Bullatine ACAS# 1354-84-3 |
- Denudatine
Catalog No.:BCN5406
CAS No.:26166-37-0
Quality Control & MSDS
3D structure
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| Cas No. | 1354-84-3 | SDF | Download SDF |
| PubChem ID | 71300866 | Appearance | Powder |
| Formula | C22H33NO2 | M.Wt | 343.51 |
| Type of Compound | Alkaloids | Storage | Desiccate at -20°C |
| Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
| Chemical Name | (5R,11R,14S,15R,16R)-7-ethyl-5-methyl-12-methylidene-7-azahexacyclo[7.6.2.210,13.01,8.05,16.010,15]nonadecane-11,14-diol | ||
| SMILES | CCN1CC2(CCCC34C2CC(C31)C56C4C(C(CC5)C(=C)C6O)O)C | ||
| Standard InChIKey | OVXLNQAYPUEDSI-LVIQKLEBSA-N | ||
| Standard InChI | InChI=1S/C22H33NO2/c1-4-23-11-20(3)7-5-8-22-15(20)10-14(18(22)23)21-9-6-13(12(2)19(21)25)16(24)17(21)22/h13-19,24-25H,2,4-11H2,1,3H3/t13?,14?,15-,16+,17+,18?,19-,20+,21?,22?/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects, may be used for the treatment of neurodegenerative diseases such as arthritis. Bullatine A produces antinociception without induction of tolerance and inhibits morphine antinociceptive tolerance, and provide pharmacological basis for concurrent bullatine A and morphine treatment for chronic pain and morphine analgesic tolerance. |
| Targets | NOS | IL Receptor | NO | P2X receptor |
| In vitro | Bullatine A, a diterpenoid alkaloid of the genus Aconitum, could attenuate ATP-induced BV-2 microglia death/apoptosis via P2X receptor pathways.[Pubmed: 23769848 ]Brain Res Bull. 2013 Aug;97:81-5.Bullatine A (BLA), a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. The mechanism underlying the effects was examined in the present study.
Effects of volatile oil of Rhizoma zingiberis and other two kinds of volatile oil on percutaneous penetration of bullatine A via hairless mouse skin in vitro[Pubmed: 18536371]Zhongguo Zhong Yao Za Zhi. 2008 Mar;33(5):513-6.To investigate the effects of volatile oils of Rhizoma Acori Tatarinowii (RAT), Semen Myristicae (SM) and Pericarpium Citri Reticulatae (PCR) on percutaneous penetration of Bullatine A via hairless mouse skin in vitro.
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| In vivo | Bullatine A stimulates spinal microglial dynorphin A expression to produce anti-hypersensitivity in a variety of rat pain models.[Pubmed: 27577933]J Neuroinflammation. 2016 Aug 30;13(1):214.Aconiti brachypodi Radix (Xue-shang-yi-zhi-hao) has been prescribed to manage chronic pain, arthritis, and traumatic injuries. Bullatine A, a C20-diterpenoid alkaloid, is one of its principle effective compounds. This study aimed to investigate the anti-hypersensitivity of Bullatine A in a variety of rat pain models and explore its mechanisms of action.
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| Animal Research | Concurrent bullatine A enhances morphine antinociception and inhibits morphine antinociceptive tolerance by indirect activation of spinal κ-opioid receptors.[Pubmed: 27989510 ]J Ethnopharmacol. 2017 Jan 20;196:151-159.Bullatine A, a C20-diterpenoid alkaloid and one of the major effective ingredients in Aconiti brachypodi Radix (Xue-shang-yi-zhi-hao), can block pain hypersensitivity in a variety of rodent models through expression of spinal microglial dynorphin A.
To assess the interaction between Bullatine A and morphine on antinociception in acute nociception and pain hypersensitivity states, with the exogenous synthetic dynorphin A as a comparison |
Bullatine A Dilution Calculator
Bullatine A Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9111 mL | 14.5556 mL | 29.1112 mL | 58.2225 mL | 72.7781 mL |
| 5 mM | 0.5822 mL | 2.9111 mL | 5.8222 mL | 11.6445 mL | 14.5556 mL |
| 10 mM | 0.2911 mL | 1.4556 mL | 2.9111 mL | 5.8222 mL | 7.2778 mL |
| 50 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.1644 mL | 1.4556 mL |
| 100 mM | 0.0291 mL | 0.1456 mL | 0.2911 mL | 0.5822 mL | 0.7278 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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[Effects of volatile oil of Rhizoma zingiberis and other two kinds of volatile oil on percutaneous penetration of bullatine A via hairless mouse skin in vitro].[Pubmed:18536371]
Zhongguo Zhong Yao Za Zhi. 2008 Mar;33(5):513-6.
OBJECTIVE: To investigate the effects of volatile oils of Rhizoma Acori Tatarinowii (RAT), Semen Myristicae (SM) and Pericarpium Citri Reticulatae (PCR) on percutaneous penetration of Bullatine A via hairless mouse skin in vitro. METHOD: By an improved Franz diffusion, the effects of three kinds of volatile oils on the percutaneous penetration of Bullatine A were observed and compared with Azone, and the cumulative amount of Bullatine A was determined by HPLC. RESULT: The penetration enhancement ratios of Bullatine A with 7% volatile oil RAT and SM, 5% volatile oil of PCR and 3% Azone were 6.52, 6.74, 2.18, 6.03, respectively. CONCLUSION: The volatile oil of RAT, SM and PCR enhance permeation of Bullatine A, effectively.
