GRAVIOLA

Clinical References on Graviola (Annona muricata)

Kim GS, Muricoreacin and murihexocin C, mono-tetrahydrofuran acetogenins, from the leaves of Annona muricata. Phytochemistry 1998 Sep;49(2):565-71
(Abstract Available)

Lopez Abraham AM, et.al., [Plant extracts with cytostatic properties growing in Cuba. I.] Rev Cubana Med Trop, 31: 2, 1979 May-Aug, 97-104
(Abstract Available)

Hernández L., et.al., Use of medicinal plants by ambulatory patients in Puerto Rico. Am J Hosp Pharm, 41: 10, 1984 Oct, 2060-4
(Abstract Available)

Bories C., et.a., Antiparasitic activity of Annona muricata and Annona cherimolia seeds. Planta Med, 57: 5, 1991 Oct, 434-6
(Abstract Available)

Wu FE, et.al., Two new cytotoxic monotetrahydrofuran Annonaceous acetogenins, annomuricins A and B, from the leaves of Annona muricata. J Nat Prod, 58: 6, 1995 Jun, 830-6
(Abstract Available)

Wu FE, et.al., Muricatocins A and B, two new bioactive monotetrahydrofuran Annonaceous acetogenins from the leaves of Annona muricata. J Nat Prod, 58: 6, 1995 Jun, 902-8
(Abstract Available)

Wu FE, et.al., New bioactive monotetrahydrofuran Annonaceous acetogenins, annomuricin C and muricatocin C, from the leaves of Annona muricata. J Nat Prod, 58: 6, 1995 Jun, 909-15
(Abstract Available)

Wu FE, et.al., Additional bioactive acetogenins, annomutacin and (2,4-trans and cis)-10R-annonacin-A-ones, from the leaves of Annona muricata. J Nat Prod, 58: 9, 1995 Sep, 1430-7
(Abstract Available)

Kooiman P., Structures of the galactomannans from seeds of Annona muricata, Arenga saccharifera, Cocos nucifera, Convolvulus tricolor, and Sophora japonica. Carbohydr Res, 20: 2, 1971 Dec, 329-37

Bourne RK., A preliminary study of the sedative effects of Annona muricata (sour sop). West Indian Med J, 28: 2, 1979 Jun, 106-10

Rieser MJ., et.al., Bioactive single-ring acetogenins from seed extracts of Annona muricata. Planta Med, 59: 1, 1993 Feb, 91-2



Muricoreacin and murihexocin C, mono-tetrahydrofuran acetogenins, from the leaves of Annona muricata.
Kim GS, Zeng L, Alali F, Rogers LL, Wu FE, Sastrodihardjo S, McLaughlin JL
Phytochemistry 1998 Sep;49(2):565-71
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47906, USA.
Bioactivity-directed fractionation of the leaves of Annona muricata L. (Annonaceae) resulted in the isolation of two new Annonaceous acetogenins, muricoreacin (1) and murihexocin C (2). Compounds 1 and 2 showed significant cytotoxicities among six human tumor cell lines with selectivities to the prostate adenocarinoma (PC-3) and pancreatic carcinoma (PACA-2) cell lines.

[Plant extracts with cytostatic properties growing in Cuba. I.]
Lopez Abraham AM; Rojas Hernandez NM; Jimenez Misas CA
Rev Cubana Med Trop, 31: 2, 1979 May-Aug, 97-104
Abstract
The cytostatic activity of aqueous, alcoholic and ketonic extracts of 9 species of superior plants of the families Fitolacaceae, Compositae, Moraceae, Zingiberaceae, Martiniaceae, Mirtaceae, Verbenaceae and Annonaceae was assessed. The Kubas microbiologic method and the fungus Ascomiceto Neurospora crassa were used in the assessment. The fungus growth was measured in millimeters. Inhibition percentages for every case regarding control are reported. The best results were obtained from Annona muricata, Costus spiralis, Cecropia peltata, Xanthium chinense and Pluchea adorata extracts.

