Journal of Chinese Pharmaceutical Sciences

Chemical constituents of the aerial parts of Glycyrrhiza uralensis and their inhibitory activities against PTP1B and α-glucosidase

Jingran Fan, Zeyuan Dong, Yi Kuang, Yanxia Zhou, Xue Qiao, Min Ye

2020, 29(5): 305-313. DOI: 10.5246/jcps.2020.05.028

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In the present study, a total of 11 compounds were isolated from the aerial parts of Glycyrrhiza uralensis, including two new compounds, glycyuralin Q (1) and glycyuralin R (2), and nine known compounds, including licoriphenone (3), orobol (4), trifoliol (5), 7,2′,4′-trihydroxy-5-methoxy-3-arylcoumarin (6), 11-hydroxy-9(Z),12(Z)-octadecadienoic acid (7), 11-hydroxy-9(E),12(E)-octadecadienoic acid (8), licoricone (9), glycyrin (10), and 2′-hydroxyformononetin (11). Structures of the new compounds were identified by 1D, 2D NMR and HR-MS data analyses. Compounds 1, 2 and 10 showed potent inhibitory activities against PTP1B, with IC₅₀ values of 1.43, 4.71 and 3.79 μM, respectively. Compounds 2, 4 and 10 inhibited α-glucosidase with IC₅₀ values of 13.61, 11.13 and 17.48 μM, respectively.

Correlation between 5-hydroxymethylfurfural content and color of Rehmanniae Radix and Rehmanniae Radix Praeparata

Cui Wu, Liang Xu, Bo Xu, Zhuojun Li, Zhimao Chao

2020, 29(5): 314-321. DOI: 10.5246/jcps.2020.05.029

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In the present study, we explored the correlation between 5-hydroxymethylfurfural (5-HMF) and color of Rehmanniae Radix (RR) and Rehmanniae Radix Praeparata (RRP). The color was observed by human eyes under sunlight. The chromatic value and color difference were detected by a colorimeter. The water content was determined by an oven-drying method. The 5-HMF content was determined by an HPLC method. The correlation between the 5-HMF content and the color was analyzed by bivariatecorrelation analysis. The results showed that the color was greyish-brown and dark brown for RR, and it was black for RRP. The deepening color of RRP was reflected in the decrease of L^*, a^* and b^* values. The water content was in accord with the requirement of Chinese Pharmacopoeia. The 5-HMF contents of RR and RRP were 0.9711–25.71 µg/g and 213.4–4010 µg/g, respectively. The average 5-HMF contents of RR and RRP were 8.059 µg/g and 1433 µg/g, respectively. The 5-HMF content in RRP was higher than that in RR. The correlations between 5-HMF content and L^*, a^* and b^* values were significant. The color of RRP was deeper than that of RR. The 5-HMF content of RRP was higher than 0.02%, while it was less than 0.02% of RR, which could be used as a marker component for judging RR and RRP.

Esculin alleviates acute kidney injury and inflammation induced by LPS in mice and its possible mechanism

Xiao Cheng, Yinglin Yang, Weihan Li, Man Liu, Shanshan Zhang, Yuehua Wang, Guanhua Du

2020, 29(5): 322-332. DOI: 10.5246/jcps.2020.05.030

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Acute kidney injury (AKI) is a common clinical serious illness. Esculin (ES) is a coumarin compound of traditional Chinese medicine Cortex Fraxini. Our previous study has found that ES protects against inflammation and renal damage in diabetic rats.In the present study, we aimed to investigate the effects and the possible mechanism of ES against lipopolysaccharides (LPS)-induced AKI in mice. Renal morphology was observed by H&E staining. Renal function was evaluated by blood urea nitrogen (BUN) level and creatinine content in serum. Inflammatory factor levels were measured by ELISA assay. The inflammatory proteins were analyzed by RT-PCR and Western blotting analysis. The results showed that ES alleviated LPS-induced pathological injury and renal dysfunction, and decreased BUN level and creatinine content in serum. In addition, ES significantly reduced the release of pro-inflammatory factors, including IL-1β, IL-6 and TNF-α, chemokine MCP-1 and cell adhesion molecule ICAM-1. Furthermore,the expressions of inflammatory pathway proteins P2X7, HMGB1, TLR4 and MyD88 both at the mRNA and protein levels were all down-regulated by ES in the kidney tissue of LPS-challenged mice. These results suggested ES protected against LPS-induced AKI through inhibiting P2X7 expression and HMGB1/TLR4 inflammatory pathway.

