1.Antidepressant effects of DS-1226 on mouse models of depression induced by chronic sleep interruption
Beiyue ZHANG ; Jinli SHI ; Zhiquan ZHENG ; Linxi FAN ; Jingwei LV ; Xinmin LIU
Acta Laboratorium Animalis Scientia Sinica 2017;25(1):85-89
Objective To investigate the antidepressant effect of DS-1226, a hydrolysate of ginsenosides, on a mouse model of depression induced by chronic sleep interruption, and provide scientific evidence for the research and de?velopment of antidepressant drugs. Methods 72 male ICR mice were divided into control group, model group, positive control group (paroxetine hydrochloride, 10 mg/kg) and 3 treatment groups (20 mg/kg, 40 mg/kg, 80 mg/kg of DS?1226). Except the control group, the other mice were put into a rotary roller (parameter settings:1 min/rev;rest 2 min af?ter 1 rev) for 3 days of drum adaptation, 3 h/d. Then making model for 14 days in the roller( parameter settings:1 min/rev;rest 2 min after 1 rev) . The antidepressant effects of DS?1226 were evaluated by weight monitoring, open?field test, tail suspension test, and forced swimming test. Results After 14 d sleep disturbance, compared with the control group,the body weight, immobility time in tail suspension test and forced swimming test were significantly decreased in the model group. Compared with the model group, DS?1226(40 mg/kg)significantly reversed the weight loss caused by sleep disturb?ance. Paroxetine significantly reduced the immobility time of tail suspension test. DS?1226 (40 mg/kg, 80 mg/kg)signifi?cantly decreased the immobility time of tail suspension test, and DS?1226 (80 mg/kg) significantly decreased the immobil?ity time of forced swimming test. Conclusion The hydrolysate of ginsenosides DS?1226 shows antidepressant effect on mouse model of depression induced by chronic sleep interruption.
2.Lx2-32c, a novel semi-synthetic taxane, exerts antitumor activity against prostate cancer cellsand.
Guangyao LV ; Dengjun SUN ; Jingwen ZHANG ; Xiaoxia XIE ; Xiaoqiong WU ; Weishuo FANG ; Jingwei TIAN ; Chunhong YAN ; Hongbo WANG ; Fenghua FU
Acta Pharmaceutica Sinica B 2017;7(1):52-58
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.