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1.
Article in Chinese | WPRIM | ID: wpr-879151

ABSTRACT

The paclitaxel-loaded and folic acid-modified poly(lactic-co-glycolic acid) nano-micelles(PTX@FA-PLGA-NMs) were prepared by the emulsion solvent evaporation method, and the parameters of paclitaxel-loaded nano-micelles were optimized with the particle size and PDI as evaluation indexes. The morphology of the nano-micelles was observed by transmission electron microscopy(TEM), and the stability, drug loading and encapsulation efficiency were systematically investigated. In vitro experiments were performed to study the cytotoxic effects of nano-micelles, apoptosis, and cellular uptake. Under the optimal parameters, the nano-micelles showed the particle size of(125.3±1.2) nm, the PDI of 0.086±0.026, the zeta potential of(-20.0±3.8) mV, the drug loading of 7.2%±0.75%, and the encapsulation efficiency of 50.7%±1.0%. The nano-micelles were in regular spherical shape as observed by TEM. The blank FA-PLGA-NMs exhibited almost no inhibitory effect on the proliferation and growth of tumor cells, while the drug-loaded nano-micelles and free PTX exhibited significant inhibitory effects. The IC_(50) of PTX@FA-PLGA-NMs and PTX was 0.56 μg·mL~(-1) and 0.66 μg·mL~(-1), respectively. The paclitaxel-loaded nano-micelles were potent in inhibiting cell migration as assessed by the scratch assay. PTX@FA-PLGA-NMs had good pro-apoptotic effect on cervical cancer HeLa cells and significantly promoted the uptake of HeLa cells. The results of in vitro experiments suggested that PTX@FA-PLGA-NMs could target and treat cervical cancer HeLa cells. Therefore, as nanodrug carriers, PTX@FA-PLGA-NMs with anti-cancer activity are a promising nano-system for improving the-rapeutic effects on tumors.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Drug Carriers , Female , Folic Acid , Glycolates , HeLa Cells , Humans , Micelles , Paclitaxel , Particle Size , Uterine Cervical Neoplasms/drug therapy
2.
Article in Chinese | WPRIM | ID: wpr-828092

ABSTRACT

The aim of this paper was to explore the effect of Xueshuantong Injection(freeze-dried powder,XST) on κ-carrageenan-induced thrombosis and blood flow from the aspects of interactions among blood flow,vascular endothelium and platelets. Fifty male Sprague-Dawley rats(190-200 g) were randomized into five groups: control group, model group, heparin sodium(1 000 U·kg~(-1)) group, low-dose and high-dose(50, 150 mg·kg~(-1)) XST groups. Rats were intraperitoneally injected with corresponding drugs and normal saline(normal control and model groups) for 10 days. One hour after drugs were administered intraperitoneally on the 7 th day, each rat was injected with κ-carrageenan(Type Ⅰ, 1 mg·kg~(-1)) which was dissolved in physiological saline by intravenous administration in the tail to establish tail thrombus model. The lengths of black tails of the rats were measured at 2, 6, 24 and 48 h after modeling. Vevo®2100 small animal ultrasound imaging system was used to detect the internal diameter of rat common carotid artery, blood flow velocity and heart rate, and then the blood flow and shear rate were calculated. Meanwhile, the microcirculatory blood flow perfusion in the thigh surface and tail of rats were detected by laser speckle blood flow imaging system. Platelet aggregometry was used to detect the max platelet aggregation rate in rats. Pathological changes in tail were observed through hematoxylin-eosin staining, and Western blot was used to detect the protein content of platelet piezo1. According to the results, XST could inhibit the rat tail arterial thrombosis and significantly reduce the length of black tail(P<0.05). The blood flow of common carotid artery in XST low dose group was significantly higher than that in the model group(P<0.05). XST high dose group could significantly increase the microcirculatory blood flow perfusion of the tail in rats as compared with the model group(P<0.05). XST high dose group could significantly inhibit platelet aggregation rate(P<0.05) and XST low dose group could significantly inhibit platelet piezo1 protein expression(P<0.01). In summary, XST could play an effect in fighting against thrombosis induced by κ-carrageenan in rats, which may be related to significantly inhibiting platelet aggregation, improving body's blood flow state, maintaining normal hemodynamic environment and affecting mechanical ion channel protein piezo1.