Use of medicinal plants by ambulatory patients in Puerto Rico.
Hernández L; Muñoz RA; Miró G; Martínez M; Silva-Parra J; Chávez PI
Am J Hosp Pharm, 41: 10, 1984 Oct, 2060-4
Abstract
The use of medicinal plants by the patients at the outpatient clinics of five health-care centers in Puerto Rico was evaluated. Medication histories were obtained for 802 patients ranging in age from two months to 91 years. The most frequent medical diagnosis was cardiovascular disease (54% of the patients). Respiratory and digestive disorders were the least frequent conditions, identified in only 9% and 6% of the cases, respectively. Medicinal plants were used by 57% of the population. Patients 65 years or older tended to use herbal remedies more often. Seven of the 11 most commonly used plants were used to treat gastrointestinal disorders. Other medicinal uses given were for sedation, sleep disorders, elevated blood pressure, kidney disorders, and respiratory ailments. The most frequently used plant was Citrus aurantium L. (sour orange), which was used as a sedative by 39% of the patients and for gastrointestinal disorders by 17%. Two potentially toxic plants, Solanum americanum and Annona muricata, were among the most commonly used plants. Medicinal plants were used widely by the outpatient population studied. Most herbs were used to treat self-limiting conditions but some were used to treat potentially serious medical problems, such as hypertension.

Antiparasitic activity of Annona muricata and Annona cherimolia seeds.
Bories C; Loiseau P; Cortes D; Myint SH; Hocquemiller R; Gayral P; Cavé A; Laurens A
Laboratoire de Parasitologie, Faculté de Pharmacie, Université Paris-Sud, Châtenay-Malabry, France.
Planta Med, 57: 5, 1991 Oct, 434-6
Abstract
Methanolic extracts of Annona muricata and A. cherimolia (Annonaceae) seeds were tested for antiparasitic acetogenins isolated from these extracts are found to be responsible for the important activity on infective larvae of Molinema desetae.

Two new cytotoxic monotetrahydrofuran Annonaceous acetogenins, annomuricins A and B, from the leaves of Annona muricata.
Wu FE; Gu ZM; Zeng L; Zhao GX; Zhang Y; McLaughlin JL; Sastrodihardjo S
Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907, USA.
J Nat Prod, 58: 6, 1995 Jun, 830-6
Abstract
The leaves of Annona muricata have yielded eight monotetrahydrofuran Annonaceous acetogenins. Two of them, annomuricins A [1] and B [2], whose chemical structures were deduced by ms, nmr, ir, and uv spectral and chemical methods, are novel and unusual. Compounds 1 and 2 each possess five hydroxyl groups; two hydroxyl groups are vicinal, with the vicinal group of 1 threo and that of 2 erythro. The absolute configurations of 1 and 2 were determined by Mosher ester methodology. Six monotetrahydrofuran acetogenins, previously described in the seeds, were found in the leaves; these are gigantetrocin A, annonacin-10-one, muricatetrocins A and B, annonacin, and goniothalamicin.

Muricatocins A and B, two new bioactive monotetrahydrofuran Annonaceous acetogenins from the leaves of Annona muricata.
Wu FE; Zeng L; Gu ZM; Zhao GX; Zhang Y; Schwedler JT; McLaughlin JL; Sastrodihardjo S
J Nat Prod, 58: 6, 1995 Jun, 902-8
Abstract
The leaves of Annona muricata have yielded the novel monotetrahydrofuran Annonaceous acetogenins, muricatocins A [1] and B [2]. Each compound possesses five hydroxyl groups, with two hydroxyl groups at the C-10 and C-12 positions. The absolute configurations of 1 and 2 (except for positions C-10 and C-12) were determined by Mosher ester methodology. The C-10, C-12 acetonides (1c, 2c) suggested relative stereochemistry and significantly enhanced cytotoxicity against the A-549 human lung tumor cell line. Three known monotetrahydrofuran acetogenins, annonacin A, (2,4-trans)-isoannonacin, and (2,4-cis)-isoannonacin, were also found.

