Tetrahydroalstonine
(Synonyms: 四氢鸭脚木碱) 目录号 : GC39016
Tetrahydroalstonine 是从 Rhazya stricta 的果实中分离出来的吲哚生物碱，是选择性的 α2-肾上腺素受体拮抗剂。
Cas No.:6474-90-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tetrahydroalstonine, a indole alkaloid isolated from the fruits of Rhazya stricta, is a selective alpha 2-adrenoceptor antagonist[1][2].
[1]. Malik S, et al. Tetrahydroalstonine from Fruits of Rhazya stricta. Planta Med. 1984 Jun;50(3):283. [2]. Roquebert J, et al. Inhibition of the alpha 1 and alpha 2-adrenoceptor-mediated pressor response in pithed rats by raubasine, tetrahydroalstonine and akuammigine. Eur J Pharmacol. 1984 Oct 30;106(1):203-5.https://www.ncbi.nlm.nih.gov/pubmed/6099269
| Cas No. | 6474-90-4 | SDF | |
| 别名 | 四氢鸭脚木碱 | ||
| Canonical SMILES | O=C(OC)C1=CO[C@@H](C)[C@@]2([H])[C@]1([H])C[C@@]3([H])C4=C(C5=CC=CC=C5N4)CCN3C2 | ||
| 分子式 | C21H24N2O3 | 分子量 | 352.43 |
| 溶解度 | DMSO : 100 mg/mL (283.74 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8374 mL | 14.1872 mL | 28.3744 mL |
| 5 mM | 0.5675 mL | 2.8374 mL | 5.6749 mL |
| 10 mM | 0.2837 mL | 1.4187 mL | 2.8374 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。
Tetrahydroalstonine from Fruits of Rhazya stricta
Planta Med 1984 Jun;50(3):283.PMID:17340319DOI:10.1055/s-2007-969707.
An indole alkaloid isolated from the fruits of RHAZYA STRICTA Dec., has been identified as Tetrahydroalstonine on the basis of spectroscopic studies and by comparison with the authentic sample.
Network pharmacology and molecular docking approach to elucidate the mechanisms of Liuwei Dihuang pill in diabetic osteoporosis
J Orthop Surg Res 2022 Jun 14;17(1):314.PMID:35701780DOI:10.1186/s13018-022-03194-2.
Background: Diabetic osteoporosis (DOP) is one of the chronic complications of diabetes mellitus, but without a standardized treatment plan till now. Liuwei Dihuang pill (LDP) has gradually exerted a remarkable effect on DOP in recent years; its specific mechanism is not clear yet. Methods: We adopted network pharmacology approaches, including multi-database search, pharmacokinetic screening, network construction analysis, gene ontology enrichment analysis, Kyoto Encyclopedia of Genes and Genomes pathway analysis and molecular docking to elaborate the active components, signaling pathways and potential mechanisms of LDP in the treatment of DOP. Results: Twenty-seven active ingredients and 55 related disease targets have been found through integrated network pharmacology. Functional enrichment analysis shows that five key active ingredients, including beta-sitosterol, stigmasterol, diosgenin, Tetrahydroalstonine, and kadsurenone, may give full scope to insulin secretion estrogen-level raising and angiogenesis in biological process through the pivotal targets. In addition, the underlying effect of PI3K/AKT/FOXO and VEGF pathways is also suggested in the treatment. Conclusion: Based on systematic network pharmacology methods, we predicted the basic pharmacological effects and potential mechanisms of LDP in the treatment of DOP, revealing that LDP may treat DOP through multiple targets and multiple signaling pathways, which provide evidence for the further study of pharmacological mechanism and broader clinical thinking.
Improved accumulation of ajmalicine and Tetrahydroalstonine in Catharanthus cells expressing an ABC transporter
J Plant Physiol 2009 Sep 1;166(13):1405-12.PMID:19403195DOI:10.1016/j.jplph.2009.02.015.
The biosynthetic pathway of monoterpenoid indole alkaloids in Catharanthus roseus is located throughout various membranes at both the cellular and intercellular levels. ATP-binding cassette (ABC) transporters are known to export vincristine and vinblastine from human cancer cells. It has recently been shown that ABC transporters are also involved in the transport of various monoterpenoid alkaloids in Catharanthus roseus cells. Over-expression of an ABC transporter in this plant might therefore affect the regulation of the alkaloid biosynthetic pathway. CjMDR1, an ABC transporter gene originally isolated from Coptis japonica, was expressed in Catharanthus roseus cell cultures. Cells showing a positive PCR signal of the transgene in both cDNA and genomic DNA samples were subject to transport studies using selected substrates. Unexpectedly, transport of the isoquinoline alkaloid berberine, the main substrate of CjMDR1 transporter in Coptis japonica, was not affected as compared with control and wild-type Catharanthus cells. On the other hand, the endogenous alkaloids ajmalicine and Tetrahydroalstonine were accumulated significantly more in Catharanthus roseus cells expressing CjMDR1 in comparison with control lines after feeding these alkaloids.
Partial purification and characterization of a NADPH dependent Tetrahydroalstonine synthase from Catharanthus roseus cell suspension cultures
Plant Cell Rep 1985 Aug;4(4):216-9.PMID:24253886DOI:10.1007/BF00269293.
A new enzyme was discovered which specifically hydrogenates the iminium form of cathenamine at position 21 to yield the heteroyohimbine alkaloid Tetrahydroalstonine. The enzyme was partially purified (35-fold) from Catharanthus roseus cell suspension cultures. It was shown to use exclusively NADPH as reductant, the pH optimum is at 6.6, the temperature optimum at 30°C, the half life of the soluble enzyme preparation is 26 min at 37°C, and the molecular weight is 81 000 ± 3%. Evidence is presented for the occurrence of two distinct and different cathenamine reductases, one reducing the iminium form of this central intermediate to give Tetrahydroalstonine, the other one reducing cathenamine to yield ajmalicine. Tetrahydroalstonine synthase was present in cell suspension cultures of C. ovalis, C. roseus, Picralima nitida, Rhazya stricta, and Vinca herbacea.
Inhibition of the alpha 1 and alpha 2-adrenoceptor-mediated pressor response in pithed rats by raubasine, Tetrahydroalstonine and akuammigine
Eur J Pharmacol 1984 Oct 30;106(1):203-5.PMID:6099269DOI:10.1016/0014-2999(84)90698-8.
The relative potencies of raubasine, Tetrahydroalstonine (THA) and akuammigine on alpha 1- and alpha 2-adrenoceptors were assessed by comparing their effects on the rise in blood pressure induced by stimulation of the sympathetic outflow from the spinal cord or by injection of noradrenaline in pithed rats. Akuammigine was inactive in both cases. Raubasine preferentially antagonized the effects of electrical stimulation while THA antagonized the effects of injected noradrenaline. The results suggest that raubasine preferentially blocks alpha 1-adrenoceptors while THA is more selective for alpha 2-adrenoceptors.