商陆皂苷甲

商陆皂苷甲用途

Esculentoside A (EsA),一种从商陆 Phytolacca esculenta 根部分离出来的三萜皂苷。Esculentoside A (EsA) 在具有抗炎活性,对环氧合酶-2 (COX-2) 具有选择性抑制活性。Esculentoside A (EsA) 通过抑制 (NF-ΚB) 和丝裂原活化蛋白激酶 (MAPK) 信号通路抑制 LPS 诱导的急性肺损伤 (ALI) 中的炎症反应。

商陆皂苷甲名称

[ CAS 号 ]:
65497-07-6

[ 中文名 ]:
商陆皂苷甲

[ 英文名 ]:
Esculentoside A

[中文别名 ]:

[英文别名 ]:

Esculentoside
EsculentosideA
Phytolacaponin E

商陆皂苷甲生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[体外研究]

Esculentoside A(0-10μM; 24小时)降低了引物巨噬细胞中TNF浓度的释放[4]。

[体内研究]

Esculentoside A(EsA)(腹腔注射；20 mg/kg；每天一次；4周)通过调节炎性细胞因子,抑制肾细胞增殖和诱导细胞凋亡在治疗BXSB小鼠中起重要作用[2]。Esculentoside A(EsA)(腹腔注射；5,10和20 mg/kg；每天一次；7天)剂量依赖性地降低LPS攻击后小鼠血清中的TNF,IL-1和IL-6水平[4]。动物模型：BXSB小鼠[2]剂量：20 mg/kg给药：腹腔注射；20 mg/kg；每天一次；4周结果：减轻LN的肾损伤。

[参考文献]

[1]. Wu F, et al. Synthesis, in vitro inhibitory activity towards COX-2 and haemolytic activity of derivatives of esculentoside A. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6430-3. Epub 2007 Oct 5.

[2]. Ma H, et al. The effect of esculentoside A on lupus nephritis-prone BXSB mice. Arch Med Sci. 2013 Apr 20;9(2):354-60.

[3]. Zhong WT, et al. Protective effect of esculentoside A on lipopolysaccharide-induced acute lung injury in mice. J Surg Res. 2013 Nov;185(1):364-72.

[4]. Ju DW, et al. Esculentoside A inhibits tumor necrosis factor, interleukin-1, and interleukin-6 production induced by lipopolysaccharide in mice. Pharmacology. 1998 Apr;56(4):187-95

商陆皂苷甲物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
935.8±65.0 °C at 760 mmHg

[ 分子式 ]:
C₄₂H₆₆O₁₆

[ 分子量 ]:
826.964

[ 闪点 ]:
275.1±27.8 °C

[ 精确质量 ]:
826.435059

[ PSA ]:
262.36000

[ LogP ]:
3.01

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.620

商陆皂苷甲毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RK0177530

CHEMICAL NAME :: Olean-12-ene-28,29-dioic acid, 2,23-dihydroxy-3-((4-O-beta-D-glucopyranosyl-beta-D- xylopyranosyl)oxy)-, 29-methyl ester, (2-beta,3-beta,4-alpha,20-beta)-

CAS REGISTRY NUMBER :: 65497-07-6

LAST UPDATED :: 198706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C42-H66-O16

MOLECULAR WEIGHT :: 827.08

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 42300 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: SYHJAM Saengyak Hakhoechi. Journal of the Society of Pharmacognosy. (Hanguk Saengyak Hakhoe, c/o Natural Products Institute, Seoul National Univ., 28 Yunkeon-Dong, Chong-ro-ku, Seoul 110, Korea) 1970- Volume(issue)/page/year: 10,73,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1200 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Skin and Appendages - hair Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: SHZAAY Shoyakugaku Zasshi. Journal of Pharmacognosy. (Nippon Shoyaku Gakkai, c/o Nippon Gakkai Jimu Senta, 2-4-16 Yayoi, Bunkyo-ku, Tokyo 113, Japan) V.6- 1952- Volume(issue)/page/year: 33,111,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 486 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Skin and Appendages - hair Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: SHZAAY Shoyakugaku Zasshi. Journal of Pharmacognosy. (Nippon Shoyaku Gakkai, c/o Nippon Gakkai Jimu Senta, 2-4-16 Yayoi, Bunkyo-ku, Tokyo 113, Japan) V.6- 1952- Volume(issue)/page/year: 33,111,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 23600 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: SYHJAM Saengyak Hakhoechi. Journal of the Society of Pharmacognosy. (Hanguk Saengyak Hakhoe, c/o Natural Products Institute, Seoul National Univ., 28 Yunkeon-Dong, Chong-ro-ku, Seoul 110, Korea) 1970- Volume(issue)/page/year: 10,73,1979

商陆皂苷甲安全信息

[ 安全声明 (欧洲) ]:
24/25