- Aconine
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- $0.00 / 25kg
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2024-04-12
- CAS:509-20-6
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 2000ton
- ACONINE
-
- $1.00 / 1KG
-
2019-07-06
- CAS:509-20-6
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 100KG
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| Product Name: | ACONINE | | Synonyms: | ACONINE;(15S,16S)-20-Ethyl-1α,6α,16-trimethoxy-4-(methoxymethyl)aconitane-3α,8β,13β,14α,15-pentol;20-Ethyl-1α,6α,16β-trimethoxy-4-(methoxymethyl)aconitane-3α,8,13,14α,15α-pentol;(1alpha,3alpha,6alpha,14alpha,15alpha,16beta)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol;Jesaconine;Aconitane-3,8,13,14,15-pentol,20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1a,3a,6a,14a,15a,16b)-;Aconine (Jesaconine);Aconitane-3,8,13,14,15-pentol, 20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1α,3α,6α,14α,15α,16β)- | | CAS: | 509-20-6 | | MF: | C25H41NO9 | | MW: | 499.6 | | EINECS: | | | Product Categories: | Alkaloids;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract | | Mol File: | 509-20-6.mol |  |
| | ACONINE Chemical Properties |
| Melting point | 129-131℃ | | alpha | D +23° | | Boiling point | 590.79°C (rough estimate) | | density | 1.42 | | refractive index | 1.6000 (estimate) | | storage temp. | -20°C Freezer | | solubility | Chloroform (Slightly), DMSO (Slightly) | | pka | 9.52(at 25℃) | | form | Solid | | color | Off-White to Pale Yellow |
| | ACONINE Usage And Synthesis |
| Toxicity | In vivo, aconine is toxic to mice when administered intravenously at a dose of 120 mg/kg. It induces flaccid paralysis and toxicity in rats with toxic dose (TD50) and LD50 values of 1.5 and 1.7 μmol per animal, respectively.
| | Description | Aconine is an alkaloid originally isolated from Aconitum species and active metabolite of aconitine. It inhibits osteoclast differentiation of RANKL-stimulated RAW 264.7 cells and bone resorption in a pit formation assay in a concentration-dependent manner. Aconine also inhibits RANKL-induced activation of NF-κB and NFATc1 in RAW 264.7 cells.
| | Description | Aconine is an alkaloid originally isolated from Aconitum species and active metabolite of aconitine. It inhibits osteoclast differentiation of RANKL-stimulated RAW 264.7 cells and bone resorption in a pit formation assay in a concentration-dependent manner. Aconine also inhibits RANKL-induced activation of NF-κB and NFATc1 in RAW 264.7 cells. In vivo, aconine is toxic to mice when administered intravenously at a dose of 120 mg/kg. It induces flaccid paralysis and toxicity in rats with toxic dose (TD50) and LD50 values of 1.5 and 1.7 μmol per animal, respectively. | | Uses | Aconine is a derivative of Aconitine (A189875), a neurotoxin which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction. | | Definition | ChEBI: Aconine is a diterpene alkaloid with formula C25H41NO9 that is isolated from several Aconitum species. It has a role as a plant metabolite, a human urinary metabolite, a NF-kappaB inhibitor and a xenobiotic. It is a bridged compound, a diterpene alkaloid, an organic heteropolycyclic compound, a polyether, a tertiary amino compound, a pentol, a secondary alcohol and a tertiary alcohol. It derives from a hydride of an aconitane. | | Synthesis | 1) Extraction: the main component in the CaoWu is aconitine alkaloids, the dried CaoWu tuberous roots about 4.8kg crushed to about 1 ~ 2 sieve, crushed particles are divided into 6L of the dispensing funnel, with 1000mL 25% ammonia immersion herbs for 2 ~ 4 hours, and then dichloromethane soak CaoWu granular herbs, immersion for 24 hours, every two days percolation, a total of 4 times extraction, decompression recovery The solvent was recovered under reduced pressure, and the extract was combined and weighed to obtain an ointment rate of 20.10-23.20 g/kg, and the extract was stored at 4C for spare use. With 18-19% HCl solution ultrasonic dissolution of CaoWu extract, filtration of the aqueous layer to remove the oil in the CaoWu, with about 40% NaOH solution precipitation of the aqueous layer, a large number of yellow-white precipitate appeared, cooling, filtration of the precipitate, precipitate freeze-drying, weighed yellow-white precipitate of 7.2-7.9g/kg, 4 to save standby.
2) Separation of aconite protoalkali: Take part of the yellow-white precipitate of NaOH base and separate it with 200-300 mesh silica gel, use n-hexane/ethyl acetate as the mobile phase and rinse the silica gel column. The column separation was stopped by tracking aconitine with thin-layer chromatography until the point of aconitine disappeared. The resulting crude aconitine was recrystallized by dichloromethane to obtain the pure aconitine.
| | IC 50 | NF-κB | | References | [1] KENTARO WADA Youkichi O Makoto Nihira. Effects of chronic administrations of aconitine on body weight and rectal temperature in mice[J]. Journal of ethnopharmacology, 2006, 105 1: Pages 89-94. DOI: 10.1016/j.jep.2005.10.007
[2] XIANG-ZHOU ZENG. Aconine inhibits RANKL-induced osteoclast differentiation in RAW264.7 cells by suppressing NF-κB and NFATc1 activation and DC-STAMP expression[J]. Acta Pharmacologica Sinica, 2015, 37 2: 255-263. DOI: 10.1038/aps.2015.85
[3] TENG-FEI LI Y W Nian Gong. Ester Hydrolysis Differentially Reduces Aconitine-Induced Anti-hypersensitivity and Acute Neurotoxicity: Involvement of Spinal Microglial Dynorphin Expression and Implications for Aconitum Processing[J]. Frontiers in Pharmacology, 2016, 7 1. DOI: 10.3389/fphar.2016.00367 |
| | ACONINE Preparation Products And Raw materials |
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