[Structure of a saponin of Polygala chinensis (author's transl)].
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OBJECTIVE: This study describes the in vitro action of the hydroalcoholic extract and the 1,7-dihydroxy-2,3-dimethoxy xanthone isolated from P. cyparissias on agonist and ovalbumin induced contractions in trachea, from normal and actively sensitised guinea pigs. RESULTS: The hydroalcoholic extract of P. cyparissias (0.125 to 1 mg/ml), incubated with the guinea-pig trachea for 20 min, had no effect on the resting tone of the preparations, but caused a concentration-dependent, reversible and non competitive inhibition of contractions induced by acetylcholine, histamine, compound 48/80, bradykinin, substance P, prostaglandin E2 and the stable analogue of thromboxane A2 mimetic U 46619. The calculated mean IC50 values for the hydroalcoholic extract were: 0.37, 0.51, 0.06, 0.32, 0.48, 0.3 and 0.17 mg/ml, respectively. Also, the extract of P. cyparissias (0.125 to 0.5 mg/ml) antagonised, in a graded manner (IC50 of 0.46 mg/ml) ovalbumin-induced contractions in guinea-pig trachea obtained from animals which had been actively sensitised to this antigen. Pre-incubation of the preparations with the purifed xanthone isolated from P. cyparssias (2.5 to 80 microg/ml; 10.0 to 310.0 microM) caused significant and concentration-dependent, reversible and noncompetitive inhibition of the contractile responses elicited by acetylcholine, histamine, bradykinin, substance P, U 46619 and prostaglandin E2. The calculated mean IC50 values for these effects were: 132.0, 73.0, 9.2, 32.0, 110.6 and 66.0 microM, respectively. At very high concentrations (I55.0-620.0 microM) the xanthone also antagonised contraction induced by KCl in guinea-pig trachea (IC50 of 190.0 microM). CONCLUSIONS: Taken together these and our previous in vivo results are consistent with the view that the active principles present in P. cyparissias, including the 1,7-dihydroxy-2,3-dimethoxy xanthone, antagonise, in a non competitive but, reversible manner the contractions induced by chemical inflammatory mediators in the guinea pig trachea in vitro. Thus, these results might explain at least in part, the medicinal use of this plant in the management of inflammation, asthma and allergy.
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Twenty-four South African medicinal plants were screened against Candida albicans standard strain ATCC 10231 and two clinical isolates from a 5-month-old baby and an adult, in an attempt to find a traditional remedy to treat oral candidiasis, which is prevalent in HIV-patients. Allium sativum L. and Tulbaghia violacea L. aqueous bulb extracts had MIC values of 0.56 and 3.25mg/ml respectively, whilst Polygala myrtifolia L. leaves and Glycyrrhiza glabra L. rhizome extracts had MIC values of 1.56 mg/ml when tested against the 5-month-old isolate. Fresh water extracts stored at 4, 23 and 33 degrees C over a period of a week, were used to determine the stability of these extracts. Allium sativum and Tulbaghia violacea maintained activity at 4 degrees C, but not at higher temperatures, whereas Polygala myrtifolia and Glycyrrhiza glabra lost activity within a day even at 4 degrees C. The unpleasant taste of the two species with a garlic smell, could however not be masked, and as the smell following the eating of the two species would lead to HIV-patients being recognised, these two plants where not considered for further investigation. Therefore, Polygala myrtifolia and Glycyrrhiza glabra are being further investigated for use as an oral mouthwash in clinics and homes.
DX-9386 is a traditional Chinese medicinal prescription consisting of ginseng (Panax Ginseng C. A. Meyer), polygala (Polygala Tenuifolia Willdenew), acorus (Acorus Gramineus Soland) and hoelen (Poria Cocos Wolf). We recently found that oral administration of the prescription at a dose of 500 mg/kg intensified the formation of long-term potentiation (LTP) in the dentoff gyrus of anesthetized rats. To evaluate the individual contribution of separate ingredients in DX-9386 towards the observed biological activity, we investigated their direct influence upon LTP formation in vivo. A single oral administration of hoelen and ginseng (250 and 500 mg/kg) significantly increased the spike amplitude evoked by a subthreshold tetanic stimulation at time intervals up to 30 min after tetanus. Only minor effects of polygala (500 mg/kg) and no influence of acorus up to 500 mg/kg were observed. No drugs affected the basal spike amplitude induced by a test stimulus. In addition, we ascertained that DX-9386 was also active at a dose of 250 mg/kg. Taken together, these results indicate that hoelen and ginseng are the active components of DX-9386 with regard to the enhancement of hippocampal LTP.
The growth inhibitory and differentiation inducing effects of euxanthone (1,7-dihydroxyxanthone) from the medicinal plant Polygala caudata on the neuroblastoma (Neural 2A, subclone BU-1) were investigated. At the concentration range of 0-100 microM, euxanthone inhibits the growth of BU-1 cells in a dose dependent manner. The 50% growth inhibitory concentration (IC50) was 41 microM. Significant induction of morphological differentiation and neurite growth was observed at the concentration of 100 microM. Frequency of proliferative neuroblastoma cells was determined after induction of differentiation. The frequency of proliferating BU-1 cells was markedly reduced from 1/1.1 to <1/99. Confocal microscopy also confirmed that the morphological differentiation of BU-1 was associated with the expression of neurite specific marker MAP-2 protein in neurites. These data suggest that euxanthone may be one of the neuropharmacological active compounds in the medicinal plant Polygala caudata.