Studies On The Chemical Constituents And Bioactivity Of Ilex Centrochinensis S.Y.Hu And Ilex Ficoidea Hemsl

The genus Ilex is the largest of the family Aquifoliaceae, comprising approximately 400-500 species. This genus contains various chemical compositions and possesses extensive pharmacological activities. Some Ilex species are distributed widely in China and have been used extensively as traditional Chinese medicine. Ilex ficoidea Hemsl and Ilex centrochinensis S.Y.Hu are used commonly in Chinese folk medicine. In order to better development and utilization of the two kinds of medicinal resource, studies on the bioactivity and chemical constituents of the two Ilex species were carried out.1. Appraisal of anti-inflammatory and free radical scavenging activities of ethanol extract of Ilex ficoidea Hemsl and Ilex centrochinensisThis part was to appraise the anti-inflammatory and free radical scavenging activities of ethanol extracts of Ilex ficoidea Hemsl (EIFH) and Ilex centrochinensis S.Y.Hu (EICC). Anti-inflammatory activities were evaluated using xylene-induced ear edema and the cotton pellet granuloma tests. Some antioxidants produced during chronic inflammation were quantitated and the DPPH, superoxide anion and hydroxyl free radicals scavenging activities in vitro were also investigated. EICC showed a significant anti-inflammatory effect during the acute inflammation and chronic inflammation without any acute oral toxicity. However, EIFH exhibited a negligible anti-acute inflammatory and a moderate anti-chronic inflammatory activity. EICC significantly inhibited the formation of MDA and markedly raised the activities of SOD, CAT and GSH-Px. EIFH could reduce the level of MDA and elevate the activity of SOD only at the high dose. The free radical scavenging activities of EICC are higher than that of EIFH. These results suggest that EICC possesses significant anti-inflammatory and free radical scavenging activities. The anti-inflammatory mechanism is attributed, in part, to enhance the activities of antioxidant enzymes. The results may also provide scientific evidence to support the folk medicinal utilization of Ilex centrochinensis for the treatment of rheumatoid arthritis. 2. Studies on chemical constituents of Ilex centrochinensis S.Y.Hu and the cytotoxic activities of a few compoundsThe chemical constituents study of Ilex centrochinensis S.Y.Hu afforded 14 compounds, and they were identified as six flavans:(2S)-5,3',4'-trihydroxy-7-methoxyflavan (IC1), (2S)-5-hydroxy-7,3',4'-trimethoxyflavan (IC2), (2S)-5,4'-dihydroxy-7,3'-dimethoxy-flavan (IC3), (2S)-5,4'-dihydroxy-7-methoxy-flavan (IC4), (2R)-7,3',4'-trimethoxy-5,8-quinoflavan(IC5), (2S)-7-methoxy-4'-hydroxy-5,8-quino-flavan (IC6); three flavones:Naringenin (IC7), Kaempferol (IC8), Quercetin (IC9); three triterpenoids:Oleanolic acid (IC10), Ursolic acid (IC11), Uvaol (IC12); one sterol:?-sitosterols (IC13); one polyphenol:1,4-benzenediol (IC13). Compound IC1, IC5, IC6 are new compounds, Compound IC2 is a new natural product.The cytotoxic activities against Caco-2 cell and HuH7 cell of six flavans (compounds IC1-6) were evaluated in vitro using the MTT method. They all displayed no cytotoxic activity against Caco-2 cell lines. Compounds IC3 and IC4 showed strong cytotoxic activity against Huh7 cell lines with IC50 values of 8.98?g/ml and 13.04?g/ml, respectively. Compound IC1, IC2, IC5, IC6 exhibited relative weak cytotoxic activity with IC50 values of 25.77?g/ml,26.42?g/ml, 20.20?g/ml,22.48?g/ml, respectively.3. Studies on chemical constituents of Ilex ficoidea HemslIn the present reports, Seventeen compounds were isolated from ethanol extract of the leaves of Ilex ficoidea Hems, and they were identified as:six triterpenoids: Friedelan-3-one (IF1),4-epifriedelin (IF2), Lupeol (IF3), Oleanolic acid (IF4), 3-acetyloxy-oleanoic acid (IF5),3?-acetoxy-6?,13?-dihydroxyolean-7-one (IF6); 2-(4-hydroxybenzyl) malic acid (IF7),2-(4-hydroxybenzyl) malic acid-4-ethyl ester (IF8); three anthraquinones:Emodin (IF9), Chrysophanol (IF10), Physcion (IF11); four glycosides:Quercetin-3-O-?-L-arabinopyranoside (IF14), Hyperoside (IF15), Cis-syringin (IF16), Ethyl-O-?-L-arabinopyranoside (IF17); two sterols:(?-sitosterols (IF12),?-spinasterol (IF13). All these compounds were isolated from Ilex ficoidea Hemsl for the first time, and compound IF8 is new.