Hupehenine
(Synonyms: 湖贝甲素) 目录号 : GC38619
Hupehenine is a steriodal alkaloid extracted from the bulbs of Fritillaria Hupehensis, with the potential for inhibiting acetylcholine, antagonism for muscarinic receptors and cholinesterase inhibition.
Cas No.:98243-57-3
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
Hupehenine is a steriodal alkaloid extracted from the bulbs of Fritillaria Hupehensis, with the potential for inhibiting acetylcholine, antagonism for muscarinic receptors and cholinesterase inhibition.
| Cas No. | 98243-57-3 | SDF | |
| 别名 | 湖贝甲素 | ||
| Canonical SMILES | O[C@H]1CC[C@@]2(C)[C@]([C@H](O)C[C@]3([H])[C@]2([H])C[C@]4([H])[C@@]3([H])CC[C@]5([H])[C@@]4([H])CN6[C@](CC[C@H](C)C6)([H])[C@@H]5C)([H])C1 | ||
| 分子式 | C27H45NO2 | 分子量 | 415.65 |
| 溶解度 | Soluble in DMSO | 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 | 2.4059 mL | 12.0294 mL | 24.0587 mL |
| 5 mM | 0.4812 mL | 2.4059 mL | 4.8117 mL |
| 10 mM | 0.2406 mL | 1.2029 mL | 2.4059 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 and validation of Hupehenine in rat plasma by UPLC-MS/MS and its application to pharmacokinetic study
Biomed Chromatogr 2015 Dec;29(12):1805-10.PMID:26033449DOI:10.1002/bmc.3499.
In this work, a sensitive and selective ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for determination of Hupehenine in rat plasma was developed and validated. After addition of imperialine as an internal standard (IS), protein precipitation by acetonitrile-methanol (9:1, v/v) was used to prepare samples. Chromatographic separation was achieved on a UPLC BEH C18 column (2.1 × 100 mm, 1.7 µm) with 0.1% formic acid and acetonitrile as the mobile phase with gradient elution. An electrospray ionization source was applied and operated in positive ion mode; multiple reaction monitoring mode was used for quantification using target fragment ions m/z 416.3 → 98.0 for Hupehenine, and m/z 430.3 → 138.2 for IS. Calibration plots were linear throughout the range 2-2000 ng/mL for Hupehenine in rat plasma. Mean recoveries of Hupehenine in rat plasma ranged from 92.5 to 97.3%. Relative standard deviations of intra-day and inter-day precision were both <6%. The accuracy of the method was between 92.7 and 107.4%. The method was successfully applied to a pharmacokinetic study of Hupehenine after either oral or intravenous administration. For the first time, the bioavailability of Hupehenine was reported as 13.4%.
Analysis of Hupehenine in the total alkaloids from Fritillaria hupehensis by HPLC-ELSD
J Huazhong Univ Sci Technolog Med Sci 2008 Feb;28(1):118-20.PMID:18278474DOI:10.1007/s11596-008-0130-9.
A reverse-phase high pressure liquid chromatography (HPLC) method with evaporative light scattering detection (ELSD) has been developed for the quantitative analysis of Hupehenine in the total alkaloids from Fritillaria hupehensis. Samples were analyzed on a reverse-phase column (Hypersil C-18) with a mobile phase of methanol:water:chloroform: triethylamine (85:15:1:0.6). The ELSD was set at the drift tube temperature of 68.3 degrees C and gas flow rate of 1.8 L/min. Hupehenine's retention time was 13.7 min with an asymmetry factor of 1.2. The validity of the method has been verified with linearity, limit of detection, accuracy and precision. The logarithmic linear curve was obtained from 8.936 to 134.04 microg/mL (r=0.9993). The detection limit (S/N>3) of Hupehenine was 1.79 microg/mL on the column. Intra-day RSD was 1.42% and inter-day RSD was 2.26% (3 days within a week). The average recovery of Hupehenine was 101.50%, and RSD was 1.62%.
