Bryostatin 1

Bryostatin 1用途

Bryostatin 1 是一种天然的大环内酯类化合物,从苔藓虫 Bugula neritina 中分离出来,也是一种有效的中枢神经系统 (CNS) 渗透性的 PKC 调节剂。Bryostatin 1 以 Ki 值为 8.07 nM 和 0.45 nM 分别结合到分离的 Munc13-1 的 C1 域和全长的 Munc13-1 蛋白。Bryostatin 1 具有抗癌,抗炎,神经保护,抗 HIV-1 感染的特性。

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Bryostatin 1名称

[ CAS 号 ]:
83314-01-6

[ 英文名 ]:
Bryostatin 1

[英文别名 ]:

MFCD00893832
bryostatin1,0
BRYO 1
bryostatine-1
BRYOSTATIN 1
BRYOSTATIN

Bryostatin 1生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 癌症

信号通路 >> 抗感染 >> HIV

研究领域 >> 感染

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

PKC[1] HIV-1[4]

[体外研究]

Bryostatin 1(1μM；5分钟；HT22细胞)处理成功地将Munc13-1从细胞溶胶招募到质膜。Bryostatin 1对其他Munc13家族成员ubMunc13-2和bMunc13-2的影响与Munc13-1的易位作用相似[1]。用Bryostatin 1孵育24小时后,在HT22和原代小鼠海马细胞中观察到Munc13-1表达水平的增加[1]。Bryostatin 1还可以通过MyD88独立途径通过toll样受体4(TLR4)调节树突状细胞(dc),从而影响免疫系统,该途径通过诱导2型表型促进CD4+T辅助(Th)淋巴细胞分化为Th2和Th1效应细胞,从而有利于抗炎环境[2]。Western Blot分析[1]细胞株：HT22细胞浓度：1μM孵育时间：5分钟结果：导致Munc13-1向膜部分转移。

[体内研究]

Bryostatin 1(30μg/kg；腹腔注射；每周3d；持续2周；C57BL/6J小鼠)治疗可消除EAE的发生[2]。动物模型：雌性C57BL/6J小鼠(8-12周龄),MOG35-55[2]剂量：30μg/kg,腹腔注射,每周3d,连续2周,结果：消除了实验性自身免疫性脑脊髓炎(EAE)的发病。

[参考文献]

[1]. Blanco FA, et al. Munc13 Is a Molecular Target of Bryostatin 1. Biochemistry. 2019 Jul 9;58(27):3016-3030.

[2]. Kornberg MD, et al. Bryostatin-1 alleviates experimental multiple sclerosis. Proc Natl Acad Sci U S A. 2018 Feb 27;115(9):2186-2191.

[3]. Zeng N, et al. Bryostatin 1 causes attenuation of TPA-mediated tumor promotion in mouse skin. Mol Med Rep. 2018 Jan;17(1):1077-1082.

[4]. Proust A, et al. HIV-1 infection and latency-reversing agents bryostatin-1 and JQ1 disrupt amyloid beta homeostasis in human astrocytes. Glia. 2020 Apr 6.

Bryostatin 1物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
954.7±65.0 °C at 760 mmHg

[ 分子式 ]:
C₄₇H₆₈O₁₇

[ 分子量 ]:
905.033

[ 闪点 ]:
270.0±27.8 °C

[ 精确质量 ]:
904.445679

[ PSA ]:
240.11000

[ LogP ]:
5.39

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.565

Bryostatin 1MSDS

详细MSDS(安全技术说明书)

Bryostatin 1毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EH9455000

CHEMICAL NAME :: Bryostatin 1

CAS REGISTRY NUMBER :: 83314-01-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C47-H68-O17

MOLECULAR WEIGHT :: 905.15

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 400 nmol/kg

REFERENCE :: CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 9,555,1988

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Bryostatin 1安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

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

[ RTECS号 ]:
EH9455000

Bryostatin 1文献

Bryostatin-1 promotes long-term potentiation via activation of PKCα and PKCε in the hippocampus.

Neuroscience 226 , 348-55, (2012)

Activation of protein kinase C (PKC) by bryostatin-1 affects various functions of the central nervous system. We explored whether bryostatin-1 influenced synaptic plasticity via a process involving PK...

Bryostatin-I: A dendritic cell stimulator for chemokines induction and a promising adjuvant for a peptide based cancer vaccine

Cytokine 52(3) , 238-44, (2010)

Bryostatin-1 (Bryo-1), a PKC modulator, was previously shown to activate monocytes and lymphocytes to produce cytokines. In this report, we investigated the adjuvanticity of Bryo-1 both in vitro and i...

Differentiation therapy in poor risk myeloid malignancies: Results of a dose finding study of the combination bryostatin-1 and GM-CSF.

Leuk. Res. 35(1) , 87-94, (2011)

Pharmacologic differentiating agents have had relatively limited clinical success outside of the use of ATRA in acute promyelocytic leukemia and DNA methyltransferase inhibitors in myelodysplastic syn...

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