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BACKGROUND@#Cisplatin acquired resistance is a vital problem in the chemotherapy of non-small cell lung cancer, which needs to be further addressed. In recent years, obtaining drug resistant cells from cell cultivation and serving for metabolomics research to find differential metabolites and get potential biomarkers, is a good reference for clinical research and cancer treatment. This study aimed to obtain metabolite information related to cisplatin resistance through metabolomics analysis.@*METHODS@#Metabolites were extracted from A549 cells and cisplatin resistant A549/DDP cells, and ultraperformance liquid chromatography coupled with time of flight mass spectrometry was used to perform metabolomic analysis of endogenous molecules of the two cells and obtain metabolic differences.@*RESULTS@#Through data analysis, 40 metabolites were identified as differential metabolites, mainly involving phospholipids, fatty acids, amino acids and metabolites related to energy metabolism.@*CONCLUSIONS@#The drug resistance of A549/DDP cells may be caused by the changes of cell membrane structure and related metabolic pathways.
Subject(s)
Humans , A549 Cells , Carcinoma, Non-Small-Cell Lung , Pathology , Chromatography, High Pressure Liquid , Drug Resistance, Neoplasm , Lung Neoplasms , Pathology , Mass Spectrometry , Metabolomics , MethodsABSTRACT
Objective:To study the chemical constituents in the roots of Tripterygium wilfordii. Methods: The compounds from Tripterygium wilfordii were isolated and purified by silica gel, Sephadex LH-20 and prep-HPLC chromatography, and their structures were elucidated based on the physiochemical properties and spectroscopic analysis. Results:Twelve compounds were isolated and iden-tified as wilforgine(1),wilforine(2),triptonoterpene methyl ether(3),glut-5-en-3β,28-diol(4),wilforol E(5),triptobenzene L (6),maytenoic acid(7),triptophenolide(8),celastrol(9),demethylzeylasteral(10),1-desacetyl wilforgine(11) and wilfortrine (12). Conclusion:The 1D and 2D NMR data of 1 and 2 are assigned for the first time,and the absolute configurations of 1 are con-firmed by X-ray single crystal diffraction.
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Objective:To study the metabolism of pedunculoside treated with rat intestinal bacteria in vitro. Methods:Pedunculo-side and rat intestinal bacteria were incubated in vitro for 0, 4, 8, 24 and 48 hours under anaerobic condition. After extracted repeat-edly by ethyl acetate, the metabolites in the incubation media were qualitatively and quantitatively analyzed by HPLC. Results:Totally 90. 8% of pedunculoside was transformed to M2 after incubated with rat intestinal bacteria in vitro for 48 hours, and a detailed compari-son of HPLC profiles between M2 and rotundic acid showed M2 was rotundic acid. Conclusion: Pedunculoside can be metabolized to rotundic acid by rat intestinal bacteria in vitro.
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The aim of this study is to investigate the protection effect of tanshinone IIA (Tan) against triptolide (TP)-induced liver injury and the mechanisms involved. Acute liver injury was induced by intraperitoneal injection of TP (1 mg x kg(-1)) in mice. The activities of AST, ALT and LDH in serum and the levels of GSH, GST, GSH-PX, SOD, CAT and MDA in liver tissue were detected. The histopathological changes of liver tissues were observed after HE staining. Nrf2 translocation in liver tissue was detected by Western blotting, and real-time PCR was used to measure the expression levels of GCLC, NQO1 and HO-1 mRNA. The results showed that pretreatment with Tan significantly prevented the TP induced liver injury as indicated by reducing the activities of AST, ALT and LDH (P < 0.01). Tan pretreatment also prevented TP-induced oxidative stress in the mice liver by inhibiting MDA and restoring the levels of GSH, GST, SOD and CAT (P < 0.05). Parallel to these changes, pretreatment with Tan could attenuate histopathologic changes induced by TP. Furthermore, the results indicated that Tan pretreatment caused nuclear accumulation of Nrf2 as well as induction of mRNA expression of antioxidant response element (ARE)-driven genes such as GCLC, NQO1 and HO-1. These results indicated that Tan could protect against TP-induced acute liver injury via the activation of Nrf2/ARE pathway.
