Effects of Platycodonis Radix-Curcumae Rhizoma on oral nanoparticle uptake and in vitro inhibition against breast cancer metastasis / 中国中药杂志

This study combined the herbal pair Platycodonis Radix-Curcumae Rhizoma(PR-CR) possessing an inhibitory effect on tumor cell proliferation and metastasis with the active component of traditional Chinese medicine(TCM) silibinin-loaded nanoparticles(NPs) with a regulatory effect on tumor microenvironment based on the joint effect on tumor cells and tumor microenvironment to inhi-bit cell metastasis. The effects of PR-CR on the cellular uptake of NPs and in vitro inhibition against breast cancer proliferation and metastasis were investigated to provide an experimental basis for improving nanoparticle absorption and enhancing therapeutic effects. Silibinin-loaded lipid-polymer nanoparticles(LPNs) were prepared by the nanoprecipitation method and characterized by transmission electron microscopy. The NPs were spherical or quasi-spherical in shape with obvious core-shell structure. The mean particle size was 107.4 nm, Zeta potential was-27.53 mV. The cellular uptake assay was performed by in vitro Caco-2/E12 coculture cell model and confocal laser scanning microscopy(CLSM), and the results indicated that PR-CR could promote the uptake of NPs. Further, in situ intestinal absorption assay by the CLSM vertical scanning approach showed that PR-CR could promote the absorption of NPs in the enterocytes of mice. The inhibitory effect of NPs on the proliferation and migration of 4T1 cells was analyzed using 4T1 breast cancer cells and co-cultured 4T1/WML2 cells, respectively. The results of the CCK8 assay showed that PR-CR-containing NPs could enhance the inhibition against the proliferation of 4T1 breast cancer cells. The wound healing assay indicated that PR-CR-containing NPs enhanced the inhibition against the migration of 4T1 breast cancer cells. This study enriches the research on oral absorption of TCM NPs and also provides a new idea for utilizing the advantages of TCM to inhibit breast cancer metastasis.

Comparison of in vivo plasma pharmacokinetics and urine excretion of main components in Xihuang Formula in rats with precancerous lesions of breast cancer / 中国中药杂志

The UPLC-MS/MS was established for the determination of acetyl-11-keto-beta-boswellic acid(AKBA) and β-boswellic acid(β-BA), the main active components of Olibanum and Myrrha extracts in Xihuang Formula, in rat plasma and urine. The effects of compatibility on the pharmacokinetic behaviors of AKBA and β-BA in rats were investigated, and the differences in pharmacokinetic behaviors between healthy rats and rats with precancerous lesions of breast cancer were compared. The results showed that compared with RM-NH and RM-SH groups, the AUC_(0-t) and AUC_(0-∞) of β-BA increased(P<0.05 or P<0.01), T_(max) decreased(P<0.05 or P<0.01), and C_(max) increased(P<0.01) after compatibility. The trends of AKBA and β-BA were the same. Compared with RM-SH group, the T_(max) decreased(P<0.05), C_(max) increased(P<0.01), and the absorption rate increased in the normal group of Xihuang Formula. The results of urinary excretion showed that there was a decreasing trend in the urinary excretion rate and total urinary excretion of β-BA and AKBA after compatibility, but there was no statistical difference. Compared with normal group of Xihuang Formula, the AUC_(0-t) and AUC_(0-∞) of β-BA increased(P<0.05), T_(max) increased(P<0.05), and the clearance rate decreased in the breast precancerous lesion group. AUC_(0-t) and AUC_(0-∞) of AKBA showed an increasing trend, the in vivo retention time was prolonged, and the clearance rate was reduced, but there was no significant difference compared with the normal group. The cumulative urinary excretion and urinary excretion rate of β-BA and AKBA decreased under pathological conditions, indicating that pathological conditions could affect the in vivo process of β-BA and AKBA, and reduce their excretion in the form of prototype drugs, showing different pharmacokine-tic characteristics from normal physiological conditions. In this study, UPLC-MS/MS analysis method was established, which was sui-table for in vivo pharmacokinetic analysis of β-BA and AKBA. This study laid a foundation for the development of new dosage forms of Xihuang Formula.

Effects of Omega-3 Polyunsaturated Fatty Acids on Cognitive Function after Splenectomy in Rats.

