1.Development in New Dosage Forms of Active Components from Ginkgo Biloba Extracts
Xiaolei SHI ; Yuan ZHU ; Jiangnan YU ; Ximing XU
China Pharmacist 2014;(11):1943-1946
The main active components in Ginkgo biloba extracts were Ginkgo biloba flavonoids and lactone compounds. This pa-per reviewed on the kinds and pharmacological effects of the active ingredients in Ginkgo biloba extracts, and focused on four aspects including controlled-release preparations, solubilized solid preparations, nanoparticle formulations and time- and site-specific formula-tions to introduce the development in the new dosage forms of Ginkgo biloba flavonoids and lactone compounds.
2.Research Progress in the Pharmacological Mechanism of Active Ingredients in Semen Ziziphi Spinosae
Yangyang YUAN ; Congyong SUN ; Ximing XU ; Jiangnan YU
China Pharmacist 2017;20(9):1622-1627
Semen Ziziphi spinosae ( SZS) , as a commonly used traditional Chinese medicine in clinic for insomnia therapy, is rich in pharmacological active ingredients such as saponins, flavonoids, alkaloids, oil and the other chemical compounds. The recent stud-ies indicated that some active ingredients in SZS exhibited a variety of activities including sedative hypnotics, antianxiety and anti-de-pression by regulating particular neurotransmitters such as 5-hydroxytryptamine (5-HT), gamma-amino butyric acid (GABA), norepi-nephrine, dopamine and glutamate. In accordance with the previous studies on pharmacological activities of SZS, this paper summa-rized and reviewed the applications of SZS in the treatment of central nervous system diseases, myocardial diseases and hepatic disea-ses, which might provide solid evidence for the application development of SZS.
3.The expression and significance of IFN-γR and sIL-2R in plasma of patients with recurrent oral ulcer
Xiaozhe MA ; Yanjun LI ; Aili FU ; Jiangnan XUE ; Ping YU
Journal of Practical Stomatology 2015;(5):656-659
Objective:To examine the plasma soluble interleukin 2 receptor (sIL-2R)and the expression of IFN-γR in helper T (Th)cells in peripheral blood of patients with recurrent oral ulcer(ROU).Methods:The peripheral blood was obtained from 21 pa-tients in active stage of ROU and 21 healthy controls.Flow cytometry was used to detect the quantity of IFN-γR in CD +4 T cells,ELISA was used to detect the level of sIL-2R.Results:The expression of IFN-γR in CD +4 T cells and sIL-2R content in plasma of the patients with ROU were significantly higher than those in the healthy controls(P <0.05).Conclusion:Over expression of IFN-γR in CD +4 T cells and sIL-2R in peripheral blood may be related to the genesis of ROU.
4.Correlation between the uncertainty in illnessand social support in elderly patients with prediabetes
Jiangnan ZHAO ; Wei ZHENG ; Meng SUN ; Fang YU ; Lixia ZHANG
Chinese Journal of Geriatrics 2014;33(9):965-968
Objective To investigate the level of uncertainty of illness and social support state in patients with prediabetes,and to discuss the correlation between the two.Methods 243 cases with prediabetes were analyzed by Uncertainty in Illness Scale and Social Support Rating Scale.Results There was a middle uncertainty in the elderly patients with prediabetes.The objective support,sabjective support,social support utilization degree and social support score were negatively related to the complexity of uncertainty(r--0.419,-0.433,-0.390 and-0.421,respectively,all P< 0.05).Conclusions Medical staff should evaluate the uncertainty in illness in elderly patients with prediabetes and conduct nursing intervention accordingly,in order to reduce the uncertainty,increase social support,and ultimately improve the quality of life.
5.Research Progress in Spice Composition-loaded Sustained and Controlled Release Preparations
Shengli WANG ; Yuan ZHU ; Jiangnan YU ; Ximing XU
China Pharmacist 2015;(8):1372-1375
The spices, with a wide range of remarkable pharmacological effects, were limited in developing clinical drugs because of their poor solubility, high irritation and low bioavailability. Controlled release preparations can delay the release of drugs on the basis of solubility enhancement to improve bioavailability. The research on spice ingredient-loaded controlled release preparations was sum-marized in the paper for the further development of spice active ingredients.
6. Analysis of metabolites of doxorubicin in breast cancer cell line MCF-7
Yu-Jiao CHEN ; Ren-Jie HUI ; Xu WANG ; Jing-Yu ZHU ; Lei JIA ; Jian JIN ; Yun CHEN
Chinese Pharmacological Bulletin 2021;37(9):1271-1277
Aim To investigate the intracellular disposition process of doxorubicin (DOX) in human breast cancer MCF-7, providing reference for explaining the pharmacology and their side effects of anti-tumor drugs. Methods The drug-resistant cell line MCF-7/DOX of breast cancer with DOX indication was selected as the material, and ultra-high performance liquid chromatography quadrupole tandem time-of-flight high-resolution mass spectrometry (UPLC-Q-TOF-MS/MS) method was established to analyze the disposal of DOX by target cells. Results Two unreported trace a-mounts of new metabolites of doxorubicin were found, and their structures were deduced by high-resolution multistage mass spectrometry. Molecular docking showed that its affinity for DNA was lower than that of DOX. Conclusion Target cells have unique and diverse drug metabolism pathways for DOX, which may be related to drug resistance mechanisms.
