KIUCHI Fumiyuki Kanazawa Univ., Faculty of Pharmaceutical Sciences, Assistant Professor, 薬学部, 助手 (60161402)
AKAO Nobuaki Kanazawa Univ., School of Medicine, Assistant Professor, 医学部, 講師 (00126559)
KONDO Kaoru Kanazawa Univ., School of Medicine, Aossociate Professor, 医学部, 助教授 (00079724)
|Budget Amount *help
¥2,000,000 (Direct Cost : ¥2,000,000)
Fiscal Year 1993 : ¥600,000 (Direct Cost : ¥600,000)
Fiscal Year 1992 : ¥1,400,000 (Direct Cost : ¥1,400,000)
A nepali traditional medicine "Bayubidanga", fruits of Embelia ribes (a family of Myrsinaceae), has been known to be effective to tapeworms. Since the medicine is reported to be also effective to whipworms and Ascaris, our work was undertaken to clarify what constituent(s) is responsible to this activity.
Extraction of E.ribes with ether gave known constituent, embelin, as an active principle, while extraction with hot water resulted in another active principle, gallic acid, suggesting that embelin was decomposed into different compound(s) on contact with hot water. In vitro activities of these principles were 0.01 mg/ml and 0.5-1 mg/ml to dog whipworm. Trichuris vulpis, respectively.
The features of decomposition of embelin in boiling water and in methanol (organic solvant) were clarified that the former treatment yielded a "dimer" and the leatter treatment gae O-methyl derivative.
In vivo anti-Trichuris activity of embelin and its derivatives was examined using mice infected with T.muris. It was found that, among E.ribes decoction, embelin, and its derivatives, onlyh potassium embelate was effective (70-100%) cure rate), when applied to BALB/c mice pretreated with hydrocortisone acetate before infection. The activity was comparable to the known anti-Trichuris drug, mebendazole. On the other hand, neither potassiumembelate nor mebendazole was effective, when applied to infected mice (both BALB/c and ICR) pretreated with predonisolone butylacetate, suggesting that infection method largely influences on the result of eficacy of medicine. Contrary to these medicines, ivermectin was constantly effective to all mice tested in this investigation.