甘草西定性質(zhì)、用途與生產(chǎn)工藝
研究發(fā)現(xiàn)，甘草西定對(duì)耐甲氧西林金黃色葡萄球菌等耐藥菌以及多種口腔致病菌具有抗菌活性，在腫瘤的防治方面也發(fā)揮了積極的作用。此外，甘草西定還具有抗炎、調(diào)節(jié)免疫、抗氧化、神經(jīng)保護(hù)等藥理活性。
Licoricidin (LCD) 從甘草 Glycyrrhiza uralensis Fisch 中分離，具有抗癌活性。Licoricidin (LCD) 通過(guò)誘導(dǎo)周期停滯，誘導(dǎo)細(xì)胞凋亡 (apoptosis) 和自噬 (autophagy)，可用于結(jié)直腸癌的研究。Licoricidin (LCD) 通過(guò)抑制腫瘤血管生成和淋巴管生成以及腫瘤組織局部微環(huán)境的變化抑制肺轉(zhuǎn)移。Licoricidin (LCD) 通過(guò)體外和體內(nèi) Akt 和 NF-κB 途徑的失活，增強(qiáng)吉西他濱誘導(dǎo)的骨肉瘤 (OS) 細(xì)胞的細(xì)胞毒性。Licoricidin (LCD) 通過(guò) ROS 清除阻斷 UVA 誘導(dǎo)的光老化，限制 MMP-1 的活性，被認(rèn)為是新的局部應(yīng)用的抗衰老制劑中的活性成分。
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
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Cell Line:
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SW480, HCT116, SW620 and LoVo cells
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Concentration:
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0-20 μM
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Incubation Time:
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24 hours
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Result:
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Decreased colon cancer cell lines viability.
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Western Blot Analysis
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Cell Line:
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SW480 cells
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Concentration:
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0 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:
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0 hours, 1 hour, 3 hours, 6 hours, 12 hours
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Result:
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Induced cell apoptosis.
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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.
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Animal Model:
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SW480 xenografted tumor growth in nude mice
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Dosage:
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5, 10, or 20 mg/kg
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Administration:
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Intraperitoneal injection; once daily; 15 days
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Result:
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Decreased tumor volumes.
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Animal Model:
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BALB/c mouse orthotopic model
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Dosage:
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5, 10, or 20 mg/kg
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Administration:
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Intraperitoneal injection; 5, 10, or 20 mg/kg; once daily; 32 days
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Result:
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Inhibited Lung Metastasis of 4T1 Murine Mammary Carcinoma cells.
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