BACKGROUND: Postoperative cognitive dysfunction (POCD) is a common complication after abdominal surgery. Several studies have reported that POCD is related to neuroinflammation caused by surgery. Omega-3 polyunsaturated fatty acids (PUFAs) can effectively inhibit the systematic inflammatory response. So, we use fish oil to study the effect of fish oil on inflammation, immunity, and cognitive behavior after splenectomy in rats. METHODS: 60 SD (Sprague-Dawley) rats were randomly divided into control group (group C, n = 20), surgery group (group S, n = 20), and omega-3 (fish oil) intervention group (group F, n = 20). Omega-3 PUFA was injected intraperitoneally from 3 days before operation to 7 days after operation in group F, and normal saline was injected simultaneously in group S. Rats in group S and group F received splenectomy under general anesthesia. Morris water maze behavioral evaluation was performed on the first, third, fifth, and seventh day after operation. The levels of IL-1ß (interleukin-1ß), IL-6 (interleukin-6), TNF-α (tumor necrosis factor-α), SOD (superoxide dismutase), and GSH-PX (glutathione peroxidase) were detected. RESULTS: Serums IL-1ß, IL-6, and TNF-α concentrations in group S and group F were higher than those in group C (P < 0.01), while those inflammatory cytokines in group F were significantly lower than those in group S (P < 0.01); serum GSH-PX levels in group F were higher than group S (P < 0.01). The Morris water maze behavior test performance of group F was better than that of group S (P < 0.05). CONCLUSION: Omega-3 PUFA can effectively improve postoperative inflammatory response, reduce the damage of antioxidant defense system, and improve postoperative cognitive function.

Improvement in compatibility of hot melt pressure-sensitive adhesive with cinnamon volatile oil and in vitro transdermal property by physical blending / 中国中药杂志

Hot melt pressure-sensitive adhesive(HMPSA) has broad application potential in the field of traditional Chinese medicine(TCM) plasters due to its high drug loading, weak skin irritation, satisfactory adhesion, etc. compared with rubber plasters.However, the structure of HMPSA is prone to suffer from the damage caused by volatile oils in TCM plasters. In view of this, a kind of HMPSA with a stable structure was prepared by physical blending of DINCH, polypropylene wax and liquid rubber(LIR) in the present study, which is denoted as DPL. The dosage of cinnamon volatile oil(CVO), the model drug, was selected with viscosity, softening point and cohesion as evaluation indexes. The interaction between DPL and HMPSA was investigated by Fourier transform infrared spectroscopy(FT-IR) and differential scanning calorimetry(DSC). The compatibility of HMPSA with CVO and its transdermal ability were studied by in vitro transdermal test, adhesion, scanning electron microscopy( SEM) and rheological evaluation. The results showed that 5% CVO began to damage the structure of HMPSA. The initial adhesion and holding adhesion of DPL-modified HMPSA(DPL-HMPSA) were not significantly changed compared with those of HMPSA, whereas the 180° peel strength was decreased. FI-IR unraveled that DPL formed the n-π conjugated system with styrene-isoprene-styrene block copolymer(SIS), and there was no significant difference in the glass transition temperature according to DSC results, which indicated the good compatibility of DPL with HMPSA. With 5% CVO loaded, the drug content of DPL-HMPSA was 1. 14 times higher than that of HMPSA, and the decrease rate of drug content in DPL-HMPSA was 16% lower than that in HMPSA after 3 months. SEM demonstrated that CVO did not cause obvious structural damage to DPL-HMPSA. Rheological evaluation revealed that the storage modulus and loss factor of DPL-HMPSA were higher than those of HMPSA, and the cohesion was also stronger. The percutaneous penetration rate of cinnamaldehyde in DPL-HMPSA was 2. 25 times that of HMPSA. In conclusion, DPL-HMPSA had more stable structure, better compatibility with CVO, and higher in vitro transdermal efficiency of cinnamaldehyde than before the modification. This study can provide reference for the mitigation of the matrix structure damage caused by volatile oil components in TCM plasters and the enhancement of the content and in vitro transdermal rate of drug.

