Valmas 1 Elizabeth Valmas Biology Research Paper Jackass Bitters Neurolaena lobata commonly known ass Jackass-bitters is a plant

species and a member of the Asteraceae family. Other common names for this plant are Salve Bush, Bushy Fleabane, Sour-Bush, Cough Bush and Wild Tobacco. According to the U.S. department of agriculture Jackass-bitters is geographically distributed in southern parts of Northern America (Mexico), Southern America including countries in the Caribbean, Mesoamerica, Northern South America, and Western South America. Jackass-bitters is used widely in traditional medicine, and is also known to be a convenient insecticide for house and garden plants. The Jackass-bitters plant can be found growing near manmade structures such as roadsides or construction sites. It also grows in very moist to very arid locations. The Jackass-bitters has yellow flowers, and its leaves are known for their bitter taste. It grows as a multi-branching shrub that can reach 3 meters in height. The size of the leaves varies, and can grow up to 25 cm in length (www.levypreserve.org). The shapes of the leaves also vary and are oval, oblong, or elliptical. The Jackass-bitters flowers are actinomorphic and contain both perfect and imperfect flowers in the heads, while only imperfect flowers have functional ovules. Jackass-bitters leaves contain a powerful anti-parasitic agent (sesquiterpene dialdehyde), which has proven effective against amoebas, giardia, candida and intestinal parasites (www.consejo.bz). Jackass-bitters has been used in Central America such as Belize, for medicinal purposes in treating intestinal parasites,

Valmas 2 malaria, fungus, ringworm, wounds, head lice, and for cleansing the blood (www.consejo.bz). It is also used medicinally in the Bahamas for treating colds, fevers, measles, and dermatological problems (www.levypreserve.org).

Additionally, in other parts of the Caribbean Jackass-bitters has been used for treatment of dislocations and sprains. Traditionally for treatment, leaves and roots are used to produce tea or wine that is taken internally, as well as bathing in a topical solution. In treating malaria drinking a range of 3 glasses a day for 4 days to 1 glass a day for 7 days is suggested (drugs.com). Jackass-bitters is also used recreationally, while using the leaves as a substitute for tobacco. There is no clinical data that confirms the effectiveness of Jackass-Bitters, therefore Ethnomedicinal resources vary for dosage. The sesquiterpene lactones are the primary medicinal components, found in the leaf of the Jackass-Bitters plant. Additionally the germacranolide sesquiterpene lactones contain neurolenins A, B, C, D, E, and F and lobatin A (Drugs.com). The neurolenin chemicals are found in high concentrations in the leaves, and are suspected to be involved with treating dysentery. The neurolenins are the chemicals responsible for Jackass-Bitters extreme bitter taste. While germacranolide sesquiterpene lactones possess structural necessities for anticancer and cytotoxic activities, neurolenins A and B were inactive in an animal model against sarcoma180 (Drugs.com). Sesquiterpene is also linked with Jackass-Bitters activity against insects and antimalarial activity. The Jackass-Bitters plant may show qualitative and quantitative variations in its sesquiterpene lactone content contingent to the geographical origin it is found. Additional chemicals were identified in the leaf

Valmas 3 content including thymols, acid, mellilotic, iridoids, alkaloids, coumarins, and 12 different Flavonoids (drugs.com). Medical literature has been published regarding in vitro and animal studies on Jackass-Bitters antimalarial, antiplasmodial, antibacterial, hypoglycemic and anthelminthic, activity, though clinical trials are unavailable that supports its effectiveness (drugs.com). In a recent study 11 medicinal plants were used for in vitro macrofilaricidal activity against the parasite B. pahangi. Results confirmed that the ethanolic extract of leaves of Neurolaena lobata showed the greatest inhibiting activity against the motility of adult worms (Natural Products as a Source for Treating Neglected Parasitic Diseases, 2013). In addition the in vitro assay of the extract revealed potential micro-and macro-filaricidal activities. Further data has revealed N. lobata to have activity against trypanosomatids (Natural Products as a Source for Treating Neglected Parasitic Diseases, 2013). Additional testing and isolation of N. lobata extracts is advised to obtain new molecules to fight these parasitic diseases. Jackass-Bitters have been commonly used by Q'eqchi' Maya and indigenous healers in Belize in treatment of inflammatory conditions (Walshe-Roussel, 2013). This encouraged the study of the anti-inflammatory activity of Jackass-Bitters. The studies objective was aimed towards investigating the effects against inflammatory symptoms, and to evaluate the in vitro anti-inflammatory activity of leaf extracts and isolated sesquiterpene lactones. This study supported the hypothesis that the Jackass-Bitters leaf extract and the sesquiterpene lactones it contains, possess antiinflammatory activity as well as a phytochemical and pharmacological origin.

Valmas 4 Work Cited Berger, Ingeborg, Claus Martin Passreiter, Armando Caceres, and Wolfgang Kubelka. "Antiprotozoal Activity of Neurolaena Lobata." Phytotherapy Research 15.4 (2001): 327-30. Print. "Jackass Bitters." Professional Information from Drugs.com. Wolters Kluwer Health, 2009. Web. 02 Aug. 2013. <http://www.drugs.com/npp/jackass bitters.html>. Ndjonka, Dieudonne, Ludmila N. Rapado, and Ariel M. Silber. "Natural Products as a Source for Treating Neglected Parasitic Diseases." International Journal of Molecular Sciences (2013): 1-45. Print. "Neurolaena Lobata Information from NPGS/GRIN." Neurolaena Lobata Information from NPGS/GRIN. United States Department of Agriculture, n.d. Web. 01 Aug. 2013. "Plant Information." Leon Levy Native Plant Preserve Content. Design & Development IBS International, n.d. Web. 28 July 2013. <http://www.levypreserve.org/PlantListings/Neurolaena-lobata>. "The Bush Medicine of Belize and Central America." Bush Medicine of Belize and Central America. Consejo.BZ, n.d. Web. 01 Aug. 2013. <http://consejo.bz/belize/bushmedicine.html>. Walshe-Roussel, Brendan, Christin Choueiri, and Ammar Saleem. "Potent Antiinflammatory Activity of Sesquiterpene Lactones from Neurolaena Lobata (L.) R. Br. Ex Cass., a Qeqchi Maya Traditional Medicine." Phytochemistry 92 (2013): 122-27. Print.

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The leaf extract of N. lobata and the isolated sesquiterpene lactones 15 are potent inhibitors of TNF-a production in LPS-stimulated THP-1 monocytes, with the isolated sesquiterpene lactones 15 demonstrating greater anti-inflammatory activity then that of parthenolide. Lobatin B (4) is a particularly powerful antiinflammatory agent as its TNFa inhibition is an order of magnitude greater than that of parthenolide. The crude 80% EtOH extract of N. lobata leaves administered at 100g/mL reduced LPS-stimulated TNF- production in THP-1 monocytes by 72% relative to the stimulated vehicle control. Isolated sesquiterpene lactones, neurolenins B, C+D, lobatin B and 9-hydroxy-8-isovalerianyloxy-calyculatolide were more active (IC50=0.17-2.32M) than the positive control parthenolide (IC50=4.79M). The results provide a pharmacological and phytochemical basis for the traditional use of this leaf for inflammatory conditions.