Influence of Processing on the Content of Toxic Carboxyatractyloside and Atractyloside and the Microbiological Status of Xanthium sibiricum Fruits (Cang'erzi).

The dried ripe fruits of Xanthium sibiricum (Cang'erzi) are used in traditional Chinese medicine for the treatment of nasal congestion, nasal discharge, allergic rhinitis, sinusitis, and wind-cold headaches. Carboxyatractyloside and atractyloside are important constituents of the fruits because these diterpenoid glycosides are responsible for their toxicity. In order to evaluate procedures for reducing the amount of the more toxic carboxyatractyloside, the fruits were dried and heated with different methods. Carboxyatractyloside and atractyloside were analysed by a new reversed-phase high-performance liquid chromatographic method using liquid chromatography-diode array detector-tandem mass spectrometry analysis. The results revealed that temperature and drying methods have a strong influence on the content of carboxyatractyloside and atractyloside. Fruits which were treated at higher temperatures showed a lower content of carboxyatractyloside and an increased content of atractyloside, which is 50 times less toxic. This indicates that the roasting process can reduce toxicity effectively. The microbiological colonisation of Xanthium fruits is also reduced by roasting and by drying above 100 °C. For the safe use of Cang'erzi, the effect of processing should be monitored and analysis of carboxyatractyloside and atractyloside should be obligatory in quality control.

[Determination of carboxyatractyloside and atractyloside in Xanthii Fructus by HPLC].

OBJECTIVE: To determine carboxyatractyloside and atractyloside in Xanthii Fructus by HPLC. METHOD: By HPLC, Agilent ZORBAX SB-phenyl (4.6 mm x 250 mm, 5 microm) column was adopted, with acetonitrile-0.01 mol x L(-1) NaH2PO4 (pH 6) as the mobile phase for gradient elution at the flow rate of 1.0 mL x min(-1). The detection wavelength was 203 nm, and the temperature was set at 35 degrees C. RESULT: Carboxyatractyloside showed a good linearity within the range of 0.0972-1.944 microg and atractyloside showed a good linearity within the range of 0.1030-2.060 microg. The recovery rate of carboxyatractyloside was 100. 3% and that of atractyloside was 102.5%. The RSD were 0.67% and 1.4% (n=6). CONCLUSION: This method is so simple, practical and highly repeatable that is can be used for quality control of Xanthii Fructus.

Atractylis gummifera L. poisoning: an ethnopharmacological review.

Atractylis gummifera L. (Asteraceae) is a thistle located in the Mediterranean regions. Despite the plant's well-known toxicity, its ingestion continues to be a common cause of poisoning. The toxicity of Atractylis gummifera resides in atractyloside and carboxyatractyloside, two diterpenoid glucosides capable of inhibiting mitochondrial oxidative phosphorylation. Both constituents interact with a mitochondrial protein, the adenine nucleotide translocator, responsible for the ATP/ADP antiport and involved in mitochondrial membrane permeabilization. Poisoned patients manifest characteristic symptoms such as nausea, vomiting, epigastric and abdominal pain, diarrhoea, anxiety, headache and convulsions, often followed by coma. No specific pharmacological treatment for Atractylis gummifera intoxication is yet available and all the current therapeutic approaches are only symptomatic. In vitro experiments showed that some compounds such as verapamil, or dithiothreitol could protect against the toxic effects of atractyloside, but only if administered before atractyloside exposure. New therapeutic approaches could come from immunotherapy research: some studies have already tried to produce polyclonal Fab fragments against the toxic components of Atractylis gummifera.

The isolation of a storage organelle of atractyloside in Callilepis laureola.

A method has been developed for the preparation of protoplasts from both the leaves and tubers of Callilepis laureola, a plant used extensively as a medicament by black people in South Africa. The cellular vacuoles from these protoplasts were isolated and tested for the presence of the nephrotoxic substance, atractyloside, by thin layer chromatography and immunoassay. Both methods indicate that the vacuole of C. laureola is the primary site of storage for atractyloside in the cells of the tuber.

Toxicity of Callilepis laureola.

Callilepis laureola, which has been found to cause fatal liver necrosis in the Black population of Natal, is widely used as a herbal medicine. Chemical extraction has yielded a product, identified as atractyloside, which is responsible for the nephrotoxic and hypoglycaemic effects of Callilepis laureola. The hepatotoxic principle has not yet been isolated.