Objective To investigate the affecting mechanism of Jie Yu No.1 Decoction(JY),which was a complex prescription with the function of adjusting spleen and stomach,on the HPA-axis function of depression model rats.Methods60 SD rats were randomly divided into the normal,the model,the Amitriptyline and the JY decoction groups,with 15 each.Isolated-living condition and chronic mild unpredictable stress were applied suceessively to set up DEP rat model.Radiative immunotherapy was used to measure the content of hormone(CRH),somatostatin(SS) and Cortisol(CORT) in the blood plasma.The correlativity was Analyzed between SS,CRH and CORT to preliminary discuss the affecting mechanism of JY on the function of SS adjusting HPA-axis,and to clarify the antidepressant mechanism of the JY.ResultsThe correlation coefficient between SS and CRH was r=-0.5094,P=0.1972,t=1.4501.The result indicated that SS and CRH had the remarkable negatively correlation.The correlation coefficient between SS and CORT was r=0.010,P=0.9613,t=0.0244.The result indicated that SS and CORT had no remarkable correlation.ConclusionThe antidepressant mechanism of JY may be as that SS reduces CRH contents and reaches the adjustment of HPA-axis function in order to play its antidepressant effect.

Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.
Adenosine Diphosphate ; Drug Design ; Phthalic Acids ; Platelet Aggregation ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship ; Sulfonamides ; chemical synthesis ; chemistry

Twelve compounds were isolated from the aerial parts of Achillea alpina by column chromatographies on silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures were elucidated on the basis of spectral analysis. The compounds were identified as pellitorine(1), 8,9-dehydropellitorine(2), (E,E)-2,4-undecadien-8, 10-diynoic acid isobutylamide(3), (E,E)-2,4-tetradecadien-8,10-diynoic acid isobutylamide(4),sintenin(5), 4',5,7,8-tetramethoxyflavone(6), chrysoplenetin(7), formononetin(8), aurantiamide(9), asperglaucide(10), artemetin(11), and eupatorin(12). compounds 1-5 were isolated from this plant for the first time, and compounds 6-10 were isolated from the genus Achillea for the first time.
Achillea ; chemistry ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

OBJECTIVETo explore the clinical anesthesia value of transcutaneous acupoint electrical stimulation (TAES) combined with general intravenous anesthesia in endoscopic bilateral thyroidectomy patients.

METHODSTotally 60 patients who underwent endoscopic bilateral thyroidectomy were equally randomly assigned to 2 groups, the treatment group and the control group, 30 in each group. Patients in the treatment group received TAES combined general intravenous anesthesia, while those in the control group received total intravenous anesthesia. Anesthesia was maintained by target controlled infusion of propofolum combined constant speed infusion of remifentanil in the two groups. TAES was maintained from 30 min before anesthesia induction to the end of endoscopic thyroidectomy at bilateral Hegu (L14) and Neiguan (PC6). The mean artery pressure (MAP) and heart rate (HR) were recorded at different time points of anesthesia, i.e., immediately after entry into the operating room (TO), immediately after intubation (T1), 5 min after intubation (T2), 5 min before incision (T3), 5 min after incision (T4), 30 min after inflation (T5), at the end of surgery (T6), 5 min before extubation (T7), immediately after extubation 0 (T8), and 5 min after extubation (T9). The concentration of IL-6 and TNF-alpha were measured at TO, T3, T5, and T6. The target concentration of propofol was also recorded at T3, T4, and T5.

RESULTSThere was no statistical difference in the operation time between the two groups (P >0.05). Compared with TO in the same group, HR at T3-T4 decreased and increased at T8-T9, and MAP increased at T7-T9 in the treatment group; HR decreased at T3 and increased at T7-T9, MAP increased at T1, T5, T7-T9, and MAP decreased at T2-T3 in the control group. IL-6 increased at T5-T6, while TNF-alpha decreased at T6 in the two groups (P <0.01,P <0.05). Compared with the control group at the same time point, HR decreased at T6-T9, MAP decreased at T1, T4, T5, T7-T9, MAP increased at T3, and IL-6 decreased at T5-T6 in the treatment group (P <0. 05). The concentration and the total amount of propofol were significantly lower in the treatment group than in the control group (P <0.01,P <0.05).

CONCLUSIONSTAES could maintain the hemodynamics more stably and inhibit the stress response in endoscopic thyroidectomy. It also reduce the dosage of anesthetics and improve the safety of anesthesia.

Acupuncture Points ; Anesthesia, General ; Anesthesia, Intravenous ; Electric Stimulation ; methods ; Endoscopy ; methods ; Heart Rate ; Hemodynamics ; Humans ; Interleukin-6 ; Piperidines ; Propofol ; Thyroidectomy ; methods ; Transcutaneous Electric Nerve Stimulation ; Tumor Necrosis Factor-alpha

In recent years, root rot diseases of Chinese herbal medicine have been posing grave threat to the development of the traditional Chinese medicine industry. This article presents a review on the occurring situation of the root rot disease, including the occurrence of the disease, the diversity of the pathogens, the regional difference in dominant pathogens,and the complexity of symptoms and a survey of the progress in bio-control of the disease using antagonistic microorganisms. The paper also discusses the existing problems and future prospects in the research.
Animals ; Antibiosis ; Bacteria ; growth & development ; Fungi ; physiology ; Nematoda ; growth & development ; Pest Control, Biological ; methods ; Plant Diseases ; microbiology ; parasitology ; prevention & control ; Plant Roots ; microbiology ; parasitology ; Plants, Medicinal ; microbiology ; parasitology

