶蝉碱是植物来源的主要生物碱,也是GABAA受体拮抗剂。 (-)- Securinine对HeLa细胞生长抑制显着有效,IC50值为7.02±0.52μg/ mL(32.3μM)。 (-)- Securinine在受试细胞中以剂量依赖性方式诱导细胞凋亡,增加ROS阳性细胞和去极化细胞的百分比以及刺激ERK1/2,caspase-9和-3/7的活性。 (-)- Securinine还诱导S期细胞周期停滞。实时PCR分析显示肿瘤坏死因子受体超家族(TNFRSF)基因在(-)- Securinine刺激的细胞中高表达[1]。

[体内研究]

在该肿瘤模型中,(-)- Securinine治疗显着损害肿瘤生长,表明(-)- Securinine具有作为急性髓性白血病(AML)治疗剂的潜力。 (-)-在研究期结束时,使用Securinine治疗的小鼠(n = 5只小鼠,双侧肿瘤),肿瘤平均比载体治疗小鼠小75％[2]。

[激酶实验]

将细胞接种在12孔板（1×105 /孔）中，并用浓度为1.0至50.0μg/ mL的（ - ） - Securinine处理。将对照细胞以0.5％（v / v）的浓度暴露于DMSO。暴露6小时和24小时后，根据制造商的说明，通过Caspase-Glo 9 Assay Kit和Glomax Multi + Detection System测量胱天蛋白酶-9的活性。在将细胞暴露于（ - ） - 叶蝉碱24小时后评估胱天蛋白酶-3/7的活性。然后根据制造商的方案使用Muse Caspase-3/7测定试剂盒收获并制备细胞。通过Muse Cell Analyzer分析染色的细胞。实验至少在三个独立的重复中进行[1]。

[细胞实验]

通过MTT测定确定细胞的活力。将HeLa细胞以5×103细胞/孔的密度接种在96孔板中，并用（ - ） - 叶蝉碱以1.0至20.0μg/ mL的浓度处理24小时。在所有MTT实验中使用的溶剂的最大浓度分别为甲醇和DMSO的5.0％（v / v）和1.0％（v / v）。用平板读数器测量所得甲crystals溶液的吸收。活力结果表示为至少三次独立实验的IC50平均值[1]。

[动物实验]

使用6周龄雌性裸鼠并用10×106 HL-60细胞双侧皮下注射。（ - ） - 在肿瘤细胞注射后10天开始血清素处理。在开始药物治疗之前，已建立的肿瘤模型存在可触及的肿瘤。每天腹膜内注射15mg / kg（ - ） - 叶蝉碱或载体（30μLDMSO和70μL水）5天，然后每天注射一次，持续2天。这个注射时间表再重复两周[2]。

[参考文献]

[1]. Stefanowicz-Hajduk J, et al. Securinine from Phyllanthus glaucus Induces Cell Cycle Arrest and Apoptosis in Human Cervical Cancer HeLa Cells. PLoS One. 2016 Oct 28;11(10):e0165372.

[2]. Kalpana Gupta, et al. Securinine, a Myeloid Differentiation Agent with Therapeutic Potential for AML. PLoS One. 2011; 6(6): e21203.

[相关活性小分子]

一叶萩碱物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
459.0±45.0 °C at 760 mmHg

[ 熔点 ]:
140-142ºC

[ 分子式 ]:
C₁₃H₁₅NO₂

[ 分子量 ]:
217.264

[ 闪点 ]:
197.0±19.6 °C

[ 精确质量 ]:
217.110275

[ PSA ]:
29.54000

[ LogP ]:
0.60

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.633

[ 储存条件 ]:
2-8C

一叶萩碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VS4115000

CHEMICAL NAME :: Securinine, (-)-

CAS REGISTRY NUMBER :: 5610-40-2

LAST UPDATED :: 199201

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C13-H15-N-O2

MOLECULAR WEIGHT :: 217.29

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 :: >800 mg/kg

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

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 41 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 15100 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17400 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4300 ug/kg

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

REFERENCE :: YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 83,800,1963

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 270 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31800 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20420 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6230 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 19320 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >10 mg/kg

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

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >54 mg/kg

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

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 8 mg/kg

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - change in acuity Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - other changes

REFERENCE :: CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 54,234,1974 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 50 mg/kg

SEX/DURATION :: male 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

REFERENCE :: NATWAY Naturwissenschaften. (Springer-Verlag, Heidelberger Platz 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.1- 1913- Volume(issue)/page/year: 52,483,1965

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一叶萩碱安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25

[ 安全声明 (欧洲) ]:
36/37/39-45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
VS4115000

一叶萩碱文献

Proteomic and systems biology analysis of monocytes exposed to securinine, a GABA(A) receptor antagonist and immune adjuvant.

PLoS ONE 7(9) , e41278, (2012)

Securinine, a GABA(A) receptor antagonist, has been reported to enhance monocyte cell killing of Coxiella burnetii without obvious adverse effects in vivo. We employed multiplex 2D gel electrophoresis...

Securinine, a myeloid differentiation agent with therapeutic potential for AML.

PLoS ONE 6(6) , e21203, (2011)

As the defining feature of Acute Myeloid Leukemia (AML) is a maturation arrest, a highly desirable therapeutic strategy is to induce leukemic cell maturation. This therapeutic strategy has the potenti...

L-securinine induced the human colon cancer SW480 cell autophagy and its molecular mechanism.

Fitoterapia 82(8) , 1258-64, (2011)

To investigate the anti-tumor effects of L-securinine inducing colon cancer SW480 cell autophagy and explore its potential molecular mechanism.MTT method was used to detect the antitumor effect of SW4...

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