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环巴胺

环巴胺用途

Cyclopamine 是 Hedgehog 通路的拮抗剂,在细胞实验中的 IC50 为 46 nM。

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环巴胺名称

[ CAS 号 ]:
4449-51-8

[ 中文名 ]:
环巴胺

[ 英文名 ]:
Cyclopamine

[中文别名 ]:

环杷明

[英文别名 ]:

11-DEOXYJERVINE
alkaloidv
deoxojervine
11-Desoxo-jervin
Veratraman-3-ol, 17,23-epoxy-, (3β,23β)-
Cyclopamine
(3β,22S,23R)-17,23-Epoxyveratraman-3-ol
11-deoxojervine
MFCD01735266
(3β,17β,22S,23R)-17,23-Epoxyveratraman-3-ol

环巴胺生物活性

[ 描述 ]:

Cyclopamine 是 Hedgehog 通路的拮抗剂,在细胞实验中的 IC50 为 46 nM。

[ 相关类别 ]:

信号通路 >> 干细胞及 Wnt 通路 >> Hedgehog

天然产物 >> 类固醇

研究领域 >> 癌症

[ 靶点 ]

IC50: 46 nM (Hedgehog, in Hh cell assay)[1]

[体外研究]

用小分子Hh抑制剂如HhAntag和天然产物Cyclopamine(均与Smo结合)治疗可诱导成神经管细胞瘤基因小鼠模型的肿瘤缓解[1]。环巴胺是一种Hedgehog(Hh)通路拮抗剂。环巴胺抑制细胞生长。环巴胺(3μM)抑制Hh通路活性和消化道肿瘤细胞系的生长与PTCHmRNA的表达相关[2]。 Cyclopamine是一种甾体生物碱,通过与Smo的直接相互作用抑制Hh信号传导[3]。

[体内研究]

环巴胺导致异种移植肿瘤持续消退。环巴胺治疗动物的肿瘤完全消退12天[2]。环巴胺(1.2 mg)治疗在移植入裸鼠后阻断人胰腺癌细胞的肿瘤形成[3]。

[细胞实验]

将细胞在96孔板中一式三份培养在测定培养基中，在0h以正文中指出的浓度加入5E1单克隆抗体，ShhNp和/或环巴胺（3μM）。使用CellTiter96比色测定，通过在490nm（OD490）在2天和4天的光密度测量来确定活细胞质量。相对生长计算为OD（第4天）-OD（第2天）/ OD（第2天）[2]。

[动物实验]

小鼠[3]将总共0.1mL Hanks'平衡盐溶液和含有2×106个细胞的基质胶（1：1）皮下注射到CD-1裸鼠中。使肿瘤生长4天至最小体积125mm 3;对所有受试者同时开始治疗。每天皮下注射小鼠皮下注射载体（三油酸甘油酯：乙醇4：1v / v）或环巴胺悬浮液（每小鼠1.2mg三油酸甘油酯：乙醇4：1v / v），持续7天。在治疗期结束时，从小鼠切下肿瘤，称重，然后在4℃下用4％多聚甲醛固定3小时，包埋在石蜡中并切片（6μm）。使用重组Tdt通过TUNEL鉴定凋亡细胞。然后将切片用曙红复染。从随机选择对应于两个对照和两个环巴胺处理的肿瘤的外部，中间和内部的区域的8×20-放大的视野。我们手动计算了TUNEL阳性细胞核的数量。进行苏木精/伊红染色。

[参考文献]

[1]. Peukert S, et al. Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorg Med Chem Lett, 2009, 19(2), 328-331.

[2]. Berman DM, et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature, 2003, 425(6960), 846-851.

[3]. Thayer SP, et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature, 2003, 425(6960), 851-856.

[4]. Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246.

[相关活性小分子]

维莫地尼 | HPI-4 (Ciliobrevin A) | 蒜藜芦碱 | N-(4-乙氧基苯基)-4-(2-甲基咪唑并[1,2-a]吡啶-3-基)噻唑-2-胺

环巴胺物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
550.8±50.0 °C at 760 mmHg

[ 熔点 ]:
236-238ºC

[ 分子式 ]:
C₂₇H₄₁NO₂

[ 分子量 ]:
411.620

[ 闪点 ]:
286.9±30.1 °C

[ 精确质量 ]:
411.313721

[ PSA ]:
41.49000

[ LogP ]:
5.44

[ 外观性状 ]:
白色结晶固体

[ 蒸汽压 ]:
0.0±3.4 mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Store in Freezer at - 20°C

[ 水溶解性 ]:
DMSO: soluble

环巴胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GY0750000

CHEMICAL NAME :: Cyclopamine

CAS REGISTRY NUMBER :: 4449-51-8

LAST UPDATED :: 199712

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C27-H41-N-O2

MOLECULAR WEIGHT :: 411.69

WISWESSER LINE NOTATION :: L D6 B566 FX DU LUTJ A1 E1 OQ F-& CT56 BOX FMTJ D1 H1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 180 mg/kg

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

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 149,302,1975

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 170 mg/kg

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

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 149,302,1975 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 120 mg/kg

SEX/DURATION :: female 6-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 1,1187,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 300 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 29(2),22A,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 44500 ug/kg

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

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 136,1174,1971

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 116 mg/kg

SEX/DURATION :: female 7-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - eye/ear

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 136,1174,1971

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 250 mg/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 149,302,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 170 mg/kg

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

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 149,302,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 54546 ug/kg

SEX/DURATION :: female 30-31 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 142,1287,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30 mg/kg

SEX/DURATION :: female 14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 192,153,1989 *** REVIEWS *** TOXICOLOGY REVIEW AEMBAP Advances in Experimental Medicine and Biology. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) V.1- 1967- Volume(issue)/page/year: 27,107,1972

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环巴胺安全信息

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 安全声明 (欧洲) ]:
22-24/25

[ WGK德国 ]:
3

[ RTECS号 ]:
GY0750000

环巴胺

环巴胺用途

环巴胺名称

环巴胺生物活性

环巴胺物理化学性质

环巴胺毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

环巴胺安全信息

环巴胺合成路线

详细合成路线

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