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Fourteen compounds were isolated from the ethyl acetate fraction of 90% EtOH extracts of the dried fruits of Alpinia oxyphylla by silica gel, MCI, RP-18, Sephadex LH-20, TLC and semi-preparative HPLC column chromatography. Their structures were identified by HR-ESI-MS, UV, IR, NMR, ECD and X ray single crystal diffraction spectroscopic data as: (2R,5R,7R,10S)-2,7-dihydroxyl-eudesmane-3(4),11(12)-diene (1), α-rotunol (2), diketone I (3), (1S,4S,5R,7S)-1-hydroxyl-eremophilane-9(10),11(12)-diene-8-one (4), cyperusol A1 (5), (6R,9S,10S)-10-hydroxyl-11,12,13-trinor-cadinane-4(5)-ene-3-one (6), (2E,4E)-6-hydroxy-2,6-dimethylhepta-2,4-dienal (7), oxyphyllacinol (8), yakuchinone A (9), (5R)-5-hydroxy-1,7-diphenylhept-3-heptanone (10), (5S)-5-hydroxy-7-(4″-hydroxyphenyl)-1-phenylhept-3-heptanone (11), (5S)-5-hydroxy-7-(4″-hydroxyl-3″-methoxyphenyl)-1-phenyl-3-heptanone (12), 7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-3,5-heptadione (13), bis-(2-ethylhexyl) terephthalate (14). Compounds 1-6 were sesquiterpenoids in which compound 1 is a new eudesmane sesquiterpenoid and compound 7 was a monoterpenoid. Compounds 8-13 were diarylheptanoids, and compounds 2-6 and 14 were isolated from A.oxyphylla for the first time. The experiments on H2O2 induced SH-SY5Y cells showed that compounds 2, 6, 7, 12 and 13 had neuroprotective effects at low and medium concentrations. In particular, compound 6 showed obvious neuroprotective effect at low, medium and high concentrations whose cell viability was higher than that of the positive control.
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OBJECTIVES@#To explore the possible mechanism of Yunaconitine poisoning by studying the changes of urine metabolic profile in rats chronically poisoned by Yunaconitine via non-targeted metabolomics.@*METHODS@#A rat model of Yunaconitine poisoning was established, and a metabolomics method based on UPLC-QTOF-MS technology was used to obtain the urine metabolic profile. Principal component analysis (PCA), orthogonal projections to latent structures-discriminant analysis (OPLS-DA), variable importance in projection (VIP) value greater than 1, fold change (FC) value greater than 3 or less than 0.33 and P value less than 0.05 were used to screen potential biomarkers related to the toxicity of Yunaconitine. The metabolic pathway analysis was performed through the MetaboAnalyst website and pathological changes of related tissues were observed.@*RESULTS@#Sixteen potential biomarkers including L-isoleucine were screened, which mainly involved six metabolic pathways including the biosynthesis and degradation of valine, leucine and isoleucine, pentose and glucuronate interconversions, and propanoate metabolism, alanine, aspartate and glutamate metabolism, tyrosine metabolism. Pathological studies showed that rat toxic change in nervous system, liver and cardiac caused by Yunaconitine.@*CONCLUSIONS@#Yunaconitine may cause neurotoxicity, hepatotoxicity and cardiotoxicity by affecting amino acid and glucose metabolism.
Subject(s)
Animals , Rats , Aconitine/analogs & derivatives , Biomarkers/metabolism , Chromatography, High Pressure Liquid , Metabolome , MetabolomicsABSTRACT
Aim To explore the mechanism of Fluspirilene inhibiting HCC through decreasing the expression of Akt.Methods The difference of mRNA was verified by the test of protein expression between Fluspirilenc treatment group and control group by HCC experiment in vivo and vitro, including Western blot, IHC after mRNA array.Results Akt expression was lower in Fluspirilene treatment group than that in control group by mRNA array.Protein expression of Akt, phosphorylate-CDK2 and phos- phorylate-Rb decreased massively in Fluspirilene treatment group in a concentration-dependent manner in HepG2 and Huh7 cells by Western blotting compared with those in control group.Declined expression of phosphorylate-Akt was proved in a concen- tration-dependent manner in xenograft tumor tissues in Fluspirilene treatment group compared with that in control group in IHC test.Conclusions Fluspirilene inhibits HCC by decreasing significantly the protein expression of Akt, phosphorylat-Akt, phos- phorylate-CDK2 and phosphorylate-Rb.
