Warangalone(Synonyms: 攀登鱼藤异黄酮; Scandenolone)

天然产物 黄酮类 Flavonoids

Warangalone (Synonyms: 攀登鱼藤异黄酮; Scandenolone) 纯度: ≥98.0%

Warangalone 是抗疟疾化合物,能够抑制 3D7 (氯喹敏感) 和 K1 (氯喹耐药) 寄生虫的生长, IC50 值分别为 4.8 μg/mL 和 3.7 μg/mL。 Warangalone 还可以抑制环 AMP 依赖性蛋白激酶催化亚基 (cAK),其 IC50 值为 3.5 μM。

Warangalone(Synonyms: 攀登鱼藤异黄酮; Scandenolone)

Warangalone Chemical Structure

CAS No. : 4449-55-2

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生物活性

Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.

IC50 & Target

IC50: 4.8 μg/mL (3D7), 3.7 μg/mL (K1)[1]
IC50: 3.5 μM (cAK)[2]

体外研究
(In Vitro)

Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively[1]. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM[2]. When HL-60 cells are exposed to Warangalone (30 μM) for 24 h, Warangalone induces a significant decrease (8%) in cell viability compare to controls. Warangalone also inhibits HL-60 cell growth within 24 h in a time-dependent fashion. A time-dependent increase in caspase-9 activity is observed in Warangalone-treated cells[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

404.46

Formula

C25H24O5

CAS 号

4449-55-2

中文名称

攀登鱼藤异黄酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Tati Herlina, et al. ANTI-MALARIAL COMPOUND FROM THE STEM BARK OF Erythrina variegate. Indo. J. Chem., 2009, 9 (2), 308-311.

    [2]. Wang BH, et al. Specific inhibition of cyclic AMP-dependent protein kinase by warangalone and robustic acid. Phytochemistry. 1997 Mar;44(5):787-96.

    [3]. Induction of apoptosis by isoflavonoids from the leaves of Millettia taiwaniana in human leukemia HL-60 cells. Planta Med. 2006 Apr;72(5):424-9.

Kinase Assay
[3]

The enzyme activities of caspase-3 and caspase-9 are measured using a caspase fluorometric assay kit. Cells are seeded in 24-well plates at a density of 3×106 cells per well. After exposure of the cells to Warangalone for the allotted time periods, the cells are washed three times with PBS, and then lysed in a lysis buffer for 10 min on ice. The protein content of the cell lysates is assayed with a Micro BCA reagent. Cell lysates containing 50 μg of protein are incubated with a caspase-3 fluorogenic substrate (DEVD-AFC) or a caspase-9 fluorogenic substrate (LEHD-AFC) for 1 h at 37°C. Caspase activity is measured by fluorometric detection[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[3]

Cell viability is determined using the Cell Titer 96 Aqueous assay kit. Cells are seeded in 96-well plates at a density of 1×105 cells per well. The cells are maintained for 24 h at 37°C and then Warangalone (30 μM) is added to the culture medium. MTS solution is added to the 96-well plates at the indicated time points, and the cells are incubated for 1 h at 37°C. The absorbance is measured at a wavelength of 490 nm with a microplate counter[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Tati Herlina, et al. ANTI-MALARIAL COMPOUND FROM THE STEM BARK OF Erythrina variegate. Indo. J. Chem., 2009, 9 (2), 308-311.

    [2]. Wang BH, et al. Specific inhibition of cyclic AMP-dependent protein kinase by warangalone and robustic acid. Phytochemistry. 1997 Mar;44(5):787-96.

    [3]. Induction of apoptosis by isoflavonoids from the leaves of Millettia taiwaniana in human leukemia HL-60 cells. Planta Med. 2006 Apr;72(5):424-9.