Vasicinone (Quinazoline Alkaloid · Bronchodilatory · Mucolytic · Vasaka)

Compound	Vasicinone
Chemical class	Alkaloid — Quinazoline (Pyrrolo[1,2-b]quinazoline)
CAS	486-64-6
Primary source	Adhatoda vasica (Malabar nut / Vasaka / Adulsa) leaves
Key applications	Bronchodilatory, mucolytic, anti-asthmatic, uterotonic (traditional), anti-inflammatory
Claim strength	Moderate
Typical form	Vasaka leaf extract standardised to total alkaloids (vasicine + vasicinone); Adhatoda extract
Buy from Herbuno	Vasaka Leaf Extract Powder →

Name origin: From Vasaka (the Sanskrit/common name for Adhatoda vasica, from Sanskrit vasa = tonic). Vasicinone is the quinazoline alkaloid formed from vasicine (the primary Adhatoda alkaloid) by oxidation. Vasicinone has a ketone at C-3 that vasicine lacks. Both are present in Vasaka leaves — vasicine typically in higher concentration (0.5–2% dry weight), vasicinone in lower (0.05–0.5%). Traditional use: Vasaka (Adhatoda vasica, Malabar nut; Vasa in Ayurveda; Arusa in Unani) is one of the most important medicinal plants in Indian traditional medicine for respiratory conditions — used for over 2,000 years for asthma, chronic bronchitis, cough, and tuberculosis. The leaves, roots, and flowers are used, with the alkaloid fraction (vasicine + vasicinone) identified as the primary bronchodilatory active. Research trajectory: Vasicinone has documented bronchodilatory activity (β2-adrenergic receptor partial agonism, phosphodiesterase inhibition), mucolytic properties, and anti-inflammatory effects. Its pharmacological similarity to the synthetic bronchodilator bromhexine (which was designed based on vasicine) provides strong mechanistic support. Multiple human studies with Vasaka leaf preparations confirm bronchodilatory and expectorant activity. Vasicinone is particularly important as the natural prototype for the bromhexine/ambroxol pharmaceutical class. Commercial source: Vasaka Leaf Extract Powder and Vasaka Leaf Liquid Extract from Herbuno. See sourcing options below.

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Evidence for Vasicinone Applications

Bronchodilatory (β2-adrenergic and PDE inhibition): Vasicinone relaxes bronchial smooth muscle via partial agonism of β2-adrenergic receptors and inhibition of phosphodiesterase (preventing cAMP breakdown, promoting smooth muscle relaxation). Human studies with Vasaka leaf preparations (fresh juice, decoctions) demonstrate measurable increases in FEV1 and peak expiratory flow in asthmatic patients. Claim strength: Moderate (human studies with Vasaka; vasicinone as component).

Mucolytic and expectorant: Vasicinone and vasicine stimulate bronchial gland secretion (expectorant) and reduce mucus viscosity (mucolytic) via mechanisms parallel to bromhexine. Used clinically in Indian phytomedicine for chronic obstructive pulmonary conditions with excessive mucus. Claim strength: Moderate.

Anti-inflammatory: Vasicinone inhibits NF-κB, reduces COX-2, and decreases pro-inflammatory cytokines in macrophage and bronchial epithelial cell models. Anti-inflammatory activity complements bronchodilation for comprehensive respiratory health formulation. Claim strength: Moderate.

Uterotonic (traditional — safety advisory): Vasicine and vasicinone have documented uterotonic and abortifacient activity at high doses in animal models and traditional medical contexts. Vasaka leaf preparations have been used traditionally as emmenagogues and to induce labour. This is a critical safety consideration: Adhatoda vasica preparations are contraindicated in pregnancy. Claim strength: High (traditional and experimental; this is a safety advisory, not a therapeutic claim).

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Dosage & Formulator Specification

Traditional Vasaka preparation: 3–6 g fresh Vasaka leaves/day or equivalent extract for respiratory applications. Vasaka leaf extract standardised to total alkaloids (vasicine + vasicinone by HPLC): 100–300 mg/day extract typically used in respiratory supplement formulations. Specify individual vasicine and vasicinone content on CoA — their ratio varies by plant part and extraction method. MANDATORY SAFETY LABEL: All Vasaka/Adhatoda preparations must carry “Do not use during pregnancy” advisory — the uterotonic risk from vasicinone is clinically significant and must be communicated on product labels in all markets.

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Frequently Asked Questions — Vasicinone

Is vasicinone the same as bromhexine?
No — but bromhexine was directly designed based on vasicine (the parent alkaloid of vasicinone). Bromhexine (a pharmaceutical mucolytic/expectorant) is a synthetic modification of vasicine: the quinazoline ring is replaced by a benzylamine with bromine substituents. Bromhexine is then metabolically converted to ambroxol (another pharmaceutical mucolytic). Vasicinone is the natural oxidised form of vasicine. The pharmacological relationship is direct — vasicinone is the natural prototype for an entire class of pharmaceutical respiratory drugs.

Why is Vasaka important in Ayurvedic respiratory medicine?
Vasaka (Vasa) is classified in Ayurveda as a primary Kasahara (anti-cough) and Shvasahara (anti-asthma) herb — among the most important traditional respiratory medicines. The AYUSH ministry recognises Vasaka in several approved formulations for bronchial asthma and chronic bronchitis. Unlike many traditional herbs where modern pharmacological validation has been challenging, vasicine and vasicinone provide strong mechanistic and preclinical evidence supporting the traditional bronchodilatory claims.

Can Vasaka be combined with other respiratory botanicals?
Yes — Vasaka is traditionally combined and is rationally paired with: Tulsi (Ocimum sanctum, anti-inflammatory and immunomodulatory via eugenol), Mulethi/Licorice (Glycyrrhiza glabra, mucosal soothing via glycyrrhizin + flavonoids), and Pippali (Piper longum, bioavailability-enhancing via piperine). Synergistic respiratory formulation addresses bronchodilation (Vasaka), mucus clearance (Vasaka + licorice), immune support (Tulsi), and absorption enhancement (Pippali). This is consistent with traditional compound respiratory formulations (like Kanakasava) in Ayurveda.

Is Vasaka extract safe for long-term respiratory management?
At therapeutic doses for respiratory management (extracts delivering 10–50 mg vasicine + vasicinone/day), Vasaka has a reasonable short-term safety profile in human use. Long-term controlled safety data are limited. The primary safety concern is the uterotonic effect — absolutely contraindicated in pregnancy. For chronic respiratory supplement use in non-pregnant adults, Vasaka extract at standard doses appears well-tolerated, but monitoring for hepatotoxicity signals is prudent at higher doses (paralleling some other quinazoline alkaloid plants).

Related compounds: Deoxyvasicinone, Glycyrrhizin, Andrographolide, Thymol

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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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