Diterpenoids as PPARγ agonists from Siegesbeckia pubescens and their anti-inflammatory effects in vitro / 中国中药杂志

This study aims to investigate the PPARγ agonists isolated from the aqueous extract of Siegesbeckia pubescens( SPA) and their anti-inflammatory activities in vitro. The 293 T cells transfected transiently with PPARγ recombinant plasmid were used as a screening model to guide the isolation of PPARγ activitating components,and then PPARγ activities were measured by double luciferase reporter gene assay. The chemical structures were identified by chromatography or spectroscopic techniques. Furthermore,a UC inflammatory model in vitro was established on HT-29 cells by stimulating with TNF-α． The mRNA levels and secretion of proinflammatory cytokines on HT-29 cells,such as IL-1β,TNF-α,IL-8,were detected by RT-PCR and ELISA. The results showed that five diterpenoids were obtained from the fraction D_(50) with the strongest PPARγ activity among others in SPA,and determined as kirenol( 1),darutigenol( 2),enantiomeric-2-ketone-15,16,19-three hydroxypinomane-8( 14)-ene-19-O-β-D-glucoside( 3),darutoside( 4),enantiomeric-2-β,15,16,19-four hydroxypinomane-8( 14)-ene-19-O-β-D-glucoside( 5),respectively. All the compounds exhibited active effects on PPARγ in a concentration-dependent manner( P<0. 01). In addition,compound 1 significantly inhibited the expression of IL-1β mRNA and secretion of IL-8 on HT-29 cells inflammation model( P<0. 001); both compounds 2 and 3 effectively inhibited the expression of IL-1β,TNF-α,IL-8 mRNA and secretion of IL-8( P<0. 01 or P<0. 001),although at different extent; compound 4 significantly inhibited the expression of IL-1β and TNF-α mRNA( P<0. 01 or P<0. 001),while compound 5 inhibited the expression of IL-1β mRNA obviously( P<0. 001). In conclusion,the diterpenoids 1-5 isolated from S. pubescens have the PPARγ activation activities and potential effects of anti-UC in vitro.

Clinical efficacy of shenfu injection in treating severe sepsis and its effects on serum levels of interleukin-6 and interleukin-10 / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To observe the therapeutic efficacy of Shenfu Injection (SFI) on patients with severe sepsis and its effects on serum levels of interleukin-6 (IL-6) and interleukin-10 (IL-10).</p><p><b>METHODS</b>Sixty-eight patients with severe sepsis were randomly assigned to the SFI group (36 cases, treated by SFI + routine therapy) and the control group (32 cases, treated by routine therapy). The acute physiology and chronic health evaluation II (APACHE II) score and Marshall score were observed before treatment, 3 and 7days after treatment. The therapeutic efficacy was assessed, and the 28th-day mortality rates were compared. The serum levels of IL-6 and IL-10 were determined by enzyme-labeled immunosorbent assay (ELISA) before and after treatment. C-reactive protein (CRP) was determined by immunoturbidimetric assay.</p><p><b>RESULTS</b>There was no significant difference in the APACHE II score, Marshall score, IL-6, IL-10, or CRP between the two groups before treatment (P>0.05). APACHE II score and Marshall score of all patients decreased after treatment, with more obvious decrease shown in the SFI group (P<0.05). The mortality rate in the SFI group and the control group was 25.0% (9/36) and 37.5% (12/32) respectively, with no significant difference shown between the two groups (P>0.05). The serum levels of IL-6 and CRP obviously decreased after 7 days of treatment (P<0.05). But more decrement was shown in the SFI group, showing significant difference when compared with the control group (P<0.05). There was no significant difference in the serum IL-10 level between the two groups before and after treatment (P>0.05).</p><p><b>CONCLUSION</b>SFI could lower the serum IL-6 level, regulate the equilibrium of proinflammatory factors and anti-inflammatory cytokines in severe sepsis patients, thus playing a role in improving the therapeutic efficacy.</p>

Saponins from roots of Stephanotis mucronata / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from n-BuOH fraction of the roots of Stephanotis mucronata.</p><p><b>METHOD</b>The compounds were separated by chromatographic methods. A combination of UV, MS, and NMR spectroscopic methods was applied to identify structure of these compounds.</p><p><b>RESULT</b>Four oleane saponins were isolated and identified as sitakisoside VII (1), sitakisoside VI (2), sitakisoside II (3), and sitakisoside I (4).</p><p><b>CONCLUSION</b>These four compounds were obtained for the first time from this plant.</p>

Studies on the chemical constituents in radix Astilbes chinensis / 中国中药杂志

<p><b>OBJECTIVE</b>To isolate and determine the chemical constituents from Astilbe chinensis.</p><p><b>METHOD</b>Four compounds were isolated and purified by extraction and column chromatography on silica gel. The chemical structures were determined on the basis of physical-chemical evidence and extensive spectral analysis(HR-EIMS, EIMS, 13C-NMR, 1H-NMR, DEPT, 1H-1H-COSY, HMQC and HMBC).</p><p><b>RESULT</b>Their structures were elucidated as beta-sitosterol palmitate I, daucosterol II beta-sitosterol III and Bergenin IV, respectively.</p><p><b>CONCLUSION</b>Compound I and II were isolated from A. chinensis for the first time.</p>