Computational investigation of the anti-HIV activity of Chinese medicinal formula Three-Huang Powder.

An essential step in the life cycle of human immunodeficiency virus type 1 (HIV-1) is integration of the double-stranded retroviral DNA into the genome of the host cell. HIV-1 integrase, the enzyme that inserts the vital DNA into the host chromosome, is an attractive and rational target for anti-AIDS drug design because it is essential for HIV replication and there are no known counterparts in the host cell. Inhibitors of this enzyme have the great potential to complement the therapeutic use of HIV protease and reverse transcriptase inhibitors.

[Terpenoids from leaves of Aeschynanthus mengxinensis].

Objective: To study the chemical constituents from the ethyl acetate portion of an ethanolic extractive of the leaves of Aeschynanthus mengxinensis.

Method: The column chromatographic techniques were applied to isolate constituents. A combination of IR, ESI-MS, NMR and 2D-NMR spectroscopy was used to identify structures.

[Study on extraction and drying of Ligusticum chuanxiong in Gan-ning Granule].

Objective: To find out the optimum extract process for Ligusticum chuanxiong in Gan-ning Granule, and studyed the methods of concentration and dry for the extract.

Method: With the yield of ferulic acid as the assessment index, to optimize the 80% alcohol totalling, extracting times and circumfluence time for extract process by the orthogonal design, to optimize the inlet-air temperature, feed speed and density of feed for spry drying by the orthogonal design.

Result: The optimum procedure was the ferulic acid were extracted for 1 hour with 3 times of 80% alcohol.

[Effects of stigma maydis polysaccharide on gastrointestinal movement].

Objective: To study the effect of stigma maydis polysaccharide (SMPS) on gastrointestinal movement.

Method: Taking charcoal as the indicator and taking ratio of charcoal movement, beginning time of black excretion and stool amount as the index to observe the effect of SMPS on intestinal movement in mice. Taking emthylorange as the indicator and taking the ratio of residual rate of methylorange as the index to observe the effect of SMPS on gastric emptying in mice.

[Study on the chemical constituents of Mitragyna rotundifolia].

Twelve compounds were isolated from the EtOAc-soluble and ButOH-soluble portions of the EtOH extract from the bark of Mitragyna rotundifolia. These compounds were identified by their spectral data as dauricine (1), 3,4-dihydroxybezoic acid (2), beta-sitosterol (3), scopleton (4),3,4,5-trimethyoxyphenol-1-glucopyranoside (5), taraxerol (6), 4-hydroxy-3-methyloxybenzoic acid (7), 3-hydroxy-4-methyloxybenzoic acid (8), caffeic acid (9), gambirine (10), gambireine (11),1,1-dimetheyl-2-acetl-diethyl ether (12), respectively. All compounds were isolated from this genus for the first time.

Bcl-2 switches the type of demise from apoptosis to necrosis via cyclooxygenase-2 upregulation in HeLa cell induced by hydrogen peroxide.

Bcl-2 is best known for its anti-apoptotic function in a wide variety of cell types. The objective of this study was to investigate the effects of bcl-2 on the types of cell demise in the HeLa/bcl-2 cells induced by H2O2. The HeLa cell expressed stably bcl-2 was established and defined as the HeLa/bcl-2 cell strain, while the cell transfected with the empty expression vector was defined as the HeLa/vector cell strain.

Thalidomide inhibits growth of tumors through COX-2 degradation independent of antiangiogenesis.

Thalidomide is an antiangiogenic drug and is clinically useful in a number of cancers. However, the molecular mechanism by which thalidomide exerts its antitumor effects is poorly understood. This study was designed to clarify the relationship between antiangiogenesis and antitumor effects of thalidomide and to explore the molecular mechanism for its antitumor activity.

[Synthesis and antibacterial activity of 2-(3-pyridyl)-5-([(5-aryl-1,3,4-oxadiazol-2-yl) methylene]thio)-1,3,4-oxadiazoles].

Aim: Studies on synthesis and antibacterial activity of new heterocycles.

Methods: The cyclocondensation of [(3-pyridyl)-1,3,4-oxadiazol-2-yl] thio acetic acid with various aroyl hydrazines in the presence of POCl3 and xylene gave the corresponding titled compounds, and the in vitro antibacterial activity was primarily evaluated by the method of cupplate diffusion solution.

Results: Sixteen novel titled compounds were synthesized, their structures were confirmed by IR, 1HNMR, MS and elemental analysis.