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替尼泊苷

替尼泊苷用途

Teniposide 是一种足叶草毒素衍生物,是拓扑异构酶 II (topoisomerase II) 的抑制剂,同时为一种化疗剂。

替尼泊苷名称

[ CAS 号 ]:
29767-20-2

[ 中文名 ]:
替尼泊苷

[ 英文名 ]:
Teniposide

[中文别名 ]:

鬼臼噻吩甙

[英文别名 ]:

etp
Pipodophyllotoxin VM 26
Teniposide/VM-26
vm-26
vehem
Teniposide
Teniposide(VuMon)
EINECS 249-831-2
MFCD00866516
Vumon

替尼泊苷生物活性

[ 描述 ]:

Teniposide 是一种足叶草毒素衍生物,是拓扑异构酶 II (topoisomerase II) 的抑制剂,同时为一种化疗剂。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

研究领域 >> 癌症

[ 靶点 ]

Topoisomerase II

[体外研究]

替尼泊苷是拓扑异构酶II抑制剂。替尼泊苷(VM-26,0.15-45mg/L)以剂量依赖性方式抑制Tca8113细胞的增殖,IC50为0.35mg/L.替尼泊苷(5 mg/L)诱导Tca8113细胞凋亡。替尼泊苷(5.0 mg/L)导致细胞在Tca8113细胞中停滞于G2/M期[2]。当细胞中miR-181b水平较高时,替尼泊苷对患者原代培养的胶质瘤细胞具有活性,IC50为1.3±0.34μg/ mL。与对照细胞相比,用具有低MDM2的替尼泊苷处理的细胞具有降低的活力,并且在MDM2抑制时IC50从5.86±0.36μg/ mL降低至2.90±0.35μg/ mL。替尼泊苷还通过MDM2的介导抑制具有高水平miR-181b的神经胶质瘤细胞的活力[3]。

[体内研究]

替尼泊苷(0.5mg/kg,ip)显着增加微核多色红细胞(MNPCE)频率,其与骨髓毒性直接相关,因为注意到显着的骨髓抑制。替尼泊苷(24mg/kg,ip)显着降低BrdU标记的精子的频率。替尼泊苷(12,24 mg/kg,ip)也可显着诱导雄性小鼠生殖细胞中的二体精子[1]。

[细胞实验]

将对数生长的Tca8113细胞用胰蛋白酶消化并制成单细胞悬浮液，然后以5×104细胞/孔的浓度接种于96孔培养板中，对于替尼泊苷8个柱，在每个板中用于CDDP的7个柱，每个柱中3个孔。培养24小时后，每个培养皿中3个孔的培养基更换为含有0.15 mg / L，0.5 mg / L，1.5 mg / L，5.0 mg / L，15 mg / L和45 mg /的替尼泊苷的培养基。 L或CDDP分别为0.1 mg / L，0.3 mg / L，1.0 mg / L，3.0 mg / L和9.0 mg / L.空白对照孔加入不含药物的培养基。然后将细胞再培养24小时，48小时，72小时，96小时和120小时。除去上清液，在每个孔中加入20μLMTT溶液，然后再培养4小时。小心弃去上清液，加入200μL二甲基亚砜（DMSO）并剧烈摇动以溶解紫色沉淀形成。使用波长为450nm的分光光度计测试每个孔的光密度（OD）。该实验一式三份重复[2]。

[动物实验]

用0.5mg / kg替尼泊苷处理动物（小鼠），并在处理后24小时取样骨髓。秋水仙碱和丝裂霉素C分别以2mg / kg的剂量用作阳性对照aneugen和clastogen。制备骨髓涂片并用May-Gruenwald / Giemsa溶液染色。为每只动物制备至少四个载玻片并使其干燥过夜。每只动物的一个载玻片用May-Gruenwald / Giemsa溶液染色，用于常规评估多色红细胞（PCE）和正常红细胞（NCE）中的微核（MN）频率。将剩余的未染色载玻片储存在-20℃，通过用小鼠DNA探针鉴定MN的来源，区分致裂和气动作用。对于每只动物，对1000个编码载玻片的PCE评分是否存在MN。此外，记录每只动物1000 NCE中PCE的数量以评估骨髓抑制，并且有丝分裂活性计算为％PCE = [PCE /（PCE + NCE）]×100 [1]。

[参考文献]

[1]. Attia SM, et al. Molecular cytogenetic evaluation of the aneugenic effects of teniposide in somatic and germinal cells of male mice. Mutagenesis. 2012 Jan;27(1):31-9.

