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September 15,2015
Volume 8,Issue 17
Pages -
Subject Area:Chinese and Western Integrative Medicine,Chemistry of Traditional Chinese Medicine,Basic Theories of Traditional Chinese Medicine

Title: Research of chemical constituents from twigs and leaves of Rhododendron micranthum

Authors: ZHANG Mengke, ZHAN Guanqun, LEI Liang, XUE Yongbo, LUO Zengwei, WAN Qian, YAO Guangmin, ZHANG Yonghui
PP: 1861-1865
Abstract: Objective: To study the chemical constituents in the twigs and leaves of Rhododendron micranthum. Methods: The compounds were isolated by column chromatography, and the structures were elucidated by spectral analyses. Results: Eleven compounds are isolated and identified as (4R,8S)- uroterpenol (1), angelicoidenol (2), 6-exo-hydroxyborneol (3), 5-methoxymethyl-1H-pyrrole-2-carboxal-dehyde (4), vanillic acid (5), scopoletin (6), trans-isoferulic acid (7), dihydrosyringenin (8), 3-(4-hydroxy-3,5-dimethoxyphenyl)-1,2-propanediol (9), shanyegenin B (10), and jasmololone (11). Conclusion: Compound 1 is isolated as a natural product for the first time. Compounds 1-5 and 7-11 are isolated from R. micranthum for the first time, and compounds 1-4 and 7-11 are firstly isolated from the plants of Rhododendron.
Keywords: medicinal chemistry; Ericaceae; Rhododendron micranthum; chemical constituents; (4R,8S)-uroterpenol; scopoletin

Title: Optimization of ultrasonic extraction of phenol compounds using response surface methodology and antioxidant activity from Schisandra chinesnsis fruits

Authors: ZHANG Yueyi, ZHAO Yan, CAI Enbo, LIU Shuangli, YANG He, ZHANG Lianxue
PP: 1851-1860
Abstract: Objective: The phenolic compounds from Schisandra chinesnsis fruits was extracted using ultrasonic-assisted extraction methodology. Methods: Central composite design method was employed to optimize three extraction variables, including ethanol concentration (x1), extraction time (x2), and liquid-solid ratio (x3), for the achievement of high extraction yield of the phenolic compounds. Results: The results show that the optimized conditions are x1 of 44%, x2 of 15 min, and x3 of 215 mL/g. Under these conditions, the experimental yield is 1.12% (n = 3), which is well matched with the predicted yield of 1.19%. The evaluation of antioxidant activity by DPPH assay indicates that the phenolic compounds from S. chinesnsis fruits possess significant antioxidant activity. High performance liquid chromatography (HPLC) analysis reveals that pyrogallol, chlorogenic acid, epicatechin, rutin and ferulic acid are the major composition in the extracts. Conclusion: Ultrasonic-assisted extraction was proved to be a kind of efficient and rapid method for extraction of S. chinesnsis fruits.
Keywords: medicinal chemistry; total phenolic; ultrasonic extraction; central composite design; response surface analysis; antioxidant activity

Title: Synthesis and inhibitory activity on human umbilical vein endothelial cells of mutual prodrug of Combretastatin A-4 and aminosaccharides

Authors: LIU Kun, ZHU Qihua, XU Yungen
PP: 1844-1850
Abstract: To improve the solubility and druggability of Combretastatin A-4 (CA-4), six coupling compounds (12a-12f) of CA-4 and aminosaccharides were designed and synthesized. Their structures were characterized by 1H NMR, MS. Preliminary biological evaluation results showed that all the target compounds on the concentration of 1×10^5, 1×10^6, 1×10^7 mol/L could inhibit human umbilical vein endothelial cells (HUVECs) proliferation well in vitro. The inhibitory effects of 12d and 12f were more potent than positive drug Combretastatin A-4 at the concentration 1×10^5 mol/L and 1×10^7 mol/L respectively.
Keywords: medicinal chemistry; angiogenesis inhibitor; Combretastatin A-4; aminosaccharides; mutual prodrug

Title: Biomimetic synthesis of calcium phosphate nanoparticles by employing template method

Authors: GUO Shanshan, YANG Hua, SONG Xueying, GU Wei
PP: 1839-1843
Abstract: The calcium phosphate (CaP) nanoparticles were biomimetically prepared in aqueous solution at ambient temperature and pressure using carboxymethylcellulose (CMC) as the template. The morphology change and the phase transition of CaP during the biomimetic process were investigated by Fourier transform infrared (FTIR) spectrometer, transmission electron microscope (TEM) and X-ray diffractometer (XRD). It was revealed that the CaP prepared in the presence of CMC experienced a transition from spherical amorphous CaP (ACP) to more thermostable needle-like hydroxyapatite (HAp).
Keywords: pharmaceutics; biomimetic preparation; calcium phosphate; template; carboxymethylcellulose

