Delsoline
(Synonyms: 硬飞燕草碱) 目录号 : GC38153
A diterpene alkaloid with diverse biological activities
Cas No.:509-18-2
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
Delsoline is a diterpene alkaloid that has been found in Delphinium and has diverse biological activities.1,2,3 It inhibits binding of α-bungarotoxin to rat neuronal α7 nicotinic acetylcholine receptors (nAChRs; IC50 = 19 ?M).1 Delsoline (3 mg/ml) is repellent against adult red flour beetles (T. castaneum) in a filter paper assay.2 In vivo, delsoline (75 mg/kg) lowers systolic blood pressure in a rat model of left renal artery ligation-induced hypertension.3
1.Hardick, D.J., Blagbrough, I.S., Cooper, G., et al.Nudicauline and elatine as potent norditerpenoid ligands at rat neuronal alpha-bungarotoxin binding sites: Importance of the 2-(methylsuccinimido)benzoyl moiety for neuronal nicotinic acetylcholine receptor bindingJ. Med. Chem.39(24)4860-4866(1996) 2.Ulubelen, A., Meri?li, A.H., Kilin?er, N., et al.Insect repellent activity of diterpenoid alkaloidsPhytother. Res.15(2)170-171(2001) 3.Lian, Q.S., and Feng, G.H.Hypotensive effect of delsolineZhongguo Yaoli Xuebao6(1)37-40(1985)
| Cas No. | 509-18-2 | SDF | |
| 别名 | 硬飞燕草碱 | ||
| Canonical SMILES | O[C@@H]1C(C(N(CC)C2)C3(O)[C@H]4OC)([C@@](C[C@@]5([H])[C@@H]6OC)([H])[C@@]6([H])[C@@]3(C[C@@H]5OC)O)[C@@]4([H])[C@@]2(COC)CC1 | ||
| 分子式 | C25H41NO7 | 分子量 | 467.6 |
| 溶解度 | Chloroform: soluble,Methanol: soluble | 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 | 2.1386 mL | 10.6929 mL | 21.3858 mL |
| 5 mM | 0.4277 mL | 2.1386 mL | 4.2772 mL |
| 10 mM | 0.2139 mL | 1.0693 mL | 2.1386 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。
Pharmacokinetics and UPLC-MS/MS of Delsoline in Mouse Whole Blood
J Anal Methods Chem 2018 Oct 11;2018:9412708.PMID:30405933DOI:10.1155/2018/9412708.
Delsoline, a major alkaloid of Delphinium anthriscifolium Hance, has both a curare-like effect and a ganglion-blocking effect and is used to relieve muscle tension or hyperkinesia. A ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was established for the determination of Delsoline in mouse blood, and the pharmacokinetics of Delsoline after intravenous administration (1 mg/kg) and intragastric administration (9, 6, and 3 mg/kg) were studied. Gelsenicine served as an internal standard, and a UPLC BEH C18 chromatographic column was used. The mobile phase consisted of acetonitrile and 0.1% formic acid; the gradient elution flow rate was 0.4 mL/min. The MRM model was used for the quantitative analysis of Delsoline m/z 468.3⟶108.1 and the internal standard m/z 327.1⟶296.1. Mouse blood samples were treated with acetonitrile precipitation to remove proteins. In the concentration range of 0.1-1000 ng/mL, Delsoline in mouse blood showed a good linearity (r 2 > 0.995), and the lower limit of quantitation was 0.1 ng/mL. The intraday precision relative standard deviation (RSD) was below 14%, and the interday precision RSD was below 15%. The accuracy ranged between 94.3% and 110.1%, the average recovery was above 90.8%, and the matrix effect ranged between 97.0% and 102.5%. The UPLC-MS/MS method was sensitive, rapid, and selective in the study of pharmacokinetics of Delsoline. The absolute bioavailability of Delsoline was 20.9%.
Diterpenoid Alkaloids from Consolida regalis S. F.Gray subsp.paniculata (Host) Soo var. paniculata
Sci Pharm 2017 Aug 16;69(1):61-65.PMID:28813032DOI:10.3797/scipharm.aut-01-07.
Seven diterpenoid alkaloids : delcosine(1), Delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var. paniculata. The presence of compounds 1,2,5,6 and 7 in this plant has not been previously reported.
Diterpenoid alkaloids from Consolida oliveriana
J Nat Prod 1996 Sep;59(9):907-10.PMID:8864243DOI:10.1021/np960219k.
From the aerial parts of Consolida oliveriana (DC) Schröd. a new norditerpenoid alkaloid consolidine (2) has been isolated, in addition to the known alkaloids pubescenine (1), gigactonine, and Delsoline and the diterpenoid alkaloid ajaconine (4). The structure of alkaloid 2 was established on the basis of its physical and spectroscopic data including detailed NMR studies. A detailed NMR study on ajaconine (4) resulted in the revision of 11 13C chemical shift assignments.
Norditerpene and diterpene alkaloids from Aconitum variegatum
Phytochemistry 2005 Apr;66(7):837-46.PMID:15797610DOI:10.1016/j.phytochem.2005.01.019.
Aerial parts of Aconitum variegatum L. from the Pyrenees furnished four norditerpene alkaloids, 16 beta-hydroxycardiopetaline, 8-ethoxysachaconitine, 14-acetylgenicunine B, N-deethyl-N-19-didehydrosachaconitine, five diterpene alkaloids 15-veratroyldictizine, 15-veratroyl-17-acetyldictizine, 15-veratroyl-17-acetyl-19-oxodictizine, N-ethyl-1 alpha-hydroxy-17-veratroyldictizine, variegatine and the known alkaloids sachaconitine, 14-O-acetylsachaconitine, karakoline, talatizamine, 10-hydroxytalatizamine, 14-acetyltalatizamine, 14-acetyl-10-hydroxytalatizamine, N-methylarmepavine, pengshenin B, Delsoline, dihydrodelsoline, delcosine and genicunin B. Structures of the alkaloids were established by MS, 1D- and 2D-NMR techniques.
Nudicauline and elatine as potent norditerpenoid ligands at rat neuronal alpha-bungarotoxin binding sites: importance of the 2-(methylsuccinimido)benzoyl moiety for neuronal nicotinic acetylcholine receptor binding
J Med Chem 1996 Nov 22;39(24):4860-6.PMID:8941400DOI:10.1021/jm9604991.
Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. We have shown that, among a number of selected norditerpenoid alkaloids, elatine (2) and nudicauline (3) are equipotent with, or better than, MLA (1) in binding to brain [125I]-alpha BgTX binding sites, with IC50 values of 6.1, 1.7, and 7.6 nM, respectively. The 2-((S)-methylsuccinimido)benzoyl moiety of these ligands is crucial for high-affinity binding, whereas structural modifications to the norditerpenoid core of the ligand can be tolerated without loss of activity or selectivity. In addition to MLA (1), elatine (2), and nudicauline (3), we have examined lycoctonine (4), inuline (6), lappaconitine (7), N-desacetyllappaconitine (8), Delsoline (10), delcorine (11), deltaline (12), condelphine (13), and karacoline (14). This study therefore extends the range of norditerpenoids, other than MLA, which can be used to probe this important class of nAChR. All 12 alkaloids were assessed for activity at [3H]nicotine binding sites which are considered to represent alpha 4 beta 2 nAChR. Furthermore, the 1H and 13C NMR spectroscopic data of MLA and elatine have been critically compared.