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Jackass Bitters

Scientific Name(s): Neurolaena lobata (L.) R. Br.
Common Name(s): Capitana, Contragavilana, Cow-gall bitter, Gavilana, Herbe-a-pique, Inaciabi, Jackass bitters, Mano de lagarto, Tres puntas, Zeb-a-pique

Medically reviewed by Drugs.com. Last updated on Apr 25, 2019.

Clinical Overview

Use

The plant species has numerous ethnomedicinal uses. Medical literature documents in vitro and animal studies on the plant's antibacterial, antimalarial, antiplasmodial, anthelminthic, and hypoglycemic activity, but there are no clinical trials to support its use for any indication.

Dosing

None validated by clinical data. Ethnomedicinal resources vary for dosage of an N. lobata leaf decoction in treating malaria, ranging from 3 glasses daily for 4 days to 1 glass daily before breakfast for 7 days.

Contraindications

Patients with known hypersensitivity reactions to any of the components of the plant species.

Pregnancy/Lactation

Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

None well documented.

Adverse Reactions

None well documented.

Toxicology

Chemical analysis revealed the presence of pyrrolizidine alkaloids. No toxicity was observed with oral doses up to 5,000 mg/kg in mice.

Scientific Family

  • Asteraceae (daisy)

Botany

The weedy herbaceous plant N. lobata grows in northwestern South America through Central America and into southern Mexico. The plant species also is found throughout the Caribbean islands. It grows 1 to 2 m tall and has alternate trilobed leaves. The yellow flowers grow in compact groups at the end of the branches. All portions of the plant have a bitter taste. When handled, the fresh leaves and stems stain the skin yellow.Borges-del-Castillo 1982, Manchand 1978, Passreiter 1995, USDA 2017

History

The plant species has numerous ethnomedicinal uses. In Mesoamerica, the herb was used to treat several diseases, including cancer, diabetes, dysentery (amebiasis), and malaria. In Panama, an infusion of the leaves was used to treat diabetes, hypertension, and hepatic ailments. In the Panamanian province of Darian, it is used for malaria and as an insect repellent. In Caribbean folk medicine, the herb was used medicinally to treat skin diseases, gastric pain, ulcers, and as a general pain reliever. In Guatemala, the plant has been used to treat malaria, anemia, and nervous weakness. It also has been used as a tonic and an antipyretic.Borges-del-Castillo 1982, Caceres 1998, Franssen 1997, Giron 1991, Gracioso 1998, Passreiter 1995, Passreiter 1997

Chemistry

The primary medicinal components, the sesquiterpene lactones, are found in the leaf. The germacranolide sesquiterpene lactones include neurolenins A, B, C, D, E, and F and lobatin A. The neurolenins are found in the leaves in high concentrations and may be involved with the plant's medicinal use in treating dysentery. The neurolenins are extremely bitter substances. The germacranolide sesquiterpene lactones possess the structural requirements for cytotoxic and anticancer activities; however, neurolenins A and B were inactive in an animal model against sarcoma-180. Examples of isolated furanoheliangolides from N. lobata include lobatins B and C. The sesquiterpene content also is associated with the plant's antimalarial activity and activity against insects. N. lobata plants of different geographical origin show some qualitative and quantitative variations in their sesquiterpene lactone content. Flavonoids, coumarins, thymols, mellilotic acid, iridoids, and alkaloids also have been identified. More than 12 flavonoids have been isolated.Bohimann 9789, Borges-del-Castillo 1982, Castro 1996, Kerr 1981, Manchand 1978, Passreiter 1995, Passreiter 1997, Passreiter 1998, Passreiter 1999, Passreiter 1998, Todorova 1997

Uses and Pharmacology

Clinical studies are lacking.

Anti-inflammatory effects

Animal data

Studies in rodents (induced paw edema) and in vitro suggest chemical constituents of N. lobata may have anti-inflammatory activity.Gracioso 1998, Lajter 2014, McKinnon 2014

Clinical data

Research reveals no clinical studies regarding the use of N. lobata for anti-inflammatory effect.

