Davilla rugosa

Davilla rugosa (Cipó-Caboclo): A Comprehensive Reference

1. Identity and Botanical Classification

1.1 Taxonomy and Nomenclature

Davilla rugosa Poir. is classified within the order Dilleniales, family Dilleniaceae, genus Davilla. The accepted botanical name is Davilla rugosa Poir., first formally described in 1812. The species was described by Lamarck and Poiret in the Encyclopédie Méthodique, Botanique, Supplément, Tome 2, published in Paris by H. Agasse, at page 2:457.

Recognized synonyms include Davilla brasiliana A.DC., Davilla itaparicensis Casar., Davilla pilosa Miq., and Tetracera lima Willd. ex DC. Several botanical varieties have also been described, including Davilla rugosa subsp. rugosa, var. capitata Rusby, var. kunthii Eichler, var. luschnathii Eichler, var. martii Eichler, var. riedelii Eichler, var. sellowii Eichler, and var. willdenowii Eichler.

1.2 Common Names

Davilla rugosa Poiret, Dilleniaceae, is a liana known commonly as cipó-caboclo, which grows in Brazil and in other countries of Central and South America. It is also popularly known as "folha de lixa e cipó-caboclo," a woody vine native to forest edges widely distributed across Brazil. D. rugosa is also known as "fire liana" and is very common in forest edges, with very wide geographic distribution in Brazil.

1.3 Morphology and Natural Habitat

The native range of this species is Central and South Tropical America. It is a climbing shrub that grows primarily in the wet tropical biome. The species belongs to the Dilleniaceae family, which is composed of approximately 12 genera and 300 species, exclusively tropical, mostly comprised of vines and shrubs.

In Rio de Janeiro, three genera of Dilleniaceae occur: Davilla, Doliocarpus, and Tetracera. Doliocarpus and Tetracera have successive cambia, a cambial variation that facilitates the separation of these genera from Davilla. Davilla has a stem with a segmented vascular cylinder. In Rio de Janeiro, Brazil, six species of Davilla occur: Davilla glaziovii, Davilla grandifolia, Davilla latifolia, Davilla nitida, D. rugosa, and D. tintinnabulata. The stems of all these species have very similar external morphology.

1.4 Common Preparations and Dosage Forms in Commerce

Since it was discovered by the Carijó Indians, the stems are widely used for the preparation of anti-inflammatory, antiulcer, purgative, stimulant, aphrodisiac, and tonic hydroalcoholic extracts and aqueous infusions. The stems of cipó-caboclo are sold in major herb markets in Rio de Janeiro State and open-air street markets in the City of Rio de Janeiro.

Davilla rugosa is also an ingredient in a registered topical ointment product (Hemovirtus) available in Brazilian pharmacies without a prescription. This product contains Hamamelis virginiana L., Davilla rugosa P., Atropa belladonna L., menthol, and lidocaine hydrochloride as active ingredients.

Three Davilla species are used medicinally, with varying effects and potential toxicities requiring scrutiny. Ethnomedicinal uses of D. rugosa and other species highlight the importance of accurate identification in herbal medicine.

2. Traditional and Historical Use

2.1 Indigenous Origins

Davilla rugosa Poiret, Dilleniaceae, is a liana known commonly as cipó-caboclo. Since it was discovered by the Carijó Indians, its stems are widely used for the preparation of anti-inflammatory, antiulcer, purgative, stimulant, aphrodisiac, and tonic hydroalcoholic extracts and aqueous infusions. The ethnobotanical literature records the Carijó as among the earliest known users of the plant, and references to its application date to early twentieth-century Brazilian botanical literature (Le Cointe, 1934; Silva, 1935; Corrêa, 1984, as cited in Guaraldo et al., 2000).

2.2 Brazilian Folk Medicine

In Brazilian folk medicine, stems of Davilla rugosa, locally known as cipó-caboclo, are known for their anti-inflammatory and antiulcer uses, as well as their use as a laxative, stimulant, aphrodisiac, and tonic. The plant is also important in religious rituals. The ethnomedicinal use of D. rugosa has been reported all over Brazil.

It is used as an analgesic, vasoconstrictor, and anti-ulcer agent and is useful in the treatment of hemorrhoids and varicose veins. Several species of the genus Davilla are known in folk medicine and widely used by the Brazilian population in the treatment of different disorders, such as elephantiasis, swelling of the limbs, diuretic, aphrodisiac, and ulcer, among others.

