| Cyclosorus acuminatus (Houtt) Nakai is a member of Cyclosonis of Thelypteridaceae of Ferns subphylum of Pteridophyta. The whole plant or the rhizomes could be used as medicine and full-year harvest. It also has the medicinal name as Heisujing, niuneiba, xiaoyefenghuangweibacao and so on. It tastes bitter, astringent and flat. Chinese medicine believes that it has the effect of anti-inflammatory, spleen, calm, clearing heat and detoxification. Cyclosorus acuminatus is widely used in folk, especially in Jiangsu and Zhejiang provinces, to treat indigestion, infantile malnutrition, dysentery, diarrhea, hot shower, burns, rabies bites, sore throat and wind dampness. In the previous study, our group found the plant is rich in flavonoids. We separated and elucidated the structures of7new flavanone compounds. In order to systematic reveal the biological activity of the plant, this study was taken to investigate the biological activity and pharmacological mechanism of Cyclosorus acuminatus based on the traditional Chinese medicine theory, practical folk using and modern medical theory.The contents of this paper are divided into4parts. That is:A:The in vitro pharmacological analysis and the enrichment of the valid target. B:Investigation of the activity in metabolic syndrome and the lower-jiao syndrome using animal model. C:Investigate the synergism of the various parts and to determine the finally effective parts. D:Identify the pharmacological activity and its mechanism.In this study, macroporous resin was used to get segmentation G, S and H from the total methanol extract of Cyclosorus acuminatus. The refined crude polysaccharide was also get. Finally the H was identified as the main valid target via7in vitro free radical scavenging model, Cu2+induced LDL oxidation model, the liver spontaneous peroxidation model, the Fe2+-H2O2and Fe2+-Vc induced peroxidation of mitochondrial. And then, the main compounds of H were identified as total flavonoids using chemical color test and the best extraction and purification measure was optimized using orthogonal design.Then, the normal KM mice TC-lowing model and postprandial blood lipids model were used to examine the activity of lowing blood lipids. The OGTT model was to examine the activity of lowing blood glucose. The retinoic acid-induced bone calcium losing model was to examine the activity of anti-osteoporosis. The K2Cr2O7-induced acute renal toxicity model was to examine the activity of renal protection. The whole results suggested that Cyclosorus acuminatus has the activity of lowing blood lipids and glucose, and renal protection potential. The total flavonoids have the strongest pharmacological activity. The refined crude polysaccharide showed a certain potential for lowing blood glucose, but its effect is much weaker than the total flavonoids. And the crude polysaccharide did not show a diversity activity in lowing lipids and renal protection. At this stage, it can be concluded that the material base of Cyclosorus acuminatus is the total flavonoids.In order to investigate the synergism of the various parts and to determine the finally effective parts, the STZ-high fat diet-induced diabetic mice were used to study the hypoglycemic effect. In addition to the positive control, the total flavonoids group, the refined crude polysaccharide group and the total flavonoids-refined crude polysaccharide=1:1group were set. The results showed that the total flavonoids-refined crude polysaccharide=1:1group did not exert a synergistic effect. So the total flavonoids were finally identified as the activity part.Eventually, the protective effect of human umbilical vein endothelial cells against oxidative injury, the differentiation inhibition of3T3-L1preadipocytes, the protective activity in long-term high-fat diet-induced hyperlipemia mice and the renal protective effect in puromycin nephritic syndrome and diabetic nephropathy mice and the its specific mechanism were investigated. |
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