Ch'ang Shan, a Chinese Antimalarial Herb

Jang, C. S.; Fu, Fangqiu; Wang, C. Y.; Huang, K. C.; Lu, Guangyu; Chou, Ting‐Chao

doi:10.1126/science.103.2663.59-b

Cited by 88 publications

(23 citation statements)

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“…Severe gastrointestinal injury, however, was also observed in a chicken model when the chickens were overdosed (8,29). Clinical studies of both the crude extract and isolated forms of febrifugine conducted in Yunnan Province, People's Republic of China, from the 1940s through the 1960s showed that it had excellent antipyretic and antiparasitic effects, similar to those of quinine (7,16). Unfortunately, the emetic effects and gastrointestinal irritation caused by the compound rendered it insignificant for further investigation.…”

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“…The medical use of chang shan was described in an ancient Chinese pharmacopoeia (17) for the treatment of malaria and stomach cancer and as an expectorant, emetic, and febrifuge, with side effects of nausea and vomiting (10). Febrifugine was extracted (7) and was later identified as a quinazoline derivative with the molecular structure C 16 H 21 O 3 N 3 (15). The purified febrifugine displayed potent antimalarial activity and was 100 times as active as quinine against P. lophurae in duck models and 50 times as active as quinine against P. cynomolgi infection in rhesus monkeys (12,13).…”

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Antimalarial Activities and Therapeutic Properties of Febrifugine Analogs

Jiang

Zeng

Gettayacamin

et al. 2005

Antimicrob Agents Chemother

126

102

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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 extracted from the dry roots of D. febrifuga. The properties of the extracted febrifugine were comparable to those obtained from the standard febrifugine provided by our collaborators. A febrifugine structure-based computer search of the Walter Reed Chemical Information System identified 10 analogs that inhibited parasite growth in vitro, with 50% inhibitory concentrations 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 indices, >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 effective dose. Subcutaneous 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 compounds that require intensive study for optimization for further down-selection and development.

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confidence: 99%

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confidence: 99%

Antimalarial Activities and Therapeutic Properties of Febrifugine Analogs

Jiang

Zeng

Gettayacamin

et al. 2005

Antimicrob Agents Chemother

126

102

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“…Acute toxicity tests of Ch'ang Shan, the roots of D. febrifuga, made on dogs showed a 50% lethal dose value of 20 g/kg (Jang et al, 1946). Fatal dose produced in dogs intense congestion with numerous hemorrhagic patches throughout the whole gastrointestinal tract.…”

Section: Discussionmentioning

confidence: 99%

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

Miyase

Terada

2003

Phytotherapy Research

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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 prepared in the usual manner to obtain an alkaloid fraction. All mice treated with the fraction containing febrifugine and isofebrifugine mixture at 1 mg/kg twice a day for 5 consecutive days survived during the experiment, and the change of mean parasitemia level showed almost the same pattern as that from mice treated with the hot-water extract of the same plant leaves. Activity of this fraction, however, was markedly reduced compared with the hot-water extract. Furthermore, no antimalarial activity was shown in the hotwater extract from H. macrophylla var. Otaksa roots or Dichroa febrifuga Lour. leaves.

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“…Need for antimalarial drugs in the United States during the Second World War shaped many projects to screen synthetic and natural products [8]. In the early 1940s in China, Jang et al [10] studied antimalarial properties from crude extracts of D. febrifuga and found them to be effective against chicken malaria. For centuries, the Chinese people are using roots (Chang Shan) and leaves (Shuu Chi) of this plant as medicine against malarial fevers [9].…”

Section: Discoverymentioning

confidence: 99%