Pinosylvin 是从 Pinus spp 的心材中分离出来的一种感染前的类苯乙烯类毒素,具有抗菌 (anti-bacterial) 活性。 Pinosylvin 是一种白藜芦醇的类似物,可以诱导白血病细胞凋亡 (apoptosis) 和自噬 (autophapy)。
Pinosylvin(静脉注射; 10 mg / kg)产生的血浆AUC,尿液t,CL和Vd值分别为5.23±1.20 mgh mL-1、13.13±2.05 h,1.84±0.44 Lh-1kg-1和2.29 Lkg-1, 在一项PK研究中,分别在雄性Sprague-Dawley大鼠中。
Pinosylvin(0-100μM; 24小时)对THP-1和U937细胞具有细胞毒性,在白血病细胞中的IC50值为20-30μM,孵育24小时后最大的细胞毒性作用发生在100μM。
Pinosylvin(0-100μM; 24小时)以50μM的浓度增加U937群体中膜联蛋白V +和PI +细胞的数量,以100μM的浓度增加THP-1群体中膜联蛋白V +和PI +细胞的数量。
Pinosylvin(0-100μM; 24小时)通过增强白血病细胞中LC3-II和p62 / SQSTM1降解的水平来促进白血病细胞自噬。
Pinosylvin 是从 Pinus spp 的心材中分离出来的一种感染前的类苯乙烯类毒素,具有抗菌 (anti-bacterial) 活性。 Pinosylvin 是一种白藜芦醇的类似物,可以诱导白血病细胞凋亡 (apoptosis) 和自噬 (autophapy)。
Pinosylvin (0-100 μM; 24 hours) is cytotoxic to THP‐1 and U937 cells, exhibits an IC
50
value of 20-30 μM in leukemia cells, the maximal cytotoxic effect occurred at 100 μM following incubation for 24 hr.
Pinosylvin (0-100 μM; 24 hours) enhances the number of annexin V
+
and PI
+
cells in the U937 population at 50 μM, increases annexin V
+
and PI
+
cells in the THP‐1 population at 100 μM.
Pinosylvin (0-100 μM; 24 hours) promotes autophagy in leukemia cells by enhancing the level of LC3‐II and p62/SQSTM1 degradation in leukemia cells.
Cell Viability Assay
Cell Line:
|
Leukemia cells
|
Concentration:
|
0 μM; 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
|
Incubation Time:
|
24 hours
|
Result:
|
Was cytotoxic to leukemia cells at high concentrations.
|
Apoptosis Analysis
Cell Line:
|
U937 and THP‐1 cells
|
Concentration:
|
0 μM; 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
|
Incubation Time:
|
24 hours
|
Result:
|
Induced apoptosis cell number in U937 and THP‐1 cells.
|
Western Blot Analysis
Cell Line:
|
U937 and THP‐1 cells
|
Concentration:
|
0 μM; 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
|
Incubation Time:
|
24 hours
|
Result:
|
Induced autophagy in leukemia cells.
|
化学性质
类白色粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于山药,虎杖。
用途
赤松素具有抗菌的作用。