Subject(s)
Animals , Drugs, Chinese Herbal , Male , Microcirculation , Rats , Rats, Sprague-Dawley , Thrombosis
3.
Acta Pharmaceutica Sinica ; (12): 2501-2509, 2020.
Article in Chinese | WPRIM | ID: wpr-837510

ABSTRACT

It is now widely accepted that platelet aggregation plays an important role in physiological hemostasis and pathological thrombosis associated with cardiovascular and cerebrovascular diseases. Anti-platelet aggregation drug research is also a hot spot of current research. The biggest challenge of antiplatelet therapy has been the molecular overlap of the hemostasis and thrombosis, leading to a serious risk of bleeding. Recent studies have emphasized the importance of shear stress generated from blood flow, which will primarily drive platelet activation and aggregation in thrombosis. So if we can take advantage of the differences between the physiological and pathological vascular blood flow environment, the development of selective anti-platelet therapy may be a safer treatment for cardiovascular and cerebrovascular diseases. In this review, we discuss the underlying mechanisms of shear-induced platelet activation. Later, we summarize the effects and mechanisms of compounds and traditional Chinese medicine on shear-induced platelet activation. The aim is to provide a reference for the study of biological pharmacology of traditional Chinese medicine for promoting blood circulation and removing blood stasis.

4.
Article in Chinese | WPRIM | ID: wpr-801858

ABSTRACT

Objective:To investigate the effect of Shenghuitang on learning and memory, biological clock gene[brain and muscle arnt-like 1 (Bmal1)] in hypothalamus and interleukin-6(IL-6)and tumor necrosis factor-α(TNF-α)in hippocampus of APP/PS1 double transgenic dementia model mice, in order to explore the possible mechanism of Shenghuitang to improve learning and memory and sleep disorders. Method:The experimental mice were randomly divided into model group, blank control group, melatonin group, high-dose Shenghuitang group and low-dose Shenghuitang group. Autonomic activity analysis system was used to detect the autonomic activities of mice in each group. Morris water maze was used to detect the learning ability and spatial memory ability of each group. quantitative real-time fluorescence polymerase chain reaction(Real-time PCR) was used to detect the expression of Bmal1 mRNA in the hypothalamic area of mice. Western blot was used to detect the expression of Bmal1 protein in each group. The content of inflammatory factors IL-6 and TNF-α in hippocampus of mice was detected by enzyme-linked immunosorbent assay(ELISA). The correlation between inflammatory factors IL-6, TNF-α and Bmal1 gene was analyzed by pearson analysis. Result:The results of voluntary activities showed that compared with the control group, the number of activities and activity distance of the model group were significantly decreased (PPPPPPPPPPPPPPα in the model group were significantly higher than those in the control group (Pα in the drug group were significantly lower(Pα and Bmal1 were correlated and negatively correlated. Conclusion:Shenghuitang may reduce the levels of inflammatory factors IL-6 and TNF-α in hippocampus by up-regulating the expression of Bmal1 gene in hypothalamic region, thus improving Alzheimer' s disease(AD) and circadian rhythm disorders.

5.
Article in Chinese | WPRIM | ID: wpr-801700

ABSTRACT

Objective: To observe the effect of Shenghuitang on learning and memory and expressions of interleukin-6(IL-6), tumor necrosis factor-α(TNF-α) and cyclooxygenase-2(COX-2) in hippocampus of chronic sleep deprived mice, in order to explore the possible mechanism of Shenghuitang in improving learning and memory ability. Method: Mice were randomly divided into sleep deprivation group, blank group, melatonin group(7.8×10-4 g·kg-1·d-1), high, middle and low-dose Shenghuitang groups(54,27,13.5 g·kg-1·d-1). The model of chronic sleep deprivation in mice was established using the "multi-platform water environment method". 28 d sleep deprivation and intragastric administration were provided. Morris water maze was used to detect the learning and memory ability of mice in each group. Real time-PCR was used to detect mRNA expressions of IL-6, TNF-α and COX-2 in the hippocampus of each group. Result: The results of Morris water maze test showed that compared with the blank group, the total time spent on finding the platform and the total swimming distance of the model group were significantly prolonged (PPPPPPPPPα, and COX-2 were increased in the model group compared with the blank group. Compared with the model group, mRNA expressions of IL-6, TNF-α, and COX-2 were decreased in the treated group. COX-2 mRNA expression was down-regulated. Conclusion: Shenghuitang may improve the learning and memory ability of mice by decreasing mRNA expressions of IL-6, TNF-α and COX-2 in hippocampus.

