棕矢车菊素

应用生物活性靶点体外研究体内研究棕矢车菊素试剂级价格

棕矢车菊素

CAS号:18085-97-7
英文名:Jaceosidin
中文名:棕矢车菊素
CBNumber:CB51515205
分子式:C17H14O7
分子量:330.29
MOL File:18085-97-7.mol

棕矢车菊素化学性质

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 :2-8°C(protect from light)
溶解度 :DMSO (Slightly), Methanol (Slightly, Sonicated), Pyridine (Slightly)
形态 :Solid
酸度系数(pKa) :6.47±0.40(Predicted)
颜色 :Pale Yellow to Light Yellow
稳定性 :Hygroscopic
LogP :1.300 (est)

棕矢车菊素性质、用途与生产工艺

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

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).

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.