棕矢车菊素

中文名称:

棕矢车菊素

中文同义词:

爵筛奥素;棕矢车菊素;棕矢车菊素、合金欢素;4,5,7-三羟基-3,6-二甲氧基苯并吡喃-4-酮;4,5,7-三羟基-3,6-二甲氧基黄酮;合金欢素;棕矢车菊素(合金欢素,爵筛奥素);棕矢车菊素(标准品)

英文名称:

Jaceosidin

英文同义词:

JACEOSIDIN;3,6-Dimethoxy-4,5,7-trihydroxyflavone;5,7-Dihydroxy-2-(4-hydroxy-3-methoxyphenyl)-6-methoxy-4H-1-benzopyran-4-one;6-Hydroxyluteolin 3,6-dimethyl ether;Jacesiolin;4,5,7-Trihydroxy-3,6-dimethoxyflavone;4H-1-Benzopyran-4-one, 5,7-dihydroxy-2-(4-hydroxy-3-methoxyphenyl)-6-methoxy-;5,7-dihydroxy-2-(4-hydroxy-3-methoxy-phenyl)-6-methoxy-chromen-4-one

CAS号:

18085-97-7

分子式:

C17H14O7

分子量:

330.29

EINECS号:

相关类别:

天然产物;植物提取物;中药对照品;标准品;对照品;医药中间体;分析试剂标准品;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;标准品-中药标准品;标准品-对照品;黄酮;标准品 -中药标准品;标准品，对照品

Mol文件:

18085-97-7.mol

熔点

259-260 °C

沸点

619.0±55.0 °C(Predicted)

密度

1.483±0.06 g/cm3(Predicted)

储存条件

Keep in dark place,Sealed in dry,2-8°C

酸度系数(pKa)

6.47±0.40(Predicted)

应用

从艾叶中分离得到的棕矢车菊素和异泽兰黄素属于环烯醚萜苷类，其主要具有清热、镇痛等相关活性作用。

生物活性

Jaceosidin 是从 Artemisia vestita 中得到的黄酮类化合物，可激活 Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。Jaceosidin 具有抗癌和抗炎作用，能够降低炎性因子水平，激活 NF-κB，抑制 COX-2 的表达。

靶点

Bax COX-2

Bax

COX-2

体外研究

Jaceosidin (30, 50, 75 μM) induces apoptosis in human renal carcinoma Caki cells after treatment for 24 h, shows no obvious effect on normal cells. Jaceosidin (75 μM) reduces MMP levels and causes cytochrome c release into the cytoplasm through Bax activation. Jaceosidin-mediated apoptosis is involved in downregulation of Mcl-1, c-FLIP expression, which is via inhibition of NF-κB and/or Sp1 transcriptional activity. Jaceosidin shows cytostatic activity to HES and HESC cells with IC 50 s of 52.68 and 55.10 μM, and is less cytotocxic on Hec1 A and KLE (IC 50 , 70.54, 147.14 μM, respectively), after treatment for 48 h. Cell Viability Assay Cell Line: Hec1A, KLE, HES and HESC cells Concentration: 3.125, 6.25, 12.5, 25, 50, and 100 μM Incubation Time: 48 hour Result: Showed cytostatic activity to HES and HESC cells with IC 50 s of 52.68 and 55.10 μM, less cytotocxic on Hec1 A and KLE (IC 50 , 70.54, 147.14 μM).

Cell Line:

Hec1A, KLE, HES and HESC cells

Concentration:

3.125, 6.25, 12.5, 25, 50, and 100 μM

Incubation Time:

48 hour

Result:

Showed cytostatic activity to HES and HESC cells with IC 50 s of 52.68 and 55.10 μM, less cytotocxic on Hec1 A and KLE (IC 50 , 70.54, 147.14 μM).

体内研究

Jaceosidin (10 and 20 mg/kg, p.o., once a day for 3 days) blocks carrageenan-induced increase in leukocyte number and protein levels in air pouch exudates in mice. Jaceosidin (10, 20 mg/kg, p.o.) suppresses COX-2 expression and NF-κB activation in mice. Jaceosidin (20 mg/kg, p.o. for 2 hours) reduces hind paw edema volume in rats. Animal Model: 5-week-old male BALB/c mice (23-26 g) Dosage: 10 and 20 mg/kg Administration: P.O. once a day for 3 days Result: Decreased the volumes of exudates (inflammatory markers), cell number and protein levels. Inhibited TNF-α by 46.7% and 50.8%, IL-1β by 46.0% and 44.7%, and PGE2 by 21.7% and 16.9%, respectively, at 20 mg/kg. Blocked COX-2 expression and NF-κB activation. Animal Model: Male Sprague-Dawley rats (180-200 g) Dosage: 20 mg/kg Administration: P.O., for 2 hour Result: Reduced hind paw edema volume by 27.1% at 1 h, and 24.0% at 2 h, respectively.

Animal Model:

5-week-old male BALB/c mice (23-26 g)

Dosage:

10 and 20 mg/kg

Administration:

P.O. once a day for 3 days

Result:

Decreased the volumes of exudates (inflammatory markers), cell number and protein levels. Inhibited TNF-α by 46.7% and 50.8%, IL-1β by 46.0% and 44.7%, and PGE2 by 21.7% and 16.9%, respectively, at 20 mg/kg. Blocked COX-2 expression and NF-κB activation.

Animal Model:

Male Sprague-Dawley rats (180-200 g)

Dosage:

20 mg/kg

Administration:

P.O., for 2 hour

Result:

Reduced hind paw edema volume by 27.1% at 1 h, and 24.0% at 2 h, respectively.

化学性质

黄色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于艾叶，长叶山金车花，银蒿地上部分，甜叶菊，地黄叶，过江藤地上部分。

用途

棕矢车菊素具有降血脂的作用。