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@#Chemical constituents and biological activities of the Mitrella kentii leaf oil were investigated in this study. Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used to determine the chemical constituents of the oil. The oil was evaluated for its ability to inhibit prostaglandin E2 (PGE2 ) and thromboxane B2 (TXB2 ) productions in human whole blood using a radioimmunoassay technique. Its inhibitory effect on plateletactivating factor (PAF) receptor binding with rabbit platelets using 3 H-PAF as a ligand and its free radical scavenging effect on DPPH were also investigated. Caryophyllene oxide (33.8%w/w), E,Z-farnesol (6.9%), benzyl benzoate (6.5%w/w) and viridiflorol (6.5%w/w) were among the major components of the oil. Even though weak inhibitory activities were observed in both PGE2 and TXB2 assays, significant results were obtained in both PAF receptor binding inhibition and 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging effect with IC50 value of 6.6 µg/mL and 155.6 µg/mL respectively. These promising activities warrant the development of the oil as an anti-inflammatory agent.
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Objective To explore the role of regulatory T-lymphocytes(Treg) in the immune pathogenesis of suba-cute thyroiditis (SAT). Methods The proportion of Treg in CD4+T cells in peripheral blood of 46 SAT patients and15 controls was detected using flow cytometry. And the concentration of interleukin-10(IL-10), transforming growth factor-beta1(TGF-β1) and prostaglandin E2(PGE2) in serum of 46 SAT patients and 15 controls was measured with ELISA. In addition, the Forkhead box protein 3 (Foxp3) positive cells in thyroid tissue of 29 SAT patients and20 controls was detected by immunohistochemistry. Results The proportion of Treg in peripheral blood of SAT pa-tients was significantly lower than that of controls (P＜0.05). And the concentration of TGF-β1 in serum of SAT patients was apparently higher than that of controls(P＜0.05). Additionally, the positive rate of Foxp3 in thyroid tissue of SAT patients was markedly higher than that of controls(P＜0.05).Conclusions The decrease of Treg may play an important role in the immune pathogenesis of SAT.
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AIM To study the effects and action mechnism of Xiaoding Ointment (Pyrolusite,Catechu,Rhei Radix et Rhizoma,etc.) on rabbits' fracture healing in terms of cyclooxygenase-2 (COX-2),prostaglandin E2 (PGE2),cyclic adenosine monophosphate (cAMP) expressions at different time points.METHODS One hundred and twenty-eight New Zealand white rabbits were randomly divided into blank group,model group,Qingpeng Ointment (Oxytropis Falcatae Herba,Rhei lhasaense Radix et Rhizoma,Terminalia chebula Fructus,etc.) group and Xiaoding Ointment group.All the other groups,except the blank group,were made with ulna 3 mm bone defect,after which external fixation was applied to both the blank group and the model group.On the 3rd,7th,14th and 28th days after the medications,eight rabbits randomly selected from various groups had their callus morphopathology changes observed under optical microscope,their callus tissue COX-2 mRNA expression levels were detected by realtime fluorescence quantitative polymerase chain reaction (qRT-PCR),and their callus tissue PGE2 and cAMP protein expressions were determined by immunohistochemistry.RESULTS Compared with the model group and the Qingpeng Ointment group,the Xiaoding Ointment group exhibited significantly better formation of callus and collagen fibers.The mRNA expression of COX-2,and the protein expressions of PGE2 and cAMP in the Xiaoding Ointment group were remarkably enhanced as revealed on the 7th and 14th days' postoperative check (P ＜ 0.05),and the peak values arrived around the 14th day after the operation.CONCLUSION Xiaoding Ointment's obvious effect on promoting fracture healing may associate with its impact on COX-2/PGE2/cAMP signaling pathway.
