Alstonine
目录号 : GC39796
Alstonine 是一种植物性药物的主要吲哚生物碱化合物。Alstonine 具有抗精神病，抗焦虑，抗癌和抗疟疾的特性。
Cas No.:642-18-2
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
Alstonine is a major indole alkaloid compound of a plant-based remedy. Alstonine has antipsychotic, anxiolytic, anticancer and antimalarial properties[1].
[1]. E Elisabetsky, et al. The Alkaloid Alstonine: A Review of Its Pharmacological Properties. Evid Based Complement Alternat Med. 2006 Mar;3(1):39-48.
| Cas No. | 642-18-2 | SDF | |
| Canonical SMILES | COC(C1=CO[C@@H](C)[C@@]2([H])[C@]1([H])CC3=[N+](C2)C=CC4=C3[N-]C5=C4C=CC=C5)=O | ||
| 分子式 | C21H20N2O3 | 分子量 | 348.4 |
| 溶解度 | Soluble in DMSO | 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 | 2.8703 mL | 14.3513 mL | 28.7026 mL |
| 5 mM | 0.5741 mL | 2.8703 mL | 5.7405 mL |
| 10 mM | 0.287 mL | 1.4351 mL | 2.8703 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。
Alstonine as an antipsychotic: effects on brain amines and metabolic changes
Evid Based Complement Alternat Med 2011;2011:418597.PMID:19189988DOI:10.1093/ecam/nep002.
Managing schizophrenia has never been a trivial matter. Furthermore, while classical antipsychotics induce extrapyramidal side effects and hyperprolactinaemia, atypical antipsychotics lead to diabetes, hyperlipidaemia, and weight gain. Moreover, even with newer drugs, a sizable proportion of patients do not show significant improvement. Alstonine is an indole alkaloid identified as the major component of a plant-based remedy used in Nigeria to treat the mentally ill. Alstonine presents a clear antipsychotic profile in rodents, apparently with differential effects in distinct dopaminergic pathways. The aim of this study was to complement the antipsychotic profile of Alstonine, verifying its effects on brain amines in mouse frontal cortex and striatum. Additionally, we examined if Alstonine induces some hormonal and metabolic changes common to antipsychotics. HPLC data reveal that Alstonine increases serotonergic transmission and increases intraneuronal dopamine catabolism. In relation to possible side effects, preliminary data suggest that Alstonine does not affect prolactin levels, does not induce gains in body weight, but prevents the expected fasting-induced decrease in glucose levels. Overall, this study reinforces the proposal that Alstonine is a potential innovative antipsychotic, and that a comprehensive understanding of its neurochemical basis may open new avenues to developing newer antipsychotic medications.
Antiplasmodial activity of the natural product compounds Alstonine and himbeline
Int J Parasitol Drugs Drug Resist 2021 Aug;16:17-22.PMID:33915339DOI:10.1016/j.ijpddr.2021.04.003.
Malaria, caused by Plasmodium parasites, continues to be a devastating global health issue. Despite a decline in malaria related deaths over the last decade, overall progress has plateaued. Key challenges to malaria prevention and control include the lack of a broadly effective vaccine and parasite drug resistance, including to the current gold standard artemisinin combination therapies (ACTs). New drugs with unique modes of action are therefore a priority for both the treatment and prevention of malaria. Unlike treatment drugs which need to kill parasites quickly to reduce or prevent clinical symptoms, compounds that kill parasites more slowly may be an option for malaria prevention. Natural products and natural product derived compounds have historically been an excellent source of antimalarial drugs, including the artemisinin component of ACTs. In this study, 424 natural product derived compounds were screened for in vitro activity against P. falciparum in assays designed to detect slow action activity, with 46 hit compounds identified as having >50% inhibition at 10 μM. Dose response assays revealed nine compounds with submicromolar activity, with slow action activity confirmed for two compounds, Alstonine and himbeline (50% inhibitory concentration (IC50) 0.17 and 0.58 μM, respectively). Both compounds displayed >140-fold better activity against P. falciparum versus two human cell lines (Selectivity Index (SI) >1,111 and > 144, respectively). Importantly, P. falciparum multi-drug resistant lines showed no cross-resistance to Alstonine or himbeline, with some resistant lines being more sensitive to these two compounds compared to the drug sensitive line. In addition, Alstonine displayed cross-species activity against the zoonotic species, P. knowelsi (IC50 ~1 μM). Outcomes of this study provide a starting point for further investigations into these compounds as antiplasmodial drug candidates and the investigation of their molecular targets.
