Bufotenidine
(Synonyms: 蟾蜍特尼定) 目录号 : GC63599
Bufotenidine 是天然的生物碱，是色氨酸受体的阻滞剂。
Cas No.:487-91-2
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
Bufotenidine, a natural indole alkaloid, is a blocking agent of the tryptaminic receptors[1][2].
[1]. Ying-Hui Dai, et al. A New Indole Alkaloid from the Toad Venom of Bufo bufo gargarizans. Molecules. 2016 Mar 16;21(3):349.
[2]. L F De Oliveira, et al. Blockade by bufotenidine of the serotonin- and narcotic-analgesics-induced contraction of dog intestine in vivo. Eur J Pharmacol
| Cas No. | 487-91-2 | SDF | |
| 别名 | 蟾蜍特尼定 | ||
| 分子式 | C13H18N2O | 分子量 | 218.29 |
| 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 | 4.5811 mL | 22.9053 mL | 45.8106 mL |
| 5 mM | 0.9162 mL | 4.5811 mL | 9.1621 mL |
| 10 mM | 0.4581 mL | 2.2905 mL | 4.5811 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。
[Determination of six compounds in Berberidis Cortex and comparative study of its different species]
Zhongguo Zhong Yao Za Zhi 2019 Mar;44(5):968-974.PMID:30989857DOI:10.19540/j.cnki.cjcmm.20181226.014.
In order to clarify the characteristic components of Berberidis Cortex,the preparative liquid chromatography and spectral analysis methods were used to separate and identify the unknown components in the water extract of Berberidis Cortex. Two compounds were isolated and identified as Bufotenidine and ferulic acid 4-O-β-D-glucopyranoside. They were both isolated for the first time from Berberidis Cortex and Berberis. In addition,an HPLC method was successfully established for simultaneously determination of six compounds in Berberidis Cortex,and chemometric methods were used to study the chemical differences among three main species of Berberidis Cortex. The results suggested that jatrorrhizine and Bufotenidine are the main difference compounds among the three species.Compared with B. kansuensis and B. diaphana,B. vernae contains significantly more jatrorrhizine(P<0. 01),and the content of Bufotenidine in B. vernae was significantly higher than that in B. kansuensis(P<0. 05). Considering these results,further research is necessary to reveal the pharmacological activities of Bufotenidine and the pharmacodynamic differences between the three species. The results could provide a reference for quality control,the basic research on effective substances,and development of Berberidis Cortex.
Two new polyamine alkaloids from the Bufo viridis toad venom
Nat Prod Res 2022 Jun 8;1-5.PMID:35675547DOI:10.1080/14786419.2022.2086545.
Two new polyamine alkaloids (bufonines A-B), together with four known alkaloids, Bufotenidine (3), bufotenine (4), 1-(β-d-ribofuranosyl)-lH-1,2,4-triazone (5) and proline (6) were isolated from the Bufo viridis toad venom. Their structures were identified by UV, HR-ESI-MS, NMR spectral analyses, and comparison of theoretical and experimental ECD data. All compounds were tested in vitro cytotoxicity against three human cancer cell lines (HT-29, A549 and Hela). None of the compounds showed cytotoxicity towards all tested cell lines. To the best of our knowledge, this is the first report of alkaloid components from Bufo viridis toad venom.
[Study on anti-inflammatory activity and mechanism of indolealkylamines in toad skin on LPS-activated neutrophils]
Zhongguo Zhong Yao Za Zhi 2021 Sep;46(18):4774-4781.PMID:34581088DOI:10.19540/j.cnki.cjcmm.20210616.401.
