8-O-Acetylharpagide

目录号: GN10719纯度: >98.00%同义词: 8-O-乙酰哈巴苷
8-O-Acetylharpagide是从Ajuga属爬行动物中分离的一种环烯醚萜类化合物。该化合物具有抗菌、解痉、强心和解热作用。

8-O-Acetylharpagide
Cas No.: 6926-14-3
规格价格库存数量操作
5mg¥182.00现货
1
10mg¥280.00现货
1
20mg¥427.00现货
1

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产品描述 Description

8-O-Acetylharpagide is an iridoid compound isolated from Ajuga reptile. The compound has antibacterial, antispasmodic, cardiotonic and antipyretic properties[1] [2].

8-O-Acetylharpagide (1-10μM; 24h) treatment inhibited ROS in a concentration-dependent manner in old HDFs. Low concentrations (less than 10μM) of 8-O-Acetylharpagide (5-50μg/ml; 48h) can fully inhibit the senescence-associated phenotypic expression of p53 and SA-β-gal in aged HDFs[1]. Different concentrations of 8-O-Acetylharpagide (100-250μg/ml; 24h) were active against Bacillus anthracis, but inactive against Staphylococcus aureus, Streptococcus agalactiae, Staphylococcus epidermidis, Aeromonas sobria, Shigella boydii, Vibrio cholerae, Corynebacterium diphtheriae, Salmonella typhi (Gram-positive bacteria), and Pseudomonas aeruginosa (Gram-positive bacteria) [2].

8-O-Acetylharpagide (100-1000µg/ml; immersion 20s) showed spasmolytic effects on isolated ileum and cardiotonic effects on isolated rabbit hearts at a test dose of 100µg/ml. No harmful or toxic effects of 8-O-Acetylharpagide (1-100 μg; po; 1 time) were detected[2].

References:
[1].Shafi N, Khan G A, Arfan M, et al. Isolation and pharmacological screening of 8-O-acetyl harpagide from Ajuga bracteosa Wall[J]. Biological Sciences-PJSIR, 2004, 47(3): 176-179.
[2].Hsu W H, Lin B Z, Leu J D, et al. Involvement of 8-O-acetylharpagide for Ajuga taiwanensis mediated suppression of senescent phenotypes in human dermal fibroblasts[J]. Scientific reports, 2020, 10(1): 19731.

8-O-Acetylharpagide是从Ajuga属爬行动物中分离的一种环烯醚萜类化合物。该化合物具有抗菌、解痉、强心和解热作用[1] [2]

8-O-Acetylharpagide(1-10μM;24h)以浓度依赖性方式抑制老年HDF中的ROS。低浓度(小于10μM)的8-O-Acetylharpagide(5-50μg/ml;48h)可以完全抑制老年HDF中p53和SA-β-半乳糖苷酶的衰老相关表型表达[1]。不同浓度的8-O-Acetylharpagide(100-250μg/ml;24h)对炭疽芽孢杆菌有活性,但对金黄色葡萄球菌、无乳链球菌、表皮葡萄球菌、温和气单胞菌、鲍氏志贺氏菌、霍乱弧菌、白喉棒状杆菌、伤寒沙门氏菌(革兰氏阳性菌)和铜绿假单胞菌(革兰氏阳性菌)无效[2]

8-O-Acetylharpagide(100-1000µg/ml;浸泡20s)在 100µg/ml 测试剂量下对离体回肠表现出解痉作用,对离体兔心脏表现出强心作用。未检测到 8-O-Acetylharpagide (1-100μg;po;1 次) 的有害或毒性作用[2]

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Human dermal fibroblasts cells

Preparation Method

Human dermal fibroblasts cells were seeded in 96-well transparent bottom black-plate. After 8-O-Acetylharpagide treatment for 24h, the media was removed and 20μM DCFDA was added to the corresponding wells and incubated for 30min at 37°C.

Reaction Conditions

1-10μM; 24h

Applications

8-O-Acetylharpagide treatment inhibited ROS in a concentration-dependent manner in old HDFs.
Animal experiment [2]:

Animal models

Fever model

Preparation Method

During the assay, acetylsalicylic acid was used as a standard. Young rabbits of either sex weighing between 1.5-1.8kg of inbred Himalayan Strain were divided into three groups. The animals were housed under uniform environmental conditions and maintained on a standard diet consisting of green fodder and vegetables. All animals were administered a subcutaneous injection of yeast (2.5ml/kg, 12%). Rectal temperature of hyperthermic animals were recorded prior and after 16h of injection. Test animals received 100-500mg/kg doses of 8-O-Acetylharpagide and the other group received 150mg/kg of the standard drug. The control group was given only the vehicle 1% carboxymethyl cellulose. The temperature of each group of animals were recorded at intervals of 90, 180 and 270min. after treatment.

Dosage form

100-500mg/kg; sc; 1 time

Applications

The antipyretic evaluation of 8-O-Acetylharpagide showed antipyretic effect only when treated with a larger dose (500mg/kg), and smaller doses of the test compound failed to produce the same effect as the standard drug acetylsalicylic acid.

References:
[1].Shafi N, Khan G A, Arfan M, et al. Isolation and pharmacological screening of 8-O-acetyl harpagide from Ajuga bracteosa Wall[J]. Biological Sciences-PJSIR, 2004, 47(3): 176-179.
[2].Hsu W H, Lin B Z, Leu J D, et al. Involvement of 8-O-acetylharpagide for Ajuga taiwanensis mediated suppression of senescent phenotypes in human dermal fibroblasts[J]. Scientific reports, 2020, 10(1): 19731.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
6926-14-3
同义词
8-O-乙酰哈巴苷
化学名
[(1S,4aS,5R,7S,7aS)-4a,5-dihydroxy-7-methyl-1-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,5,6,7a-tetrahydrocyclopenta[c]pyran-7-yl] acetate
SMILES
CC(=O)OC1(CC(C2(C1C(OC=C2)OC3C(C(C(C(O3)CO)O)O)O)O)O)C
分子式
C17H26O11
分子量
406.38 g/mol
溶解性
DMSO : 25 mg/mL (61.52 mM; Need ultrasonic)
保存条件
4°C, protect from light
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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