New bioactive monotetrahydrofuran Annonaceous acetogenins, annomuricin C and muricatocin C, from the leaves of Annona muricata.
Wu FE; Zeng L; Gu ZM; Zhao GX; Zhang Y; Schwedler JT; McLaughlin JL; Sastrodihardjo S
J Nat Prod, 58: 6, 1995 Jun, 909-15
Abstract
The leaves of Annona muricata have yielded two additional monotetrahydrofuran Annonaceous acetogenins, annomuricin C [1] and muricatocin C [2]. Compounds 1 and 2 each possess five hydroxyl groups; two hydroxyl groups are at the C-10/C-11 and C-10/C-12 positions in 1 and 2, respectively. The absolute configurations of 1 and 2, except for positions C-10 and C-11 or C-12, were determined by Mosher ester methodology. The C-10/C-11 and C-10/C-12 acetonides (1c, 2c) suggested relative stereochemistry and significantly enhanced the cytotoxicities against the A-549 human lung and the MCF-7 human beast solid tumor cell lines. One known onotetrahydrofuran acetogenin, gigantetronenin, not described previously from this plant, was also found.

Additional bioactive acetogenins, annomutacin and (2,4-trans and cis)-10R-annonacin-A-ones, from the leaves of Annona muricata.
Wu FE; Zhao GX; Zeng L; Zhang Y; Schwedler JT; McLaughlin JL; Sastrodihardjo S
J Nat Prod, 58: 9, 1995 Sep, 1430-7
Abstract
In a continuation of our research on bioactive components from the leaves of Annona muricata, three novel monotetrahydrofuran Annonaceous acetogenins, namely, annomutacin [1], (2,4-trans)-10R-annonacin-A-one [2], and (2,4-cis)-10R- annonacin-A-one [3], have been identified. Their structures were deduced by ms, nmr, ir, and uv spectral and chemical methods, and the absolute configurations were determined by Mosher ester methodology. A known bioactive amide, N-p-coumaroyl tyramine, was also found. Compound 1 and the mixture of compounds 2 and 3 showed selective cytotoxicities against the human A-549 lung tumor cell line.

GUARANA

Clinical References on Guarana (Paullinia cupana)

Henman AR. Guaraná (Paullinia cupana var. sorbilis): ecological and social perspectives on an economic plant of the central Amazon basin. J Ethnopharmacol, 1982 Nov
(Abstract Available)

Belliardo F, et al. HPLC determination of caffeine and theophylline in Paullinia cupana Kunth (guarana) and Cola spp. samples. Z Lebensm Unters Forsch, 1985 May
(Abstract Available)

Bydlowski SP, et al. A novel property of an aqueous guaraná extract (Paullinia cupana): inhibition of platelet aggregation in vitro and in vivo. Braz J Med Biol Res, 1988
(Abstract Available)

Bydlowski SP, et al. An aqueous extract of guaraná Paullinia cupana) decreases platelet thromboxane synthesis. Braz J Med Biol Res, 1991
(Abstract Available)

Morton JF. Widespread tannin intake via stimulants and masticatories, especially guarana, kola nut, betel vine, and accessories. Basic Life Sci, 1992
(Abstract Available)

da Fonseca CA, et al. Genotoxic and mutagenic effects of guarana (Paullinia cupana) in prokaryotic organisms. Mutat Res, 1994 May
(Abstract Available)

Schultes RE. Amazonian ethnobotany and the search for new drugs. Ciba Found Symp, 1994
(Abstract Available)

  • Miura T, et al. Effect of guarana on exercise in normal and epinephrine-induced glycogenolytic mice. Biol Pharm Bull. 1998 Jun;21(6):646-8.
    (Abstract Available)

  • Carlson M, et al. Liquid chromatographic determination of methylxanthines and catechins in herbal preparations containing guarana. J AOAC Int. 1998 Jul-Aug;81(4):691-701.
    (Abstract Available)

  • Mattei R, et al. Guarana (Paullinia cupana): toxic behavioral effects in laboratory animals and antioxidants activity in vitro. J Ethnopharmacol. 1998 Mar;60(2):111-6.
    (Abstract Available)

  • Espinola EB, et al. Pharmacological activity of Guarana (Paullinia cupana Mart.) in laboratory animals. J Ethnopharmacol. 1997 Feb;55(3):223-9.
    (Abstract Available)

