Detail of "24159-07-7"

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Comparison of antimalarial activity of the alkaloidal fraction of Hydrangea macrophylla var

Comparison of antimalarial activity of the alkaloidal fraction of Hydrangea macrophylla var. Otaksa leaves with the hot-water extract in ICR mice infected with Plasmodium yoelii 17 XL. Ishih, Akira; Miyase, Toshio; Terada, Mamoru (Department of Parasitology, Hamamatsu University School of Medicine, Hamamatsu, Japan). Phytotherapy Research, 17(6), 633-639 (English) 2003 John Wiley & Sons Ltd. CODEN: PHYREH. ISSN: 0951-418X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The antimalarial activity of the fractions isolated from the leaves of Hydrangea macrophylla Seringe var. Otaksa Makino was evaluated against Plasmodium yoelii 17 XL in mice. Four different fractions were prepd. in the usual manner to obtain an alkaloid fraction. All mice treated with the fraction contg. febrifugine and isofebrifugine mixt. at 1 mg/kg twice a day for 5 consecutive days survived during the expt., and the change of mean parasitemia level showed almost the same pattern as that from mice treated with the hot-water ext. 32434-44-9 and 24159-07-7 are also in the experiment. of the same plant leaves. Activity of this fraction, however, was markedly reduced compared with the hot-water ext. Furthermore, no antimalarial activity was shown in the hotwater ext. from H. macrophylla var. Otaksa roots or Dichroa febrifuga Lour. leaves. .

Antimalarial activities and therapeutic properties of febrifugine analogs

Antimalarial activities and therapeutic properties of febrifugine analogs. Jiang, Suping; Zeng, Qiang; Gettayacamin, Montip; Tungtaeng, Anchalee; Wannaying, Srisombat; Lim, Apassorn; Hansukjariya, Pranee; Okunji, Christopher O.; Zhu, Shuren; Fang, Daohe ( Departments of Parasitology and Medicinal Chemistry, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA). Antimicrobial Agents and Chemotherapy, 49(3), 1169-1176 (English) 2005 American Society for Microbiology. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Febrifugine is the active principal isolated 50 years ago from the Chinese herb chang shan (Dichroa febrifuga Lour), which has been used as an antimalarial in Chinese traditional medicine for more than 2,000 years. However, intensive study of the properties of febrifugine has been hindered for decades due to its side effects. We report new findings on the effects of febrifugine analogs compared with those of febrifugine extd. from the dry roots of D. febrifuga.Some chemicals with cas registry numbers like 24159-07-7 are also used. The properties of the extd. febrifugine were comparable to those obtained from the std. febrifugine provided by our collaborators. A febrifugine structure-based computer search of the Walter Reed Chem. Information System identified 10 analogs that inhibited parasite growth in vitro, with 50% inhibitory concns. ranging from 0.141 to 290 ng/mL. The host macrophages (J744 cells) were 50 to 100 times less sensitive to the febrifugine analogs than the parasites. Neuronal (NG108) cells were even more insensitive to these drugs (selectivity indexes, >1,000), indicating that a feasible therapeutic index for humans could be established. The analogs, particularly halofuginone, notably reduced parasitemias to undetectable levels and displayed curative effects in Plasmodium berghei-infected mice. Recrudescence of the parasites after treatment with the febrifugine analogs was the key factor that caused the death of most of the mice in groups receiving an ED. S.c. treatments with the analogs did not cause irritation of the gastrointestinal tract when the animals were treated with doses within the antimalarial dose range. In summary, these analogs appear to be promising lead antimalarial compds. that require intensive study for optimization for further down-selection and development. .