2.Preparation process of rutacarpine-hydroxypropyl-beta-cyclodextrin inclusion complex.
Chun-Lin YAN ; Ji ZHANG ; Yong HOU ; Gui-Ping XUE ; Shu WANG ; Qing-Ya ZHAO
China Journal of Chinese Materia Medica 2014;39(5):828-832
Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.
2-Hydroxypropyl-beta-cyclodextrin
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Alkaloids
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chemistry
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Chemistry, Pharmaceutical
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methods
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Drug Carriers
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chemistry
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Drugs, Chinese Herbal
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chemistry
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Rutaceae
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chemistry
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Solubility
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beta-Cyclodextrins
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chemistry
5.Effect of electroacupuncture pretreatment on the protein expression of c-fos in fastigial nucleus and lateral hypothalamus area in rats with acute myocardial ischemia-reperfusion injury
Rong-Lin CAI ; Xue-Fang SHAO ; Qing YU ; Ya-Ting ZHANG ; Xiao-Tong WEI ; Ling HU
Journal of Acupuncture and Tuina Science 2021;19(1):10-18
Objective: To observe the effect of electroacupuncture (EA) pretreatment on the protein expression of c-fos in fastigial nucleus (FN) and lateral hypothalamus area (LHA) in rats with acute myocardial ischemia-reperfusion injury (MIRI), and to explore the role and mechanism of FN and LHA in EA at the Heart Meridian fighting against acute MIRI reaction. Methods: Seventy Sprague-Dawley rats were randomly divided into a sham operation group, a model group, an EA-Heart Meridian group and an EA-Lung Meridian group, with 14 rats in each group; an LHA lesion plus EA-Heart Meridian group (LHA+EA-Heart Meridian group) and a FN lesion plus EA-Heart Meridian group (FN+EA-Heart Meridian group), with 7 rats in each group. Except the sham operation group, the left anterior descending branch of coronary artery was ligated to establish acute MIRI rat models in the other 5 groups. In the three groups with EA-Heart Meridian treatment, Shenmen (HT 7) and Tongli (HT 5) were selected; Taiyuan (LU 9) and Lieque (LU 7) were selected in the EA-Lung Meridian group. All the EA groups received EA stimulation prior to modeling, with 1 mA in current intensity and 2 Hz in frequency, 20 min each time, once a day for a total of 7 d. The sham operation group and the model group did not receive EA stimulation. The electrocardiogram was observed in the rats to analyze the ST-segment deviation and cardiac arrhythmia score. The expression of c-fos protein in FN and LHA was detected by immunohistochemistry method. Results: Compared with the sham operation group, the ST-segment deviation, cardiac arrhythmia score and the expression of c-fos protein in the FN and LHA increased significantly in the model group (all P<0.05). Compared with the model group, the ST-segment deviation, cardiac arrhythmia score and the expression of c-fos protein in FN and LHA decreased significantly in the EA-Heart Meridian group (all P<0.05). Compared with the EA-Heart Meridian group, the ST-segment deviation and cardiac arrhythmia score increased significantly in the EA-Lung Meridian group, LHA+EA-Heart Meridian group and FN+EA-Heart Meridian group (all P<0.05); the expression of c-fos in FN increased significantly in the EA-Lung Meridian group and LHA+EA-Heart Meridian group (both P<0.05); the expression of c-fos in LHA increased significantly in the EA-Lung Meridian group and FN+EA-Heart Meridian group (both P<0.05). Conclusion: FN and LHA are involved in the mechanism of EA at Heart Meridian to improve the acute MIRI reactions, and the cerebellum may participate in the improvement of cardiac function by EA through the cerebellum-hypothalamus projection.
6.Effect of Huanglian Jiedu Decoction on Monocyte Development in apoE Gene Knockout Mice.
Bing CHEN ; Ya-xian KONG ; Yu-mei LL ; Xin XUE ; Jian-ping ZHANG ; Hui ZENG ; Jing- qing HU ; Ya-luan MA
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(1):99-103
OBJECTIVETo observe monocyte (Mo) development in wild type C57BL/6 mice and apoE gene knockout (apoE(-/-)) mice, and to evaluate the immuno-regulatory effect of Huanglian Jiedu Decoction (HJD) on peripheral Mo development in apoE(-/-) mice.
METHODSFour, 8, 12, and 16 weeks old female C57BL/6 mice were set up as control groups of different ages, while 4, 8, 12, and 16 weeks old female apoE(-/-) mice were set up as hyperlipidemia groups of different ages. Four-week old female C57BL/6 mice were recruited as a blank group. Four-week old female apoE(-/-) mice were randomly divided into the control group, the Western medicine group, and the Chinese medicine group by paired comparison, 5 in each group. Equivalent clinical dose was administered to mice according to body weight. Mice in the Western medicine group were administered with Atrovastatin at the daily dose of 10 mg/kg by gastrogavage, while those in the Chinese medicine group were administered with HJD at the daily dose of 5 g/kg by gastrogavage. Body weight was detected each week. After 4 weeks blood lipids levels (such as TG, TC, LDL-C, and HDL-C), and the proportions of Mo and Ly6c(hi) were detected.