  • Benoni H, et al. Studies on the essential oil from guarana. Z Lebensm Unters Forsch. 1996 Jul;203(1):95-8.
    (Abstract Available)





    Guaraná (Paullinia cupana var. sorbilis): ecological and social perspectives on an economic plant of the central Amazon basin.
    Henman AR
    J Ethnopharmacol, 6: 3, 1982 Nov, 311-38
    Abstract
    Guaraná is considered an ideal crop for supplementing the incomes of small peasant farmers in the Amazon basin. A fast-growing perennial, guaraná can be planted in the midst of manioc crops, allowing the formation of extensive orchards in the place of regenerating scrub once the manioc has been harvested. Traditional forms of guaraná agriculture practised by the Saterê-Mawé Indians compare favourably with the plantation system favoured by government agronomists. Indigenous techniques of hand-processing guaraná are also shown to produce better quality in the finished product than those practices adopted by industrial concerns. A detailed comparison of two systems of production show the Indians' implicit concern to avoid oxidization of the phenolic compounds in the seed, since this leads to the guaraná becoming dark in colour, bitter in taste, and irritating to the gastrointestinal tract. The short-term medicinal effects of guaraná are commonly thought to result from a high content of caffeine and associated alkaloids, as well as from considerable amounts of tannin. Future research may well show that various saponins also play an important part in the drug's pharmacology, particularly with regard to its long-term influence as a general tonic and prophylactic.

    HPLC determination of caffeine and theophylline in Paullinia cupana Kunth (guarana) and Cola spp. samples.
    Belliardo F; Martelli A; Valle MG
    Z Lebensm Unters Forsch, 180: 5, 1985 May, 398-401
    Abstract
    A reversed-phase high-performance liquid-chromatographic method for the determination of caffeine and theophylline in commercial guarana samples (drug obtained from the seeds of Paulinia cupana Kunth, Sapindaceae of the Amazon Region) and in Cola spp. samples is described and discussed. The methodology developed is simple and rapid with a minimum of samples preparation required. A comparison of five different techniques for the extraction of caffeine and theophylline is discussed. Furthermore the quantitative determination of caffeine and theophylline in five samples of Brasilian guarana, in two samples of dietetic products containing guarana, in two samples of Cola extract and in three of Cola seed powder are reported.

    A novel property of an aqueous guaraná extract (Paullinia cupana): inhibition of platelet aggregation in vitro and in vivo.
    Bydlowski SP; Yunker RL; Subbiah MT
    Departamento de Ciências Fisiológicas, Faculdade de Ciências Médicas da Santa Casa de São Paulo, Brasil.
    Braz J Med Biol Res, 21: 3, 1988, 535-8
    Abstract
    Aqueous extracts of guaraná were studied in terms of effects on the aggregation of human and rabbit platelets. Guaraná extracts have anti-aggregatory and de-aggregatory actions on platelet aggregation induced by ADP or arachidonate but not by collagen. The active material was shown to be water soluble and heat resistant and appeared to be different from salicylates, nicotinic acid or known xanthines. Guaraná extracts inhibited platelet aggregation in rabbits following either intravenous or oral administration.

    An aqueous extract of guaraná (Paullinia cupana) decreases platelet thromboxane synthesis.
    Bydlowski SP; D'Amico EA; Chamone DA
    Fundação Pró-Sangue Hemocentro de São Paulo, Faculdade de Medicina, Universidade de São Paulo, Brasil.
    Braz J Med Biol Res, 24: 4, 1991, 421-4
    Abstract
    The effects of an aqueous extract of guaraná (Paullinia cupana) on rabbit platelet aggregation and thromboxane synthesis were examined. The guaraná extract (100 mg/ml) and fractions separated by TLC (origin and xanthines) decreased platelet aggregation (37, 27 and 31% of control values, respectively) and platelet thromboxane formation from [14C]-arachidonic acid (78, 70 and 50% of control values, respectively). The decreased thromboxane synthesis could be responsible, at least in part, for the antiaggregatory action of guaraná.

