Table of Content

31 May 2018, Volume 27 Issue 5

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Original articles

Synthesis and biological evaluation of α,β-unsaturated carbonyl compounds targeting the NLRP3 inflammasome

Qiuyun Kong, Nan Hang, Chao Zhang, Shuchun Li, Zhongjun Li, Yang Sun, Xiangbao Meng

2018, 27(5):  295-306.  DOI: 10.5246/jcps.2018.05.031

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A series of α,β-unsaturated ketone derivatives were synthesized, and their anti-inflammatory activity toward NLRP3 inflammasome was evaluated in vitro. Several compounds were identified as anti-inflammatory agents, among which compound A21 exhibited potent anti-inflammatory activity in a dose-dependent manner with an IC₅₀ of 0.95 μM. Moreover, a preliminary structure-activity relationship was also summarized.



Synthesis, characterization and biological applications of novel Schiff bases of 2-(trifluoromethoxy) aniline

Thierry Youmbi Fonkui, Monisola Itohan Ikhile, Freddy Munyololo Muganza, Marthe Carine Djuidje Fotsing, Charmaine Arderne, Xavier Siwe-Noundou

2018, 27(5):  307-323.  DOI: 10.5246/jcps.2018.05.032

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A series of five new Schiff bases (1–5) were synthesized by reacting 2-(trifluoromethoxy) aniline with different aromatic aldehydes. The Schiff base compounds were characterized by spectroscopic and analytical methods. Crystal structure of one new compound was also reported. The pharmacological properties, including antibacterial (14 bacterial species), antifungal (7 strains),antimalarial, anti-trypanosomal and anti-HIV activities of the compounds, were investigated. Cytotoxicity of the tested compounds was evaluated against human cervix adernocarcinoma cells (HeLa). Bacterial minimum inhibitory concentration (MIC) results by broth microdilution method showed that Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Proteus vulgaris, Klebsiella oxytoc and Klebsiella pneumonia were more sensitive in the presence of tested compounds with an MIC value of 15.6 µg/mL. All the tested compounds showed good to moderate activity against fungi. The sensitivity of Aspergillus fumigatus was higher than other strains with aminimum cell death concentration (MFC) of 15.6 µg/mL. Compound 1 showed greater antimalarial and anti-trypanosomal properties with very low to no cytotoxic effects against HeLa cells as compared with compound 5, while other compounds exhibited poor activity. Compounds 1–5 demonstrated good activity against HIV type-1. These Schiff base compounds could be used as good antimicrobial agents. 



Chemical constituents from Matricaria chamomilla L. (I)

Yifan Zhao, Dong Zhang, Caixia Liang, Lixin Yang, Peng Sun, Yue Ma, Kun Wang, Xiaoqiang Chang, Lan Yang

2018, 27(5):  324-331.  DOI: 10.5246/jcps.2018.05.033

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In the present study, we aimed to perform a phytochemical investigation of the whole herb of Matricaria chamomilla L., a Uygur herbal medicine. A total of 18 phenolic compounds were isolated by silica gel and Sephadex LH-20 chromatography, together with preparative HPLC methods. By analysis of the MS and NMR spectroscopic data and comparison with those in literature, these 18 compounds were identified as apigenin (1), galangin (2), luteolin (3), kempherol (4), quercetin (5), hispidulin (6), 6-methoxykaempferol (7), eupafolin (8), 3-methylquercetin (9), ermanin (10), 5,7,4′-trihydroxy-3,6-dimethoxyflavonone (11),bracteoside (12), 7-O-(β-D-glucopyranosyl)-galactin (13), isochlorogenic acid B (14), isochlorogenic acid C (15), 4-hydroxybenzoic acid (16), 5-pentadecylbenzene-1,3-diol (17) and scopoletin (18). Among them, compounds 1–13 were identified as flavonoids. Compounds 2 and 6–17 were isolated from both the plant and the Matricaria genus for the first time.



Preparation, characterization and evaluation of multi-component-loaded liposomes containing Tat-TOS, phospholipase D inhibitor and doxorubicin

Maoyuan Song, Yuanyuan Zhang, Wenxi Zhang, Guanghua Peng, Jiaxing Wang, Mengya Yin, Jiajia Li, Yajie Liu, Xinru Li

2018, 27(5):  332-341.  DOI: 10.5246/jcps.2018.05.034

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In the present study, we aimed to co-load the α-TOS conjugate Tat-TOS with the phospholipase D inhibitor FIPI and the antitumor drug doxorubicin (DOX) in a liposome delivery system for antitumor metastasis. Firstly, Tat-TOS was synthesized by solid-phase synthesis, and its structure was confirmed. The ability of free and liposomal Tat-TOS to induce apoptosis in vitro was evaluated by flow cytometry. Biodistribution of Tat-TOS-loaded liposomes was investigated by a molecular imaging system. Multi-component-loaded liposomes modified with Tat-TOS containing FIPI and DOX was prepared by thin film dispersion method in combination with pH gradient method and post-insertion method. Physicochemical properties were determined, and the in vitro uptake ability of the formulations was evaluated. The results showed that the prepared liposomes were characterized by a uniform particle size distribution and small particle size. The encapsulation efficiency of FIPI and DOX exceeded 85%. Both free and liposomal Tat-TOS significantly improved the activity of inducing apoptosis of tumor cells. The liposomes modified with Tat-TOS were apparently accumulated in normal lung tissue and tumor metastasized lung. Multi-component-loaded liposomes exhibited the strongest cell uptake capacity, suggesting a stronger anti-metastatic effect and anti-tumor activity in vivo.



