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Bi Y.,Yantai University | Xu J.-Y.,China Pharmaceutical University | Sun F.,China Pharmaceutical University | Wu X.-M.,Jiangsu University | And 4 more authors.
Records of Natural Products | Year: 2013

A novel series of 17-carboxylic acid modified amide derivatives of 23-hydroxy betulinic acid (1) were prepared and tested in vitro against five cell lines: A549 (human lung carcinoma), BEL-7402 (human hepatoma), SF-763 (human cerebroma), B16 (mice melanoma) and HL-60 (human leukaemia). Within this series of compounds, 4a (IC50=21.08 μM in SF-763, IC50=21.63 μM in HL-60), 4b (IC50=28.45 μM in HL-60,IC50=29.32 μM in BEL-7402) and 6g (IC50=26.09 (μM in BEL-7402, IC50=22.65 (μM in HL-60) have the more potent cytotoxic activity than lead compound 1. The preliminary structure-activity relationship analysis of the C-28 amide derivatives is also discussed. © 2013 Reproduction is free for scientific studies. Source


Huang Z.,China Pharmaceutical University | Fu J.,China Pharmaceutical University | Liu L.,China Pharmaceutical University | Sun Y.,Nanjing KeyGen Biotech. Co. | And 5 more authors.
Organic and Biomolecular Chemistry | Year: 2012

A series of O2-glycosylated diazeniumdiolate-based derivatives of oleanolic acid (4-19) were synthesized and their anti-human hepatocellular carcinoma (HCC) activities were evaluated. Compound 6 selectively inhibited HCC, but not non-tumor liver cell proliferation. This inhibition was attributed to high levels of nitric oxide (NO) released in HCC cells. Importantly, 6 exhibited low acute toxicity (LD50 = 173.3 mg kg-1) and potent inhibition of HCC tumor growth in mice (3 mg kg-1 iv). Furthermore, 6 induced HCC cell apoptosis, which was accompanied by lower mitochondrial membrane potentials and Bcl2 expression, but with higher cytochrome C release, Bax, caspase 3 and 9 expression activities in HCC cells. Collectively, 6 may be a promising candidate drug for the intervention of HCC. © 2012 The Royal Society of Chemistry. Source


Li D.,China Pharmaceutical University | Cai H.,China Pharmaceutical University | Jiang B.,China Pharmaceutical University | Liu G.,Shenyang Pharmaceutical University | And 6 more authors.
European Journal of Medicinal Chemistry | Year: 2013

A series of novel spirolactone-type diterpenoid derivatives of oridonin (12a-j) were designed and synthesized. All the target compounds showed improved anti-proliferative activity against a panel of human cancer cell lines and the most effective compound 12j was more potent than positive control Taxol in K562 and Bel-7402 cells with IC50 values of 0.39 μM and 1.39 μM, respectively. The cellular mechanisms showed that compound 12j induced apoptosis at low micromolar concentrations in human hepatoma Bel-7402 cells. These results demonstrate that the spirolactone-type diterpenoid derivatives of oridonin have optimized growth inhibitory activity against cancer cells and interesting apoptosis-inducing ability.© 2012 Elsevier Masson SAS. All rights reserved. Source


Li D.,China Pharmaceutical University | Xu S.,China Pharmaceutical University | Cai H.,China Pharmaceutical University | Pei L.,China Pharmaceutical University | And 7 more authors.
European Journal of Medicinal Chemistry | Year: 2013

A series of enmein-type diterpenoid analogs (11-20) derived from natural kaurene-type diterpenoid oridonin were synthesized and biologically evaluated. All target compounds showed improved anti-proliferative activities against four human cancer cell lines compared with natural oridonin and parent compound 10. Some compounds were more potent than positive control Taxol. Furthermore, mechanistic investigation showed that the representative compound 17 affected cell cycle and induced apoptosis at low micro-molar level in human hepatoma Bel-7402 cells, via an oxidative stress triggered mitochondria-related caspase-dependent pathway. © 2013 Elsevier Masson SAS. All rights reserved. Source


Bi Y.,Yantai University | Xu J.,China Pharmaceutical University | Sun F.,China Pharmaceutical University | Wu X.,China Pharmaceutical University | And 3 more authors.
Molecules | Year: 2012

23-Hydroxybetulinic acid (1) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60). Among the obtained compounds, 6i had the most potent antitumor activity, with the IC 50 values of 8.35 μM in HL-60 cells and showed similar antitumor activity as cyclophosphamide in H22 liver tumor and as 5-fluorouracil in B16 melanoma in vivo. Source

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