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Objective To observe the effects of capsaicin on PGE2 concentration of IL-1β-induced human large cell carcinoma NCI-H460 cells,and further observe its effect on COX-2 and mPGES-1 so as to explore the possible mechanisms against non-small cell lung cancer.Methods NCI-H460 cells were cultured in vitro ;the effect of capsaicin in inhibiting NCI-H460 cells proliferation was observed.The 50% inhibitory concentration (IC50 ) was measured by MTT assay.IL-1βstimulation method was used to construct inflammation model,and the effects of capsaicin on COX-2 activity and PGE2 concentration in NCI-H460 cells were measured by ELISA.The effects of capsaicin on COX-2 and mPGES-1 protein level in NCI-H460 cells were analyzed by Western blot;the effects of capsaicin on COX-2 mRNA and mPGES-1 mRNA expressions in NCI-H460 cells were analyzed by Real-time PCR. Results MTT assay results showed that the growth of NCI-H460 cells treated with capsaicin was significantly inhibited compared with the control group (P <0.05 or P <0.01 ).Capsaicin could significantly decrease COX-2 activity and PGE2 concentration in NCI-H460 cells,and significantly decrease COX-2,mPGES-1 protein levels as well as COX-2,mPGES-1 mRNA expressions in NCI-H460 cells in a dose-dependent manner compared with the control group (P < 0.05 ).Conclusion Capsaicin inhibits the release of PGE2 by downregulating COX-2 and mPGES-1 mRNA expressions in NCI-H460 cells,which may be one mechanism of its effect against non-small cell lung cancer.
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AIM: To study the effect of Qingqi Liangying Injection on febrile rats induced by zymonsa and on content of PGE_2 as well as cAMP in rat hypothalamus. METHODS: The rat febrific model induced by 10% zymonsa solution was used to observe QingqiLiangying Injection's effect on the rat temperature, and the radioimmunoassay(RIA) was used to determin the content of PGE_2 and cAMP in hypothalamus of rats. RESULTS: Qingqi Liangying Injection had an obvious antipyretic effect on febrile rats; Qingqi Liangying Injection could significantly reduce the content of PGE_2 and cAMP. CONCLUSION: Qingqi Liangying Injection can obviously reduce the rat body temperature and the content of PGE_2 and cAMP in hypothalamus of rats.
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AIM: To evaluate the effects of rutae-carpine on ulcerative colitis and intestinal movement in experimental animals. METHODS: The mouse model of acute colitis was induced by coionic instillation of dinitro-chlorobenzene (DNCB)/alcohol. Rutaecarpine (10, 30, and 100 mg?kg-1 ) were orally administrated to animals for 3 days. Diarrheas, colon weight index, macroscopic damage in the colon were observed and the activity of MPO and the content of PGE2 in colon were also examined . Meanwhile, the inhibitory effects of rutaecarpine on ileal contraction movement in Guinea pig which was induced by acetylcoline or histamine in vitro were examined. RESULTS: The diarrhea and the colon weight index were reduced and the macroscopic damage in the in-flammatory colon was effectively attenuated by rutae-carpine. The elevated level of MPO and PGE2 were also significantly decreased. Heal contraction movement induced by acetylcoline or histamine in vitro was strongly dose-dependent inhibited by rutaecarpine. CONCLUSION: Rutaecarpine can effectively inhibit the inflammatory infiltration, bleeding and proliferation in experimental ulcerative colitis and the movement of intestinal smooth muscle. Rutaecarpine may be an effective drug in treating inflammatory bowel diseases in clinic.
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Objective:In this experiment we used pain-related neurons of Hb unit discharges recording asa standard to observe the effects of prostaglandin E2 (i. p. ) on Hb unit discharges. Methods :The methodsof unit discharges recording and radiant heat induced tail flick responce were used. Results :The dischargesof pain-excited neurons increased after the addition of PGE2 (i. p. ). The discharges of pain-inhibited neu-rons dec reased after the addition of PGE2(i. p. );PGE2(i. p. ) caused the pain threshold to drop after sym-pathetic nerves were destroyed by 6-OHDA. There were no changes of the pain threshold in undestroyedgroup (P＞0.05). The percentage changes of Hb neurons dropped compared with that of undestroyedgroup (P＜0. 05). Conclusion: The PGE2 could change the discharges of pain-related neurons in Hb, inwhich the sympathetic system might participate in the process.
