dictyostatin

Names

[ Name ]:
dictyostatin

[Synonym ]:
(-)dictyostatin
dicytostatin
(3Z,5E,11Z)-(7R,8S,10S,13S,14R,15S,17S,20R,21S,22S)-8,10,14,20-Tetrahydroxy-7,13,15,17,21-pentamethyl-22-((Z)-(S)-1-methyl-penta-2,4-dienyl)-oxacyclodocosa-3,5,11-trien-2-one
(-)-dictyostatin
dictyostatin 1
(7R,8S,10S,13S,14R,15S,17S,20R,21S,22S)-8,10,14,20-tetrahydroxy-7,13,15,17,21-pentamethyl-22-((1S)-1-methylpenta-2,4-dienyl)oxacyclodocosa-3,5,11-trien-2-one

Biological Activity

[Description]:

Dictyostatin ((-)-Dictyostatin; Dictyostatin 1) is a potent microtubule stabilizing agent. Dictyostatin also is a anti-cancer agent. Dictyostatin shows antiproliferative activity. Dictyostatin has the potential for the research of tauopathies[1][2][3].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[In Vitro]

Dictyostatin (0-100 nM; 72-120 h) 在癌细胞中显示出抗增殖活性[2]。 Cell Viability Assay[2] Cell Line: A549, EpoB40/A549, 1A9, 1A9/PTX10, 1A9/PTX22 cells Concentration: 0-100 nM Incubation Time: 72-120 h Result: Showed antiproliferative activity with GI50s of 0.5, 5.1, 1.3, 18.8, 5.1 nM for A549, EpoB40/A549, 1A9, 1A9/PTX10, 1A9/PTX22 cells, respectively.

[In Vivo]

Dictyostatin (0.3、1 mg/kg；腹腔注射；每周一次，持续 3 个月) 可改善小鼠的 MT 密度并减少轴突营养不良[3]。 Animal Model: 6-month old male B6 PS19 tau Tg mice[3] Dosage: 0.3, 1 mg/kg Administration: I.p.; once-weekly for 3 months Result: Improved MT density and reduced axonal dystrophy, with a reduction of tau pathology and a trend toward increased hippocampal neuron survival relative to vehicle-treated PS19 mice, caused a significant reduction of insoluble TauAcK280.

[References]

[1]. George R. Pettit, et al. Isolation and structure of the cancer cell growth inhibitor dictyostatin 1. J. Chem. Soc., Chem. Commun., 1995, 2373-2670.

[2]. Vollmer LL, et al. A simplified synthesis of novel dictyostatin analogues with in vitro activity against epothilone B-resistant cells and antiangiogenic activity in zebrafish embryos. Mol Cancer Ther. 2011 Jun;10(6):994-1006.

[3]. Makani V, et al. Evaluation of the brain-penetrant microtubule-stabilizing agent, dictyostatin, in the PS19 tau transgenic mouse model of tauopathy. Acta Neuropathol Commun. 2016 Sep 29;4(1):106.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₅₂O₆

[ Molecular Weight ]:
532.75200

[ Exact Mass ]:
532.37600

[ PSA ]:
107.22000

[ LogP ]:
5.14320

Related Compounds

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