Showing papers in "Chinese Pharmacological Bulletin in 2002"

Study on the interactions of berberine displace other drug from their plasma proteins binding sites

Abstract: AIM To study the interaction induced by berberine(Ber) displacing protein binding of warfarin(War),thiopental(Thi) and tolbutamide(D 860 ). METHODS Using the balance dialysis method, observed effect of Ber on War concentration in dialysate of dialysis tubing outside; using the slide method, observed effect of Ber on coagulation time of the mice administrated War; using right reflex method, observed effect of Ber on sleep time of the mice administrated Thi; determining level of blood glucose of the mice, observed effect of Ber on action of D 860 . RESULTS War concentration of the solution out dialysis tubing of War+Ber group were higher( P 0 01), compared with War+PBS group. Ber can prolong coagulation time of the mice po War( P 0 01). Ber can prolong sleep time of the mice ip Thi( P 0 01). Ber can decrease the level of blood glucose of the mice po D 860 (compared with D 860 +NS group, P 0 01). CONCLUSION Ber can displace War, Thi and D 860 from their protein binding site, increase the blood level of free drug of them, and enhance their actions or toxicity.

The establishment of the dysmenorrhea model in mice

Abstract: AIM To establish a dysmenorrhea model in mice. METHODS The mice were given with some kinds of oestrogens once a day for 3～25 days. On the last day, the mice were injected intraperitoneally with oxytocin and the number of twisting body was recorded to evaluate the intensity of dysmenorrhea. The optimum conditions to establish the model was analysed statisticly. RESULTS The optimum oestrogens was stilbestrol. Stibestrol should be given for 12～15 days. The regression equation of the dose effect curve of stibestrol was =0 03±0 04 X, r =0 9688. The optimum dosage of oxytocin was 20 U·kg -1 . The dysmenorrhea model in mice could be preserved for about 7 days. 90% of the twisting body reactions concentrated in 0～30 minutes after oxytocin was given. The effect of oxytocin (20 U·kg -1 ) had significent difference with that of prostaoglantin (1 3 mg·kg -1 ). The test of uterus in vivo showed that stilbestrol could increase the uterine contraction frequency and strengthen the contractility. The dysmenorrhea model in mice was testified by some anti dysmenorrhea drugs. CONCLUSION Compared with the hypodermic implantation in rats, the dysmenorrhea model in mice was simple, reliable, economical and testifiable,etc.

Research development on the Immumodulatory effect of polysaccharide and its mechanism

Abstract: Polysaccharides are important large molecules in the body. It has many functions such as activting the lymphocytes like T,B, NK and MΦ cells, promoting the secretion of cytokines and antibodies through binding to the CR 3 receptor of lymphocytes, affecting the concentrations of cellar [Ca 2+ ] i, cAMP, cGMP, NO and PGE 2, and promoting the gene expression of cytokines. Its function also relate to its molecule weight and structure.

Experimental study of diet-induced obesity animal model

Abstract: AIM To observe the influence of high fat diet on the success rate of diet induced obesity rat. METHODS Rats of model group were fed with hight fat diet for 16 weeks then, the weight and Lee index were measured and compared with those of normal control group. RESULTS The weight and Lee index of model group rats were 491 62±46 89 and 319 04±9 49. Those of the normal control group rats were 394 2±50 78 and 304 63±5 99. There were significant difference between the two groups( P0 01 or P0 05 ). The rat of Epididymis, kidney, pericardium and the weight of Liver and Kidney were significantly decreased. There was significant difference between model and normal groups( P0 01 or P0 05) .CONCLUSION The high fat diet composed of 12% pork fat and 18% total tallow had obvious effect of inducing obesity. The induced fat rat reached 58 9%, which was higher than previous ones.

