IngredientsAccepted botanical name: Cayaponia tayuya (Vell.) Cogn. The plant belongs to the family Cucurbitaceae, genus Cayaponia, species tayuya. Its accepted authority citation is Cayaponia tayuya (Vell.) Cogn., first formally described in Monographiae Phanerogamarum 3: 772, 1881.
Synonyms: Established botanical synonyms include Cayaponia piauhiensis, C. ficifolia, Bryonia tayuya, Trianosperma tayuya, T. piauhiensis, and T. ficcifolia. These historically used names reflect the species' repeated reclassification before its current placement in the genus Cayaponia.
Common names: Common vernacular names include tayuya, taiuiá, taioia, abobrinha-do-mato, anapinta, cabeca-de-negro, guardião, and tomba. In Brazil, Cayaponia tayuya is known as taiuiá; in Peru, it is called tayuya.
Plant description and habitat: Cayaponia tayuya is a vine that grows in the Amazon region of South America, in the nations of Brazil, Bolivia, and Peru. It is a climbing, lignified plant with a large swollen root. This important Amazon plant belongs to the Cucurbitaceae (gourd) family, which comprises over 100 genera and over 700 species — most of which are characterized by their long, tuberous roots. It is this root that is employed medicinally. Harvesting can only be performed during rainy season, when the ground is soft and wet; during dry season, the ground is too hard to extricate the root — which can extend to three feet long — from the dry clay soils in the Amazon.
Part used: The root is the part employed medicinally.
Pharmacopoeial status: It was first recorded in the Brazilian Pharmacopoeia as an official herbal drug in 1929; that document mentions the syrup "Caroba composto" obtained from tayuya roots along with other natural extracts.
Tayuya root is traditionally prepared in infusions with water, but can also be prepared by stirring 1 or 2 g of powdered root into juice, water, or food and taken in one-cup doses two to three times daily. The infusion is best prepared using one teaspoon of powder per cup of water, strained (or with the settled powder remaining), and drunk warm. It is traditionally taken in 1-cup dosages, 2–3 times daily.
The root is commercially available in several forms: dried shredded root for decoction or infusion, powdered root for direct consumption or capsule/tablet preparation, and as a standardized dry extract used in compound herbal formulas.
South American Indians have been using tayuya since prehistoric times, and the plant's value is well known. It has been used as a tonic and blood cleanser traditionally — usually with a bit of honey or stevia added to tone down its strong, bitter taste — and, in the Amazon rainforest, Indians have used the root of tayuya for snakebite and rheumatism for centuries. Indians in Colombia use the plant for sore eyes; indigenous tribes of Peru use it for skin problems.
Tayuya has a long history in Brazilian herbal medicine; it was first recorded in the Brazilian Pharmacopoeia as an official herbal drug in 1929. Brazilian botanist J. Monteiro da Silva reported that tayuya is used for the treatment of all types of pain and recommended it as an anti-syphilitic agent. It has been shown in folk medicine contexts to possess diverse pharmacological properties, acting as an analgesic, diuretic, anti-inflammatory, tonic, blood purifier, and detoxifier, and has been used in folk medicine for treating various pathologies including skin disorders, arthritis, and rheumatism. It is also commonly employed as a general analgesic for many conditions.
Tayuya has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia. In South American folk practice, tayuya is generally employed in combination with other plants and not as a monotherapy. It is generally employed by South American herbalists in combination with other plants, and not as a monotherapy.
Traditional purposes documented across cultures include:
Extensive phytochemical investigation of tayuya roots has identified two major classes of bioactive compounds: cucurbitacins (including novel nor-cucurbitacin glucosides unique to the species) and C-glycosylflavonoids.
The main plant chemicals found in tayuya include: alkaloids, cayaponosides, cucurbitacins, isoorientin, isovitexin, orientin, resins, saponins, spinosin, sterols, swertisin, vicenin-2, and vitexin.
Among the most pharmaceutically significant constituents are the cucurbitacins. Fractionation of an anti-inflammatory extract from Cayaponia tayuya roots yielded two active compounds, identified as 23,24-dihydrocucurbitacin B (1) and cucurbitacin R (2). These are tetracyclic triterpenoid compounds characteristic of the Cucurbitaceae family. These triterpenoids, present in free or glycosidic form, are generally responsible for the bitter taste of plants that contain them and are probably the principal cause of the antifeedant effects observed.