    Widespread tannin intake via stimulants and masticatories, especially guarana, kola nut, betel vine, and accessories.
    Morton JF
    University of Miami, Coral Gables, FL 33124.
    Basic Life Sci, 59:1992, 739-65
    Abstract
    Tannins are increasingly recognized as dietary carcinogens and as antinutrients interfering with the system's full use of protein. Nevertheless, certain tannin-rich beverages, masticatories, and folk remedies, long utilized in African, Asiatic, Pacific, and Latin American countries, are now appearing in North American sundry shops and grocery stores. These include guarana (Paullinia cupana HBK.) from Brazil, kola nut (Cola nitida Schott & Endl. and C. acuminata Schott & Endl.) from West Africa, and betel nut (Areca catechu L.) from Malaya. The betel nut, or arecanut, has long been associated with oral and esophageal cancer because of its tannin content and the tannin contributed by the highly astringent cutch from Acacia catechu L. and Uncaria gambir Roxb. and the aromatic, astringent 'pan' (leaves of Piper betel L.) chewed with it. In addition to the constant recreational/social ingestion of these plant materials, they are much consumed as aphrodisiacs and medications. Guarana and kola nut enjoy great popularity in their native lands because they are also rich in caffeine, which serves as a stimulant. Research and popular education on the deleterious effects of excessive tannin intake could do much to reduce the heavy burden of early mortality and health care, especially in developing countries.

    Genotoxic and mutagenic effects of guarana (Paullinia cupana) in prokaryotic organisms.
    da Fonseca CA; Leal J; Costa SS; Leitão AC
    Departamento de Radiobiologia, Instituto de Biofísica Carlos Chagas Filho, Rio de Janeiro, Brazil.
    Mutat Res, 321: 3, 1994 May, 165-73
    Abstract
    Aqueous extracts of Paullinia cupana (guarana), a species that belongs to the Sapindaceae family, were analyzed for the presence of genotoxic activities in bacterial cells. The extracts of guarana were genotoxic as assessed by lysogenic induction in Escherichia coli and they were also able to induce mutagenesis in Salmonella typhimurium. Addition of S9 microsomal fraction, catalase, superoxide dismutase or thiourea counteracted the genotoxic activity of guarana, suggesting that oxygen reactive species play an essential role in the genotoxicity of aqueous guarana extracts. The genotoxic activity in the extracts was related to the presence of a molecular complex formed by caffeine and a flavonoid (catechin or epicatechin) in the presence of potassium.

    Amazonian ethnobotany and the search for new drugs.
    Schultes RE
    Botanical Museum, Harvard University, Cambridge, MA 02138.
    Ciba Found Symp, 185:1994, 106-12; discussion 112-5
    Abstract
    Tropical rain forests offer enormous prospects for the discovery of new drugs for use in Western medicine. The Amazon supports 80,000 species of higher plants and a diverse Indian population. Focusing attention on those plants used as medicines by indigenous peoples is the most efficient way of identifying the plants that contain bioactive compounds. There is an urgent need for more ethnobotanists and ethnopharmacologists to be trained to document as much information as possible before it and the plants are lost through destruction of the rain forest and acculturation of the indigenous peoples. Ethnobotanical studies have identified plants documented by early travellers; these include Paullinia yoco and Ilex guayusa which are used as stimulants and have been shown to be rich in caffeine. Studies of the hallucinogen prepared from Banisterioposis caapi have shown that the native people know which plants to add to the mixture to lengthen and intensify the intoxication produced by the beta-carboline alkaloids in the plant. Three major snuffs are used in the Amazonia; the plants from which they are derived have been identified. One of the snuffs also has antifungal and curare-like activities; chemical analysis on the active principles has not been done. Several plants are considered as prime candidates for scientific study as sources of useful chemicals for medicine or industry. These include some used to prepare teas or other infusions for treatment of various symptoms of senile dementia.


