| My work was composed by three parts. The first part was about the material foundation study of anti-rheumatoid arthritis (RA) effect of the rhizomes of Impatiens pritzellii Hook. f. var. hupehensis Hook. f. The second part was about the material foundation study of hepatoprotective activity of Radix Actinidia chinensis Planch root. The third part was review articles. One was the survey of chemistry and activities of echinocystic acid and its saponins, and the other was the progress of the chemical study of Genus Actinidia plants.Part OneThe rhizomes of Impatiens pritzellii Hook. f. var. hupehensis Hook. f. (Balsaminaceae) was a popular folk medicine in Tujia-tribe district of Hubei Province as an anti-RA medicine and has being used in several hospitals in Enshi district. In order to confirm the anti-RA effect and screen the active fractions and active compounds of I. pritzellii, we systematically studied the chemical constituents and the medicinal effect of this plant from Enshi district of Hubei Province.Our study established one of the most widely used patho-model for rheumatoid arthritis: type II collagen-induced arthritis in mice (CIA). Administration of the MeOH extract and the n-BuOH fraction of I. pritzellii suppressed the development of CIA in mice significantly, and down-regulated the levels of anti-type II collagen antibodies. This result proved the anti-RA effect of I. pritzellii, and showed that the n-BuOH fraction is the active fraction of anti-RA effect of I. pritzellii, according with the results of active fraction of anti-inflammatory and analgesic effects we studied before. I. pritzellii and its active fraction also decreased the spleen and thymus indexes, down-regulated the levels of IgG, INF-γ, IL-18, and up-regulated the concentration of IL-10 in the serum of mice with CIA. Influencing many cytokines and then modulating the whole cytokine network is suggested to be one of the anti-RA mechanisms of I. pritzellii.Our chemical constituents study of I. pritzellii afforded 30 compounds: echinocystic acid (Comp. 1), 3-O-β-D-GluA echinocystic acid (Comp. 2), 3-O-β-D-GluA-Me echinocystic acid (Comp. 3), Impatiprin A* (Comp. 4), Impatiprin B* (Comp. 5), Impatiprin C* (Comp. 6), n-butyl-β-D-fructopyranoside (Comp. 7), 5-hydroxymethyl furfural (Comp. 8), di (2-ethylhexyl) phthalate (Comp. 9), soya-cerebrosides I (Comp. 10), soya-cerebrosides II (Comp. 11), patriscabratine (Comp. 12), hentriacontane (Comp. 13), methyl lignocerate (Comp. 14), palmitic acid (Comp. 15), stearic acid (Comp. 16), methyl stearate (Comp. 17),α-spinasterol (Comp. 18), spinasteryl-3-one (Comp. 19), 3β-acetyl-α-spinasterol (Comp. 20), 3-O-β-D-Glu-α-spinasterol (Comp. 21), 3-O-palmitoyl-α-spinasterol (Comp. 22), 3-O-[6'-O-palmitoyl-Glu]-α-spinasterol (Comp. 23), n-hexadecane acid monoglyceride (Comp. 24), tetracosanoic acid monoglyceride (Comp. 25), 2-amino-2-deoxy-α-D-glucose (Comp. 26), 2-amino-2-deoxy-β-D-glucose (Comp. 27),β-D-fructofuranose (Comp. 28),α-D-fructopyranose (1-2')β-D-fructopyranose (Comp. 29) andα-D-fructopyranose 1,2:2,3'β-D-fructopyranose (Comp. 30). Comp. 1, 2, 3, 4, 5, 6, 7, 8, 10, 11, 12, 18, 21, 24, 25 were isolated from the active fraction: n-BuOH fraction and Comp. 4~6 are new.In the purpose of screening the active components of anti-RA, several correlative activities of the constituents from I. pritzellii (especially the n-BuOH fraction) were evaluated, including anti-inflammatory, analgesic, immune suppressive effects, and the IL-18 inhibitory activity. Finally, CIA mice were established and used for evaluating the