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A new triterpenoid saponin and fourteen known triterpenoids were isolated from the methanol extract of the stems and leaves of Callicarpa integerrima Champ, which is used in Chinese folk medicine for stopping bleeding, expelling the wind, dissipating stagnation, and treating scrofula, by using various chromatographies, such as silica gel, Sephadex LH-20 and RP-C18 column chromatography. Their structures were identified as a new compound 2alpha, 3beta, 19alpha, 23-tetrahydroxy-olean-12-en-28-oic acid-28-O-beta-D-glucopyranosyl-(1 --> 4)-beta-D-glucopyranoside (1), together with fourteen known compounds: oleanolic acid (2), 3-acetyl oleanolic acid (3), 3beta-O-acetyl ursolic acid (4), 2alpha-hydroxy-ursolic acid (5), 2alpha, 3beta, 19alpha, 23-tetrahydroxy-urs-12-en-28-oic acid (6), alpha-amyrin-3-O-beta-D-glucopyranoside (7), pomolic acid (8), betulinic acid (9), ursolic acid (10), 2alpha, 3beta, 19alpha, 23-tetrahydroxy-olean-12-en-28-oic acid (arjungenin) (11), 2alpha-hydroxy-oleanolic acid (12), hederagenin (13), 2alpha, 19alpha-dihydroxy-ursolic acid (14) and pruvuloside A (15), by the spectroscopic techniques of NMR, HMBC, IR and MS, separately. All these compounds were obtained from this plant for the first time, and compounds 3, 4 and 15 were isolated from genus Callicarpa L. for the first time.
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The study is to develop an HPLC method for simultaneous determination of rhamnazin (1), rhamnocitrin (2), rhamnetin (3), rhamnazin-3-O-beta-D-glucopyranoside (4), rhamnazin-3-O-beta-D-xylopyranosyl-(1-->4)-beta-D-glucopyranoside (5), rhamnazin-3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-glucopyranoside (6), and rhamnocitrin-3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-glucopyranoside (7) in Nervilia fordii. The separation was performed on a Kromasil C18 column (250 mm x 4.6 mm, 5 microm) with 0.4% phosphoric acid-acetonitrile as the mobile phase in a gradient elution at a flow rate of 1.0 mL x min(-1). The detect wavelength was set at 256 nm, and the column temperature was set at 40 degrees C. There were good linear relationships between the logarithm values of concentrations and those of the peak areas of seven flavonoids (1-7) in the range of 0.55-70.00 microg x mL(-1) (r = 0.9997), 0.86-110.00 microg x mL(-1) (r = 0.9997), 0.39-50.00 microg x mL(-1) (r = 0.999 7), 0.55-70.00 microg x mL(-1) (r = 0.999 5), 1.33-170.00 microg x mL(-1) (r = 0.9998), 1.33-170.00 microg x mL(-1) (r = 0.9998), 0.16-20.00 microg x mL(-1) (r = 0.9995), respectively. The recoveries of the seven flavonoids were between 97.19%-99.45%, the relative standard deviations (RSDs) were between 0.91%-2.69%. The established method is rapid, accurate with high repeatability, which could provide scientific evidence for the quality control of Nervilia fordii.
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Objective To study the chemical constituents of Abacopteris penangiana.Methods The compounds were separated and purified by various chromatographic techniques and their structures were elucidated on the basis of physiochemical properties and spectroscopic methods.Results Seven compounds were purified and their structures were identified as:(7'Z)-3-O-(3,4-dihydroxy phenylethenyl)-caffeic acid(1),caffeiein B(2),matteucinol(3),protocatechuic acid(4),p-methoxybenzoic acid(5),β-sitosterol(6),and daucosterol(7).Conclusion Compound 1 is a new phenolic acid compound named abacopteric acid,and the other compounds are isolated from the plant for the first time.
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Objective To study the stilbene constituents from the traditional Chinese medicine Smilax china and to determine their antioxidant activity. Methods The compounds were separated and purified by column chromatography with silica gel, RP C18, and Sephadex LH- 20, and were identified by IR, MS, NMR. DPPH method was used to evaluate the free radical scavenging activity of the isolated compounds. Results Three compounds were isolated from the EtOAc fraction of the rhizomes of S. china and were identified as: resveratrol (1), oxyresveratrol (2) and 3, 5, 3′ , 4′ - tetrahydroxylstilbene (3). Compounds 1～ 3 showed strong antioxidant activity, and could scavenge DPPH free radicals, effectively. At the concentration of 50 ? mol/L, their DPPH free radical scavenging rates were 79.47 % , 89.89 % and 93.86 % , respectively. Conclusion Stilbenes might be the material foundation of antioxidant activities of rhizomes of S. china.
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AIM: To study the enrichment-purification process of total triterpeniods from Rabdosia lophanthoides var.gerardianus with macro porous resin. METHODS: The purify of the total triterpeniods was used as marker to optimize the adsorptive capacity and elution characteristics. RESULTS: The result showed that 20 mL of the extraction solution(0.5 g/mL) was purified with a column of macro porous resin(d15 mm?h120 mm,V=20 mL,dried weight 10 g) and washed with distilled water,then eluted with 80 mL 60% ethanol and 160 mL 90% ethanol in proper order.With macro reticular resin to adsorb and purify,the elution ratio of total triterpeniods of 90% ethanol fraction was 93.2% and the purity reached above 20%. CONCLUSION: This process of applying macro reticular resin to adsorbing and purifying total triterpeniods from Herba Rabdosia lophanthoides var.gerardianus was successful.