Title: Study on magnetic protein imprinted polymer nanoparticles

Authors: LIU Zheshuo, LIU Yu, WANG Yanming, YAN Xueying
PP: 1832-1838
Abstract: The objective of the research is to prepare magnetic molecularly imprinted nanoparticles (MMIPNs) aimed at proteins and analyze their system characterization. Spherical MMIPNs with the diameter size
Keywords: pharmaceutics; molecularly imprinting; protein; adsorption; magnetic; nanoparticles

Title: Preparation and characterization of hyaluronic acid-coated lovastatin reconstituted high density lipoprotein drug delivery system

Authors: LIU Lisha, ZHANG Wenli, HE Hongliang, ZHANG Mengyuan, ZHANG Shuangshuang, LIU Jianping
PP: 1824-1831
Abstract: Objective: Considering hyaluronic acid (HA) as coating material, the primary purpose of this study was to prepare a newly stable reconstituted high density lipoprotein (rHDL) loading lovastatin (LT) with long circulation and investigate its physic-chemical properties as well as in vitro drug release behavior. Methods: Firstly, LT loaded with nanostructured lipid carriers (LT-NLC) was prepared through thin film dispersion method and optimized by the single factor experiment. Then LT loaded with rHDL (LT-rHDL) and Apo-AI was prepared through cholate sodium mediation according to the previous study. Next, the optimal formulation of HA-LT-rHDL was prepared by electrostatic absorption and screened by the single factor experiment. The particle size, Zeta potential and morphology of HA-LT-rHDL was observed. Entrapment efficiency (EE) and drug loading content (DL) was determined under micro-column centrifugation. In vitro drug release test was studied through dialysis method. Results: In vitro characterizations indicated that the mean size and Zeta potential of HA-LT-rHDL were (152.9±2.4) nm and (-25.66±0.65) mV, respectively. EE was 90.21 % and DL was (4.34±0.59)%. Transmission electron microscope (TEM) photographs revealed that HA-LT-rHDL presented the obvious core-shell structure. In vitro drug release test showed that the cumulative drug release at 72 h of HA-LT-rHDL was merely 40%, which presented obvious sustained- release behavior. Conclusion: HA-LT-rHDL exhibited the obvious core-shell structure with effective encapsulation and sustained release behavior.
Keywords: pharmaceutics; reconstituted high density lipoprotein; lovastatin; nanostructured lipid carriers

Title: Thirty cases of clinical observation of liver dispersing with spleen strengthening combined with insulin to treat type 2 diabetes with hyperlipidemia

Authors: XU Xiaohu, WU Xiao, XIAO Fengying, ZHENG Cuihong
PP: 1818-1823
Abstract: Objective: To observe the influence of the therapy of liver dispersing with spleen strengthening combined with insulin on type 2 diabetes with hyperlipidemia. Methods: Sixty patients were divided into treatment group and control group, each group was 30. All patients were given general treatment and standard insulin hypoglycemic therapy during the treatment. The treatment group took decoction of liver dispersing with spleen strengthening while the control group did not. The courses of treatment are 8 weeks. Glycated hemoglobin (HbA1C), triglycerides (TG), total cholesterol (TC), high density lipoprotein cholesterol (HDL-c) and low density lipoprotein cholesterol (LDL-c) were measured at the baseline and 2, 4, 8 weeks after randomization while the body-weight changes and clinical symptoms were observed. Results: TG were improved after 2 weeks of treatment in each group, but there was no significant difference between the two groups. HDL-c were increased and TC, TG, HbA1C were better improved after 4 weeks\' treatment compared with the control group (P＜0.05). HDL-c were increased and TC, TG, HbA1C were better improved after 8 weeksʼ treatment compared with the control group (P＜0.05). The clinical symptoms were improved in treatment group compared with the control group after intervention (P＜0.05). Conclusion: The therapy of liver dispersing with spleen strengthening combined with insulin were better than ordinary insulin therapy alone in improving clinical symptoms and clinical efficacy in the treatment of type 2 diabetes with hyperlipidemia.
Keywords: integrated traditional Chinese and western medicine; liver dispersing with spleen strengthening; type 2 diabetes; hyperlipidemia; clinical observation