A family of novel nor-cucurbitacin glucosides unique to this species has been characterized through systematic phytochemical work by Japanese researchers. The bitter constituents in the root of Cayaponia tayuya were investigated, and 24 29-norcucurbitacin glucosides, named cayaponosides, were identified. Among 24 29-norcucurbitacin glucosides named cayaponosides, the structures of cayaponosides A5, B5, C4, C5b, and D2 were determined based mainly on spectral analyses. They are all glucosides of 29-nor-1,2,3,4,5,10-hexadehydrocucurbit-6-enes differing only in side chain structure.
The chloroform fraction obtained from the active root methanol extract was found to be more active than the ethyl acetate and butanol fractions. Subsequent phytochemical analysis demonstrated that the chloroform fraction is rich in cucurbitacins, whereas the ethyl acetate and butanol fractions are principally comprised of C-glycosyl flavonoids.
The flavonoid fraction was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were identified as the major components. A flavonoid-enriched fraction had previously been obtained from tayuya roots, and researchers identified two compounds in the butanol fraction, namely vicenin-2 and spinosin. These C-glycosylflavonoids contribute independently to the plant's anti-inflammatory profile through different mechanisms than the cucurbitacins.
A documented quality-control issue exists with commercial tayuya products. The plant drug "taiuia" is described in the Brazilian Pharmacopeia as the roots of Cayaponia tayuya (Vell.) Cogn.; however, other species of Cucurbitaceae are also popularly named "taiuia." Products labeled as C. tayuya in the Brazilian market may in fact be Wilbrandia ebracteata (Cogn.) Cogn., whose major C-glycosylflavones include spinosin, swertisin, isoswertisin, vitexin, isovitexin, vicenin-2, orientin, and isoorientin.
The cucurbitacins — particularly 23,24-dihydrocucurbitacin B and cucurbitacin R — have been the focus of the most mechanistic research. The effect of dihydrocucurbitacin B on the synthesis, release, and activity of pro-inflammatory enzymes (elastase, cyclooxygenase-2, and nitric oxide synthase-2) as well as its effect on different mediators (tumor necrosis factor-alpha and interleukin-1beta) was examined; dihydrocucurbitacin B modified the evolution of clinical symptoms, reducing swelling and bone and tissue damage along with the development of the disease, modifying cell infiltration and the expression of both nitric oxide synthase-2 and cyclooxygenase-2.
The activity of both compounds against oedema induced by serotonin was not modified by the glucocorticoid receptor antagonist mifepristone; however, the protein synthesis inhibitor cycloheximide abolished the anti-inflammatory response in both cases. Neither compound modified the production of LTB4 in rat polymorphonuclear leukocytes, nor did they exhibit analgesic properties at the dose assayed. This indicates the anti-inflammatory mechanism is likely protein-synthesis-dependent but does not operate through glucocorticoid receptor pathways.
Cucurbitacin R has been shown to exhibit activity against both adjuvant-induced arthritis and delayed-type hypersensitivity reactions. Previous studies demonstrated that the effects of cucurbitacin R stem from its inhibition of both cytokine production and lymphocyte proliferation.
At 22.30 μg/mL, the flavonoid-enriched test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively. These results indicate that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.
The nitric oxide production in RAW 264.7 macrophages was moderately reduced (42%) at 33.45 μg/mL; the flavonoid-enriched fraction had no effect on TNF-α production, but at 22.30 μg/mL it inhibited both iNOS and COX-2 expression by 98% and 49%, respectively.
Studies on dihydrocucurbitacin B in different models of delayed-type hypersensitivity (DTH) in mice showed that it inhibited inflammatory reactions induced by oxazolone, dinitrofluorobenzene, and sheep red blood cells, reducing both edema and cell infiltration. Analysis of inflamed tissues showed that dihydrocucurbitacin B reduced the presence of relevant cytokines including interleukin-1β, interleukin-4, and tumor necrosis factor-α.
