甘草西定

中文名称:

甘草西定

中文同义词:

甘草西定

英文名称:

licoricidin

英文同义词:

licoricidin;7-O-Demethyllicorisoflavan A;Licorisoflavan B;1,3-Benzenediol,4-[(3R)-3,4-dihydro-7-hydroxy-5-methoxy-6-(3-methyl-2-buten-1-yl)-2H-1-benzopyran-3-yl]-2-(3-methyl-2-buten-1-yl)-;LICORICIDIN (LCD)

CAS号:

30508-27-1

分子式:

C26H32O5

分子量:

424.53

EINECS号:

相关类别:

中药对照品;标准品;黄酮

Mol文件:

30508-27-1.mol

熔点 

161.0-162.5℃

沸点 

610.8±55.0 °C(Predicted)

密度 

1.171±0.06 g/cm3(Predicted)

酸度系数(pKa)

10.10±0.40(Predicted)

生物活性

Licoricidin (LCD) 从甘草 Glycyrrhiza uralensis Fisch 中分离，具有抗癌活性。Licoricidin (LCD) 通过诱导周期停滞，诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)，可用于结直肠癌的研究。Licoricidin (LCD) 通过抑制肿瘤血管生成和淋巴管生成以及肿瘤组织局部微环境的变化抑制肺转移。Licoricidin (LCD) 通过体外和体内 Akt 和 NF-κB 途径的失活，增强吉西他滨诱导的骨肉瘤 (OS) 细胞的细胞毒性。Licoricidin (LCD) 通过 ROS 清除阻断 UVA 诱导的光老化，限制 MMP-1 的活性，被认为是新的局部应用的抗衰老制剂中的活性成分。

体外研究

Licoricidin (LCD) (0-20 μM; 24 hours) dose-dependently inhibits the viability of colon cancer cell lines with various pathological and genetic characters, namely SW480, HCT116, SW620 and LoVo cells, with IC 50 values of 7.2, 5.4, 4.5 and 5.1 μM, respectively. Licoricidin (LCD) (0-20 μM; 0-12 hours) induces cell apoptosis was accompanied with the activation of caspase-3 by cleavage in a time- and dose-dependent manner. Licoricidin (LCD) (0-20 μM; 0-12 hours) induces autophagy of SW480 cells, increases the cleavage of LC3-I to LC3-II and the degradation of p62 in a time and dose dependent manner. Licoricidin (LCD) (0-5 μg/ml; 18 hours) inhibits cell migration, MMP-9 secretion, and VCAM expression in 4T1 cells. Cell Viability Assay Cell Line: SW480, HCT116, SW620 and LoVo cells Concentration: 0-20 μM Incubation Time: 24 hours Result: Decreased colon cancer cell lines viability. Western Blot Analysis Cell Line: SW480 cells Concentration: 0 μM, 2.5 μM, 5 μM, 10 μM, 20 μM Incubation Time: 0 hours, 1 hour, 3 hours, 6 hours, 12 hours Result: Induced cell apoptosis.

Cell Line:

SW480, HCT116, SW620 and LoVo cells

Concentration:

0-20 μM

Incubation Time:

24 hours

Result:

Decreased colon cancer cell lines viability.

Cell Line:

SW480 cells

Concentration:

0 μM, 2.5 μM, 5 μM, 10 μM, 20 μM

Incubation Time:

0 hours, 1 hour, 3 hours, 6 hours, 12 hours

Result:

Induced cell apoptosis.

体内研究

Licoricidin (LCD) (intraperitoneal injection; 5, 10, or 20 mg/kg; once daily; 15 days) significantly inhibited the growth of SW480 xenografts in nude mice with an inhibitory rate of 43.5%. Licoricidin (LCD) (intraperitoneal injection; 5, 10, or 20 mg/kg; once daily; 32 days) reduces pulmonary metastasis and the expression of CD45, CD31, HIF-1α, iNOS, COX-2, and VEGF-A in tumor tissues, additionally, decreases protein expression of VEGF-R2, VEGF-C, VEGF-R3, and LYVE-1 in tumor tissues of licoricidin-treated mice. Animal Model: SW480 xenografted tumor growth in nude mice Dosage: 5, 10, or 20 mg/kg Administration: Intraperitoneal injection; once daily; 15 days Result: Decreased tumor volumes. Animal Model: BALB/c mouse orthotopic model Dosage: 5, 10, or 20 mg/kg Administration: Intraperitoneal injection; 5, 10, or 20 mg/kg; once daily; 32 days Result: Inhibited Lung Metastasis of 4T1 Murine Mammary Carcinoma cells.

Animal Model:

SW480 xenografted tumor growth in nude mice

Dosage:

5, 10, or 20 mg/kg

Administration:

Intraperitoneal injection; once daily; 15 days

Result:

Decreased tumor volumes.

Animal Model:

BALB/c mouse orthotopic model

Dosage:

5, 10, or 20 mg/kg

Administration:

Intraperitoneal injection; 5, 10, or 20 mg/kg; once daily; 32 days

Result:

Inhibited Lung Metastasis of 4T1 Murine Mammary Carcinoma cells.