6.
Article in Chinese | WPRIM | ID: wpr-771716

ABSTRACT

On the basis of chemical content determination, the bioassay methods can be used to comprehensively evaluate and control the Chinese medicine compound. This paper analyzed the newly published literature on traditional Chinese medicine(TCM) bioassay. The selection of standard control substances and the establishment of experimental system are the main difficulties in bioassay. At present, the standard control substances mainly include: different sources of products with basically similar components, certified medicinal materials, genuine medicinal materials, commonly used chemical drugs or biological products with similar pharmacological functions, as well as Chinese medicine potency conversed by activity of biological products. In this paper, the common bioassays would be summarized from the clinical efficacy of activating blood circulation and removing stasis and clearing heat and detoxification. It is one of the important contents in the industrial production of traditional Chinese medicine to gradually establish the bioassay platform of Chinese medicine from the enterprise's internal control to the industry. recognition.


Subject(s)
Biological Assay , Drugs, Chinese Herbal , Reference Standards , Medicine, Chinese Traditional , Quality Control
7.
Article in Chinese | WPRIM | ID: wpr-705303

ABSTRACT

OBJECTIVE To explore the mechanisms of the volatiles of Wendan granule for the treatment of senile dementia,network pharmacology method integrating absorption,distribution,metab-olism, and excretion (ADME) screening, target fishing, network constructing, pathway analyzing, and correlated diseases prediction was applied. METHODS Twelve small molecular compounds of WDG were selected as the objects from 74 volatiles with the relative abundances above 2%,and their ADME parameters were collected from Traditional Chinese Medicine Systems Pharmacology platform (TCMSP), and then the corresponding targets, genes, pathways and diseases were predicted according to the data provided by TCMSP,DrugBank,Uniport and the Database for Annotation,Visualization and Integrated Discovery(DAVID).The related pathways and correlation analysis were explored by the Kyoto Encyclo-pedia and Genomes (KEGG) database. Finally, the networks of compound-target, target-pathway and pathway-disease of WDG were constructed by Cytoscape software. RESULTS Twelve compounds interacted with 49 targets, of which top three targets were Gamma-aminobutyric acid receptor subunit alpha-1 (GABRA1), Prostaglandin G/H synthase 2 (PGHS-2) and Sodium-dependent noradrenaline transporter.Interestingly,these targets were highly associated with depression,insomnia and Alzheimer′s disease that mainly corresponded to mental and emotional illnesses. CONCLUSION The integrated network pharmacology method provides precise probe to illuminate the molecular mechanisms of volatiles of WDG for relieving senile dementia related syndromes,which will also facilitate the application of traditional Chinese medicine in modern medicine,as well as follow-up studies such as upgrading the quality stan-dard of clinical medicine and novel drug development.

8.
Tianjin Medical Journal ; (12): 314-317, 2018.
Article in Chinese | WPRIM | ID: wpr-698034

ABSTRACT

Objective To study the fundus diseases that primary and middle school students may be susceptible to suffer, and to understand the prevalence rate and constituent ratio of these diseases. Methods A total of 9 504 students were examined from November 2015 to February 2017 to find out their ocular fundus conditions. They were from all the primary and secondary schools directly subordinate to Dagang Oilfield headquarters. Among the 9 504 participants 4 998 were male and 4 506 were female,with the age span of 5 to 23 and the average age of(13.40±3.41).Our medical examination included uncorrected visual acuity examination and fundus oculi photography. The distribution of fundus diseases was analyzed,including gender,vision acuity and age composition of patients with major diseases. Results Among the 9 504 students,4 314 had emmetropic eyes,and 5 190 had refractive errors.A total of 9 126 out of the 9 504 examined students had normal ocular fundus(96.02%),while those with abnormal ocular fundus accounted for 378(3.98%).The main types of abnormal ocular fundus included the tessellation fundus 354 (3.72%), followed by the large depression of optic disk 16 (0.17%). Among all the 354 cases with tessellation fundus, 179 were male and 175 were female. There were 257 students whose visual acuity≤0.3/0.3,and the prevalence was higher in 17-19 years old students(5.86%).Conclusion It has been revealed in this epidemiological survey that the main abnormal ocular fundus of primary and middle school students in Dagang is tessellation fundus.Most of the tessellation fundus are caused by middle and high myopia,and very few are found in emmetropic students. It has also been found that the incidence of tessellation fundus increases significantly with the increase of age. The large depression of optic disk ranks the second in the abnormal ocular fundus, which is mostly physiological.

