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OBJECTIVE@#To investigate the anti-leukemia effect of total saponins of Rubus parvifolius L. (TSRP) on K562 cell xenografts in nude mice and the mechanisms of action.@*METHODS@#The K562 cell xenografts in nude mice were established, and then randomly divided into 5 groups, the control group, the cytosine arabinoside group(Ara-c) and 3 TSRP groups (20, 40 and 100 mg/kg). The tumor volume and mass of each group of nude mice were measured and the anti-tumor rates of TSRP were calculated subsequently. The apoptosis status of tumor cells was detected by hematoxylin-eosin (HE) and terminal dexynucleotidyl transferase (TdT)-mediated dUTP nick end labeling (TUNEL) staining analysis. Finally, the activities of apoptosis related signaling of signal transducer and activator of transcription 3 (STAT3), eukaryotic initiation factor 4E (eIF4E) and B-cell lymphoma-2 (bcl-2) were determined with immunohistochemistry tests.@*RESULTS@#Subcutaneous injection of K562 cells induced tumor formation in nude mice, and the TSRP treated group showed a signifificant inhibitory effect on tumor formation. The nude mice treated with TSRP showed a signifificant decrease in tumor growth rate and tumor weight in comparison to the control group (all P<0.05). The HE staining and TUNEL assay showed that TSRP induced cell death by apoptosis. The immunohistochemical assay showed down-regulation of the bcl-2 gene in the TSRP treated cells. The phosphorylation levels of eIF4E and STAT3 were decreased obviously after the treatment of TSRP.@*CONCLUSION@#TSRP had an excellent tumor-suppressing effect on K562 cells in the nude mice xenograft model, suggesting that TSPR can be developed as a promising anti-chronic myeloide leukemia drug.
Subject(s)
Animals , Humans , Male , Mice , Apoptosis , Eukaryotic Initiation Factor-4E , Physiology , K562 Cells , Leukemia , Drug Therapy , Pathology , Rubus , Chemistry , STAT3 Transcription Factor , Physiology , Saponins , Pharmacology , Signal Transduction , Xenograft Model Antitumor AssaysABSTRACT
Objective: To study the chemical constituents from the roots of Rubus parvifolius. Methods: The chemical constituents were extracted and purified by silica gel column chromatography. NMR spectra were used for structural identification. Results: Phytochemical study on the roots of R. parvifolius led to the isolation of one ceramide (1), two anthraquinones ( 2 and 3), four triterpenoids (4-7), two flavonoids (8 and 9), one fatty acid ester (10), and two sterols (11 and 12). Conclusion: Compound 1 is isolated from the plants of family Rosaceae for the first time, and compounds 2-5 are isolated from genus Rubus for the first time. Though R. parvifolius shares the same major chemical types (triterpenoid, flavonoid, and anthraquinone) with those of R. alceaefolius, a substituent of R. parvifolius, their individual constituents are different. In addition, R. parvifolius contains ceramide (1) with high concentration, while caffeoylquinic acid reported in R. alceaefolius has not been found in R. parvifolius. Furthermore, the results from our phytochemical study are consistent with the DNA phylogenic relationship between R. parvifolius and R. alceaefolius (two separated subgenera), suggesting that the substitution of the former species with the latter one in folk medicine might not be suitable.
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OBJECTIVE: To study the chemical constituents from the roots of Rubus parvifolius. METHODS: Various chromatographic techniques such as silica gel, Sephadex LH-20, and prep-HPLC column chromatography were used. RESULTS: Nineteen compounds, including 12 triterpenoids were isolated from the roots of Rubus parvifolius. Based on the analysis of their spectroscopic data, the structures of these 19 compounds were identified as p-hydroxybenzoic acid(1), 4-hydroxy-3, 5-dimethoxybenzoic acid(2), 3-methoxy-4-hydroxybenzoic acid(3), β-sitosterol(4), oleanolic acid(5), ursolic acid(6), 2-oxopomolic acid(7), pomolic acid(8), p-hydroxyphenylethyl alcohol(9), psiguanin A(10), 2α-hydroxyursolic acid(11), tormentic acid(12), 2α, 3α, 19α, 23-tetrahydroxyurs-12-en-28-oic acid(13), L-epicatechin(14), 2α, 3α, 19α, 24- tetrahydroxyolean-12-en-28-oic acid(15), 2α, 3α, 19α, 24-tetrahydroxyurs-12-en-28-oic acid(16), 2α, 3β, 19α-trihydroxyolean-12-en-23, 28-dioic acid(17), suavissimoside R1(18), and daucosterol(19), respectively. CONCLUSION: Compounds 1-3, 5, 7-10, 12, and 15-17 are isolated from the roots of R. parvifolius for the first time. Compounds 7 and 9 are isolated from the genus Rubus L. for the first time. Compounds 10 and 15-17 are isolated from the family Rosaceae for the first time.