Clinical metabolomics research on Xiaozhang Tie with the umbilical compress therapy for cirrhotic ascites / 药学学报

We used metabolomics technology to identify and understand the biomarkers and therapeutic mechanisms of umbilical compress therapy based on Xiaozhang Tie (XT) to provide scientific evidence for its clinical application. A total of 10 patients with cirrhotic ascites and gastrointestinal motility disorders who were hospitalized in the Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine from November 2017 to June 2018 were divided into a placebo group (4 cases) or an XT group (5 cases), and 10 healthy volunteers were included as controls. This clinical trial was approved according to the Ethics Committee of Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine (2017-528-11-01). The patients in the XT group were given umbilical compress therapy with Xiaozhang Tie, and patients in the placebo group were administered a plaster patch in which the drug content was less than 5%, receiving one patch per day for three consecutive days. Non-targeted metabolomics technology and UPLC-Q/Orbitrap-MS/MS analysis technology were utilized to investigate the fluctuations in endogenous metabolic profiles in the patient's urine prior to and after administration of XT. By analyzing and comparing the urine metabolic profiles of patients with cirrhotic ascites to those of healthy volunteers, a total of 31 biomarkers were identified, 14 of which were significantly decreased by the intervention with Xiaozhang Tie (P <0.05). Pathway enrichment analysis revealed that phenylalanine metabolism and tryptophan metabolism are key pathways affected by XT treatment. The results suggest that XT can alleviate cirrhotic ascites by modulating abnormalities in amino acid metabolism.

Resource Value Discovery and Utilization of Wastes in Industrialization of Rhei Radix et Rhizoma / 中国实验方剂学杂志

The recycling of traditional Chinese medicine （TCM） wastes is an important research topic to be solved urgently in the industrialization of TCM resources. Rhei Radix et Rhizoma is a bulk Chinese herb mainly derived from Rheum palmatum，R. tanguticum，and R. officinale. At present，these three medicinal plants have been cultivated on a large scale and widely used in the fields of medicine，health care，food，cosmetics，and veterinary medicine，with an annual demand of more than 5 500 tons（1 ton=1 000 kg）. However，a large number of wastes such as non-medicinal parts and residues produced in the production and deep processing are discarded because there is no effective way of utilization，resulting in serious waste of resources and environmental pollution. The non-medicinal parts contain not only the chemical components and pharmacological effects similar to those of roots and rhizomes but also a variety of amino acids，mineral elements，and conventional nutrients. They have a long history of use，and the content of some resource components is higher than that in roots and rhizomes. In particular，their stems and leaves exhibit great potential to be consumed as food and medicine due to high safety. Besides，the content of anthraquinones in Rhei Radix et Rhizoma residue is high and it possesses good antibacterial activity. It can be seen that the waste from the industrialization of Rhei Radix et Rhizoma has high utilization value. Hence，based on the relevant literature and investigation on the application of producing areas in China and abroad，the paper summarized the utilization status of their medicinal and non-medicinal parts，the waste production in the industrialization，as well as the active substances and utilization ways and put forward the multi-level and multi-path utilization strategy of Rhei Radix et Rhizoma wastes，in order to provide reference for the rational development and application of Rhei Radix et Rhizoma resources and promote the effective utilization and green development of the corresponding wastes.

[Preparation and evaluation of schisandrin B-loaded F127 modified lipid-polymer nanoparticles for inhibition of breast cancer lung metastasis].

In the current study, schisandrin B(SchB)-loaded F127 modified lipid-polymer hybrid nanoparticles(SchB-F-LPNs) were developed to improve the inhibition of breast cancer lung metastasis. Modified nanoprecipitation method was used to prepare SchB-F-LPNs. The nanoparticles were spherical in shape with shell-core structure by TEM observation. SchB-F-LPNs showed a mean particle size of(234.60±6.11) nm with zeta potential of(-5.88±0.49) mV. XRD results indicated that SchB existed in the nanoparticles in an amorphous state. The apparent permeability coefficient through porcine mucus of F-LPNs was 1.43-fold of that of LPNs as shown in the in vitro mucus penetration study. The pharmacokinetics study showed that the C_(max) of SchB was(369.06±146.94) µg·L~(-1),(1 121.34±91.65) µg·L~(-1) and(2 951.91±360.53) µg·L~(-1) respectively in SchB suspensions group, SchB-LPNs group and SchB-F-LPNs group after oral administration in rats. With SchB suspensions as the reference formulation, the relative bioavailability of SchB-F-LPNs was 568.60%. SchB-F-LPNs inhibited the morphological change during transforming growth factor-ß1(TGF-ß1)-induced epithelial-mesenchymal transition. In addition, SchB-F-LPNs significantly decreased the number of metastatic pulmonary nodules in 4 T1 tumor-bearing mice, suggesting that SchB-F-LPNs may inhibit the metastasis of breast cancer. These results reveal the promising potential of SchB-F-LPNs in treatment of breast cancer lung metastasis.

