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Yu J.-P.,Shanghai Institute of Pharmaceutical Industry | Chen W.,Shanghai Institute of Pharmaceutical Industry | Zhu X.-Y.,Shanghai Institute of Pharmaceutical Industry | Zhang X.-Q.,Jiangsu Chia Tai Tianqing Pharmaceutical Group Co. | And 2 more authors.
Chinese Journal of New Drugs | Year: 2015

Objective: To optimize the synthetic process of trelagliptin succinate. Methods: Trelagliptin succinate was synthesized from 4-fluoro-2-methylbenzoic acid via eight steps, including chloro, aminolysis, dehydration, bromo, substitution, condensation, deprotection, and finally salifying. Results: Our process abolished the regents that are moderate-severely toxic environmental pollution reported in the primary literature. Meanwhile, the method of purification also abolished column chromatography, which was of lower cost and easier operation. The overall yield was 35.8% with a purity of 99.89%. Conclusion: This synthetic process is of easy operation and low cost, and is suitable for industrialization. ©, 2015, Chinese Journal of New Drugs Co. Ltd.. All right reserved.

Zheng X.,Nanjing University | Gao S.,Jiangsu Chia Tai Tianqing Pharmaceutical Group Co. | Hua H.-Q.,Nanjing University | Yang A.-Z.,Nanjing University | Qin S.-K.,Nanjing University
World Chinese Journal of Digestology | Year: 2016

AIM: To observe the effect of ginsenoside Rg3 combined with sorafenib in inhibiting tumor growth and neovascularization in nude mice with in situ transplanted human hepatocellular carcinoma xenografts and to explore the possible mechanism. METHODS: Twenty-six nude mice with highly metastatic human hepatocellular carcinoma transplanted in situ (LCI-D20) were randomly divided into an R group treated with ginsenoside Rg3 (5 mg/kg, qd), an S group treated with sorafenib (30 mg/ kg, qd), a combination group treated with both ginsenoside Rg3 (5 mg/kg, qd) and sorafenib (30 mg/kg, qd), and a control group treated with saline. After 2 wk of treatment, all mice were killed to collect orbital blood samples. The tumors were peeled off and weighed to calculate the tumor inhibition rate. Immunohistochemical method was used to detect the micro-vessel density (MVD) in the tumors. The expression of vascular endothelial growth factor (VEGF), hypoxia inducible factor-1α (HIF-1α), and VEGF receptor 2 (VEGFR-2) in tumors was detected by ELISA and Western blot. RESULTS: The tumor inhibition rates of the R group, S group and combination group were 20.60%, 34.74% and 48.64%, respectively. According to the Weeb coefficient algorithm, the combination group showed a synergistic effect in inhibiting the tumor growth in nude mice. The MVD of each treatment group was significantly lower than that of the control group (P < 0.01), although there were no significant differences between the combination group and the R or S group (P > 0.05). ELISA results showed that serum VEGF levels were significantly lower in the R, S and combination groups than in the control group (P < 0.01, P < 0.05 and P < 0.01), and in the combination group than in the S group (P <0.05), but there was no significant difference between the combination group and R group (P > 0.05). Compared with the control group, the level of HIF-1α was significantly lower in all treatment groups (P < 0.05) except the S group (P > 0.05), and the decrease was more significant in the combination group than in the S group (P < 0.05). The level of VEGFR-2 had no significant difference in the four groups (P > 0.05). Western blot showed decreased expression of VEGF, HIF-1α and VEGFR-2 in the three treatment groups (P < 0.05), although there were no significant differences between the combination group and R or S group (P > 0.05). CONCLUSION: Ginsenoside Rg3 combined with sorafenib shows a synergistic effect in inhibiting tumor growth in nude mice, via mechanisms possibly associated with regulating the expression of angiogenesis factors VEGF, HIF-1α, and VEGFR-2. © 2016 Baishideng Publishing Group Inc. All Rights Reserved.

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