Historical and ethnobotanical reports indicate that preparations made from the leaves or stems of Davilla rugosa have been applied topically to treat wounds, burns, and skin inflammations. The traditional use is largely rooted in the belief that the plant possesses anti-inflammatory, astringent, and antimicrobial properties.

Ethnobotanical surveys and records indicate that indigenous and rural communities utilize its leaves and extracts specifically to help reduce swelling and promote the healing of bruises and minor injuries.

2.3 Notes on Species Identification in Historical Literature

Aphrodisiac, healing, and emollient properties were previously described, but in earlier studies D. elliptica, D. brasiliana, D. cearensis, and other species were depicted as synonymous with D. rugosa, making precise identification of the exact Davilla species with such properties difficult. More recently, a comprehensive phylogenetic study confirmed that these species are distinct from each other, and a taxonomic revision of the Dilleniaceae family was proposed (Fraga, 2012). Researchers and practitioners using historical ethnobotanical records should therefore interpret ascribed uses cautiously when species identity cannot be confirmed with certainty.

3. Key Constituents and Active Compounds

3.1 Overview of Phytochemical Profile

A bibliographical review of cipó-caboclo (Davilla rugosa) showed phytochemical analysis (in assay tubes, chromatoplates, and HPLC) indicating the presence of flavonoids, saponins, phenolic acids, lignans, alkaloids, coumarin derivatives, polyphenols/tannins, and steroids/triterpenes in the hydroalcoholic extract.

Earlier chemical studies showed that the main constituents of the stems of D. rugosa Poiret are flavonoids, saponins, and mucilage. Alkaloids, flavonoids, saponins, polyphenols/tannins, and coumarins were identified in hydroalcoholic extracts, while lignans were found only in the extract of Davilla rugosa.

3.2 Flavonoids

Flavonoids such as myricetin, quercetin, myricetin-3-rhamnoside, quercetin-3-rhamnoside, and kaempferol were isolated from the leaves, and the alkaloid caffeine was isolated from the seeds.

A phytochemical study of stem extracts identified additional compounds. The hydromethanolic extract of the stems was partitioned between hexane, CHCl₃, and EtOAc. Chromatographic methods of fractions resulted in the isolation of friedelin, sitostenone, betulinic acid, naringenin, quercetin, and 4′-O-methyl taxifolin. The compounds were identified by spectrometric data analyses.

3.3 Triterpenes

One study described the development of methodologies for the isolation, identification, and quantification of betulinic, oleanolic, and ursolic acids in extracts from Davilla rugosa (Dilleniaceae). Davilla rugosa stems were employed as the source of pure betulinic acid, and this compound was obtained in a reasonable yield (approximately 2.4 × 10⁻² % dry weight).

3.4 Tannins and Phenolic Acids

The phytochemical analysis indicated the presence of flavonoids, saponins, phenolic acids, lignans, alkaloids, coumarin derivatives, polyphenols/tannins, and steroids/triterpenes in the extract, which corroborates with the literature data.

3.5 Seasonal Variation in Phytochemical Content

Davilla rugosa Poir. (Dilleniaceae) is a woody vine, popularly known as "folha de lixa e cipó-caboclo," native to forest edges widely distributed across Brazil. It is used as an analgesic, vasoconstrictor, and anti-ulcer agent. A study investigated the influence of seasonal changes on the contents of flavonoids and tannins and antioxidant activity in its leaves. The contents of flavonoids and tannins were determined in each of the four seasons, as recommended by the Brazilian Pharmacopeia, and found to be highest in summer (flavonoids: 0.71%; tannins: 16.73%), followed by autumn (flavonoids: 0.58%; tannins: 16.39%).

Considering that phenolic substances are probably responsible for the anti-inflammatory and anti-ulcerogenic activities, it can be inferred that the best time for collection, to obtain raw material with good concentrations of these metabolites, is in summer and autumn.

4. Established and Proposed Mechanisms of Action

The mechanisms of action of D. rugosa have not been precisely elucidated in mechanistic pharmacological studies. The evidence available is primarily from preclinical models, and the mechanisms proposed are largely inferred from the chemical classes identified in the plant.

From a scientific perspective, research into Davilla rugosa is limited. Some preliminary pharmacological studies have identified the presence of flavonoids and tannins in the plant, compounds known for their antioxidant and anti-inflammatory effects.

Alkaloids, flavonoids, saponins, polyphenols/tannins, and coumarins were identified in extracts of Davilla rugosa, and the extract presented a marked antioxidant activity. The antioxidant capacity has been demonstrated in DPPH radical-scavenging assays in preclinical settings.