Title: Establishment on Yang deficiency and bone metastasis model of nude mice

Authors: HUANG Lizhong, MAO Dan, FENG Lei, ZHANG Hui
PP: 1809-1817
Abstract: Objective: To establish a Yang deficiency and bone metastasis model of nude mice by combining disease and syndrome method. Methods: We used intramuscular injected hydrocortisone for nude mice to establish the model Yang deficiency syndrome. The bone metastasis model for nude mice was established by injecting breast cancer MDA-MB-231 cells suspension to the ventriculus sinistee. In addition, the nude mice survival and the body weight were observed and the X-ray imaging, the imaging score and pathology observation were conducted and the value of cAMP, cGMP and thyroid hormone T3 were determined. Results: After injecting hydrocortisone, the nude mice had Yang deficiency performance, such as aversion to cold, reduced activity, apathetic, fur less shiny, eating less and thin stool, as well as cAMP decreasing while cGMP increasing, cAMP/cGMP decreasing and T3 increasing obviously. After injecting breast cancer cells suspension to the ventriculus sinistee, the nude mice appeared different degree bone metastasis, and the X-ray imaging examination and histopathological examination confirmed the diagnosis. Conclusion: 1) Hydrocortisone injection can establish the Yang deficiency model of nude mice successfully. 2) Injecting breast cancer cells suspension to the ventriculus sinistee can establish the bone metastasis model of breast cancer in a high successful rate. 3) Animal model of Yang deficiency is more likely to occur with bone metastasis.
Keywords: integrated traditional Chinese and western medicine; breast cancer; bone metastasis; Yang deficiency syndrome; nude mouse model

Title: Comparison of antioxidant activity of total flavonoids from three Rhodiola species

Authors: CUI Jinlong, GUO Tingting, WANG Mengliang
PP: 1802-1808
Abstract: The total flavonoids from 3 major species of Rhodiola rosea in China were extracted. The scavenging rates of DPPH, •OH- , O2-•, NO2 free radicals, chelating of Fe2+, and total antioxidant capacity were adopted to evaluate the total flavonoids of three Rhodiola plants in vitro. The results show that the content of flovonoids in R. crenulata was higher than R. bupleuroides and R. angusta, and the scavenging effect of Fe2+ chelating, O2-• scavenging, and total antioxidant capacity of R. crenulata were also higher than the others. The scavenging effects of DPPH, •OH- and nitrite of R. bupleuroides were the strongest.
Keywords: science of Chinese medicinal material resources; Rhodiola rosea; total flavonoids; antioxidant; free radical

Title: A comparative study on technology and technological parameter optimization of polysaccharide in the peach blossom separately extracted by ultrasonic and warm immersion methods

Authors: LIANG Yongfeng, WANG Xiaojuan
PP: 1795-1801
Abstract: Taking the extraction rate of polysaccharide as index, we make a study on technology of polysaccharides in the peach blossom separately extracted by ultrasonic-assisted and warm immersion methods. At the same time, we optimize the technological parameters. Results show that ultrasonic- assisted extraction rate is better than warm immersion method. Optimum parameters of ultrasonic-assisted extraction is that the ratio of material and liquid (mass: volume) is 1: 20, ultrasonic irradiation time is 60 min, ultrasonic radiation power is 100 W, and the soaking time is 90 min. Optimum parameters of warm immersion extraction method is that the extraction temperature is 75℃, the ratio of material and liquid is 1: 20, and extraction time is 120 min.
Keywords: pharmaceutical chemistry; technology optimization; ultrasonic method; plant polysaccharide; peach blossom

Title: Optimization of extraction process for polyphenols from Ligularia jaluensis by response surface methodology

Authors: ZHAO Yan, PENG Lei, GUO Shijie, CAI Enbo, LIU Shuangli, YANG He, ZHANG Lianxue
PP: 1787-1794
Abstract: Objective: To study the best extraction technique conditions of polyphenols from Ligularia jaluensis. Methods: Using the combination of ridge regression and response surface analysis method, taking L. jaluensis as materials, the interaction effects of the ethanol concentration, ultrasonic time and liquid-solid ratio on total polyphenols extraction yield were studied. Results: The results show that the optimal levels of liquid-to-material ratio, extaction time and ethanol concentration were determined to be 228.3 mL/g, 26.7 min and 41.6% (volume ratio). Under these conditions, the extraction yield of total polyphenols is 4.48% (mass ratio). Conclusion: The research process model is suitable for polyphenols extraction from L. jaluensis, which can be used in practical production.
Keywords: pharmaceutical chemistry; Ligularia jaluensis; polyphenol; extraction technique; response surface analysis; ridge regression

