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Steroidal Saponins from the Rhizomes of Paris delavayi.

Steroids. 2009 May 14; Zhang T, Liu H, Liu XT, Chen XQ, Wang QTwo new steroidal saponins, padelaosides A (1) and B (2), along with two other known steroidal saponins (3 and 4) were isolated from the rhizomes of Paris delavayi. Their structures were elucidated by 1D and 2D NMR techniques, HRFTMS, physical data and chemical methods. The two different absolute configurations of fucose, assigned as L and D, that were found on compounds 1 and 2, respectively, were simultaneously reported in a natural medicine for the first time.

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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