Effect of Artesunate on Experimental Choroidal Neovascularization and Expression of HIF-1α and VEGF / 中国实验方剂学杂志

Objective:To observe the effects of artesunate （ART） on experimental choroidal neovascularization （CNV） and the expression of related proteins， and to explore the underlying mechanism. Method:Eighty BN rats were randomly divided into five groups： a normal group， a model group， a conbercept group， and low- （10.08 mg·kg^-1·d^-1） and high-dose （20.16 mg·kg^-1·d^-1） ART groups， with 16 rats in each group. A CNV model was established with 532 nm laser in rats of the groups except for the normal group. The rats in each group were treated with corresponding drugs by gavage for 14 days. The normal group， the model group， and the conbercept group received 1% CMC-Na solution at the same volume， while the conbercept group received an intravitreal injection （5 μL） once. On days 7 and 14， fundus fluorescein angiography （FFA） was used to evaluate the fluorescein leakage （gray value） of CNV. Hematoxylin-eosin （HE） staining was adopted to observe the histopathological changes of CNV. Western blot was employed to detect the protein expression levels of hypoxia-inducible factor-1<italic>α</italic> （HIF-1<italic>α</italic>） and vascular endothelial growth factor （VEGF） in the retina and choroid. Result:FFA results showed that compared with the normal group， other groups showed increased gray value on days 7 and 14 （<italic>P</italic><0.01）. On day 7， the gray value of the high-dose ART group and the conbercept group decreased compared with that in the model group （<italic>P</italic><0.01）. On day 14， the gray value of the ART groups and the conbercept group decreased in varying degrees compared with that in the model group （<italic>P</italic><0.05， <italic>P</italic><0.01）. HE results showed that compared with the normal group， the model group showed increased thickness of CNV on days 7 and 14 （<italic>P</italic><0.01）. Compared with the model group， the ART groups and the conbercept group displayed decreased thickness of CNV （<italic>P</italic><0.01）. Western blot results revealed that the expression of HIF-1<italic>α</italic> and VEGF in the model group increased in varying degrees on the days 7 and 14 compared with that in the normal group （<italic>P</italic><0.05， <italic>P</italic><0.01）， while compared with the model group， the ART groups and the conbercept group showed decreased expression （<italic>P</italic><0.01）. Conclusion:ART can inhibit experimental CNV by down-regulating the expression of HIF-1<italic>α</italic> and VEGF in the early stage of experimental CNV formation.

Effect of artesunate on expression of MMP-9 in rat retina / 中草药

Objective: To investigate the effects of artesunate (ART) on diabetic retinopathy of rats by detecting the expression variation of matrixmetalloproteinase-9 (MMP-9) and inhibitory factor matrix metalloproteinase inhibitor-1 (TIMP-1) in retina. Methods: A total of 24 healthy male SD rats were randomly divided into negative control, model control and ART treated groups. The model control group and ART treated group were given injection of streptozotocin (STZ) to establish the type 1 diabetic rat model. After being raised for three months, the ART treated rats' abdomina were given ART injection for 10 d. All retinas of three groups were isolated. The expression of MMP-9 and TIMP-1 mRNA was detected by Real-time PCR (RT-qPCR) and the expression of MMP-9 protein was detected by immunohistochemical staining. Results: The expression of MMP-9 in ART treated group was significantly decreased compared with model control group (P < 0.05), whereas TIMP-1 in ART treated group was significantly increased (P < 0.05). The immunohistochemical staining showed that the positive expression of MMP-9 protein in ART treated group was significantly less than that in model control group. Conclusion: ART has inhibitory effects on the expression of MMP-9 in the diabetic retinopathy of rats.

Effects of Artesunate on Free Ca~(2+) Concentration in Human Prostatic Cancer PC-3 Cells / 中国药房

OBJECTIVE:To investigate the effects of artesunate(ART) on free Ca2+ concentration([Ca2+]i) in human prostatic cancer PC-3 cells.METHODS:PC-3 cells were treated with ART and labeled using Ca2+ fluorescent probe Fluo-3/AM,and the change of[Ca2+]i was evaluated by confocal laser scanning microscopy.RESULTS:After PC-3 cells were exposed to artesunate,the intracellular [Ca2+]i concentration increased significantly at 0～0.5 h,maintained at a high level at 0.5～1 h,but decreased to the level of the initial at 4～24 h. CONCLUSION:ART can induce the marked sustained increase of[Ca2+]i and [Ca2+]i might play an important role in ART-induced apoptosis of human PC-3 cells.