Dihydrocucurbitacin B was also found to inhibit the proliferation of phytohemagglutinin-stimulated human T lymphocytes (IC₅₀ = 1.48 μM), halting the cell cycle in the G0 phase.
Results from this line of work suggest that dihydrocucurbitacin B curbs DTH reactions by inhibiting NFAT, which in turn suppresses the proliferation of the most relevant cells involved in DTH reactions, namely the T cells.
Documented data demonstrate that cucurbitacins possess strong pharmacological properties such as antitumor, anti-inflammatory, and hepatoprotective effects. Several molecular targets for cucurbitacins have been discovered, including fibrous-actin, signal transducer and activator of transcription 3 (STAT3), and cyclooxygenase-2.
Cucurbitacins are efficient antioxidants, and this property lies in their ability to scavenge free radicals such as hydroxyl radicals, superoxide anions, and singlet oxygen. This broad-spectrum radical-scavenging capacity surpasses what has been reported for other natural antioxidants such as grape-seed extract, wheat, alfalfa, and ginkgo biloba extracts. Reports also show that cucurbitacins adequately inhibit lipid peroxidation and oxidation.
Animal/preclinical evidence (the dominant body of evidence):
The earliest systematic pharmacological investigation of tayuya root was published in 1990 by RÃos et al. (Fitoterapia). Two animal studies performed in the early 1990s verify that root extracts provide analgesic and anti-inflammatory actions. One study documented that a root infusion given intragastrically to mice had an analgesic action. Another research group prepared the root in a methanol extract and reported mild anti-inflammatory actions when administered orally to mice.
A pivotal 2006 study published in the European Journal of Pharmacology specifically examined the isolated compound 23,24-dihydrocucurbitacin B in a well-established animal arthritis model. 23,24-Dihydrocucurbitacin B from the anti-rheumatic plant Cayaponia tayuya was tested on arthritis induced by adjuvant in Lewis rats to corroborate the anti-inflammatory properties of this plant. Arthritic rats were then treated with dihydrocucurbitacin B at 1 mg/kg orally, daily, for one week. This triterpenoid has been shown to exert anti-inflammatory activity on different experimental models of inflammation; it has a significant effect on adjuvant-induced arthritis in rats, reducing both inflammation and tissue damage and inhibiting the expression of several enzymes and mediators implicated in the inflammatory process, including elastase, cyclooxygenase, nitric-oxide synthase-2, and tumor necrosis factor-α.
A 2004 study published in Planta Medica by Recio et al. evaluated the two principal cucurbitacins (23,24-dihydrocucurbitacin B and cucurbitacin R) isolated from tayuya roots. The fractionation yielded two active compounds; both were evaluated for their anti-inflammatory activity on several experimental models of pain and inflammation. The activity of both compounds against oedema induced by serotonin was not modified by the glucocorticoid receptor antagonist mifepristone; however, the protein synthesis inhibitor cycloheximide abolished the anti-inflammatory response in both cases.
A 2009 study published in the Journal of Ethnopharmacology (Aquila et al.) used two mouse ear oedema models to evaluate a flavonoid fraction from tayuya roots. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction at a dose of 0.5 mg/ear inhibited the oedema by 66% (4.2 ± 0.6 mg vs. 12.3 ± 1.4 mg, P < 0.01) while in the subchronic model, the inhibition reached 37% at a dose of 0.5 mg/ear × 7 applications (7.5 ± 0.6 mg vs. 11.9 ± 1.3 mg, P < 0.05). The conclusion was that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.
Evidence strength: The anti-inflammatory and anti-arthritic evidence is entirely preclinical (animal models and in vitro cell culture). While the mechanistic data are internally consistent and the animal studies are published in peer-reviewed journals, no controlled human clinical trials have been conducted. While tayuya's compounds have come under some scientific scrutiny, and many of the documented uses in herbal medicine could be explained by some of the activities of its chemicals, very little research has been performed on the biological activity of the plant itself. Evidence must therefore be characterized as preliminary.