Indolealkylamines(IAAs) are the main hydrophilic substances in toad skin, mainly including free N-methyl-5-hydroxytryptamine, bufotenine, Bufotenidine, dehydrobufotenine, and binding bufothionine. In this study, the LPS-activated neutrophils were used to investigate the structure-activity relationship and anti-inflammatory mechanism of the above-mentioned five monomers from the toad skin in vitro. The neutrophils were divided into the control group, model group(1 μg·mL~(-1) LPS), positive drug group(100 μg·mL~(-1) indometacin), as well as the low-(50 μg·mL~(-1)), medium-(100 μg·mL~(-1)) and high-dose(200 μg·mL~(-1)) free N-methyl-5-hydroxytryptamine, bufotenine, Bufotenidine, dehydrobufotenine, and binding bufothionine groups. The levels of IL-6, TNF-α and IL-1β in the neutrophil supernatant of each group was measured by enzyme-linked immunosorbent assay(ELISA) after LPS stimulation, followed by the detection of apoptosis in each group after Annexin V/PI staining. The protein expression levels of caspase-3, Bax, Bcl-2, beclin1, LC3-I, and LC3-Ⅱ were assayed by Western blot. The results showed that IAAs reduced the excessive secretion of inflammatory cytokines caused by LPS compared with the model group. Besides, the activity of each free IAAs(N-methyl-5-hydroxytryptamine, bufotenine, Bufotenidine and dehydrobufotenine), especially bufotenine, was stronger than that of the binding bufothionine. As revealed by Annexin V/PI staining, LPS delayed the early apoptosis of neutrophils compared with the control group, while bufotenine promoted the apoptosis of neutrophils in a dose-dependent manner, which might be related to the elevated expression of apoptosis-related protein Bax/Bcl-2. In addition, LPS activated the autophagy pathways in neutrophils. This study confirmed the efficacy of IAAs in reducing the secretion of inflammatory cytokines in neutrophils induced by LPS for the first time. For instance, bufotenine exerts the anti-inflammatory effect possibly by inducing the apoptosis of neutrophils.
A New Indole Alkaloid from the Toad Venom of Bufo bufo gargarizans
Molecules 2016 Mar 16;21(3):349.PMID:26999086DOI:10.3390/molecules21030349.
A new indole alkaloid named bufobutarginine (1), along with three known bufotenines, namely, serotonin (2), Bufotenidine (3), and bufotenine (4), were isolated from the water extract of toad venom. Their structures were elucidated by spectral methods. This is the first time that arginine has been found to be involved in the biosynthesis of bufotenines in parotid of toad. The cytotoxic activities of these compounds have been assayed against A375 and A549 cell lines by the MTT method; however, they showed no cytotoxic activities.
[Quality evaluation of different Berberidis Cortex species based on ~1H-NMR metabolomics and anti-diabetic activity]
Zhongguo Zhong Yao Za Zhi 2020 Oct;45(19):4677-4685.PMID:33164432DOI:10.19540/j.cnki.cjcmm.20200620.201.
To evaluate the quality differences of four mainstream species of Berberidis Cortex,~1H-NMR metabolomics was applied to detect its primary and secondary metabolites, and the partial least squares discriminant analysis and analysis of variance were integrated to screen differential metabolites between species. Furthermore, diabetic rat model was established by high fat diet and streptozotocin to assess differences in antidiabetic activities among the four species. Sixteen compounds were simultaneously detected and identified, including alkaloids, organic acids, carbohydrates and amino acids. Interspecific difference markers were revealed as magnoflorine, jateorhi-zine, Bufotenidine and saccharose for the first time. Berberis vernae and B. kansuensis presented superior activities on reducing blood glucose level, improving insulin resistance, increasing insulin sensibility and anti-inflammation. B. dictyophylla showed moderate antidiabe-tic effect, while B. diaphana rendered inferior antidiabetic capacity. Based on the contents of four differential markers and the results of antidiabetic activity evaluation, the quality of four Berberidis Cortex species was ranked as B.vernae≈B.kansuensis>B. dictyophylla>B. diaphana. These results provided references for species collation, quality standard establishment and exploitation of Berberidis Cortex. The antidiabetic activities of B. vernae and B. kansuensis as well as their mechanisms of action merit further study in the future.