Nanocrystals self-stabilized Pickering emulsion loaded with active components of Tongmai prescription: preparation, characterization and evaluation by Caco-2 cell model / 药学学报

It is of great significance to apply the nanocrystals self-stabilized Pickering emulsion (NSSPE) to traditional Chinese medicine (TCM) compounds, and to study the effect of NSSPE on the oral absorption of various components with different solubility and permeability. In the study, NSSPE of Tongmai prescription was prepared by the high pressure homogenization method with nanocrystals of main active components (puerarin, ferulic acid, salvianolic acid B and tanshinone IIA) of Tongmai prescription as solid particle stabilizers and a mixture of Ligusticum chuanxiong essential oil and Labrafil M 1944 CS as oil phase. The NSSPE had better physical stability than nanocrystals suspension and blank emulsion. The adsorption of nanocrystals on the surface of oil droplets was confirmed by scanning electron microscopy and fluorescence microscopy. The surface adsorption rates of puerarin, ferulic acid, salvianolic acid B and tanshinone ⅡA in NSSPE were 15.40% ± 3.19%, 15.39% ± 5.07%, 10.97% ± 3.70% and 31.51% ± 1.60%, respectively. When solid active components were prepared into nanocrystals suspension, the cellular uptake and transport across Caco-2 cells were increased significantly for puerarin and tanshinone IIA. The uptake rates of ferulic acid, ligustilide and tanshinone IIA in NSSPE were further increased compared with the physical mixture of nanocrystals suspension and oil, and the transports of ligustilide and tanshinone IIA were also significantly improved. The main absorption mechanisms of NSSPE were passive diffusion and caveolin-mediated endocytosis, which were determined mainly by the microstructure of NSSPE. In conclusion, NSSPE could be applied to complicated TCM. The "micro" and "nano" synergistic microstructure with drug nanocrystals adsorbed on the surface of micron-sized oil droplets could not only improve the physical stability of NSSPE, but also promote the absorption of various components in NSSPE, which made NSSPE a promising oral drug delivery system for TCM.

Study on oral absorption mechanisms of puerarin in nanocrystals self-stabilized pickering emulsion / 中国中药杂志

Nanocrystals self-stabilized Pickering emulsion(NSSPE) is a new kind of emulsion where only nanocrystals of poorly soluble drugs are used as stabilizers. Our previous study showed that NSSPE with Ligusticum chuanxiong oil as the main oil phase can significantly promote oral absorption of puerarin. The present study aimed to explore its absorption mechanism in oral administration. The in vitro dissolution test was carried out to study the effect of NSSPE on release of puerarin. The effects and mechanism of NSSPE on uptake and transport of puerarin across Caco-2 cell were investigated. The results showed that the drug release rate of NSSPE was similar to that of nanocrystals, with their cumulative dissolution of puerarin not affected by pH of releasing mediums, both significantly higher than that of crude material. The uptake of puerarin in NSSPE was concentration-dependent and significantly higher than that of solution or surfactant stabilized emulsion. Genistein and indomethacin, inhibitors of lipid rafts/caveolin, could significantly reduce the uptake of puerarin in NSSPE. Compared with solution, NSSPE and surfactants stabilized emulsion obviously increased transport rate K_a and apparent permeability coefficient P_(app) of puerarin in AP → BL direction, but there was no significant difference in BL → AP direction. It could be inferred that there were both passive and active transport mechanisms, as well as lipid raft/caveolin mediated endocytosis for absorption of NSSPE. The promoted oral absorption of puerarin in NSSPE was mainly related to the existing nanocrystal form which could promote dissolution, puerarin as well as Ligusticum chuanxiong oil which could promote drug transmembrane transport and inhibit drug efflux. It is the unique structure and composition of the compound NSSPE that promoted the oral absorption of puerarin.

Analysis of blood components of Yougui Yin in normal rats and rats with kidney deficiency caused by adenine based on UPLC-MS technology / 中国中药杂志

