生物活性

• 描述Leurocristine Sulfate is an inhibitor for polymerization of microtubules with IC50 value of 32μM. It inhibited assembly-end addition with IC50 value of 0.085μM and exhibited 50% cell proliferation inhibition effect shown as >2 fold compared with vinblastine. Besides, the inhibitor could decrease the tumor growth in L-cells with a ratio of 57% compared to non-drug treatment control which could also be potential to inhibit cell proliferation and tumor production in B16 melanoma cells. In HepG2.2.15 and HepG2-HBV1.1 cells, 0.1 μM Leurocristine showed no significant cytotoxicity to both of them. HBV DNA copies were up-regulated by 4 fold and 5.6 fold in the two cells, respectively. Meanwhile, the secretion of HBV DNA copies and the expression of HBV pgRNA were improved. The intracellular HBsAg and HBcAg expression were also increased significantly. Most importantly, Leurocristine at 0.1μM also declined the proliferation rate by 60% in the stable HBV-expressing cell lines while it was 55% in the two cells mentioned above. This compound could also induce cell cycle arrest at S-phase while decrease the numbers of cells at G1/G0 and G2/M phases. SH-SY5Y cells treated with 0.1μM Leurocristine for different time caused decrease of the percentage of G0 /G1 phase cells gradually from 76.26% to 16.46%, while the percentage of G2/M phase cells increased gradually from 20.60% to 72.34%. The percentage of cells at sub-G1 phase increased from 5.75% to 21.25%. These treated SH-SY5Y cells also exhibited distinct changes in the microtubular structure by causing cell cycle arrest at the M phase and time-course premature termination of mitosis .
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  A-172	0.1 μM	Growth Inhibition Assay	24/72 h	inhibits cell growth time dependently	24530235
  A2780	-	Growth Inhibition Assay	-	IC50=3.5 mM	23829203
  A549	-	Growth Inhibition Assay	-	IC50=0.10 ± 0.03 μM	23971075

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• 动物研究
  剂量	Dog: 1 mg/kg[3] (i.v.) Monkey: 1 mg/kg - 4 mg/kg[3] (i.v.) Rat: 0.025 mg/kg - 0.5 mg/kg[3] (i.v.)
  给药途径	i.v.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02568683	Non-Hodgkin Lymphoma	Phase 1 Phase 2	Completed	-	United States, Mississippi ... more >> Forrest General Hospital Hattiesburg, Mississippi, United States United States, South Carolina Medical University of South Carolina Charleston, South Carolina, United States France Groupe Hospitalier du Haut Leveque Pessac, Aquitaine, France Centre Hospitalier Régional Universitaire de Lille (CHRU de Lille) Lille cedex, Nord Pas-de-calais, France Institut Paoli Calmettes Marseille, Provence Alpes Cote D'azur, France Centre Hospitalier Universitaire de Dijon Hôpital du Bocage Dijon Cedex, France Centre Hospital Lyon Sud Pierre Benite, France Collapse <<
  NCT00335738	Intraocular Retinoblastoma	Phase 3	Completed	-	-
  NCT00003935	Brain Tumors ... more >>Central Nervous System Tumors Collapse <<	Phase 1	Completed	-	-

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