Application of tissue spontaneous fluorescence in myocardial ischemia injury of rats / 中国药理学通报

Aim Todiscusstheapplicationoftissue spontaneous fluorescence in myocardial ischemia injury of rats based on specific fluorescence detection technol-ogy.Methods Thechangeofspontaneousfluores-cence was compared between the myocardial tissue of normal rats and those of rats with myocardial ischemia injury and an quantitative analysis was then made.Re-sult Theresultsshowedthatspontaneousfluorescence of myocardial tissue for myocardial ischemia injury changed significantly.Spontaneous fluorescence signal of injury considerably was enhanced.The fluorescence signal which was quantified by FX Pro had statistical significance compared with normal myocardial tissue,P<0.01orP<0.05.Conclusion Ourresearchshows that spontaneous fluorescence of myocardial tissue can be enhanced obviously after myocardial ischemia inju-ry.Our research provides a method for the research and evaluation of myocardial ischemia injury model in rats which can be used in positioning,qualitative and quan-titative comparative study and in pathological,physio-logical,pharmacological and mechanism study.

Research advances in garlic's main active ingredients and their pharmacological effects / 中国药理学通报

Garlic is a bulb from generalized liliaceous plant Alli-um sativum, it plays an essential role in the prevention and treat-ment of cardiovascular diseases, tumors and pathogenic microor-ganisms. Through consulting domestic and foreign references, the main active ingredients of garlic and their pharmacological effects are reviewed, the problems and achievement in Chinese research are also discussed. It can provide a certain reference for the further study of garlic and new drug development.

Experimental study on anaphylactoid reactions induced by different components of shengmai injection (new production process) on Beagle dogs / 中国中药杂志

<p><b>OBJECTIVE</b>To evaluate the sensitization effect of different components of Shengmai injection (new production process) on Beagle dogs.</p><p><b>METHOD</b>Beagle dogs were randomly divided into 7 groups, 3 in each group. Each group was respectively injected with 5% glucose injection, Ginseng Radix et Rhizoma Rubra extract, Ophiopogonis Radix extract, Schisandrae Chinensis Fructus extract, Schisandrae Chinersis Fructus distillate, Shengmaifang, 0.2% tween 80. The changes of each dog were observed from injection before until 24 hours after injection, and the response level was determined according to the severity of the symptoms. Blood samples were collected before injection and at 10 min after injection for measuring histamine content in plasma by ELISA. Sensitization of the injection was comprehensively determined by combined the response level of symptoms and the histamine level.</p><p><b>RESULT</b>One dog of Ginseng Radix et Rhizoma Rubra extract group showed untypical symptoms of anaphylactoid reactions, and serum histamine of two dogs increased more than doubled. The Beagle dogs administrated with 0.2% tween 80 showed typical symptoms of anaphylactoid reactions, while there was no significant increase of serum histamine. Other groups were observed with no typical anaphylactoid reactions.</p><p><b>CONCLUSION</b>The sensitization effect of Shengmai injection (new production process) may be associated with Ginseng Radix et Rhizoma Rubra extract and 0.2% tween 80.</p>

Experimental study on anaphylactoid reactions induced by shengmai injection (new production process) on Cynomolgus monkey / 中国中药杂志

<p><b>OBJECTIVE</b>To compare the anaphylactoid effect of old Shengmai injection and new Shengmai injection on Cynomolgus monkey.</p><p><b>METHOD</b>Cynomolgus monkeys were randomly divided into 4 groups, and were respectively injected with 5% glucose injection, old Shengmai injection, new Shengmai injection, positive control drug. The changes of each monkey were observed from injection before until 24 hours after injection, and the response level was determined according to the severity of the symptoms. Blood samples were collected before injection and at 10 min after injection for measuring histamine content in plasma. Blood pressure and heart rates were detected before injection and at 10 min after injection. Sensitization of the injection was comprehensively determined by combined the response level of symptoms and the histamine level.</p><p><b>RESULT</b>The Cynomolgus monkeys administrated with old Shengmai injection showed typical symptoms of anaphylactoid reactions and the content of serum histamine is not more than doubled. The Cynomolgus monkeys administrated with new Shengmai injection showed untypical symptoms of anaphylactoid reactions and the content of serum histamine did not rise.</p><p><b>CONCLUSION</b>The old Shengmai injection can induce typical anaphylactoid reactions on Cynomolgus monkeys, and the sensitization ability is strong. The symptoms of anaphylactoid reactions induced by the new Shengmai injection appeared later and showed lesser degree with the sensitization lower.</p>

