Isolation and Identification of a Potent Antimalarial and Antibacterial Polyacetylene fromBidens pilosa

Abstract

Diseases caused by malaria parasites and pathogenic bacteria were thought to be on the brink of eradication in the 1950-1960s, but they have once again become a serious threat to mankind as a result of the appearance of multidrug resistant strains. The spread of these multidrug resistant organisms has prompted a worldwide search for new classes of effective antimalarial and antibacterial drugs. Natural products have been recognized as highly important candidates for this purpose. Our attention has focused on the herbal plant Bidens pilosa, a weed common throughout the world, as one of the target plants in the search for new active compounds, owing to its empirical use in the treatment of infectious diseases and to pharmaco-chemical studies of its crude extract. We report the isolation of two new compounds of B. pilosa, the linear polyacetylenic diol 1 and its glucoside 2 which have previously been isolated from different plants. Compound 1 exhibited highly potent antimalarial and antibacterial properties in vitro as well as potent antimalarial activity by way of intravenous injection in vivo, thereby representing a promising new class of drugs potentially effective in the treatment of malarial and bacterial diseases. We suspect that discovery of these compounds in B. pilosa in appreciable quantity is because the Fijian tradition of using the fresh plant for extraction rather than the Asian tradition of using dried plants (1 is unstable in the dried state) was followed.

Traditional plants used for medicinal purposes by local communities around the Northern sector of Kibale National Park, Uganda

“…The treatment of fresh wounds by Bidens pilosa was cited by informats, 7 times out of the 11 citations. This plant has been found to have antimicrobial, anti-inflammatory properties and compounds that help in the wound healing process (Li-Ping et al, 2008;Tobinaga et al, 2009;Ashafa and Afolayan, 2009). Several isolated constituents of Bidens pilosa which have anti-inflammatory, antibacterial and antifungal properties have been studied (Geissberger and Sequin, 1991;Fabiana et al, 2011).…”

Bidens pilosaL. (Asteraceae): Botanical Properties, Traditional Uses, Phytochemistry, and Pharmacology

“…Different preparations of its whole plant and/or parts have been purported to treat over 40 categories of illnesses. Scientific studies, although not extensive, have demonstrated that B. pilosa extracts and/or compounds have antitumor [28–36], antiinflammatory [18, 32, 37–42], antidiabetic and antihyperglycemic [7, 43–46], antioxidant [47–49], immunomodulatory [29, 50], antimalarial [30, 51], antibacterial [51–53], antifungal [53, 54], antihypertensive, vasodilatory [19, 55], and antiulcerative [17] activities. In this section, the primary pharmacological properties of B. pilosa extracts and phytochemicals are presented and discussed.…”

“…Examples of drug resistance can be found in the species of the Plasmodium that cause malaria. It is important to search for new compounds to combat Plasmodium parasites [51]. A study of the anti-malarial activity of the leaf extracts of B. pilosa using a combination of phytochemistry and bioassays showed that compound 49 (Table 11) showed activity against a malaria parasite ( P. falciparum NF54 strain) with an IC 50 value of 6.0  μ g/mL [30].…”

Avaliação Etnobotânica De Plantas Utilizadas Como Potenciais Antimaláricos Na Região Da Amazônia Ocidental Brasileira

“…Segundo Tobinaga et al (2009), por meio de dois compostos isolados da planta B. pilosa, verificou-se in vitro propriedades altamente potentes, antibacterianas e antimaláricas. A atividade contra o Plasmodium tem sido atribuída à presença de flavonoides e acetilenos (ANDRADE-NETO et al, 2004).…”