Antimicrobial activity

Animal data

Based on in vitro studies, some animal experiments have been conducted.Berger 1998, Caceres 1998, Franssen 1997, Fujimaki 2005 in vitro antibacterial activity has been reported.Lentz 1998 Antiplasmodial effects of chemical constituents neurolenins, and of ethanol and methanol extracts have been demonstrated in rodents.Berger 2001, Francois 1996

Other uses

Hypoglycemic activity in mice was demonstrated in an older study; however this line of research does not appear to have been further pursued.Gupta 1984

Various fractions of a hydroalcoholic extract of N. lobata aerial parts reduced gastric lesion formation in rodent models. Researchers suggest the mechanism of action may be associated with mucus production and prostaglandin synthesis.Gracioso 2000 Wound healing in a study in rats was improved with extracts of the leaves of the plant.Nayak 2014

Extracts of the branches, leaves, and stems of N. lobata had moderate neutralization activity at doses up to 4 mg per mouse against the hemorrhagic effect of Bothrops atrox snake venom of from Antioquia and Chocó, northwestern Colombia.Otero 2000

Dosing

None has been validated by clinical data. Ethnomedicinal resources vary for dosage of an N. lobata leaf decoction in treating malaria, ranging from 3 glasses daily for 4 days to 1 glass daily before breakfast for 7 days.Berger 1998, Giron 1991

Pregnancy / Lactation

Avoid use during pregnancy and lactation because of lack of clinical studies.Francois 1996

Interactions

None validated by clinical data. The herb has the potential to produce additive effects in patients also taking analgesics, diuretics, or antimalarial medications.

Adverse Reactions

None well documented.

Toxicology

Chemical analysis revealed the presence of pyrrolizidine alkaloids; however, toxic necine pyrrolizidines were not present. No toxicity was observed with oral doses up to 5,000 mg/kg in mice. Gracioso 1998, Gracioso 1996

