Pharmacology of Ch‘ang Shan (Dichroa febrifuga), a Chinese Antimalarial Herb

Jang, C. S.; Fu, Fangqiu; Huang, K. C.; Wang, C. Y.

doi:10.1038/161400b0

Cited by 57 publications

(22 citation statements)

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“…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). 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).…”

mentioning

confidence: 98%

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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mentioning

confidence: 98%

Antimalarial Activities and Therapeutic Properties of Febrifugine Analogs

Jiang

Zeng

Gettayacamin

et al. 2005

Antimicrob Agents Chemother

126

102

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“…Since ancient times the herb D. febrifuga L. has been used in traditional Chinese medicine as an anti malarial treatment (Pines et al 2000). The extracts from roots and leaves of D. febrifuga L. including febrifugine, have been also used to protect chickens from infection with Plasmodium gallinaceum and malaria (Jang et al 1948). Tang and Eisenbrand (1992) demonstrated that febrifugine had a higher anti-malarial activity than quinine against Plasmodium lophurae, P. gallinaceum and Plasmodium cynomolgi.…”

Section: Introductionmentioning

confidence: 99%

Anticoccidial effect of halofuginone hydrobromide against Eimeria tenella with associated histology

et al. 2012

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Halofuginone (stenorol) has been used as an effective anticoccidial reagent for decades but very little is known about its mode of action. In this study, chickens were inoculated with Eimeria tenella oocysts on 14-day-old and medicated with halofuginone at days 0, 1, 2, 3, 4, 5 and 6 post inoculations (groups 0, 1, 2, 3, 4, 5 and 6, respectively). Chickens in group 7 were taken as challenge-unmedicated control and in group 8 unchallenged-unmedicated control. The survival rate, body weight gains (BWG), oocysts production, cecal scores, bloody diarrhea and histological examinations were analyzed to evaluate the anticoccidial efficacy of halofuginone and to initially elucidate its mechanisms. Results showed that halofuginone which acted as a coccidiostatic can significantly enhance the BWG, and decrease both the oocyst shedding and cecal destruction caused by E. tenella infection. The histological slide examination noted that halofuginone was effective when provided 0-2 days post inoculation but only partially effective when applied 3-7 days post infection. The second-generation schizonts treated with halofuginone appeared vacuolated and degenerated. It is concluded that halofuginone can inhibit the parasite's invasion of host cecal hypothetical cell at the early stages of life cycle and later disturb the parasite's development by vacuolation of the schizonts. The resulting abnormal schizonts could not divide into schizoites and were eventually eliminated by the host's immune response.

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“…[11,12] Substituted quinazolin-4-(3H)-ones possess a wide range of pharmacological activities. 2-Methyl-3-o-toly-quinazolin-4-(3H)-one is a potent hypnotic agent and other quinazolin-4-(3H)-ones have been reported to exhibit analgesic, antibacterial, anticancer, anesthetic, anticonvulsant, anti-inflammatory, antimalarial, and antiparasitic, diuretic, sedative and tranquilizing properties [for selected examples, see Refs.…”

Section: Introductionmentioning

confidence: 99%