Research Progress on Organic-inorganic Hybrid Nanocarriers of Active Ingredients from Chinese Materia Medica / 中国实验方剂学杂志

Nanocarriers for delivering active ingredients from Chinese materia medica play an important role in improving their solubility, membrane permeability and in vivo biological behavior, enhancing the therapeutic efficiency and reducing side effects. They are promising for extensive research and application. As novel nanocarriers, organic-inorganic hybrid nanocarriers composed of organic materials or carriers and inorganic parts possess the dual advantages of organic carriers and inorganic carriers. They may exert desirable action in drug delivery. In addition, they have been designed to improve the stability and biocompatibility, further increase the therapeutic efficiency and reduce side effects. They have also been investigated to achieve multi-functionality. In this paper, the research and application of organic-inorganic hybrid nanocarriers delivering active ingredients from Chinese materia medica were summarized and analyzed. The development and application prospect of organic-inorganic hybrid nanocarriers are prospected. The aim of this review is to provide a reference for the investigation of new drug delivery system for delivering active ingredients from Chinese materia medica efficiently and safely.

Research Progress of Nano-drug Delivery Systems for Active Ingredients from Chinese Materia Medica by Modulating EMT to Inhibit Tumor Metastasis / 中国实验方剂学杂志

The epithelial-to-mesenchymal transition (EMT), a process during which cells undergo transition from a polarized epithelial phenotype to a non-polarized mesenchymal phenotype, executed by transcription factors of Twist, Snail and Zeb families. EMT plays an important role in multiple stages of cancer progression such as initiation, tumor growth, and metastasis. Some active ingredients from Chinese materia medica can inhibit EMT by regulating transcription factors and signaling pathways by multiple targets. However, their therapeutic effect was hindered due to various limitation such as solubility, stability, tissue specificity and safety. Therefore, in order to improve the druggability of active ingredients from Chinese materia medica, enhance the therapeutic effect in inhibiting tumor metastasis mediated by EMT and reduce the toxic and side effects, a variety of nano-drug delivery systems have been developed in recent years. Here, we made a review about these drug delivery systems modulating EMT and their research progress in inhibiting tumor metastasis.

Ang-(1-7) treatment attenuates lipopolysaccharide-induced early pulmonary fibrosis.

Early pulmonary fibrosis is the leading cause of poor prognosis in patients with acute respiratory distress syndrome (ARDS). However, whether the renin-angiotensin system (RAS) can serve as a therapeutic target is unknown. In this study, an animal model of early pulmonary fibrosis was established via the LPS three-hit regimen. Afterwards, the animals were treated with intraperitoneal injections of Ang-(1-7), AVE0991, or A779 once per day for 20 days. The plasma and BALF AngII levels of the animals were increased, while there were no significant changes in Ang-(1-7) levels in lung tissue after LPS treatment. Furthermore, the AT1R protein levels were significantly increased and the Mas levels were significantly decreased on days 14 and 21. Administration of Ang-(1-7) downregulated LPS-induced AT1R mRNA expression, which was upregulated by A779. The expression of Mas mRNA responded in the opposite direction relative to AT1R. Moreover, LPS caused decreased levels of Mas and E-cadherin and increased AT1R, Vimentin, and Src phosphorylation levels. Ang-(1-7) or AVE0991 blocked these effects but was counteracted by A779 treatment. Our findings suggested that AngII and AT1R levels exhibit opposite dynamic trends during LPS-induced early pulmonary fibrosis, as do Ang-(1-7) and Mas. Ang-(1-7) exerts protective effects against early pulmonary fibrosis, mainly by regulating the balance between AngII and AT1R and between Ang-(1-7) and Mas and by inhibiting Src kinase activation.

