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.

Novel steroidal saponins from Liriope graminifolia (Linn.) Baker with anti-tumor activities.

Phytochemical investigation of the underground parts of Liriope graminifolia (Linn.) Baker resulted in the isolation of two new steroidal saponins lirigramosides A (1) and B (2) along with four known compounds. The structures were determined by extensive spectral analysis, including two-dimensional (2D) NMR spectroscopy and chemical methods, to be 3-O-[ß-d-xylopyranosyl-(1→3)-α-l-arabinopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→4)]-ß-d-glucopyranosyl-(25S)-spirost-5-ene-3ß,17α-diol (1), 1-O-[α-l-rhamnopyranosyl-(1→2)-ß-d-xylopyranosyl]-(25R)-ruscogenin (2), 1-O-ß-d-xylopyranosyl-3-O-α-l-rhamnopyranosyl-(25S)-ruscogenin (3), 3-O-α-l-rhamnopyranosyl-1-O-sulfo-(25S)-ruscogenin (4), methylophiopogonanone B (5), and 5,7-dihydroxy-3-(4-methoxybenzyl)-6-methyl-chroman-4-one, (ophiopogonanone B, 6), respectively. Compound 1 has a new (25S)-spirost-5-ene-3ß,17α-diol ((25S)-pennogenin) aglycone moiety. The isolated compounds were evaluated for their cytotoxic activities against Hela and SMMC-7721 cells.

[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.