Chemical Composition
Detailed phytochemical analysis of all bioactive compounds Chemical substances in plants with physiological effects on the human organism. Guayusa contains over 100 identified bioactive compounds. Scientific name of the Guayusa plant. First described in 1901 by Theodor Loesener. Synonyms: Ilex guayusa var. macrophylla.bioactive compounds
Ilex guayusa
- Guayusa is caffeine-rich; L-theanine
caffeine
Purine alkaloid with stimulating effects on the central nervous system. Guayusa contains 1.7-7.6% caffeine (dry weight), depending on variety, location, and processing.
More Infocan make the focus feel calmer.L-theanine
Amino acid with relaxing effects found in Guayusa (0.02-0.05%) and green tea. Acts synergistically with caffeine and reduces nervousness.
More Info - Chlorogenic acids, flavonols, and catechins shape taste and antioxidant potential.
- HPLC/LC-MS reveals profiles and differences between samples and batches.
HPLC
High-Performance Liquid Chromatography - standard method for quantitative analysis of polyphenols and alkaloids in Guayusa. Typical method: C18 column, acetonitrile gradient, UV detection at 280 nm.
More Info - Depending on brewing, guayusa can sit between tea and coffee.
Guayusa’s key compounds are caffeine, L-theanine, and polyphenols Group of secondary plant metabolites with antioxidant effects. Guayusa contains 12-18% total polyphenols (dry weight), mainly chlorogenic acids and flavonoids.polyphenols
- Readers who want a practical ingredient-based understanding
- People interested in antioxidantsand phytochemical profiles
antioxidants
Substances that prevent oxidative damage caused by free radicals. Guayusa contains high amounts of polyphenols with antioxidant effects (ORAC value: 127–159 µmol TE/g).
More Info - Users optimizing preparation for real-life effects
- Interpreting single lab values without context
- Very high caffeine intake without adjustment
- Broad health claims without evidence levels
To test Guayusa in daily life, start with a moderate brew and adjust dose and steep time gradually.
View GUYA productsEveryday overview
Values vary with origin, leaf quality, and preparation. Here’s the quick overview before the details.
- Guayusa is caffeine-rich; L-theanine can make the focus feel calmer.
- Brew time and temperature control strength.
- Chlorogenic acids, flavonols, and catechins shape taste and antioxidant potential.
- More extraction often means more bitterness and more polyphenols.
- HPLC/LC-MS reveals profiles and differences between samples and batches.
- Single numbers are ranges, not fixed constants.
- Depending on brewing, guayusa can sit between tea and coffee.
- Notable combo: caffeine plus L-theanine in one plant.
Many describe guayusa as “alert but less jittery”: caffeine for energy, L-theanine for calmer focus.
Overview
Guayusa contains a complex mixture of Bioactive Compounds that synergistically account for the unique properties of the plant. The phytochemical composition has been extensively characterized using modern analytical methods (HPLC-DAD-ESI/MSn, LC-MS, GC-MS).
The main active compound groups are Caffeine and other Polyphenols (including Flavonoids and Tannins), which together with L-Theanine are responsible for the unique adaptogenic effect.
Main Components
| Compound class | Main representatives | Concentration (% dry weight) | Biological activity |
|---|---|---|---|
| Methylxanthines | caffeine, theobromine | 1,7-7,6% | Stimulating, neuroprotective |
| Amino acids | l_theanine | 0,13% | Anxiolytic, focusing |
| polyphenols | chlorogenic_acid, Flavonole | 8-16% | , flavonols |
| saponins | ursolic_acid, Oleanolsäure | 2-4% | Antioxidant, anti-inflammatory |
| Carotenoids | Lutein, β-Carotin | 0,01-0,02% | Hepatoprotective, antidiabetic |
Methylxanthines: The Stimulating Alkaloids
Methylxanthines are Purine alkaloids responsible for the stimulating properties of Guayusa. Guayusa contains the highest Caffeine concentration of all known plants.
