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细胞松弛素 B

细胞松弛素 B用途

Cytochalasin B 是一种能透过细胞的真菌毒素,能够与肌动蛋白丝的有刺端结合,扰乱肌动蛋白聚合物的形成,对 F-actin 的 Kd 值为 1.4-2.2 nM。

细胞松弛素 B名称

[ CAS 号 ]:
14930-96-2

[ 中文名 ]:
细胞松弛素B

[ 英文名 ]:
Cytochalasin B

[中文别名 ]:

细胞松弛素 B

[英文别名 ]:

EINECS 239-000-2
Phomin
Cytochalasin B
MFCD00077704

细胞松弛素 B生物活性

[ 描述 ]:

Cytochalasin B 是一种能透过细胞的真菌毒素,能够与肌动蛋白丝的有刺端结合,扰乱肌动蛋白聚合物的形成,对 F-actin 的 Kd 值为 1.4-2.2 nM。

[ 相关类别 ]:

信号通路 >> 细胞骨架 >> Arp2/3复合物

研究领域 >> 癌症

天然产物 >> 其他

[ 靶点 ]

Kd: 2.2 nM (F-actin, with Mg2+), 1.4 nM (F-actin, with Mg2+/K+)[1]

[体外研究]

细胞松弛素B是一种细胞可渗透的霉菌毒素,与肌动蛋白丝的带刺末端结合,抑制肌动蛋白丝的延长和缩短,在MgCl2(2 mM)或MgCl2存在下,F-actin的Kds为2.2 nM和1.4 nM(分别为2 mM)和KCl [1]。细胞松弛素B(0.1-10μM)对多种小鼠癌细胞系均有抑制作用,IC50分别为2.56μM(M109c),10.46μM(B16BL6),105.5μM(P388/ADR),51.9μM(P388/S)和IC80s处理3 h后,12.23μM(M109c),44.86μM(B16BL6),188.4μM(P388/ADR),84.1μM(P388/S),IC50为0.25μM(M109c),0.37μM(B16F10),0.87处理4天后,μM(B16BL6)和0.80μM(M109c),1.21μM(B16F10),10.41μM(B16BL6)的IC80s [2]。细胞松弛素B(6μM)增加了肌原纤维碎裂指数(MFI),这是由于肌原纤维蛋白强烈分裂成短片段。细胞松弛素B还加速肌动蛋白丝的破坏。此外,细胞松弛素B加速了从F-肌动蛋白到G-肌动蛋白的转化,降低了F-肌动蛋白的含量,并在死后调理过程中显着增加了G-肌动蛋白条带[3]。

[体内研究]

细胞松弛素B(10,25,50mg/kg,ip)剂量依赖性地增加携带P388/ADR白血病的Balb/c小鼠的预期寿命。 50mg/kg的细胞松弛素B在多药耐药P388/ADR组中产生10％的长期存活率,在药物敏感的P388/S组中产生40％的长期存活[2]。

[细胞实验]

在细胞松弛素B处理前1天，将附着的细胞系M109c，B16BL6和B16F10以1至4×10 4个细胞/ mL接种于24孔培养板中2mL体积.P388 / ADR细胞的悬浮培养物接种在细胞松弛素B处理之前，以5×10 4个细胞/ mL培养过夜。用细胞松弛素B处理细胞3小时，以及2,3或4天。在连续暴露2,3或4天的情况下，将附着的细胞用胰蛋白酶消化并用血细胞计数器计数。用Coulter计数器计数白血病细胞悬浮液。在短期暴露的情况下，用新鲜培养基洗涤细胞两次，然后用胰蛋白酶消化（P388 / ADR细胞除外），重新接种，并使其再生长3天，此时将它们计数。生长结果计算为与未处理的对照细胞相比在接种密度之上产生的细胞数，并以图形方式显示为对照增加的百分比[2]。

[动物实验]

小鼠[2]对于化学疗法测试，在200μL体积下用2×105锥虫蓝阴性P388 / S或P388 / ADR细胞皮下（sc）攻击异氟烷麻醉下的Balb / c小鼠。保留未处理的小鼠以确定攻击的致死性而无需化学治疗干预。长期存活定义为在观察期间存活的受攻击小鼠。细胞松弛素B和D以悬浮形式制备在2％羧甲基纤维素1％吐温20（CMC / Tw）中，用于腹膜内（ip）给药。在初始攻击后第1-8天，将同源物或载体给予白血病攻击的小鼠[2]。

[参考文献]

[1]. Theodoropoulos PA, et al. Cytochalasin B may shorten actin filaments by a mechanism independent of barbed end capping. Biochem Pharmacol. 1994 May 18;47(10):1875-81.

[2]. Trendowski M, et al. Chemotherapy with cytochalasin congeners in vitro and in vivo against murine models. Invest New Drugs. 2015 Apr;33(2):290-9.

[3]. Zhou C, et al. The effect of Cytochalasin B and Jasplakinolide on depolymerization of actin filaments in goose muscles during postmortem conditioning. Food Res Int. 2016 Dec;90:1-7.

[相关活性小分子]

N-[2-(2-甲基-1H-吲哚-3-基)乙基]-2-噻吩甲酰胺 | CK-869

细胞松弛素 B物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
740.6±60.0 °C at 760 mmHg

[ 熔点 ]:
218-223ºC

[ 分子式 ]:
C₂₉H₃₇NO₅

[ 分子量 ]:
479.608

[ 闪点 ]:
401.7±32.9 °C

[ 精确质量 ]:
479.267181

[ PSA ]:
95.86000

[ LogP ]:
3.71

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±2.6 mmHg at 25°C

[ 折射率 ]:
1.596

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
ethanol: 20 mg/mL

细胞松弛素 BMSDS

详细MSDS(安全技术说明书)

细胞松弛素 B毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RO0205000

CHEMICAL NAME :: 2H-Oxacyclotetradec(2,3-d)isoindole-2,18(5H)-dione, 16-benzyl-6,7,8,9,10,12a,13,14,15,15a, 16,17-dodecahydro-5,13-dihydroxy-9,15-dimethyl-14-met hylene-, (E)-(5S,9R,12aS,13S,15S,15aS, 16aS,18aS)-

CAS REGISTRY NUMBER :: 14930-96-2

LAST UPDATED :: 199612

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C29-H37-N-O5

MOLECULAR WEIGHT :: 479.67

WISWESSER LINE NOTATION :: T56-14- 1A U AXVM GY TVO JU RUTJ D1R& F1 GU1 HQ M1 QQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 11 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Behavioral - coma Lungs, Thorax, or Respiration - cyanosis

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 30 mg/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 :: Oral

DOSE :: 1500 ug/kg

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

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 5 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - Central Nervous System

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Mammal - species unspecified Bone marrow

DOSE/DURATION :: 1 gm/L

REFERENCE :: TSITAQ Tsitologiya. Cytology. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.1- 1959- Volume(issue)/page/year: 24,814,1982

细胞松弛素 B安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H330

[ 警示性声明 ]:
P260-P284-P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
T+: Very toxic;

[ 风险声明 (欧洲) ]:
R26/27/28;R63

[ 安全声明 (欧洲) ]:
28-36/37-45

[ 危险品运输编码 ]:
UN 1544 6

[ WGK德国 ]:
3

[ RTECS号 ]:
RO0205000

[ 包装等级 ]:
I

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
29349990

细胞松弛素 B合成路线

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细胞松弛素 B文献

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