Based on the serum medicinal method, this study aims to investigate the migrating components of Yougui Yin in the blood after intragastric administration, and to provide reference for the basic research of its pharmacodynamics. The kidney deficiency rat model was replicated by adenine method. Normal rats and model rats were administered orally for a single gavage of Yougui Yin. The components in blood were rapidly analyzed and identified by ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS) and multiple reaction monitoring(MRM), and the migrating components in blood of Yougui Yin were explored by multivariate statistical analysis. The results showed that there were 42 characteristic peaks in the plasma of normal rats by UPLC-Q-TOF-MS technology and 13 chemical components were identified, including 6 alkaloids, 2 flavonoids, 2 triterpenoid saponins, 1 iridoid, 1 phenylpropanoid and 1 monoterpenoid. There were 22 characteristic peaks in the plasma of kidney-deficiency rats, and 12 chemical components were identified, including 2 iridoids, 6 alkaloids, 2 flavonoids, 1 monoterpenoid and 1 triterpenoid saponin. Verbascoside, isoacteoside, acteoside, pinoresinoldiglucoside, loganin and morroniside were identified by MRM both in the plasma of normal rats and kidney-deficiency rats. Compared with 85 monomer components in Yougui Yin, 17 common prototype components were found by UPLC-MS in the plasma of normal rats and kidney deficiency rats, including verbascoside, isoacteoside, acteoside, rehmapicrogenin derived from Rehmanniae Radix Praeparata, pinoresinol diglucoside and geniposidic acid from Eucommiea Cortex, loganin and morroniside derived from Corni Fructus, mesaconine, benzoylmesaconine, benzoylaconitine, benzoylhypacoitine, mesaconitine, aconitine derived from Aconiti Lateralis Radix Praeparata, liquiritin, isoliquiritin and glycyrrhizic acid derived from Glycyrrhizae Radix et Rhizoma. Thirty-one metabolites of medicinal ingredients not found in the plasma of adenine-induced kidney deficiency rats were also detected in the plasma of normal rats. Twelve metabolites of medicinal materials not found in the plasma of normal rats were detected in the plasma of kidney deficiency rats. The results of the study provide reference for explaining the material basis and mechanism of Yougui Yin in the treatment of kidney deficiency.

The cardiovascular protective effect and mechanism of calycosin and its derivatives / 中国天然药物

Cardiovascular disease is the main cause of mortality and morbidity in the world, especially in developing countries. Drug therapy is one of the main ways to treat cardiovascular diseases. Among them, great progress has been made in the treatment of cardiovascular diseases with traditional Chinese medicine. In terms of experimental research, the mechanism of traditional Chinese medicine in the treatment of cardiovascular diseases has been thoroughly discussed in vitro and in vivo. In terms of clinical treatment, traditional Chinese medicine with flavonoids, saponins and alkaloids as the main effective components has a definite effect on the treatment of cardiovascular diseases such as arrhythmia, myocardial ischemia, angina pectoris and myocardial infarction, with high safety and good application prospects. With the further research on the effective ingredients, mechanism and adverse reactions of traditional Chinese medicine, it will be beneficial to the effectiveness of traditional Chinese medicine, reduce side effects and promote the modernization of traditional Chinese medicine. Calycosin and its derivatives, the main bioactive flavonoids in Astragalus membranaceus have multiple biological effects, such as antioxidant, pro-angiogenesis, anti-tumour, and anti-inflammatory effects. Based on the above biological effects, calycosin has been shown to have good potential for cardiovascular protection. The potent antioxidant effect of calycosin may play an important role in the cardiovascular protective potential. For injured cardiac myocytes, calycosin and its derivatives can alleviate the cell damage mainly marked by the release of myocardial enzymes and reduce the death level of cardiac myocytes mainly characterized by apoptosis through various mechanisms. For vascular endothelial cells, calycosin also has multiple effects and multiple mechanisms, such as promoting vascular endothelial cell proliferation, exerting vasodilating effect and directly affecting the synthesis function of endothelial cells. The present review will address the bioactivity of calycosin in cardiovascular diseases such as protective effects on cardiac myocytes and vascular endothelial cells and elucidate main mechanism of calycosin and its derivatives to exert the above biological effects.

Prediction and verification of biological basis and mechanism for traditional Chinese drugs of reinforcing kidney for supplementing essence in treating diseases related to deficiency of kidney essence / 药学学报

