Haiyun He

Publications (2)3.94 Total impact

• Article: Preparation of the thienopyridine derivatives loaded liposomes and study on the effect of compound-lipid interaction on release behavior.

  Jing Liu, Jie Tang, Haiyun He, Lu-Lu Cai, Yimei Huang, Xiawei Wei, Min Luo, Bilan Wang, Xiang Gao, Chengli Yang, Tingting Hu, Xiangrong Song, Tao Yi, Li Yang, Yongmei Xie, Aiping Tong, Lantu Gou, Yinglan Zhao, Yu Zheng
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  ABSTRACT: The article describes characterization of two liposome formulations containing thienopyridine derivatives, namely TP-58 and TP-67. By preparing the liposomes, the concentration of the two compounds in ultrapure water was increased up to three orders of magnitude. After i.v. administration of the liposomes in rats, the initial compound plasma concentrations were enhanced more than fifty times relative to that after i.g. administration of the compound suspensions. It was found out that the release rate of TP-67 from the liposome both in vitro and in vivo was not significantly different from that of TP-58. TP-58 was more lipophilic than TP-67 according to partition coefficiency, and TP-67 had greater polarity than TP-58 based on polar surface area (PSA). With DSC, it was found out that the interaction magnitude between TP-67 and the lipid bilayer was not significantly different from that between TP-58 and the lipid bilayer, which accounted for the similarity of the two compounds in release rate both in vitro and in vivo. It indicated liposome can be used as a potential carrier for broading the application of TP-58 and TP-67. Interaction between the thienopyridine derivatives and the lipid bilayer is probably the decisive factor for compound release from the liposomes.
  Drug Delivery 06/2012; 19(5):247-54. · 1.46 Impact Factor
• Article: SKLB70326, a novel small-molecule inhibitor of cell-cycle progression, induces G₀/G₁ phase arrest and apoptosis in human hepatic carcinoma cells.

  Yuanyuan Han, Haiyun He, Feng Peng, Jiyan Liu, Xiaoyun Dai, Hongjun Lin, Youzhi Xu, Tian Zhou, Yongqiu Mao, Gang Xie, Shengyong Yang, Luoting Yu, Li Yang, Yinglan Zhao
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  ABSTRACT: We previously reported the potential of a novel small molecule 3-amino-6-(3-methoxyphenyl)thieno[2.3-b]pyridine-2-carboxamide (SKLB70326) as an anticancer agent. In the present study, we investigated the anticancer effects and possible mechanisms of SKLB70326 in vitro. We found that SKLB70326 treatment significantly inhibited human hepatic carcinoma cell proliferation in vitro, and the HepG2 cell line was the most sensitive to its treatment. The inhibition of cell proliferation correlated with G(0)/G(1) phase arrest, which was followed by apoptotic cell death. The SKLB70326-mediated cell-cycle arrest was associated with the downregulation of cyclin-dependent kinase (CDK) 2, CDK4 and CDK6 but not cyclin D1 or cyclin E. The phosphorylation of the retinoblastoma protein (Rb) was also observed. SKLB70326 treatment induced apoptotic cell death via the activation of PARP, caspase-3, caspase-9 and Bax as well as the downregulation of Bcl-2. The expression levels of p53 and p21 were also induced by SKLB70326 treatment. Moreover, SKLB70326 treatment was well tolerated. In conclusion, SKLB70326, a novel cell-cycle inhibitor, notably inhibits HepG2 cell proliferation through the induction of G(0)/G(1) phase arrest and subsequent apoptosis. Its potential as a candidate anticancer agent warrants further investigation.
  Biochemical and Biophysical Research Communications 04/2012; 421(4):684-9. · 2.48 Impact Factor