Bullatine A stimulates spinal microglial dynorphin A expression to produce anti-hypersensitivity in a variety of rat pain models.[Pubmed:27577933]
J Neuroinflammation. 2016 Aug 30;13(1):214.
BACKGROUND: Aconiti brachypodi Radix (Xue-shang-yi-zhi-hao) has been prescribed to manage chronic pain, arthritis, and traumatic injuries. Bullatine A, a C20-diterpenoid alkaloid, is one of its principle effective compounds. This study aimed to investigate the anti-hypersensitivity of Bullatine A in a variety of rat pain models and explore its mechanisms of action. METHODS: Rat neuropathic pain, inflammatory pain, diabetic neuropathic pain, and bone cancer pain models were used. Dynorphin A and pro-inflammatory cytokines were measured in the spinal cord and cultured primary microglia. Double immunofluorescence staining of dynorphin A and glial and neuronal cellular markers was also measured in the spinal cord. RESULTS: Subcutaneous and intrathecal injection of Bullatine A dose-dependently attenuated spinal nerve ligation-, complete Freud's adjuvant-, diabetes-, and bone cancer-induced mechanical allodynia and thermal hyperalgesia, with the efficacies of 45-70 % inhibition, and half-effective doses of 0.9-1.9 mg/kg for subcutaneous injection. However, Bullatine A was not effective in blocking acute nociceptive response in the normal condition. Bullatine A specifically stimulated dynorphin A expression in microglia in the spinal cord in vivo and cultured primary microglia in vitro; the stimulatory effects were completely inhibited by the microglial inhibitor minocycline. In contrast, Bullatine A did not have an inhibitory effect on peripheral nerve injury- or lipopolysaccharide-induced pro-inflammatory cytokine expression. The spinal anti-allodynic effects of Bullatine A were entirely blocked by intrathecal injection of minocycline, the specific dynorphin A antiserum, and the selective k-opioid receptor antagonist. CONCLUSIONS: We, for the first time, demonstrate that Bullatine A specifically attenuates pain hypersensitivity, regardless of the pain models employed. The results also suggest that stimulation of spinal microglial dynorphin A expression mediates Bullatine A anti-nociception in pain hypersensitivity conditions.
Concurrent bullatine A enhances morphine antinociception and inhibits morphine antinociceptive tolerance by indirect activation of spinal kappa-opioid receptors.[Pubmed:27989510]
J Ethnopharmacol. 2017 Jan 20;196:151-159.
ETHNOPHARMACOLOGICAL RELEVANCE: Bullatine A, a C20-diterpenoid alkaloid and one of the major effective ingredients in Aconiti brachypodi Radix (Xue-shang-yi-zhi-hao), can block pain hypersensitivity in a variety of rodent models through expression of spinal microglial dynorphin A. AIM OF THE STUDY: To assess the interaction between Bullatine A and morphine on antinociception in acute nociception and pain hypersensitivity states, with the exogenous synthetic dynorphin A as a comparison MATERIALS AND METHODS: Spinal nerve ligation-induced neuropathic rats and naive mice were used for assessing the acute and chronic interactions of Bullatine A/dynorphin A with morphine. RESULTS: Single subcutaneous injection of Bullatine A or dynorphin A(1-17) did not either alter formalin- and thermally (hot-plate and water immersion tests)-induced acute nociception or potentiate morphine antinociception in naive mice. In contrast, Bullatine A dose-dependently inhibited formalin-induced tonic pain with the efficacy of 54% inhibition and the half-effective dose of 0.9mg/kg. Concurrent Bullatine A additively enhanced morphine antinociception. In neuropathic rats, the antinociceptive effects of multiple bidaily intrathecal injections of Bullatine A and dynorphin A remained consistent over 13 days, whereas morphine produced progressive and complete tolerance to antinociception, which was completely inhibited by concurrent Bullatine A and dynorphin A. A single intrathecal injection of Bullatine A and dynorphin A immediately reversed established morphine tolerance in neuropathic rats, although the blockade was a less degree in the thermally induced mouse acute nociceptive tests. The inhibitory effects of Bullatine A and dynorphin A on morphine tolerance were immediately and completely attenuated by intrathecal dynorphin A antibody and/or selective kappa-opioid receptor antagonist GNTI. CONCLUSION: These results suggest that Bullatine A produces antinociception without induction of tolerance and inhibits morphine antinociceptive tolerance, and provide pharmacological basis for concurrent Bullatine A and morphine treatment for chronic pain and morphine analgesic tolerance.
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, could attenuate ATP-induced BV-2 microglia death/apoptosis via P2X receptor pathways.[Pubmed:23769848]
Brain Res Bull. 2013 Aug;97:81-5.
Bullatine A (BLA), a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. The mechanism underlying the effects was examined in the present study. The effect of BLA on extracellular ATP induced cell death/apoptosis and pro-inflammatory cytokines release were investigated using BV-2 microglia cell line. The mediation/efficacy of inflammatory cytokines and P2X receptors was evaluated by detecting the mRNA levels of iNOS, IL-6, IL-1beta and P2X receptors, respectively. The results demonstrated that BV-2 cells could be damaged after incubation with higher dose of ATP, leading to activation of pro-inflammatory cytokines, transcriptional activation of iNOS and overproduction of NO via activation of P2X receptor. The BLA (1-50muM) potently inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses via selectively suppressing the up-regulation of P2X7 receptor mRNA. Since P2X7 receptors have an important role in immune and pain response, inflammation and inflammatory disease, this discovery of BLA as a potent P2X7 antagonist indicated that BLA may be a potential useful candidate for the treatment of neurodegenerative diseases such as arthritis.