Effect of polysaccharides-2b from Mudan cortex on type 2 diabetes mellitus rats and its mechanism

Abstract: AIM To study the effect of polysaccharides 2b from Mudan cortex (PSM 2b) on type 2 diabetes mellitus (T2DM) rats and explore its mechanism. METHODS T2DM rat model was established by low dosage streptozotocin and high sucrose fat diet. The drugs were administrated by ig for 5 weeks. The serum glucose was assayed with GOD POD method. Insulin was determined by radioimmunoassay. Insulin receptors of the plasma membrane from rat liver were determined with radioligand binding assay of receptors (RBAR). RESULTS PSM 2b could significantly lower fasting blood glucose (FBG), improve impaired glucose telarance (IGT) and dyslipidemia. It could also remarkably raise receptor total (RT2) of the low affinity insulin receptor (InsR) and insulin sensitivity index (ISI) in T2DM rats. CONCLUSION PSM 2b has an obvious therapeatic effect on T2DM in rats. Its mechamsm is relatively improve insulin resistance (IR) in T2DM rats by raising the number of InsR.

Antithrombosis through activating endothelial target for acetylcholine and its molecular mechanism

Abstract: AIM To examine antithrombotic effects of arecoline on the arterial thrombosis induced by carrageenin in mice through modulating the functions of endothelium and determine its mechanisms from hemostatic system, the platelet aggregative functions and the bioactive factors released by vascular endothelial cells. METHODS Kappa carrageenin was given ip in mice and mice were fed at the temperature of 20 to 21 degrees and at the humidity of 30 percent to 50 percent. RESULTS On the foregoing models of thrombosis, arecoline could antagonize the formation of thrombosis through activating the endothelial target for acetylcholine in a dose dependent manner and its antithrombotic potency was 250 to 500 times greater than aspirin; while under the same conditions, pilocarpine could not antagonize the formation of thrombosis. The levels of TT, PT, KPTT and MAR had no prominent changes compaired with control groups. The levels of t-PA became higher greatly than normal and the levels of PAI 1 became lower greatly than normal 2 hours after intravenous injection of arecoline in rats. Arecoline could decrease the higher plasma levels of thromboxane A2 and increase the lower plasma levels of prostacyclin in a dose dependent manner in the mice tail thrombosis induced by carrageenin. CONCLUSION The antithrombotic effects of arecoline are associated with activating the endothelial target for acetylcholine closely, but are not associated with muscarinic receptors,and not relevant to hemostatic systems or functions of platelet aggregation directly.

Effects of coadministration of berberine chloride with cyclosporin on liver microsomal cytochrome P450 isoenzyme and mdr1 in rats

Abstract: AIM To study the effects of coadministration of berberine chloride(Ber) with cyclosporin (CsA) on liver microsomal cytochrome P450 isoenzyme and multi drug resistance gene in rats METHODS The activities of liver microsomal erythromycin demethylase(ERD) and aminopyrence N demethylase(ADM) were determined The levels of mRNA expression of CYP3A1, CYP1A1, CYP2E1, mdr1a and mdr1b were assayed with RT PCR RESULTS After administration for 6 days, all treatment groups except Ber at 100 mg·kg -1 exhibited inhibitory action on ERD activity in rats ERD activity markedly decreased in all drug treatment groups after taking drug for 12 days After administration for 6 days, 45 mg·kg -1 CsA, 100 mg·kg -1 Ber coadministrated with 45 mg·kg -1 CsA and 200 mg·kg -1 Ber plus 45 mg·kg -1 CsA had significant inhibitory effects on ADM activity in rats All groups except 100 mg·kg -1 Ber and 150 mg·kg -1 ketoconazole had the same effects on ADM activity after treatment for 12 days Again, after 12 days, all drug treatment groups except 100 mg·kg -1 Ber group was found of remarkable inhibition of the mRNA expression of CYP3A1, CYP2E1, mdr1a and mdr1b The CYP1A1 gene was not detected in all groups CONCLUSION The mechanism of Ber to increase CsA concentration is that Ber decreases the expression of CYP3A, mdr1a and mdr1b thereby reduces the metabolism and elimination of CsA by liver

Relation between animal models of RA and clinic

Abstract: Animal models of rheumatoid arthritis(RA)especially adjuvant arthritis(AA)in rats and collagen induced arthritis(CIA)in mice have much character similar to human RA in pathological mechanism,clinical representation and so on. The models are more ideal in investigating RA and selecting drugs of anti inflammation and immunity. To discuss the pathological mechanism and the relation between animal models of RA and clinic will be important not only to research RA in pathology,physiology,nervous endocrine immunity and so on,but also to find out safety and effective drugs of treatment RA. The articl summarizes several animal models of RA in establishment,pathological and clinical changes,inflammatory immune regulation and so on.

