| Fructus Corni, ripe sarcocarp of Cornus Offinalis Sieb. et Zucc (deciduous small arbor or shrub), was mainly grown in the mountain at the altitude of400-2000meters in Zhejiang, Shaanxi, Henan province. Fructus Corni, as a traditional Chinese medicine, has been used for treatment of liver and kidney deficiency of vertigo, tinnitus, weak knees, bleeding vaginal discharge, emission enuresis and weakness sweating sickness since2000years ago. It contains a variety of ingredients including terpenes, tannins, flavonoids, organic acids, which showed neuroprotective, antioxidant, anti-inflammatory, anti-diabetes and cardiovascular protection effect.This project was carried out in chemical composition, analysis method and biological activity of Fructus Corni, the main contents are presented as follows:1. Extraction and isolation of the chemical compounds from Fructus CorniFructus Corni was extracted by80%ethanol, the obtained extract was separated using countercurrent chromatography and other methods. During the countercurrent chromatography separation, several elution mode including classical mode, dual-mode and elution-extrusion mode were applied. After four step countercurrent chromatography run, other isolation means including reverse phase ODS silica gel chromatography, preparative high-performance liquid chromatography and preparative thin-layer chromatography were performed.32compounds were obtained in total and identified by spectroscopic methods. They are:Loganin (1), Sweroside (2), Morroniside (3), Gallic acid (4), Kingiside (5), Loganic acid (6),10-hydroxycornin (7),7-ketologanin (8),7-O-methylmorroniside (9), Cornuside I (10),8-epikingiside (11), secologanoside (12),10-hydroxyhastatoside (13), Hastatoside (14), Dihydrocornin (15), Swertimarin (16), Secologanin (17), Cornin (18),7-O-methylmorroniside (19), Cornuside Ⅱ (20), Arjunglucoside Ⅱ (21), Dehydromorroniside aglycone (22), Oleanolic acid (23), Ursolic acid (24),7-O-galloyl-D-sedoheptulose (25), Cornusiin B (26), Mevaloside (27),1,2,3-tri-O-galloyl-β-D-glucose (28), Quercetin3-O-β-D-Glucuronide (29), Ellagic acid,(30),(3beta)-pregna-5,16,20-triene-3,20-diyl diacetate (31), Eudesma-5,11(13)-dien-8,12-olide (32). These compounds belong to iridoid (1-3,5-20,22), pentacyclic triterpenoids (21,23,24), monoterpenes (27) and sesquiterpenes (32), tannins (25,26,28), phenolic acid (4,30), flavonoids (29), sterols (31). Among them, nine compounds:5,7,11,12,14,16,17,31and32were isolated from this plant for the first time.2. Establishment of component analysis method for Fructus CorniIridoids is the characteristic constituents in Fructus Corni, showing high content and many biological activities. In this study, two methods for simultaneous determination of eight characteristic iridoid glycosides in Fructus Corni were established:(1) high-performance capillary electrophoresis (HPCE-UV),(2) Ultra Performance Liquid-tandem mass spectrometry (UPLC-MS/MS), were utilized to determin morroniside,7-dehydrologanin, loganin, sweroside, morroniside,7-O-methylmorroniside, cornuside I,7-O-methylmorroniside, cornuside II in Fructus Corni. Meanwhile, based on17batches of samples, the standard UPLC fingerprint of Fructus Corni was established. Samples from different sources were processed by similarity analysis and hierarchical clustering analysis. Combining the analysis results with the determined contents of characteristic constituents, the effect of harvesting period and area on the intrinsic quality of Fructus Corni were investigated. The results show that multi-component measurement combining fingerprint analysis is a reliable identification and quality evaluation method for traditional Chinese medicine.3. Biological activity of the terpenoids from Fructus CorniTerpenoids are the main components in Fructus Corni. The fisrt part of this chapter:the effect of19isolated terpenoids on two glioma cells (LN229and U87cells) proliferation were examined. Two triterpenoids, oleanolic acid and ursolic acid, significantly inhibited both cells growth. The IC50for oleanolic acid is12μM in LN229cells and25μM in U87cells, for ursolic acid is25μM in LN229cells and35μM in U87cells. Both compounds exhibited a clear dose-response relationship.The second part of this chapter:The cornel total iridoid glycosides and morroniside, one single iridoid were investigated on their antithrombotic activity. Tain intravenous injection of norepinephrine and bovine serum albumin, resulted in rat pre-thrombotic model, followed by arotid artery thrombus formation experiment induced by electrical stimulation. The results showed that the cornel total iridoid glycosides and morroniside can inhibit thrombus formation and prolong the time-to-occlusion. The mechanism is reducing the level of thromboxane A2and serotonin in vivo, elevating the level of prostacyclin I2, thereby inhibiting platelet aggregation and causing vasoconstriction. Cornel total iridoid glycosides inhibited the extrinsic coagulation pathway by improving the levels of tissue factor pathway inhibitor; morroniside can enhance fibrinolytic activity by increasing plasmin levels. Meanwhile, cornel total iridoid glycosides and morroniside does not prolong the bleeding time out of the normal range and presented no effect on platelet count, which means they does not cause bleeding tendencies and can be used safely.
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