Genistein-loaded poloxamer 403/407 mixed micelles: preparation and pharmacokinetic study in rats

Yan Cai, Wei Dai, Fuhua Qin, Jieyin Sun, Ruilong Wei

2018, 27(5):  342-351.  DOI: 10.5246/jcps.2018.05.035

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In the present study, we aimed to prepare poloxamer 403/407 mixed micelles in order to improve the solubility and oral bioavailability of genistein.Genistein was incorporated in the mixed poloxamer micelles by thin-film hydration method, and its physicochemical properties, including particle size, zeta potential, entrapment efficiency and drug loading, were investigated.In vitro release of genistein from the mixed micelles was monitored by dialysis method, and pharmacokinetic study of genistein loaded mixed micelles was carried out in rats. We found that the particle size and zeta potential of mixed micelles were (20.31±0.43) nm and (–8.94±0.35) mV, with encapsulation efficiency 90.59%±0.67% and drug loading 7.74%±0.05%. Solubility of genistein in mixed micelles reached 3.80 mg/mL, which was about 130 times higher than that in water.Genistein-loaded mixed micelles showed sustained release characteristics in vitro with no burst release phenomenon, but it was faster than suspension.The AUC_0–t andAUC_0–∞ of mixed micelles were 196.74% and 204.62% greater than that of genisein suspension, respectively.Consequently,poloxamer 403/407 mixed micelles significantly improved the solubility and oral bioavailability of genistein, which could be used as an effective drug delivery system for oral administration of poorly soluble drugs. 



Drug administration and clinical pharmacy column

New direction for clinical pharmacy in China: adopting a “form follows function” approach to improve future healthcare outcomes

Xiao Chen, Xiang Gao, Jie Chen, Sheryl L Chow, Moses S.S. Chow

2018, 27(5):  352-360.  DOI: 10.5246/jcps.2018.05.036

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Clinical pharmacy is an important development in modern pharmacy practice. In China, the recent recognition of clinicalpharmacists by the Ministry of Health is an important step that can lead to a successful change in the functional role of the pharmacists to directly improve the health care outcomes. To optimize this role change, we propose that a “form follows function” structure be implemented. We believe that a “form” consisting of three components is highly desirable and should be established with careful coordination: (1) a formal education/training curriculum; (2) a professional organization to lead the clinical improvements in practice/research; and (3) an accrediting body for quality education/training and practice. By incorporating the clinical pharmacy experiences in USA and other countries as well as adopting this “form follows function” approach, we predict a bright future for the clinical pharmacists in China as valuable members of health care team to positively impact the health care outcomes.



Medical service utilisation, economic burden and health status of patients with rare diseases in China

Mengyuan Fu, Xiaodong Guan, Guoxu Wei, Xiaoxiong Xin, Luwen Shi

2018, 27(5):  361-369.  DOI: 10.5246/jcps.2018.05.037

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Many patients with rare diseases not only suffer from more severe conditions but often receive less disease management,which is one significant public health concern globally. Few practice-based surveys focus on the care of patients with rare diseases. In the present study, we aimed to investigate medical service utilization, economic burden and health status of patients with rare diseases in China. A cross-sectional questionnaire survey focusing on patients with rare diseases was conducted. Descriptive analysis was conducted to examine the sociodemographic characteristics, medical service utilization, economic burden and health status. Logistic regression analysis was applied to explore influencing factors of self-rated health. A total of 982 patients with 81 types of diseases were included in this survey. We found that 58.2% of patients experienced misdiagnosis, and 35.2% of the patients were misdiagnosed for at least five times. Moreover, 65.8% of patients traveled to hospitals to seek medical services, and 92.1% of patients paid expenses for their treatment. However, only 1.3% of patients could afford their medical expenditure without debts, and 86.8% of patients regarded their health status as bad or moderate. Significant factors correlated with health status were economic status, gender, age, employment and household size. From this study, the accessibility of medical service utilization, the affordability of medical economic burden, and the condition of health status for patients with rare disease in China were considerably poor. Basic medical insurance did not play its role in improving the utilization of medical services and the affordability of medical costs. Social support should be encouraged to improve patients’ health status.



Other

Professor Ah-Ng Tony Kong visited Peking University School of Pharmaceutical Sciences and delivered a seminar on Epigenome Studies of Natural & TCM Products

Siwang Yu

2018, 27(5):  370-370. 

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