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June 2009 volume 15 issue 2:atms journal.qxd

Journal of the Australian Traditional-Medicine Society Abstract
This article is a review of the medicinal plant Bidens pilosa.
Connelly P. Horrible weed or miracle herb? A review of Bidens pilosa. Journal of the Australian Traditional-MedicineSociety 2009;15(2):77–79. (25 references) Keywords
Herbal medicine; medicinal plant review; phytomedicine; Bidens pilosa.
Amember of the Asteraceae family, the weed Bidens Recent research is showing a useful side to this plant.
pilosa Linn. is found throughout the world, probably Searches of ProQuest, CINAHL, Wiley Interscience and originating in South America. First noted in Linneus’s PubMed databases showed a number of papers observing Species Plantarum (1753)(1), this weed has acquired a variety significant health benefits of B. pilosa as a botanical medi- of common names: cobblers pegs, grab-a-leg, Spanish nee- cine. Very few of the papers on this herb concerned testing dles, pitchforks, stickybeak, hairy tickweed and many more.
on humans; most used rodents or performed in vitro experi- When it was introduced to Australia is unknown, but it is ments on cultured cell lines. It is obvious that a large amount now prevalent in the Northern Territory, South Australia, of research remains to be performed on B. pilosa. This arti- Queensland and New South Wales, and is a major crop weed, cle will review fifteen of the papers, examining the potential outcompeting native species in tropical areas(2).
health benefits from its use as a herb.
B. pilosa is an erect annual which grows to an average height B. pilosa has been used as a folk remedy in many third-world of 60 cm although it can reach 2 m in favourable conditions.
countries for eons. Wounds, colds and flu, fever, hepatitis The leaves are opposite and divided into three to five lance- and jaundice, glandular sclerosis, rheumatic conditions, neu- shaped segments with serrated edges. Bright green whilst ralgia, smallpox, colic, diarrhoea, diuretic, pain, snake bite, young, leaves can develop tinges of red and brown on matu- conjunctivitis, anaemia, haemorrhage and rectal prolapse are rity. Flowers are mostly yellow but can have white elements just a few of many traditional uses of this herb(4, 6–8).
(ray florets) which can be present for periods of the flower’s The body of serious research on B. pilosa has grown over the development. The seeds are black or dark brown, slender and last decade. As the trend towards evidence-based medicine about 1cm long, clustered on the end of the stalk. They pos- became more pronounced, research on this herb began as an sess three tiny prongs at one end, which adhere to clothing attempt to validate its traditional use. In the process, a num- ber of studies have shown its potential as an antimalarial(9, 10), There are several varieties of B. pilosa. One, B. pilosa Linn anticancer(6, 11–13), antidiabetic(14–17), anti-inflammatory and var. radiata, which is found in tropical America and Japan, antiallergy(3, 18, 19), antihypertensive and smooth muscle relax- has been analysed and shown to contain active constituents ant(7, 8), antimicrobial/antiviral (including herpes)(20, 21), including flavonoids, polyacetylenes, flavone glycosides, antipyretic(6), oxytocic(22), and nutritive(4, 5, 23). As noted above, chalcones, aurones and phenylpropanoids(3). B. pilosa also most intensive research on this herb is in its infancy, but contains calcium, iron and zinc, as well as beta-carotene(4, 5).
these studies show promise for the use of B. pilosa as a pos-sible complement or alternative to pharmaceutical drugs forthe early stage of some of these conditions.
Malaria is a major disease problem in many areas of the Patrice Connelly B. Nat Therapies (SCU), Dip. Nutrition, is a world. Bidens spp are widespread in Brazil, where malaria nutritionist, energetic healer and musician practising inKilcoy, Qld. PO Box 272, Kilcoy QLD 4515. Telephone (07) parasites have exhibited increasing resistance to pharmaceu- 5422 0806. patrice@saraband.com.au. tical drugs. B. pilosa has been one of the most promising andpotent botanical anti-malarials, with a very high rate of Journal of the Australian Traditional-Medicine Society Connelly P. Horrible Weed Or Miracle Herb? A Review Of Bidens Pilosa.
reduction of parasitaemia in in vitro cultures of Plasmodium mechanism than pharmaceutical drugs for type I diabetes falciparum, the most deadly malarial strain, as well as other prevention, is far less toxic, and less suppressive of the less dangerous types of malaria(9). A later murine study con- firmed this effect in vivo, with a reduction in parasitaemia of Inflammation
up to 60% in mice infected with P. berghei. Dosages givenwere 250 and 500 mg/kg body weight. Herb samples collect- Inflammation is at the root of many diseases, so given B. ed under different conditions were also tested, showing little pilosa’s wide use in folk medicine for a variety of illnesses, it is not surprising that studies are uncovering its anti-inflam-matory properties. Research is now revealing modulation of various inflammatory cytokines which activate cyclooxyge- Cancer is another area where B. pilosa has shown promise, nase-2 (COX-2) and inducible nitric oxide synthase (iNOS).
specifically as an anti-angiogenic agent. B. pilosa Linn var.