"Kidney essence" is a profound concept in the theory of traditional Chinese medicine. But its biological basis is unknown until now, resulting in the therapeutic effects of traditional Chinese drugs on reinforcing kidney for supplementing essence hard to be evaluated. This study aimed, to explore the potential biological basis and mechanism of traditional Chinese drugs of reinforcing kidney for supplementing essence on diseases related to deficiency of kidney essence through network pharmacology analysis on the intersection of targets of drugs and diseases. The targets for ingredients in Rehmanniae radix praeparata (RRP), Polygoni multiflori radix praeparata (PMRP) and Polygonati rhizome (PR) were gathered from TCMSP and TCMID database. Osteoporosis, Alzheimer's disease, anemia, infertility and oligospermia targets were collected from OMIM and DisGeNET database. Drug-compound-target-disease (DCTD) network was established with Cytoscape 3.6.1 software, then Clue GO and DAVID database was used to acquire the annotation about GO terms and signaling pathways. Natural aging mice, an acknowledged syndrome model of deficiency of kidney essence, and RRP were used to verify the predictive targets by Western blot analysis. All animal experiments were conducted in accordance with the international guidelines and regulations for the care and use of animals. DCTD network showed that the intersection of drugs and diseases included 175 common targets. After topology analysis, 71 key were screened out targets which were associated with GO annotation exhibited that biological processes (including transcription regulation, RNA metabolism regulation, and DNA-dependent transcription regulation), cell composition (including nuclear lumen, organelle lumen, and membrane closure lumen), molecular function (including transcription regulation, transcription factor activity, and enzyme binding), and signaling pathway (including peroxisome proliferator-activated receptor alpha (PPARα), mitogen-activated protein kinase (MAPK), hypoxia-inducible factor 1 (HIF-1), erythropoietin (EPO) and other signaling pathways. In natural aging mice, the expressions of HIF-1α, growth factor receptor-bound protein 2 (GRB2), MAPK3, signal transducer and activator of transcription 5A (STAT5A), transcription factor AP-1 (JUN) and proto-oncogene c-Fos (FOS) in EPO pathway were significantly decreased. RRP significantly reversed the decrease of the above targets. Above all, these results indicated that the therapeutic effects of traditional Chinese drugs of reinforcing kidney for supplementing essence on deficiency of kidney essence may be related to the regulation of nuclear transcriptional activity and EPO signaling pathway.

Analysis of Banxia Xiexintang Based on Ancient Literatures / 中国实验方剂学杂志

Banxia Xiexin Tang is one of the classic prescriptions for treating digestive system diseases.In this paper，using the method of bibliometrics，information of Banxia Xiexintang in ancient Chinese medical literatures were collected and screened out 399 effective data from 238 kinds of ancient books．Based on the statistics and analysis of the history，drug composition，main disease and syndrome，principle of prescription，dosage，processing，preparation，decocting and taking methods of Banxia Xiexin Tang，it is found that Banxia Xiexin Tang originated from Treatise on Febrile and Miscellaneous Disease written by ZHANG Zhong-jing，a famous physician in the Eastern Han dynasty，it is composed of seven herbs，namely，Pinelliae Rhizoma，Scutellariae Radix，Zingiberis Rhizoma，Ginseng Radix et Rhizoma，Glycyrrhizae Radix et Rhizoma Praeparata cum Melle，Coptidis Rhizoma，and Jujubae Fructus. It was mainly used to treat pizheng of mixed cold and heat. Most of the Banxia Xiexin Tang recorded in later generations follow the prescription composition and indications in Treatise on Febrile and Miscellaneous Disease and its clinical application has been extended and expanded，among the 352 literatures with the main diseases and syndromes recorded，the most common （341） were pizheng，accounting for about 96.88%，in addition，it is also used sporadically for shuzheng，malaria，nausea，damp-wen，jaundice，etc. Among the 122 documents with drug dosage records，nearly half of them are identical with the original records in Treatise on Febrile and Miscellaneous Disease. Among the 112 literatures with pharmaceutical processing，licorice （86） was the most，most of them were roasted （80），followed by pinellia ternata （79），and most of them were "decoction washing and sliding" （67）. Among the 111 documents recorded in the decoction method，most of them inherited Treatise on Febrile and Miscellaneous Disease by "removing the dross and again cooking" （68），there are also "Water Decoction" （32） and "Ginseng Radix et Rhizoma and Jujubae Fructus Decoction" （11）. Among the 108 documents with the method of taking medicine，nearly half of them inherited Treatise on Febrile and Miscellaneous Disease，which is "a liter of warm taking ，three times daily". Based on the ancient Chinese medical literatures，Banxia Xiexintang was systematically analyzed in order to provide more accurate ancient literature reference for the clinical application and development of classic prescriptions.