9.
Article in Chinese | WPRIM | ID: wpr-230949

ABSTRACT

To investigate the anti-platelet adhesive effect and possible mechanisms of Xueshuantong capsule (XST) under flow conditions. Human umbilical vein endothelial cells (HUVECs) and human platelets were employed as experimental materials, and TNF-α (20 μg•L⁻¹) was used to establish vascular endothelial cell injury models. In vivo flow conditions were simulated under controlled shear stress of 0.1 Pa and 0.9 Pa by Bioflux1000 assays accordingly. Anti-platelet adhesive effects of XST at 0.3 g•L⁻¹ were dynamically monitored by microscopic time-lapse photography. Western blotting was employed to detect the VCAM-1 expression on endothelial cells, and the release of 6-keto-PGF1α and TXB2 was tested by radioimmunoassay. The results showed that XST could inhibit the platelets adhesion under both physiological and pathological flow conditions, and the inhibition rate was 15.0% and 34.1% respectively. Under pathological low shear stress or static conditions, XST could significantly inhibit endothelial cells VCAM-1 expression and TXB2 release (P<0.05). These results suggested that XST inhibited platelets adhering to injured endothelium via decreasing VCAM-1 expression and TXA2 secretion from endothelium. From the interactions among blood flow, vascular endothelium and platelets, the anti-thrombosis effects of XST were possibly related to endothelial cells protection and therefore inhibiting platelets adhesion. Under different flow conditions, the antiplatelet adhesion effect of XST was different, and the pathological low shear stress was more conducive to the efficacy of XST.

10.
Article in Chinese | WPRIM | ID: wpr-258498

ABSTRACT

Sophorae Tonkinensis Radix et Rhizoma, which has been commonly used in clinic, shows activities in antitumor, antivirus, antibacteria, analgesia, anti-inflammation, anti-liver injury, anti-oxidation and immune enhancement, but can cause liver toxicity, neurotoxicity, gastrointestinal toxicity and respiratory toxicity. Its pharmacological effect and toxicity are related to extraction process, dosage and administration time. Therefore, exploration of appropriate extraction process, toxicity-effect dosage range, toxic substance basis provides guarantee for attenuation and safe clinical medication.

11.
Article in Chinese | WPRIM | ID: wpr-610684

ABSTRACT

Background:With the progress and widely application of endoscopic techniques,the prevalence rate of periampullary diverticulum (PAD)is increasing in recent years. However,the results of studies investigating the correlation of PAD and its types with common bile duct (CBD)stone are different. Aims:To investigate the influence of PAD and its types on CBD stone. Methods:A total of 1524 consecutive inpatients who underwent diagnostic and therapeutic ERCP for pancreatobiliary diseases from Jan. 2014 to Dec. 2016 at the General Hospital of Xinjiang Military Region of Chinese PLA were enrolled and divided into two groups according to the presence or absence of PAD. Patients in PAD group were further classified into 3 subgroups by the papilla's location with respect to the diverticulum. Their clinical data were collected and retrospectively analyzed. Results:The proportion of elderly patients (≥60 years old)in PAD group was 82. 2% (310 /377),which was significantly higher than that in non-PAD group [60. 8% (697 / 1147),P < 0. 05]. The prevalences of CBD stone,gallstone associated with CBD stone,post-cholecystectomy and recurrent CBD stone were higher and the size of CBD stone was larger in PAD group than in non-PAD group (P all < 0. 05). Furthermore,stratified analysis revealed that the CBD stone was more prevalent and the size of stone was larger in type Ⅱ PAD than in type Ⅰ and type Ⅲ PAD (P <0. 05), while recurrent CBD stone was more frequent in type Ⅰ and type Ⅱ PAD than in type Ⅲ PAD (P < 0. 05). Multivariate analysis indicated that the elderly and PAD were the risk factors for recurrence of CBD stone,and cholecystectomy was a protective factor. Conclusions:The elderly is predisposed to PAD. PAD and its types are associated with the development and recurrence of CBD stone. CBD stone is more prevalent in patients with PAD especially type Ⅱ PAD. The size of stone is larger and the post ERCP recurrence rate is high in type Ⅱ PAD.