Ethyl caffeate, a phenolic compound isolated from B. pilosa, radiata extract was used on a variety of cultured cell lines.
was studied using mouse skin and in vitro cell lines, and The ethyl acetate fraction was shown to have a strong found to markedly suppress several of these cytokines, with inhibitory effect on tube formation and proliferation in significant inhibition of COX-2 expression. The production human umbilical vein endothelium cells, and the authors of PGE2, a growth promoting factor in certain carcinoma conclude that this line of research is very promising(13).
cell lines and a mediator of inflammation was also signifi- Bidens pilosa L. var. minor (Blume) Sherff was used in an in cantly inhibited by ethyl caffeate in this study(18).
vitro experiment on five leukaemic cell lines. Results were Another study used normal human dermal fibroblasts to dose-dependent, but were significant on all cell lines.
examine the effect of B. pilosa Linn. var radiata (aerial parts) Dosages of 100, 250 and 500 mcg/mL were tested, with sig- following induction of inflammation. B. pilosa was found to nificant results on all but one line which was only moderate- suppress COX-2 expression and PGE2 production(3).
ly affected in comparison, but still showed a positive effect.
The authors suggest that metabolism in vivo may producemore active constituents, and that more research on the use Many allergies occur through an inflammatory pathway, and of B. pilosa as a leukaemia treatment looks worthwhile(12).
a commercial product (ClearGuard™) has now been pro-duced, aimed at the nasal allergy market. It contains B. Diabetes
pilosa, Cinnamomum cassia and Malpighia glabra. A ran- Diabetes is one disease where B. pilosa is one of many plants domised, double-blind, placebo-controlled, double-dummy, that has been used as a folk remedy in many parts of the crossover, single-centre clinical study of twenty subjects was world. A survey of plants traditionally used in Trinidad and designed to assess the efficacy of ClearGuard™ for allergy Tobago found that B. pilosa and Bidens alba were both com- symptoms. This trial was sponsored by the manufacturer of monly used in the management of hypertension and dia- No adverse events were reported. B. pilosa was included in There is good evidence for continuing research on B. pilosa the formula for its quercetin content, which has been shown in the prevention and management of diabetes, both types I to stabilise mast cells and basophils, decrease leukotriene and II. A murine study published in 2000 found two poly- synthesis and reduce the release of histamine and other acetylenic glucosides derived from the aerial parts of B. mediators. The authors also referred to the study previously pilosa, and administered in combination in a 3:2 ratio was quoted which examined the action of ethyl caffeate on shown to have a significant hypoglycaemic effect(17).
inflammatory cytokines. The result of the trial was that In another study of its hypoglycaemic effects, a test of nor- ClearGuard™ was shown to be safe and at least as effective mal mice against experimental alloxan-diabetic mice (one as the pharmaceutical drug Loratadine(19).
group mild, the other severe) using a water ethanol extract of Hypertension
B. pilosa (whole plant) showed significant hypoglycaemic B. pilosa has been used as an antihypertensive in folk medi- results in the normal and mildly diabetic mice, but no change cine, and studies are now confirming its efficacy. Three in the severely diabetic group. The authors suggest that groups of rats (normotensive, spontaneously hypertensive, insulin in the body is required as a mediator for the hypogly- and salt-loaded hypertensive) were anaesthetised and sta- caemic effects of the plant extract(14).
bilised before the solution of B. pilosa was administered.
Cytopiloyne (a polyacetylenic glucoside) has been found to Several dosages were tested. All three groups registered a prevent type I diabetes in non-obese diabetic mice (NOD), significant decrease in blood pressure. The hypotensive through modulation of T cells. Specifically, it has been found activity appears in two successive phases. The first is due, at to inhibit CD4+ T cells in the spleen and pancreatic lymph least partially, to the effect of the extract on the cardiac pump nodes of the NOD mice, leaving CD8+ T cells untouched. It efficiency, while the second phase may be due to both beta- also suppresses differentiation of Type 1 Th cells, and pro- receptor stimulation and muscarinic receptor-mediated motes production of Type 2 Th cells. Some in vitro experi- mentation with these cell lines was carried out, which The herb has also been found to be a relaxant of smooth mus- showed less promising results than the in vivo experiments.
cle. In an in vitro study of tissue from male Wistar rat aortas The authors note that cytopiloyne works through a different which had been treated with norepinephrine and KCl, a neu- Connelly P. Horrible Weed Or Miracle Herb? A Review Of Bidens Pilosa.
Journal of the Australian Traditional-Medicine Society tral leaf extract of B. pilosa was found to reduce the aorta Nguelefack TB, Dimo T, Nguelefack Mbuyo EP, Tan PV, resting tone, and inhibit KCl contractions, demonstrating a Rakotonirina SV, Kamanyi A. Relaxant effects of the neutralextract of the leaves of Bidens pilosa Linn on isolated rat vascular vasodilatory action on the tissue(7).
smooth muscle. Phytotheraphy Research 2005;19:207–210.
