ABSTRACT
Objective To analysis and compare the content differences of three effective components of taxanes of Taxus madia Rehd. from five different habitats and growth years by High Performance Liquid Chromatography (HPLC). Methods The mixed liquor of CH3OH and CHCl3 was used for the ultrasonic extraction of 10-deacetyl-bacratin III (10-DAB III), cephalomannine and taxol before being dissolved by CH3OH to obtain sample solution. By HPLC, the contents of three effective components were performed and compared. Results There were extremely significantly differences (P SM3 > SM2, ZL3 > HK4 > ZL4, ZL3 > SM2 > HK4, HK4 > ZL3 > ZL6, respectively. Except for the contents of 10-DAB III and cephalomannine, there were significant positive correlations among the contents of other components (P < 0.01). The contents of taxol would rise or decline when the total contents of three kinds of taxanes rised or declined among different habitats and growth years. The clustering analysis results showed that the contents of taxol have certain peculiarity. In Fuzhou of Fujian, while the total contents of three kinds of taxanes were different from others in Kaifen of Henan. Conclusion Habitants and growth years have a significant impact on the contents change of three effective components of taxanes from Taxus madia Rehd.. Therefore, regulation and control of biosynthetic pathway by choosing habitat conditions and harvest years should be considered, in order to obtain more crude drug of taxol in T. madia.
ABSTRACT
Tubulin has been shown to be an effective target for the development of cytotoxic agents against prostate cancer. Previously, we reported that Lx2-32c is an anti-tubulin agent with high binding affinity to tubulin. In this study, we investigated the potential of Lx2-32c to act as an effective cytotoxic agent in the treatment of prostate cancer. MTT assays showed that Lx2-32c was cytotoxic to all tested prostate cancer cell lines. The Lx2-32c-treated cells typically exhibited a rounded morphology associated with the onset of apoptosis, as evidenced by immunocytochemical staining. Human prostate cancer cell lines treated with Lx2-32c arrest in the G2/M phase of the cell cycle and the treatment is associated with an increased ratio of cells in the sub-G0/G1 phase as determined by flow cytometry. Furthermore, expression of the cleaved form of poly (ADP-ribose) polymerase in prostate cancer cell lines treated with Lx2-32c was shown by Western blotting assay. Xenograft implants of LNCaP and PC3-derived tumors in nude mice showed that Lx2-32c treatment significant inhibited tumor growth with effects equivalent to those of docetaxel. These findings demonstrate the potential of Lx2-32c as a candidate antitumor agent for the treatment of prostate cancer.