12.
Article in Chinese | WPRIM | ID: wpr-335745

ABSTRACT

Based on the different category of syndromes between traditional Chinese medicine(TCM) and Western medicine, the relationship between the efficacy and non-clinical toxicity of the TCM was analyzed. If TCM preparations have the same pharmacological targets to treat disease with modern medicine or the Chinese herbal preparations treat the diseases with its toxicity, their toxicity often exhibits the amplification and extension of activity; on the other hand, if TCM preparations have overlapped pharmacological targets but not completely the same with modern medicine, or if they have totally different pharmacological targets, the toxicity of TCM could not be inferred by pharmacological activity. With the great progress in extraction and separation technique for active parts of TCM as well as the application of some novel technique and excipients, some toxicity may be from the reactions unrelated with the pharmacological activity. In conclusion, better design and quality control could be obtained by understanding the relationship between pharmacological and toxicological study for the investigation of new traditional medicine.

13.
Article in Chinese | WPRIM | ID: wpr-607507

ABSTRACT

Background:The diagnostic accuracy of APRI and FIB-4 for liver fibrosis in patients with chronic hepatitis B is nothigh,especially for significant liver fibrosis (F≥2). Noninvasive diagnosis for liver fibrosis has become a research hotspot;and the diagnostic value of APRI combined with FIB-4 is not clear. Aims:To investigate the diagnostic value ofAPRI combined with FIB-4 for significant liver fibrosis in patients with chronic hepatitis B. Methods:A total of 171patients with chronic hepatitis B from January 2011 to October 2016 at General Hospital of Xinjiang Military Region wereenrolled. Liver biochemical indices,routine blood test and liver biopsy pathology were performed. APRI and FIB-4 werecalculated,ROC curve was drawn,and cutoff value of APRI and FIB-4 for diagnosing significant liver fibrosis wasdetermined,and mode of APRI combined with FIB-4 for diagnosing significant liver fibrosis was established. Results:Withthe increase in degree of liver fibrosis,APRI and FIB-4 were gradually increased (P < 0. 05). Area under ROC curve(AUC)for APRI and FIB-4 were 0. 812 and 0. 770,respectively. The sensitivity of FIB-4 for diagnosing significant liverfibrosis was higher than that of APRI. Sensitivity,specificity,negative predictive value,positive predictive value,andaccuracy of APRI combined with FIB-4 for diagnosing significant liver fibrosis were superior to APRI or FIB-4 used alone;and the specificity,accuracy of mode 2 were superior to mode 1. Conclusions:APRI combined with FIB-4 can increasethe accuracy for diagnosing significant liver fibrosis.

14.
Article in Chinese | WPRIM | ID: wpr-231010

ABSTRACT

In this study, an HPLC method was developed for simultaneous determination of seven alkaloids (cytosine, oxymatrine, N-oxysophocarpine, N-methylcytisine, sophoranol, matrine, and sophocarpine) and three flavonoids (trifolirhizin, fermononetin, and maackiain) from different samples of Sophorae Tonkinensis Radix et Rhizoma. Samples were analyzed on a Welch XtimateTM C₁₈ column (4. 6 mm× 250 mm, 5 μm) eluted with the mobile phase of acetonitrile (A) and 0.01 mol•L⁻¹ ammonium acetate solution (pH 8.0) (B) in a linear gradient mode as follows: 0-20 min,4%-14% A;20-30 min,14%-25% A;30-45 min,25%-40% A;45-65 min,40%-55% A;65-75 min,55% A. The flow rate of the mobile phase, the column temperature, and the PDA detector wavelength were set at 1.0 mL•min⁻¹, 30 ℃, and 225 nm, respectively. For the method validation, these ten compounds showed good separation and satisfactory linearity (r≥0.999 7) within the concentration ranges tested. The mean recoveries were in the range of 98.60% to 102.6% with the RSD (n=6) between 0.60% and 3.7%. This method was proved to be simple, accurate and repeatable. The quantitative results showed that there were significant differences in the contents of seven alkaloids and three flavonoids among the different samples. This result revealed that the quality of Sophorae Tonkinensis Radix et Rhizoma varied widely. This method could be used for the simultaneous determination of the multi-ingredients from Sophorae Tonkinensis Radix et Rhizoma, which might provide scientific evidences to evaluate/control the quality of Sophorae Tonkinensis Radix et Rhizoma, comprehensively.

