Protective effects of Naoxintong capsule alone and in combination with ticagrelor and atorvastatin in rats with Qi deficiency and blood stasis syndrome.

CONTEXT: Naoxintong Capsule (NXT), a Chinese medicine, has been widely used for the treatment of coronary heart disease (CHD) in clinics. OBJECTIVE: This study evaluated the cardioprotective effects of NXT alone and in combination with ticagrelor (TIC) and atorvastatin (ATO). MATERIALS AND METHODS: Qi deficiency and blood stasis rats were established by 8 weeks high fat diet feeding and 16 days exhaustive swimming and randomly divided into seven groups, that is, NXT (250, 500 and 1000 mg/kg/d), TIC (20 mg/kg/d), ATO (8 mg/kg/d), NXT (500 mg/kg/d)+TIC (20 mg/kg/d) and NXT (500 mg/kg/d)+ATO (8 mg/kg/d) group, with oral administration for 12 weeks. The contents of TC, TG, LDL-C, HDL-C, IL-1ß, IL-6, IL-8, TNF-α, AST, ALT, SOD, MDA, CK-MB, LDH, TXA2, PGI2, IgA, IgG, IgM and C3 in serum were measured. RESULTS: NXT + TIC group was significantly superior to the TIC group in decreasing the levels of TC (4.34 vs. 5.54), TG (3.37 vs. 4.66), LDL-C (1.21 vs. 1.35), LDH (4919.71vs. 5367.19) and elevating SOD level (248.54 vs. 192.04). NXT + ATO group was significantly superior to the ATO group in decreasing the levels of AST (195.931 vs. 241.63), ALT (71.26 vs. 83.16), LDH (4690.05 vs. 5285.82), TXA2 (133.73 vs. 158.67), IgG (8.08 vs. 9.80), C3 (2.03 vs. 2.35) and elevating the levels of HDL-C (1.19 vs. 0.91), SOD (241.91vs. 209.49). CONCLUSIONS: The present findings demonstrate that the combined use of NXT with TIC and ATO had better integrated regulating effects than TIC and ATO, respectively. The mechanism of action requires further research.

[Soil fertility characteristics and their influencing factors in tea plantations of Jiangxi Pro-vince, China]. / æ±Ÿè¥¿çœèŒ¶å›­åœŸå£¤è‚¥åŠ›ç‰¹å¾åŠå ¶å½±å“å› å­.

To investigate soil fertility status and characteristics of typical tea plantations, we selec-ted 372 typical tea plantations of 21 areas across Jiangxi Province and analyzed the soil nutrient, spatial data, and their correlations with topography, soil type, elevation and plantation age. The results showed that soil pH, organic matter, alkaline nitrogen, available phosphorus, available potassium, total nitrogen, total phosphorus and total potassium of tea plantation in Jiangxi reached 53.9%, 60.1%, 56.1%, 22.9%, 38.5%, 43.7%, 11.1% and 95.5% of indices of high fertility, high efficiency and high yield tea plantation, respectively, with the available phosphorus showing a strong variation. Soil available copper, zinc, iron, manganese and boron reached 76.3%, 74.2%, 96.8%, 73.1% and 0.0% of the first-class standards for soil trace elements, respectively. Tea plantations with highest soil fertility located in central Jiangxi, followed by northeastern and northwestern Jiangxi, and lowest in southern Jiangxi. Soil pH was significantly positively correlated with organic matter, alkaline nitrogen, available phosphorus, available potassium, total nitrogen and total phosphorus but not for total potassium. For different topography, soil fertility was highest in the flat land, followed by the high mountains, and lowest in the mountains and hills. Across different soil types, soil fertility was higher in paddy soil, sandy soil and mountain yellow brown soil, followed by yellow soil, red-yellow soil and purple soil, and lowest in red soil. Soil pH, organic matter and total potassium increased while available phosphorus decreased with altitude. The organic matter, alkaline nitrogen, available phosphorus, total nitrogen and total phosphorus increased, but soil pH decreased with time. In summary, soil fertility of tea plantations in Jiangxi Province was generally good, with high organic matter, total potassium, available copper, zinc, iron and manganese. However, soil was acidic, available phosphorus and total phosphorus content was low, available boron was seriously limited. We suggest increase soil pH and potassium supply in central Jiangxi, increase potassium and nitrogen fertilizer supply in northeastern Jiangxi, increase organic matter and phosphorus fertilizer supply in northwestern Jiangxi, and increase nitrogen, phosphorus and potassium supply combined with organic fertilizers in southern Jiangxi. High mountain tea plantations should enhance available phosphorus and potassium supply. Mountain tea plantations should enhance nitrogen and phosphate supply. Tea plantations with red and yellow soil should increase pH and total potassium supply. Tea plantations with red soil should apply nitrogen, phosphorus and potassium fertilizers combined with organic fertilizers. Tea plantations with yellow soil and mountain yellow brown soil required additional phosphorus supply, and tea plantations with purple soil should increase soil organic matter supply. Tea plantations need to increase dolomite powder, physiological alkaline fertilizers and organic fertilizers to prevent soil acidification.

