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蛇床子素

蛇床子素用途

Osthole 是一种天然抗组胺药替代试剂。Osthole 可有效抑制组胺 H1 受体 (histamine H1 receptor) 活性。

蛇床子素名称

[ CAS 号 ]:
484-12-8

[ 中文名 ]:
蛇床子素

[ 英文名 ]:
Osthole

[中文别名 ]:

[英文别名 ]:

Ostol
MFCD00076049
Cnidium Monnieri Extract
DaMiana Extract
7-methoxy-8-(3-methylbut-2-enyl)chromen-2-one
7-Methoxy-8-isopentenylcoumarin
7-Methoxy-8-(3-methyl-2-butenyl)coumarin
Osthol/Osthole
7-methoxy-8-(3-methylbut-2-enyl)-2H-chromen-2-one
Ostole

蛇床子素生物活性

[ 描述 ]:

Osthole 是一种天然抗组胺药替代试剂。Osthole 可有效抑制组胺 H1 受体 (histamine H1 receptor) 活性。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 癌症

天然产物 >> 苯丙酸类

[ 靶点 ]

Histamine H1 receptor[1]

[体外研究]

在研究组中,蛇床子素(p <0.0001)和非索非那定(p <0.001)抑制由组胺诱导的HRH-1 mRNA表达增加。在用组胺/ Osthole培养的细胞中也观察到该结果;其中组合物质与组胺相比降低HRH-1 mRNA表达(p <0.0001)[1]。当Osthole以高达100μM的剂量使用时,细胞活力的评估未检测到明显的毒性。然而,当剂量达到500μM时,Osthole开始显示出毒性作用。基于这些观察结果,Osthole用于所有体外研究,剂量范围为10至100μM。蛇床子素剂量依赖性地促进成骨细胞分化,如成骨细胞分化标志物基因如I型胶原(col1),骨涎蛋白(BSP)和骨钙蛋白(OC)的上调所示(培养2天)。 Osthole以剂量依赖的方式促进小鼠原代成骨细胞的ALP活性[2]。

[体内研究]

每天以5mg/kg的剂量向小鼠颅盖骨皮下注射Osthole可显着刺激局部骨形成,如最后一次注射后2周收获的颅骨样品的组织学分析所示,并用H＆E橙色G染色。组织形态学分析显示Osthole与阳性对照微管抑制剂TN-16一样,对骨形成有显着影响。然而,当Osthole以每天1mg/kg的剂量使用时,没有观察到这种效果。腹腔注射Osthole 8周显着逆转卵巢切除大鼠的骨质流失。用三硝基苯酚一品红染色的L4样品的组织学检查显示用Osthole处理的切除卵巢的大鼠中的小梁结构的部分恢复。组织形态学分析显示,使用Osthole治疗可显着增加总BMD,骨小梁体积和小梁厚度,并减少小梁分离[2]。

[细胞实验]

在第一个研究日的上午7点到9点之间从参与者收集外周血样品，并将这些样品浓缩在具有K3EDTA的分组管中。然后制备新鲜的PBMC。将分离的细胞以RPX-1640每孔1×106接种在24孔板上，并补充1％热灭活的人AB血清，1％庆大霉素和0.25％PHA。 24小时后向每个孔中加入活性试剂，纯培养基形成每种物质的对照。然后在另外三天后收获细胞[1]。

[动物实验]

小鼠[2]将4周龄ICR瑞士小鼠皮下注射到颅骨表面，每天两次或不同时处理Osthole，连续5天，剂量为1和5 mg / kg /天（每组3只小鼠））。微管抑制剂TN-16用作阳性对照（每天5mg / kg，通过皮下注射，每天两次，持续2天;每组3只小鼠）。处理后3周对所有小鼠实施安乐死，解剖颅盖骨，用10％磷酸盐缓冲的福尔马林固定2天，在10％EDTA中脱钙2周，并包埋在石蜡中。切割组织切片并用苏木精和伊红橙G染色。使用OsteoMeasure系统通过组织形态学定量颅骨表面上的新骨区域。为了测量矿物质附着率（MAR）和骨形成率（BFR），在第7天和第14天通过腹膜内注射（20mg / kg）进行双钙黄绿素标记，并且在第二次标记后7天对小鼠实施安乐死。标签在塑料部分进行检查。将解剖的颅骨样品固定在75％乙醇中并包埋在甲基丙烯酸甲酯中。用荧光显微镜检查未染色的横切面（3μm厚）。 MAR和BFR使用OsteoMeasure系统测量。大鼠[2]使用30只6个月大的雌性Sprague-Dawley大鼠。在腹膜内戊巴比妥注射（30mg / kg）麻醉后，将大鼠按体重随机分成三组进行手术（n = 10 /组）：组1：假手术，然后进行PBS载体治疗（假+ VEH）;第2组：卵巢切除术后接受载体治疗（OVX + VEH）;第3组：卵巢切除术，然后进行Osthole治疗（OVX + OST）。手术后1个月开始治疗，持续8周。每天一次口服给予载体或Osthole（100mg / kg /天），持续8周。在实验结束时对大鼠实施安乐死之前，使用双能X射线吸收测定法测量总骨矿物质密度（BMD，g / m 2）。然后解剖第四腰椎（L4）用于组织形态学和微计算机断层扫描（μCT）分析，并且左股骨轴用于生物力学测试。

[参考文献]

[1]. Kordulewska NK, et al. Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-κB, CCR1, chemokine CCL5/RANTES and interleukin-1β in PBMC allergic and non-allergic patients. Immunobiology.