Immobilization of β-glucuronidase: biocatalysis of glycyrrhizin to 18β-glycyrrhetinic acid and in-silico lead finding

Makhmur Ahmad, Mohammad Rashid, Babar Ali, Shamshir Khan, Naseem Akhtar, Mohd Faiyaz Khan, Bibhu Prasad Panda

2020, 29(5): 333-340. DOI: 10.5246/jcps.2020.05.031

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The non-covalent immobilization of β-glucuronidase enzyme obtained from Rhizopus oryzae was carried outby entrapment in natural fiber (papaya and coconut).The bioconversion capability of immobilized enzyme was analyzed based on conversion ofglycyrrhizin to 18β-glycyrrhetinic acid under different conditions. The hydrolytic activity of the β-glucuronidase enzyme was highly depended on the microbial source and matrix, in which enzyme was immobilized. R. oryzae β-glucuronidase immobilized in papaya fibers produced the highest GA content (13.170 µg/mL) at 10 h of reaction. However R. oryzae β-glucuronidase immobilized in coconut fibers produced the highest GA content (21.425 µg/mL) at 15 h of reaction. Online Molinspiration software was used to predict drug like molecular properties of the 18β-glycyrrhetinic acid, and software suggested that the compounds had potential of becoming the orally active molecules. Therefore, in silico studies were conducted on proposed 18β-glycyrrhetinic acid to select the best possible drug candidates based on drug properties and bioactivity score of the compounds.

A prospective cohort study on the relationship between vancomycin steady-state trough concentration and efficacy and safety in Chinese adults

Chaohui Wu, Huifen Lin, Weiwei Lin, Yiwei Liu, Xiang You, Cuihong Lin, Rongfang Lin, Dayong Zeng, Pinfang Huang

2020, 29(5): 341-354. DOI: 10.5246/jcps.2020.05.032

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Clinical guidelines recommend a steady-state vancomycin(VCM) trough concentration (SVTC) of 10–15 mg/L for regular infections and 15–20 mg/L for severe infections. However, clinical trials have shown that increasing SVTC is not beneficial for efficacy, and instead it leads to nephrotoxicity. To verify whether increasing the SVTC results in improved clinical outcomes with sustainable adverse effects, we prospectively determined its correlation with clinical efficacy and safety. The participants included patients hospitalized with Gram-positive bacterial infections from March 2017 through October 2018. The patients were classified into group I (SVTC<10 mg/L), II (10≤SVTC≤20 mg/L), or III (SVTC>20 mg/L). Clinical, microbiological, and laboratory data were collected. Clinical outcomes between group I and IIwere matched after propensity score matching (PSM). A total of 331 patients were included in this study. Clinical failure occurred in 59 (29%) of 204 patients on day 14, with no significant differencebetween groups I and II (P = 0.535). Infection recurred at 28 d in 62 (30%) of 204 patients, and no significant difference ininfection recurrence was observed between both the groups (log-rank, P = 0.674). Except for a significant increase in the incidence of acute kidney injury in group II, no significant difference was observed between two groups for any clinical results. The incidence of adverse events in groups I and II was significantly lower than that in group III (P<0.001). SVTC had an applicable cut-off point at 14.55 mg/L. SVTC was not correlated with VCMclinical efficacy, while it was a good indicator of nephrotoxicity.

Research on Moflo XDP high speed cell sorting techniques and parameter optimization

Yufang Sun, Chen Zheng, Bo Xu

2020, 29(5): 355-363. DOI: 10.5246/jcps.2020.05.033

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This article aims to discuss strategies to operate Moflo XDP high-speed sorting equipment for cell sorting and optimize the instrument to run in the best operating state. Using fluorescent microspheres to quickly calibrate the position of the main liquidflow and the laser beam, adjust the amplitude and frequency according to different size CytoNozzles to find the best breakoff point, and adjust the four-way side flow to achieve the stable maintaining of the equipment, so as to quickly sort sample at high-speed. The absence of air bubbles in the sheath liquid barrel and the liquid path is the key to achieving a stable sorting-maintaining in the sorting process. The accurate calculation of the breakoff point and drop delay is the key to improve sorting efficiency and cell activity.

Pharmacists’ perceptions of generic drugs in China

Yuyao Nie, He Wang, Linguang Zhou, Luwen Shi, Bin Jiang

2020, 29(5): 364-368. DOI: 10.5246/jcps.2020.05.034

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Perceptions of Chinese pharmacists towards generic drugs were evaluated by a cross-sectional study from Aug. 2018 to Dec. 2018. Online survey tool Sojump was adopted to release the questionnaires using convenience sampling. A total of 577 questionnaires by pharmacists were analyzed. A meaningful proportion of pharmacists expressed negative perceptions of generic drugs, such as perceiving generics as less effective, less safe and more likely to cause side effects compared to their branded equivalents. Educational campaigns that focus on misperceptions of generic drugs may be necessary.

Tao Liu research group of Peking University School of Pharmaceutical Sciences and Mo Li research group of Peking University Third Hospital joint developed CRISPR non-natural amino acid coupling technique to improve the efficiency of precise genome editing

Shuxiang Song

2020, 29(5): 369-371.

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