石松鹼
- CAS号:466-61-5
- 英文名:lycopodine
- 中文名:石松鹼
- CBNumber:CB41480614
- 分子式:C16H25NO
- 分子量:247.38
- MOL File:466-61-5.mol
- 熔点 :114-115°; mp (racemate) 130-131°
- 比旋光度 :D -24° (alc)
- 沸点 :125 °C(Press: 0.2 Torr)
- 密度 :1.18 g/cm3
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :9.36±0.40(Predicted)
- 旋光性 (optical activity) :-24.521 (c 1.1, ethanol)
石松鹼性质、用途与生产工艺
- 生物活性 Lycopodine，一种石松 (Lycopodium clavatumspores) 孢子重要的生物活性成分，通过调节难治性前列腺癌细胞中 5-脂氧合酶 (5-lipoxygenase)，极化线粒体膜电位而不调节 p53 活性来诱导细胞凋亡。 Lycopodine 通过激活 caspase-3 诱导细胞凋亡来抑制 HeLa 细胞的增殖。
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靶点
Caspase-3
5-Lipoxygenase
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体外研究
Lycopodine (5.22-78.3 μg/mL; 12 hours) has 50% viability at 57.62±0.086 μg/mL and 51.46±1.43 μg/mL for PC3 and LnCaP, respectively.
Treated with Lycopodine (74-222 mM; 12 hours), the apoptotic index is with respect to the gradual increase in doses for the PC3 and LnCaP cells.
Lycopodine (74-222 mM; 12 hours) induces cell cycle arrest at G0/G1 phase in PC3 and LnCaP cells.
Lycopodine (0-200 µg/mL; 48 hours) shows cytotoxicity to HeLa cells in a dose and time dependent manner. However, Lycopodine shows minimal cytotoxic effects in normal peripheral blood mononuclear cells (PBMC) even at the highest dose (200 µg/mL).
Lycopodine (100, 200 µg/mL; 24 hours) increases level of Bax and decreases the mitochondrial cytochrome c. This is followed by an increase in expression of cytochrome c in cytosolic fraction. Lycopodine also cleaves the caspase-3 in the total cell lysate, while the expression of Bcl-2 is down regulated.
Cell Viability Assay
Cell Line: PC3 and LnCaP cells Concentration: 5.22-78.3 μg/mL Incubation Time: 12 hours Result: Reached 50% viability at 57.62±0.086 μg/mL and 51.46±1.43 μg/mL for PC3 and LnCaP, respectively. Apoptosis Analysis
Cell Line: PC3 and LnCaP cells Concentration: 74, 148, 222 mM Incubation Time: 12 hours Result: The apoptotic index was with respect to the gradual increase in doses. Cell Cycle Analysis
Cell Line: PC3 and LnCaP cells Concentration: 74, 148, 222 mM Incubation Time: 12 hours Result: Arrested growth of the cells at G0/G1 phase in the case of PC3 and LnCaP cells. Cell Cytotoxicity Assay
Cell Line: Hela cells and PBMC Concentration: 0-200 µg/mL Incubation Time: 48 hours Result: A linear increase of the cytotoxicity was along with the increase of time of treatment and also of the dose. Western Blot Analysis
Cell Line: HeLa cells Concentration: 100, 200 µg/mL Incubation Time: 24 hours Result: Increased level of Bax and decreased the mitochondrial cytochrome c.
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