Caffeine - Detailed Analysis
Concentrations in Various Studies
| Study | Year | Method | Caffeine (% DW) |
|---|---|---|---|
| Holmstedt & Lindgren | 1972 | Spectrophotometry | 1,8% |
| Lewis et al. | 1987 | HPLC | 1,7% |
| Lewis et al. (Dekokt, 1h) | 1991 | HPLC | 3,33% |
| Wise & Negrin | 2020 | HPLC (Durchschnitt) | 3,9% |
| García-Ruiz et al. | 2017 | HPLC-MS | 2,4-3,1% |
| Maximale Konzentration | Various | - | 7,6% |
The Caffeine concentration varies greatly depending on:
- Young leaves: 4-7.6%, old leaves: 1.7-2.5%
- Harvest time: Dry season higher than rainy season
- Altitude, soil composition
- Fermentation reduces Caffeine by 15-20%
Pharmacokinetics (Krieger et al. 2016)
Clinical study with 20 healthy adults, 400 mg Caffeine from Guayusa vs. synthetic caffeine:
| Parameter | Guayusa Caffeine | Synthetic Caffeine | Difference |
|---|---|---|---|
| Cmax (μg/mL) | 4,8 ± 1,2 | 5,1 ± 1,3 | Nicht signifikant |
| Tmax (hours) | 1,8 ± 0,6 | 1,2 ± 0,4 | Delayed (p<0,05) |
| AUC (μg·h/mL) | 28,3 ± 7,1 | 29,1 ± 7,5 | Bioequivalent |
| t½ (hours) | 5,2 ± 1,1 | 5,0 ± 1,0 | Nicht signifikant |
Guayusa Caffeine is absorbed slightly more slowly (delayed Tmax) but is bioequivalent to synthetic caffeine. The delayed absorption could lead to smoother, longer-lasting effects.
Extraction Efficiency (Lewis et al. 1991)
Quantitative measurement of different preparation methods:
| Method | Caffeine extraction (%) | Final concentration in beverage |
|---|---|---|
| 1 Stunde kochen | 100% | 3,33% (maximal) |
| 10 Minuten kochen | 77,8% | 2,59% |
| 24 Stunden kalt | 83,5% | 2,78% |
| 5 Minuten Aufguss (90°C) | ~60% | ~2,0% |
The traditional Achuar method (1 hour boiling) is optimal for maximum Caffeine extraction. Modern preparations (5-10 minutes) extract 60-78% of the caffeine.
Theobromine
Theobromine is another methylxanthine found in Guayusa, but in significantly lower concentrations than Caffeine.
| Study | Theobromin (% DW) | Caffeine:Theobromine ratio |
|---|---|---|
| Lewis et al. 1991 | 0,02% | 85:1 |
| Wise & Negrin 2020 | 0,01-0,04% | 100:1 bis 200:1 |
| For comparison: Cacao | 1,5-3,0% | 1:10 (umgekehrt!) |
Theobromine has weaker stimulating effects than Caffeine, but:
- Longer half-life (7-8 hours vs. 5 hours for Caffeine)
- Bronchodilatory effect (expands airways)
- Diuretic effect
- Vasodilatory (expands blood vessels)
- Mood-enhancing
L-Theanine - The Special Feature
L-Theanine is an amino acid found almost exclusively in Camellia sinensis (Tee) vorkommt. Die Entdeckung von L-Theanin in Guayusa (García-Ruiz et al. 2017) war eine wissenschaftliche Sensation.
Concentration
| Plant | L-Theanine (mg/g DW) |
|---|---|
| Guayusa | 1,3 ± 0,2 |
| Green tea | 5-15 |
| Black Tea | 2-8 |
| White Tea | 4-12 |
| Yerba Mate | 0 (not detected) |
| Coffee | 0 (not detected) |
Bedeutung: Guayusa is the only known non-Camellia plant, die L-Theanin in signifikanten Mengen enthält.