AIM To investigate the effect of fenofibrate and simvastatin on the serum free fatty acids of alcoholic fatty liver in rats. METHODS The rat model of alcoholic fatty liver was reproduced by chronic ethanol ingestion plus olive oil diet. The model rats were divided into three groups as follows: finofibrate treatment group(finofibrate 80 mg?kg -1 po, once a day),simvastatin treatment group (simvastatin 4 mg?kg -1 po, once a day)and control group without either above-mentioned treatment. Experimental rats were treated for four weeks and then sacrificed for blood sampling. Serum free fatty acids were analyzed by gas chromatography. RESULTS Fenofibrate significantly ameliorated the decrease in polyunsaturated fatty acids induced by ethanol [oleic acid:(38.212?7.788) ?g?L -1 vs (31.620?6.142) ?g?L -1,linoleic acid:(37.269?8.065) ?g?L -1 vs (30.254?9.063) ?g?L -1,arachidonic acid:(11.646?2.601) ?g?L -1 vs (9.012?1.236) ?g?L -1] accompanied by the improvement of the fat infiltration of the liver, but demonstrated no effect on the increase in serum saturated fatty acids by ethanol. In the contrast, simvastatin can aggravate the decrease in polyunsatrurated fatty acids and significantly increase the levels of satrurated fatty acids in serum induced by ethanol along with the pathological aggravation of alcoholic fatty liver. CONCLUSION The results of present study revealed that fenofibrate and simvastatin exerted different effect on the serum free fatty acids of alcoholic fatty liver. Polyunsatrurated fatty acids in the serum play an important role in the pathogenesis and treatment response of alcoholic fatty liver.

This paper is aim to investigate the pharmacokinetics and absolute bioavailability of neoline in Beagle dogs, and provide a theoretical basis for further study. Ethyl acetate was used for liquid-liquid extracting after 10% ammonia alkalizing. The method of UPLC-Q-TOF-MS was established for the determination of neoline plasma concentrations. Beagle dogs were orally or intravenously administered with neoline for pharmacokinetic and absolute bioavailability study. Good linear relationship of neoline was found over the range of 0.1-4 mg x L(-1) (R2 = 0.9982) and 2-100 microg x L(-1) (R2 = 0.9945). Intra-and inter-day precision, expressed as the relativestandard (RSD) were less than 5.0%. Accuracy, expressed as the relative error (RE) was within 90.0%-115%. The recovery of neoline in dog plasma was more than 80%. After 6 mg x kg(-1) for ig and 1 mg x kg(-1) for iv administration of neoline, the main pharmacokinetic parameters were analyzed with Winnonlin software. t(1/2) were (313.88 +/- 63.18), (236.33 +/- 229.84) min, and AUC(0-infinity) were (58,027.40 +/- 14,132.69), (473,578.02 +/- 82,333.08) min x microg x L(-1) for ig and iv administration respectively. The absolute bioavail ability was (73.15 +/- 10.29) %. The method of UPLC-Q-TOF-MS described in the report was sensitive, reliable and specific, and suitable for pharmacokinetic study of neoline in Beagle dog. The high absolute bioavailability of neoline in dog suggested good absorption of neline which was worth of further investigation.
Aconitine ; analogs & derivatives ; chemistry ; pharmacokinetics ; Animals ; Biological Availability ; Dogs ; Drug Stability ; Female ; Male

Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.

This paper is to report the study of the metabolism of forscolin in plasma and liver microsomes for guiding clinical therapy. Forscolin was quantified by HPLC-MS/MS. The metabolic stability of forscolin in rat, Beagle dog, monkey and human plasma and liver microsomes, mediated enzymes of forscolin and its inhibition on cytochrome P450 isoforms in human liver microsomes were studied. Results showed that forscolin was not metabolized in plasma of the four species but metabolized in liver microsomes of the four species. The t1/2 of forscolin in rat, Beagle dog, monkey and human liver microsomes were (52.0 +/- 15.0), (51.2 +/- 5.9), (6.0 +/- 0.2) and (11.9 +/- 1.8) min; CL(int) were (75.6 +/- 18.7), (60.9 +/- 6.8), (513.8 +/- 14.3) and (176.2 +/- 25.6) mL x min(-1) x kg(-1); CL were (34.8 +/- 4.5), (23.3 +/- 1.0), (40.3 +/- 0.5) and (17.9 +/- 0.3) mL x min(-1) x kg(-1), respectively. Forscolin was metabolized by CYP3A4 in human liver microsomes. There was definite inhibition on CYP3A4 at the concentrations of forscolin between 0.1 ng x mL(-1) and 5 microg x mL(-1). Therefore, forscolin is rapidly excreted from liver microsomes. Attention should be paid to the drug interaction when forscolin was used along with other drugs metabolized by CYP3A4 in clinics.
Animals ; Chromatography, High Pressure Liquid ; Coleus ; chemistry ; Colforsin ; blood ; isolation & purification ; metabolism ; Cytochrome P-450 CYP3A ; metabolism ; Dogs ; Humans ; Macaca ; Metabolic Clearance Rate ; Microsomes, Liver ; metabolism ; Plants, Medicinal ; chemistry ; Rats ; Tandem Mass Spectrometry

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.
Bacillus subtilis ; metabolism ; Biotransformation ; Fermentation ; Flavanones ; metabolism ; Flavonoids ; metabolism ; Glucosides ; metabolism ; Soy Foods ; microbiology