Experimental study on anaphylactoid reactions of guinea pig induced by danshen injection and its components / 中国中药杂志

<p><b>OBJECTIVE</b>To compare the anaphylactoid effect of Danshen injection and its components on guinea pig.</p><p><b>METHOD</b>Applying active systemic anaphylaxis (ASA) tests, the corresponding experimental injections were administrated to guinea pigs to sensitized, and allergen with double doses was injected to stimulate in the 11 days after the last sensitized. The anaphylaxis situation of guinea pigs was observed.</p><p><b>RESULT</b>Danshen injection and its components are suspicion on guinea pigs, while negative reaction was observed on guinea pigs which injected by the liquid excipients of Danshen injection.</p><p><b>CONCLUSION</b>Danshen injection using the ultrafiltration method still have some antigenic impurities which cannot be removed completely, and this may be one of the reasons for anaphylactic reaction.</p>

Experimental model of histamine-induced anaphylactoid reaction on beagle dogs / 中国中药杂志

<p><b>OBJECTIVE</b>To establish animal model of histamine-induced anaphylactoid reactions on Beagle dogs through intravenous injection of histamine phosphate injection.</p><p><b>METHOD</b>Anaphylactoid reactions was determined according to the changes of praxiology and blood pressure of Beagle dogs after one intravenous injection of histamine phosphate injection.</p><p><b>RESULT</b>It showed that typical anaphylactoid reactions be caused by histamine phosphate injection on Beagle dogs, and the response of the high-dose group was more obvious than that of the low-dose group.</p><p><b>CONCLUSION</b>Intravenous injection of histamine phosphate injection could simulate Beagle dogs to bring typical clinical anaphylactoid reaction, that could be used as a sensitive animal model to evaluate anaphylactoid reaction of traditional Chinese medicine injections (TCMIs) in the pre-clinical experiments of both TCMIs and their composition.</p>

Anaphylactoid reactions induced by polysorbate 80 on Beagle dogs / 中国中药杂志

<p><b>OBJECTIVE</b>To evaluate the sensitization effect of polysorbate 80 from different factories on Beagle dogs.</p><p><b>METHOD</b>Beagles dogs were randomly divided into 5 groups, 3 in each group, received respectively the intravenous infusion of polysorbate 80 made by four factories in the concentration of 0.5%, with the constant infusing speed of 5 mL x min(-1) and volume of 10 mL x kg(-1). Changes were observed before infusion and in the 24 h after infusion, time of symptom appearance and disappearance was recorded, and the grade of response was determined. Moreover, blood pressure and heart rates were tested by the machine of Bp-98E, blood samples of animals were collected before infusion and at 10 min after ending infusion for measuring histamine content in plasma using ELISA. Then the sensitization effect was comprehensively estimated by combined consideration of the responding grade and histamine level.</p><p><b>RESULT</b>Typical symptoms of anaphylactoid reactions were found in sample 3 group, atypical symptoms were found in other polysorbate 80 groups. Different degrees of heart rate speeding and blood pressure downing were found in polysorbate 80 groups. No over 1-fold increase of plasma histamine level was found in all groups. The atypical anaphylactoid reactions and blood pressure of sample 2 group was lighter than other polysorbate 80 groups. Estimation showed that the sample 3 induced the suspicious anaphylactoid reactions, other test solutions did not induce the typical anaphylactoid reactions on Beagle dogs.</p><p><b>CONCLUSION</b>For allergies and other special populations, there is still a certain risk to applicate polysorbate 80 in the concentration of 0.5%. Production process of polysorbate 80 have a certain influence on allergenicity, refined polysorbate 80 increase the security, but further reasearchs are needed to confirmed.</p>

