Ent-11α-Hydroxy-15-oxo-kaur-16-en-19-oic-acid Inhibits Growth of Human Lung Cancer A549 Cells by Arresting Cell Cycle and Triggering Apoptosis.

OBJECTIVE: To examine the apoptotic effect of ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F), a compound isolated from Pteris semipinnata L (PsL), in human lung cancer A549 cells. METHODS: A549 cells were treated with 5F (0-80 µg/ml) for different time periods. Cytotoxicity was examined using a MTT method. Cell cycle was examined using propidium iodide staining. Apoptosis was examined using Hoechst 33258 staining, enzyme-linked immunosorbent assay (ELISA) and caspase-3 activity analysis. Expression of representative apoptosis-related proteins was evaluated by Western blot analysis. Reactive oxygen species (ROS) level was measured using standard protocols. Potential interaction of 5F with cisplatin was also examined. RESULTS: 5F inhibited the proliferation of A549 cells in a concentration- and time-dependent manner. 5F increased the accumulation of cells in sub-G1 phase and arrested the cells in the G2 phase. Exposure to 5F induced morphological changes and DNA fragmentation that are characteristic of apoptosis. The expression of p21 was increased. 5F exposure also increased Bax expression, release of cytochrome c and apoptosis inducing factor (AIF), and activation of caspase-3. 5F significantly sensitized the cells to cisplatin toxicity. Interestingly, treatment with 5F did not increase ROS, but reduced ROS production induced by cisplatin. CONCLUSION: 5F could inhibit the proliferation of A549 cells by arresting the cells in G2 phase and by inducing mitochondrial-mediated apoptosis.

[Studies on quality standard of PsL 5F injections].

OBJECTIVE: To establish the quality standard of PsL injections containing mainly 5F (ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid). METHOD: The identification of PsL was performed by thin-layer chromatography, and the content was determined by HPLC. The column was Hypersil C18 (4.6 mm x 250 mm, 5 microm), the mobile phase was the mixture of methane-water-acitic acid (55:45: 0.045) with a flow rate of 1.0 mL x min(-1), the detective wavelength was 254 nm, and the column temperature was maintained at 35 degrees C. The pH value and K+ content of the three batchs injection were determined with pH meter and flame photometric meter, and the contents of tannin, protein, oxalic acid salt and heavy metals were detected by deferent methods. RESULT: The TLC method was suitable for the identification of PsL5F. The linearity for 5F was obtained over the range of 30-240 microg x mL(-1) (r = 0.999 8), the average recovery of 5F was 99.8%. The injections were of pH value range from 7.80 to 8.20, K+ contents less than 10 mmol x L(-1), and the contents of tannin, protein, oxalic acid salt and heavy metals were qualified with the Chinese pharmacopoeia, respectively. CONCLUSION: It's sensitive and reliable that can be used as quality control methods of PsL5F injections.

[Advances in study on chemical constituents and pharmacological activities of plants of genus Pteris].

The main chemical constituents in plants of genus pteris include diterpenoids, diterpenoid glycosides, flavonoids, flavonoid glycosides, sesquiterpenoids and volatile oils, etc. Some of extracts show the following activities, such as antitumor, antifungi and antibacteria. Some of compounds have inhibitory effect on platelet aggregation and antiinflamatory action. The latest progress on chemical constituents and pharmacological activity were reviewed in the paper. Main problems and study directions in future of pteris were indicated.

[Determination of 5F in Pteris semipinnata L. from various origins by TLC-scanning].

OBJECTIVE: To determine the content of 5F in Pteris semipinnata L. from various origins. METHODS: 5F was determined by TLC-Scanning. RESULTS: The linear relationship was in range of 0. 504 - 2. 520 microg. The mean recovery was 96. 68% and RSD = 1.24% (n = 5). CONCLUSION: The method is available with a good reproducibility, and pretreatment is simple and easy to operate.