Bufalin suppresses the migration and invasion of prostate cancer cells through HOTAIR, the sponge of miR-520b.

Bufalin, the major active component of the traditional Chinese medicine ChanSu obtained from the skin and parotid venom glands of toads, has long been known as an anticancer agent. Recent studies show that microRNAs (miRs) are involved in the anticancer activities of bufalin, while long non-coding RNAs (lncRNAs) are known to interact with miRNAs to regulate various biological functions. In this paper, we investigated the possible network related to the antimetastatic effect of bufalin in prostate cancer (PCa) cells. We demonstrated that bufalin (0.05-10 µM) dose-dependently suppressed the proliferation of prostate cancer DU145 and PC3 cells with IC50 values of 0.89 and 1.28 µM, respectively. Furthermore, bufalin treatment significantly suppressed the cell migration and invasion. To explore the role of lncRNAs in the antimetastatic activity of bufalin, we used an lncRNA microarray and found that HOX transcript antisense RNA (HOTAIR) was the most markedly downregulated lncRNA in bufalin-treated PCa cells. Overexpression of HOTAIR counteracted the suppressing effects of bufalin on DU145 and PC3 cells. We then predicted and verified that HOTAIR upregulated FGFR1 expression by sponging miR-520b in PCa cells. In 40 patients with PCa bone metastasis, we used in situ hybridization or immunohistochemical assay to assess the HOTAIR and FGFR1 expression, which revealed that both HOTAIR and FGFR1 expression were significantly higher in bone metastasis tissues than in the primary PCa tissues. In addition, the level of serum HOTAIR was positively associated with the levels of serum bone metabolic markers (CTx, OST, B-ALP and PINP) and may serve as a reasonable biomarker for PCa bone metastasis. Taken together, this is the first study revealing that HOTAIR promotes PCa bone metastasis, and bufalin may be a promising candidate for the treatment of this disease.

Chromatogram-Bioactivity Correlation-Based Discovery and Identification of Three Bioactive Compounds Affecting Endothelial Function in Ginkgo Biloba Extract.

Discovery and identification of three bioactive compounds affecting endothelial function in Ginkgo biloba Extract (GBE) based on chromatogram-bioactivity correlation analysis. Three portions were separated from GBE via D101 macroporous resin and then re-combined to prepare nine GBE samples. 21 compounds in GBE samples were identified through UFLC-DAD-Q-TOF-MS/MS. Correlation analysis between compounds differences and endothelin-1 (ET-1) in vivo in nine GBE samples was conducted. The analysis results indicated that three bioactive compounds had close relevance to ET-1: Kaempferol-3-O-α-l-glucoside, 3-O-{2-O-{6-O-[P-OH-trans-cinnamoyl]-ß-d-glucosyl}-α-rhamnosyl} Quercetin isomers, and 3-O-{2-O-{6-O-[P-OH-trans-cinnamoyl]-ß-d-glucosyl}-α-rhamnosyl} Kaempferide. The discovery of bioactive compounds could provide references for the quality control and novel pharmaceuticals development of GRE. The present work proposes a feasible chromatogram-bioactivity correlation based approach to discover the compounds and define their bioactivities for the complex multi-component systems.

