1.Metagenomics and their application in the research of marine natural drugs
Tong ZHOU ; Rongli NIU ; Xiukun LIN
Chinese Journal of Marine Drugs 1994;0(02):-
Objective To study the chemical constituents of marine sponge Craniella australiensis collected from the South China Sea.Methods Compounds were isolated and purified by column chromatography and their structures were identified based on spectral analyses and chemical evidence.Results Four compounds were isolated from the ethanol extract and identified as: ?-sitosterol(Ⅰ),3?,6?-stigmast-4-en-3,6-diol(Ⅱ),1,12-diazacyclodocosane-2,11-dione(Ⅲ),uracil(Ⅳ).Conclusion All these compounds were isolated from this sponge for the first time.
2.Oleanolic acid inhibits proliferation of HUVECs, and inhibits migration and tube formation via VEGF pathway.
Jianteng WEI ; Ming LIU ; Haizhou LIU ; Jin ZHAO ; Lin XIAO ; Lijun HAN ; Xiukun LIN
Acta Pharmaceutica Sinica 2012;47(11):1457-62
To investigate the effects of oleanolic acid (OA) on the proliferation, migration and the formation of tube-like structure in human vascular endothelial cells (HUVECs). MTT assay, flat plate scarification, Transwell plates and matrigel-induced tube formation assay were performed to detect the effects of OA on proliferation, migration and tube formation. MTT assay showed that the inhibition rates of HUVECs treated with 60 and 100 microg x mL(-1) of OA for 24 h were 19% and 83% respectively. Treatment of HUVECs significantly inhibited the cell migration in a dose-dependent manner. The vascular indexes of HUVECs treated with 40 and 60 microg x mL(-1) OA were 33% and 20% respectively. Western blotting analysis showed that treatment of the cells with OA significantly attenuated the expression and secretion of VEGF. Additionally, VEGF could in part reverse the effects of OA on migration and tube formation of HUVECs. In conclusion, OA inhibits the proliferation, and VEGF plays an important role in OA induced decreased migration and tube formation of HUVECs.
3.Lidamycin inhibits angiogenesis of zebrafish embryo via down-regulation of VEGF.
Lili DING ; Ming LIU ; Shenghua ZHANG ; Xiangzhong ZHAO ; Ning WU ; Lei CHEN ; Guangjian WANG ; Xiukun LIN
Acta Pharmaceutica Sinica 2010;45(4):456-61
Lidamycin (LDM) is a potent antitumor antibiotic. Previous studies have shown that LDM could inhibit proliferation and migration in endothelial cells. In the present report, the effect of LDM on angiogenesis of zebrafish embryo was studied. The results showed that treatment of zebrafish embryos with LDM resulted in significant inhibition of angiogenesis. Morphological observation, quantitative endogenous alkaline phosphatase (EAP) assay, alkaline phosphatase staining, and transgenic zebrafish assay were performed to evaluate vascular development defects in zebrafish. The results indicated that after the zebrafish embryos were exposed to LDM, angiogenesis defects of zebrafish embryos were observed, including pericardial edema, reduced numbers of circulating red blood cells, suppression of zebrafish vessel growth, and absences of SIV (subintestinal vein). The expression of VEGF was detected by RT-PCR assay, quantitative reverse transcriptase real-time PCR (qRT-PCR) assay and Western blotting analysis. The results revealed that LDM could inhibit the expression of VEGF protein, while the expression of mRNA was not significantly affected. The study suggests that LDM could inhibit the zebrafish embryo angiogenesis by down-regulation ofVEGF expression.
4.Study on Improvement Effect and Mechanism of 4-hydroxy-2-benzoxazolone on Carbon Tetrachloride-induced Hepatic Fibrosis in Rats
Xiukun HUANG ; Xuemei SUN ; Xunshuai ZHU ; Lin LIU ; Xing LIN ; Jun LIN
China Pharmacy 2019;30(6):747-751
OBJECTIVE: To observe the improvement effect and mechanism of 4-hydroxy-2-benzoxazolone (HBOA) on carbon tetrachloride-induced hepatic fibrosis in rats. METHODS: Male SD rats were randomly divided into normal control group, model group, colchicine group (positive control, 0.4 mg/kg) and HBOA low-dose, medium-dose and high-dose groups (50, 75, 100 mg/kg), with 12 rats in each group. Except for normal control group was given constant volume of normal saline intragastrically, other groups were given 50%CCl4-olive oil solution (2 mL/kg, initial dose double) intragastrically, twice a week, for consecutive 12 weeks, to induce hepatic fibrosis model. Since the 9th week of modeling, administration groups were given relevant medicine intragastrically. Normal control group and model group were given constant volume of 0.6% Carboxymethylcellulose sodium solution intragastrically, once a day, for consecutive 4 weeks. After last administration, the serum contents of ALT, AST, IL-1β and IL-10, the protein expression of NF-κB p65, TNF-α, IL-6 and ICAM-1 in liver tissue were determined. RESULTS: Compared with normal control group, the positive expression of NF-κB p65 in liver tissue was increased significantly in model group; serum contents of ALT, AST and IL-1β as well as protein expression of NF-κB p65, TNF-α, IL-6 and ICAM-1 in liver tissure were increased significantly, while serum content of IL-10 was decreased significantly (P<0.05). Compared with model group, the positive expression of NF-κB p65 in liver tissue were decreased to different extents in administration groups; serum contents of ALT, AST and IL-1β as well as protein expression of NF-κB p65, TNF-α, IL-6 and ICAM-1 in liver tissue were decreased significantly, while serum content of IL-10 was increased significantly (P<0.05). CONCLUSIONS: HBOA can improve carbon tetrachloride-induced hepatic fibrosis in rats, and the mechanism of which may be associated with relieving inflammatory reaction by blocking NF-κB signaling pathway and down-regulating the protein expression of ICAM-1.