Studies on mechanisms of antimalarial action of artemisinin and its derivatives had been reviewed after artemisinin as an antimalarial drug was developed in 1972. The research work, which was mainly done by Chinese scholars, was introduced in the paper, and comprised 4 aspects:histopathology on the ultrastructure by electro-microscopy, the metabolism including the pigment clumping of the malarial parasite by biochemical pharmacology, and oxidation and Fe iron’s effect that were discussed in details based on studies from both domestic and international labs.

Cerebral microdialysis is a new sampling method that collects the perfusates from the specific brain region continuously. Disorders of extracellular excitatorary amino acids, monoamines and acetylcholine transmitters release cause brain injury during the cerebral ischemia and reperfusion. Microdialysis has been used to study the dynamic change of neurotransmitters during the acute cerebral ischemia and reperfusion lately, and the real change of neurotransmitters has been monitored in animals brain. The present paper reviews the progress on the microdialysis and its application in the study of neurotransmitters in cerebral ischemia animals in the world.

AIM　To investigate the poteintation of vincristine-induecd apoptosis by tetrandrine, neferine and dauricine isolated from Chinese medicinal plants in the human mammary MCF-7 multidrug resistant cells. METHODS　The apoptotic cells were detected by fluorescent staining of a combination of Hoechst 33342 and propidium iodide (PI), flow cytometry and agarose electrophoresis. RESULTS　The apoptotic cells induced by vincristine alone accounted for about 10% of all the cancer cells, while the percentage of apoptotic cells induced by a combination of vincristine with tetrandrine, neferine, or dauricine was found to be significantly higher than that by vincristine alone, and their reversal effects were positively correlated with the drug concentration and the exposure time. In addition, tetrandrine was shown to be the most potent in the reversal efficacy among the three compounds to be tested for apoptosis in vitro. CONCLUSION　Tetrandrine, neferine and dauricine showed obvious potenitiation of vincristine-induced apoptosis in the human mammary MCF-7 multidrug-resistant cells.

OBJECTIVETo observe the effects of compound red yeast rice extract (CRYRE) on blood lipids, hemorheology and blood coagulant system in rats with hyperlipidemia.

METHODSD rats were randomly divided into six groups: normal control group, model group, Xuezhikang group (0. 24 g x kg(-1)), CRYRE high dose group (2.4 g x kg(-1)), middle dose group (1.2 g x kg(-1)) and low dose group (0.6 g x kg(-1)). The normal control rats were given pure water, and rats of other five groups were given 10 mL kg lipid emulsion and subjected to daily intragastric administration simultaneously in two days, continuously for 3 weeks. After the last medication, all the rats were sacrificed for measurement of blood lipids, hemorheology and coagulation factors.

RESULTCRYRE 2.4 g x kg(-1) could significantly reduce the serum TG, TC levels and increase the HDL-C level (P < 0.01, P < 0.05). CRYRE 0.6-2.4 g x kg(-1) could significantly increase the ratios of HDL-C/TG,HDL-C/TC and HDL-C/LDL-C (P < 0.01). CRYRE 2.4 g x kg(-1) also reduced whole blood viscosity and plasma viscosity (P < 0.01, P < 0.05), prolonged active partial thromboplastin time, and lowered fibrinogen content (P < 0.01, P < 0.05).

CONCLUSIONCRYRE 2.4 g x kg(-1) could reduce blood lipids, blood viscosity and fibrinogen content, improve blood circulation, and depress the alteration of blood coagulant system resulted from lipid metabolic disorder in rats with hyperlipidemia.

Animals ; Biological Products ; administration & dosage ; chemistry ; Blood Circulation ; drug effects ; Disease Models, Animal ; Humans ; Hyperlipidemias ; blood ; drug therapy ; physiopathology ; Hypolipidemic Agents ; administration & dosage ; chemistry ; Lipids ; blood ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley

Objective To study computer toxicity prediction technology and predict the acute toxicity of Chinese materia medica; To provide a new way and method for safety evaluation of traditional Chinese medicine. Methods First, Mold2 software (version 2.0.0) was used to calculate molecular descriptors of 7409 chemical components. After preliminary screening of molecular descriptors, quantitative structure-activity relationship (QSAR) models were built up with Random Forest (RF) for screening the optimum prediction model. From the 83 kinds of toxic Chinese materia medica in Chinese Pharmacopoeia (2010 edition), acute toxicity of 60 kinds of Chinese materia medica reported from monomer structure (1692 chemical components) were under prediction.Results Totally 7409 pieces of data were obtained. When the descriptors were 52, RF modeling accuracy and Kappa were the highest, 0.712 and 0.436 respectively. Compound clusters were divided into 3 types according to optimum molecule descriptors (52). The accuracy and Kappa of the optimum model for the first type of compounds were 0.666 and 0.476 respectively; the accuracy and Kappa of the optimum model for the second type of compounds were 0.804 and 0.381 respectively; the accuracy and Kappa of the optimum model for the third type of compounds were 0.709 and 0.373 respectively. It was predicted that 60 kinds of Chinese materia medica containing 0 violent toxic compound, 2 high toxic compounds, 172 medium toxic compounds and 1518 low toxic compound.Conclusion QSAR model for prediction study on acute toxicity of chemical components of Chinese mareria medica can provide references combination medication and experimental studies.

