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OBJECTIVE：To study the improvement ef fects of sanggenone C on lipid accumulation in human liver cancer HepG2 cells induced by free fatty acid （FFA）. METHODS ：HepG2 cells were divided into control group ，model group ， fenofibrate group （10 μmol/L），sangerone C low ，medium and high concentration groups （2，4，8 μmol/L）. Except for control group，other groups were treated with 1 mmol/L FFA to induce lipid accumulation model ，and administration groups were cultured with relevant medium containing drugs. The lipid accumulation was observed by oil red O staining ，and lipid level and triglyceride （TG） content were also determined. Real-time PCR and Western blot assay were adopted to detect the mRNA and protein expression of PPARα，CPT-1，SREBP-1c，FAS，SIRT1 and PGC- 1α in HepG2 cells. RESULTS ：Compared with control group ， the nucleus was atrophied significantly and the volume became smaller ，and the number of lipid droplets was significantly increased；the level of lipid ，TG content ，mRNA and protein expression of SREBP- 1c and FAS were significantly increased （P＜ 0.05 or P＜0.01），mRNA and protein expression of PPARα，CPT-1，SIRT1 and PGC- 1α were decreased significantly（P＜0.01）. Compared with model group ，no obvious nucleus atrophy and normal volume were observed in sangerone C groups ，and the number of lipid droplets was significantly reduced ；the levels of lipid ，TG content ，mRNA and protein expression of PPARα pathway related genes （except for SREBP- 1c protein in saggenone C low concentration group ）were significantly reversed （P＜ 0.05 or P＜0.01）. CONCLUSIONS ：Sangenone C can significantly improve the lipid accumulation of HepG 2 cells，and its mechanism may associated with regulating PPAR α signaling pathway，improving cell lipid oxidation ability and inhibiting lipid synthesis.
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SAbstact:Objective To establish a method for detecting t he pharmacokinetic parameters of te tramethylpyragine(TMPz ),the main active component in Xiongbing nasal spray(A),Chuanxiong nasal spray(B)and Xiongbing decoction(C),in the rat brain .Methods Gas chromatography was applied for pharmacokinetic analysis of TMPz in v arious time after nasal administration or gastr ic infusion.Results The concentration -time process of A can be described in an open two -department model,which is simi lar to the process of intravenous adm inistration.As compared with B and C,A has its characteristics:quick absorpt ion,quick distribution and quick excretion of TMPz.TMPz passed through blood -brain barrier almost right after administration,and reach the peak concentra tion 1minute after the administrati on.95.7%of TMPz was cleared from brain within 1.5h.Conclusion The application of Borneolum makes T MPz of A enter into the rebral tissue easily.Therefore Xiongbing nasal spray is a quick -effective pre paration for acute ischemic stoke an d can be medicated repeatedly.
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Objective To compare the pharmacokinetics of borneolum syntheticum(BS)and borneol in compound Danshen dropping pills in rats.Method Rats were administrated orally with BS or Danshen dropping pills containing equal amount of borneol in a single dose.The blood contents of borneol at a series of time points were assayed by GC-MS and GC-FID after administration.The drug-time curve was estimated by PK Solution 2.0 pharmacokinetic software(USA).Results The pharmacokinetic parameters are quite different between the single dose of BS and the borneol in the compound Danshen dropping pills:the velocity constants of absorption(2.630h-1),distribution(1.788 h-1)and elimination(0.273 h-1)of BS were much greater than those(1.635h-1,0.784h-1,0.116h-1)of the same quantity of borneol in compound Danshen dropping pills,while the Tmax(0.5 h)of former was shorter than that(0.75 h)in the latter,and the Cmax(16.8 ?g/mL)in the former was about half of the latter(31.02 ?g/mL).And,at the 18h after administration,the former blood concentration(0.043 ?g/mL)was approximately one tenth of the latter.Conclusion It is suggested that we should pay attention to the influence of other ingredients on the main objective component in the study of pharmacokinetics of compound traditional chinese drug.
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Objective To isolate and purify the antioxidant compounds from fructus xanthii and to study their antioxidant activity.Methods Compounds were isolated by repeated silica gel,macroreticular resin Diaion HP-20 and Sephadex LH-20 column chromatography and their antioxidant property was determined by scavenging activity to DPPH and ?OH.Results Five antioxidant compounds were isolated from the ethyl acetate extracts of Xanthium sibiricum fruits and their structures were identified as 5,7,3',4'-tetramethoxyisoflavone,myricetin-3'-methyl ether,falcalindiol,1,8-heptadecadiene-4,6-diyne-3,10-diol and 3,4-dihydroxybenzoic acid.Among them,3,4-dihydroxybenzoic acid had the highest radical scavenging activity.Conclusion All above 5 compounds have high antioxidant activities,and antioxidant activity of 3,4-dihydroxybenzoic acid is the highest.
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Objective To establish a method for extracting compounds in Fructus Xanthii by accelerated solvent extraction(ASE),and to simultaneously determine the compounds by GC-MS.Methods The extraction was performed by ASE in which the conditions were optimized by orthogonal test,then the compounds in different extracts with different polarity were determined by GC-MS.Results The optimized conditions of ASE for compounds in Xanthium sibiricum fruits were as follows: petroleum ether,ethyl acetate and methanol as extracting solvent in turn in 33 mL extracting tube and the volume of solvent being 65 mL;6 g sample,9 MPa of extracting pressure,90 ℃of extracting temperature,5 min of extracting time,two cycles and one time for each extraction.The GC-MS conditions were as follows: 1 ?L extract was analysed by GC-MS(Shimadzu Model QP-2010) instrument fitted with a flame ionisation detector,separation was achieved on a DB-5ms,DB-17ms and DB-WAX column(J&W Scientific,30 m,0.25 ?m id film thickness,1.4 ?m,USA) respectively,the column temperature was maintained at 60 ℃for 3 min and increased to 250 ℃,the scanning range was from m/z 40 to m/z 700(scanning interval: 0.5 s),and the compounds were identified by searching NIST and Wiley registry of mass spectral data.Conclusion There are 61 compounds found in the petroleum ether extract and in which 48 are identified,22 in the ethyl acetate extract and 18 identified,as well as 34 in the methanol extract and 29 identified with the methods of optimized ASE combined with GC-MS.
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The concentrations of borneol in the serum and brain tissue of rats were determined by gas chromatography. Using brain tissue as a relatively independent system, PHARMFIT and PCNONLIN softwares are applied for the kinetic analysis of the infracorporal process of borneol in order to find out and compare the pharmacokinetic characteristics of borneol in the brain and serum. The results showed that borneol was absorbed very rapidly in the gastrointestinal tract and readily permeates the blood-brain barrier into brain tissue. There was a higher specific value of borneol concentration in the brain and serum. Moreover, the half life of distribution phase of borneol in the brain was three times higher than that in the serum. But the constants of elimination rate of borneol in the brain and serum decreased simultaneously and parallelly, hence the accumulation of borneol in brain will not be found.