Andrographis paniculata | Supplementopedia

Overview

Andrographis paniculata, commonly called “king of bitters,” is a herbaceous plant native to South‑East Asia.
The aerial parts (particularly the leaves and flowering tops) have been used for centuries in traditional Ayurvedic and Chinese medicine.
Modern research focuses on the plant’s standardized extract—rich in the diterpenoid andrographolide—as a botanical supplement.
It is aimed primarily at supporting immune function and managing acute inflammatory conditions.

Immune modulation: Randomized trials show that standardized Andrographis extracts (≥30 % andro‑grapholide) reduce the duration and severity of upper‑respiratory infections, likely by enhancing macrophage activity and cytokine balance.
Anti‑inflammatory: Clinical data demonstrate reductions in C‑reactive protein and symptom scores in mild‑to‑moderate inflammatory diseases (e.g., osteoarthritis, allergic rhinitis).
Antimicrobial: In‑vitro and limited human data suggest activity against Streptococcus spp., Staphylococcus spp., and certain viruses (influenza, SARS‑CoV‑2) through viral entry inhibition.
Antioxidant: The extract scavenges free radicals and up‑regulates Nrf2‑dependent antioxidant enzymes, supporting cellular oxidative balance.
Metabolic support: Pilot studies indicate modest improvements in fasting glucose and lipid profiles in overweight adults, likely mediated by hepatic enzyme modulation.
Potential neuro‑protective effect: Pre-clinical models suggest reduced neuroinflammation and preservation of cognitive function in rodent models of Alzheimer’s disease; human data remain preliminary.

Process: Andrographolide, the principal bioactive diterpenoid, binds to the NF‑κB p65 subunit, inhibiting its nuclear translocation and thereby suppressing pro‑inflammatory cytokine transcription (TNF‑α, IL‑1β, IL‑6).
Pathway: Simultaneously, it activates the JAK/STAT pathway, enhancing interferon‑γ production and NK‑cell activity.
Antioxidant Pathway: The compound also stimulates the Nrf2/ARE pathway, increasing expression of antioxidant enzymes (HO‑1, SOD, catalase) and reducing oxidative stress.
Antiviral Action: In vitro, andro‑grapholide inhibits viral protease (e.g., SARS‑CoV‑2 3CL‑pro) and blocks the interaction of viral spike proteins with host ACE2 receptors.
Additional Actions: Additional actions include inhibition of COX‑2 and LOX enzymes, contributing to anti‑pain and anti‑inflammatory effects.
Overall Effect: The combined immunomodulatory, antiviral, and antioxidant actions underlie the observed clinical benefits.

Standardized Andrographis extracts (≥30 % andro‑grapholide) are typically taken in the range of 300 – 600 mg/day (divided into two doses) for acute respiratory support, with a typical course of 5–7 days.
For chronic inflammatory support, 900 mg‑1 g/day (divided 2–3 times daily) is used, often for 2‑4 weeks before re‑assessment.
Extracts with higher andro‑grapholide content (≥60 %) may be dosed at 200 mg/day (≈100 mg of pure andro‑grapholide).
It is advisable to take the supplement with food to reduce gastric upset.
In athletes or individuals seeking metabolic benefits, lower doses (150 mg, 1–2 times/day) are sometimes used.
For pediatric use, doses are scaled by weight (≈10 mg/kg/day) but only under professional supervision.

Andrographis is generally well‑tolerated; mild adverse effects include gastrointestinal discomfort, nausea, and occasional headache.
Rare cases of allergic dermatitis have been reported.
Contra‑indications: pregnancy (potential uterine stimulant) and lactation are cautioned against.
Interaction Risks: Interaction risks include potentiation of anticoagulants (e.g., warfarin) via platelet‑inhibitory activity, and possible additive effects with immunosuppressants (cyclosporine, tacrolimus).
Patients on antihypertensives or antidiabetic drugs should monitor blood pressure/glucose as the herb may modestly lower both.
Children under 12 years, pregnant women, and patients with autoimmune diseases should avoid or use only under medical guidance.

Andrographis contains the diterpenoid andrographolide (C₂₀H₃₀O₅, mol. wt ≈ 350.44 g·mol⁻¹).
Its IUPAC name is (1S,4R,5R,6S,7R,8S,9S,10R,12S)-1,4,5,6,7,8,9,10,12‑nonahydro‑3,13‑dihydroxy‑1‑[(2‑R‑hydroxy-3‑hydroxymethyl-2‑propyl)‑5‑hydroxy‑3‑methyl‑2‑oxabicyclo[5.3.0]‑dec-9‑en-7‑yl]‑4‑hydroxy‑5,7‑dimethoxy‑3‑methoxy‑1‑oxopent‑2‑en‑7‑yl‑2‑propyl‑7‑yl‑2‑octen‑4‑yl‑2‑oxobut-3-ene‑4‑yl‑1‑hydroxy‑2‑phenyl‑1‑dimethyl‑2‑oxabicyclo[6.3.0]‑dec‑7‑yl‑2‑oxoprop‑3‑en‑4‑yl‑1‑hydroxy‑2‑oxabicycle[5.3.0]‑dec‑9‑en‑7‑yl‑1‑hydroxy‑2‑oxabicycle[5.3.0]‑dec‑9‑en‑7‑yl‑1‑hydroxy‑2‑oxabicycle[5.3.0]‑dec‑9‑en‑7‑yl‑1‑hydroxy‑2‑oxabicycle[5.3.0]‑dec‑9‑en‑7‑yl‑1‑hydroxy‑2‑oxabicycle... (truncated for readability).
The molecule features a lactone ring, multiple hydroxyl groups, and a three‑dimensional fused cyclopentane‑lactone scaffold essential for NF‑κB inhibition.
It is moderately polar (log P ≈ 2.5) and soluble in ethanol, methanol, and partially in water, enabling extraction via ethanol‑based methods.

Andrographis paniculata is cultivated primarily in India, Thailand, and China.
The aerial parts are harvested at the flowering stage (≈70 days after sowing) for optimal andro‑grapholide content.
Commercial extracts are prepared using ethanol or ethanol‑water (70 %) maceration followed by spray‑drying into capsules or tablets; supercritical CO₂ extraction is emerging for higher purity.
Quality parameters include andro‑grapholide content ≥30 % (standardized), low heavy‑metal levels, and absence of pesticide residues (verified by USP or WHO GMP standards).
Some manufacturers employ biotechnological fermentation to produce pure andro‑grapholide, but most dietary supplements rely on plant‑derived extracts.
For optimal consistency, look for products certified by third‑party labs (e.g., USP, NSF) that disclose extraction solvent, standardization level, and batch‑specific analysis.