Apoptosis of human breast cancer MCF-7 cells induced by oxymatrine

Abstract: AIM To investigate the mechanism of apoptosis induced by oxymatrine on MCF 7 cell line METHODS Using light microscopy, electron microscopy, laser scanning confocal microscopy, flow cytometry (FCM) and DNA gel electrophoresis to demonstrate the presence of apoptosis RESULTS Morphological characteristics of apoptosis were observed on oxymatrine treated MCF 7 cells, such as condensation of nucleus, bubble of cytoplasm, fragment of nucleus, a ladder like pattern of DNA fragmentation in agarose gel eletrophoresis Laser scanning confocal microscopy showed decreasing of the content of DNA Sub G1 peak and increased S period ratio were analysed by FCM CONCLUSION Oxymatrine can induce the inhibition of cell growth by apoptosis and the mechanism of apoptosis is involved in blocking of S period cells

Effects of thymectomy on glucose metabolism in rats and modulation of rehmannia glutinosa oligosaccharides on glucose metabolism in thymectomized rats

Abstract: AIM To observe the changes of blood glucose level, plasma insulin level and liver glycogen content and regulatory effects of rehmannia glutinosa oligosaccharides(ROS) on glucose metabolism in thymectomized rats METHODS ①Plasma glucose level, liver glycogen content and plasma insulin level of thymectomized rats were determined three,four, eight and fifteen month after thymectomy operation; ②Effects of ROS (250 mg·kg -1 , po ,×60 d) on spleencyte proliferation,blood glucose level,liver glycogen content, plasma insulin level and plasma corticosterone level in thymectomized rats were investigated seven month after thymectomy RESULTS From 8 months after thymectomy liver glycogen content and plasma insulin level increased in thymectomized rats, though no obvious changes in blood glucose level were found during the experiment; ②Changes of glucose metabolism in thymectomized rats were largely reversed and normalized with ROS: Increased liver glycogen content turned to be normal,increased plasma insulin level,decreased corticosterone level and decreased splenocyte proliferation in thymectomized rats became normal CONCLUSION Some changes in glucose metabolism are induced by thymectomy in rats, which can be largely reversed by ROS

Effects of four extracts of traditional Chinese medicinal materials on the proliferation of human lung cancer A549 cell line

Abstract: AIM To study the influence of four extracts of traditional Chinese medicinal materials(sodium cantharidinate, matrine, cinobufotain and sodium ferlate) on the proliferation of human lung cancer A549 cell line and breast cancer MCF7 cell line;the possible mechanism of sodium ferlate on the inhibition of A549 cells. METHODS The inhibition of cell proliferation was determined by MTT assay and cell cycle was determined by flow cytometry. RESULTS All four extracts of traditional Chinese medicinal materials showed growth inhibition to breast cancer MCF7 cells while only sodium ferlate showed inhibition to lung cancer A549 cells. Synergistic inhibition was found when sodium ferlate was combined with each of the three commonly-used chemotheraputic drugs. Sodium ferlate could induce A549 cell apoptosis. CONCULSION The inhibition of cell proliferation induced is by sodium cantharidinate, matrine, and cinobufotain is quite different between different cancer cell lines. Sodium ferlate can inhibit cancer cell proliferation and show synergistic action while combined with chemotheraputic drugs. The mechanism of sodium ferlate on A549 cell proliferation seem to be related to the cell apoptosis.

Endothelial cell and angiogenesis

Abstract: Recent evidence suggests that, in spite of the redundancy of angiogenic factors involved in pathological angiogenesis , strategies aimed at inhibiting specific endothelial cell angiogenic factors at their release or receptor level may form the basis for effective and safe treatment of angiogenic mediated disease processes. Physiologic angiogenesis is fundamental to reproduction, development and repair. Pathological angiogenesis sustains the progression of many neoplastic and proinflammatory diseases. And endothelial cell is an important target especially for the angiogenesis. The target represents a novel strategy for the treatment of the human disorders where pathological angiogenesis is involved.

