Ranaconitine
(Synonyms: 7-羟基高乌甲素) 目录号 : GC39135An alkaloid with analgesic and anesthetic activities
Cas No.:1360-76-5
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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Ranaconitine is an alkaloid that has been found in Aconitum and has analgesic and local anesthetic activities in mice (ED50s = 6.99 and 0.167 ?mol/kg, respectively).1
1.Bello-Ramírez, A.M., and Nava-Ocampo, A.A.A QSAR analysis of toxicity of Aconitum alkaloidsFundam. Clin. Pharmacol.18(6)699-704(2004)
Cas No. | 1360-76-5 | SDF | |
别名 | 7-羟基高乌甲素 | ||
Canonical SMILES | CO[C@@H]1C23C4C(O)([C@]5(O)[C@]6(O)[C@@]3([H])C[C@@]([C@@H](OC)C5)([H])[C@@H]6OC)C[C@]2([H])[C@@](CN4CC)(OC(C7=C(C=CC=C7)NC(C)=O)=O)CC1 | ||
分子式 | C32H44N2O9 | 分子量 | 600.7 |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.6647 mL | 8.3236 mL | 16.6472 mL |
5 mM | 0.3329 mL | 1.6647 mL | 3.3294 mL |
10 mM | 0.1665 mL | 0.8324 mL | 1.6647 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
X-ray crystallographic study of Ranaconitine
Nat Prod Commun 2011 Nov;6(11):1589-90.PMID:22224266doi
The crystal structure of natural diterpenoid alkaloid Ranaconitine isolated from Aconitum sinomontanum Nakai has been determined by single crystal X-ray diffraction analysis. The crystal presents a monoclinic system, space group C2 with Z = 4, unit cell dimensions a = 30.972(19) angstrom, b = 7.688(5) angstrom, and c = 19.632(12) angstrom. Moreover, the intermolecular O-H...O hydrogen bonds and weak pi-pi interactions play a critical role in expanding the dimensionality.
X-ray structure study of Ranaconitine hydrobromide
Nat Prod Res 2012;26(15):1451-3.PMID:21988549DOI:10.1080/14786419.2011.603319.
Ranaconitine is an important diterpenoid alkaloid from Aconitum sinomontanum Nakai. The absolute configuration of natural Ranaconitine was determined through an X-ray structure analysis of hydrated Ranaconitine hydrobromide. The crystal presents a monoclinic system, space group P2(1) with Z = 2, unit cell dimensions: a = 10.6604(12) Å, b = 12.3674(14) Å, c = 12.2938(13) Å and β = 91.056(2)°. The chirality of the asymmetric carbon atoms was as follows: C10(S), C13(S), C14(S), C15(S), C16(S), C17(R), C23(S), C25(R), C26(S), C27(S), C28(S) and C30(S). Moreover, a complex network of hydrogen bonds occurred between neighbouring molecules.
Preparative separation of lappaconitine, Ranaconitine, N-deacetyllappaconitine and N-deacetylranaconitine from crude alkaloids of sample Aconitum sinomontanum Nakai by high-speed counter-current chromatography
J Chromatogr A 2002 Jan 18;943(2):219-25.PMID:11833641DOI:10.1016/s0021-9673(01)01464-9.
Analytical high-speed counter-current chromatography (HSCCC) was used for the systematic selection and optimization of the two-phase solvent system to separate alkaloids from Aconitum sinomontanum Nakai. The optimum solvent systems CHCl3-MeOH-0.3 M/0.2 M HCl (4:1.5:2, v/v) thus obtained led to the successful separation of lappaconitine, Ranaconitine, N-deacetyllappaconitine and N-deacetylranaconitine from 60 to 500 mg of crude alkaloid sample by preparative HSCCC separation.
Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum
J Nanobiotechnology 2015 Jul 10;13:47.PMID:26156035DOI:10.1186/s12951-015-0107-3.
