杠柳毒苷

杠柳毒苷用途

Periplocin 是一类从 Periploca forrestii 中分离出的强心类固醇。Periplocin 可促进肿瘤细胞凋亡并抑制肿瘤生长。Periplocin 通过激活 Na/K-ATPase 介导的 Src/ERK 和 PI3K/Akt 途径而具有促进伤口愈合的潜力。

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杠柳毒苷名称

[ CAS 号 ]:
13137-64-9

[ 中文名 ]:
杠柳毒苷

[ 英文名 ]:
Periplocin

[中文别名 ]:

[英文别名 ]:

Glucoperiplocymarin
corchorusoside C
Periplogenin + D-cymarose + D-glucose [German]
periplocin
Periplogenin + D-cymarose + D-glucose
Periplocoside

杠柳毒苷生物活性

[ 描述 ]:

[ 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 >> 炎症/免疫

[ 靶点 ]

Apoptosis[2]

[体外研究]

杠柳毒素(5-20μM；48小时；L929细胞)处理显示在20μM时增殖增加至131%[1]。杠柳毒素(5-20μM；30-120分钟；L929细胞)以剂量依赖和时间依赖的方式增加活性部位Src、ERK、PI3K和Akt的磷酸化,杠柳毒素(5-20μM；48小时)显著促进成纤维细胞的迁移[1]。杠柳碱(5-20μM；48小时)增加L929成纤维细胞的胶原生成[1]。杠柳碱诱导Na/KATPase介导Src/ERK和PI3K/Akt通路的激活[1]。细胞活力测定[1]细胞株：L929细胞浓度：5μM,10μM,20μM孵育时间：48小时结果：20μM时增殖率高达131%。Western Blot分析[1]细胞株：L929细胞浓度：5μM,10μM,20μM孵育时间：30分钟,60分钟,120分钟结果：Src磷酸化增加,ERK、PI3K和Akt在活性部位呈剂量依赖性和时间依赖性。

[体内研究]

杠柳碱(5-20 mg/kg；腹腔注射；每日；连续14天；雌性SCID小鼠)治疗抑制小鼠异种移植瘤模型中肝细胞癌(HCC)的生长[2]。动物模型：6-8周龄雌性SCID小鼠,注射Huh-7细胞[2],剂量：5mg/kg,20mg/kg,腹腔注射,每日一次,连续14d,结果：抑制小鼠异种移植瘤模型肝细胞癌(HCC)的生长。

[参考文献]

[1]. Chen L, et al. Periplocin promotes wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase. Phytomedicine. 2019 Apr;57:72-83.

[2]. Cheng CF, et al. Antitumor Effect of Periplocin in TRAIL-Resistant Human Hepatocellular Carcinoma Cells through Downregulation of IAPs. Evid Based Complement Alternat Med. 2013;2013:958025.

杠柳毒苷物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
877.4±65.0 °C at 760 mmHg

[ 熔点 ]:
205°C

[ 分子式 ]:
C₃₆H₅₆O₁₃

[ 分子量 ]:
682.795

[ 闪点 ]:
272.8±27.8 °C

[ 精确质量 ]:
682.356445

[ PSA ]:
193.83000

[ LogP ]:
-1.36

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.624

[ 储存条件 ]:
2-8C

杠柳毒苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: FH4919700

CHEMICAL NAME :: Card-20(22)-enolide, 3-((2,6-dideoxy-4-O-beta-D-glucopyranosyl-3-O-methyl- beta-D-ribo- hexopyranosyl)oxy)-5,14-dihydroxy-, (3-beta,5-beta)-

CAS REGISTRY NUMBER :: 13137-64-9

BEILSTEIN REFERENCE NO. :: 0075742

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C36-H56-O13

MOLECULAR WEIGHT :: 696.92

WISWESSER LINE NOTATION :: L E5 B666TJ A1 E1 IQ MQ F- DT5OV EHJ& OO- FT6OTJ B1 CQ DO- BT6OTJ CQ DQ EQ F1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 480 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 27,449,1926

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 2500 ug/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Cardiac - arrhythmias (including changes in conduction) Gastrointestinal - nausea or vomiting

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 27,449,1926

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 120 ug/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Cardiac - arrhythmias (including changes in conduction) Gastrointestinal - nausea or vomiting

REFERENCE :: 85ELDJ "Die Herzwirksamen Glykoside," Baumgarten, G., and W. Forster, Leipzig, Ger. Dem. Rep., VEB Georg Thieme, 1963 Volume(issue)/page/year: -,193,1963

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 121 ug/kg

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

REFERENCE :: 85ELDJ "Die Herzwirksamen Glykoside," Baumgarten, G., and W. Forster, Leipzig, Ger. Dem. Rep., VEB Georg Thieme, 1963 Volume(issue)/page/year: -,151,1963

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Cardiac - arrhythmias (including changes in conduction) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 27,449,1926

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: 34 mg/kg

TOXIC EFFECTS :: Cardiac - pulse rate Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 27,449,1926