    Liquid chromatographic determination of methylxanthines and catechins in herbal preparations containing guarana.
    Carlson M, Thompson RD
    U.S. Food and Drug Administration, Minneapolis, MN 55401, USA.
    J AOAC Int     1998 Jul-Aug;81(4):691-701
    Herbal preparations derived from the dried seeds of guarana (Paullinia cupana) have become a popular nutritional supplement used for stimulatory purposes. Once considered a drug substance in the United States, guarana currently is classified as a food additive and dietary supplement. The pharmacological activity of guarana-containing products is primarily due to methylxanthine alkaloids. For guarana preparations, methylxanthine levels and, more significantly, the presence of several polyphenol compounds (i.e., catechins) provide phytochemical markers of authenticity. Methylxanthines and polyphenols are extracted from sample matrix with a heated phosphate buffer-methanol solution, the cooled extract is filtered, and the extract is injected into the liquid chromatographic (LC) system. A Nova-Pak C18 column eluted with phosphate buffer-methanol mobile phase (pH = 3.50) and monitored at 272 nm gave satisfactory resolution for the methylxanthines theobromine, theophylline, caffeine and the polyphenols (+)-catechin and (-)-epicatechin. Twenty-four products including dried seeds, dried paste, seed powders, tablets, and capsule formulations were assayed and conclusions were drawn about their authenticity. The LC system responded linearly to methylxanthines over the 100-fold range in concentration from 0.043 to 4.30 micrograms/mL for theobromine and caffeine and from 0.041 to 4.10 micrograms/mL for theophylline. Precision data for the 3 methylxanthines obtained from 10 different products (n = 5) gave relative standard deviation (RSD) values of 1.18-15.52% within a concentration range of 0.01-52.28 mg/g. Recoveries of methylxanthines from fortified products varied from 87.5 to 120.0%. The response for catechins was linear over a 200-fold range in concentration of 0.05-10.0 micrograms/mL. Precision data from 5 products (n = 5) gave RSD values of 1.08-5.54% within a concentration range of 0.34-32.65 mg/g. Recoveries from these products ranged from 87.7 to 109.7%. Results and chromatographic profiles for 14 commercial products in solid dosage form indicate that a number of these products may not contain authentic guarana as an active ingredient or contain less than the declared quantity of guarana. The proposed procedure also was applied to 2 carbonated soft drinks and a sample of mate.

    Effect of guarana on exercise in normal and epinephrine-induced glycogenolytic mice.
    Miura T, Tatara M, Nakamura K, Suzuki I
    Department of Clinical Nutrition, Suzuka University of Medical Science, Faculty of Health Science, Mie, Japan.
    Biol Pharm Bull 1998 Jun;21(6):646-8
    The tonic action of water Guarana extract, (Paullinia cupana MART.), was investigated in normal, exercised, and epinephrine-induced glycogenolytic mice. A water extract of Guarana (GW) (500 mg/kg) increased the blood glucose level (p < 0.001) and decreased the liver glycogen contents of mice 60 min after oral maltose administration (p < 0.05). GW also significantly suppressed exercise-induced hypoglycemia (60 min: p < 0.05). However, GW did not affect the blood glucose in epinephrine-induced glycogenolytic and exercise mice. These findings indicate that the suppressive mechanism of hypoglycemia might be due to the promotion of glycogen resolution.

    Guarana (Paullinia cupana): toxic behavioral effects in laboratory animals and antioxidants activity in vitro.
    Mattei R, Dias RF, Espinola EB, Carlini EA, Barros SB
    Department of Psychobiology, Universidade Federal de Sao Paulo, Brazil.
    J Ethnopharmacol 1998 Mar;60(2):111-6
    The effects on toxic and behavioral levels of guarana (Paullinia cupana) were assessed in rats and mice subsequent to acute and chronic administrations and were compared to those produced by Ginseng (Panax ginseng). Experimental parameters included tests for antioxidant capacity in vitro and measured in vivo, toxicological screening, progress in weight, motor activity, death rate, and histopathological examination of the viscera. Guarana showed an antioxidant effect because, even at low concentrations (1.2 microg/ml), it inhibited the process of lipid peroxidation. In high doses of 1000-2000 mg/kg (i.p. and p.o.) it did not induce significant alterations in parameters for toxicological screening. No effects on motor activity were observed, neither did guarana alter the hypnotic effect of pentobarbital. Ginseng (250-1000 mg/kg i.p.), however, elicited reductions in motor activity, eyelid ptosis and bristling fur. Consumption of liquids containing guarana or ginseng and progress in weight of the animals remained at levels similar to the controls, even after prolonged administration. The percentage mortality was equivalent in control and in treated groups. The absence of toxicity of guarana was also demonstrated by histopathological examination, with no alteration being detected in heart, lungs, stomach, small and large intestine, liver, pancreas, kidneys, bladder and spleen.