15.
Article in Chinese | WPRIM | ID: wpr-230073

ABSTRACT

PNS (total saponins of Panax notognseng, PNS) has a clear effect and wide application prospect for cardiovascular diseases. At the same time, saponins have hemolytic properties, which are related to its molecular structure type and dosage. On one hand, this article summarizes the research progress of PNS in heart cerebrovascular pharmacology pharmacological in recent five years, a number of studies both in vitro and in vivo for overall body, organs, cells and molecules, show that PNS could improve myocardial and cerebral ischemia injury, and it has effects in resisting thrombosis, inflammation, oxidation, atherosclerosis, and modulating vascular endothelial cells function and improving the cerebral ischemia injury etc. On the other hand, the hemolysis effect of PNS is closely related to its molecular structure type and administrating dosage. Different structures bring about different hemolysis activities. Structure-activity relationship suggests that the length of sugar side chains attached to C-20 and the disaccharide connection mode on C-3 may influence the hemolysis activity of PNS. Within the dose range from 2.5 to 250 mg•L⁻¹, PNS has no hemolysis activity. However, PNS exhibits hemolytic properties at high concentrations(≥500 mg•L⁻¹). Based on the hemolytic or anti-hemolysis characteristics of saponins, and dose-response relationship, the rational clinical application of PNS can be guaranteed by controlling the ratio of hemolytic monosaponins in PNS and improving the hemolytic test method.

16.
Acta Pharmaceutica Sinica ; (12): 973-979, 2015.
Article in Chinese | WPRIM | ID: wpr-257039

ABSTRACT

The dosage-efficacy/toxicity relationship of the 50% alcohol extracts of Polygonum multiflorum was comparatively investigated on either normal or CCl4-induced chronic liver injury rats, by determining the general condition, serum biochemical indices and liver histopathology, coupled with the factor analysis. The dosages were 10 and 20 g raw materials per kg body weight. Compared with the normal control group, the normal high dose group showed significant increases of the serum alanine transaminase (ALT), total bilirubin (TBIL), high mobility group box 1 (HMGB-1) and interleukin-1β (IL-1β) (P < 0.05 or P < 0.01), as well the frequent incidences of inflammatory cell infiltration, hepatic sinus enlargement and fiber stripes formation in histopathological sections. Compared with the model control group, the model low dose group showed significant declines of serum ALT, aspartate transaminase (AST) and total bile acid (TBA) (P < 0.05), as well the alleviation of vacuoles of hepatocytes, but no amelioration of the inflammatory cell infiltration and fibrous tissue hyperplasia; moreover, the model high dose group showed significant degeneration declines of serum HMGB-1, tumor necrosis factor-α (TNF-α) and IL-1β (P < 0.05, P < 0.01), as well the evident alleviation of vacuoles degeneration of hepatocytes, inflammatory cells infiltration and fibrosis degree. The factor analysis showed that the low dosage treatment had almost neither injuring effect on the normal rats nor protective effect on the model rats; while the high dosage treatment showed observable injuring effect on the normal rats, expressed by the significant increases of the factor-1 (HMGB-1, TNF-α and IL-1β as the main contributors) and factor-2 (TBIL, ALT and TBA as the main contributors) relative to the normal control group. The liver protective effect of the high dosage treatment could be observed with the significant reduction of the factor-1, indicating the effective alleviation of the expression of inflammatory cytokines. In conclusion, it could illustrated the phenomenon of symptom-based prescription theory of Polygonum multiflorum on rat livers: the high dosage of the herb had either an injuring effect on normal rats, or a therapeutic effect on the rats with chronic liver injury.