Caffeine-Theanine Synergy
The combination of Caffeine and L-Theanine is unique and scientifically well documented:
| Effect | Only Caffeine | Caffeine + L-Theanine |
|---|---|---|
| Alertness | +++ | +++ |
| Nervousness/Jitteriness | ++ | +/- |
| Focus | ++ | +++ |
| Relaxation | - | ++ |
| Alpha-Wellen (EEG) | Reduced | Increased |
| Heart rate | Increased | Normal |
Mechanism of action:
- Increases GABA, serotonin, and dopamine in the brain
- Blocks excitatory glutamate receptors
- Promotes alpha wave activity (relaxed alertness)
- Reduces Caffeine-induced vasoconstriction
- Extends attention span without sedation
Optimal Caffeine:Theanine Ratio
Studies show that a ratio of 2:1 bis 4:1 (Koffein:Theanin) optimal ist für:
- Maximum cognitive performance
- Minimal side effects
- Longer duration of action
Guayusa ratio: With ~3% Caffeine and 0.13% L-Theanine, Guayusa has a ratio of approximately 23:1. Dies ist höher als das Optimum, aber:
- Polyphenols (especially catechins) enhance L-Theanine effects
- Theobromine contributes to relaxation
- Traditional preparation (long cooking time) can increase L-Theanine extraction
Learn More About L-Theanine
Discover our partner wiki with in-depth information on L-Theanine: effects, optimal dosage, daily dose calculator, scientific studies and much more.
Visit L-Theanine Wiki →Polyphenols: The Antioxidant Powerhouses
Polyphenols are secondary plant compounds with strong antioxidant, anti-inflammatory, and health-promoting effects. Guayusa contains an exceptionally high concentration of various polyphenols.
Total Polyphenol Content
| Study | Method | TPC (mg GAE/g DW) |
|---|---|---|
| García-Ruiz et al. 2017 | Folin-Ciocalteu | 127,8 ± 8,3 |
| Pardau et al. 2016 | Folin-Ciocalteu | 145,2 ± 12,1 |
| Dueñas et al. 2016 | Folin-Ciocalteu | 112,4 ± 9,7 |
| Average | - | 128,5 mg GAE/g |
For comparison (mg GAE/g DW):
- Green tea: 80-120
- Black tea: 60-90
- Yerba Mate: 90-110
- Coffee: 50-70
- Guayusa: 128,5 ((highest value!))
New findings (2024–2026) with direct relevance to constituents, bioavailability, and processing. Evidence level is indicated for each point.
29 phenolics identified with chlorogenic-acid derivatives dominant. Longer infusion increased total phenolic content; water vs ethanol differed markedly. During in vitro digestion, total phenolics increased by stage, while Flavonoids and di-O-CQA derivatives decreased.
Not a typical household brew (very long times and ethanol). Still important: preparation and digestion shift the phenolic profile that may be available.
29 metabolites by GC-MS; activity varied by origin/age. No hemolysis and no alpha-amylase inhibition reported; alpha-glucosidase inhibition observed (best IC50 ~68 µg/mL).
Mechanistic in vitro screening (incl. docking). Useful to show variability by origin/age; not a clinical efficacy proof.
PMID/DOI: 38472807 · 10.3390/foods13050694 · 41097306 · 10.3390/molecules30193885
Chlorogenic acids (Hydroxycinnamic acids)
Chlorogenic acids are esters of caffeic acid and quinic acid. They are the most common Polyphenols in Guayusa.
Identified Chlorogenic Acids (García-Ruiz et al. 2017)
| Compound | Concentration (mg/g DW) | % of Polyphenols |
|---|---|---|
| 5-O-Caffeoylquinic acid (5-CQA) | 42,3 ± 3,8 | 33% |
| 3-O-Caffeoylquinic acid (3-CQA) | 18,7 ± 2,1 | 15% |
| 4-O-Caffeoylquinic acid (4-CQA) | 12,4 ± 1,6 | 10% |
| 3,4-Dicaffeoylquinic acid | 8,9 ± 1,2 | 7% |
| 3,5-Dicaffeoylquinic acid | 6,2 ± 0,9 | 5% |
| 4,5-Dicaffeoylquinic acid | 4,1 ± 0,7 | 3% |
| Total | 92,6 mg/g | 73% |
Biological activity of chlorogenic acids:
- Neutralizes free radicals, protects DNA
- Inhibits α-glucosidase and α-amylase (slows glucose absorption)
- Hepatoprotective: Protects liver from toxins
- Cardioprotective: Lowers blood pressure, improves endothelial function
- Neuroprotective: Protects against oxidative stress in the brain
- Anti-inflammatory: Reduces pro-inflammatory cytokines
Flavonols
Flavonols are a subclass of Flavonoids with strong antioxidant activity.
