Herald of Medicine

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药物研究

The Mechanism of Killing Effects against Hepatoma Cell by Hydroxycamptothecine Combined with Doxorubicin

LV Xiao-hong;ZHANG Xiao-mei;ZHENG Jian-wei;WANG Cong-jun;XUE Xi-bo

2010, 29(7): 835-839. https://doi.org/10.3870/yydb.2010.07.001

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Objective To explore the mechanism of killing effects against hepatoma cell by hydroxycamptothecine (HCPT) combined with doxorubicin (ADM). Methods The growth difference between human hepatoma carcinoma cell(HepG2) and normal hepatic cell LO2 by 1.5 mg•L^-1ADM, 2 mg•L^-1HCPT and two drugs combination, respectively, was observed by MTT method. The expression of Eselectin, VEGF, MMP-9, Bcl-2, Bax were examined by realtime PCR and E-selectin and MMP-9 were detected by Westernblot as well. Results It was shown that the growth rates of HepG2 treated by 1.5 mg•L-1 ADM and 2 mg•L^-1 HCPT were 16.58% and 39.92%, respectively, while those treated by ADM (1 mg•L^-1)and HCPT（2 mg•L^-1） were 66.61%, ADM(1.5 mg•L^-1) and HCPT(2.0 mg•L^-1) were 74.47%. The expression of Eselectin mRNA was increased from （52.13±0.58）in ADM group to（93.41±8.43）in drug combined group. The expression of MMP-9 and VEGF mRNA was decreased from（26.49±0.11）in ADM to （6.48±0.05）in drug combination. The change of Bcl-2 and Bax were statistically significant in the experiment groups（P< 0.05）. Conclusion HCPT arrest the growth of HepG2 more effectively than ADM. While, HCPT combined with ADM kill more hepatoma cells than HCPT or ADM alone. Combined use of ADM and HCPT could reduce the dose and cytotoxicity of the single drug.

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药物研究

Effects of Pregnancy Estrogen and Progesterone on the Regulatory T Cells in Mice

LIN Xing-guang;WANG Li;GAO Ying;ZHANG Wei-na;LUO Zhen-long;CHEN Zhong-hua;CHANG Sheng

2010, 29(7): 839-843. https://doi.org/10.3870/yydb.2010.07.002

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Objective To investigate whether the estrogen(E₂), progesterone(P₄) within the physiological concentration range of the early pregnancy could affect the expansion of CD⁺₄CD⁺₂₅Foxp3⁺ regulatory T cells. Methods We administrated pregnancy E₂/P₄or saline in the ovariectomized and orchiectomized mice. After reconstituting the sex hormone to the physiological concentration range of the early pregnancy for two weeks, the mice were sacrificed, and lymphocytes were isolated from thymus, spleen, iliac lymph nodes and peripheral blood. The CD⁺₄CD⁺₂₅Foxp3⁺regulatory T cells were detected by flow cytometry and immunohistochemistry. Results The groups received E₂ alone showed a notable increase in the proportion of the Tregs that marked CD⁺₄CD⁺₂₅ Foxp3⁺ in spleen, iliac lymph nodes and blood. CD⁺₄CD⁺₂₅ Foxp3⁺cells constituted (8.56±1.85)% of all CD⁺₄ cells in spleen, (7.63±1.68)% in iliac lymph nodes and (6.13±1.32)% in blood, While the proportion in the thymus could not be enhanced compared to the vehicle groups. The P4 administration could improve the proportion of Tregs lightly, but without statistical significance During the group combine with E2 and P4, each tissue samples showed a same trend in the increase of Tregs with E2 alone. Furthermore, no difference was found in the change of Tregs between the ovariectomized and orchiectomized mice. The similar Results could be found in immunohistochemistry. Conclusion in vivo, E2 could drive the expansion of the Tregs in the secondary lymphoid organs and peripheral blood, but not P4. Neither of them could improve the proportion of Tregs in thymus. No gender difference could be found in the effect, which might be involved in the same distribution of hormone corelative receptors. Conclusion In vivo, E2 can drive the expansion of the Tregs in the secondary lymphoid organs and peripheral blood, but not P4. Neither of them can improve the proportion of Tregs in thymus. No gender difference could be found in the effect, which may involve in the same distribution of hormone corelative receptors.

