Andrographolide (Diterpene Lactone · Antiviral · Anti-inflammatory · Immunostimulatory)

Compound	Andrographolide
Chemical class	Terpenoid — Diterpene Lactone (Labdane)
CAS	5508-58-7
Primary source	Andrographis paniculata (Kalmegh / King of Bitters, leaves)
Key applications	Antiviral, anti-inflammatory, immunostimulatory, hepatoprotective
Claim strength	Moderate
Typical form	Andrographis extract standardised to andrographolide (10–50%); Kalmegh extract
Buy from Herbuno	Kalmegh Liquid Extract (Water Soluble) - Andrographis Paniculata → Kalmegh Oil Soluble Extract - Andrographis Paniculata →

Name origin: From Andrographis paniculata — the plant genus from which it was first isolated. Andrographolide is a bicyclic diterpene lactone (labdane skeleton), the primary and most bioactive compound in Andrographis. Traditional use: Andrographis paniculata (Kalmegh in Hindi; Bhunimba in Sanskrit; “King of Bitters” for its intensely bitter taste) is one of the most important medicinal plants in Ayurveda, TCM, and Southeast Asian traditional medicine. Used for respiratory infections, fever, liver conditions, digestive complaints, and as a general tonic. Marketed as “Indian Echinacea” in Western markets. Research trajectory: Andrographolide has multiple human RCTs for respiratory infection symptom reduction (common cold, influenza-like illness), with several comparing favourably to pharmaceutical antivirals. Anti-inflammatory mechanisms (NF-κB inhibition, COX-2 suppression), hepatoprotective activity, and immunostimulatory effects are well-characterised. COVID-19 research has driven increased interest since 2020. Commercial source: Available from Andrographis paniculata (Kalmegh) water-soluble and oil-soluble extracts. See sourcing options below.

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Evidence for Andrographolide Applications

Respiratory infections — antiviral and symptom relief: Multiple human RCTs demonstrate Andrographis extract (standardised to andrographolide) significantly reduces duration and severity of common cold, influenza-like illness, and upper respiratory tract infection symptoms. A systematic review (Coon & Ernst 2004, updated) confirms efficacy for uncomplicated respiratory infections. Andrographolide inhibits viral replication via protease inhibition and interferon induction. Claim strength: Moderate.

Anti-inflammatory — NF-κB inhibition: Andrographolide covalently modifies NF-κB (alkylation of cysteine-62 on p50 subunit), irreversibly inhibiting NF-κB-driven inflammatory gene expression. This covalent mechanism is pharmacologically distinctive among botanical anti-inflammatories. Reduces COX-2, TNF-α, IL-6, and IL-1β across multiple inflammatory models. Claim strength: Moderate.

Hepatoprotective: Andrographolide protects against carbon tetrachloride and paracetamol-induced liver injury in animal models via Nrf2 activation and antioxidant enzyme induction. Human pilot data from Andrographis extract preparations in hepatitis and liver health contexts are documented in TCM and Indian clinical literature. Claim strength: Moderate.

Immunostimulatory: Andrographolide stimulates macrophage phagocytosis, NK cell activity, and T-lymphocyte proliferation. Promotes interferon-γ production. In vivo immunostimulatory effects in animal models are consistent. Claim strength: Moderate.

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Dosage & Formulator Specification

Clinical dose range from RCTs: 300–1,200 mg/day Andrographis extract (standardised to 10–30% andrographolide, delivering 30–360 mg andrographolide/day). Most RCTs for respiratory infections used 200–400 mg extract (standardised to 11.2–30% andrographolide) 3× daily for 5–7 days. The European Medicines Agency (EMA) has a Community Herbal Monograph for Andrographis paniculata for traditional use in cold symptoms.

Andrographolide is intensely bitter — encapsulation is essentially mandatory for palatability in oral dosage forms. Enteric coating is not required (unlike peppermint oil) but improves GI tolerability at higher doses. Andrographolide has poor aqueous solubility (logP ~2.8); bioavailability is moderate but variable. Phospholipid complexation (phytosome technology) improves plasma AUC 2–3-fold in animal studies. For respiratory supplement blends, Andrographis extract pairs well with elderberry (C3G), echinacea (chicoric acid), and zinc.

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Frequently Asked Questions — Andrographolide

Is andrographolide the same as “Indian Echinacea”?
“Indian Echinacea” is a marketing term applied to Andrographis paniculata by analogy to Echinacea’s immune-support positioning. Both have human RCT evidence for respiratory infection symptom reduction, but they are botanically unrelated and have different primary mechanisms (andrographolide: NF-κB covalent inhibition, viral protease inhibition; echinacea: macrophage stimulation, chicoric acid-mediated immunostimulation). Andrographolide has stronger antiviral mechanism specificity; echinacea has more extensive overall clinical trial volume.

What does “covalent NF-κB inhibition” mean and why is it significant?
Most NF-κB inhibitors (curcumin, resveratrol, quercetin) block NF-κB reversibly by competing for binding sites. Andrographolide forms a covalent bond with cysteine-62 of the NF-κB p50 subunit — a permanent, irreversible modification that remains active even after andrographolide is cleared from plasma. This produces a prolonged and potent anti-inflammatory effect from each dose, analogous (mechanistically) to aspirin’s covalent COX inhibition. This pharmacologically distinctive mechanism underlies andrographolide’s strong clinical anti-inflammatory profile.

Is Andrographis safe for long-term use?
Andrographis at clinical doses (up to 1,200 mg/day extract) for up to 12 weeks has a well-documented safety profile in RCTs. GI side effects (nausea, vomiting, diarrhoea) are the most common at higher doses — encapsulated formulations reduce this. Andrographolide has been associated with rare cases of anaphylaxis in susceptible individuals. Contraindicated in pregnancy (potential uterotonic effects in animal models). Standard advisory for autoimmune conditions (immunostimulatory activity) is appropriate.

Has andrographolide been studied for COVID-19?
Yes. Andrographolide received significant research attention after 2020. Computational studies and in vitro work demonstrated activity against SARS-CoV-2 main protease and spike protein binding. A Thai clinical trial (Andrographolide 180 mg/day for 5 days) showed reduced viral load and improved clinical outcomes in mild COVID-19 cases. These findings are preliminary and andrographolide should not be positioned as a COVID-19 therapeutic without further clinical validation, but the antiviral mechanism is relevant to formulator positioning in broad-spectrum respiratory immune support blends.

Related compounds: Glycyrrhizin, Ginsenosides, Betulinic Acid, Ursolic Acid

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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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