Ancient Literatures of Classical Famous Prescription Dihuang Yinzi / 中国实验方剂学杂志

Classical famous prescription Dihuang Yinzi is widely used in modern clinical practice，and can treat many kinds of diseases，especially the diseases of nervous system in internal medicine. Its clinical effect is accurate，but it has not been converted into Chinese patent medicine preparations. Therefore，the authors have collected ancient traditional Chinese medicine（TCM） literatures of Dihuang Yinzi by the methods of bibliometrics，and selected and sorted out 254 pieces of effective data， involving 144 ancient books of TCM，and systematically summarized and analyzed the historical development origin，main treatment syndrome，formula making principle，dosage，preparation method，decoction method and medicine taking method of Dihuang Yinzi，in order to provide the ancient literary evidence support for the development and clinical application of classic famous prescriptions. It is found that Dihuang Yinzi was from Xuanming Lunfang written by LIU He-jian，a doctor of Jin dynasty. It was composed of 12 kinds of herbs，namely Rehmanniae Radix Praeparata，Morindae Officinalis Radix，Corni Fructus，Cistanches Herba，Dendrobii Caulis，Aconm Lateralis Radix Praeparaia，Schisandrae Chinensis Fructus，Cinnamomi Ramulus，Poria，maimendong，Acori Calami Rhizoma and Polygalae Radix, and mainly used for the treatment of Yinfei. The later records of Dihuang Yinzi mostly followed the prescription composition and main treatment set forth in Xuanming Lunfang，and its clinical application was expanded. In the 199 articles with the indications for disease treatment，Yinfei was the most commonest indication, and took up about half of the total，which was followed by stroke，taking up about two fifths of the total. It was also used for the treatment of sudden aphonia，flaccidity syndrome，vertigo，enuresis. Dihuang Yinzi has a wide range of treatment，but the pathogenes is always belongs to "the deficiency of water and fire in the kidney". The recipe of Dihuang Yinzi was unique，and can be used to treat both the upper and lower parts of the body，as well as both the outward symptoms and root causes of an illness at the same time， in particular，it mainly focuses on the treatment of the lower and the root. Among the 56 literatures with drug dosage records，about one third of them inherited the records of Xuanming Lunfang: "Equal division，the top is the end，3 qian for each dose." The dosage was generally light. The preparations are mostly decoction and boiled powder. In the decocting and taking methods，it was suggested that "turbid medicine shall be boiled for a short time，and taken after several boilings，with no limit to time."

Clinical observation of rapid massage at Shuidao (ST 28) to prevent postpartum urinary retention / 中国针灸

OBJECTIVE@#To explore the clinical effect of rapid massage at Shuidao (ST 28) to prevent puerpera from postpartum urinary retention.@*METHODS@#A total of 200 puerpera giving birth through vagina were enrolled and divided into an observation group and a control group according to the random number table method, 100 cases in each group. In the observation group, rapid massage at Shuidao (ST 28) was applied. In the control group,there was no intervention and urinated naturally. The traditional Chinese medicine syndrome scale was used to evaluate poor sense of urination, and record puerpera with or without postpartum urinary retention, the poor sense of first urination, the first time of urination, the amount of first urination and postpartum hemorrhage.@*RESULTS@#The poor sense of first urination in the observation group was significantly lower than that in the control (<0.001), the first time of urination in the observation group was significantly earlier than that in the control group (<0.001), the amount of first urination in the observation group was significantly more than that in the control group (<0.001), the observation group was superior to the control group to prevent postpartum urinary retention (<0.05).@*CONCLUSION@#Rapid massage at Shuidao (ST 28) can reduce the poor sense of first urination, significantly advance the time of spontaneous urination, significantly increase the amount of first urination and effectively prevent postpartum urinary retention.

Efficacy of the herbal cake-separated moxibustion with new-type moxibustion device on urinary retention after spinal cord injury / 中国针灸

OBJECTIVE@#To compare the clinical effect of the herbal cake-separated moxibustion with new-type moxibustion device combined with bladder function exercise and simple bladder function exercise on improving urinary retention after spinal cord injury.@*METHODS@#Sixty-eight patients were randomly divided into a control group and an observation group, 34 cases in each group. The bladder function exercise was given in the control group. On the basis of the treatment in the control group, herbal cake-separated moxibustion with new-type moxibustion decice was applied at Shenque (CV 8), Guanyuan (CV 4), Qihai (CV 6), Zhongji (CV 3) for 30 min, once a day in the observation group. The two groups were treated for 4 weeks as a course, 2 courses of treatment were needed. Bladder maximum volume, bladder residual urine volume and urinary tract infection before and after treatment were compared, and the clinical efficacy was evaluated in the two groups.@*RESULTS@#The total effective rate in the observation group was 88.2% (30/34), which was better than 64.7% (22/34) in the control group (<0.05). The increase of bladder maximum volume and decrease of bladder residual urine volume in the observation group were significantly better than those in the control group (<0.01). At the 4th, 6th and 8th weeks for treatment, the improvement of urinary tract infection in the observation group was better than that in the control group (<0.05).@*CONCLUSION@#At the same time of bladder function training, herbal cake-separated moxibustion with new-type moxibustion device could improve urinary retention after spinal cord injury.

