Studies On The Chemical Constituents In The Root Bark Of Morus Alba And Their Bioactivities

Cortex Mori is the dry root bark of Morus alba L,and a famous traditional Chinese medicine,which used to treat bacterial infection,cough with lung-fire,asthma,edema and other diseases.Therefore,the C.Mori has once become an important research object for scientists.The natural pharmaceutical chemistry researchers have isolated more than 150 compounds from the C.Mori,the main compounds were flavonoids and stilbenes.Meanwhile,pharmacological researchers using scientific methods have proved that crude extracts and some monomeric compounds of the C.Mori have various bioactivities,like neuroprotective,anti-inflammatory,anti-microbial,anti-tumor,anti-diabetic and so on.M.alba is rich in resources,and the whole body of M.alba is treasure,especially the root bark of M.alba has extensive utilization value and development potential,So the chemical constituents and biological activities of the C.Mori have been systematically studied in this paper which basis on previous research findings,and this paper was divided into four chapters:The first chapter described in detail the chemical constituents and biological activities of the C.Mori.According to previous literatures,more than 60 kinds of flavonoids and stilbenes each have been isolated from the root bark of M.alba,flavonoids manly included dihydroflavones,dihydroflavonols and flavonoids,stilbenes manly included 2-phenylbenzofuran compounds.The biological activities of the C.Mori manly included anti-inflammatory,anti-tumor,anti-microbial,heart protection,liver protection,nervous system protection,anti-oxidant and diabetes treatment.The second chapter described the whole process of C.Mori’s extraction,separation and identification of monomeric compounds,this study used 75%ethanol to extract C.Mori,and then a variety of separation methods（TLC,silica gel column chromatography,recrystallize,Sephadex LH-20,reversed-phase column chromatography,HPLC,etc.）were used to isolated compounds from the C.Mori,subsequently a variety of methods(¹H-NMR,¹³C-NMR,DEPT,2D-NMR,UV and HRESIMS,etc)were used to identified monomeric compounds.62 compounds were isolated from the root bark of M.alba,including fifteen dihydroflavones（1-15）,seven flavones（16-22）,twenty-two 2-phenylbenzofuran compounds（23-44）,nine cyclized triterpenoids（45-53）,one open cyclized triterpenoid（57）,three steroids（54-56）,two tocopherols（58,59）,two coumarins（60,61）and a fatty acid（62）.Compounds 1-4,45and 60 were identified as six new compounds,Additionally,compounds 56,57 and 61were isolated from the Moraceae family for the first time,compound 49 was first discovered in the Morus genus,and compounds 50 and 55 were first isolated from the M.alba species,these compounds will provide new chemical evidences for the classification of Moraceae plants.The third chapter have evaluated anti-inflammatory and anti-tumor activities of flavonoids,stilbenes and coumarins.The anti-inflammatory activities were determined by Griess method,the results showed that compounds 21,26,27 and 61 have some level of anti-inflammatory activities,and the IC₅₀ of the compound 27 was 15.6±0.3μM,which was comparable to the IC₅₀ of the positive control drug L-NMMA 15.2±0.2μM.The anti-tumor activities were determined by MTT method,the results showed that compounds 6,7,12,22,25,28 and 34 moderately inhibited HCT8 tumor cell,compounds 10,11,17,18,19,31,37,38,39 and 40 showed cytotoxicity against two human tumor cells（HCT8 and Hep G2）,and compound 19showed the strongest inhibitory effect on two human tumor cells with IC₅₀ of 12.5 and25.7μM,respectively.The inhibitory effect of compound 19 on HCT8 tumor cells was slightly stronger than the positive control drug cisplatin,and its cytotoxicity on human normal liver cells（LO2）was less than the positive control drug cisplatin.The fourth chapter have summarized this paper and prospected the research of C.Mori.