丁福明

生物活性体外研究体内研究

丁福明

CAS号:692-13-7
英文名:1-butylbiguanide
中文名:丁福明
CBNumber:CB7913312
分子式:C6H15N5
分子量:157.2168
MOL File:692-13-7.mol

丁福明化学性质

熔点 :174-176 °C
沸点 :271.89°C (rough estimate)
密度 :1.0291 (rough estimate)
折射率 :1.8070 (estimate)
酸度系数(pKa) :12.27±0.10(Predicted)

丁福明性质、用途与生产工艺

生物活性 Buformin (1-Butylbiguanide) 是一种有效的 AMPK 活化剂，也是具有口服活性的双胍类降血糖试剂 (antidiabetic agent)。Buformin 降低肝糖异生并降低血糖生成。Buformin 也具有抗癌活性，可以应用于癌症研究，如宫颈癌、乳腺癌等。

体外研究

Buformin (0-10 mM; 5 days) inhibits SKBR3 and BT474 cells growth as a concentration-dependent manner, exhibits IC ₅₀ values of 246.7 μM and 98.6 μM for erbB-2-overexpressing SKBR3 and BT474 cells, respectively.Buformin (0-3 mM; 48 hours) increases the percentage of cells in G0/G1 phase and reduced the percentage of cells in S phase, especially in the SKBR3 cells.Buformin (0-3 mM; 24 hours) suppresses RTK activation, including erbB-2 and IGF1R signaling downstream, and Akt activation/phosphorylation is inhibited in both SKBR3 and BT474 cells.

Cell Viability Assay

Cell Line:	ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration:	0 μM, 1 μM, 3 μM, 10 μM, 30 μM, 100 μM, 300 μM, 1, 3, or 10 mM
Incubation Time:	5 days
Result:	Reduced cell viability in erbB-2-overexpressing breast cells.

Cell Cycle Analysis

Cell Line:	ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration:	0.5 mM; 1 mM; 3 mM
Incubation Time:	48 hours
Result:	Increased cells arresting in G0/G1 phase.

Western Blot Analysis

Cell Line:	ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration:	0 mM, 0.1 mM, 0.3 mM, 1 mM, or 3 mM
Incubation Time:	24 hours
Result:	Decreased p-AMPK, p-p706S, p-ERK1/2 expression in a concentration-dependent manner.

体内研究

Buformin (oral administation; 7.6 mmol/kg of chow; 7 days) exhibits significantly reduced tumor volumes and weights, and hinders mammary morphogenesis and proliferation in MMTV-erbB-2 transgenic mice

Animal Model:	Female MMTV-erbB-2 transgenic mice
Dosage:	7.6 mmol/kg
Administration:	Oral administation; 7 days
Result:	Inhibited mammary syngeneic tumor growth in MMTV-erbB-2 transgenic mice.