Background: Lipid-based nanosystems have great potential for transdermal drug delivery. In this study, nanostructured lipid carriers (NLCs) for short-acting alkaloids lappacontine (LA) and Ranaconitine (RAN) isolated from Aconitum sinomontanum (AAS) at 69.47 and 9.16% (w/w) yields, respectively, were prepared to enhance percutaneous permeation. Optimized NLC formulations were evaluated using uniform design experiments. Microstructure and in vitro/in vivo transdermal delivery characteristics of AAS-loaded NLCs and solid lipid nanoparticles (SLNs) were compared. Cellular uptake of fluorescence-labeled nanoparticles was probed using laser scanning confocal microscopy and fluorescence-activated cell sorting. Nanoparticle integrity during transdermal delivery and effects on the skin surface were also investigated. Results: NLC formulations were less cytotoxic than the AAS solution in HaCaT and CCC-ESF cells. Moreover, coumarin-6-labeled NLCs showed biocompatibility with HaCaT and CCC-ESF cells, and their cellular uptake was strongly affected by cholesterol and lipid rafts. Significantly greater cumulative amounts of NLC-associated LA and RAN than SLN-associated alkaloids penetrated the rat skin in vitro. In vivo microdialysis showed higher area under the concentration-time curve (AUC)0-t for AAS-NLC-associated LA and RAN than for AAS-SLN-associated alkaloids. Conclusions: NLC formulations could be good transdermal systems for increasing biocompatibility and decreasing cytotoxicity of AAS. AAS-NLCs showed higher percutaneous permeation than the other preparations. These findings suggest that NLCs could be promising transdermal delivery vehicles for AAS.
Traditional processing, uses, phytochemistry, pharmacology and toxicology of Aconitum sinomontanum Nakai: A comprehensive review
J Ethnopharmacol 2022 Jul 15;293:115317.PMID:35469829DOI:10.1016/j.jep.2022.115317.
Ethnopharmacological relevance: As a folk medicine, Aconitum sinomontanum Nakai (Ranunculaceae) a perennial herbaceous flowering plant, is a widely used traditional Chinese medicine. Its rhizomes and roots are known as 'Gaowutou' in China, and it has been traditionally used for the treatment of rheumatoid arthritis, painful swelling of joints, bruises and injuries and has been known to grow well in regions of high altitude such as Gansu, Tibet etc. THE AIM OF THE REVIEW: This systematic review the comprehensive knowledge of the A. sinomontanum, including its traditional processing and uses, chemical constituents, pharmacological activities, toxicity assessment, pharmacokinetics and metabolism, and its use in clinical settings to emphasize the benefits of this species. We also discuss expectations for prospective research and implementation of this herb. This work lays a solid foundation for further development of A. sinomontanum. Materials and method: Information on the studies of A. sinomontanum was collected from scientific journals, books, and reports via library and electronic data search (PubMed, Elsevier, Scopus, Google Scholar, Springer, Science Direct, Wiley, ACS, EMBASE, Web of Science and CNKI). Meanwhile, it was also obtained from published works of material medica, folk records, ethnopharmacological literatures, Ph.D. and Masters dissertation. Results: As a member of the Ranunculaceae family, A. sinomontanum possesses its up-and-coming biological characteristics. It is widely reported for treating rheumatoid arthritis, painful swelling of joints, bruises and injuries. Currently, over 71 phytochemical ingredients have been obtained and identified from different parts of A. sinomontanum. Among them, alkaloids, flavonoids, steroids, glycosides are the major bioactive constituents. Activities such as antinociceptive, anti-inflammatory, antitumor, antiarrhythmic, local anesthetic, antipyretic, antimicrobial, insecticidal and others have been corroborated in vivo and in vitro. These properties are attributed to different alkaloids. In addition, many of the active ingredients, such as lappaconitine, Ranaconitine and total alkaloids have been used as quality markers. Conclusion: This work contributes to update the ethnopharmacological uses, chemical constituents, pharmacological activities, toxicity assessment, pharmacokinetics and metabolism, and clinical settings information for A. sinomontanum, which provide basic information to help better understand the pharmacological and toxicological activities of A. sinomontanum in human. However, further in-depth studies are needed to determine the medical uses of this herb and its chemical constituents, pharmacological activities, clinical applications and toxicology.