Title: Study on HPCE fingerprint of traditional Scorpio

Authors: LI Feng, XU Jing, ZHANG Zhenqiu
PP: 1781-1786
Abstract: Objective: The high performance capillary electrophoresis (HPCE) method fingerprint of traditongal Scorpio was established, in order to provide methods to species identification and quality evaluation. Methods: The HPCE fingerprint of traditongal Scorpio were obtained, with 40 mmol·L-1 borate and 0.2 mol·L-1 boric acid (pH=8.2) as HPCE buffer, temperature was 25℃, isolating voltage was on 20 kV, and the wavelength was at 214 nm, the press was 3 kPa and the time was 5 s. Results: The mutual mode of HPCE fingerprints is set up. The similarities of HPCE fingerprints from different commodity Scorpio were compared. Conclusion: The method is stable, repeatable and reliable, which provides references to evaluation quality of traditional Scorpio.
Keywords: science of Chinese pharmacology; fingerprint; high performance capillary electrophoresis; Scorpio

Title: Influence of peptide extracts from scorpion venom on P210 and JAK1 expression in chronic myelocytic leukemia mice

Authors: HAO Zheng, YANG Wenhua
PP: 1776-1780
Abstract: Objective: To investigate the peptide extract from scorpion venom (PESV) producing effects on P210, JAK1 expression in chronic myelocytic leukemia (CML)-NOD/SCID mice. Methods：K562 cells were injected into NOD/SCID mice, and the mice were irradiated on body by 137-Cs beforehand in order to establish the animal model of CML-NOD/SCID mice. Then, we randomly divided the mice of model establishment into several groups, and we used Western blotting method to examine P210 expression in mice, and simultaneously used ELISA method to examine JAK1 expression. Results: PESV could suppress P210 expression and inhibit JAK1 expression, the inhibiting effect depends on PESV concentration. Conclusion: PESV can inhibit CML cell transmutation by influencing the expression of P210 and JAK1, which reveals the microscopic mechanism on PESV inhibiting CML transmutation.
Keywords: internal medicine of traditional Chinese medicine; peptide extract from scorpion venom; chronic myelocytic leukemia; P210; JAK1

Title: Effect of tonifying kidney yang on serum melatonin and bone metabolism in ovariectomized rat

Authors: LI Yue, HOU Xueqin, JIANG Ziwei, YANG Bing, CHEN Peng, HUANG Feng
PP: 1769-1775
Abstract: Objective: To observe the effect of tonifying kidney yang on serum melatonin (MT), bone alkaline phosphotase (B-ALP), procollagen typeⅠ amino-terminal propeptide (PINP), N-telopeptide of typeⅠcollagen (NTX) and C-telopeptide of typeⅠcollagen (CTX) in ovariectomized (OVX) rat, explore possible mechanism of its efficacy on postmenopausal osteoporosis. Methods: 24 SD rats were divided into three groups, sham operation group, OVX group and tonifying kidney yang group. Three months after the operation, rats in tonifying kidney yang group were given intragastric administration with Guifudihuang pill by 0.92 g/(kg·d), and rats in the rest two groups were given intragastric administration with saline. Three months after medicine intervention, bone mineral density (BMD) of right femur was detected with dual-energy X-ray absorptiometry (DXA), the bone morphology of left femur was observed with HE staining, serum levels of B-ALP, PINP, NTX and CTX were detected with ELISA, and serum level of melatonin were detected with high performance liquid chromatography (HPLC). Results: Tonifying kidney yang can significantly increase BMD, ameliorate bone microstructure, decrease serum levels of B-ALP, PINP, NTX and CTX, and improve serum level of MT. Conclusion: Tonifying kidney yang has efficacy to treat OVX-induced osteoporosis in rat, reducing bone turnover rate and improving serum level of MT might be the mechanism.
Keywords: traditional Chinese medicine; tonifying kidney yang; osteoporosis; melatonin; bone metabolism

Title: Bibliometric analysis of the literatures on diabetes mellitus treated from liver

Authors: HU Jiahui, XIE Qingyu, MENG Qinggang
PP: 1761-1768
Abstract: Taking CNKI, Wanfang data and VIP database as retrieval source, this paper searched the relevant literatures on diabetes mellitus treated from liver using bibliometrics method. With the reference management software NoteExpress, we analyzed those literatures statistically, which were in accordance with the inclusive criteria in terms of the temporal distribution, journals distribution, author distribution, author’s unit distribution and provinces, type distribution and high-frequency key words. We investigated the current situation, hot spots and the trend of diabetes mellitus treated from liver. In addition, we focused on the hot spot issue based on the retrieved keywords, providing a reference and direction for clinical doctors and researchers. The results showed that, as a treatment method, diabetic mellitus from liver is not widely used in clinic. The relevant clinical researches are mostly observational literatures, for example, case series, and randomized controlled trials are not very common. Furthermore, we inferred that it played a strong supporting role using bibliometrics analysis method to study the medical literatures.
Keywords: basic theories of traditional Chinese medicine; diabetes mellitus treated from liver; bibliometrics analysis; high-frequency key words

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