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Ischemia-reperfusion (IR) is one of the significant medical problems in China. Triphenyltetrazolium chloride (TTC) stainingis used to detect the status of the infarct size, and real-time PCR and western blotting are used to detect expressions ofgenes. TUNEL assay has been used to detect apoptosis. Using a tree shrew myocardial IR model, we found that in thereperfusion period, resina draconis (RD) treatment reduced the infarct size by TTC staining, and significantly enhanced thesuperoxide dismutase expression and down-regulated the malondialdehyde concentration in a dose-dependent manner. Inhearts showing IR, Bax was increased and Bcl-2 was reduced, and RD treatment inhibited the IR-induced Bax expressionand up-regulated the IR suppressed level of Bcl-2. TUNEL assay showed that IR induced the apoptosis of myocardial cells,and RD treatment suppressed the IR-induced apoptosis. CHOP and GRP78 were also upregulated in IR hearts, and RDtreatment could significantly attenuate the CHOP and GRP78 levels compared with IR group. We further found that IRdecreased the miR-423-3p expression and upregulated its target gene ERK both in mRNA and protein levels, and RDtreatment upregulated miR-423-3p expression and downregulated ERK expression compared with the IR group. Importantly, miR-423-3p mimics inhibited IR increased ERK, CHOP and GRP78 expressions, and enhanced IR decreased Bcl-2expression, and inhibited the IR-induced apoptosis of myocardial cells. The findings of this study suggest that RD treatmentinhibited the endoplasmic reticulum induced apoptosis of myocardial cells via regulating miR-423-3p/ERK signalingpathway in a tree shrew myocardial IR model.
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<p><b>OBJECTIVE</b>To establish an ex vivo model of myocardial ischemia reperfusion in tree shrews.</p><p><b>METHODS</b>The Langendorff ex vivo heart perfusion system was used to establish the myocardial ischemia reperfusion model in tree shrews with different irrigation and reperfusion time settings. Alanine aminotransferase (ALT), aspartate transaminase (AST) and lactic dehydrogenase (LDH) levels were measured by enzyme-labeled immunosorbent assay, creatine kinase MB (CK-MB) was detected using immunosuppression method, and malondialdehyde was measured with thiobarbital staining method; the infarct size was measured using 2, 3, 5-triphenyltrazoliumchloride (TTC) method.</p><p><b>RESULTS</b>Ischemia for 30 min and reperfusion for 30 and 60 min caused more significant increase in CK-MB and LDH levels in the perfusion fluid and also in the levels of ALT, CK-MB and AST in the myocardial tissue compared with other experimental settings (P<0.05), but these parameters were comparable between the former two settings (P>0.05). The mean heart rate in 30-min ischemia with 60-min reperfusion group was obviously lower than that in continuous reperfusion group, 15-min ischemia with 30-min reperfusion group and 30-min ischemia with 30-min reperfusion group (P<0.05), and the heart rate was similar between the latter 3 groups (P>0.05). ECG analysis showed that the mean heart rate in 30-min ischemia with 30-min reperfusion group was closer to the physiological heart rate of tree shrews.</p><p><b>CONCLUSION</b>We successfully established an ex vivo myocardial ischemia reperfusion model using tree shrews, and ischemia for 30 min followed by reperfusion for 30 min is the optimal experimental setting.</p>
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This experiment aimed to explore and research the process of preparing baicalein and wogonin through liquid fermentation with Bacillus natto. Active enzymes of produced by B. natto was used for the biological transformation of baclin and wogonoside, in order to increase the content of the haicalein and wogonin in the scutellaria. With the content of the baicalein and wogonin as evaluating indexes, the effects of carbon source, nitrogen source, the types and suitable concentration of inorganic salt, medium pH, granularities of medical materials, liquid volume in flask, shaking speed, liquid-to-solid ratio, fermentation time on the fermentation process were studied. The optimal process conditions for liquid fermentation of scutellaria were 1.0% of peptone, 0.05% of NaCl, pH at 6, the granularities of medical materials of the scutellaria screened through 40-mesh sifter, 33% of liquid, shaker incubator speed at 200 r x min(-1), liquid-to-solid ratio of 5:1, temperature at 37 degrees C, fermentation for 6 days, baclin's conversion rate at 97.6% and wogonoside's conversion rate at 97% in the scutellaria. According to the verification test, the process was stable and feasible, and could provide data reference for the industrial production.