Studies have examined the effects of dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, on different models of delayed-type hypersensitivity (DTH) in mice. In experiments with mice, dihydrocucurbitacin B inhibited the inflammatory reactions induced by oxazolone, dinitrofluorobenzene, and sheep red blood cells, reducing both the edema and cell infiltration. Analysis of inflamed tissues showed that dihydrocucurbitacin B reduced the presence of the most relevant cytokines implicated in these processes, including interleukin-1β, interleukin-4, and tumor necrosis factor-α.
A separate study by Escandell et al. (2010, Journal of Pharmacology and Experimental Therapeutics) examined cucurbitacin R on the same models. Cucurbitacin R is known to exhibit an anti-inflammatory effect in different experimental models of inflammation; this study outlined the effect of cucurbitacin R on T lymphocyte proliferation, cytokine production, and nuclear factor activation, as well as its influence on various experimental models of DTH in mice.
Evidence strength: All immunomodulatory evidence is animal and in vitro. No human trials have been performed. Mechanistic findings (NFAT inhibition, T-cell proliferation suppression, cytokine downregulation) are suggestive but cannot be extrapolated to clinical efficacy in humans.
The cayaponosides — the nor-cucurbitacin glucosides unique to tayuya roots — have been examined in in vitro cancer-screening assays. In a primary screening of twenty-four 29-nor-cucurbitacin glucosides isolated from the roots of Cayaponia tayuya, cayaponosides B, B3, D, D3b, and C2 exhibited significant inhibitory effects on Epstein-Barr virus (EBV) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA). This research was reported by the National Cancer Center Research Institute, Kyoto Pharmaceutical University, Japan (Konoshima et al., 1995, Biological and Pharmaceutical Bulletin).
Dihydrocucurbitacin B has been found to possess potential anticancer properties, and it could have applications as an immunodepressant, acting by means of a mechanism in which the inhibition of both TNF-α and interleukin-1β is involved.
Several plants used in traditional medicine to treat both inflammatory diseases and various types of tumors are rich in cucurbitacins, a fact which has given rise to studies concerning their potential use as anti-inflammatory and anticancer agents. Nevertheless, since many cucurbitacins are extremely toxic, relatively few papers have dealt with their pharmacological activity. Recently, however, the relationship between the toxicity of a compound and its chemical pattern of substitution has been established, allowing for a more in-depth understanding of this class of triterpenes.
Evidence strength: Exclusively in vitro (EBV-activation assay) and animal data. No human oncology trials have been conducted specifically with tayuya or its isolated cayaponosides. This area must be characterized as early exploratory research only.
Animal studies performed in the early 1990s verify that root extracts provide analgesic and anti-inflammatory actions; one study documented that a root infusion given intragastrically to mice had an analgesic action. However, when isolated cucurbitacins were tested, neither 23,24-dihydrocucurbitacin B nor cucurbitacin R modified the production of LTB4 in rat polymorphonuclear leukocytes, nor did they exhibit analgesic properties at the dose assayed. This suggests that the analgesic effects observed with crude root preparations may arise from compounds other than the principal cucurbitacins, or require specific dose ranges not yet fully defined.
While tayuya has a long history of traditional use by herbalists in the United States and South America for all types of pain and joint aches, it is at best a mild analgesic.
Evidence strength: Limited and inconsistent animal data; no human clinical trials. The analgesic signal in crude extracts is not clearly attributable to specific isolated compounds at the doses studied.
Flavone phytochemicals in tayuya have been reported to act as potent scavengers of free radicals, providing an antioxidant effect as well as protecting against damage induced by gamma-radiation. The flavonoid-enriched fraction showed no toxicity at 33.45 μg/mL on RAW 264.7 macrophages, and while nitric oxide production was moderately reduced (42%) at this concentration, the fraction had no effect on TNF-α production.
Evidence strength: In vitro antioxidant data only. No clinical antioxidant studies have been conducted in humans.
One in vitro study by Brazilian scientists reported that tayuya did not evidence any antimicrobial properties against several common bacteria, fungi, and yeast.
Evidence strength: Single in vitro study with negative findings; no evidence of clinically relevant antimicrobial activity.
Based on the available peer-reviewed literature, tayuya and its isolated compounds have been most extensively studied in relation to the following body systems, all at a preclinical level:
In traditional use, tayuya was additionally associated with the digestive system (dyspepsia, IBS), the nervous system (neuralgia, sciatica), dermatology (acne, eczema), and metabolic regulation, though none of these applications have been formally investigated in clinical trials.