Antioxidant Activity and Hepatoprotective Potential of Quercetin 7-Rhamnoside In Vitro and In Vivo.

Hypericum japonicum is traditionally used as a folk medicine to treat cholestasis and hepatitis. Quercetin 7-rhamnoside (Q7R) is one of the main flavonoid components of Hypericum japonicum and has been rarely studied. The aim of the present study was to evaluate the antioxidant activity and hepatoprotective potential of Q7R. In the in vitro experiments, DPPH, ABTS and ferric reducing antioxidant power (FRAP) assays were first performed to assess the antioxidant properties of Q7R, and then a H2O2-induced oxidative damage cellular model was used to determine the cytoprotective and antioxidant properties of Q7R in human liver L-02 cells. In the in vivo experiment, the hepatoprotective activity of Q7R was evaluated by carbon tetrachloride (CCl4)-induced liver damage model in mice. The results of the three in vitro assays (DPPH, ABTS and FRAP) demonstrated that Q7R significantly exhibited antioxidant activity. The cell experiment results showed that Q7R possessed cytoprotective and antioxidant effects on H2O2-treated L-02 cells. In the in vivo experiments, Q7R suppressed the up-regulation of serum activities of ALT, AST, LDH and triglyceride (TG) levels with dose-dependency. Q7R down-regulated the production of MDA and increased the hepatic GSH content and antioxidant enzymes CAT activities. Hepatic morphological analysis was also performed to confirm the biochemical changes. In summary, these results suggested that Q7R could be considered as a potential source of natural antioxidants, and may become a promising candidate for the treatment of liver injury in the future.

Hyperbaric oxygen inhibits production of CD3+ T cells in the thymus and facilitates malignant glioma cell growth.

Objective Hyperbaric oxygen (HBO) is an emerging complementary alternative medical approach in glioma treatment. However, its mode of action is unknown, so this was investigated in the present study. Methods We constructed an intracranial glioma model of congenic C57BL/6J mice. Glioma growth under HBO stimulation was assessed by bioluminescent imaging and magnetic resonance imaging. Flow cytometry assessed direct effects of HBO on reactive oxygen species (ROS) signaling of transplanted glioma cells and organs, and quantified mature T cells and subgroups in tumors, the brain, and blood. Results HBO promoted the growth of transplanted GL261-Luc glioma in the intracranial glioma mouse model. ROS signaling of glioma cells and brain cells was significantly downregulated under HBO stimulation, but thymus ROS levels were significantly upregulated. CD3+ T cells were significantly downregulated, while both Ti/Th cells (CD3+CD4+) and Ts/Tc cells (CD3+CD8+) were inhibited in tumors of the HBO group. The percentage of regulatory T cells in Ti/Th (CD3+CD4+) cells was elevated in the tumors and thymuses of the HBO group. Conclusion HBO induced ROS signaling in the thymus, inhibited CD3+ T cell generation, and facilitated malignant glioma cell growth in vivo in the intracranial glioma mouse model.

[Clinical observation of modified Da Chaihu decoction in treating essential hypertension with anxiety].

To observe the clinical efficacy of modified Da Chaihu decoction in treating essential hypertension with anxiety, the randomized, controlled, clinical trial was performed in this study. One hundred and twenty-six hypertensive patients with anxiety meeting the inclusive criteria were randomized into the treatment group and the control group. All of the included patients in the above 2 groups were treated by amlodipine besylate tablets. Patients in the treatment group were given Chinese herbal medicine modified Da Chaihu decoction every day. And patients in the control group were given flupentixol and melitracen tablets. The treatment course was 4 weeks. Blood pressure, the score of traditional Chinese medicine syndrome, blood lipids, C reactive protein, the Hamilton anxiety scale score and adverse effects were observed. It has been identified that, both systolic and diastolic blood pressure were significantly reduced (P<0.05). However, no significant difference between the treatment group and the control group was identified. For traditional Chinese medicine syndrome, it was significantly improved in the treatment group (P<0.05). For blood lipids, TC, TG, HDL-C, and LDL-C were significantly improved in the treatment group (P<0.05). After treatment, only TC was significantly reduced in the treatment group when compared to the control group (P<0.05). For C reactive protein, it was significantly reduced in the treatment group after treatment (P<0.05). For anxiety, no significant difference between the treatment group and the control group on the Hamilton anxiety scale score was identified. For adverse effect, no severe adverse effect was identified in this study. The modified Da Chaihu decoction maybe effective in the treatment of essential hypertension with anxiety. In addition to a certain role in lowering blood pressure, the modified Da Chaihu decoction was also effective in improving traditional Chinese medicine syndrome and blood lipids, reducing the level of C reactive protein, relieving anxiety with little adverse effect.