Integrated computational and experimental approach for novel anti-leishmanial molecules by targeting Dephospho-coenzyme A kinase
Int J Biol Macromol 2023 Mar 31;232:123441.PMID:36708902DOI:10.1016/j.ijbiomac.2023.123441.
Coenzyme A acts as a necessary cofactor for many enzymes and is a part of many biochemical processes. One of the critical enzymes involved in Coenzyme A synthesis is Dephospho-coenzyme A-kinase (DPCK). In this study, we have used integrated computational and experimental approaches for promising inhibitors of DPCK using the natural products available in the ZINC database for anti-leishmanial drug development. The top hit compounds chosen after molecular docking were Veratramine, Azulene, Hupehenine, and Hederagenin. The free binding energy of Veratramine, Azulene, Hupehenine, and Hederagenin was estimated. Besides the favourable binding point, the ligands also showed good hydrogen bonding and other interactions with key residues of the enzyme's active site. The natural compounds were also experimentally investigated for their effect on the L. donovani promastigotes and murine macrophage (J774A.1). A good antileishmanial activity by the compounds on the promastigotes was observed as estimated by the MTT assay. The in-vitro experiments revealed that Hupehenine (IC50 = 7.34 ± 0.37 μM) and Veratramine (IC50 = 12.46 ± 2.28 μM) exhibited better inhibition than Hederagenin (IC50 = 23.36 ± 0.54 μM) and Azulene (IC50 = 24.42 ± 3.28 μM). This work has identified novel anti-leishmanial molecules possibly acting through the inhibition of DPCK.
[Simultaneous determination of six major isosteroidal alkaloids in Beimu by UPLC-ELSD]
Zhongguo Zhong Yao Za Zhi 2020 Mar;45(6):1393-1398.PMID:32281353DOI:10.19540/j.cnki.cjcmm.20191223.201.
An UPLC method was established for the direct determination of six major bioactive isosteroidal alkaloids, namely peimisine, imperialine, sipeimine-3-D-glucoside, verticinone, verticine and Hupehenine from the bulbus of Fritillaria(Beimu), a commonly used antitussive traditional Chinese medicinal(TCM) herb. An Acquity UPLC~(TM) CSH C_(18) column(2.1 mm×100 mm, 1.7 μm) was used for all analysis. The investigated six compounds were all separated with gradient mobile phase consisting of 0.02% diethylamine-water-methanol at a flow rate of 0.3 mL·min~(-1). The temperature of sample manager was set at 20 ℃. Drift tube temperature was 45 ℃, and spray parameter was 40% with injection volume of 1 μL. Then, the further quality assessment of Beimu was carried out by cluster analysis(CA) and principal component analysis(PCA). The investigated all had good linearity(r≥0.998 9) over the tested ranges. The method is simple, accurate and reproducible, and can be used for determining the content of six major bioactive isosteroidal alkaloids.
Natural Alkaloid Compounds as Inhibitors for Alpha-Synuclein Seeded Fibril Formation and Toxicity
Molecules 2021 Jun 19;26(12):3736.PMID:34205249DOI:10.3390/molecules26123736.
The accumulation and aggregation of α-synuclein (α-syn) is the main pathologic event in Parkinson's disease (PD), dementia with Lewy bodies, and multiple system atrophy. α-Syn-seeded fibril formation and its induced toxicity occupy a major role in PD pathogenesis. Thus, assessing compounds that inhibit this seeding process is considered a key towards the therapeutics of synucleinopathies. Using biophysical and biochemical techniques and seeding-dependent cell viability assays, we screened a total of nine natural compounds of alkaloid origin extracted from Chinese medicinal herbs. Of these compounds, synephrine, trigonelline, cytisine, harmine, koumine, peimisine, and Hupehenine exhibited in vitro inhibition of α-syn-seeded fibril formation. Furthermore, using cell viability assays, six of these compounds inhibited α-syn-seeding-dependent toxicity. These six potent inhibitors of amyloid fibril formation and toxicity caused by the seeding process represent a promising therapeutic strategy for the treatment of PD and other synucleinopathies.