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药物研究

Content Determination and Tissue Distribution of S-allylcysteine in Rats

YAN Jing-ting;HU Xia-min;ZENG Fan-dian

2010, 29(7): 847-850. https://doi.org/10.3870/yydb.2010.07.004

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Objective To establish the high perfromance liquid chromatography for determining serum and tissue concentrations of S-allylcysteine (SAC) and tissue distribution in rats. Methods A stainless steel Hypersil ODS2 analytical column was used. Separation was carried out with 50 mmol•L^-1 acetate buffer (pH 5.8 )methanol acetonitrile (50：22：28) at 35 ℃. Sallylcysteine was measured fluorimetrically at excitation and emission wavelengths of 350 and 455 nm, respectively. Biological samples were pretreated with methanol extraction and then fluorescent derivatives with ophthalaldehyde(OPA) in an alkaline medium. Results Linear response between the peak height and concentration of Sallylcysteine was obtained over the concentration range 2-120 mg•L^-1 (mg•kg^-1 for tissue). The mean value of intraday precision, expressed as percent relative standard deviation (RSD) was 4.1%-6.2%; the mean value of interday precision, expressed as RSD was 6.2%-7.7%. The recovery of extraction procedures for serum and tissue samples was more than 70%. Among the selected tissues, the kidney presented the highest peak concentration (Cmax of 65.7 mg•kg-1) following the iv single dose as 50 mg•kg^-1, followed by the liver (Cmax of 58.1 mg•kg^-1 ), spleen(Cmax of 51.3 mg•kg-¹), heart(Cmax of 43.3 mg•kg^-1), lung (C_max of 35.1 mg•kg^-1), and finally brain (Cmax of 26.7 mg•kg^-1). The kidney also had the highest AUC0-8(171.9 mg•h•kg^-1), followed by heart(113.9 mg•h•kg^-1), liver(107.2 mg•h•kg^-1), lung(93.6 mg•h•kg^-1), spleen(90.4 mg•h•kg^-1) and brain(79.8 mg•h•kg^-1). Conclusion The method is accurate, sensitive, specific and rapid. SAC is more distributed in kidney than in brain of the rat.

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中药及天然药物专栏

Fingerprints of Artemisia rupestris L.from Xinjiang by HPLC

HE Fei;HOU Gui-ping;ZHONG Jie;ABULIMITI&#;Yi-li;HAJI AKBER&#;Aisa

2010, 29(7): 854-857. https://doi.org/10.3870/yydb.2010.07.007

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Objective To study the HPLC fingerprints and establish a sensitive and specific method for controlling the quality of Artemisia rupestris L. from xinjiang. Methods The sample was separated on an Inertsil ODS-3 column(4.6 mm×250 mm, 5 μm) with the mobile phase consisting methanol0.2% methyl acid by gradient elution; with flow rate at 1.0 mL•min^-1,wavelength at 245 nm and the temperature at 32 ℃. Results The chemical constituents of Artemisia rupestris L. were optimally separated, among which 14 fingerprint peaks in common were confirmed. Conclusion This method is simple, accurate and with good reproducibility, which can be used specifically for the quality control of Artemisia rupestris L.from xinjiang.