RESULTSCompared with 4-week-old homogenic mice, the proportion of Mo decreased in 16-week-old C57BL/6 mice (P < 0.05). Levels of TC and TG, and the proportion of Ly6c(hi) subtype increased, but the proportion of Mo de- creased in 8-week-old apoE(-/-) mice (P <0. 05). Levels of TC, TG, and LDL-C increased in 12-week-old apoE(-/-) mice (P < 0.05). Levels of TC, TG, LDL-C, and HDL-C increased in 16-week-old apoE(-/-) mice (P < 0.05, P < 0.01). Compared with 8-week-old homogenic mice, the proportion of Mo decreased in 16-week-old C57BL/6 mice (P < 0.05); levels of TC and LDL-C increased in 12-week-old apoE(-/-) mice (P < 0.05); levels of TC and HDL-C increased in 16-week-old apoE(-/-) mice (P < 0.05, P < 0.01). Compared with C57BL/6 mice of the same age, TC and TG increased, HDL-C decreased (P < 0.01) in 4-and 8-week-old apoE(-/-) mice (P < 0.01); levels of TC, TG, LDL-C increased, and HDL-C level decreased in 12- and 16-week-old apoE(-/-) mice (P < 0.05, P < 0.01); the proportion of Mo increased in 4-week-old apoE(-/-) mice (P < 0.05); proportions of Mo and Ly6c(hi) increased in 8-week-old apoE(-/-) mice (P < 0.05). Compared with the blank control group, levels of TC, TG, and LDL-C, proportions of Mo and Ly6c(hi) increased (P < 0.01, P < 0.05), but HDL-C level decreased (P <0. 01) in the control group after intervention. Compared with the control group, body weight gained less in the Western medicine group and the Chinese medicine group (P < 0.05); the proportion of Ly6c(hi) subtype decreased in the Chinese medicine group (P < 0.05).
CONCLUSIONSIn development process blood lipids levels in apoE(-/-) mice are not only associated with age. Blood lipids levels induced growth changes in natural immune system are also correlated with age. In early stage of lipids development HJD intervention could correct this special immune disorder in apoE(-/-) mice.
Animals ; Apolipoproteins E ; genetics ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Female ; Gene Knockout Techniques ; Hyperlipidemias ; Lipids ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Monocytes ; physiology
7.Effect of Action Observation Therapy on Upper Limb Function in Children with Spastic Hemiplegic Cerebral Palsy
Ya-Min WEI ; Zhi-Mei JIANG ; Jing-Hua TANG ; Jia-Yin DU ; Xue-Mei LI ; Ya-Nan WANG ; Meng-Qing LI
Chinese Journal of Rehabilitation Theory and Practice 2018;24(4):432-436
Objective To explore the effect of action observation therapy (AOT) on upper limb function in children with spastic hemiplegic cerebral palsy,and the better program. Methods From March to November,2017,45 children with spastic hemiplegic cerebral palsy were randomly assigned to control group and AOT group.The control group was further divided into group A(n=11)and group B(n=11), and received conventional rehabilitation treatment and scenic-observation therapy, 20 minutes every time for group A,and 30 minutes every time for group B.AOT group was further divided into group C(n=10)and group D (n=11), and received AOT in addition, 20 minutes every time for group C, and 30 minutes every time for group D,five times each week for twelve weeks for all the groups.Before treatment,eight and twelve weeks af-ter treatment, they were assessed with hand grip strength, Upper Extremities Functions Test (UEFT), and Wee Functional Independence Measure(WeeFIM). Results After treatment,the hand grip strength and the score of UEFT were better in group D than in groups B and C(P<0.05),and were better at twelve weeks than at eight weeks(P<0.05).No significant difference was found in the score of WeeFIM among groups after treatment(P>0.05). Conclusion AOT could improve upper limp function in children with spastic hemiplegic cerebral palsy,and it's more ef-fective after more training.
8.Study on supercritical CO2 extraction of xiaoyaosan and its GC-MS fingerprint.