    Evaluation of the toxicity of guarana with in vitro bioassays.
    Santa Maria A, Lopez A, Diaz MM, Munoz-Mingarro D, Pozuelo JM
    Departamento Biotecnologia, Instituto de Salud Carlos III, Madrid, Spain.
    Ecotoxicol Environ Saf 1998 Mar;39(3):164-7
    A natural stimulant, Paullinia cupana, commonly called guarana, was tested for its ability to induce in vitro toxicity in Chinese hamster ovary (CHO) cells and bacterial cells (Photobacterium phosphoreum). The cytotoxic effects of aqueous guarana extracts were evaluated by three endpoint systems: neutral red (NR) uptake assay, total protein content [kenacid blue (KB)] assay, and tetrazolium (MTT) assay. The Microtox test was also used. Results indicated that the lowest concentration of guarana tested was not toxic and that the IC50 values calculated with the NR, KB, and MTT assays were lower than the highest concentration tested (40 mg/ml). There was no significant difference in cytotoxicity between the three test systems. The EC50 values obtained with the Microtox assay were consistent with these data. The present in vitro analysis suggests that the concentration of guarana is of critical importance in its cytotoxic activity and high doses could be harmful to human health.

    Pharmacological activity of Guarana (Paullinia cupana Mart.) in laboratory animals.
    Espinola EB, Dias RF, Mattei R, Carlini EA
    Laboratorio de Tecnologia Farmaceutica, Universidade Federal da Paraiba, Brazil.
    J Ethnopharmacol 1997 Feb;55(3):223-9
    Mice that ingested a suspension of guarana (Paullinia cupana, Sapindaceae) in a dose of 0.3 mg/ml showed a significant increase in physical capacity when subjected to a stressful situation such as forced swimming after 100 and 200 days of treatment. Such an effect, however, was not obtained with a concentration of 3.0 mg/ml, nor with the ingestion of a suspension of ginseng 5.0 mg/ml, nor of a solution of caffeine 0.1 mg/ml. Guarana, both after a single (3.0 and 30 mg/kg) or chronic administrations (0.3 mg/ml), was able to partially reverse the amnesic effect of scopolamine as measured through a passive avoidance test in mice and rats, indicating a positive effect on memory acquisition. However, no effect was observed when an active avoidance task was used in rats, even after 20 days of guarana administration. There was also a tendency of rats treated with 0.3 mg/ml of guarana to better maintain the memory of a Lashley III maze path. The animals had the same average lifespan, indicating a low toxicity of guarana, even after 23 months of treatment.


    Studies on the essential oil from guarana.
    Benoni H, Dallakian P, Taraz K
    Institut fur Organische Chemie der Universitat Koln, Koln, Germany.
    Z Lebensm Unters Forsch 1996 Jul;203(1):95-8
    The essential oil from guarana [Paullinia cupana H.B.K. var. sorbilis (Mart.) Ducke] was analysed. Nine components were identified, namely (2) methylbenzenes, (1) cyclic monoterpene and (2) cyclic sesquiterpene hydrocarbons, (2) methoxyphenylpropenes and (2) alkylphenol derivatives. The alleged psychoactivity of the essential oil is presumably due to the identified constituents estragole and anethole. Any contribution of aminated metabolites of estragole/anethole to the alleged psychoactivity of the essential oil of guarana can be excluded. Neither the psychoactive 4-methoxyamphetamine nor tert-aminoketones could be traced in human urine after oral application of guarana.
    PMID: 8765992, UI: 96331684


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