Anticoccidial activity of traditional Chinese herbal Dichroa febrifuga Lour. extract against Eimeria tenella infection in chickens.

The study was conducted on broiler birds to evaluate the anticoccidial efficacy of an extract of Chinese traditional herb Dichroa febrifuga Lour. One hundred broiler birds were assigned to five equal groups. All birds in groups 1-4 were orally infected with 1.5 × 10(4) Eimeira tenella sporulated oocysts and birds in groups 1, 2 and 3 were medicated with 20, 40 mg extract/kg feed and 2 mg diclazuril/kg feed, respectively. The bloody diarrhea, oocyst counts, intestinal lesion scores, and the body weight were recorded to evaluate the anticoccidial efficacy. The results showed that D. febrifuga extract was effective against Eimeria infection; especially 20 mg D. febrifuga extract/kg feed can significantly increase body weight gains and reduce bloody diarrhea, lesion score, and oocyst excretion in comparison to infected-unmedicated control group.

Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents.

Febrifugine is an alkaloid isolated from Dichroa febrifuga Lour as the active component against Plasmodium falciparum. Adverse side effects have precluded febrifugine as a potential clinical drug. In this study novel febrifugine analogues were designed and synthesized. Lower toxicity was achieved by reducing or eliminating the tendency of forming chemically reactive and toxic intermediates and metabolites. Synthesized compounds were evaluated for acute toxicity and in vitro and in vivo antimalarial efficacy. Some compounds are much less toxic than the natural product febrifugine and existing antimalarial drug chloroquine and are expected to possess wide therapeutic windows. These compounds, as well as the underlying design rationale, may find usefulness in the discovery and development of new antimalarial drugs.

[Fluorescence spectra of Dichroa febrifuga aqueous extraction].

Fluorescence spectra of chang shan (Dichroa febrifuga Lour) aqueous extraction were studied. In the three-dimensional fluorescence contour spectrum, three fluorescence peaks of quinazoline alkaloids, which are the active components of chang shan, were observed. The excitation wavelengths of the peaks were 235, 270 and 320 nm, respectively, and the emission wavelength of all the peaks was 430 nm. Three-dimensional fluorescence contour spectrum is the very image of fingerprint, suitable for qualitative identification of traditional Chinese medicine. In the range of pH 3 to pH 6, the fluorescence spectrum of chang shan aqueous extractions changes with the variation in pH value. The reason for this spectral change might be the protonation of N-1 in quinazolone ring of beta-dichroine (febrifugine) molecule. There is an excellent linear relationship between the fluorescence intensity and the concentration of chang shan under nearly neutral conditions, thereby a quantitative method for the determination of quinazoline alkaloids may be established.

Suppression of ethanol and lipopolysaccharide-induced liver injury by extracts of Hydrangeae Dulcis Folium in rats.

In female SD rats that were injected with 4 g/kg BW ethanol p.o. followed by a 5 mg/kg BW lipopolysaccharide (LPS) i.v. injection, serum glutamic pyruvic transaminases (GPT) activity increased to about eight times that of normal rats. In this model, rats that had been fed a diet containing 1% Hydrangeae Dulcis Folium (HDF) extracts for fifteen days showed significantly lower serum GPT activity (380.0+/-58.2 IU/l) than the control group (3527.0+/-774.1 IU/l). HDF's efficacy was far superior to milk thistle in this model (2950.0+/-915.9 IU/l). When mouse macrophages were treated with HDF extracts at 50 microg/ml, TNF-alpha production induced by LPS was suppressed to about 10% of the control. Rat serum TNF-alpha levels induced by LPS was decreased to 58.7% of the control by administering 1000 mg/kg BW HDF extract p.o. These results indicate that HDF prevents alcohol-induced liver injury through the inhibition of TNF-alpha production.

Purification and characterization of an ethylene-induced antifungal protein from leaves of guilder rose (Hydrangea macrophylla).

An ethylene-induced, chitin-binding protein (designated as HM30) from leaves of Hydrangea macrophylla was identified and purified to apparent homogeneity by chitin affinity chromatography followed by FPLC on a Superose 12 column. The molecular mass of HM30 was 30,010.0 Da determined by mass spectrometry and its isoelectric point of 8.4 was estimated by isoelectric focusing. The amino acid composition of HM30 was also determined. The initial 15 amino acid residues of the N-terminal were found to be N-S-M-E-R-V-E-E-L-R-K-K-L-Q-D by automatic Edman degradation. This chitin-binding protein showed antifungal activity toward several crop fungal pathogens. Knowledge of properties of HM30 should be useful for its potential application as a plant fungicidal agent.

New anti-malarial flavonol glycoside from Hydrangeae Dulcis Folium.

Bioassay-guided fractionation of the MeOH extract of Hydrangeae Dulcis Folium resulted in isolation of a new flavonol glycoside and two known congeners as anti-malarial principles. These flavonol glycosides showed characteristic proliferation inhibition of Plasmodium falciparum at significantly low concentration without showing any cytotoxicity. In addition, several naturally occurring flavonol glycosides were also shown to exert similar anti-malarial behavior.