A Multi-center, Randomized, Controlled and Open Clinical Trial of Heyan Kuntai Capsule () and Hormone Therapy in Perimenopausal Women / 中国结合医学杂志

<p><b>OBJECTIVE</b>To evaluate the efficacy and safety of Heyan Kuntai Capsule (, HYKT) and hormone therapy (HT) on perimenopausal syndromes (PMSs).</p><p><b>METHODS</b>From 2005 to 2008, 390 women with PMSs were recruited from 4 clinic centers. The inclusion criteria included ages 40 to 60 years, estradiol (E2) below 30 ng/L, and follicle stimulating hormone (FSH) above 40 IU/L, etc. The patients were randomly assigned to HYKT group or HT group by random number table method, administrated HYKT or conjugated estrogen with/without medroxyprogesterone acetate tablets for 12 months. During treatment, the patients were interviewed quarterly, Kupperman Menopausal Index (KMI) scores, hot flush scores, insomnia scores, Menopause-Specific Quality of Life (MENQOL) scores and adverse effects were used for evaluating drug efficacy and safety respectively. The last interview was made at the end of 12-month treatment RESULTS: After treatment, KMI scores of HYKT group and HT group were both significantly decreased compared with baseline (P <0.01) and there was no significant difference between groups (P >0.05), except that KMI of HYKT group was higher after 3-month treatment (P <0.05). After treatment, hot flush and insomnia scores were both improved significantly in two groups (P <0.01); and HT had a better performance than HYKT in improving hot flush (P <0.05). MENQOL were significantly improved in both groups after treatment (P <0.01); but there was no significant difference between two groups (P >0.05). The incidence of adverse event in the HYKT group was much lower than that in the HT group (P <0.01).</p><p><b>CONCLUSIONS</b>HYKT could effectively relieve PMSs and improve patients quality of life without severe adverse reactions. Although HYKT exerted curative effects more slowly than hormone, it possessed better safety profile than hormone.</p>

Perilla resources of China and essential oil chemotypes of Perilla leaves / 中国中药杂志

This study, based on the findings for Perilla resources, aimed to describe the species, distribution, importance, features, utilization and status of quantitative Perilla resources in China. This not only helps people to know well about the existing resources and researching development, but also indicates the overall distribution, selection and rational use of Perilla resource in the future. According to the output types, Perilla resources are divided into two categories: wild resources and cultivated resources; and based on its common uses, the cultivated resources are further divided into medicine resources, seed-used resources and export resources. The distribution areas of wild resources include Henan, Sichuan, Anhui, Jiangxi, Guangxi, Hunan, Jiangsu and Zhejiang. The distribution areas of medicine resources are concentrated in Hebei, Anhui, Chongqing, Guangxi and Guangdong. Seed-used resources are mainly distributed in Gansu, Heilongjiang, Jilin, Chongqing and Yunnan. Export resource areas are mainly concentrated in coastal cities, such as Zhejiang, Jiangsu, Shandong and Zhejiang. For the further study, the essential oil of leaf samples from different areas were extracted by the steam distillation method and analyzed by GC-MS. The differences in essential oil chemotypes among different Perilla leaves were compared by analyzing their chemical constituents. The main 31 constituents of all samples included: perillaketone (0.93%-96.55%), perillaldehyde (0.10%-61.24%), perillene (52.15%), caryophyllene (3.22%-26.67%), and α-farnesene (2.10%-21.54%). These samples can be classified into following five chemotypes based on the synthesis pathways: PK-type, PA-type, PL-type, PP-type and EK-type. The chemotypes of wild resources included PK-type and PA-type, with PK-type as the majority. All of the five chemotypes are included in cultivated resources, with PA-type as the majority. Seed-used resources are all PK-type, and export resources are all PA-type. The P. frutescens var. frutescens include five chemotypes, with PK-type as the majority. The PK-type leaves of P. frutescens var. acuta are green, while the PA-type leaves are reddish purple. The P. fruteseens var. crispa was mainly PA type with reddish purple leaves. The differences of the main chemotypes provide a scientific basis for distinguishing between Zisu and Baisu in previous literatures. Based on the lung toxicity of PK and the traditional use of Perilla, the testing standard of essential oil and Perilla herb shall be built, and PA type is recommended to be used in traditional Chinese medicine.

Effect of Jiawei Foshou San and its compatibility on hepatic P450 enzyme activity and hepatocyte morphology in rats / 中国中药杂志