Research on regional distribution and industrial status analysis of genuine medicinal resources of flowers in Henan province / 中国中药杂志

Flower medicinal materials usually refer to Chinese medicinal materials with a complete flower,inflorescence,or part of a flower as the different medicinal parts,they have an important share in the Chinese herbal medicine market and appeared frequently in Chinese medicine prescriptions. Firstly,the species and regional distribution of the flower medicinal materials resources in China were briefly summarized. Secondly,the characteristics,yield,producing area and origin distribution of the main flower medicinal materials in Henan province were discussed. Finally,the present situation and the main problems of the flower medicinal materials industry in Henan province were comprehensively analyzed,and the corresponding industrial development countermeasures were put forward.This research was intended to provide decision-making demonstration and scientific basis for the rational exploitation and utilization of resources,breeding of new varieties,planting division,production layout and the healthy and sustainable development of the flower medicinal materials industry in Henan province.

Is fluoroquinolone monotherapy a useful alternative treatment for Pseudomonas aeruginosa bacteraemia?

PURPOSE: Pseudomonas aeruginosa bacteraemia is associated with high mortality, and most monotherapies are beta-lactam-based. We aimed to investigate clinical outcomes of definitive fluoroquinolone monotherapy versus beta-lactam monotherapy for P. aeruginosa bacteraemia. METHODS: This retrospective study enrolled adult patients receiving definitive monotherapy with beta-lactam or fluoroquinolone between November 2013 and November 2014 at Taipei Veterans General Hospital. The independent risk factors for 28-day mortality were analyzed by logistic regression and propensity score-adjusted analysis. RESULTS: Among the 105 patients enrolled, 78 patients received beta-lactams and 27 received fluoroquinolones (20 with ciprofloxacin and 7 with levofloxacin). Primary bacteraemia (39.0%) and urinary tract infections (37.1%) were the most common sources of bacteraemia. The 28-day mortality rate was 11.1% for those receiving fluoroquinolones and 32.1% for those receiving beta-lactams (P = 0.062). The 28-day mortality rate between the two groups stratified by APACHE II and Pitt bacteraemia scores showed no significant differences in each category. Propensity score-adjusted multivariate analysis revealed that definitive therapy with a fluoroquinolone was not associated with 28-day mortality (OR 0.42; 95% CI 0.08-2.23; P = 0.305). CONCLUSIONS: Fluoroquinolone might be an alternative to beta-lactam as a definitive monotherapy for P. aeruginosa bacteraemia provided they are active in vitro. Our results could be a basis for further studies and provide a possible target for antibiotic stewardship interventions in P. aeruginosa bacteraemia.

Comparison of clinical efficacy between early low and high enteral nutrition (EN) administration in the early treatment of hyperlipidemic severe acute pancreatitis / 肠外与肠内营养

Objective: This study aimed to compare the effects of high versus low calorie early enteral nutrition (EEN) administration on the complications and prognosis of hyperlipidemic acute pancreatitis (HLAP) patients. Methods: In this study, HLAP patients were randomly divided into high calorie EEN group and low calorie EEN group. The nutritional support was carried out within 48h at patients' admission. The serum lipid levels, inflammatory parameters, the incidence of EN intolerance, hospitalization duration, ICU duration, the incidence of organ failure and infected pancreatic necrosis as well as mortality rate were recorded and compared between two groups. Results: 48 patients with diagnosis of HLAP were included in this study from January 2014 to June 2017. In the first two days, the serum lipid levels of patients in low-calorie group decreased gradually. The serum lipid levels of the two groups were 2. 3 (1. 7-3. 4) mmol/L versus 5. 2 (2. 9-6. 1) mmol/L (P = 0. 05) respectively on third day after EN administration. There was no significant difference in the incidence of MODS and mortality rate between the two groups while the ICU duration of low-calorie group was significantly shorter than that in high-calorie group. The incidence of IPN in low-calorie group showed an elevated trend but there was no statistical significance. Conclusion: For HLAP patients, low calorie-high protein nutrition supply could benefit the patients to gain lean body weight due to the positive nitrogen balance, and to consume body fat due to the deficiency of calories. It is an effective nutrition support strategy for the patients' recovery.

Research progress on Chinese medicines with topical administration in umbilical region / 中国中药杂志

Based on the Chinese medicines with topical administration in umbilical region approved by China Food and Drug Administration (CFDA), this paper would comb and analyze their dosage forms, varieties and clinical applications. On the other hand, through consulting literature materials, the research progress was reviewed and the main challenges faced by the medicines were discussed in detail as well. This paper elaborates that the preparations with topical administration in umbilical region, as an important branch in Chinese medicine external therapy, have unique advantages. However, there are still some problems such as rough workmanship, lacking internationally accepted quality control standards, scarcity of pharmacological and clinical evidences and biopharmaceutical researches. Meanwhile, proper measures and suggestions are put forward.