Colletotrilactam A-D, novel lactams from Colletotrichum gloeosporioides GT-7, a fungal endophyte of Uncaria rhynchophylla.

Four novel lactams, colletotrilactam A-D (1-4), along with six known compounds (5-10) were isolated from the culture broth of Colletotrichum gloeosporioides GT-7, a fungal endophyte of Uncaria rhynchophylla. The structures of these compounds were elucidated by comprehensive NMR spectroscopy. Isolates were tested for monoamine oxidase (MAO) inhibitory activity and compound 9 showed potent MAO inhibitory activity with IC50 value of 8.93±0.34µg/mL, when the IC50 value of iproniazid as a standard was 1.80±0.5µg/mL.

[Optimization of Enzymatic Hydrolysis Conditions of Xiaoyao-pill Herb Residues by Cellulase].

Objective: To explore the enzymatic hydrolysis conditions of Xiaoyao-pill herb residues by cellulose. Methods: Based on the single factor test,an Box-Benhnken design was used to optimize the parameters, three factors, including cellulase dosage, enzymolysis time, and solid-liquid ratio were regarded as investigation factors,the yield of enzymatic hydrolysis as index, Xiaoyao-pill herb residues enzymatic hydrolysis catalyzed by cellulase, and a mathematical regression model was established. Results: The optimal parameters were obtained as follows,cellulase dosage was 6%,enzymolysis time was 5. 6 h and solid-liquid ratio was 1 ∶ 12( g / m L). Under this condition,the yield of enzymatic hydrolysis was 43. 89%. Conclusion: The results may provide new reference for further exploring Chinese herbal medicine efficiently.

Discovery of Anti-inflammatory Ingredients in Chinese Herbal Formula Kouyanqing Granule based on Relevance Analysis between Chemical Characters and Biological Effects.

Kouyanqing Granule (KYQG) is a traditional Chinese herbal formula composed of Flos lonicerae (FL), Radix scrophulariae (RS), Radix ophiopogonis (RO), Radix asparagi (RA), and Radix et rhizoma glycyrrhizae (RG). In contrast with the typical method of separating and then biologicalily testing the components individually, this study was designed to establish an approach in order to define the core bioactive ingredients of the anti-inflammatory effects of KYQG based on the relevance analysis between chemical characters and biological effects. Eleven KYQG samples with different ingredients were prepared by changing the ratios of the 5 herbs. Thirty-eight ingredients in KYQG were identified using Ultra-fast liquid chromatography-Diode array detector-Quadrupole-Time-of-flight-Tandem mass spectrometry (UFLC-DAD-Q-TOF-MS/MS) technology. Human oral keratinocytes (HOK) were cultured for 24 hours with 5% of Cigarette smoke extract (CSE) to induce inflammation stress. Interleukin-1ß (IL-1ß), interleukin-6 (IL-6), interleukin-8 (IL-8), and tumour necrosis factor-α (TNF-α) were evaluated after treatment with the eleven KYQG samples. Grey relational analysis(GRA), Pearson's correlations (PCC), and partial least-squares (PLS) were utilized to evaluate the contribution of each ingredient. The results indicated that KYQG significantly reduced interleukin-1ß, interleukin-6, interleukin-8, and tumour necrosis factor-α levels, in which lysine, γ-aminobutyric acid, chelidonic acid, tyrosine, harpagide, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, isoquercitrin, luteolin-7-o-glucoside, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, angoroside C, harpagoside, cinnamic acid, and ruscogenin play a vital role.

An open-labeled, randomized, multicenter phase IIa study of gambogic acid injection for advanced malignant tumors.