To investigate the effect of Jiawei Foshou San and its various combined administration on hepatic P450 enzyme activity and hepatocyte morphology in rats. Rats were orally administered with drugs for four weeks and then sacrificed to prepare liver microsomes. The liver microsomes were incubated with the cocktail method; The metabolites were determined with the rapid liquid chromatography with tandem mass spectrometry (LC-MS/MS) to investigate the hepatocyte P450 enzyme activity. In addition, the hepatic pathological changes were observed by using the hematoxylin and eosin (HE) staining. Compared with the control group, the enzyme activity of CYP1A2 and CYP3A4 in the Jiawei Foshou san group showed a significant rise (P < 0.05); the enzyme activity of CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 in the ferulic acid + ligustrazine group and the ligustrazine + tetrahydropalmatine group showed a significant rise (P < 0.05) ; the enzyme activity of CYP1A2, CYP2D6 and CYP2E1 in the ligustrazine group showed a significant rise (P < 0.05); the enzyme activity of CYP3A4 in the ferulic acid group showed a significant reduction (P < 0.05). After the administration with various drugs, the hepatocyte morphologies in the ferulic acid group and the ligustrazine group were normal. The pathological changes were observed in the tetrahydropalmatine group, such as unclear boundary of hepatic lobules, disordered hepatic cell arrangement, blurred edge, anisokaryosis and infiltration of inflammatory cells. The ferulic acid + tetrahydropalmatine group, the ligustrazine + tetrahydropalmatine group and the Jiawei Foshou San group also showed inflammatory infiltration, but with less pathological changes, particularly the Jiawei Foshou San group. The study result shows that Jiawei Foshou San can induce the enzyme activity of CYP1A2 and CYP3A4, and ligustrazine may be the effective substance for inducing CYP1A2. Its combination with ferulic acid and ligustrazine can significantly reduce the liver toxicity of tetrahydropalmatine.

Yinxingye Capsule Intervened Vascular Endothelial Cell Apoptosis of Hyperhomocysteinemia Rats: an Experimental Study / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To explore targets of Chinese herbal medicine at cellular and molecular leve1s through an experimental study on Yinxingye Capsule (YC) intervening vascular endothelial cell apoptoeis of hyperhornocysteinemia (HHcy) rats.</p><p><b>METHODS</b>The HHcy model was prepared in male Wistar rats. Totally 42 rats were randomly divided into 4 groups, i.e., the control group (n =10), the model group (n = 11), the YC group (n =11), the folic acid group (n =10). Carboxy methyl cellulose (CMC) solution (1%) was administered to rats in the control group by gastrogavage.3% methionine suspension at 1. 5 g/kg was administered to rats in the model group by gastrogavage. 3% methionine suspension at 1. 5 g/kg and folic acid suspension at 0. 06 g/kg was administered to rats in the folic acid group by gastrogavage. 3% methionine suspension at 1. 5 g/kg and YC at 0. 02 g/kg was administered to rats in the YC group by gastrogavage. Morphological changes of aortic tissue were observed by hematoxylin eosin (HE) staining. The plasma homocysteine (Hcy) level was detected in each group. The endothelium-dependent diastolic functions of the thoracic aorta on different concentrations of sodium nitroprusside (SNP) and acetylcholine (Ach) were detected. Gene expressions of Bcl-2-associated X protein (BAX), inducible nitric oxide synthase (iNOS), c-Fos, cellular inhibitor of apoptosis protein 2 (c-IAP2) were detected by real time polymerase chain reaction (RT-PCR).</p><p><b>RESULTS</b>Pathological results showed that thickening aortic endothelium, swollen and desquamated endothelial cells. Few foam cells could be seen in the model group. Myoma-like proliferation of smooth muscle cells in tunica media could also be seen. These pathological changes were milder in the YC group and the folic acid group. Compared with the control group, plasma Hcy levels increased in the model group (P <0. 05). The endothelium-dependent diastolic rates at 10(-6) and 10(-4)mol/L Ach and 10(-7) -10(-3)mol/L SNP all decreased in the model group (P <0. 01, P <0. 05). Gene expressions of Bax, c-Fos, and iNOS increased, but c-IAP2 gene expressions decreased in the model group (all P <0. 05). Compared with the model group, plasma Hcy levels decreased in the YC group and the folic acid group (P <0. 05). The endothelium-dependent diastolic rates increased in the YC group and the folic acid group at various SNP concentrations except 10(-6) mol/L SNP in the folic acid group. The endothelium-dependent diastolic rates increased in the YC group and the folic acid group at 10(-6) and 10(-4)mol/L Ach (all P <0. 05). Gene expressions of Bax, c-Fos, and iNOS decreased in the YC group and the folic acid group, but c-IAP2 gene expression increased in the folic acid group (all P <0. 05).</p><p><b>CONCLUSION</b>YC could reduce plasma Hcy levels, down-regulate gene expressions of Bax, c-Fos, and iNOS, thereby reducing apoptosis of vascular endothelial cells, improving vascular endothelial function, and delaying atherosclerotic process.</p>

Effect of Jinlida on changes in expression of skeletal muscle lipid transport enzymes in fat-induced insulin resistance ApoE -/- mice / 中国中药杂志