Regulatory effect of a Chinese medicine prescription Hu Qi Shan on the telomerase activity in hepatic precancerous lesions in rats / 中国比较医学杂志

Objective To explore the possible mechanism of action of telomerase in hepatic precancerous lesions, and the regulatory effect of a Chinese medicine prescription HU Qi Shan ( HQS) and its principal drug mistletoe alkali on the telomerase activity in rat liver tissues.Methods Rat model of hepatic precancerous lesions was established by Solt-Farber two-step protocol.The model rats were randomly divided into 5 groups, including the model group, high-dose HQS [8 g/(kg· d)] group, low-dose HQS [4 g/(kg· d)] group, and mistletoe alkali[8 mg/(kg· d)] group.γ-Glutamy-transpeptidase (γ-GT) was analyzed by immunohistochemistry.AFP was detected by immunofluorescence technique.The telomerase activity was detected using a quantitative telomerase detection kit.The expression of NF-κB P65 was detected by immunohistochemistry.The cytoplasmic protein IκB-αwas detected by western blotting.Results After treated with HQS and mistletoe alkali, the areas ofγ-GT-positive foci and number of AFP-positive cells in the liver tissus were significantly decreased than those of the model group ( P<0.05 for both) , the telomerase activity was decreased, the number of NF-κB P65-positive cells was also decreased ( P <0.05 ) , whereas the intracytoplasmic expression of IκB-αproteins was significantly increased ( P <0.05 ) .Conclusions HQS and mistletoe alkali can suppress the telomerase activity.Its possible mechanism may be through inhibition of the over-expressed apoptosis-related genes such as NF-κB P65 and increase the expression of IκB-αdecreasing the telomerase activity.

Effect of stability and dissolution of realgar nano-particles using solid dispersion technology / 中国中药杂志

<p><b>OBJECTIVE</b>To improve the stability and dissolution of realgar nano-particles by solid dispersion.</p><p><b>METHOD</b>Using polyethylene glycol 6000 and poloxamer-188 as carriers, the solid dispersions were prepare by melting method. XRD, microscopic inspection were used to determine the status of realgar nano-particles in solid dispersions. The content and stability test of As(2)0(3) were determined by DDC-Ag method. Hydride generation atomic absorption spectrometry was used to determine the content of Arsenic and investigated the in vitro dissolution behavior of solid dispersions.</p><p><b>RESULT</b>The results of XRD and microscopic inspection showed that realgar nano-particles in solid dispersions were amorphous. The dissolution amount and rate of Arsenic from realgar nano-particles of all solid dispersions were increased significantly, the reunion of realgar nano-particles and content of As(2)0(3) were reduced for the formation of solid dispersions.</p><p><b>CONCLUSION</b>The solid dispersion of realgar nano-particles with poloxamer-188 as carriers could obviously improve stability, dissolution and solubility.</p>

Altered claudin-4 expression in progesterone-treated endometrial adenocarcinoma cell line Ishikawa.

OBJECTIVE: To detect the expression change of claudin-4 in Ishikawa endometrial adenocarcinoma cell line in response to progesterone. To determine whether claudin-4 is involved in the anticancer effect of progesterone. METHODS: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was used to determine the 50% inhibitory concentration (IC50) of megestrol acetate (MA) in treating Ishikawa cells. After the Ishikawa cells were treated with MA at IC50, cell apoptosis was examined by flow cytometry and transmission electron microscopy. The messenger RNA and protein expression levels of claudin-4 were further quantified by real-time polymerase chain reaction and Western blot. The localization of claudin-4 was examined by immunofluorescent staining. RESULTS: The IC50 of MA on Ishikawa cells was 15 mg/L incubated for 72 hours. Apoptosis percentage was elevated from 0.07% ± 0.02% to 3.93% ± 0.81% after MA treatment. The expression of claudin-4 at both protein and messenger RNA levels was significantly decreased after the treatment of MA (P < 0.05). The localization of claudin-4 transferred from cytomembrane to cytoplasm and nucleus. CONCLUSION: Megestrol acetate can inhibit the growth of Ishikawa cells. It may work through decreasing claudin-4 expression and cell apoptosis. The localization change of claudin-4 may also be involved in the anticancer effect of progesterone.