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中药及天然药物专栏

Anti-aging Effects of Skin Care Emulsion Mixed with Chinese Herbal Extracts

GAO Rui-ying;ZHANG Xiu-yu;MU Dan;FU Zhong

2010, 29(7): 857-860. https://doi.org/10.3870/yydb.2010.07.008

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Objective To study the antiaging effects of skin care emulsion mixed with five kinds of Chinese herbal extracts (CHE). Methods Sixty female mice of 12 months were randomly divided into 3 groups (n＝20): normal aging control group(N), low dose(L) and high dose(H) of CHE groups. Twenty other female mice of 3 months were used as young control groups (Y group). Skin care emulsion with 4% CHE was besmeared on the skin of mice in L group, that with 16% CHE was besmeared on H group, and cosmetic matrix without CHE was besmeared on N and Y groups for 60 d. The dorsal skin samples were collected to determine the contents of hydroxyproline (HYP), superoxide dismutase (SOD), malondialdehyde (MDA) and lipofuscin (LF). Results The SOD activity of natural aging group (N group) decreased more significantly, and the contents of MDA and LF increased obviously than those in the Y group, which showed that the natural aging model was successfully set up. The content of HYP in L and H groups reached to (30.85±3.71 ) and (35.46±3.54) mg•g^-1, SOD were(17.92±0.58) and (20.38±0.71) U•mL^-1, MDA were (6.92±1.38) and (5.96±1.25) mmol•g^-1, LF were (6.13±1.73) and (4.89±1.15) μg•g^-1 ,respectively, which were significantly different from those of the control group (P<0.05). Conclusion The skin care emulsion with five CHE including angelicae sinensis has a noticeable antiskin aging effect.

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中药及天然药物专栏

Pharmacological Screening of Antihypertensive Active Sites of Ephedrae Root

YANG Yan-fang;LU Yi;WU Gao-feng;LI Li-zhan;WU He-zhen

2010, 29(7): 860-862. https://doi.org/10.3870/yydb.2010.07.009

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Objective To screen the antihypertensive active sites of Ephedra root. Methods The spontaneously hypertensive rats (SHR) were divided into 7 groups at random: blank control, positive control (luobuma composed tablets), ethanol extracted,petroleum ether extracted, acetic ether extracted,nbutanol extracted and water extracted groups.The data of systolic pressure and diastolic pressure were recorded after the rats were treated by intragastric administration. Results The blood pressures of the acetic ether extracted and ,n-butanol extracted groups were significant different compared with the blank control one. Their diastolic pressures but not systolic pressures were not significant different from the positive control group. The effects on diastolic pressure by acetic ether extraction and nbutanol extraction were equated to that of the positive drug, while their effects on systolic pressure were not as good as the positive one. No statistical difference was found between these two groups. Conclusion The acetic ether extracts and nbutanol extracts are both antihypertensive active sites of Ephedra root.

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中药及天然药物专栏

Antioxidation of Seven Species of Water Extracts of Chinese Herbs In Vitro

GONG Yan-ling;JIN Hong;XUAN Guang-shan

2010, 29(7): 863-865. https://doi.org/10.3870/yydb.2010.07.010

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Objective To explore the antioxidation of seven species of Chinese herbs and their doseeffect relationship. Methods The liver microsomal lipid peroxidation model in mice was established by induction of Vit C/Fe2+. The contents of malondialdehyde (MDA) were examined to evaluate the protective effects by Fructus lycii, Epimedium, Sedum sarmentosum Bunge, Scutellaria, Giant knotweed rhizome, Forsythia suspensa and Pueraria. Results The Results showed that the seven water extracts had antioxidative effects in different degrees, in which Fructus lycii, Epimedium sagittatum and Sedum sarmentosum showed the most significant effects. Fructus lycii also displayed a good doseeffect relationship. Scuytellaria baicalenksis and Polygonum cuspidaum had the moderate antioxidative effects and the former also showed a certain degree of doseeffect relationship. The effects of Fructus forsthiae and Radix puerariae were relatively weaker. Conclusion These Results will provide basis for development of antioxidative functional food.

