ABSTRACT
Objective:To investigate the effects of pristimerin therapy on the functions of Th17 and Treg cells in patients with allergic asthma,and expore the function of immune factors in therapy on allergic asthma. Methods:Extracted mononuclear cells in pe-ripheral blood of patients with allergic asthma,and given pristimerin intervention in vitro. Then used fluorescence-activated cell sorting analysis to detect the contect of Th17 and Treg,enzyme-linked immunosorbent assay to detect cytokine production of IL-17 and TGF-β, and Real-time PCR to detect the contect of RORγT and Foxp3. Results: Compared with the control group, experimental group had reduced expression of CD4+IL-17+T cells ( Th17 cells) ,and increased expression of CD4+CD25+Foxp3+T cells ( Treg cells) ,which all had the statistical significance (P<0. 05);displayed decreased level of IL-17,and increased level of TGF-β,which all had the statistical significance (P<0. 05);had reduced expression of RORγT,and increased expression of Foxp3,which all had the statistical significance (P<0. 05). Conclusion: Pristimerin therapy can remit the unbalance of Th17/Treg in vitro,hinting this drug may regulate allergic asthma by influencing immunologic balance,which offers the theoretical support for pristimerin in clinical application.
ABSTRACT
Cancer constitutes the second main mortality cause in the world, after cardiovascular diseases. In spite of the progresses in the chemotherapeutics treatments, many patients fail chemotherapy, mainly because of side effects or multi-drugs resistance, proving the need and importance of the research for new molecules with anticancer activity, more effective and with smaller adverse effects. Various compounds derived from plant secondary metabolites are commonly used in the chemotherapy against cancer and the natural products play an important role in the research for new molecules. Among several molecules of natural origin evaluated by MTT assay in murine tumor cell lines [breast (LM3) and lung (LP07)] the quinona-methide triterpenes tingenone and pristimerin showed marked cytotoxic activity presenting IC50 around 2 and 5 µM respectively. The structure-activity relationship suggests that rings A and B containing an α, ß-unsaturated carbonyl group are essential for the observed cytotoxic activity. The interaction between these positions and acetylcisteyne residues suggests a probable mechanism of action. The in vitro mutagenic activity was also evaluated by the Salmonella microsome assay (Ames test) for pristimerin and tingenone with and without metabolic activation (S9) in the strains TA98, TA97a, TA100 and TA102, none of which showed mutagenic potential in any strains. Estrogenic and anti-estrogenic activities were also studied by the e-screen assay in MCF-7 cells with negative results. The present data point to the importance of pristimerin and tingenone as representative of an emerging class of potential anticancer chemicals.
ABSTRACT
AIM:To study the chemical constitutes of Celastrus orbiculatus Thunb. METHODS:Root of celastmus orbiculatus was macerated with cool ethanol to obtain the extract under the vaccum drying processing,extract obtained was extracted respectively by petroleum ester and ethyl acetate. Final extracts were purified by Silicagel column and analyzed by UV,IR,Ms and NMR to identify the chemical structural formula. RESULTS:Seven compounds were isolated from Celastrus orbiculatus Thunb,from which five constituents came from petroleum ester extract,and identified as sugiol (1),pristimerin (2),?-sitosterol (3),celastrol (4),from which two constituents came from ethyl acetate extract,salapermic acid(5),benzoic acid (6) and daucosterol (7),respectively. CONCLUSION:Compounds 1,5 were obtained from the plant for the first time.
ABSTRACT
AIM To study the anti-inflammatory effects and mechanisms of pristimerin. METHODS Several inflammatory models were established, such as ear edema induced by croton oil, hind paw swelling by carrageenan, elevation of capillary permeability by acetic acid in mice and a-cute peritonitis induced by carrageenan in rats. Protein content was measured by Coomassie brilliant blue method, nitric oxide (NO) content by Griess reaction assay, N-acetyl-?-D-glucosamini-dase (NAG) activity by colorimetry, superoxide dismutase (SOD) activity by hydroxylamine method, catalase (CAT) activity by ultraviolet spectro-photometry, and malondialdehyde (MDA) content by fluorescence method in peritoneal exudate in rats. RESULTS Pristimerin ip 0. 156 - 0. 625 mg ? kg-1 or im 1-4 mg - kg-1 inhibited ear edema, hind paw swelling, and elevation of capillary permeability in mice. In the rat peritonitis induced by carrageenan, pristimerin im 1 - 2 mg ?kg-1 reduced neutrophil counts, lessened protein and NO content, inhibited the production of MDA and decreased NAG activity, while augmented the SOD and CAT activity in exudate. CONCLUSION Pristimerin has a significant anti-inflammatory effect which may be related to the inhibition of NO production, scavenging oxygen free radicals, anti-lipoperoxidation and stabilizing lysosome membrane.