<p><b>OBJECTIVE</b>To study the effect of Jinlida on changes in expression of skeletal muscle lipid transport enzymes in fat-induced insulin resistance ApoE -/- mice.</p><p><b>METHOD</b>Eight male C57BL/6J mice were selected in the normal group (NF), 40 male ApoE -/- mice were fed for 16 weeks, divided into the model group (HF), the rosiglitazone group ( LGLT), the Jinlida low-dose group (JLDL), the Jinlida medium-dose group (JLDM), the Jinlida high-dose group (JLDH) and then orally given drugs for 8 weeks. The organization free fatty acids, BCA protein concentration determination methods were used to determine the skeletal muscle FFA content. The Real-time fluorescent quantitative reverse transcription PCR ( RT-PCR) and Western blot method were adopted to determine mRNA and protein expressions of mice fatty acids transposition enzyme (FAT/CD36), carnitine palm acyltransferase 1 (CPT1), peroxide proliferators-activated receptor α( PPAR α).</p><p><b>RESULT</b>Jinlida could decrease fasting blood glucose (FBG), cholesterol (TC), triglyceride (TG), free fatty acid (FFA) and fasting insulin (FIns) and raise insulin sensitive index (ISI) in mice to varying degrees. It could also up-regulate mRNA and protein expressions of CPT1 and PPARα, and down-regulate mRNA and protein levels of FAT/CD36.</p><p><b>CONCLUSION</b>Jinlida can improve fat-induced insulin resistance ApoE -/- in mice by adjusting the changes in expression of skeletal muscle lipid transport enzymes.</p>

Effect of Morinda officinalis capsule on osteoporosis in ovariectomized rats / 中国天然药物

AIM@#To explore the therapeutic effects of Morinda officinalis capsules (MOP) on osteoporosis in ovariectomized rats.@*METHODS@#Six-month-old female Sprague-Dawley rats were induced for postmenopausal osteoporosis (PMOP) by bilateral ovariectomy and divided into seven groups as follows: sham-operated group, ovariectomized (OVX) control group, OVX treated with xianlinggubao (XLGB) (270 mg·kg⁻¹·d⁻¹), OVX treated with alendronate sodium (ALN) (3 mg·kg⁻¹·d⁻¹), and OVX treated with Morinda officinalis capsule (MOP) of graded doses (90, 270 and 810 mg·kg⁻¹·d⁻¹) groups. Oral treatments were administered daily on the 4(th) week after ovariectomy and lasted for 12 weeks. The bone mineral density was evaluated by dual-energy X-ray absorptiometry. The tartrate-resistant acid phosphatase (TRAP), alkaline phosphatase (AKP), and osteocalcin (OC) levels in the serum and plasma were determined by standard colorimetric and enzyme immunoassays methods. Bone biomechanical properties and morphological parameters were analyzed by three-point bending test and histomorphometry respectively.@*RESULTS@#Morinda officinalis capsules at all doses were able to significantly prevent the OVX-induced loss of bone mass due to diminishing serum AKP and TRAP levels while elevating OC level in the plasma. Morinda officinalis capsules also enhanced the bone strength and prevented the deterioration of trabecular microarchitecture.@*CONCLUSION@#Morinda officinalis capsules possess potent anti-osteoporotic activity in OVX rats which could be an effective treatment for postmenopausal osteoporosis.

Impact of drug molecules on HP-β-CD compound inclusion / 中国中药杂志

To study the interaction of drugs of different properties, namely puerarin, borneol and catalpol in the process of in- clusion, in order to explore the inclusion regularity of multi-component and multi-property traditional Chinese medicine compound in- clusions. With HP-β-CD as the inclusion material, the freeze-drying method was used to prepare the inclusion. The inclusion between puerarin, borneol and catalpol was tested by measuring the inclusion concentration, DSC and X-ray diffraction. According to the find- ings, when insoluble drugs puerarin and borneol were included simultaneously, and puerarin was overdosed, puerarin included was almost equal to puerarin included, and borneol was not included. When puerarin was under-dosed, and HP-β-CD was overdosed, borne- ol was included, and the simultaneous inclusion was lower than the separate inclusion of borneol. When water-soluble drug catalpol was jointly included with puerarin or borneol, the simultaneous inclusion was almost the same with their separate inclusion, without charac- teristic peak of catalpol in DSC and X-ray diffraction patterns. There is a competition in the simultaneous inclusion between water-solu- ble drugs puerarin and borneol and a stronger competition in puerarin. The water-soluble drug catalpol could be included with HP-β-CD with no impact on the inclusion of puerarin or borneol.