Study on anaphylaxis and hemocytolysis of 6 kinds of tween-80 injection from different souce / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the anaphylaxis and hemocytolysis of 6 kinds of tween-80 injection from different source.</p><p><b>METHOD</b>The Hartley albinism guinea pig was used to carry on the active systematic anaphylaxis (ASA) and the passive cutaneous anaphylaxis (PCA). The in vitro hemolytic experiment and the hemocytolysis was observed by means of spectrophotometry on the domestic rabbit.</p><p><b>RESULT</b>The result of ASA and PLA of 6 kinds of tween-80 injection from different source assumed the negative. In observation time, the temolysis rate of 3 kinds of tween-80 injection are more than 5%, while the others are also more than 5% only in the highly concentrated test tube.</p><p><b>CONCLUSION</b>Six kinds of tween-80 injection from different source have not caused the immune-mediated anaphylaxis, but it may have hematolysis tendency on intravenous injection. The hemocytolysis of tween-80 may not be entirely caused by the impurities. It is worthy of further study that the physical and chemical properties of the product itself and the undeserved concentration is doubtful whether there is also some internal relations with the generation of hemolytic.</p>

Improvement and enhancement of traditional Chinese medicine injections / 中国中药杂志

Compared to oral administrations, traditional Chinese medicine (TCM) injections act more rapidly and stronger, which is good for the treatment of acute or complicated diseases and makes up for the deficiencies of the oral ways. As an innovative dosage form which combines the modern pharmaceutical technology with the TCM, it represents the spirit of improvement and enhancement. With the expansion of clinical applications and adverse reactions or even death caused by individual dosages, TCM injections are receiving concerns from all fields of society and facing tremendous challenges and pressures. Some even suggested the cancellation. This study discussed the background, current situation and the reasons for the occurrence of adverse reactions. Taking Houttuynia injection as an example, it introduced the principle of improvement and described in detail the ideas and methods for it, which provided some reference for the improvement and enhancement of the TCM injections and reduced the safety risks of TCM injections to minimum.

Effects of methyl protodioscin on Ca2+i and ATPase activity in cardiomyocytes and analysis of mechanisms / 中国中药杂志

<p><b>OBJECTIVE</b>To study the effects of methyl protodioscin on the [Ca2+]i and the ATPase activity in cardiomyocytes, as well as their mechanisms.</p><p><b>METHOD</b>The cardiomyocytes were randomly divided into three groups, the control group treated with no serumal DMEM, the MPD group treated with MPD and the dilthiazem group treated with dilthiazem. Fluorospectrophotometer was used to determined the level of myocardial cell intracellular Ca2+ [Ca2+]i. In the experiment of ATPase activity on cellular membrane, the cardiomyocytes were randomly divided into two groups, the control group treated with no serumal DMEM, the MPD group treated with MPD. The activity of Na+-K+-ATPase,Ca2+-Mg2+-ATPase and Mg2+-ATP ATPase were determined. The quantitative analysis of SERCA2a mRNA expression was studied by RT-PCR that the groups and treatments in cardiomyocytes same as the experiment for ATPase activity assay.</p><p><b>RESULT</b>Under the quiescent condition, compared to the control group, the level of [Ca2+]i in cardiomyocytes of the MPD group and dilthiazem group was no different. After treatment with 40 mmol x L(-1) KCl, [Ca2+] was significantly lower in the MPD group and the dilthiazem group, and the intensity of peak value in time course of 60 s, the dilthiazem group and the MPD group also were lower than the control group (P < 0.001). Ca2+-Mg2+-ATPase and Na+-K+-ATPase in cultured rat were increased after treated with MPD compared to treatment with no serumal DMEM (P < 0.05, P < 0.01), but Mg2+-ATPase in these groups had no different. The expression of SERCA2a mRNA between the MPD group and the control group was no different. MPD could not up-regulated or down-regulated SERCA2a in endocytoplasmic reticulum.</p><p><b>CONCLUSION</b>Methyl protodioscin could block the volt dependent form calcium channel in cellular membrane, and up-regulate the function of sodium pump and calcium pump, so that it could remain low calcium in the internal environment in cardiomyocytes.</p>

A shallow review of minimally invasive pharmacology and evidence-based pharmacology / 中国药理学通报

Development of minimally invasive medicine and needs of pharmacology and relevant fields lead to the establishment and expansion of minimally invasive pharmacology and evidence-based pharmacology. Some principal views on the minimally invasive pharmacology and evidence-based pharmacology are discussed in this review.