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药物与临床

Efficacy and Safety of Caspofungin Followed by Itraconazole Oral Solution for Patients with Invasive Fungal Infection

ZHANG Chi;WAN De-ning;ZHANG Sheng;WANG Yan-lin;LUO Hua;ZHANG Wei-xing

2010, 29(7): 875-878. https://doi.org/10.3870/yydb.2010.07.014

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Objective To evaluate the efficacy and safety of caspofungin and itraconazole on treating invasive fungal infection(IFI) in intensive care unit(ICU). Methods 42 patients with IFI were divided into two groups by different treatment: 24 patients in the treatment group were i.v. injected with caspofungin 70 mg•d^-1 at day 1 and 50 mg•d^-1 in N.S. later on, over 1 h, with itraconazole oral solution instead 2-4 weeks later; 18 in control group were i.v. treated with caspofungin 70 mg•d^-1for the first day, and 50 mg•d^-1 since then till the end. The therapeutic effect and side effects in two groups were observed. Results 5 patients in the treatment group were cured, 10 showed effective,3 were advanced, 6 were invalid, and 2 cases of side effects occured; 5 were cured in the control group, 7 showed effective ,2 were advanced, 4 were invalid, 3 cases of side effects were observed.Conclusion The both regimes are effective for IFI, i.v. caspofungin followed with itraconazole is effect and safe, with fewer side reactions.

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药物制剂

Preparation and Quality Control of Magnesium Valproate Suppository

CHEN Qian;LIU Dong

2010, 29(7): 915-918. https://doi.org/10.3870/yydb.2010.07.028

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Objective To study the formulation, technology and quality control of magnesium valproate suppository. Methods Orthogonal test was used to optimize the formulation and technology of magnesium valproate suppository. The dissolution rate was determined with potentiometric titration.Influence of different concentration of princible drug on dissolution was investigated. Results The best matrix was glycerogelatin (glycerine：gelatine：water＝6：2：2), and each granule contained 200 mg of magnesium valproate.The accumulative dissolution rate was 91%. The average recovery was 99.93%, and RSD was 1.88%(n=9).Conclusion The preparation technique is simple and praticable, and its quality is controllable.

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药物制剂

Extraction Technology of Honokiols from Magnolia officinalis Rehd.et Wils. in Qianbeis

FENG Hua;SHEN Gui-xia;ZOU Kong-qiang

2010, 29(7): 918-919. https://doi.org/10.3870/yydb.2010.07.029

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Objective To study the extaction technology of honokiols from Magnolia officinalis. Methods The orthogonal test was used to optimize the extracting conditions based on refluxing time, amount of methanol added, methanol concenration and the content of honokiol trihydrate. Results Refluxing for 30 min and adding 25 mL pure methanol were the best extaction procdures. Conclusion The optimized technology is practical and can be used for formulating the extaction technology of magnolols.

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药物制剂

Preparation of TanshinoneⅡA Self-emulsifying Micro-pill by Spray Drying Method

YANG Jing;HAN Jing;SUN Ming;ZHANG Yue;ZHANG Duo-ting;XIANG Wen-juan

2010, 29(7): 920-922. https://doi.org/10.3870/yydb.2010.07.030

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Objective To prepare self-emulsifying micro-pills by using the spray drying method. Methods The encapsulation efficiency was considered to evaluate the influence of different formulation and preparation factors. The formulation was optimized by L9（34） orthogonal design to improve stability and oral bioavailability of tanshinoneⅡA. Results The optimum processing conditions were as follows: inletair temperature at 115 ℃, air flow rate at 500 L•h^-1, PVP(aq) concentration as 0.01 g•mL^-1, ratio of PVP to tanshinoneⅡA as 1：6. Conclusion The preparation of the self-micro emulsified tanshinoneⅡA is easy, stable and with remarkable solubility. The method of spray drying is feasible for the preparation of tanshinoneⅡA self-emulsifying micro-pill.

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药物制剂

Preparation and Identification of Artificial Antigen of Estrone

GONG Yue-hong;FENG Xiao-hui;GAO Xiao-li;QI Xin-wei;ZHANG Jing-ping;WEN Hao

2010, 29(7): 923-925. https://doi.org/10.3870/yydb.2010.07.031

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Objective To prepare artificial antigen of estrone. Methods Esterone as a hapten was linked with bovine serum albumin to prepare the immune conjugates by carbodimide method, and rate of linking was detected with UV spectrophtometer to determine the serum antibody effective value. Results The coupling ratio was tested as 12：1 and the rabbits serum antibody effective value was determined as 6.4×103. Conclusion The method is simple, accurate and reliable, which could be applied for the preparation of artificial antigen of estrone.