BACKGROUND: Gambogic acid is a pure active compound isolated from the traditional Chinese medicinal plant gamboge (Garcinia morella Desv.). Based on the preliminary results of a phase I study, this phase IIa study compared the efficacy and safety of different dosage schedules of gambogic acid in patients with advanced malignant tumors. METHODS: Patients with advanced or metastases cancer who had not received any effective routine conventional treatment or who had failed to respond to the existing conventional treatment were randomly assigned to receive either 45 mg/m(2) gambogic acid intravenously from Days 1 to 5 of a 2-week cycle (Group A), or 45 mg/m(2) every other day for a total of five times during a 2-week cycle (Group B). The primary endpoint was objective response rate (ORR). RESULTS: Twenty-one patients assigned to Group A and 26 to Group B were included in the final analysis. The ORRs were 14.3% in Group A and 0% in Group B. It was not possible to analyze the significant difference because one of the values was zero. The disease control rates (DCRs) were 76.2% in Group A and 61.5% in Group B (P = 0.0456). The observed adverse reactions were mostly Grades I and II, and occurred in most patients after administration of the trial drug. There was no significant difference in the incidence of adverse reactions between the two arms. CONCLUSIONS: The preliminary results of this phase IIa exploratory study suggest that gambogic acid has a favorable safety profile when administered at 45 mg/m(2). The DCR was greater in patients receiving gambogic acid on Days 1 - 5 of a 2-week cycle, but the incidence of adverse reactions was similar irrespective of the administration schedule.

[Effects of shuang shen tong guan decoction on the blood flow dynamics in rat model with myocardial infarction].

OBJECTIVE: To research the effects of Shuang Shen Tong Guan Decoction (SSTGD) on hemodynamics in rats with acute myocardial infarction (AMI). METHODS: SD rats were divided into sham operation group,model group, SSTGD low-dose group (2.5 g/kg), SSTGD middle-dose group (5 g/kg) and SSTGD high-dose group (7.5 g/kg). The levels of HR, MAP, LVSP, LVEDP, LVdp/ dt(max) and LVdp/dt(min) were detected by PowerLab at 0, 15, 30, 60, 90, 120, 180 min after administration. RESULTS: Compared with the sham operated group, the levels of HR, MAP were increased, the levels of LVSP, LVEDP, LVdp/dt(max) and LVdp/dt(min) were reduced at each detected point in model group, the difference was significant (P < 0.05). Compared with the model group, HR and MAP were decreased in SSTGD low-dose group, SSTGD middle-dose group and SSTGD high-dose group after 15 min; LVSP, LVEDP, LVdp/dt(max) and LVdp/dt(min) were higher, there was significantly difference (P < 0.05). Compared with SSTGD low-dose group and SSTGD middle-dose group, the difference of LVSP, LVEDP, LVdp/dt(max) and LVdp/dt(min) was statistically significant in SSTGD high-dose group (P < 0.05). CONCLUSION: SSTGD can improve cardiac function by increasing heart stroke volume, decreasing cardiac oxygen consumption and total peripheral vascular resistance.

[Clinical efficacy evaluation of shuangshen tongguan capsule on acute myocardial infarction patients after direct percutaneous coronary intervention].

OBJECTIVE: To evaluate the therapeutic efficacy of Shuangshen Tongguan Capsule (STC) on acute myocardial infarction (AMI) patients after direct percutaneous coronary intervention (PCI). METHODS: Using a randomized controlled method, AMI patients with elevated ST segment after successful direct PCI were randomly assigned to the control group (62 cases) and the treatment group (67 cases). On the basis of the standard Western medical treatment, patients in the treatment group took STC, while those in the control group took STC placebos, 4 pills each time, three times daily. The Chinese medicine syndrome integrals, the cardiac function in the resting and loading states, the microcirculation perfusion rate, and the changes of Seattle Angina Scale score were evaluated after 6 months of treatment. RESULTS: Five cases were lost, accounting for 3.88%. Six months later the Chinese medicine syndrome integrals obviously decreased, the efficacy of Chinese medicine syndrome was enhanced, the LVEF in the loading state and the percentage of normal myocardium obviously increased, anterior myocardial infarction segments with increased k value of the microcirculation perfusion increased, the total score of Seattle Angina score, the satisfactory degree of the treatment, and the integrals for the disease recognition degree were significantly enhanced (all P<0.05). CONCLUSIONS: STC could improve the angina symptoms of AMI patients after direct PCI and elevate their heart functions. It has certain roles in improving microcirculation perfusion of myocardium, thus elevating patients' quality of life.