References

Berger I, Barrientos AC, Caceres A, et al. Plants used in Guatemala for the treatment of protozoal infections: II. Activity of extracts and fractions of five Guatemalan plants against Trypanosoma cruzi. J Ethnopharmacol. 1998;62:107-115.9741882
Berger I, Passreiter CM, Caceres A, Kubelka W. Antiprotozoal activity of Neurolaena lobata. Phytother Res. 2001;15:327-330.11406857
Bohimann F, Natu AA, Kerr K. Naturally occurring terpene derivatives. Part 185. Thymol derivatives from Neurolaena species. Phytochemistry. 1979;18:489-490.
Borges-del-Castillo J, Manresa-Ferrero MT, Rodríguez-Lius F, Vázquez-Bueno P, Gupta MP, Joseph-Nathan P. Panama flora. II. New sesquiterpene lactones from Neurolaena lobata. J Nat Prod. 1982;45:762-765.
Caceres A, Lopez B, Gonzalez S, Berger I, Tada I, Maki J. Plants used in Guatemala for the treatment of protozoal infections. I. Screening of activity to bacteria, fungi and American trypanosomes of 13 native plants. J Ethnopharmacol. 1998;62:195-202.9849628
Castro O, Barrios M, Chinchilla M, Guerrero O. Chemical and biological evaluation of the effect of plant extracts against Plasmodium berghei [in Spanish]. Rev Biol Trop. 1996;44:361-367.9246360
Francois G, Passreiter CM, Woerdenbag HJ, Van Looveren M. Antiplasmodial activities and cytotoxic effects of aqueous extracts and sesquiterpene lactones from Neurolaena lobata. Planta Med. 1996;62:126-129.8657743
Franssen FF, Smeijsters LJ, Berger I, Medinilla Aldana BE. In vivo and in vitro antiplasmodial activities of some plants traditionally used in Guatemala against malaria. Antimicrob Agents Chemother. 1997;41:1500-1503.9210673
Fujimaki Y, Kamachi T, Yanagi T, Caceres A, Maki J, Aoki Y. Macrofilaricidal and microfilaricidal effects of Neurolaena lobata, a Guatemalan medicinal plant, on Brugia pahangi. J Helminthol. 2005;79:23-28.15831109
Giron LM, Freire V, Alonzo A, Caceres A. Ethnobotanical survey of the medicinal flora used by the Caribs of Guatemala. J Ethnopharmacol. 1991;34:173-187.1795521
Gracioso JS, Hiruma-Lima CA, Souza Brito AR. Antiulcerogenic effect of a hydroalcoholic extract and its organic fractions of Neurolaena lobata (L.) R.Br. Phytomedicine. 2000;7:283-289.10969721
Gracioso JS, Paulo MQ, Hiruma Lima CA, Souza Brito AR. Antinociceptive effect in mice of a hydroalcoholic extract of Neurolaena lobata (L.) R. Br. and its organic fractions. J Pharm Pharmacol. 1998;50:1425-1429.10052860
Gupta MP, Solis NG, Avella ME, Sanchez C. Hypoglycemic activity of Neurolaena lobata (L.) R. Br. J Ethnopharmacol. 1984;10:323-327.6748709
Kerr KM, Mabry TJ, Yoser S. 6-Hydroxy- and 6-methoxyflavonoids from Neurolaena lobata and N. macrocephala. Phytochemistry. 1981;20:791-794.
Lajter I, Vasas A, Béni Z, et al. Sesquiterpenes from Neurolaena lobata and their antiproliferative and anti-inflammatory activities. J Nat Prod. 2014;77(3):576-582.24476550
Lentz DL, Clark AM, Hufford CD, et al. Antimicrobial properties of Honduran medicinal plants. J Ethnopharmacol. 1998;63:253-263.10030730
Manchand PS, Blount JF. Chemical constituents of tropical plants. 11. Stereostructures of neurolenins A and B, novel germacranolide sesquiterpenes from Neurolaena lobata (L.) R. Br. J Org Chem. 1978;43:4352-4354.
McKinnon R, Binder M, Zupkó I, et al. Pharmacological insight into the anti-inflammatory activity of sesquiterpene lactones from Neurolaena lobata (L.) R.Br. ex Cass. Phytomedicine. 2014;21(12):1695-1701.25442279
Nayak BS, Ramlogan S, Chalapathi Rao A, Maharaj S. Neurolaena lobata L. promotes wound healing in Sprague Dawley rats. Int J Appl Basic Med Res. 2014;4(2):106-110.25143886
Neurolaena lobata. USDA, NRCS. 2016. The PLANTS Database (http://plants.usda.gov, April 2017). National Plant Data Team, Greensboro, NC 27401-4901 USA. Accessed April 2017.
Otero R, Nunez V, Barona J, et al. Snakebites and ethnobotany in the northwest region of Colombia. Part III: neutralization of the haemorrhagic effect of Bothrops atrox venom. J Ethnopharmacol. 2000;73:233-241.11025161
Passreiter CM. Pyrrolizidine alkaloids from Neurolaena lobata. Biochem Syst Ecol. 1998;26:839-843.
Passreiter CM, Isman MB. Antifeedant bioactivity of sesquiterpene lactones from Neurolaena lobata and their antagonism by γ-aminobutyric acid. Biochem System Ecol. 1997;25:371-377.
Passreiter CM, Medinilla A, Beatriz E. Variability of sesquiterpene lactones in Neurolaena lobata of different origin. Planta Medica. 1998;64:427-430.17253261
Passreiter CM, Sandoval-Ramirez J, Wright CW. Sesquiterpene lactones from Neurolaena oaxacana. J Nat Prod. 1999;62:1093-1095.10479310
Passreiter CM, Wendisch D, Gondol D. Sesquiterpene lactones from Neurolaena lobata. Phytochemistry. 1995;39:133-137.
Todorova MN, Ognyanov IV, Navas H. Sesquiterpene lactones in Neurolaena lobata from Costa Rica. Biochem Syst Ecol. 1997;25:267-268.

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This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs. This information should not be used to decide whether or not to take this product. This information does not endorse this product as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this product. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this product. This information is not specific medical advice and does not replace information you receive from your health care provider. You should talk with your health care provider for complete information about the risks and benefits of using this product.

This product may adversely interact with certain health and medical conditions, other prescription and over-the-counter drugs, foods, or other dietary supplements. This product may be unsafe when used before surgery or other medical procedures. It is important to fully inform your doctor about the herbal, vitamins, mineral or any other supplements you are taking before any kind of surgery or medical procedure. With the exception of certain products that are generally recognized as safe in normal quantities, including use of folic acid and prenatal vitamins during pregnancy, this product has not been sufficiently studied to determine whether it is safe to use during pregnancy or nursing or by persons younger than 2 years of age.

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