The aim of this study is to explore the tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats. Healthy male SD rats were randomly divided into two groups (30 each). Both were given PEGylated puerarin at a dose of 488 mg x kg(-1). After 5 min of medication, one group was normal rats, another group with acute myocardial ischemia was established by peritoneal injection of 50 mg x kg(-1) isoprenaline. After administration, the animals were executed at 30, 60, 90, 120, 150 and 180 min, then heart, liver, spleen, lung, kidney were extracted. The content of puerarin in organ tissue was determined by HPLC. The results showed that the AUC of tissue distribution of PEGylated puerarin in normal rats was liver > kidney > heart ≈ spleen > lung > brain. While the AUC of tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats was liver ≈ heart > kidney > lung ≈ spleen > brain. AUC(heart) of PEGylated puerarin in acute myocardial ischemia model rats was 1.7 times than that of the normal rats, and there was significant difference (P < 0.05). Thus, PEGylated puerarin had a good heart-targeting property in early myocardial infarction area, drugs could accumulate in the ischemic myocardium. It provided important information for further study and clinic use of PEGylated puerarin.

In order to provide a new way and method for safety evaluation of Chinese materia medica (CMM) and also to provide a reference for conventional animal experiments, computer toxicity prediction technique and method were established to predict the cardiotoxicity of CMM. Mold2 software (version 2.0.0) was used to calculate molecular descriptors of 1034 chemical components. Then, the random forest (RF) method and the support vector machine (SVM) method were used to screen the descriptors. After that, boosting trees method, SVM, regularized discriminant analysis method and RF method were used to build up prediction model, respectively. Finally, the cardiotoxicity of chemical components was predicted by the quantitative structure-activity relationship (QSAR) model with the best accuracy and Kappa value. The results showed that by comparing the accuracy and Kappa value of prediction model, it was found that the RF model was the optimal algorithm model with 86.3%accuracy and the Kappa value of 0. 725. Through the prediction research on chemical components of Chinese herbs with toxicity recorded in the Pharmacopoeia of People’s Republic of China (version2010),suchasEvodia rutaecarpa,North bean root,Murraya incense,some meaningful results had been received. It was concluded that QSAR model on prediction research of chemical components of Chinese herbs provided important references for further experimental studies and clinical researches.

Objective To observe the antioxidative dosage-effect relationship of Marigold lutein, and provide experimental data for clinical use. Methods The mice were randomly divided into seven groups:blank control group, model control group, 1 mg/kg lutein group, 5 mg/kg lutein group, 25 mg/kg lutein group, 125 mg/kg lutein group and 625 mg/kg lutein group. The mice in blank control group were dealt with saline solution by intraperitoneal injection, the others were dealt with D-galactose (120 mg/kg) by intraperitoneal injection for seven weeks to make oxidative damage model, meanwhile the mice were given corresponding dose of the drug. Subsequently, the level of malondialdehyde (MDA) and activity of superoxide dismutase (SOD) in the serum were measured, and the antioxidative dosage-effect relationship was observed. Results The 1, 5, 25 mg/kg lutein reduced the MDA level and increased SOD activity, and the 125, 625 mg/kg dose of lutein did not show significant antioxidant activity. Conclusion Lutein has significant antioxidant activity in mouse dealt with D-galactose within the dose range of 1-25 mg/kg. The results suggest that the clinical dosage range of lutein should be kept within reasonable limits.

Objective The toxicological compatibility of Aconiti Carmichaeli Radix, as a toxic Chinese medicinal herb, combined with the other ingredients in Sini Decoction was investigated to elucidate the rationality of the combination of the ingredients in Sini Decoction from toxicological point of view. Methods Three kinds of experiments, acute toxicity in mice, heart toxicity in rats and aconitines level in water extract of Sini Decoction and its ingredients including Aconiti Carmichaeli Radix alone and its combination with licorice or dried ginger were adopted in this study. In the toxicological experiments, LD50 values for the acute toxicity test and TD50 values for the heart toxicity (arrhythemia as a parameter) of Sini Decoction, Aconiti Carmichaeli Radix alone and its combination with licorice or dried ginger were comparatively determined. And levels of individual aconitines of the water extracts from Sini Decoction, Aconiti Carmichaeli Radix alone and its combination with licorice or dried ginger were measured, respectively. Results The LD50 and TD50 of the combination of Aconiti Carmichaeli Radix and licorice in Sini Decoction were found to be higher than Aconiti Carmichaeli Radix alone or Sini Decoction, while the LD50 and TD50 of the combination of Aconiti Carmichaeli Radix and dried ginger appeared to be not different from those of Aconiti Carmichaeli Radix alone. The level of the main toxic compound of the water extracts for the combination of Aconiti Carmichaeli Radix and licorice, and Sini Decoction was lower than that of Aconiti Carmichaeli Radix alone and its combination with dried ginger. Conclusion The combination of Aconiti Carmichaeli Radix and licorice can attenuate the toxicity of Aconiti Carmichaeli Radix.

This article discusses the characteristics of cmmunity herbal monographs for traditional herbal medicinal products and its establishment procedure. It also reviews the new development of cmmunity traditional herbal monographs. The purpose is to clarify the relationship between cmmunity herbal monographs and simplified registration for traditional herbal medicinal product in European Union and provide reference to the registration of taditional Chinese mdicinal products in Europe.
Drug Approval ; legislation & jurisprudence ; European Union ; Humans ; Phytotherapy ; Plants, Medicinal