[Studies on the alkaloids of Senecio scandens growing in Guangdong].

OBJECTIVE: To study alkaloids of Senecio scandens growing in Guangdong. METHODS: The rapid resolution liquid chromatography-electrospray ionization mass spectrometry (RRLC-ESI-MS/MS) was used to analyse alkaloids of Senecio scandens growing in Guangdong, and senkirkine was isolated and purified by silica gel column chromatography. RESULTS: Four alkaloids were identified as senkirkine, dehydrosenkirkine, monocrotaline and adonifoline, and senkirkine was firstly isolated from Senecio scandens growing in Guangdong. CONCLUSION: Senkirkine is the main component of Senecio scandens growing in Guangdong.

Fermentation effects of oligosaccharides of Radix Ophiopogonis on alloxan-induced diabetes in mice.

In this study, oligosaccharides extracted from Ophiopogon japonicus vinegar (OOV) by alcoholic and acetic acid fermentation with water extracts from Radix Ophiopogon and oligosaccharides extracted from Radix Ophiopogonis (OOJ) were investigated. Characterization of the extracts indicated that OOV are proteoglycans, whereas OOJ are not. Moreover, compared with OOJ, monosaccharide compositions of OOV only include fructose and galactose and not glucose. MALDI-TOF-mass spectrometric results showed that the molecular weight of OOV was smaller after fermentation. Changes in the characteristics of OOV would inevitably lead to changes in its hypoglycemic properties. The OOV inhibition activity against α-glucosidase was stronger than that of OOJ. The inhibition activity became stronger with higher dosages of OOV. The hypoglycemic effect of OOV on alloxan-induced diabetic mice was stronger than that of OOJ. More important, the ability of OOV to reduce damage on islets in diabetic mice was stronger than that of OOJ. Overall, alcoholic and acetic acid fermentation improved the hypoglycemic activity of OOJ.

[Analyze and compare activities of polysaccharide form rhizoma chuanxiong and radix paeoniae rubra].

OBJECTIVE: To explore the difference of biological activities between two Chinese Herbs polysaccharides. METHODS: Extracted two kinds of Chinese Herbs Polysaccharides by hot water, and determined the content of Polysaccharides. Determined the antibacterial activity with turbidimetry. Explored antioxidant activity using an in vitro antioxidant analysis, probed into the effects on cell growth with MTT colorimetric analysis. RESULTS: The two polysaccharides both showed activities on the antibacterial, anti-oxidation and promotion of cell growth but different in degree. The Radix Paeoniae Rubra polysaccharide was stronger than Rhizoma Chuanxiong in antioxidant and antimicrobial activities, and weaker in promotion of cell growth activity. CONCLUSION: Activity differences exist between the two polysaccharides and the activities show some complementary effects. The differences provide important value in research on polysaccharide compound.

[Effects of phytoestrogens on testosterone production of rat Leydig cells].

OBJECTIVE: To investigate the effects of phytoestrogens (daidzein and genistein) on the testosterone production of rat Leydig cells and the possible mechanisms. METHODS: Primary Leydig cells were obtained from 3-month old male SD rats using discontinuous Percoll density gradient centrifugation. The effects of phytoestrogens at various concentrations were evaluated by ELISA, with hCG as the positive control. The mRNA expression of P450 side-chain cleavage enzyme (P450scc) was analyzed by semi-quantitative RT-PCR. RESULTS: Genistein at 0.1 micromol/L obviously promoted the secretion of testosterone and upregulated the mRNA level of P450scc. At a higher concentration of 5 micromol/L, however, both daidzein and genistein significantly inhibited the testosterone production of Leydig cells (P > 0.05). CONCLUSION: Genistein can promote the testosterone production of Leydig cells at a low concentration (0.1 micromol/L), but both daidzein and genistein can inhibit it at a higher concentration ( >5 micromol/L).