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Two new oleanane-type triterpenoids, parvifolactone A (1) and rubuside P (2), together with 11 known triterpenoids, fupenzic acid (3), 18,19-seco,2α,3α-dihydroxyl-19-oxo-urs-11,13(18)-dien-28-oic acid (4), euscaphic acid (5), maslinic acid (6), 1β- hydroxyeuscaphic acid (7), 2α,3α,19α,23-tetrahydroxyolean-12-en-28-oic acid (8), 2α,3β,19α,23-tetrahydroxyurs-12-en-28-oic acid (9), glucosyl pinfaensate (10), rubuside J (11), 2α,3α,19α,23-tetrahydroxyurs-12-en-24,28-dioic acid (12), and 2α,3β,19α- trihydroxyurs-12-en-23,28-dioic acid (13), were isolated from the roots of Rubus parvifolius.
Subject(s)
Molecular Structure , Plant Extracts , Chemistry , Plant Roots , Chemistry , Rubus , Chemistry , Terpenes , ChemistryABSTRACT
Several 19alpha-hydroxyursane-type triterpenoids and hydrolysable tannins have beneficial effects on human health. Rubus crataegifolius (Rosaceae) has the cleft simple leaf whereas R. parvifolius has pinnate compound leaves. This research was aimed to find the variation in the contents of the triterpenoids and tannins between the infected versus uninfected leaves of R. coreanus and R. parvifolius and between young versus mature leaves. Triterpenoids and tannins were quantitatively analyzed by HPLC. Six triterpenoids including tormentic acid, euscaphic acid, 23-hydroxytormentic acid, coreanoside F1, kaji-ichigoside F1 and niga-ichigoside F1 were used for standard compounds. Gallotannins and ellagitannins were quantitatively evaluated using the indicatives of methyl gallate and ellagic acid. The infected leaves of R. crataegifolius contained higher levels of triterpenoids and tannin than the uninfected leaves; however, lower quantity of total tannin was observed in the mature leaves than in the young leaves. Although the pinnate compound leaves of R. parvifolius exhibited similar tendency of those compositional variation with R. crataegifolius each other, its contents of triterpenoids do not considerably vary. Variation of the contents of triterpenoids and tannins were particularly distinct in R. crataegifolius by growth and infection.
Subject(s)
Humans , Chromatography, High Pressure Liquid , Ellagic Acid , Hydrolyzable Tannins , Rosaceae , TanninsABSTRACT
Objective; To establish a method for content determination of total saponins in Rubus parvifolius L.. Methods; Total saponins was determined by UV - VIS spectrophotometry after different extracts of the sample had been coloured. Results; The method was linear in the range of 22-176?g (r = 0.9997),and the average recovery was 102. 1 % , RSDwas 2. 82% (n = 6). The content of total saponins was highest by the method of 70% ethanol reflux. Conclusion; The sample is stable after coloured. The method is sensitive and reliable , which may be used for the quality control of Rubus parvifolius L. .
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Aim To study the effect of the total saponins of Rubus parvifolius(TSRP)on the intracellular free calcium levels in ischemic hippocampus neurons.Methods The cytosolic free calcium concentration in ischemic hippocampal neurons was measured by using Ca2+-sensitive fluorescent probe fluo-2/AM with a laser scanning confocal microscope.Results Application of TSRP inhibited free intracellular calcium in ischemic hippocampus neurons in a concentration-dependent manner.Conclusions These results suggest that TSRP might protect hippocampus neurons via attenuating calcium overload induced by ischemia.
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Objective: To study the technological parameters of the purification process of total saponins of Rubus parvifolius L. with macroreticular resin. Methods: The adsorptive characteristics and elutive parameters of the process were studied by taking the elutive and purified ratio of total saponins of Rubus parvifolius L. as marker. Results: 19.3mL of the extractive of total saponins of Rubus parvifolius L. was purified with a column of macroreticular resin (R1cm?H20cm,dried weight 2.68g) and was washed with 100mL of distilled water, then was eluted with 100mL of 50% ethanol. Conclusion: With macroreticular resin to adsorb and purify, the elutive ratio of total saponins of Rubus parvifolius L. was over 79.2% and the purity reached 55.3%. So this process of applying macroreticular resin to adsorb and purify total saponins of Rubus parvifolius L. is feasible.