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Lignans with Anti-HIV Activity from Schisandra propinqua var. sinensis.

J Nat Prod. 2009 May 4; Li XN, Pu JX, Du X, Yang LM, An HM, Lei C, He F, Luo X, Zheng YT, Lu Y, Xiao WL, Sun HDFourteen new lignans, tiegusanins A-N (1-14), together with 13 known compounds were isolated from the aerial parts of Schisandra propinqua var. sinensis. The structures and absolute configurations of 1-13 were established using a combination of spectroscopic techniques. Compound 14 was obtained as a racemate. When evaluated for inhibitory activity against HIV-1, tiegusanin G (7) showed anti-HIV-1 activity with an EC(50) value of 7.9 muM and a therapeutic index (TI) of more than 25.

[Comparative pharmacophore analysis of dual dopamine D2/5-HT(2A) receptor antagonists]

Yao Xue Xue Bao. 2009 Mar; 44(3): 314-20Guo YS, Guo ZRDual dopamine D2/5-HT2A receptor antagonists have potent activity and are referred to atypical antipsychotics due to their lower propensity to elicit EPS and their moderate efficacy toward negative symptoms. However, an on-going challenge in developing atypical antipsychotics drugs is to maintain the favorable profiles and avoid of cardiovascular risk. In this paper, comparative pharmacophore analysis of dual dopamine D2/5-HT2A receptor antagonists, hERG K+ channel blockers, and alA adrenoceptor antagonists is carried out, and the results could give some insight into multi-target drug design.

[Recent advance in the study of novel anti-tumor targets and drugs--aurora kinase and Pin1]

Yao Xue Xue Bao. 2009 Mar; 44(3): 264-9Chen XG, Zhang YMalignant tumor, one of the most refractory diseases, plays a threaten role in human health, the therapy and research on malignant tumor have taken a long way to go. The anti-tumor drugs which are the essential therapy strategies upgrade with the development of new anti-tumor targets and the research on tumor pathogenesis. Aurora kinase and Pin1, the novel anti-tumor targets, maintain the important relationship with tumor. Many new compounds designed on these targets have excellent anti-tumor effects and also enter into phase I or phase II clinical trial.

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