Distribution and pharmacokinetics of penehyclidine hydrochloride raceme and its four optical isomers in mice

Abstract: AIM To study the distribution and pharmacokinetics of penehyclidine hydrochloride(PH) raceme and its four optical isomers in mice. METHODS The tissue and blood concentration of PH raceme and its four optical isomers in mice were determined by gas chromatography mass spectrometry with selected ion monitoring(GC MS/SIM) PH(m/z 175) and PH 5 (m/z 180) as internal standard. RESULTS The concentration time curves in mice after im a single dose (0.1 mg·kg -1 ) could be fitted to first order absorption two compartments open model. The main pharmacokinetic parameters of PH raceme were as follows: T 1/2α 0.23 h, T 1/2β 3.28 h, T 1/2 K a 0.013 h, T max 0.067 h, C max 18.76 μg·L -1 , AUC 50.42 μg·L -1 . The speed of absorption and distribution of PH raceme in mice were fast.There were some differences for the level of the blood drug concentration of PH raceme and the four optical isomers within 8 hour after dosing the PH and four isomers, respectively. The R 2 isomer maintained a higher level of blood drug concentration compared with the other isomers. The drug concentration remained at a high level in submandibular glands and in brain for more than 48 h. The half life of PH in brain was 10.7 times greater than that in blood and 7.1 times greater than that in the submandibular glands. The distribution in mice brain showed that the concentration of R 2 isomer was high. And the isomer with S configuration in mice brain eliminated fast and isomer with R configuration eliminated slowly. The distribution in mice submandibular glands showed that the drug concentration of S 1 isomer had a high level and the elimination was slow. These findings suggest that S 1 isomer had a high affinity with mAChR in submandibular glands. CONCLUSION There is a close relationship between the concentration of the isomers in mice brain and submandibular gland and the affinity of the isomers to mAChR.

Apoptosis regulated by (-)-epigallocatechin-3-gallate in nasopharyngeal carcinoma cells using apoptosis cDNA expression array

Abstract: AIM To investigate the mechanism of apoptosis induced by (-) epigallocatechin 3 gallate (EGCG) and the intervenient effect of EGCG on apoptosis inducted by Epstein Barr(EB)virus latent membrane protein 1 (LMP1). METHODS The established doxycycline regulated nasopharyngeal carcinoma cell line pTet on LMP1 HNE2 were exposed to 0 6 mg·L -1 Dox and 100 mg·L -1 EGCG for 24 h. Total RNAs were extracted from cells hybridized with the Atlas apoptosis cDNA expression array membrane containing mainly apoptosis related genes. RESULT EGCG regulated several apoptosis related genes, they were either up or down regulated. CONCLUSION EGCG induced apoptosis might be mediated through some specific genes and signal transduction pathways, and the presence U of EGCG showed some intervenient effect on LMP1 induced cell apoptosis.

The effects of TGP on CJ-S_(131)-induced systemic lupus erythematosus-like model in mice

Abstract: AIM To investigate the effects of TGP on immunologic changes associated with CJ S 131 induced SLE like model in mice METHODS SLE like syndrome was induced by injection of CJ S 131 and CFAVarious doses of TGP were given by gavage once daily for 28 days RESULTS The levels of IgG anti single stranded DNA(ssDNA) and histone autoantibodies were increased in sera four weeks after injectionThe proliferation response of splencytes to ConA and LPS and the production of IL 1 were also increased TGP(50,100,200 mg·kg -1 ·d -1 ,ig) inhibited the aboved changes of SLE like mouse model partly or completely CONCLUSION The SLE mouse model was similar to idiopathic SLE in humans TGP has modulating effects on alternations of immunity of SLE like mouse model

Effects of extracts from Codonopsis pilosula and Atractylodes macrocephala on growth and differentiation of IEC-6 cells

Abstract: AIM To investigate the effects of extracts from dangshen (Codonopsis pilosula,D h) and baizhu (Atractylodes macrocephala, B t) individually and in combination on the proliferation and differentiation of rat small intestinal crypt like cell line (IEC 6). METHODS IEC 6 cells were plated and treated with D h, B t or D h+B t at 24 h to 48 h. The cell proliferation was estimated by MTT assay and the cell differentiation was observed under microscope after HE stainning. RESULTS Compared with control,D h promoted the cell growth in a dose dependence manner. While B t induced the cell differentiation. Treatment with D h plus B t resulted in a more significant increase of the cell proliferation than treatment with D h alone. CONCLUSION D h and B t both have effect on IEC 6 cells in which D h stimulated proliferation yet B t promoted differentiation. A treatment of D h plus B t stimulated IEC 6 cell proliferation more evidently than D h treatment alone suggesting that these two extracts have a synergistic action on IEC 6 cell proliferation.

