Inhibition of growth and induction of apoptosis in A549 cells by compounds from oxheart cabbage extract.

BACKGROUND: Oxheart cabbage (Brassica oleracea var. capitata) is a member of the Brassica genus. Although some studies on the anticancer effects of extracts from oxheart cabbage have been reported, comprehensive information on the bioactive fractions and components from oxheart cabbage extracts is still lacking. The aim of this study was to isolate and identify the bioactive fractions and components from oxheart cabbage seeds using activity-guided isolation methods. RESULTS: The cytotoxicity and apoptotic effects of fraction II, fraction III, iberverin, sulforaphane and iberin from oxheart cabbage seed extract were investigated. The results showed that all five components had inhibitory effects on the in vitro growth of A549 cells which were dose-dependent. These compounds also changed the morphology of A549 cells, and their inhibitory activity on A549 cells was as follows: sulforaphane > iberin > iberverin > fraction III > fraction II. The IC50 values were 3.53 ± 0.63, 4.93 ± 1.02, 7.07 ± 0.51, 15.56 ± 0.24 and 27.32 ± 0.63 µg mL(-1) respectively. Fraction II, fraction III, iberverin, sulforaphane and iberin induced cell apoptosis by increasing early apoptosis and late apoptosis/necrosis, and activation of caspase-3, -8 and -9. CONCLUSION: These results indicated that the decrease in A549 cell viability by active compounds from oxheart cabbage seed extract was due to the induction of apoptosis. © 2015 Society of Chemical Industry.

Mitochondria-mediated apoptosis in human lung cancer A549 cells by 4-methylsulfinyl-3-butenyl isothiocyanate from radish seeds.

4-Methylsulfinyl-3-butenyl isothiocyanate (MTBITC) found in the radish (Raphanus sativus L.), is a well- known anticancer agent. In this study, the mechanisms of the MTBITC induction of cell apoptosis in human A549 lung cancer cells were investigated. Our PI staining results showed that MTBITC treatment significantly increased the apoptotic sub-G1 fraction in a dose-dependent manner. The mechanism of apoptosis induced by MTBITC was investigated by testing the change of mitochondrial membrane potential (Δψm), the expression of mRNAs of apoptosis-related genes by RT-PCR, and the activities of caspase-3 and -9 by caspase colorimetric assay. MTBITC treatment decreased mitochondrial membrane potential by down-regulating the rate of Bcl-2/ Bax and Bcl-xL/Bax, and activation of caspase-3 and -9. Therefore, mitochondrial pathway and Bcl-2 gene family could be involved in the mechanisms of A549 cell apoptosis induced by MTBITC.

A new lignan with anti-tumour activity from Polygonum perfoliatum L.

The methanol extract of the tubers of Polygonum perfoliatum L. afforded a new lignan: 8-oxo-pinoresinol (1), and five known compounds 3',5-dihydroxy-3,4',5',7-tetramethoxy-flavone (2), catechin (3), quercetin (4), quercetin-3-O-ß-D-glucuronide (5) and rutin (6). Their structures were established by MS, one- and two-dimensional NMR experiments. Compound 1 showed cytotoxicity against human mammary carcinoma (Bcap-37), human colon carcinoma (RKO), human hepatocellular carcinoma (SMMC-7721), human prostate carcinoma (PC3) and human erythroleukaemia (K562) cells.

[A novel C27-steroidal glycoside sulfate from Liriope graminifolia].

An unusual novel C27-steroidal glycoside sulfate was isolated from the underground organs of Liriope graminifolia (Linn.) Baker with three known compounds. Their chemical structures were determined by spectral analysis, including HR-MS, 1D and 2D NMR as (25S)-ruscogenin 1-sulfate-3-O-alpha-L-rhamnopyranoside (1), (25S)-ruscogenin 1-O-beta-D-xylopyranosyl-3-O-alpha-L-rhamnopyranoside (2), hesperidin (3), and 4', 7-dihydroxy-5-methoxyflavanone (4). Compound 1 has cytotoxic activities against K562 and HL60 cells with IC50 values of 18.6 microg x mL(-1) and 16.5 microg x mL(-1), respectively.

A new rearranged abietane diterpenoid from Clerodendrum kaichianum Hsu.

A new abietane diterpenoid, (3S,16R)-12,16-epoxy-3,6,11,14,17-pentahydroxy-17(15 â†’ 16)-abeo-5,8,11,13-abietatetraen-7-one (1), was isolated from the stems of Clerodendrum kaichianum Hsu, together with four known diterpenoids. The structures of the isolated compounds were assigned on the basis of their NMR spectra including 2D NMR techniques such as COSY, HMQC, and HMBC experiments, and were compared with those of the literature data. This new compound showed significant cytotoxicity against the HL-60 and A-549 tumor cell lines.

Bioactive diterpenes from Clerodendrum kaichianum.

Bioassay-guided isolation studies of the extract of Clerodendrum kaichianum Hsu., a new rearranged abietane diterpene and five known diterpene compounds were isolated by various chromatography methods. Their structures were identified by means of spectroscopic methods, including 1D- and 2D-NMR spectroscopy, as (16R)-12,16-epoxy-11,14,17-trihydroxy-17(15-->16)-abeo-8,11,13-abietatrien-7-one (1), villosin A (2), salvinolone (3), 14-deoxyloleon U (4), 5,6-dehydrosugiol (5), and coleon U (6). Compounds 1, 2, 3, and 5 are reported for the first time for this genus. Compounds 1, 2, and 6 demonstrated potent cytotoxic activities against the HL-60 tumor cell line.

Rapid separation and characterization of active flavonolignans of Silybum marianum by ultra-performance liquid chromatography coupled with electrospray tandem mass spectrometry.

Ultra-performance liquid chromatography (UPLC) interfaced with the electrospray ionization (ESI) tandem mass spectrometer (MS(n)) was developed for the simultaneous determination of silychristins A (1) and B (2), silydianin (3), silybins A (4) and B (5), and isosilybins A (6) and B (7), major bioactive flavonolignans in silymarin, a herbal remedy derived from the milk thistle Silybum marianum. In this study, the seven major active flavonolignans including the diastereomers 1/2, 4/5, and 6/7 were completely separated using UPLC with an ACQUITY UPLC C(18) column and a MeOH/water/formic acid mobile phase system. The collision-induced dissociation (CID) MS(n) spectra of these flavonolignans were studied systematically using ESI-MS. The results with the present methodology show that UPLC-MS(n) can be useful for general screening of active natural products from plant extracts and for the specific quality control of silymarin.

A new biflavonoid from Daphniphyllum angustifolium Hutch.

An investigation of the flavonoids in Daphniphyllum angustifolium Hutch. resulted in the identification of a new biflavonoid, 5,7,4'-trihydroxyflavan (2alpha-->O-->7, 4alpha-->8) kaempferol (1), together with five known flavonoids. Their structures were determined by spectroscopic method.

[Study on triterpenes of Microtropis tiflora].

OBJECTIVE: To study the chemical constituents of Microtropis triflora. METHOD: The compounds were isolated by chromatography on silica gel and Sephadex LH-20. There structures were elucidatedby by chemical methods and spectral analysis. RESULT: Five triterpenoids were isolated and elucidated as friedelin (1), 3-oxo-28-friedelanoic acid (2), 29-hydroxy-3-friedelanone (3), salaspermic acid (4), orthosphenic acid (5). CONCLUSION: Compounds 1-5 are all isolated from M. triflora for the first time.