For the gastroprotective activity specifically, results suggest that the D. rugosa Poiret hydroalcoholic extract has antiulcer activity in rats and that the active components are in the two more polar fractions. This points to water-soluble constituents — most likely tannins, polyphenols, or saponins — as the probable mediators, though definitive mechanistic studies have not been published.

Regarding adaptogen/stress-related activity, the extract exerted a moderate antiulcer effect in rats submitted to cold immobilization stress. It did not, however, inhibit the increase in the levels of ACTH and corticosterone induced by stress. This finding indicates that the gastroprotective effect is not mediated via suppression of the hypothalamic-pituitary-adrenal (HPA) axis.

5. Scientific Evidence by Area of Use

5.1 Gastric Antiulcer Activity

Evidence type: preclinical (animal models); no human clinical trials identified.

The hydroalcoholic extract of the stems (HE) was fractionated with chloroform (CF), chloroform/ethyl acetate (CAF), ethyl acetate (AF), ethyl acetate/ethanol (AEF), ethanol (EF), and ethanol/water (EWF). The hydroalcoholic extract (HE) and fractions of the stems of D. rugosa Poiret were investigated for possible antigastric ulcer properties. These extracts were shown to protect rats from developing gastric ulcers induced by two acute models: HCl/ethanol (400 mg/kg i.p.) and immersion-restraint stress (15 and 30 mg/kg of the HE and 15 mg/kg either of the ethanol or the ethanol/water fractions, p.o.).

The daily oral dose of 800 mg/kg of HE for 30 consecutive days was tested for possible toxic effects. There were no modifications in body weight, water or food intake, or in the external aspect of kidneys, spleen, lungs, and liver. The only difference observed was a decrease of liver weight.

Pharmacological investigations carried out with hydroalcoholic extracts of the stems from this species have demonstrated a gastric antiulcer activity in many experimental models in rats.

These are preclinical findings from rat models. No controlled human trials evaluating D. rugosa for gastric ulcer treatment have been identified in the peer-reviewed literature. The evidence should be characterized as preliminary and species-specific to the rodent models used.

5.2 Central Nervous System Effects: Motor Activity and Anxiety-Related Behavior

Evidence type: preclinical (animal models); no human clinical trials identified.

Davilla rugosa Poiret is commonly used in Brazilian folk medicine. The use as a stimulant prompted investigators to study the effects on motor activity and anxiety using an open-field and an elevated plus-maze, respectively.

The hydroalcoholic extract of the stems (HE) was fractionated with chloroform (CF), chloroform/ethyl acetate (CAF), ethyl acetate (AF), ethyl acetate/ethanol (AEF), ethanol (EF), and ethanol/water (EWF). Rats were treated orally with HE (7.5, 15, 30, or 60 mg/kg) or fractions (15 mg/kg).

In the open-field, HE (15 mg/kg), AEF, EF, and EWF increased locomotion frequency and decreased immobility time; the contrary was observed with 30 and 60 mg/kg of HE. These doses also increased defecation. No effects were observed with 7.5 mg/kg of HE, CF, CAF, or AF, except for an increase in defecation induced by AF.

In the elevated plus-maze, total entries and number of entries into the open and closed arms, and the time spent in the open arms and its percentage, were increased only with 15 mg/kg of HE. This pattern of results — increased open-arm activity in the elevated plus-maze — is a recognized preclinical indicator of anxiolytic-like effect.

A systematic review of plant-based medicines for anxiety disorders noted that Davilla rugosa is among plants for which preclinical evidence of anxiolytic activity (without human clinical trials) was found.

The bidirectional dose-dependent effect on motor activity (stimulant at 15 mg/kg; apparent sedation at 30–60 mg/kg) is a notable pharmacological observation, though its clinical relevance is unknown. All data derive from animal studies and cannot be extrapolated to human doses or effects without further investigation.

5.3 Antioxidant Activity

Evidence type: preclinical (in vitro and animal assays); no human clinical trials identified.

Alkaloids, flavonoids, saponins, polyphenols/tannins, and coumarins were identified in extracts of Davilla rugosa, while lignans were found only in the extract of Davilla rugosa. This extract presented a marked antioxidant activity.

The hydroalcoholic extract also exerted a marked antioxidant activity, as demonstrated in adaptogen-screening experiments. The antioxidant activity has been attributed to the polyphenolic and flavonoid content. This evidence is limited to preclinical assays.

5.4 Anti-inflammatory and Wound-Healing Activity

Evidence type: traditional use supported by preliminary preclinical data; no human clinical trials identified.