Effects of resveratrol on secondary spinal cord edema and activity of lactic dehydrogenase and ATPase in experimental spinal cord injury of rats

Abstract: AIM To study the effects of resveratrol on secondary spinal cord edema and the activity of lactic dehydrogenase and Na +, K + ATPase in experimental spinal cord injury (SCI)rat. METHODS The weight dropping method was used to produce the experimental spinal cord injury in adult rats. Resveratrol (Res) and methylprednisolone (MPSS) were intraperitoneally by the bolus injections of 50 mg·kg -1 , 100 mg·kg -1 and 100 mg·kg -1 , respectively, immediately after the induction of SCI. And then the effects of Res were observed at 1 h, 24 h, 48 h after SCI compared with MPSS. RESULTS Res could obvious inhibit the secondary spinal cord edema with the most remarkable suppressing rate by 11 5% at 48 h. Res was able to significantly suppress the activities of the lactic dehydrogenase with the highest suppressing rate for over 40% at 24 h. In the meantime, Res markedly improved the Na +, K + ATPase activities that promoted to the biggest extent to 60% at 48 h. The effects of Res were the same as or even stronger than those of MPSS. CONCLUSION Res may effectively protect the spinal cord from secondary spinal cord edema and improve the energy metabolism system in SCI. It suggested that Res may be having potent therapeutic effect on SCI.

The effects of a diterpenoid compound 5F isolated from Pteris semipinnata L. on the expressions of several oncogenes of K562 cells

Abstract: AIM To study the effects of diterpenoid compound 5F (ent 11α hydroxy 15 oxo kaur 16 en 19 oic acid) isolated from Pteris Semipinnata L. on the expressions of Bcl 2?Bax?c Fos and c Jun of K562 cells. METHODS K562 cells were treated with compound 5F for 24 hours first. Then Western blotting was used to detect the effects of compound 5F on the expressions of Bcl 2?Bax?c Fos and c Jun. RESULTS The expression of Bcl 2 decreased while the expression of Bax, c Fos and c Jun increased after the treatment of 5F. CONCLUSIONS One possible mechanism of the anti tumor effects of compound 5F may be through up Bax, c Fos, c Jun and down Bcl 2 regulation.

Effect of dauricine on platelet aggregation of patients with acute myocardial infarction

Abstract: AIM To investigate the possibility of dauricine (DAU) to inhibit the irreversible platelet aggregation of patients with acute myocardial infarction (AMI). METHODS GlycoproteinⅣ (GPⅣ) and thrombospondin(TSP) levels on the membrane surface of the stationary platelet or platelet activated by thrombin(50?100? 500? 1 000 U·L -1 ) in 12 patients with AMI were measured with a washed platelet flowcytometric assay and compared with those of the healthy ( n =14). RESULTS The GPⅣ, TSP level of stationary platelet and activated platelet in patients with AMI were higher than those in the healthy significantly( P 0 05, 0 01), DAU (50 μmol·L -1 ) inhibited the GPⅣ membrane redistribution and the release of TSP from intracellular α granules induced by thrombin (50 U·L -1 , 100 U·L -1 , 500 U·L -1 ) apparently ( P 0 05, 0 01), inhibitory effect of DAU was not found in platelets activated with high concentraction of thrombin ( 1 000 U·L -1 ). CONCLUSION The activity and reactivity to thrombin of platelets increased in patients with AMI and DAU may have a blocking effect on the consolidation of platelet aggregation in AMI.

Advances in study on pharmacological effects of polyactin

Abstract: This paper summarizes the recent 6～7 year advances in the research of pharmacological effects of polyactin including mainly six aspects: ①Effects of polyactin on functions of macrophages in vitro ; ② Mechanism enhancive effect ofpolyactin on NK cell activity; ③Effects of polyactin on the human lymphocyte immunofunction; ④Effects of polyactin on the proliferation and cytotoxicity of LAK; ⑤Enhances in specific antitumor activity in mice in vivo ; ⑥Effects of polyactin on erythrocyte deformability and immunofunction in Rabbit and Rat.