anti-RA activity of several active components. The results of the screening experiments showed the obvious anti-inflammatory effects of Comp. 3, 5, 6 to dimethylbenzene-induced ear edema in mice. Both of the high and low doses groups of Comp. 5 and the high dose group of Comp. 6 exhibited the analgesic effects to acetic acid-induced writhings in mice. Comp. 1, 3, 5, 7, 12, 23 could inhibited the T lymphocyte proliferation, and Comp. 1, 3, 4, 5, 7, 20, 23 exhibited depressive effect to the B lymphocyte proliferation. Administration of Comp. 2 and 6 decreased the serum hemolysin level significantly and showed obviously depressive effect to humoral immunity. Comp. 1, 2, 6, 12, 26 showed obvious activities to inhibit the production of IL-18 in PBMCs induced by LPS. At last, Comp. 5 and 6 were evaluated by CIA mice, but both of them could not suppress the development of CIA in mice significantly. From these results, it is suggested that the anti-RA effect of I. pritzellii follows the multitarget theory and the mechanism is multiplicity.Part TwoThe root of Actinidia chinensis Planch. was a traditional Chinese medicaine and used to cure hepatitis and other illness in folk. We began the material foundation study of hepatoprotective activity of Radix Actinidia chinensis.We evaluated the effects of the alcohol extract of Radix A. chinensis root and its fractions on carbon tetrachloride (CCl4) induced acute liver damage in mice. Polysaccharides fraction and EtOAc fraction were revealed moderate or limited hepatoprotective activity. The assaying of the polysaccharides was carried out on behalf of the further study of actinidia chinensis polysaccharide (ACPS).Our chemical constituents study of the root of Radix A. chinensis afforded 31 compounds, and 30 of them were identified: 2α,3β-dihydroxyurs-12-en-28,30-olide* (Comp. 1), 2α,3β,24-trihydroxyurs-12-en-28,30-olide* (Comp. 2), oleanolic acid (Comp. 3), 3-epi-corosolic acid (Comp. 4), 2α,3α,24-trihydroxyurs-12-en-28-oic acid (Comp. 5), 23-hydroxyursolic acid (Comp. 6), asiatic acid (Comp. 7), 2α,3α,19,24- tetrahydroxyurs-12-en-28-oic acid (Comp. 8), 3β-hydroxyurs-12,18-dien-28-oic acid (Comp. 9), 2α,23 dihydroxylmicromeric acid (Comp. 10), vanillic acid (Comp. 11), di (2-ethylhexyl) phthalate (Comp. 12), tachioside (Comp. 13), isotachioside (Comp. 14), 5-hydroxy-6-methoxy-7-O-β-D-glucosyl coumarin (Comp. 15), 1-O-(β-D-glucosyl)- 2-[2-methoxy-4-(ω-hydroxypropyl)-phenoxy]-propan-3-ol (Comp. 16), (?)-epi- catechin (Comp. 17), (+)-catechin (Comp. 18), uracil (Comp. 19), adenine (Comp. 20), myo-inositol (Comp. 21), disaccharide (Comp. 22), ceramide (Comp. 23), n-butyl-β-D-fructopyranoside (Comp. 24),β-sitosterol (Comp. 25),β-daucosterol (Comp. 26), palmitic acid (Comp. 27), stearic acid (Comp. 28), hexadecane or octadecane (Comp. 29), alkenes (Comp. 30). Ten triterpenoids (Comp. 1~10) of them were isolated from the hepatoprotective EtOAc fraction, including two new compounds: Comp. 1 and Comp. 2. These triterpenoids were thought to be the material foundation of hepatoprotective activity of EtOAc fraction of Radix Actinidia chinensis.Part ThreeEchinocystic acid (EA) and its saponins are main active constituents in I. pritzellii. One of our review in this thesis covers the chemistry and the activities of EA and its saponins from the first discovery of EA (1934) to now (2006) (157 literatures), and could be helpful to further develop and utilize of EA and its saponins. The other review article was the progress of the chemical study of Genus Actinidia plants (60 literatures).
|
PDF Full Text Request