Determination and pharmacokinetic comparison of rhein in rats after oral dosed with Da-Cheng-Qi decoction and Xiao-Cheng-Qi decoction.

Da-Cheng-Qi decoction (DCQD) is composed of dahuang, houpu, zhishi and mangxiao, while Xiao-Cheng-Qi decoction (XCQD) just contains dahuang, houpu, and zhishi. A validated high-performance liquid chromatographic (HPLC) method was developed for the determination and pharmacokinetic comparison of rhein in rats. It was performed on a reversed-phase C(18) column (150 x 4.6 mm) with a mobile phase of methanol and 0.2% acetic acid (89:11, v/v) and ultraviolet detection at 254 nm. The assay was linear over the range 30-3000 ng/mL (r(2) = 0.9991), with mean percentage recovery of 101.4%. The RSD of intra- and inter-day precision were less than 3.0%, with accuracy in the range 96.8-102.5% for each of the concentrations tested. Following oral administration, rhein plasma levels revealed curves characterized by peaks at 20.5 and 30.1 min corresponding to dosages of 15 mg/kg (XCQD) and 20 mg/kg (DCQD) at mean concentrations of 1184.67 and 1814.27 ng/mL, respectively. The half-lives of rhein from XCQD and DCQD were 45.3 and 139.6 min, respectively. AUC(0-12h) of rhein after oral dosage with XCQD and DCQD were 3435.68 and 5382.25 microg/L h, respectively. The pharmacokinetic parameters may be used to guide the clinical prescription compatibility of traditional Chinese prescriptions related to dahuang and mangxiao.

Simultaneous determination and pharmacokinetic studies of aloe emodin and chrysophanol in rats after oral administration of Da-Cheng-Qi decoction by high-performance liquid chromatography.

A validated high-performance liquid chromatography (HPLC) method was developed for simultaneous determination and pharmacokinetic study of aloe emodin and chrysophanol in rats. It was performed on a reverse-phase C(18) column and a mobile phase made up of methanol and 0.2% acetic acid (83:17, v/v). The ultraviolet detection was 254 nm. 1,8-dihydroxyanthraquinone was used as the internal standard. The assay was linear over the range 28-2800 ng/mL (r(2) = 0.9993) for aloe emodin and 25.6-2560 ng/mL (r(2) = 0.9991) for chrysophanol. The average percentage recoveries of three spiked plasmas were 98.8-104.8% and 97.7-103.2% for aloe emodin and chrysophanol, respectively. Their RSD of intra-day and inter-day precision at concentrations of 56, 280 and 1400 ng/mL for aloe emodin and 51.6, 258 and 1290 ng/mL for chrysophanol were less than 3.5%. This method was applied for the first time to simultaneously determinate aloe emodin and chrysophanol in rats following oral administration of traditional Chinese medicine of Da-Cheng-Qi decoction. The pharmacokinetic parameters showed that chrysophanol was better absorbed with higher concentrations in plasma than aloe emodin did. They both eliminated slowly in male rats. The assay is suitable for identifying the plasma and tissue levels of aloe emodin and chrysophanol in preclinical investigations.

[Experimental studies on antitussive, expectorant and antiasthmatic effects of extract from Citrus grandis var. tomentosa].

OBJECTIVE: To observe the antitussive, expectorant and antiashmatic effects of the extract from Citrus grandist var. tomentosa. METHOD: The cough models induced by ammonia liquor in mice and citric acid in guines pigs were used to observe the antitussive effects. The methods of phenel red execretion in mice and phlegm displacement of rats were used to investigate the expectorant effects. Bronchial asthma model induced by histamine-acetylcholine in guinea pigs was used to observe the antiasthmatic effects. RESULT: The extract from the title plant could inhibit the cough induced by ammonia in mice, decrease the frequency of cough induced by citric acid in guineas pig and prolong the latent period of cough. The extract also could obviously increase phenol red output of trachea in mice, promote expectoration in rats and prolong the latent period of asthma induced by histamine-acetylcholine in guinea pigs. CONCLUSION: The extract from C. grandis var. tomenfosa has significant antitussive, expectorant and antiasthmatic effects.