Identified Flavonols (García-Ruiz et al. 2017)
| Compound | Concentration (mg/g DW) |
|---|---|
| Quercetin-3-O-hexoside | 14,2 ± 1,8 |
| Quercetin-3-O-rutinoside (Rutin) | 8,7 ± 1,2 |
| Kaempferol-3-O-hexoside | 5,3 ± 0,8 |
| Quercetin-3-O-rhamnoside | 3,1 ± 0,5 |
| Kaempferol-3-O-rutinoside | 2,4 ± 0,4 |
| Isorhamnetin-3-O-hexoside | 1,8 ± 0,3 |
| Total | 35,5 mg/g |
The most common flavonol in Guayusa
- Strong antioxidant (higher than vitamin C and E)
- Antihistamine (reduces allergy symptoms)
- Anti-inflammatory (inhibits COX-2 and lipoxygenase)
- Antiviral (inhibits virus replication)
- Cardioprotective (lowers LDL cholesterol)
- Cancer preventive (induces apoptosis in cancer cells)
- Neuroprotective (protects against Alzheimer’s and Parkinson’s)
- Antidiabetic (improves insulin sensitivity)
Catechins
Catechins are flavan-3-ols, best known from green tea. Guayusa also contains catechins, but in smaller amounts.
| Catechin | Guayusa (mg/g DW) | Green tea (mg/g DW) |
|---|---|---|
| Epigallocatechin gallate (EGCG) | 2,1 ± 0,4 | 30-80 |
| Epicatechin (EC) | 1,8 ± 0,3 | 10-25 |
| Epigallocatechin (EGC) | 1,2 ± 0,2 | 15-40 |
| Epicatechin gallate (ECG) | 0,9 ± 0,2 | 10-20 |
| Total | 6,0 mg/g | 65-165 mg/g |
Although Guayusa contains fewer catechins than green tea, they still contribute to antioxidant capacity and enhance the effect of L-Theanine.
Saponins & Triterpenes
Saponins are glycosylated triterpenes or steroids with soap-like properties (name from Latin sapo = = soap). Guayusa contains pentacyclic triterpenoid Saponins.
Identified Saponins (Chianese et al. 2019)
| Compound | Structure | Concentration (mg/g DW) |
|---|---|---|
| Ursolic acid derivatives | Pentacyclic triterpene | 12,4 ± 2,1 |
| Oleanolic acid derivatives | Pentacyclic triterpene | 8,7 ± 1,6 |
| Ilexsaponin A | Glycosylated Ursolic acid | 5,2 ± 0,9 |
| Ilexsaponin B | Glycosylated oleanolic acid | 3,8 ± 0,7 |
| Total | - | 30,1 mg/g |
Biological Activity
Ursolic acid
- Hepatoprotective: Protects liver from toxins and fatty liver
- Improves insulin sensitivity, activates AMPK
- Increases muscle mass, reduces muscle breakdown
- Anti-inflammatory: Inhibits NF-κB signaling pathway
- Antitumoral: Induces apoptosis in cancer cells
Oleanolic Acid
- Cardioprotective: Lowers cholesterol, protects the heart
- Hepatoprotective: Regenerates liver cells
- Antidiabetic: Lowers blood sugar
- Neuroprotective: Protects against neurodegenerative diseases
Carotenoids