The inhibition activity of chemical constituents in hawthorn fruit and their synergistic action to HMG-CoA reductase / 中国中药杂志

<p><b>OBJECTIVE</b>To study the hypolipidemic active compounds from Crataegus pinnatifida and mechanism of action of those.</p><p><b>METHOD</b>Guided by the inhibitory activity to HMG-CoA reductase, the active compounds were separated and purified with macroporous resin and silica gel.</p><p><b>RESULT</b>Four active compounds were obtained, which were quercetin, hyperoside, rutin and chlorogenic acid, the sum of their inhibitory rate was 50.01%, and the total inhibitory rate of the mixture of four active compounds matched was 79.48%.</p><p><b>CONCLUSION</b>Quercetin and hyperoside were the principle active components inhibiting HMG-CoA reductase in Hawthorn fruit, and there were synergistic action among them.</p>

Determination of vitexin-rhamnoside in Beagle dog plasma and preliminary pharmacokinetics of Yixintong sustained release tablets / 中国中药杂志

<p><b>OBJECTIVE</b>To develop an HPLC method to determine vitexin-rhamnoside in plasma of Beagle dogs and study the pharmacokinetics and bioavailability of Yixintong sustained release tablets in Beagle dogs.</p><p><b>METHOD</b>A newly-developed HPLC method using C18 column and methanol-acetonitrile-tetrahydrogenfuran-0.5% acetic acid (1:1:19.4:78.6) as mobile phase was validated, and then was employed to determine vitexin-rhamnoside in plasma of Beagle dogs after oral administration of Yixintong sustained release tablets and general tablets. The main pharmacokinetic parameters were estimated by pharmacokinetic program 3p87. The non-compartmental pharmacokinetic parameters were also calculated on basis of the statistic moment theory.</p><p><b>RESULT</b>The pharmacokinetic profiles of Yixintong sustained release tablets and the general tablets were fitted to a one-and two-compartment open model, respectively. The T1/2, Tmax, AUC0-infinity and MRT for Yixintong sustained release tablets were 5.22 h, 4.0 h, 6,792.75 ng x h x mL(-1) and 8.4 h, respectively, compared with 8.94 h, 1.0 h, 5,880.4 ng x h x mL(-1) and 6.1 h for the general tablets. The relative bioavailability of the Yixintong sustained release tablets was 115.5% in Beagle dogs.</p><p><b>CONCLUSION</b>The sustained-release characteristic of Yixintong sustained release tablets were confirmed by pharmacokinetic study.</p>

Effects of syndrome dependent umbilical sticking with shizhang cataplasm and xuzhang cataplasm in treating Cirrhosis caused ascites / 中国中西医结合杂志

<p><b>UNLABELLED</b>To investigate the effects of Shizhang Cataplasm (SC) and Xuzhang Cataplasm (XC) in treating liver cirrhosis caused ascites of excessive syndrome (ES) type and deficient syndrome (DS) type respectively.</p><p><b>METHODS</b>All the 77 patients (37 of ES type and 40 of DS type) enrolled were treated by conventional treatment but with restrictive use of diuretics. SC and XC were given respectively to 26 patients of ES type and 26 of DS type additionally by umbilical sticking, they were regarded as the treated group, and those (11 of ES type and 14 of DS type) not received the cataplasm treatment were regarded as the control group. The changes of symptoms, body weight, abdominal perimeter and amount of urine before and after treatment were observed, and amount of ascites was examined with B-ultrasound to evaluate the efficacy according to comprehensive grading criteria. Also, the toxicity was observed.</p><p><b>RESULTS</b>Sixty-two cases completed the full course, 15 were withdrawn. As compared with the corresponding control group, body weight, abdominal perimeter and amount of ascites decreased, while amount of urine and flatus discharging increased remarkably in the treated group (P < 0.05). The comprehensive efficacy in patients of ES type was better than that in DS type (P < 0.05). The effective rate of grade I/II was 7.1% and 9.1% for patients in the control group of DS type and ES type respectively, while it was 57.2% and 69.2% in the treated group of DS and ES type respectively. Better therapeutic effect was shown in patients of ES type treated with SC.</p><p><b>CONCLUSION</b>SC and XC showed good assistant effects in treating patients with liver cirrhosis caused ascites of ES and DS type respectively.</p>