ILs-HPLC simultanesous determination of five alkaloids in phellodenddri chinensis cortex / 中国中药杂志

A RP-HPLC method was established for simultaneous determination of phellodendrine hydrochloride (PH1), magnoflorine hydrochloride (MH), jatrorrhizine hydrochloride (JH), palmatine hydrochloride (PH2) and berberine hydrochloride (BH) in Phellodendri Chinensis Cortex by using ionic liquids as mobile phase additives. The separation was performed on a Kromasil C18 (4.6 mm x 250 mm, 5 μm) coupled with ultraviolet (UV) detection. The effect of extraction solvent, detection wavelength, length of alkyl chain on different imidazolium ionic liquids and concentration of ionic liquids on the separation and determination of alkaloids were investigated. Ionic liquid, [BMIm] BF4, can obviously improve the resolution and peak shape. This ILs-HPLC method is simple, rapid, and reliable, which can be used for determination of alkaloids in Phellodenddri Chinensis Cortex.

The development of quality of life questionnaire of Chinese medicine for postoperative patients with colorectal cancer and item screening / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To develop quality of life questionnaire of Chinese medicine for postoperative patients with colorectal cancer (QLQ-CMPPCC), thus comprehensively and objectively evaluating the clinical efficacy of Chinese medicine and pharmacy in treating postoperative patients with colorectal cancer (CC).</p><p><b>METHODS</b>The theoretical structure model of the questionnaire was addressed in combined with basic theories of Chinese medicine according to the principle of WHO quality of life (QOL). The primary questionnaire was developed using methods of structuralization policy making after we extensively retrieve various universal and specific questionnaires for CC cancer patients at home and abroad. The 205 CC patients were tested by questionnaire. The items were screened using experts grading method, item selection analysis, dispersion trends of standard deviation, t-test, correlation coefficient method, factor analysis,and Cronbach's alpha.</p><p><b>RESULTS</b>The QLQ-CMPPCC was developed containing four domains of physical, psychological, independence, and social functions, involving 20 aspects and 54 items. Of them, non-fistula patients answered 43 items and fistula patients answered 46 items. One item covered the general QOL evaluation.</p><p><b>CONCLUSIONS</b>QLQ-CMPPCC showed Chinese medical features. It comprehensively reflected the connotation of QOL for postoperative CC patients. It could be taken as a tool for evaluating Chinese medical efficacy for postoperative CC patients.</p>

Protective effects of da chai hu granules (DCHKL) against alloxan (AXN)-induced rat pancreatic islets damage / 药学学报

The protective effects of Da Chai Hu Granules (DCHKL) on islet cells which were incubated with 4 mmol x L(-1) alloxan (AXN) were studied. The viability of islet cells were measured with MTT. Insulin released into medium and in islets was detected by radioimmunoassay. Cell apoptosis rate was determined by flow cytometry. The expression of anti-apoptotic gene Bcl-2 and pro-apoptotic gene Bax in islet cells were measured with RT-PCR (reverse transcription polymerase chain reaction). Serum containing DCHKL can promote the activity of islet cells significantly (P < 0.01). Basal insulin secretion and high glucose-stimulated insulin secretion increased significantly (P < 0.01). Serum containing DCHKL can inhibit apoptosis of islet cells, the ratio of apoptosis was decreased. Serum containing DCHKL increased expression of Bcl-2 mRNA and decreased expression of Bax mRNA. DCHKL can significantly promote proliferation of islet cells and increase the amount of basal secretion of pancreatic islet cells and high glucose-stimulated insulin secretion. The expression of Bcl-2 increased significantly. The expression of Bax decreased significantly. DCHKL have a protective effect on the islet cells.

Management and prognostic factors for 119 patients with follicular thyroid carcinoma / 中华肿瘤杂志

<p><b>OBJECTIVE</b>To explore the optimal management and analyze the prognostic factors for follicular thyroid carcinoma.</p><p><b>METHODS</b>The clinicopathological data of 119 patients with well-differentiated follicular thyroid carcinoma treated in our hospital from 1970 to 2008 were retrospectively reviewed. The overall survival (OS) rate was estimated by Kaplan-Meier method. Log rank and Cox regression analyses were used to identify the prognostic factors.</p><p><b>RESULTS</b>The 5- and 10-year OS rates were 81.1% and 66.7%, respectively. The 3- , 5- and 10-year cumulative distant metastasis rates were 27.4%, 29.6% and 35.9%, respectively. The age of ≥ 45 years old was one of the most important factors affecting survival rate (P < 0.05) and an independent factor for distant matastasis.</p><p><b>CONCLUSIONS</b>Follicular thyroid carcinoma has some special features such as diffuse growth and vascular tumors thrombosis and with a relatively poor prognosis. The key measure to improve local control and prognosis is radical resection. Some aggressive management such as total thyroidectomy combined with (13)1I therapy and regular follow-up should be performed to improve the survival rate and to control postoperative distant metastasis for patients ≥ 45 years old.</p>