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OBJECTIVES: The trial was performed to obtain an unbiased comparison of the relative merits of endocervical and vaginal prostaglandin E2(PGE2) in the case of parous and nulliparous woman with favorable and unfavorable cervical features. This study was performed to determine the clinical usefullness of endocervical PGE2 comparing with the vaginal PGE2 in cervical ripening and induction of labor. METHOD: The randomized trial with 65 Participants was performed with sealed envelopes for parity and Bishop score (from March to september, 1998). PGE2 tablet(3mg Dinoprostone) was administrated intravaginally to the 32 pregnant women and endocervically to the 33 pregnant women every eight hours with maximum three times until the regular labor develped. RESULT: Outcomes of labor and delivery were clearly related to cervical score at trial entry. endocerval PGE2 had a more marked effect on cervical ripeness than did vaginal PGE2. There were no significant differences on age distribution, gestatioanal period, primiparity, cervical status, initial B-score in each group. There were no significant differences in cesarian section rate, fetal distress, uterine hyperstimulation, side effect and poor infant outcome between the groups The mean induction time was statistically shorter in cervical group with multiparous women than other group(p=0.0195). In the induction-active labor time, cervical with primi group was statistically shorter than other group(p=0.0245). Statistically significant differences were noted between the nulliparous woman and multiparous women in mean induction time, induction-active labor time, time to B-score 8. In the factor that effects induction-active labor, route was significantly better than other factor.(p=0.0001) CONCLUSION: edocervical PGE2 is more effctive than vaginal PGE2 in cervical ripening and induction of active labor. the endocervical PGE2 resulted in a significantly shorter induction to active labor time compared with vaginal PGE2 and has almost no side effect. Because differences in effectiveness between endocervical and vaginal PGE2 are marginal, preference of woman and clinicians can the choice between them.
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Female , Humans , Infant , Pregnancy , Age Distribution , Cervical Ripening , Dinoprostone , Fetal Distress , Parity , Pregnant WomenABSTRACT
Objective:To study the effects of green-tea polyphenol, (epigallocatechin gallate,EGCg) on the cellular inflammatory responses of gingival epithelial cells. In order to find out a safe and efficient inflammation-inhibitor for periodontitis prevention and treatment. Methods:A model of cellular inflammatory responses of gingival epithelial cells stimulated by Porphyromonas gingivalis vesicles in vitro was established. The effects of EGCg on PGE2 production of gingival epithelial cells was detected by ELISA. Further more, the effects of EGCg on COX (cyclooxygenase)-2 and MMP (matrix metalloproteinase)-3 mRNA expression were determined by Real-time RT-PCR. Results:EGCg dose-dependently inhibited PGE2 production and COX-2, MMP-3 mRNA expressions. Conclusion:EGCg has inhibitory effects on cellular inflammatory responses of gingival epithelial cells and possesses the potentiality to be a periodontal inflammation-inhibitor.
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Objective To observe the effects of tetramethylpyrazine (TMP) on acute nociception in rat hindpaw induced by purine 2X (P2X) receptor agonists, such as adenosine triphosphate (ATP) and ?, ?-meATP, prostaglandin E 2 (PGE 2), and substance P (SP). Methods The effects of TMP administered intraplantarlly on the acute nociception induced by P2X receptor agonists, PGE 2, or SP in the rat hindpaw were investigated by the method of the behavioral study. Results TMP (10 mmol/L) significantly depressed the acute nociception induced by ATP (1 ?mol/L) or ?, ?-meATP (0.6 ?mol/L) in the rat hindpaw. TMP (10 mmol/L) could inhibit the acute nociception induced by PGE 2 (5 ?mol/L) or ?, ?-meATP (0.2 ?mol/L) coinjected with PGE 2 (5 ?mol/L). TMP (10 mmol/L) could not affect the acute nociception induced by ?, ?-meATP (0.2 ?mol/L) coinjected with SP (10 ?mol/L). TMP could not obviously affect the inflammatory edema in rat hindpaw induced by the local administration of PGE 2, SP, or ?, ?-meATP coinjected with PGE 2 or SP individually. Conclusion The antinociceptive effects of TMP may mainly be associated with inhibiting the transmission of nociceptive information mediated by P2X receptor activation.
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The total aralosides extracted from Aralia elata (Miq) Seem. were studied in mice ( 50 mg/kg/d for 7 d ) to investigate the pharmacological mechanisms on the molecular level.The results showed that aralosides can obviously stimulate the production of PGE2、PGF2, and cAMP but reduce the cGMP level and nave no effect on histamine release.It is suggested that the changes in the level of cyclic nucleotide might be due to the alternations of PGs, which is now been suspected as the "Second Messenger" . These findings could explain in part the pharmacological activities of aralosides on the molecular level.