Inhibition of osteosarcoma cell proliferation in vitro and tumor growth in vivo in mice model by Alstonine through AMPK-activation and PGC-1α/TFAM up-regulation
Acta Biochim Pol 2022 Aug 17;69(3):543-549.PMID:35975969DOI:10.18388/abp.2020_5769.
Osteosarcoma, a leading malignant tumor of bones is diagnosed mostly in adolescents and young adults worldwide. The present study investigated Alstonine as anti-osteosarcoma agent in vitro as well as in vivo and evaluated the underlying mechanism. Treatment with Alstonine led to a significant (P<0.05) reduction in MG63 and U-2OS cell viability. Alstonine treatment of MG63 and U-2OS cells caused a significant reduction in colony formation compared to the control cells. Viability of osteoblasts was not affected by Alstonine treatment in 1.25 to 20 µM concentration range. In Alstonine treated MG63 and U-2OS cells apoptotic cells increased significantly (P<0.05) compared to the control cells. Moreover, in MG63 and U-2OS cells treatment with Alstonine caused a prominent increase in expression of cleaved caspase-9, caspase-3, and PARP. Treatment of MG63 and U-2OS cells with Alstonine caused a prominent increase in AMPKα (Thr172) phosphorylation and elevated the count of mtDNA copies compared to the untreated cells. Alstonine treatment of the cells caused a remarkable increase in expression of PGC-1α and TFAM proteins. Treatment of the mice with Alstonine at 5 and 10 mg/kg doses for 30 days caused a significant (P<0.05) reduction in xenograft growth. Expression of PGC-1α and TFAM proteins in tumor tissues of the mice treated with Alstonine was significantly (P<0.05) raised compared to the control group. Thus, Alstonine inhibits osteosarcoma cell growth and activates apoptosis through AMPK dependent pathway. Therefore, Alstonine may be considered for treatment of osteosarcoma as it effectively arrests tumor growth in mice.
Antipsychotic-like profile of Alstonine
Pharmacol Biochem Behav 1998 May;60(1):133-41.PMID:9610935DOI:10.1016/s0091-3057(97)00594-7.
Although recently developed drugs have brought significant improvement, the treatment of psychotic disorders still presents serious drawbacks. Because inherent complexity and lack of satisfactory understanding of the underlying pathophysiology impose limits for rational drug design, resourceful approaches in the search for antipsychotics are pertinent. This article reports pharmacological properties of Alstonine, a heteroyohimbine-type alkaloid, which exhibited an antipsychotic-like profile, inhibiting amphetamine-induced lethality, apomorphine-induced stereotypy, and potentiating barbiturate-induced sleeping time. Atypical features of Alstonine were the prevention of haloperidol-induced catalepsy and lack of direct interaction with D1, D2 and 5-HT2A receptors, classically linked to antipsychotic mechanism of action.
Original mechanisms of antipsychotic action by the indole alkaloid Alstonine (Picralima nitida)
Phytomedicine 2015 Jan 15;22(1):52-5.PMID:25636871DOI:10.1016/j.phymed.2014.10.010.
Alstonine is the major component of plant based remedies that traditional psychiatrists use in Nigeria. Alstonine is an indole alkaloid that has an antipsychotic experimental profile comparable with that of clozapine and is compatible with the alleged effects in mental patients. Representing a desirable innovation in the pharmacodynamics of antipsychotic medications, the evidence indicates that Alstonine does not bind to D2 dopamine receptors (D2R) and differentially regulates dopamine in the cortical and limbic areas. The purpose of this study was to further investigate the effects of Alstonine on D2R binding in specific brain regions using quantitative autoradiography (QAR) and its effects on dopamine (DA) uptake in mouse striatal synaptosomes. The effects of Alstonine on D2R binding were determined in the nucleus accumbens and caudate-putamen using QAR in mice treated with Alstonine doses that have antipsychotic effects. The effects of Alstonine [3H]DA uptake were assessed in synaptosomes prepared from striatal tissue obtained from mice treated acutely or for 7 days with Alstonine. Alstonine did not change the D2R binding densities in the studied regions. DA uptake was increased after acute (but not after 7 days) treatment with Alstonine. Consistent with the Alstonine behavioral profile, these results indicate that Alstonine indirectly modulates DA receptors, specifically by modulating DA uptake. This unique mechanism for DA transmission modulation contributes to the antipsychotic-like effects of Alstonine and is compatible with its behavioral profile in mice and alleged effects in patients. These results may represent an innovation in the antipsychotic development field.