[2]. Li J, et al. Topoisomerase II trapping agent teniposide induces apoptosis and G2/M or S phase arrest of oral squamous cell carcinoma. World J Surg Oncol. 2006 Jul 6;4:41.

[3]. Sun YC, et al. MiR-181b sensitizes glioma cells to teniposide by targeting MDM2. BMC Cancer. 2014 Aug 25;14:611.

[相关活性小分子]

替尼泊苷物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
864.3±65.0 °C at 760 mmHg

[ 熔点 ]:
274 - 277ºC

[ 分子式 ]:
C₃₂H₃₂O₁₃S

[ 分子量 ]:
656.654

[ 闪点 ]:
476.5±34.3 °C

[ 精确质量 ]:
656.156372

[ PSA ]:
189.07000

[ LogP ]:
1.71

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

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.697

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
水溶性：不溶；水溶解度：5.9 mg/l 25 °C

替尼泊苷MSDS

详细MSDS(安全技术说明书)

替尼泊苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KC0180000

CHEMICAL NAME :: Epipodophyllotoxin, 4'-demethyl-, 9-(4,6-O-2-thenylidene-beta-D-glucopyranoside)

CAS REGISTRY NUMBER :: 29767-20-2

LAST UPDATED :: 199801

DATA ITEMS CITED :: 44

MOLECULAR FORMULA :: C32-H32-O13-S

MOLECULAR WEIGHT :: 656.70

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 9579 mg/kg

TOXIC EFFECTS :: Behavioral - anorexia (human) Gastrointestinal - nausea or vomiting Skin and Appendages - hair

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 26 mg/kg/10D-I

TOXIC EFFECTS :: Blood - agranulocytosis Blood - aplastic anemia Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 132 mg/kg/7W-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Blood - leukopenia

TYPE OF TEST :: LD17 - Lethal Dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 15 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - hypermotility, diarrhea Blood - leukopenia

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 29570 ug/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31560 ug/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 168 mg/kg/4W-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 18 mg/kg/7D-I

TOXIC EFFECTS :: Gastrointestinal - other changes Liver - changes in liver weight Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1 mg/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - respiratory system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1 mg/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1 mg/kg

SEX/DURATION :: female 6 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - oogenesis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1 mg/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material)

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Primate - monkey Kidney

DOSE/DURATION :: 100 umol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 48,1722,1988 *** REVIEWS *** TOXICOLOGY REVIEW EJCAAH European Journal of Cancer. (Oxford, UK) V.1-17(6), 1965-1981. For publisher information, see EJCODS. Volume(issue)/page/year: 9,477,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X7293 No. of Facilities: 7 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 14 (estimated) No. of Female Employees: 14 (estimated)

替尼泊苷安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H350

[ 警示性声明 ]:
P201-P308 + P313

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S36

[ 危险品运输编码 ]:
3276

[ WGK德国 ]:
3

[ RTECS号 ]:
KC0180000

替尼泊苷文献

Pathologic risk-based adjuvant chemotherapy for unilateral retinoblastoma following enucleation.

J. Pediatr. Hematol. Oncol. 36(6) , e335-40, (2014)

There are no standardized diagnostic or treatment guidelines for patients with advanced unilateral retinoblastoma.Patients with advanced unilateral retinoblastoma were prospectively treated after enuc...

Action of db-cAMP on the bystander effect and chemosensitivity through connexin 43 and Bcl-2-mediated pathways in medulloblastoma cells.

Oncol. Rep. 28(3) , 969-76, (2012)

Medulloblastoma (MB) is one of the most common malignant brain tumors of childhood and is associated with a poor prognosis. Gap-junctional intercellular communication (GJIC) is an important mode for c...

Dose intensification of methotrexate and cytarabine during intensified continuation chemotherapy for high-risk B-precursor acute lymphoblastic leukemia: POG 9406: a report from the Children's Oncology Group.

J. Pediatr. Hematol. Oncol. 36(5) , 353-61, (2014)

To determine the efficacy and toxicity of higher dose versus standard dose intravenous methotrexate (MTX) and pulses of high-dose cytosine arabinoside with asparaginase versus standard dose cytosine a...

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