Bulleyaconitine a

• CAS: 107668-79-1
• Catalog Number: ACM107668791
• Category: Main Products
• Molecular Weight: 627.76
• Molecular Formula: C₃₅H₄₉NO₉
• Synonyms: METHANONE,[(1,6,14,16)-8-(ACETYLOXY)-20-ETHYL-13-HYDROXY-1,6,16-TRIMETHOXY-4-(METHOXYMETHYL)ACONITAN-14-YL](4-METHOXYPHENYL); 16-trimethoxy-4-(methoxymethyl)aconitan-14-yl)(4-methoxyphenyl)-y-6; BULLEYACONITINE A(P); BULLEYACONITINE A: METHANONE,[(1,6,14,16)-8-(ACETYLOXY)-20-ETHYL-13-HYDROXY-1,6,16-TRIMETHOXY-4-(METHOXYMETHYL)ACONITAN-14-YL](4-METHOXYPHENYL); BulleyaconicineA; 20-ethyl-13-hydroxy-1,6,16-trimethoxy-4-(methoxymethyl)aconitan-14-yl](4-methoxyphenyl); BULLEYACONITINE A(RG)
• IUPAC Name: Bulleyaconitine A
• Canonical SMILES: CCN1CC2(CCC(C34C2C(C(C31)C5(CC(C6(CC4C5C6C(=O)C7=CC=C(C=C7)OC)O)OC)OC(=O)C)OC)OC)COC
• InChI Key: YRECILNLFWZVRM-JNQVLWDESA-N
• Boiling Point: 690.9ºC at 760mmHg
• Flash Point: 371.7ºC
• Density: 1.28g/cm³
• Appearance: solid
• Exact Mass: 627.34100

Case Study

Study on the Mechanism of Bulleyaconitine A in Treating Chronic Pain

Xie M X, et al. Molecular Pain, 2018, 14, 1744806918797243.

Bulleyaconitine A (BLA) is a diterpene alkaloid that has been used to treat chronic pain. Research indicates that therapeutic doses of BLA effectively suppress both peripher, but have no effect on acute pain. In rodents, oral administration of BLA, local application of DRG, and intrathecal injection have all proven to be effective in inhibiting neuropathic pain, bone cancer-induced pain, and chemotherapy-induced pain. The mechanism by which BLA alleviates chronic pain involves targeting multiple molecules.
The mechanism of BLA treating chronic pain
· In neuropathic conditions, there is an upregulation of protein kinase C and voltage-gated sodium channels in dorsal root ganglion neurons, intensifying the effectiveness of bulleyaconitine A.
· Bulleyaconitine A blocks voltage-gated sodium channels in a use-dependent manner, leading to the inhibition of ectopic discharges crucial for neuropathic pain.
· Bulleyaconitine A has been observed to inhibit neuropathic pain by modulating spinal microglia, which play a role in chronic pain but not in acute (nociceptive) pain.

Anti-Anxiety and Antivisceral Hypersensitivity Effects of Bulleyaconitine A

Huang S N, et al. Frontiers in Pharmacology, 2020, 11, 328.

Anxiety and chronic visceral pain are highly prevalent comorbidities in gastrointestinal disease. The study evaluated the inhibitory effect of Bulleyaconitine A (BAA) on visceral pain and its effect on anxiety. The results showed that BAA was found to produce significant anti-acetic acid-induced visceral pain effects by stimulating the expression of dynorphin A in spinal microglia. In addition, BAA has been confirmed to exert a huge anxiolytic effect in comorbid animals.
Experimental methods with Bulleyaconitine A
· The analgesic effects of BAA on acute visceral pain were assessed in three groups of rats using the Paw Withdrawal Threshold (PWT) test. These groups received a single subcutaneous injection of either normal saline (1 ml/kg), BAA (30 μg/kg), or BAA (90 μg/kg). One hour after the injection of saline or BAA, the rats were intraperitoneally injected with a 1% v/v acetic acid solution (10 ml/kg).
· In order to investigate the antianxiety effect of BAA in the chronic visceral pain-anxiety comorbidity model, the impact of BAA was studied in TNBS+HeICS rats. Three groups of TNBS+HeICS rats were separately injected with normal saline (1 ml/kg), BAA at a dose of 30 μg/kg, and BAA at a dose of 90 μg/kg on the first day (EPM) and the second day (OFT) following HeICS.