Ya-Mei ZUO ; Jun-Sheng TIAN ; Xiao-Qing GUO ; Yu-Zhi ZHOU ; Xiao-Xia GAO ; Xue-Mei QIN
China Journal of Chinese Materia Medica 2014;39(4):674-678
To determine the optimum conditions of supercritical CO2 extraction of Xiaoyaosan, and establish its fingerprint by gas chromatography-mass spectrometry (GC-MS), the yield of extract were investigated, an orthogonal test was used to quantify the effects of extraction temperature, pressure, CO2 flow rate and time, and fingerprint analysis of different batches of extracts were by GC-MS. The optimal extraction conditions were determined as follows: extraction pressure 20 MPa, extraction temperature 50 degrees C, CO2 flow rate 25 kg x h(-1), extraction time 3 h, and average yield 2.2%. The GC-MS fingerprint was established and 27 common peaks were found, whose contents add up to 81.89% of the total peak area. Among them, 21 compounds were identified, accounting for 53.20% of the total extract. The extraction process is reasonable and favorable for industrial production. The GC-MS method is accurate, reliable, reproducible, and can be used for quality control of supercritical CO2 extract from Xiaoyaosan.
Carbon Dioxide
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chemistry
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Chromatography, Supercritical Fluid
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methods
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Drugs, Chinese Herbal
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chemistry
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isolation & purification
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Gas Chromatography-Mass Spectrometry
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methods
9.Effect of Danhong injection on intimal hyperplasia and expressions of bFGF and TF in carotid artery of rabbits after PTA
Geng LIAO ; Ya-Qing SHU ; Xue-Qiang HU
Chinese Journal of Neuromedicine 2011;10(7):673-678
Objecfive To study the effect of Danhong injection(DI)on intimal hyperplasia and expressions of basic fibroblast growth factor(bFGF)and tissue factor(TF)in carotid arteries of rabbits after percutaneous transluminal angioplasty(PTA). Methods Fifty New Zealand White rabbits were randomly divided into 5 groups (n=10),namely sham-operated group,model group,and DI treatment groups(low-,medium-and high-dose DI treatment groups).The animals in the sham-operated group were only given external carotid artery ligation.The rabbit models of carotid stenosis in the later 4 groups were established by ballon-injury.Before the carotid balloon injury,the animals in the DI treatment groups were given DI at doses of 1 mL/kg·d-1,2mL/kg·d-1 and 4 mL/kg·d-1,respectively,for 7 or 14 d via intravenous injection;the animals in the sham-operated and model groups were given saline solution(2mL/kg·d-1)instead.The animals were sacrificed and their common carotid arteries were removed on the 7th and 28th d of surgery;morphology changes of the arterial wall with hematoxylin eosin staining were observed by optical microscope,and the expressions ofbFGF and TF of the vascular wall were detected through immunohistochemical techniques;with the help of an image analysis system,semiquantitative analysis was performed.Results On the 7th d of surgery,the intimal area and intima area/media area (I/M)ratio in the model group showed no significant differences as compared with those in the other 4groups(P>0.05).On the 28th d of surgery,the intimai area and I/M ratio in the model group were increased markedly as compared with those in the sham-operated group (P<0.05), and the intimal area and I/M ratio in the medium and high dose DI treatment groups were significantly reduced as compared with those in the in the model group (P<0.05). The expressions of TF and bFGF in the neointima of carotid arteries of rabbits treated with medium and high dose of DI were significantly weaker than those of the model group (P<0.05), and those of rabbits treated with low dose of DI had no obvious differences as compared with those of the model group (P>0.05). Conclusion Medium and high dose of DI can inhibit the intimal hyperplasia resulting from percutaneous transluminal angioplasty, might through the inhibition of expressions of bFGF and TF in the neointima of the arterial wall.
10.Selection of choriocarcinoma-associated genes using bioinformatics
Xue-Nong LI ; Ya-Ling LI ; Guo-Bing LIU ; Yan-Qing DING
Journal of Southern Medical University 2005;25(1):1-6
Objective To analyze the data of gene expression profiles of choriocarcinoma and screen for choriocarcinomarelated genes. Methods Human cDNA expression microarray containing 4 096 genes was used to study the gene expression profiles in specimens of complete hydatidiform moles (n=3) and choriocarcinomas (n=3), with normal placental villi serving as the control group. The candidate genes with similar expression profiles were identified by hierarchical cluster analysis, and their expressions in normal and neoplastic tissues analyzed by electronic Northern analysis and other bioinformatics methods.Three selected genes were analyzed by β-actin semiquantitative reverse transcriptase-PCR to confirm the data. Results A total of 52 coexpressed candidate genes were identified from the gene expression data derived from the choriocarcinoma specimens, of which 19 genes were selected as choriocarcinoma-related genes by further cluster analysis, such as dynamin (L07807), kataninp60 (AF056022), zinc fingerproteinZNF184 (U6656), calmodulin (U12022), carboxypeptidaseM (BC022276), calcineurin-binding protein cabin 1 (NM_012295) and transducin-like enhancer protein TLE1 (M99435).Conclusion The identification of choriocarcinoma-related genes by cluster analysis provides new clues for seeking the key genes associated with the progression and metastasis of choriocarcinoma.