Antimicrobial Action
Dimo T, Nguelefack TB, Tan PV, Yewah MP, Dongo E,Rakotonirina SV, et al. Possible mechanisms of action of the neu- B. pilosa has been found to have potent antimicrobial effects, tral extract from Bidens pilosa L. leaves on the cardiovascular sys- including antiviral activity against types I and II herpes sim- tem of anaesthetized rats. Phytotheraphy Research plex (HSV) viruses. In vitro experiments using hot water extracts of the herb showed significant, dose-dependent Krettli AU, Andrade-Neto VF, Brandao MGL, Ferrari WMS. Thesearch for new antimalarial drugs from plants used to treat fever effects against HSV. Measured against Acyclovir, B. pilosa and malaria or plants randomly selected: a review. Mem Inst at 500 mcg/mL performed equally against HSV2. Against Oswaldo Cruz. 2001;96(8):1033–1042.
HSV1, B. pilosa was more efficacious than against HSV2, Andrade-Neto VF, Brandao MGL, Oliviera FQ, Casali VWD, but not quite as potent as Acyclovir(20). This is welcome, as Njaine B, Zalis MG, et al. Antimalarial activity of Bidens pilosa L.
(Asteraceae) ethanol extracts from wild plants collected in various the authors say that quite high dosages of the plant extract localities or plants cultivated in humus soil. Phytotherapy Research are well tolerated by human cells. Acyclovir, on the other hand, can have significant side effects including gastroin- Chiang L-C, Cheng H-W, Chen C-C, Lin C-C. In vitro anti- testinal upset, headache, vertigo, arthralgia, neurological leukemic and antiviral activities of traditionally used medicinalplants in Taiwan. The American Journal of Chinese Medicine reactions including convulsions, fatigue, fever, pruritus and Chang J-S, Chiang L-C, Chen C-C, Liu L-T, Wang K-C, Lin C-C.
An in vitro study of ten medicinal plants used in Colombian Antileukemic Activity of Bidens pilosa L. var. minor (Blume)Sherff and Houttuynia cordata Thunb. American Journal of folk medicine, which included B. pilosa, showed that this Chinese Medicine 2001;29(2):303–312.
herb was active against several strains of bacteria including Wu L-W, Chiang Y-M, Chuang H-C, Wang S-Y, Yang G-W, Chen Bacillus cereus and Escherichia coli, outstripping the per- Y-H, et al. Polyacetylenes function as anti-angiogenic agents.
formance of Gentamycin sulfate. It was also active against Pharmaceutical Research 2004;21(11):2112–2119.
Alarcon-Aguilar FJ, Roman-Ramos R, Florez-Saenz JL, Aguirre-Garcia F. Investigation of the hypoglycaemic effects of extracts of Conclusion
four Mexican medicinal plants in normal and Alloxan-diabeticmice. Phytotherapy Research 2002;16:383–386.
It is clear from these findings, despite the lack of high-grade Chang CL-T, Chang S-L, Lee Y-M, Chiang Y-M, Chuang D-Y, Kuo human trials, that there is a great deal of promise for the use H-K, et al. Cytopiloyne, a polyacetylenic glucoside, prevents type of B. pilosa as a botanical medicine. However, before herbal- 1 diabetes in nonobese diabetic mice. Journal of Immunology ists locate and experiment with this plant, it is useful to note Lans CA. Ethnomedicines used in Trinidad and Tobago for urinary that B. pilosa is a cadmium hyperaccumulator. In a study problems and diabetes mellitus. Journal of Ethnobiology and (which also included Matricaria chamomilla) B. pilosa and B. frondosa were found to be excellent environmental biore- Ubillas RP, Mendez CD, Jolad SD, Luo J, King SR, Carlson TJ, et mediators of cadmium pollution(25), but has no known human al. Antihyperglycemic acetylenic glucosides from Bidens pilosa.
Planta Medica 2000;66(1):82–3.
chelation effect. Therefore, selection and harvesting of plants Chiang Y-M, Lo C-P, Chen Y-P, Wang S-Y, Yang N-S, Kuo Y-H, et for medicinal use needs to be very carefully considered, and al. Ethyl caffeate suppresses NF-kB activation and its downstream assayed if there is any doubt as to its origins.
inflammatory mediators, iNOS, COX-2, and PGE2 in vitro or inmouse skin. British Journal of Pharmacology 2005;146:352–363.
Corren J, Lemay M, Lin Y, Rozga L, Randolph RK. Clinical and Australian Plant Name Index: Bidens pilosa. [cited 19 February biochemical effects of a combination botanical product 2009]; Available from: http://www.anbg.gov.au/cgi-bin/apni? (ClearGuard™) for allergy: a pilot randomized double-blind place- bo-controlled trial. Nutrition Journal 2008;7:20:1–8.
Bidens pilosa: Cobblers pegs. 2008 Sept 08 [cited 19 February Chiang L-C, Chang J-S, Chen C-C, Ng L-T, Lin C-C. Anti-herpes simplex virus activity of Bidens pilosa and Houttuynia cordata. http://www.sutherland.nsw.gov.au/ssc/rwpattach.nsf/viewasattach The American Journal of Chinese Medicine. 2003;31(3):355–362.
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Source: http://health.saraband.com.au/Research/Bidens%20pilosa.%202009%2015(2)%2077-79.pdf

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