RRC ID 61301
著者 Kwofie KD, Tung NH, Suzuki-Ohashi M, Amoa-Bosompem M, Adegle R, Sakyiamah MM, Ayertey F, Owusu KB, Tuffour I, Atchoglo P, Frempong KK, Anyan WK, Uto T, Morinaga O, Yamashita T, Aboagye F, Appiah AA, Appiah-Opong R, Nyarko AK, Yamaguchi Y, Edoh D, Koram KA, Yamaoka S, Boakye DA, Ohta N, Shoyama Y, Ayi I.
タイトル Antitrypanosomal Activities and Mechanisms of Action of Novel Tetracyclic Iridoids from Morinda lucida Benth.
ジャーナル Antimicrob Agents Chemother
Abstract Trypanosoma brucei parasites are kinetoplastid protozoa that devastate the health and economic well-being of millions of people in Africa through the disease human African trypanosomiasis (HAT). New chemotherapy has been eagerly awaited due to severe side effects and the drug resistance issues plaguing current drugs. Recently, there has been an emphasis on the use of medicinal plants worldwide. Morinda lucida Benth. is a popular medicinal plant widely distributed in Africa, and several research groups have reported on the antiprotozoal activities of this plant. In this study, we identified three novel tetracyclic iridoids, molucidin, ML-2-3, and ML-F52, from the CHCl3 fraction of M. lucida leaves, which possess activity against the GUTat 3.1 strain of T. brucei brucei The 50% inhibitory concentrations (IC50) of molucidin, ML-2-3, and ML-F52 were 1.27 μM, 3.75 μM, and 0.43 μM, respectively. ML-2-3 and ML-F52 suppressed the expression of paraflagellum rod protein subunit 2, PFR-2, and caused cell cycle alteration, which preceded apoptosis induction in the bloodstream form of Trypanosoma parasites. Novel tetracyclic iridoids may be promising lead compounds for the development of new chemotherapies for African trypanosomal infections in humans and animals.
巻・号 60(6)
ページ 3283-90
公開日 2016-6-1
DOI 10.1128/AAC.01916-15
PII AAC.01916-15
PMID 26953191
PMC PMC4879371
MeSH Animals Antiprotozoal Agents / chemistry Antiprotozoal Agents / pharmacology* Apoptosis / drug effects Cell Cycle / drug effects Humans Inhibitory Concentration 50 Iridoids / chemistry Iridoids / pharmacology* Morinda / chemistry* Plant Extracts / chemistry Plant Extracts / pharmacology Plants, Medicinal / chemistry* Trypanocidal Agents / chemistry Trypanocidal Agents / pharmacology* Trypanosoma / drug effects Trypanosoma / pathogenicity Trypanosomiasis, African / physiopathology
IF 4.904
リソース情報
ヒト・動物細胞 NB1RGB(RCB0222) HF19(RCB0210)