Effects of ZMS on deposition of β-amyloid peptide and cholinergic function in rats with β-amyloid injection into right nucleus basalis magnocellularis

Abstract: AIM To observe the effects of ZMS active component of Zhimu on deposition of β amyloid peptide and cholinergic function in rats with β amyloid injection into right nucleus basalis magnocellularis (NBM). METHODS A combined injection of β AP 25-35 and excitatory amino acid into the right NBM was used as a dementid like rat model and model animals were divided into sham operation group, model group and ZMS group. The area of depositive spots of β AP 25-35 was detected by the ABC immunohistochemical and the image analysis methods. The learning and memory abilities were detected by step down test and step through test, the activity of brain choline acetyltransferase (ChAT) and the muscarinic receptor (MR) density were determined by 3H acetyl CoA binding analysis and 3H QNB binding tests respectively. RESULTS It was found that the deposition of β AP 25-35 in nucleus basalis increased, 30 d to 60 d after combined injection; while the cleposition decreased in model rats with once a day oral administration of ZMS for 60 d. ZMS significantly improved the learning and memory ability of the model animals. It also increased the brain activity of ChAT and the brain muscarinic receptor density of these animals. CONCLUSION These results suggeste that ZMS may help in scavenging action for the deposition of β AP 25-35 and in improving and treating the cholinergic disfunction in Alzheimers disease.

Effect of l-menthol pretreated nasal cavity on insulin pharmacological bioavailability

Abstract: AIM To study the effect l-menthol pretreated nasal cavity on insulin pharmacological bioavailability(PBA). METHODS To set up diabetic rats model,nasal cavities were pretreated with l-menthol for two hours,insulin was dripped, blood glucose concentrations of different time were determined,and the area over the curve (AOC) and pharmacological bioavailability(PBA) were calculated. RESULTS After rats nasal cavity was pretreated with different concentrations l-menthol, nasal cavity absorption of insulin markedly increased between 2 h and 3 h,and PBA of insulin nasal cavity absorption increased respectively 5.77,7.00 and 3.12 times than control group. CONCLUSION l-Menthol promotes the nasal cavity absorption of insulin.

Protective effect of abelmischl manihot l.medic against cerebral ischemia-reperfusion injury

Abstract: AIM To study the protective effect of TFA against cerebral ischemia reperfusion injury. METHORDS The cerebral ischemia model in mice was made by means of ligating bilalateral common carotid arteries.The mice survive rate during 6 h was observed,and malondialdehyde (MDA) in the ischemic cerebral cortex was measured. Using nitrogen anoxia model in mice,the survive time was observed. Ligating bilateral common carotid arteries and descending blood pressure,the cerebral ischemia reperfusion model in rabbits was established. The brain of rabbits was initiated by ischemia for 60 min followed by 30 min of reperfusion. The electroencephalogra phy (EEG) of cerebral ischemia and reperfusion was recorded. Malondialdehyde(MDA) and lactate dehydrogenase(LDH) in the ischemic cerebral cortex were measured. RESULTS TFA(30,60,120 mg·kg -1 ) prolonged the survive time after anoxia in mice,enchanced the survive rate after cerebral ischemia and inhibited the increasing of MDA contents in the cerebral cortex in mice.TFA(12,24,48 mg·kg -1 ) inhibitid the changes of EEG,MDA and LDH induced by cerebral ischemia reperfusion in rabbits. CONCLUSION TFA has protective effects on cerebral ischemia reperfusion injury,the mechanism may relate to attenuating free radical and lipid peroxidation.

Research on independent activity patterns of mice

Abstract: AIM To investigate the mices central nerve system function and the effect of drugs through independent activity pattern observation. METHODS By observing the influence of drugs on the independent activity patterns of mice of different testing time and testing times, sex, sound, and brightness. RESULTS The mices independent activity is related to testing times, sound and drugs applied, but not related to testing interval, sex, and brightness. CONCLUSION Individual difference of the independent activity of mice is great. The quietness of the experimental environment influences the result.