| Summary: | 博士 === 國立成功大學 === 化學系碩博士班 === 98 === Five compounds, panajaponol A (731), pseudoginsenoside RT1 butyl ester (732), panaxjapyne A (738), panaxjapyne B (739) and panaxjapyne C (740) , together with 37 known compounds, were isolated from the roots of Panax japonicus C. A. Meyer var. major. In pharmacological studies, oleanolic acid (177), chikusetsusaponin Ib (181), taibaienoside I (733), chikusetsusaponin IVa methyl ester (735) and pseudo-ginsenoside RT1 methyl ester (737) exhibited strong inhibition of superoxide anion generation and elastase release by human neutrophils in response to formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B (fMLP/CB), with IC50 values ranging from 43.63 to 0.78 μM, respectively. In addition, C17 polyacetylene exhibited the inhibitory activities on baker’s yeast α-glucosidase. Amoung them, (3S,10S)-panaxydiol (242) showed stronger inhibitory activity with the IC50 value of 22.21 ?M. Panajaponol A (731) showed greater than two- to three-fold selective cytotoxic activity against KB and DU145 cancer cell lines with the GI50 values of 6.27 and 7.30 μg/mL, respectivily.
Bioassay-guided fractionation of the EtOH soluble portion of the water extract of the roots of Panax quinquefolium and Panax ginsen afforded active compounds, ginsenoside Re (51) and ginsenoside Rg2 (5) (EC50=95.1 and 114.7 μM), to relaxation in rabbit corpus cavernosum. In addition, we studies the phytochemical analysis on of the water extract of the roots of Panax quinquefolium, and isolated thirty-one compounds, including four new compounds, including panajaponol B (750), panaxjapyne D (751), panaxjapyne E (752) and panaxjapyne F (753).
Twenty-six compounds were isolated from the methanol extracts of the roots and the leaves of Salvia nipponica var. formosana, and they showed potent inhibitory effects on superoxide anion production in fMLP/CB-activated human neutrophils as well as other anti-inflammatory effects. Among them, ursolic acid (689), salvianolic acid B (771), 3-epi-corosolic acid (779), 2α,3α-23-trihydroxyurs-12-en-28-oic acid (780), oleanolic acid 3-O-ferulate(781), caffeic acid methyl ester (772) and vanillic acid (755) exhibited more potent inhibitory effect. Methyl rosemarinate (767), rosemarinic acid (768) and caffeic acid methyl ester (772) exhibited stronger antioxidative activities than α-tocopherol (IC50=21.33 μM). Moreover, These isolated compounds showed stronger inhibitoy activities on BChE rather than AChE, and taxodione (503) was with IC50 value of 2.88 μM. On the other hand, we also studied the synthesis of melodamide A (783) and its derivatives (837-852).
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