Brucine (Dimethoxystrychnine · Nux Vomica Indole Alkaloid · Anti-inflammatory · Glycine Antagonist)
| Compound | Brucine (2,3-Dimethoxystrychnidin-10-one) |
| Chemical class | Alkaloid — Indole / Strychnan (Dimethoxy analogue of strychnine) |
| CAS | 357-57-3 |
| Primary source | Strychnos nux-vomica (Nux Vomica seeds, 0.5–1% of dry weight) |
| Key applications | Glycine antagonist (weaker than strychnine); anti-inflammatory; analgesia research; tumour microenvironment; traditional Nux Vomica component |
| Claim strength | Moderate (anti-inflammatory, anticancer preclinical); Toxicological reference |
| Typical form | Co-constituent of Nux Vomica extract (alongside strychnine); brucine isolate (research grade) |
| Buy from Herbuno | Nux Mica Seed Oil Soluble Extract - Strychnos nux-vomica → |
Name origin: Named after James Bruce, the 18th-century Scottish explorer of Africa who first documented the plant Strychnos nux-vomica in detail during his Ethiopian expeditions. Brucine was isolated alongside strychnine by Pelletier and Caventou in 1819. The “2,3-dimethoxy” prefix refers to the two methoxy groups on the aromatic ring — the only structural difference from strychnine. Despite this minimal structural change, brucine is pharmacologically meaningfully different from strychnine: approximately 10–30× less potent as a GlyR antagonist, with additional alpha-adrenergic blocking and anti-inflammatory activities. Research trajectory: While strychnine is primarily a toxicological and historical reference compound, brucine has attracted genuine pharmaceutical research interest for: (1) anti-inflammatory activity via NF-κB inhibition; (2) tumour microenvironment modulation — brucine interferes with cancer-associated fibroblast signalling and immunosuppressive cytokine production; (3) analgesia via sigma receptor modulation (separate from the strychnine-type glycine antagonism); (4) anti-inflammatory applications in traditional Ayurvedic formulations at detoxified doses. Commercial source: Nux Vomica oil soluble extract from Herbuno co-delivers strychnine and brucine. Isolated brucine is available as research-grade standard.
Evidence for Brucine Applications
Anti-inflammatory — NF-κB inhibition: Brucine suppresses NF-κB nuclear translocation and reduces TNF-α, IL-6, and COX-2 in macrophage models. Animal models of arthritis, colitis, and acute inflammation show anti-inflammatory efficacy with brucine at doses below the acute toxicity threshold. The anti-inflammatory mechanism is independent of the glycine receptor interaction. Claim strength: Moderate.
Tumour microenvironment and cancer-associated fibroblasts: Brucine has been studied in Chinese research groups for its effects on the immunosuppressive tumour microenvironment — specifically its ability to inhibit cancer-associated fibroblast (CAF) activation and reduce IL-6 and TGF-β production that suppress anti-tumour immunity. This is an emerging research area with no clinical translation yet. Claim strength: Emerging.
Analgesic activity (sigma receptor): Brucine modulates sigma receptors and demonstrates analgesic activity in rodent pain models (hot plate, writhing test) at sub-convulsant doses. The analgesia appears to be partially opioid-receptor-independent. This aligns with traditional Ayurvedic use of Nux Vomica preparations for neuralgic pain. Claim strength: Moderate.
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Dosage & Formulator Specification
Critical safety note: Brucine shares the same narrow therapeutic/toxic margin as strychnine, though at 10–30× higher doses. Both alkaloids must be quantified in Nux Vomica extract materials. Traditional Ayurvedic dose: as for strychnine above. For any brucine-specific research formulation, request isolated brucine with purity CoA and ensure dosing stays well below the estimated human NOAEL. Brucine sulfate is the water-soluble salt form used in research.
Frequently Asked Questions — Brucine
What are the two methoxy groups that distinguish brucine from strychnine?
Strychnine has an unsubstituted aromatic ring (benzene ring) in positions 2 and 3. Brucine has methoxy groups (–OCH3) at both the 2 and 3 positions of this aromatic ring. This dimethoxylation increases the electron density of the aromatic ring, alters the molecular shape and electronic distribution, and reduces binding affinity at the glycine receptor (explaining the reduced potency). The methoxy groups also contribute to brucine’s additional pharmacological activities not shared by strychnine (alpha-adrenergic blocking, enhanced anti-inflammatory profile).
Can brucine be separated from strychnine in Nux Vomica extracts?
Yes — brucine and strychnine have different solubilities and chromatographic properties, allowing separation. Brucine is more soluble in ethanol and has different HPLC retention time from strychnine. Pharmaceutical manufacturers have historically separated the two (strychnine for rodenticide use; brucine for laboratory reagent use). For Herbuno’s Nux Vomica oil soluble extract, the ratio of strychnine to brucine should be quantified by HPLC CoA — request full alkaloid profile to ensure known concentrations of both compounds.
Is brucine used as a resolving agent in chemistry?
Yes — this is an important non-pharmacological application of brucine. Brucine (being a chiral alkaloid) forms diastereomeric salts with racemic acidic compounds. These diastereomers have different solubilities and can be separated by fractional crystallisation, allowing resolution of racemic acids into enantiomers. This classical resolution method (“Pasteur resolution using brucine”) has been a standard technique in organic chemistry for over a century for resolving chiral acids where enzymatic resolution is not available.
Is there a specific application for brucine in sports or performance contexts?
Historically yes — strychnine and brucine were used as performance stimulants in early 20th-century athletics (see strychnine page). This historical use was exploitative of the CNS stimulant properties at sub-toxic doses. Modern sports pharmacology does not recognise any legitimate performance role for brucine. It is detectable by modern anti-doping analytical methods and would be considered a masking agent or stimulant under WADA regulations. No therapeutic window for brucine as a performance agent can be defined without unacceptable toxicity risk.
Related compounds: Strychnine, Coniine, Colchicine, Aconitine
Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.
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