海柯吉宁

中文名称:

海柯吉宁

中文同义词:

海柯吉宁;海柯皂甙元;海柯皂苷元;(25R)-5α-螺甾(烷)-3β-醇-12-酮;(3β,5α,25R)-3-羟基螺甾(烷)-12-酮;番麻皂苷元;海柯皂苷元 (海柯吉宁;辛酸己酯, 来源于蒺藜

英文名称:

Hecogenin

英文同义词:

HECOGENIN;5-ALPHA, 20-ALPHA, 22-ALPHA, 25D-SPIROSTAN-3-BETA-OL-12-ONE;5ALPHA-SPIROSTAN-3BETA-OL-12-ONE;3BETA-HYDROXY-5ALPHA-SPIROSTAN-12-ONE;25R,5ALPHA-SPIROSTAN-3BETA-OL-12-ONE;Hecoginin;(25R)-5-Spirostan-3-ol-12-one;(3,5,25R)-3-Hydroxysiprostan-1

CAS号:

467-55-0

分子式:

C27H42O4

分子量:

430.62

EINECS号:

207-392-4

相关类别:

医药中间体;消化系统药物;医药与生物化工;原料药;中药对照品;标准品;植物提取物;Steroids;Biochemistry;Steroids (Others);对照品;化学连接;467-55-0;分析试剂标准品;标准品-对照品;对照品-中药对照品;标准品，对照品;化工原料;中国药典中药成分对照品

Mol文件:

467-55-0.mol

熔点 

268°C

比旋光度 

7.2 º (c=0.8 g/100ml, CHCl3)

沸点 

464.85°C (rough estimate)

密度 

1.0040 (rough estimate)

折射率 

1.4840 (estimate)

储存条件 

Sealed in dry,Room Temperature

酸度系数(pKa)

15.10±0.70(Predicted)

Merck 

14,4622

CAS 数据库

467-55-0(CAS DataBase Reference)

生物活性

Hecogenin 是从龙舌兰 (Agave sisalana) 分离的类固醇皂苷，是人 UDP-葡萄糖醛酸糖基转移酶的选择性抑制剂。Hecogenin 具有广泛的药理活性，包括抗炎，抗真菌和胃保护作用。

靶点

Target Value UGT1A4 () 1.5 μM

Target

Value

UGT1A4 ()

1.5 μM

体内研究

Hecogenin (3.1-90 mg/kg; oral administration; for 15 hours; male Swiss mice) acutely administered, before ethanol, exhibits a potent gastroprotective effect. The Hecogenin pretreatment normalizes GSH levels and significantly reduces lipid peroxidation and nitrite levels in the stomach, as evaluated by the ethanol-induced gastric lesion model. Hecogenin also decreases MPO release and significantly protects the gastric mucosa. Animal Model: Male Swiss mice (20-30 g) with ethanol Dosage: 3.1 mg/kg, 7.5 mg/kg, 15 mg/kg, 30 mg/kg, 60 mg/kg and 90 mg/kg Administration: Oral administration; for 15 hours Result: Normalized GSH levels and significantly reduced lipid peroxidation and nitrite levels in the stomach, as evaluated by the ethanol-induced gastric lesion model. Decreased MPO release and significantly protected the gastric mucosa.

Animal Model:

Male Swiss mice (20-30 g) with ethanol

Dosage:

3.1 mg/kg, 7.5 mg/kg, 15 mg/kg, 30 mg/kg, 60 mg/kg and 90 mg/kg

Administration:

Oral administration; for 15 hours

Result:

Normalized GSH levels and significantly reduced lipid peroxidation and nitrite levels in the stomach, as evaluated by the ethanol-induced gastric lesion model. Decreased MPO release and significantly protected the gastric mucosa.

化学性质 

结晶化合物（丙酮）。熔点 264-266℃。（有报道称具三种晶形，熔点 245℃，253℃，268℃）[α]D+8°（氯仿）/-10°（二噁烷）。

用途 

倍他米松、地塞米松等皮质激素类药物的原料。

用途 

用作激素类药物的原料药

生产方法 

可用Hechtia texensis，Agave 属和属等桂状提取。