ABSTRACT
Four prenylated flavonoids compounds 1-4, named sinopodophyllines A-D, and a flavonoid glycoside (compound 13), sinopodophylliside A, together with 19 known compounds (compounds 5-12 and 14-24) were isolated from the fruits of Sinopodophyllum hexandrum. The structures of new compounds were elucidated by extensive spectroscopic analysis, including HRESIMS, 1D and 2D NMR. Compounds 1-6, 9-11, and 14-17 were tested for their cytotoxicity against human breast-cancer T47D, MCF-7 and MDA-MB-231 cells in vitro, and compounds 2, 5, 6, 10 and 11 showed significant cytotoxicity (IC50 values < 10 µmol·L-1) against T47D cells.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Berberidaceae/chemistry , Breast Neoplasms/drug therapy , Flavonoids/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Breast Neoplasms/physiopathology , Cell Line, Tumor , Cell Proliferation/drug effects , Flavonoids/chemistry , Flavonoids/isolation & purification , Fruit/chemistry , Humans , Molecular StructureABSTRACT
Constituents of the fruit of Sinopodophyllum hexandrum (Royle) Ying (Sinopodophylli Fructus) were investigated. A new flavonoid, 8,2'-diprenylquercetin 3-methyl ether along with 9 known compounds were isolated and identified. Among them, the new compound 8,2'-diprenylquercetin 3-methyl ether exhibited cytotoxic activities against MDA-231 and T47D breast cancer cell lines, quercetin, kaempferol and rutin were isolated from Sinopodophylli Fructus for the first time.
Subject(s)
Antineoplastic Agents, Phytogenic/therapeutic use , Berberidaceae/chemistry , Breast Neoplasms/drug therapy , Phytotherapy , Plant Extracts/therapeutic use , Quercetin/analogs & derivatives , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Female , Flavonoids/isolation & purification , Flavonoids/pharmacology , Flavonoids/therapeutic use , Fruit , Humans , Kaempferols/isolation & purification , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Quercetin/isolation & purification , Quercetin/pharmacology , Quercetin/therapeutic use , Rutin/isolation & purificationABSTRACT
OBJECTIVE: To detect the Immune regulating activity of ethaselen-1 (Eb1), a novel organoselenium compound, in C57/BL mice transplanted with Lewis lung cancer(LLC). METHODS: The LLC transplanted C57/BL mice models were established, and the mice was randomly divided into four groups, including high dose Eb1 group (25.0 mg/kg),low dose Eb1 group (12.5 mg/kg), positive control group (levamisole, LMS, 2.0 mg/kg) and negative control group(solvent). Intraperitoneal injections (ip.) of the four pharmaceuticals were performed once a day through the abdominal wall separately, from the second to the eighth day after cancer was transplanted. On the eleventh day, six mice of each group were killed and relative weight of spleen, transforming activity of spleen lymphocytes, NK cell activity, LAK cell activity and percentage of CD4(+)CD8(+)T lymphocyte were detect. RESULTS: Compared with the control group, high dose Eb1 could obviously increase the relative weight of spleen (150.59% and 122.55%), transforming activity of spleen lymphocytes(162.25% and 561.98%), NK cell activity(78.60% and 219.42%) and percentage of CD4(-)/CD8(+) T lymphocyte(104.72% and 105.87%) in normal mice and LLC mice. Compared with the control group, high dose Eb1 could also increase LAK cell activity of LLC mice by 195.11%. CONCLUSION: The novel organoselenium compound Eb1 has immune regulating activity in vivo.
Subject(s)
Adjuvants, Immunologic/pharmacology , Carcinoma, Lewis Lung/immunology , Killer Cells, Natural/drug effects , Organoselenium Compounds/pharmacology , Animals , CD4-CD8 Ratio , Carcinoma, Lewis Lung/pathology , Cell Line, Tumor , Killer Cells, Lymphokine-Activated/drug effects , Killer Cells, Lymphokine-Activated/immunology , Killer Cells, Natural/immunology , Male , Mice , Mice, Inbred C57BL , Neoplasm TransplantationABSTRACT
OBJECTIVE: To detect the antitumor activity of Shuang-Xi-Zuo-Wan-1(Eb), a novel organoselenium compound, in C57/BL mice transplanted with Lewis lung cancer(LLC). METHODS: The LLC transplanted C57/BL mice model was established,and the mice were randomly divided into four groups, including high dose Eb group (25.0 mg/kg), low dose Eb group (12.5 mg/kg), positive control group (DDP, 2.0 mg/kg) and negative control group (solvent). Each group had twelve mice. Intraperitoneal injections (ip.) of four pharmaceuticals were performed once a day through the abdominal wall separately, from the second to the eighth days after cancer was transplanted. On the eleventh day, six mice of each group were killed and the influences of Eb on growth speed, size, weight, invasion, inhibitory rate, proliferation index and apoptosis rate of LLC were observed and calculated. The remaining mice were fed till all of them died naturally and the average survival time of each group was calculated. RESULTS: Eb could inhibit the growth and infiltration of LLC (the cancer inhibitory rate of high does Eb was 80.31%) obviously and prolong the average survival time of these with mice cancer. After being given Eb, the nuclear of the cancer cell concentrated and the fission phase cells reduced. In addition,the number of apoptosis cancer cells increased. CONCLUSION: The novel organoselenium compound Eb has antitumor activity in vivo. It can inhibit the growth and infiltration of LLC in mice, and induce the apoptosis of cancer cells.