Tayuya root is traditionally prepared in infusions with water, but can also be prepared by stirring 1 or 2 g of powdered root into juice, water, or food, taken in one-cup doses two to three times daily.
In the scientific literature, dosages were specific to experimental models:
No standardized human clinical dosages have been established in the peer-reviewed literature. Traditional dosage ranges reported in herbal reference sources are not derived from clinical trials.
The latter group reported no toxic effects in mice (oral dosages of a methanol root extract) at 2 g per kg of body weight; however, an LD50 of 500 mg/kg was established when injected intraperitoneally. This divergence between oral and intraperitoneal toxicity thresholds is consistent with the general toxicology of cucurbitacins and is pharmacologically important.
The toxicity for the butanol extract (flavonoid-rich fraction) was higher than 2000 mg/kg for both intraperitoneal and oral administration in the animal models studied. The cucurbitacin-rich chloroform fraction showed lower oral and IP LD50 values, consistent with the general understanding that cucurbitacins as a class can be acutely toxic at higher doses.
Several plants used in traditional medicine to treat inflammatory diseases and tumors are rich in cucurbitacins. Since many cucurbitacins are extremely toxic, relatively few papers have dealt with their pharmacological activity.
Cucurbitacins as a chemical class are widely recognized as highly bioactive molecules with a narrow margin between therapeutic and toxic concentrations. Cucurbitacins possess strong pharmacological properties, and several molecular targets including fibrous-actin, STAT3, and COX-2 have been identified, indicating broad cellular effects. Disruption of actin cytoskeletal dynamics is a particularly well-known mechanism of cucurbitacin toxicity.
A significant practical concern is botanical adulteration. The plant drug "taiuia" is described in the Brazilian Pharmacopeia as the roots of Cayaponia tayuya (Vell.) Cogn.; however, other species of Cucurbitaceae are also popularly named "taiuia," and products labeled as C. tayuya in the Brazilian market may actually be Wilbrandia ebracteata. This creates uncertainty about the phytochemical consistency and predicted safety profile of commercial products.
No controlled human safety studies exist for tayuya during pregnancy, breastfeeding, or in pediatric populations. Given the known cytotoxic and immunomodulatory activity of cucurbitacins at cellular level — including inhibition of T-lymphocyte proliferation and halting of the cell cycle — particular caution is warranted in immunocompromised individuals and pregnant women. These considerations are based on the mechanistic properties of the plant's principal bioactive constituents as documented in peer-reviewed studies.
No specific human drug-interaction studies have been published in the peer-reviewed literature for tayuya as a whole plant or extract. Given the demonstrated COX-2 inhibitory properties of both its cucurbitacin and flavonoid fractions, pharmacodynamic additive effects with other anti-inflammatory drugs and NSAIDs are theoretically possible. The immunosuppressive properties of dihydrocucurbitacin B demonstrated in vitro and in animal models suggest that potential interactions with immunosuppressant drugs could be mechanistically plausible, though this has not been studied in humans.
The body of scientific evidence for tayuya is entirely preclinical. The published peer-reviewed research — including studies in Journal of Ethnopharmacology, European Journal of Pharmacology, Planta Medica, and Journal of Pharmacology and Experimental Therapeutics — consistently demonstrates anti-inflammatory, anti-arthritic, and immunomodulatory effects of isolated compounds (particularly 23,24-dihydrocucurbitacin B, cucurbitacin R, and the flavonoid fraction) in rodent models and cell culture. The mechanistic basis for these effects is well-characterized. However, no randomized controlled human clinical trials, systematic reviews of clinical trials, or formal dose-finding studies in humans have been published. Traditional use in Brazilian, Peruvian, and Colombian folk medicine extends back centuries and its formal inclusion in the Brazilian Pharmacopoeia from 1929 reflects long-standing recognized use, but this does not constitute evidence of clinical efficacy or safety by modern standards. The gap between preclinical results and any established human evidence remains entirely unfilled as of the available literature.
Health conditions that Tayuya may help support.
Body systems that Tayuya may help support.
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