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药物制剂

Extraction Technics of Total Coumarins from the Leaf of Fraxinus Hupehensis

MA Li;YAN Hui-juan;QU Jia-jia;ZHANG Yu

2010, 29(7): 925-928. https://doi.org/10.3870/yydb.2010.07.032

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Objective To optimize the extraction of total coumarins from Fraxinus hupehensis. Methods The extraction method was optimized by orthogonal design L9(34) according to the content of aesculin.The extracting times, decocting time, temperature, and concentration of ethanol were evaluated. Results The optimum conditions were A1B2C1D3 as following：extracting three times at 80 ℃, each time for 1 h with 60% ethanol.Conclusion The extracting technics optimized by orthogonal design could obtain total coumarins and fit for the extraction of them from Fraxinus hupehensis.

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药物制剂

Preparation of Volatile Oilβ-Cyclodextrin Inclusion in Yinqiao Jiedu Granule

HUANG Tao-yang;WANG Hui

2010, 29(7): 928-931. https://doi.org/10.3870/yydb.2010.07.033

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Objective To study the optimum preparation technology for volatile oilβ-cyclodextrin inclusion in yinqiao jiedu granule. Methods The study was carried out by orthogonal design, taking the rate of inclusion and recovery as the appraisement criteria, to optimize the preparation technology. Results The optimum preparation technology were as follows: volatile oil: β-cyclodextrin being 1：8, inclusion temperature at 60 ℃, mixing time as 2 h, β-cyclodextrin and water ratio as 1：10. Conclusion The method can be used for preparation of volatile oilβ-cyclodextrin inclusion in yinqiao jiedu granule, in which the stability of the volatile oil can be enhanced.

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药物与临床

The Preparation and Quality Control of Celecoxib Gel

HUANG Liang-yong;ZHENG Jiang-ping;YAN Wen-qiang

2010, 29(7): 931-933. https://doi.org/10.3870/yydb.2010.07.034

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Objective To prepare celecoxib gel and to establish the method for its quality control. Methods The celecoxib gel for external use was prepared by using carbopol 940 as the base, laurocapram and oleic acid as skin penetration enhancer and DMSO as solvent for celecoxib and the drug content was determined by HPLC. Results The preparation was stabililty and without irritation. Celecoxib can be completely separated with a linear range of 2.12-212.00 μg•mL^-1 and correlation coefficients of r=0.999 9. The average recovery was 100.29% with a RSD of 0.55 %. Conclusion The preparation technique is simple and feasible for the quality control.

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药品质量控制

Determination of Metronidazole and Chloramphenicol in Lvxiaozuo Tincture by Double Wavelength Spectrophotometry

SHI Chun-yang;MIN Min;WANG Wen-qing;LI Jian

2010, 29(7): 936-938. https://doi.org/10.3870/yydb.2010.07.036

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Objective To develop the double-wavelength spectrophotometry for determination of metronidazole and chloramphenicol in lvxiaozuo tincture. Methods A double-wavelength spectrophotometry was used to directly determine the concentration of metronidazole and chloramphenicol in lvxiaozuo tincture with diluted alcohol as solvent. The detective wavelength of chloramphenicol was 277 nm, the reference wavelength of which was 352 nm; that of metronidazole was 309 nm, and the reference wavelength of which was 243 nm. Results The linear concentration range of metronidazole was 4.5-45.0 μg•mL-1 (r=0.999 0), the average recovery was 99.7% with the RSD=0.72%; The linear concentration range of chloramphenicol was 4.6-23.2 μg•mL-1 (r=0.999 2), the average recovery was 98.7% with the RSD=1.36%. Conclusion The method developed is simple, accurate, which can be applied for the determination of metronidazole and chloramphenicol in lvxiaozuo tincture directly.

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