Subject(s)
Bacillus subtilis , Metabolism , Biotransformation , Fermentation , Flavanones , Metabolism , Flavonoids , Metabolism , Glucosides , Metabolism , Soy Foods , MicrobiologyABSTRACT
Laggera pterodonta is commonly used for treating influenza in Southwest China, especially in Yunnnan province. The main clinical effects of L. pterodonta include anti-influenza, anti-microbial, anti-inflammatory. To investigate the anti-influenza A (H1N1) virus effect of L. pterodonta, neutralization inhibition and proliferation inhibition tests were performed. MDCK culture method was used to observe the cytopathic effect (CPE) of extracts from L. pterodonta in inhibiting influenza A (H1N1) virus and haemagglutination titre of H1N1 virus in vitro. The culture medium were collected at 24 h, 48 h, 72 h, 96 h, and detected by Real time RT-PCR, in order to compare the effect of different extracts from L. pterodonta on in vitro proliferation of H1N1, virus. The result of neutralization inhibition test showed that hemagglutination titer of ethyl acetate extract were 8 times lower at 72 h; in proliferation inhibition test, hemagglutination titer of ethyl acetate extracts reduced by 2 and 4 times. According to the results of Real time RT-PCR test, the H1N1 inhibition ratio of ethyl acetate extract was 72.5%, while the proliferation inhibition ratio of ethyl acetate extract was 25.3%; as for petroleum ether extracts, the H1N1 inhibition ratio was 60.2%, while the proliferation inhibition ratio was 81.4%. In conclusion, both ethyl acetate extract and petroleum ether extract of L. pterodonta have significant neutralization and direct proliferation inhibition effects on influenza A virus.
Subject(s)
Humans , Asteraceae , Chemistry , China , Ethnology , Drugs, Chinese Herbal , Pharmacology , Influenza A Virus, H1N1 Subtype , Physiology , Influenza, Human , Drug Therapy , Virology , Medicine, Chinese TraditionalABSTRACT
<p><b>OBJECTIVE</b>To compare the event-related potentials (ERPs) waves of verbs and prepositions in the brain.</p><p><b>METHODS</b>We recorded ERPs in the brain while participants judged the legality of the collocation for verbs and prepositions.</p><p><b>RESULTS</b>Both verbs and prepositions elicited a negativity at the frontal site in 230-330 ms and 350-500 ms window. No difference was seen in 230-330 ms and 350-500 ms window; In difference waves, a negativity was elicited in the left and right hemisphere at about 270-400 ms and 470-600 ms window for both open and closed-class words.</p><p><b>CONCLUSION</b>These may demonstrate that prepositions in modern Chinese are probably not a separate class from verbs and that N280 may be not a specific component for only prepositions (or closed-class words).</p>
Subject(s)
Adult , Female , Humans , Male , Asian People , Brain , Physiology , Electroencephalography , Evoked Potentials , Physiology , Language , Photic Stimulation , ReadingABSTRACT
Aim & methods The antagonism of L-dicentrine to contraction of isolated porcine coronary artery strips induced by 5-HT KCl and Ca2+ was observed with U-135 electrophsiological recorder.Results The contractions induced by 5-HT KCl and Ca2+ after high K+ depolarization in the strips of porcine coronary artery were markediy inhibited by L-dicentrine.L-dicentrine significantly depressed maximal response and caused rightward displacement of the dose -response curve. Showing a non-competitive antagonism. In Ca2+ free solution,L-dicentrine inhibited 5-HT-induced contraction of porcine coronary artery,which is dependent on Ca2+ relesed from intracellular store. After Ca2+ concentration in bath solution was restored,L-dicentrine did not influence the contraction of porcine coronary artery depending on extracellular Ca2+.Conclusion L-D have significant relaxation on porcine coronary artery ,which possibly has 5-HT receptor and histamine receptor.