Asparagus polysaccharide and gum with hepatic artery embolization induces tumor growth and inhibits angiogenesis in an orthotopic hepatocellular carcinoma model.

Liver cancer is one of leading digestive malignancies with high morbidity and mortality. There is an urgent need for the development of novel therapies for this deadly disease. It has been proven that asparagus polysaccharide, one of the most active derivates from the traditional medicine asparagus, possesses notable antitumor properties. However, little is known about the efficacy of asparagus polysaccharide as an adjuvant for liver cancer chemotherapy. Herein, we reported that asparagus polysaccharide and its embolic agent form, asparagus gum, significantly inhibited liver tumor growth with transcatheter arterial chemoembolization (TACE) therapy in an orthotopic hepatocellular carcinoma (HCC) tumor model, while significantly inhibiting angiogenesis and promoting tumor cell apoptosis. Moreover, asparagine gelatinous possessed immunomodulatory functions and showed little toxicity to the host. These results highlight the chemotherapeutic potential of asparagus polysaccharide and warrant a future focus on development as novel chemotherapeutic agent for liver cancer TACE therapy.

[Synthesis of 5-fluorouracil derivatives containing alkanoic acid].

OBJECTIVE: To synthesize 5-fluorouracil derivatives containing 2-5 carbon alkanoic acid. METHODS: N1-substituted derivatives containing alkanoic acid were prepared through the hydrolysis of these products of the reaction of haloesters and excessive amount of 5-fluorouracil. 5-fluorouracil were protected with tertbutoxycarbonyl (Boc) at N1-position, then reacted with haloesters and deprotected in turn, through this "one-pot" method, N3-substituted 5-FU alkanoic acid esters can be obtained, with high yields (75%-85%). The hydrolysis of these products gave N3-substituted 5-FU alkanoic acid at last. RESULTS: Including 10 new compounds and 8 aim compounds, 16 derivatives of 5-fluorouracil were obtained and confirmed by the spectral detection. CONCLUSIONS: The reaction of excessive amount of 5-fluorouracil and haloesters can produce a good yield of N1-substituted derivatives. N3-substituted derivatives can be obtained through the reactions of 5-fluorouracil protected with Boc at N1-position and haloesters.

C-mycprotein expression upregulated by 2-(3-estrone-N-ethyl piperazine-methyl) tetracycline in bone.

AIM: To study the effect of XW630 on expression of pro-oncogene c-myc in the long bones of fetal mice in vitro for postulating the mechanism by which XW630 exerts its effect on bone. METHODS: The fetuses of pregnant mice were removed on day 16 of gestation, the long bones of the forelimbs of female fetal mice were freed of muscle and soft tissue and cultured in a specific device for 48 h in BGJb medium treated with 1 x 10(-7), 1 x 10(-8) and 1 x 10(-9) mol.L-1 XW630 in the final medium. After cultured for 48 h, the long bones were harvested and immunohistochemical analysis was performed for determination of c-Myc protein expression in epiphyseal plates. The areas of positive cells in the resting zone, proliferative zone and hypertrophic zone in epiphyseal plate were determined under image analytic system. RESULTS: When the concentration of XW630 in the medium was 1 x 10(-9) mol.L-1, the area of c-Myc positive cells increased in the proliferative zone compared with 1 x 10(-9) mol.L-1 in the estrone group, significant increase was also observed in the resting zone compared with the control group. When the concentration of XW630 in medium was 1 x 10(-8) or 1 x 10(-7) mol.L-1, stronger expression than that in the control group and the estrone group at the same concentration was observed in each of the three zones. CONCLUSION: The estrogenic effect of XW630 on bone was stronger than that of estrone. XW630 may promote proliferation and differentiation of chondroncytes by promoting c-Myc protein expression in chondroncytes. Thus, endochondral bone formation was enhanced.