Influence of Shenqi Recipe on mesangial cells and interstitial fibroblasts of chronic renal failure rats / 中西医结合学报

OBJECTIVE: To observe the effect of Shenqi Recipe on the proliferation of glomerular mesangial cells (MC) and interstitial fibroblasts (FC) in rats. METHODS: The effect of serum containing prepared drugs from normal and chronic renal failure rats treated by Shenqi Recipe on glomerular mesangial cells and intersititial fibroblasts in vitro was observed by MTT colorimetric assay and serophrmacology. RESULTS: Compared with the blank sample normal rats, serum containing Shenqi Recipe inhibited the proliferation of MC and FC (P<0.001), and the serum containing Shenqi Recipe of CRF rats had significantly inhibited the proliferation of MC and FC compared with the model group(P<0.001). Conclusion Shenqi Recipe can postpone CRF progress by this mechanism.

Effect of MPD on Acute Myocardial Ischemia in Dogs / 中药新药与临床药理

Objective To study the protecitve effect of methy Protodioscin(MPD)on myocardial infarction in dogs. Methods Dog models of myocardial infarction were induced by ligation of coronary artery. The degree of myocardial ischemia was calculated by measuring the epicardial electrogram, and the myocardial infarction area was detected with N-BT histochemistry staining method. The changes of ET, 6-Keto-PGF1a, TXB2 in blood plasma were observed with radioimmunoassay. Meanwhile, the coronary blood flow was measured. Results MPD can obviously relieve the pathological changes of the acute myocardial infarction, decrease the infarction size, reduce the myocardium ischemic degree, dilate the coronary artery , and increase the myocardial blood supply. Meanwhile, MPD can improve the vascular endothelial cell function. Conclusion MPD had obvious effect for relieving acute myocardial infarction in dogs.

Effects of MPD on Heart Hemodynamics in Normal Anesthetic Dogs / 中药新药与临床药理

Objective To investigate the pharmacological effects of MPD on heart hemodynamics and myocardial oxygen consumption in dogs, and to study its mechanism. Methods The changes of parameters such as blood pressure (BP), coronary blood flow, myocardial oxygen consumption and heart rates were observed in normal anesthetic dogs. Results Compared to those in the normal group, MPD can obviously lower the BP and peripheral vascular resistance, dilate the coronary and peripheral artery, increase the coronary blood flow and improve the left ventricle function and myocardium oxygen consumption rate. Conclusion MPD can improve the heart hemodynamics and regulate myocardium oxygen consumption.

Effects of Shuanglong Prescription on Heart Hemodynamics and Myocardial Oxygen Consumption in Dogs / 中药新药与临床药理

Objective To investigate the pharmacological action of Shuanglong Prescription on cardiac function in dogs and to study its mechanism. Methods The changes of the parameters such as coronary blood flow, myocardial oxygen consumption and heart rates were observed in normal anesthetic dogs. Results Compared to those in the normal group, the coronary blood flow increased and the heart rates decreased in Shuanglong Prescription group. Conclusion Shuanglong Prescription can regulate and improve the cardiac function of dogs.

Comparative pharmacokinetics of active component in Guanxin Suhe Pills containing Radix Inulae in place of Radix Aristolochiae / 中草药

Objective To study the pharmacokinetics of the active component in series of Guanxin Suhe Pills including the prescription containing Radix Aristolochiae(QG),the prescription containing Radix Inulae(TG),and the prescription without any of them(BG) in Beagle dogs and to compare the pharmacokinetics among the series of prescription.Methods HPLC Method was developed to determine acid in plasma of Beagle dogs.Blood plasma was collected after series of Guanxin Suhe Pills were ig administrated to Beagle dogs 0—8 h later.The concentration of cinnamic acid in the plasma was determined and DAS 2.1 software was used in calculation of compartment model and pharmacokinetic parameters.Results The standard curve was linear from 0.031 25 to 32 mg/L in plasma of Beagle dogs,the lowest detectable limit was 31.25 ?g/L,the recovery rate of the method was over 90 % with satisfactory relative standard deviations(RSDs) of intra-day and inter-day both lower than 5 %.The metabolism of cinnamic acid in plasma of Beagle dogs after medication of series in QG,TG,and BG all fitted in a first order absorption of two-compartment model.The peak concentration and the area under curve in TG and BG groups had the higher tendency than those in the QG group,but there was no significant difference among the three groups.Conclusion The series of Guanxin Suhe Pills all have a similar pharmacokinetic process.Taking away the Radix Aristolochiae from the previous prescription that including the Radix Aristolochiae or taking the place of the Radix Aristolochiae with Radix Inulae does not influence the pharmacokinetic process of the main active component.

