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Yang S.-J.,Guizhou University | Yang S.-J.,Sinphar Tian Li Pharmaceutical Co. | Yang S.-J.,Yangtze River Pharmaceutical Group Co. | Liu M.-C.,Guizhou University | And 5 more authors.
European Journal of Medicinal Chemistry | Year: 2015

Structural modification was performed at the C-28 position of betulonic acid (BetA). Twenty-five BetA derivatives were synthesized, and evaluated for their antitumor activities against MGC-803, PC3, Bcap-37, A375, and MCF-7 human cancer cell lines by MTT assay. Among the derivatives, most of the derivatives had significant antiproliferative ability (IC50 < 19 μM). Compound 3k, the most active compound, showed IC50 values of 3.6, 5.6, 4.2, 7.8, and 5.2 μM on the five cancer cell lines respectively, and was selected to investigate cell apoptosis by subsequent florescence staining and flow cytometry analysis. The results revealed that compound 3k could induce apoptosis in MGC-803 cell lines, and the apoptosis ratios reached 28.33% after 36 h of treatment at 10 μM. In addition, the study of cancer cell apoptotic signaling pathway indicated that the apoptosis of MGC-803 cells induced by compound 3k could be through the mitochondrial intrinsic pathway. © 2015 Elsevier Masson SAS.

Sun Q.,Dalian University | Zheng J.-F.,Dalian University | Liu D.-N.,Yangtze River Pharmaceutical Group Co.
Chinese Journal of Cancer Prevention and Treatment | Year: 2010

OBJECTIVE: To investigate the influence of the physical and mechanical properties of polymethyl methacrylate (PMMA) bone cement mixed with anti-cancer drugs, and the situation of the release of the drugs in vitro. METHODS: Forty g PMMA was mixed with 50 mg doxorubicin hydrochloride and 20 mg zoledronic acid respectively which were divided into Group II and Group III, and the PMMA mixed with nothing was Group I . In accordance with the IS05833: 2002 "surgical implants - acrylic resin cement", a variety of bone cement samples were made in aseptic conditions. The compressive strength, flexural modulus and flexural strength of the samples were checked, the release situation of the drugs was checked after soak elution of the samples. RESULTS: The compressive strength, flexural modulus and flexural strength of bone cement were not significant different between experimental groups and control group (P>0.05). The drugs can be released from the bone cement, and the release law and quantity were not significantly different between group II and group III. Throughout the elution process, more than 0.83% of the doxorubicin hydrochloride and 0.66% of zoledronic acid were released. CONCLUSIONS: There is no influence on the physical and mechanical properties of bone cement when 40 g of which is mixed with less than 1g of the drug. The anti-cancer drugs can be released from bone cement effectively. The PMMA bone cement can be a release carrier of anti-cancer drugs.

Luo H.,Guizhou Academy of Agricultural science | Luo H.,Guizhou University | Yang S.,Yangtze River Pharmaceutical Group Co. | Yang S.,Guizhou University | And 2 more authors.
Medicinal Chemistry Research | Year: 2014

A series of novel curcumin (CC) analogs were synthesized by reacting substituted aldehydes with inter-mediates 4a and 4b. The inhibitory activities of these CC analogs were investigated on human cancer cells PC3, Bcap-37, and MGC-803 in vitro by MTT assay. The results showed that most of the title compounds displayed moderate to high levels of antitumor activities. Compound 5f, the most active CC analogs, has the IC50 values of 1.34 ± 0.28, 3.90 ± 0.36, and 0.86 ± 0.44 μM against the three human cancer cells assayed, respectively. Furthermore, subsequent fluorescence staining and flow cytometry analysis indicated compound 5f could induce apoptosis in PC3, Bcap-37, and MGC-803 cells, and the apoptosis ratio reachs the peak (27.1%) in MGC-803 cells at 24 h after treatment at 10 μM. © Springer Science+Business Media 2013.

Sun Q.,Shenyang Pharmaceutical University | Li F.-F.,Shenyang Pharmaceutical University | Li F.-F.,Yangtze River Pharmaceutical Group Co. | Wang D.,Shenyang Pharmaceutical University | And 7 more authors.
RSC Advances | Year: 2016

Thirteen new flavan compounds named daphnegiravans A-M (1-13) and eight known analogues (14-21) were isolated from the stem and root bark of Daphne giraldii. Their structures were established by comprehensive analysis of NMR data and CD spectra. Five human cancer cell lines (MCF-7, Bcap37, HepG2, Hep3B and A549) were used to evaluate the antitumor activity of all the isolates and their structure-activity relationships were also discussed. Interestingly, prenylated and some methoxy flavans exhibited the highest activities against Hep3B compared with the other cell lines, especially 3 and 9-12 with IC50 values ranging from 5.15 to 9.66 μM. Furthermore, flow cytometry analysis indicated that 3 and 9-11 possessing a 2,2-dimethylpyran moiety in ring B induced G2/M phase arrest in Hep3B cells, while 12 with different structural features effectively inhibited cell proliferation by evoking apoptotic cell death. The reactive oxygen species (ROS) generation might be responsible for the induction of arrest and apoptosis. © 2016 The Royal Society of Chemistry.

Yangtze River Pharmaceutical Group Co., TIANJIN NORTH PHARMA Science and Technology CO. | Date: 2010-01-11

The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.

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