ABSTRACT
Apiaceae are a family of medicinal plants widely used in traditional medicine. The apoptotic activities of seven ethanol extracts from fruits of seven species of Apiaceae, Eryngium planum, Archangelica officinalis, Pastinaca sativa, Heracleum sibiricum, Carum carvi, Foeniculum vulgare, Levisticum officinale against ML-1--human acute myeloblastic leukaemia, J-45.01--human acute T cell leukaemia, EOL--human eosinophilic leukaemia, HL-60--human Caucasian promyelocytic leukaemia, 1301--human T cell leukaemia lymphoblast, C-8166--human T cell leukaemia, U-266B1--human myeloma, WICL--human Caucasian normal B cell, and H-9--human T cell, were investigated.
Subject(s)
Apiaceae/chemistry , Apoptosis/drug effects , Leukemia/drug therapy , Phytotherapy , Plant Extracts/pharmacology , Cell Line , Cell Line, Tumor , Cell Survival/drug effects , Fruit , Humans , Plant Extracts/isolation & purificationABSTRACT
INTRODUCTION: The chemical and pharmaceutical studies carried out on species from Polygonum L. genus showed biological activity both of the extracts and the components isolated from them. These results were the impulse to examine Polygonum amphibium L. OBJECTIVE: The aim of this study was the isolation of active components from methanol extract and the determination of their cytotoxic effect on human leukaemic cell lines. METHODOLOGY: Three flavonoid components from butanol soluble fractions of methanol extract by CC and PC preparative chromatography were isolated. Their structures were established on the basis of 1H, 13C and correlation (DEPT, H-H, COSY, HMQC, HMBC) NMR, UV and FAB-MS spectroscopic techniques. The evaluation of the anti-leukaemic activities of 1 and 2 against Jurkat and HL60 cell lines was carried out in vitro using annexin V fluorescence assay. RESULTS: Two new flavonoid glucuronides, quercetin-3-O-beta-glucuronide (1) and quercetin-3-O-alpha-rhamnosyl-(1 --> 2)-beta-glucuronide (2), and kaempferol-3-O-alpha-rhamnosyl-(1 --> 2)-beta-glucuronide (3), were isolated from Polygonum amphibium L. It was demonstrated that the glucuronides of quercetin are able to induce apoptosis in the tested human leukaemic cells. These compounds penetrate through cytoplasm to the cellular nucleus of the cultured cells, and give intensive apoptotic responses in the stimulated leukaemic cells. The number of apoptotic cells increased with the concentration (1 nm to 10 microm) of 1 or 2 and periods of exposure (1-3 days). CONCLUSION: Compounds 1 and 2 may be considered good candidates for leukaemia chemotherapeutic agents.
Subject(s)
Antineoplastic Agents/isolation & purification , Antineoplastic Agents/pharmacology , Flavonoids/isolation & purification , Flavonoids/pharmacology , Glucuronides/isolation & purification , Glucuronides/pharmacology , Leukemia/drug therapy , Phytotherapy , Polygonum/chemistry , Apoptosis/drug effects , HL-60 Cells , Humans , Jurkat Cells , Kaempferols/isolation & purification , Kaempferols/pharmacology , Methanol/chemistry , Quercetin/analogs & derivatives , Quercetin/isolation & purification , Quercetin/pharmacologyABSTRACT
The influence of an ethyl acetate extract from Polygonum amphibium L. and quercetin-3-methyl ether isolated from them were examined on the human immune system. The investigations were made on peripheral blood mononuclear cells from healthy donors. The cells were stimulated by plant extract and quercetin-3-methyl ether in 24 h culture and analysed inflow cytometry. The following mice monoclonal antibody anti human activate markers were used: anti HLA-DR PE, anti CD25 FITC, anti CD69 FITC and anti CD71 FITC. The level of Interleukine-2 in blood serum and in culture supernatants was measured by ELISA method. Ethyl acetate extract from Polygonum amphibium caused the rise in the number of CD25 and HLA-DR positive lymphocytes and increased the expression of CD25 and CD71 antigens. The level of IL-2 was increasing for the duration of the culture, independently from the presence of stimulators. Besides quercetin-3-methyl ether, from herb of Polygonum amphibium L., trans-taxifolin, quercetin and kaempferol were isolated The structure of the isolated compounds was determined by spectroscopic (UV, (1)H NMR, (13)C NMR and CI-MS) methods.
Subject(s)
Adjuvants, Immunologic/pharmacology , Lymphocytes/drug effects , Phytotherapy , Polygonum , Quercetin/pharmacology , Adjuvants, Immunologic/administration & dosage , Adjuvants, Immunologic/therapeutic use , Animals , Antibodies, Monoclonal , Antigens, CD/immunology , Cells, Cultured , Enzyme-Linked Immunosorbent Assay , Flow Cytometry , Humans , Interleukin-2/blood , Interleukin-2/metabolism , Leukocytes, Mononuclear/drug effects , Leukocytes, Mononuclear/immunology , Lymphocytes/immunology , Mice , Plant Extracts/administration & dosage , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Quercetin/administration & dosage , Quercetin/analogs & derivatives , Quercetin/therapeutic useABSTRACT
The interferon inducing abilities of eleven ethanolic extracts obtained from nine taxons of Polygonum L. genus, were tested in the cell culture of monkey kidney. The extracts from the herb of Polygonum amphibium L. and the rhizome and fruit of Polygonum bistorta L. induced a substance showing an interferon-like activity. Biological activity studies showed that the protective titre (the highest dilution which protected cells by 50% against virus infection) of the interferon-like materials was 1:10-1:15.