Carotenoids are fat-soluble pigments with antioxidant effects. Despite its green color, Guayusa contains significant amounts of carotenoids Fat-soluble plant pigments with antioxidant effects. Guayusa contains β-carotene (0.8-1.2 mg/100g), lutein (5.2-7.8 mg/100g), and zeaxanthin.carotenoids
Identified Carotenoids (García-Ruiz et al. 2017)
| Carotenoid | Concentration (μg/g DW) | Function |
|---|---|---|
| Lutein | 87,3 ± 12,4 | Eye health (macular protection) |
| β-Carotin | 42,1 ± 6,8 | Provitamin A, immune system |
| Violaxanthin | 18,7 ± 3,2 | Antioxidant |
| α-Carotin | 12,3 ± 2,1 | Provitamin A |
| Neoxanthin | 8,9 ± 1,5 | Antioxidant |
| Total | 169,3 μg/g | - |
The most common carotenoid in Guayusa
- Protects the macula (yellow spot) in the eye from oxidative stress
- Reduces risk of age-related macular degeneration (AMD)
- Improves visual acuity and contrast vision
- Anti-inflammatory
Comparison with other Caffeine-containing plants
Comprehensive Comparison Table
| Compound | Guayusa | Green tea | Black Tea | Yerba Mate | Coffee | Cocoa | Guarana | Kola Nut |
|---|---|---|---|---|---|---|---|---|
| Caffeine (% DW) | 3,9 | 2,5-4,5 | 2,0-4,0 | 0,7-1,7 | 1,2-1,5 | 0,1-0,7 | 3,5-7,0 | 1,5-3,5 |
| Theobromin (% DW) | 0,02 | 0,01-0,02 | 0,01-0,02 | 0,3-0,9 | 0 | 1,5-3,0 | 0,02-0,05 | 0,02-0,1 |
| L-Theanine (mg/g) | 1,3 | 5-15 | 2-8 | 0 | 0 | 0 | 0 | 0 |
| Polyphenole (mg GAE/g) | 128 | 80-120 | 60-90 | 90-110 | 50-70 | 40-60 | 30-50 | 20-40 |
| Chlorogenic acids (mg/g) | 92,6 | 5-15 | 3-10 | 40-80 | 70-120 | 0,5-2 | 10-20 | 5-15 |
| Catechins (mg/g) | 6,0 | 65-165 | 10-40 | 2-8 | 0,5-2 | 30-80 | 1-5 | 1-3 |
| Saponins (mg/g) | 30,1 | 0,1-0,5 | 0,1-0,3 | 5-15 | 0 | 0 | 2-8 | 0,5-2 |
| ORAC (μmol TE/g) | 127,8 | 60-100 | 40-80 | 80-120 | 30-50 | 80-200 | 40-70 | 20-40 |
Unique Properties of Guayusa
- Highest polyphenol content aller koffeinhaltigen Pflanzen
- Only non-tea plant mit L-Theanin
- Highest chlorogenic acid concentration (außer Kaffee)
- High saponin content (nur Yerba Mate höher)
- Balanced Caffeine:Theobromine ratio
- Highest ORAC values (außer Kakao)
Analytical Methods
The phytochemical characterization of Guayusa is carried out using modern chromatographic and spectroscopic methods.
Constituent takeaway: origin, light/shade, and age are major drivers when comparing profiles or product batches.
Shows cultivation/harvest parameters (age, shade management) can measurably shift metabolite classes, affecting aroma, taste, and standardization.
