Tectol
(Synonyms: 乌楠酚) 目录号 : GC61318
Tectol，从Lippiasidoides中分离，对人白血病细胞株HL60和CEM具有显著的抑制作用。Tectol是一种farnesyltransferase(FTase)抑制剂，在人和布氏锥虫的IC50分别为2.09和1.73μM。Tectol抑制耐药恶性疟原虫(FcB1)，IC50为3.44μM。
Cas No.:24449-39-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM[1]. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM[1][2].
[1]. Costa SM, et al. Chemical constituents from Lippia sidoides and cytotoxic activity. J Nat Prod. 2001;64(6):792-795. [2]. Cadelis MM, et al. Discovery and preliminary structure-activity relationship studies on tecomaquinone I and tectol as novel farnesyltransferase and plasmodial inhibitors. Bioorg Med Chem. 2016;24(14):3102-3107.
| Cas No. | 24449-39-6 | SDF | |
| 别名 | 乌楠酚 | ||
| Canonical SMILES | OC1=C(C=CC=C2)C2=C(O3)C(C=CC3(C)C)=C1C4=C(C=CC5(C)C)C(O5)=C6C(C=CC=C6)=C4O | ||
| 分子式 | C30H26O4 | 分子量 | 450.53 |
| 溶解度 | 储存条件 | Store at -20°C | |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2196 mL | 11.098 mL | 22.1961 mL |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL |
| 10 mM | 0.222 mL | 1.1098 mL | 2.2196 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。
Discovery and preliminary structure-activity relationship studies on tecomaquinone I and Tectol as novel farnesyltransferase and plasmodial inhibitors
Bioorg Med Chem 2016 Jul 15;24(14):3102-7.PMID:27240468DOI:10.1016/j.bmc.2016.05.024.
Biological screening of a library of synthesized benzo[c]chromene-7,10-dione natural products against human farnesyltransferase (FTase) has identified tecomaquinone I (IC50 of 0.065±0.004μM) as being one of the more potent natural product inhibitors identified to date. Anti-plasmodial screening of the same library against a drug-resistant strain of Plasmodium falciparum identified the structurally-related dichromenol Tectol as a moderately active growth inhibitor with an IC50 3.44±0.20μM. Two novel series of analogues, based on the benzo[c]chromene-7,10-dione scaffold, were subsequently synthesized, with one analogue exhibiting farnesyltransferase inhibitory activity in the low micromolar range. A preliminary structure-activity relationship (SAR) study has identified different structural requirements for anti-malarial activity in comparison to FTase activities for these classes of natural products. Our results identify tecomaquinone I as a novel scaffold from which more potent inhibitors of human and parasitic FTase could be developed.
Chemical constituents from Lippia sidoides and cytotoxic activity
J Nat Prod 2001 Jun;64(6):792-5.PMID:11421746DOI:10.1021/np0005917.
Eleven known compounds and a new prenylated naphthoquinone, lippsidoquinone (13), were isolated from ethanol extracts of Lippia sidoides. Their structures were established by a combination of 1D and 2D NMR, IR, and EIMS spectral data analysis. The cytotoxic properties of compounds 3--13 were evaluated against HL60, SW1573, and CEM cell lines. Only Tectol (6) and lippsidoquinone (13) exhibited significant activity against human leukemia cell lines HL60 and CEM.