ABSTRACT
Objective To isolate and identify chemical ingredients with anti-complement activity from Aster ageratoides and investigate the key targets and anti-inflammatory activities of obtained compounds with good anti-complement activity. Methods Using silica gel column, sephadex LH-20 column, Medium Pressure Liquid Chromatography system, and Semi-preparative HPLC, chemical ingredients that displayed anti-complement activity were isolated. Their chemical structures were identified by 1H-NMR and 13C-NMR and their anti-complement activities and targets were investigated by erythrocyte hemolysis in vitro. In addition, using LPS-stimulated RAW264.7 cells, we investigated the anti-inflammatory activity of compound 2. Results A total of 14 compounds were obtained from A. ageratoides and identified as oleanolic acid (1), quercetin (2), kaempferol (3), 3,5,7,3’-tetrahydroxy- 4’-methoxyflavone (4), kaempferol-7-O-α-L-rhamnopyranoside (5), quercetin-3-O-β-D-glucopyranoside (6), kaempferol-3-O-α-L- rhamnoside (7), quercetin-3-O-α-L-rhamnoside (8), kaempferide-3-O-β-D-glucopyranoside (9), kaempferol-3-O-β-D- glucopyranoside (10), kaempferol-7-O-β-D-glucopyranoside (11), kaempferol-3-O-β-D-glucopyranoside-7-O-β-D-glucopyranoside (12), kaempferide-3-O-α-L-rhamnoside-(1→6)-β-D-glucopyranoside (13), and rutin (14). They all exhibited anti-complement activity to some certain degree and good structure-activity relationship. The targets of compounds 1 and 2 were C1q, C5, and C9 and C1q, C2, C5, and C9, respectively. The anti-inflammatory experiments indicated that compound 2 exhibited a significant biological activity, which significantly suppressed the release of NO, TNF-α, and IL-6 and expressions of iNOS and COX-2. Conclusion A total of 14 compounds were obtained and they all displayed anticomplement activity, of which compounds 1, 4, 6, 9, 12, and 13 are firstly discovered in A. ageratoides. Compound 2 exhibited a significant anti-inflammatory activity.
ABSTRACT
Objective To study the effective composition of Aster ageratoides Turcz for relieving asthma and its toxicity . Methods Seventy‐two qualified male guinea pigs ,body mass(300 ± 20)g ,were randomly divided into the control group ,aminophyl‐line group(0 .047 g/kg) and different ratio group of total saponins and total flavonoids (8∶1 ,4∶1 ,2∶1 ,1∶1 ,1∶2 ,1∶4 ,1∶8) . Every group received at dose of 0 .38 g/kg once a day for 3 days by intragastric administration .The effect of relieving asthma was taken as the indicators for the optimization of compositions ,which was detected by observing the latent period of asthma induced by acetylcholine‐histamine in guinea rats .The relaxation percentage of smooth muscle retracted by acetylcholine was detected by Pow‐erlab biological signal collecting system when aminophylline(1 .25 mg/mL) and different matching drugs(0 .02 g/mL) were added in Krebs′solution .The acute toxicities of total saponins ,total flavonoids and mixture of total saponins with total flavonoids (ratio of 1∶2) were detected by classical acute toxicity test of mice .Results Compared with the control group ,aminophylline group ,each group latent period of inducing asthma significantly or very significantly prolonged (P<0 .05) ,among them ,1∶1 ,1∶2 ,1∶4 group and other matching group were significantly different(P<0 .05) ,but 1∶2 group cited the longest incubation period .Aminophylline group and the ratio could significantly relaxe guinea pig tracheal smooth muscle retracted by acetylcholine .Aminophylline group di‐astolic percentage was the largest(24 .12 ± 1 .20)% ,all the groups were less than the percentage of diastolic aminophylline group (P<0 .05) ,but in 1∶2 group with the closest .Aster ageratoides Turcz ,tatarian aster total saponins ,total flavonoids and the ratio of 1∶2 to mice maximum tolerance was respectively 300 ,345 ,325 g/kg .Conclusion For the same total dosage ,the relieving asth‐ma effects of proportions of 1∶2 Aster ageratoides Turcz were obvious .There are no abnormal changes in the acute toxicity trila with total flavonoids ,total saponins ,as well as the ratio of 1∶2 ,safety is relatively good .