Subject(s)
Alanine Transaminase , Blood , Animals , Aspartate Aminotransferases , Blood , Bile Acids and Salts , Metabolism , Bilirubin , Blood , Chemical and Drug Induced Liver Injury , Drug Therapy , Drugs, Chinese Herbal , Pharmacology , Fallopia multiflora , Chemistry , HMGB1 Protein , Metabolism , Hepatocytes , Interleukin-1beta , Metabolism , Liver , Pathology , Plant Extracts , Pharmacology , Rats , Tumor Necrosis Factor-alpha , Metabolism
17.
Article in Chinese | WPRIM | ID: wpr-250447

ABSTRACT

A in vitro platelet aggregation bioassay was developed for the quality control of XST capsules. The in vitro anti-platelet aggregation effect in rats was observed to detect the bioactivity of XST capsules. Panax notoginseng saponins and Xuesaitong lyophilizedpowder for injection were taken as standard control substances to determine the potency. According to the results, XST capsules showeda significant inhibitory effect on thrombin-induced platelet aggregation in a dose-dependent manner. The in vitro anti-platelet activity oflyophilized powder for injection was stabler than that of Panax notoginseng saponins, and so suitable to serve as a standard control substance. The biological potency of XST capsules compared with standard control substance was detected by using parallel line assay. According to the results, the established bioassay method had a good repeatability (RSD 2.92%). The sample test results could pass thereliability test(linear deviation P > 0.05, parallel deviation P > 0.05). This bioassay method could be used as one of the complementary quality control methods for XST capsules.


Subject(s)
Animals , Capsules , Pharmacology , Drugs, Chinese Herbal , Pharmacology , Male , Panax notoginseng , Chemistry , Platelet Aggregation , Platelet Aggregation Inhibitors , Pharmacology , Rats , Rats, Sprague-Dawley , Saponins , Pharmacology
18.
Acta Pharmaceutica Sinica ; (12): 28-33, 2015.
Article in Chinese | WPRIM | ID: wpr-251822

ABSTRACT

The liver injury induced by Polygonum multiflorum Thunb. (PM) was investigated based on idiosyncratic hepatotoxicity model co-treated with lipopolysaccharide (LPS) at a non-hepatotoxic dose. Sprague-Dawley (SD) rats were intragastrically administered with three doses (18.9, 37.8, 75.6 g crude drug per kg body weight) of 50% alcohol extracts of PM alone or co-treated with non-toxic dose of LPS (2.8 mg·kg(-1)) via tail vein injection. The plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities were assayed and the isolated livers were evaluated for histopathological changes. The dose-toxicity relationships of single treatment of PM or co-treatment of LPS were investigated comparatively to elucidate the idiosyncratic hepatotoxicity of PM. The results showed that no significant alterations of plasma ALT and AST activities were observed in the groups of solo-administration of LPS (2.8 mg·kg(-1), i.v.) or different dosage (18.9, 37.8 and 75.6 g·kg(-1), i.g.) of PM, compared to normal control group (P > 0.05); while significant elevations were observed in the co-administration groups of PM and LPS. Treatment with LPS alone caused slight infiltration of inflammatory cells in portal area but no evident hepatocytes injury. Co-treatment with LPS and PM (75.6 g·kg(-1), i.g.) caused hepatocyte focal necrosis, loss of central vein intima and a large number of inflammatory cell infiltration in portal areas. When further reduce the dosage of PM, significant increases of plasma ALT and AST activities (P < 0.05) were still observed in co-administration groups of LPS and PM (1.08 or 2.16 g·kg(-1)), but not in LPS or PM solo-administration groups. Nevertheless, the co-treatment of low dosage of PM (0.54 g·kg(-1)) with LPS did not induce any alteration of plasma ALT and AST. In conclusion, intragastric administration with 75.6 g·kg(-1) of PM did not induce liver injury in normal rats model; while the 2 folds of clinical equivalent dose of PM (1.08 g·kg(-1)) could result in liver injury in the LPS-based idiosyncratic hepatotoxicity model, which could be used to evaluate the idiosyncratic hepatotoxicity of PM.