Determination of glaucocalyxin A by HPLC and its protein binding rate in plasma of rat / 中草药

Objective To study the protein binding rate of glaucocalyxin A in plasma of rat. Methods The plasma balance dialysis was used. An HPLC for the quantitative determination of glaucocalyxin A was presented and used to calculate the protein binding rate in plasma of rat. Results There were protein binding rate results of 74.46%, 77.87%, and 75.29% at three various concentrations 20, 10, and 1 ?g/ mL of glaucocalyxin A in plasma of rat. Conclusion The HPLC method used to determine glaucocalyxin A is simple, rapid, and sensitive with good specificity, precision and accuracy, and glaucocalyxin A has medium capacities in protein binding rate in plasma of rat.

Studies on Hemostatic Activity and Pharmacology of Shenxueling / 中草药

Pharmacology of Shpnxueling(SXL),a traditional Chinese medicine used for the treatment of idiopathicthrombocytopenic purpura,and its hemostatic activity were studied in experimental animals. Results showedthat SXL shortened the time of bleeding and coagulation,raised BPC in mice,increased platelet megakaryocyteproduction in rabbit,prolong the time of swiming of 1oaded mice,increased body liver and kidney weights ofyoung mice, increased p1asma cortisol Ievel. Acute and chronic toxicity tests reveaIed that SXL was nontoxicto mice or rats. These results suggested that hemostasis was associated with effects of SXl, which could faci1i-tate division and maturity of megakaryocyte,increase the BPC,accelerate coagulation and regulate the functionof endocrine. SXL could resist fatigue,endure hypoxia,faciIitate growth. lt is safe and nontoxic in its use of'SXL.

Effects of Different Compositions of Guanxin Ⅱ(GXⅡ)Prescription on Experimental Myocardial Infarct in Rats / 中药新药与临床药理

Objective To compare effects of the whole prescription of Guanxin Ⅱ(GXⅡ),the hemorheologic agents and the Qi-regulating agents of the whole prescription on acute myocardial infarction in rats.Methods Acute myocardial infarct(AMI)model was established by coronary artery ligation,and then the model rats were treated with intraduodenal administration of different compositions of GXⅡ 5～10 minutes after the artery ligation.Five hours after modeling,blood was collected to determine the levels of endothelin(ET),thromboxane(TXB2),isoenzymes of creatine kinase(CK-MB)and andlactate dehydrogenase(LDH).The heart of rats was cut into five slices and dyed by nitrotetrazolium blue chloride(N-BT)for 5 minutes,and then the infarcted area(non-N-BT staining area)and the noninfarcted area(N-BT staining area)were detected.Results Compared to the model group,both the whole prescription of GXⅡ and the hemorheologic agents significantly reduced infarct size,ameliorated blood ET,TXB2,CK-MB and LDH levels(P

Therapeutic Effects of Methyl Protodioscin for Myocardial Infarction in Rats / 中药新药与临床药理

Objective To study the therapeutic effects of methyl protodioscin (MPD ) on myocardial infarction in rats. Methods Rat models of myocardial infarction were induced by ligation of coranary artery. Then myocardium infarction area and the vasoactive substance were measured to evaluate the therapeutic effect of MPD on acute myocardial infarction in rats. Results Compared with the control group,MPD lessened the myocardial infarction size dramatically,inhibited the increase of CK and LDH ,lowered the increased MDA content level and improved the activity of SOD and NO. Conclusion MPD reduces the level of myocardium enzyme and the myocardial infarction size,and increases the capability of clearing oxygen free radical and function of the vascular endothelial cell. MPD by intravenous injection has a better effect than that by oral use.