Ethnobotanical surveys have documented the use of Davilla rugosa leaves and extracts by indigenous and local populations for their purported anti-inflammatory and wound-healing properties. The plant is primarily used in traditional medicine in Brazil and other parts of South America to treat inflammation and related conditions.

Some preliminary pharmacological studies suggest that extracts from Davilla rugosa possess anti-inflammatory and antioxidant activities, but this evidence is not robust, usually limited to in vitro assays or animal models, and lacks large-scale clinical trials in humans.

5.5 Adaptogen Activity

Evidence type: preclinical; evidence is negative for core adaptogen endpoints.

Hydroalcohol extracts of Davilla rugosa and Baccharis trimera were investigated with regard to their pharmacological activity in tests that evaluate adaptogen activity. Alkaloids, flavonoids, saponins, polyphenols/tannins, and coumarins were identified, while lignans were found only in Davilla rugosa. The extract exerted a moderate antiulcer effect in rats submitted to cold immobilization stress. It did not, however, inhibit the increase in the levels of ACTH and corticosterone induced by stress. Moreover, Davilla rugosa did not improve the physical performance of mice submitted to forced exercise and the learning time of old rats in the T-maze, neither did it reduce the blood viscosity of old animals.

The results point to the absence of an adaptogen activity of Baccharis trimera, with some effects that could be related to such an activity as regards Davilla rugosa. Overall, the evidence for classical adaptogen activity (HPA axis modulation, physical performance enhancement, cognitive improvement) is weak to negative in the available preclinical tests.

5.6 Use in Hemorrhoids and Vascular Conditions

Evidence type: traditional use; limited pharmacological rationale; no human clinical trials identified for D. rugosa as a monotherapy.

Davilla rugosa Poir. (Dilleniaceae) is a woody vine popularly known as "folha de lixa e cipó-caboclo." It is used as an analgesic, vasoconstrictor, and anti-ulcer agent and is useful in the treatment of hemorrhoids and varicose veins. This use is primarily traditional; the pharmacological basis for vasoconstriction has not been characterized in controlled in vitro or in vivo experiments published in the peer-reviewed literature.

6. Body Systems and Health Areas Associated with Davilla rugosa

• Gastrointestinal system: Anti-inflammatory and antiulcer uses, as well as use as a laxative, are the most prominent and best-documented applications in Brazilian folk medicine.
• Central nervous system: Its traditional use as a stimulant prompted preclinical studies evaluating effects on motor activity and anxiety-related behavior.
• Cardiovascular and vascular system: Traditional use as an analgesic and vasoconstrictor, and in the treatment of hemorrhoids and varicose veins, has been documented.
• Immune and inflammatory response: Used in traditional medicine primarily in Brazil and other parts of South America to treat inflammation and related conditions, with ethnobotanical surveys documenting its use for anti-inflammatory and wound-healing purposes.
• Skin and wound healing: Preparations made from the leaves or stems have been applied topically to treat wounds, burns, and skin inflammations, rooted in the belief that the plant possesses anti-inflammatory, astringent, and antimicrobial properties.
• Endocrine/stress response: Investigated for adaptogen-like properties, but without confirmed HPA axis modulation.
• Reproductive system: Use as an aphrodisiac has been documented in popular tradition.

7. Dosage Forms and Study Dosages

No human dosing standards, pharmacopoeal monographs, or standardized clinical protocols for Davilla rugosa have been published. The following dosages are those reported exclusively in preclinical (animal) studies:

• In a central nervous system study, the hydroalcoholic extract of the stems (HE) was fractionated and rats were treated orally with HE at doses of 7.5, 15, 30, or 60 mg/kg, or with fractions at 15 mg/kg.
• For antiulcer activity testing, extracts were shown to protect rats from gastric ulcers induced by HCl/ethanol (400 mg/kg i.p.) and immersion-restraint stress at doses of 15 and 30 mg/kg of the HE and 15 mg/kg of ethanol or ethanol/water fractions, administered orally.
• For subacute toxicity evaluation, a daily oral dose of 800 mg/kg of HE for 30 consecutive days was tested in rats.
• From the pharmacological point of view, the extract presented low toxicity by the oral route; it did not affect animal behavior on motor coordination, locomotor activity, open field, and sleeping time tests at doses of 12.5 to 100 mg/kg.

In traditional practice, the stems are typically prepared as hydroalcoholic extracts and aqueous infusions, though specific volumes, concentrations, or durations of use have not been formally standardized or validated in any pharmacopoeal document identified in the published literature.