Subject(s)
Alanine Transaminase , Blood , Animals , Aspartate Aminotransferases , Blood , Chemical and Drug Induced Liver Injury , Pathology , Hepatocytes , Pathology , Lipopolysaccharides , Polygonum , Toxicity , Rats , Rats, Sprague-Dawley
19.
Acta Pharmaceutica Sinica ; (12): 973-9, 2015.
Article in Chinese | WPRIM | ID: wpr-483404

ABSTRACT

The dosage-efficacy/toxicity relationship of the 50% alcohol extracts of Polygonum multiflorum was comparatively investigated on either normal or CCl4-induced chronic liver injury rats, by determining the general condition, serum biochemical indices and liver histopathology, coupled with the factor analysis. The dosages were 10 and 20 g raw materials per kg body weight. Compared with the normal control group, the normal high dose group showed significant increases of the serum alanine transaminase (ALT), total bilirubin (TBIL), high mobility group box 1 (HMGB-1) and interleukin-1β (IL-1β) (P < 0.05 or P < 0.01), as well the frequent incidences of inflammatory cell infiltration, hepatic sinus enlargement and fiber stripes formation in histopathological sections. Compared with the model control group, the model low dose group showed significant declines of serum ALT, aspartate transaminase (AST) and total bile acid (TBA) (P < 0.05), as well the alleviation of vacuoles of hepatocytes, but no amelioration of the inflammatory cell infiltration and fibrous tissue hyperplasia; moreover, the model high dose group showed significant degeneration declines of serum HMGB-1, tumor necrosis factor-α (TNF-α) and IL-1β (P < 0.05, P < 0.01), as well the evident alleviation of vacuoles degeneration of hepatocytes, inflammatory cells infiltration and fibrosis degree. The factor analysis showed that the low dosage treatment had almost neither injuring effect on the normal rats nor protective effect on the model rats; while the high dosage treatment showed observable injuring effect on the normal rats, expressed by the significant increases of the factor-1 (HMGB-1, TNF-α and IL-1β as the main contributors) and factor-2 (TBIL, ALT and TBA as the main contributors) relative to the normal control group. The liver protective effect of the high dosage treatment could be observed with the significant reduction of the factor-1, indicating the effective alleviation of the expression of inflammatory cytokines. In conclusion, it could illustrated the phenomenon of symptom-based prescription theory of Polygonum multiflorum on rat livers: the high dosage of the herb had either an injuring effect on normal rats, or a therapeutic effect on the rats with chronic liver injury.

20.
Acta Pharmaceutica Sinica ; (12): 28-33, 2015.
Article in Chinese | WPRIM | ID: wpr-457207

ABSTRACT

The liver injury induced by Polygonum multiflorum Thunb. (PM) was investigated based on idiosyncratic hepatotoxicity model co-treated with lipopolysaccharide (LPS) at a non-hepatotoxic dose. Sprague-Dawley (SD) rats were intragastrically administered with three doses (18.9, 37.8, 75.6 g crude drug per kg body weight) of 50% alcohol extracts of PM alone or co-treated with non-toxic dose of LPS (2.8 mg·kg(-1)) via tail vein injection. The plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities were assayed and the isolated livers were evaluated for histopathological changes. The dose-toxicity relationships of single treatment of PM or co-treatment of LPS were investigated comparatively to elucidate the idiosyncratic hepatotoxicity of PM. The results showed that no significant alterations of plasma ALT and AST activities were observed in the groups of solo-administration of LPS (2.8 mg·kg(-1), i.v.) or different dosage (18.9, 37.8 and 75.6 g·kg(-1), i.g.) of PM, compared to normal control group (P > 0.05); while significant elevations were observed in the co-administration groups of PM and LPS. Treatment with LPS alone caused slight infiltration of inflammatory cells in portal area but no evident hepatocytes injury. Co-treatment with LPS and PM (75.6 g·kg(-1), i.g.) caused hepatocyte focal necrosis, loss of central vein intima and a large number of inflammatory cell infiltration in portal areas. When further reduce the dosage of PM, significant increases of plasma ALT and AST activities (P < 0.05) were still observed in co-administration groups of LPS and PM (1.08 or 2.16 g·kg(-1)), but not in LPS or PM solo-administration groups. Nevertheless, the co-treatment of low dosage of PM (0.54 g·kg(-1)) with LPS did not induce any alteration of plasma ALT and AST. In conclusion, intragastric administration with 75.6 g·kg(-1) of PM did not induce liver injury in normal rats model; while the 2 folds of clinical equivalent dose of PM (1.08 g·kg(-1)) could result in liver injury in the LPS-based idiosyncratic hepatotoxicity model, which could be used to evaluate the idiosyncratic hepatotoxicity of PM.

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