Chemical Constituents From Roots Of Actinidia And Their Antitumor Activities

The dry roots of Actinidia which are often used to clear heat, treat dyspepsia and fractures, have shown a wide spectrum of pharmacological functions including antitumor, antioxidant and liver protection, especially in case of digestive system neoplasia which have attracted more and more attention. Until now there are several types of chemical components which have been confirmed in the roots of Actinidia, including triterpenoids, flavonoids, phenols, anthraquinones, coumarins and steroids.To date, few studies have been reported on the chemical fingerprints of Actinidia roots, especially the fingerprints of different species of Actinidia, which play an important role in rapid authentication and quality control of this medicinal material. Meanwhile, it can be better to take a whole quality control for the raw material quality by combining chemical fingerprints with activity data. Up to now, more than 100 compounds have been isolated from Actinidia roots. However, its pharmacodynamic chemical basis remains unclear. Therefore, the separation and activity tests of these compounds isolated from Actinidia roots as well as its action mechanism is still important in Actinidia roots related research and applications.The extraction method of total triterpenoids and flavonoids from roots of Actinidia chinensis Planch has been investigated, and finally the ultrasound extraction method was chosen as the preferred one. Based on the preferred extraction method, the operating conditions have been optimized using single factor and orthogonal experimental design. The optimized conditions were as follows:70% ethanol was used as the extraction solvent; the ratio of material to liquid was 1:15; the extraction was for 30 min each time with 3 times.The fingerprint of polyphenols from three species of Actinidia roots including Actinidia chinensis Planch, Actinidia deliciosa and Actinidia arguta was developed using the combination of polyamide column chromatography and HPLC-MS under the optimized extraction conditions. As a result,27 peaks were detected, of which 9 peaks were common among all the three species,7 peaks were unique for Actinidia chinensis Planch, while 6 peaks for Actinidia deliciosa and 1 peak for Actinidia arguta. For the detected peaks,16 of them were identified by HPLC-ESI-MS/MS in this work, and the relative peak area (RPA) was used for a quantitative analysis of the detected compounds. As a result, the RPA of common peaks for roots of Actinidia chinensis Planch, Actinidia deliciosa and Actinidia arguta were 81.4%,80.27% and 91.52% respectively, and the RPA for the unique peaks were 11.52%,15.63% and 7.68%, respectively. Furthermore, the anti-gastric carcinoma, anti-colorectal carcinoma, anti-liver cancer and anti-carcinoma of uterine cervix activities of the polyphenols enriched from the three species of Actinidia roots were tested. The results showed that the roots of Actinidia deliciosa showed the most remarkable antitumor activity, followed by Actinidia chinensis and Actinidia arguta. Thus, we drew a conclusion that the antitumor activities of Actinidia roots were possibly be correlated with the compositions and contents of their characteristic polyphenol components.Meanwhile, some chemical compounds have been extracted and isolated from the Actinidia chinensis Planch roots systematically using various kinds of phytochemical methods, such as gradient extraction, column chromatography with AB-8 macroporous resin, silica gel and sephadex and preparative liquid chromatography. As a result,7 compounds were separated from the ethyl acetate extracts and compound 1 was identified as 2a,3β,23-trihydroxyurs-12,20(30)-dien-28-oic acid by NMR, while the other six compounds were not identified yet. Meanwhile, the anti-gastric carcinoma and anti-colorectal carcinoma activity of the ethyl acetate, n-butyl alcohol extracts,50% and 70% ethanol fraction of AB-8 of the ethyl acetate was verified by MTT method. The n-butyl alcohol extracts showed the best antitumor activity followed by ethyl acetate,70% ethanol and 50% ethanol fraction of AB-8 of the ethyl acetate extracts.