8. Safety Considerations

8.1 General Toxicity

No relevant side effects have been reported previously, and some studies found low toxicity and genotoxicity. However, further studies are still needed and should focus on molecular mechanisms involved in bioactive components' effects based on both fractions and isolated compounds. Preliminary studies showed that the hydroalcoholic extract of D. rugosa is not toxic by the oral route when given acutely.

In a 30-day repeated-dose preclinical study in rats at 800 mg/kg/day oral HE, there were no modifications in body weight, water or food intake, or in the external aspect of kidneys, spleen, lungs, and liver. The only difference observed was a decrease of liver weight. The clinical significance of this hepatic finding (reduced liver weight) has not been further investigated, and its relevance to human use is unknown.

Plants of the genus Davilla are used to make safe herbal medicines with only a few and insignificant side effects. This general characterization is based on traditional use experience and limited preclinical data rather than controlled clinical safety evaluations.

8.2 Genotoxicity Considerations

While no published genotoxicity studies specifically on D. rugosa were identified, research on closely related species in the same genus is informative. In studies on Davilla nitida and Davilla elliptica, none of the extracts showed genotoxic activity in mouse cells. In the presence of metal ions, however, aqueous and ethyl-acetate fractions, as well as their isolated compounds, induced single- and double-strand DNA breaks. The two species of Davilla possess qualitatively similar chemical profiles. The mutagenic and genotoxic potential of their isolated compounds was tested in the Salmonella typhimurium assay (Ames test) and in the micronucleus test with peripheral blood cells of mice treated in vivo.

For the genus as a whole, no relevant side effects have been reported previously, and some studies found low toxicity and genotoxicity. Given the chemical similarities across Davilla species, the genotoxicity data from related species are relevant context but cannot be directly attributed to D. rugosa.

8.3 Laxative Effects

At doses of 30 and 60 mg/kg in preclinical open-field tests, the hydroalcoholic extract increased defecation in rats. The ethyl acetate fraction (AF) also produced increased defecation at 15 mg/kg. This is consistent with the traditional use of the plant as a laxative or purgative, and suggests dose-dependent gastrointestinal stimulation at higher doses in rats.

8.4 Species Adulteration and Misidentification

A specific safety concern documented in the literature is commercial adulteration. In Rio de Janeiro, six species of Davilla occur with very similar external morphology. Davilla glaziovii is an endangered species and must not be sold. The stems of cipó-caboclo are sold in major herb markets and open-air street markets. Anatomical and histological studies have been conducted to provide tools for distinguishing authentic D. rugosa material from other species in commercial settings.

8.5 Absence of Drug Interaction Data

No peer-reviewed studies characterizing pharmacokinetic drug-drug interactions for D. rugosa were identified. Given that the seeds contain caffeine (the alkaloid caffeine was isolated from the seeds) and that flavonoids in the plant include quercetin — a known modulator of CYP enzymes and drug transporters in vitro — interactions with pharmaceutical drugs are theoretically plausible but have not been investigated in published studies.

8.6 Overall Evidence Strength Summary

Across all investigated areas, the entire body of evidence for Davilla rugosa derives from traditional ethnobotanical records and preclinical (in vitro and animal) studies. Scientific validation remains limited. Some preliminary pharmacological studies suggest anti-inflammatory and antioxidant activities, but this evidence is not robust, usually limited to in vitro assays or animal models, and lacks large-scale clinical trials in humans. The traditional use is more thoroughly documented than scientific validation, and most sources cite its use based on local knowledge passed through generations. No randomized controlled trials, systematic reviews with clinical data, or regulatory-level assessments (such as EMA assessments or WHO monographs) were identified for this species.

References

• Guaraldo L, Chagas DA, Konno AC, et al. Hydroalcoholic extract and fractions of Davilla rugosa Poiret: effects on spontaneous motor activity and elevated plus-maze behavior. J Ethnopharmacol. 2000;72(1–2):61–7. PubMed PMID: 10967455
• Guaraldo L, Sertie JA, Bacchi EM. Antiulcer action of the hydroalcoholic extract and fractions of Davilla rugosa Poiret in the rat. J Ethnopharmacol. 2001. PubMed PMID: 11390136
• Mendes FR, Tabach R, Carlini EA. Evaluation of Baccharis trimera and Davilla rugosa in tests for adaptogen activity. Phytother Res. 2007. PubMed PMID: 17326041
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• Biso FL et al. Assessment of DNA damage induced by extracts, fractions and isolated compounds of Davilla nitida and Davilla elliptica (Dilleniaceae). Mutat Res Genet Toxicol Environ Mutagen. 2010. ScienceDirect.
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