[2]. Tang DZ, et al. Osthole stimulates osteoblast differentiation and bone formation by activation of beta-catenin-BMP signaling. J Bone Miner Res. 2010 Jun;25(6):1234-45.

[3]. Sun W, et al. Osthole pretreatment alleviates TNBS-induced colitis in mice via both cAMP/PKA-dependent and independent pathways. Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128.

[相关活性小分子]

蛇床子素物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
396.7±42.0 °C at 760 mmHg

[ 熔点 ]:
83-84°C

[ 分子式 ]:
C₁₅H₁₆O₃

[ 分子量 ]:
244.286

[ 闪点 ]:
167.6±22.5 °C

[ 精确质量 ]:
244.109940

[ PSA ]:
39.44000

[ LogP ]:
3.87

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.557

[ 储存条件 ]:
room temp

[ 水溶解性 ]:
水溶性：不溶；易溶于：甲醇；可溶于：乙醇

蛇床子素MSDS

详细MSDS(安全技术说明书)

蛇床子素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GN7700000

CHEMICAL NAME :: Coumarin, 7-methoxy-8-(3-methyl-2-butenyl)-

CAS REGISTRY NUMBER :: 484-12-8

LAST UPDATED :: 199803

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C15-H16-O3

MOLECULAR WEIGHT :: 244.31

WISWESSER LINE NOTATION :: T66 BOVJ IO1 J2UY1&1

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 :: 2905 mg/kg

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

REFERENCE :: IJMRAQ Indian Journal of Medical Research. (Indian Council of Medical Research, Ansari Nagar, New Delhi 110 029, India) V.1- 1913- Volume(issue)/page/year: 55,241,1967

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 600 mg/kg

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

REFERENCE :: IJMRAQ Indian Journal of Medical Research. (Indian Council of Medical Research, Ansari Nagar, New Delhi 110 029, India) V.1- 1913- Volume(issue)/page/year: 55,241,1967

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 190 mg/kg

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

REFERENCE :: IJMRAQ Indian Journal of Medical Research. (Indian Council of Medical Research, Ansari Nagar, New Delhi 110 029, India) V.1- 1913- Volume(issue)/page/year: 55,241,1967

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 16 mg/kg

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

REFERENCE :: PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 11,331,1977

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >40 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 150,425,1964

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >70 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 138,400,1962

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 25 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 138,400,1962

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 150,425,1964

蛇床子素安全信息

[ 危害码 (欧洲) ]:
Xi,Xn

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin . R20/21/22:Harmful by inhalation, in contact with skin and if swallowed .

[ 安全声明 (欧洲) ]:
S26-S36/37-S36/37/39

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

[ WGK德国 ]:
3

[ RTECS号 ]:
GN7700000

[ 海关编码 ]:
29081000

蛇床子素合成路线

详细合成路线

蛇床子素上下游产品

蛇床子素上游产品

蛇床子素下游产品

蛇床子素海关

[ 海关编码 ]: 2932209090

[ 中文概述 ]:
2932209090. 其他内酯. 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 ]:
2932209090. other lactones. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

蛇床子素文献

[Effect of osthole on bone metabolism in rat femoral tissues in vitro].

Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 35(5) , 561-6, (2013)

To investigate the effect of osthole on bone metabolism in rat femoral tissues in vitro.The rat femoral tissues were isolated in vitro. The optimal concentrations of ostehole (1×10(-5) mol/L) and estr...

Osthole attenuates spinal cord ischemia–reperfusion injury through mitochondrial biogenesis–independent inhibition of mitochondrial dysfunction in rats

J. Surg. Res. 185(2) , 805-14, (2013)

Background Osthole, the main bioactive compounds isolated from the traditional Chinese medical herb broad Cnidium monnieri (L.) cusson, has been shown to exert spectrum of pharmacologic activities. Th...

Osthole activates glucose uptake but blocks full activation in L929 fibroblast cells, and inhibits uptake in HCLE cells

Life Sci. 102(2) , 105-10, (2014)

Aims Osthole, a coumarin derivative, has been used in Chinese medicine and studies have suggested a potential use in treatment of diabetes and cancers. Therefore, we investigated the effects of osthol...

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