PMID/DOI: 41604851 · 10.1016/j.chroma.2026.466732 · 41643380 · 10.1016/j.foodchem.2026.148238
Methods & details
HPLC-DAD-ESI/MSn (García-Ruiz et al. 2017)
High Performance Liquid Chromatography with Diode-Array Detector and Electrospray Ionization Mass Spectrometry
Method Details:
- Luna C18 (25 cm × 0.46 cm, 5 μm)
- Methanol/Water with formic acid (Gradient)
- Flow rate: 1,0 mL/min
- Injection volume:
- Detection wavelengths: 280, 330, 360, 520 nm
- MS-Modus: Negativ-Ionisation
- Mass range: m/z 100-1200
Identified Compounds:
- 14 Polyphenols (chlorogenic acids, flavonols)
- Structural elucidation by MSn fragmentation
- Quantification by external calibration
RRLC (Rapid Resolution Liquid Chromatography)
For carotenoid analysis:
- Extraction: Hexan/Aceton (1:1 v/v)
- Saponification: Methanolisches KOH (30 g/100 mL)
- Detection: 450 nm (DAD)
- Quantification: Externe Kalibrierung mit Standards
Antioxidant Capacity
ORAC (Oxygen Radical Absorbance Capacity)
- Measures ability to neutralize peroxyl radicals
- Fluorescence-based (fluorescein as probe)
- Result: μmol Trolox equivalents/g
- Guayusa: 127.8 ± 8.3 μmol TE/g
DPPH (2,2-Diphenyl-1-picrylhydrazyl)
- Measures radical scavenging activity
- Spectrophotometrically (515 nm)
- Fast and simple
FRAP (Ferric Reducing Antioxidant Power)
- Measures reducing power
- Fe3+ → Fe2+ reduction
- Correlates with polyphenol content
Influence of processing on constituents
The processing of Guayusa leaves has significant effects on the phytochemical composition.
Optimized (120 bar/45°C), chlorogenic acids were concentrated (43.02 → 237 mg/g) while Caffeine was selectively reduced to <1% w/w; PVP improved recovery yield substantially.
Ingredient/processing context, not brewed tea. Relevant as a green route to polyphenol-rich, low-Caffeine guayusa ingredients for products.
PMID/DOI: 39598698 · 10.3390/molecules29225309
Processing Steps and Their Effects (García-Ruiz et al. 2017)
| Processing | Polyphenols | Caffeine | Carotenoids | ORAC |
|---|---|---|---|---|
| Fresh leaves | 100% | 100% | 100% | 100% |
| Blanched | 92% | 98% | 78% | 88% |
| Fermented | 85% | 82% | 65% | 79% |
| Dried (sun) | 88% | 95% | 70% | 85% |
| Freeze-dried | 97% | 99% | 92% | 96% |
Recommendations for Maximum Bioactivity
- Freeze drying preserves most ingredients (but expensive)
- Sun drying is acceptable (traditional method)
- reduces bitterness but also bioactivity
- inactivates enzymes, stabilizes color
- Dark, dry, airtight → minimizes degradation
Effect of Preparation
| Preparation Method | Polyphenol Extraction | Caffeine extraction |
|---|---|---|
| Boiling (1 hour) | 95-100% | 100% |
| Boiling (10 minutes) | 75-85% | 78% |
| Infusion (5 minutes, 90°C) | 60-70% | 60% |
| Cold extraction (24 hours) | 70-80% | 84% |
Boil for 10-15 minutes or steep for 5-10 minutes at 90-95°C for a good compromise between extraction and taste.
Important Sources
- García-Ruiz, A., et al. (2017). Guayusa (Ilexguayusa L.) new tea: phenolic and carotenoid composition and antioxidant capacity. Journal of the Science of Food and Agriculture, 97(12), 3929-3936.
Ilex
Botanical genus of hollies with about 400-600 species worldwide. This genus includes Ilex guayusa, Ilex paraguariensis (Mate), and Ilex vomitoria (Yaupon).
More Info - Krieger, D.R., et al. (2016). The safety, pharmacokinetics, and nervous system effects of two natural sources of Caffeine in healthy adult males.
- Lewis, W.H., et al. (1991). Ritualistic use of the holly Ilex guayusa by Amazonian Jivaro Indians. Journal of Ethnopharmacology, 33(1-2), 25-30.
- Chianese, G., et al. (2019). Phytochemical analysis of the Ecuadorian plant Ilex guayusa Loes.
- Pardau, M.D., et al. (2016). Antioxidant properties of Ilex guayusa: A new source of dietary Polyphenols.
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