8-O-Acetylharpagide
(Synonyms: 8-O-乙酰哈巴苷) 目录号 : GN10719
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。
Cas No.:6926-14-3
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
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Cell lines |
Human dermal fibroblasts cells |
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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]: | |
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Animal models |
Fever model |
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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. |
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References: |
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| Cas No. | 6926-14-3 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | DMSO : 25 mg/mL (61.52 mM; Need ultrasonic) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4608 mL | 12.3038 mL | 24.6075 mL |
| 5 mM | 0.4922 mL | 2.4608 mL | 4.9215 mL |
| 10 mM | 0.2461 mL | 1.2304 mL | 2.4608 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet