title: Isolation and identification of a potent antimalarial and antibacterial polyacetylene from Bidens 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.
authors.affiliation: Showa Pharmaceutical University, Higashi-tamagawagakuen, Machida, Tokyo 194-8543, Japan. tobinaga@xqd.biglobe.ne.jp
authors.forename: Seisho
authors.initials: S
authors.lastname: Tobinaga
authors.forename: Mukesh K
authors.initials: MK
authors.lastname: Sharma
authors.forename: William G L
authors.initials: WG
authors.lastname: Aalbersberg
authors.forename: Kinzo
authors.initials: K
authors.lastname: Watanabe
authors.forename: Kazuo
authors.initials: K
authors.lastname: Iguchi
authors.forename: Koji
authors.initials: K
authors.lastname: Narui
authors.forename: Masanori
authors.initials: M
authors.lastname: Sasatsu
authors.forename: Seizi
authors.initials: S
authors.lastname: Waki
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000962:Antimalarials / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects; D031176:Bidens / Q000737:chemistry*; D002176:Candida albicans / Q000187:drug effects; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D053279:Polyynes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: C544497:(R)-1,2-dihydroxytrideca-3,5,7,9,11-pentayne; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D000962:Antimalarials; D010936:Plant Extracts; D053279:Polyynes