7. Effect of Vaccarin on atherosclerosis in mouse model and its mechanism
Xin-Yu MA ; Fei XU ; Lei-Lei GONG ; Rui-Tang CHENG ; Sun-Han MIAO ; Yu-Wei ZHU ; Wei-Wei CAI ; Bao HOU ; Li-Ying QIU
Chinese Pharmacological Bulletin 2021;37(11):1518-1523
Aim To investigate the effect of vaccarin on mouse atherosclerosis in vivo and the underlying mechanism. Methods AopE mice aged 6 to 8 weeks old were used to establish the atherosclerosis model. Oil red O staining was used to determine the lipid levels in aorta and aortic root. Enzyme linked immunosorbent assay (ELISA) was used to detect the levels of serum inflammatory factors. Results Vaccarin could effectively reduce the levels of blood glucose and blood pressure in AopE
8.Characterization of a sucrose phosphorylase from Leuconostoc mesenterides for the synthesis of α-arbutin.
Xiaoyu LI ; Yuanyuan XIA ; Wei SHEN ; Haiquan YANG ; Yu CAO ; Xianzhong CHEN
Chinese Journal of Biotechnology 2020;36(8):1546-1555
Sucrose phosphorylase (SPase) gene from Leuconostoc mesenteroides ATCC 12291 was synthesised after codon optimization, and inserted into pET-28a plasmid to generate pET-28a-spase. The recombinant strain Escherichia coli BL21 (DE3)/pET-28a-spase was induced for Spase expression. The recombinant protein Spase was purified and characterized. The specific enzyme activity of SPase was 213.98 U/mg, the purification ratio was 1.47-fold, and the enzyme activity recovery rate was 87.80%. The optimal temperature and the optimal pH of the SPase were identified to be 45 °C and 6.5 respectively, and Km, Vmax and kcat of the SPase for sucrose was 128.8 mmol/L, 2.167 μmol/(mL·min), and 39 237.86 min-1. The recombinant SPase was used for α-arbutin production from hydroquinone and the reaction process was evaluated. The optimal conditions for synthesis of α-arbutin by SPase were 40 g/L hydroquinone, 5:1 molar ratio of sucrose and hydroquinone, and 250 U/mL recombinant SPase at pH 7.0 and 30 °C for 24 h in the dark, and then 500 U/mL glucoamylase was added at 40°C for 2.5 h. Under the optimized process, the yield of α-arbutin reached 98 g/L, and the hydroquinone conversion rate was close to 99%. In summary, the recombinant SPase was cloned and characterized, and its application for α-arbutin production was feasible.
9.Production of limonene and its derivative in Saccharomyces cerevisiae via metabolic engineering.
Yao HUANG ; Haiquan YANG ; Wei SHEN ; Yuanyuan XIA ; Yu CAO ; Xianzhong CHEN
Chinese Journal of Biotechnology 2023;39(11):4647-4662
Limonene and its derivative perillic acid are widely used in food, cosmetics, health products, medicine and other industries as important bioactive natural products. However, inefficient plant extraction and high energy-consuming chemical synthesis hamper the industrial production of limonene and perillic acid. In this study, limonene synthase from Mentha spicata was expressed in Saccharomyces cerevisiae by peroxisome compartmentalization, and the yield of limonene was 0.038 mg/L. The genes involved in limonene synthesis, ERG10, ERG13, tHMGR, ERG12, ERG8, IDI1, MVD1, ERG20ww and tLS, were step-wise expressed via modular engineering to study their effects on limonene yield. The yield of limonene increased to 1.14 mg/L by increasing the precursor module. Using the plasmid with high copy number to express the above key genes, the yield of limonene significantly increased up to 86.74 mg/L, which was 4 337 times higher than that of the original strain. Using the limonene-producing strain as the starting strain, the production of perillic acid was successfully achieved by expressing cytochrome P450 enzyme gene from Salvia miltiorrhiza, and the yield reached 4.42 mg/L. The results may facilitate the construction of cell factory with high yield of monoterpene products by S. cerevisiae.
Saccharomyces cerevisiae/metabolism*
;
Limonene/metabolism*
;
Metabolic Engineering
;
Monoterpenes/metabolism*
10.Biocatalytic access to β-alanine by a two-enzyme cascade synthesis.
Yu GAO ; Zhongmei LIU ; Ke LIU ; Zhemin ZHOU ; Wenjing CUI
Chinese Journal of Biotechnology 2017;33(5):875-879
Enzymatic synthesis is an important way to produce β-alanine, but the biological method is expensive generally because of the high price of substrate. In this paper, a two-step enzymatic cascade system was developed, combining L-aspartase from Escherichia coli DH5α and L-aspartate α-decarboxylase from Corynebacterium glutamicum. This system catalyzes Fumarate and ammonia to β-alanine. The optimal ratio of AspA and PanD was 1:80 (W/W), and the concentration of AspA was 10 μg/mL, at 37 ℃ and pH 7.0. When the concentration of Fumarate was 100 mmol/L, the reaction reached its equilibrium after 8 h, and the yield of β-alanine was 90 mmol/L (7 g/L). The yield of β-alanine can reach 126 mmol/L (9.8 g/L) when the concentration of Fumarate increased to 200 mmol/L. Extending reaction time, the conversion rate did not change obviously. Using this two-step enzymatic cascade system, β-alanine from cheaper substrate Fumarate can be obtained.