Journal of Chinese Pharmaceutical Sciences

Integrated combination delivery of IDO inhibitor and paclitaxel for cancer treatment

Dakuan Wang, Bo Peng, Mengmeng Qin, Minghui Li, Ge Song, Bing He, Hua Zhang, Wenbing Dai, Qiang Zhang, Xiangbao Meng, Huan Meng, Xueqing Wang

2021, 30(1): 1-16. DOI: 10.5246/jcps.2021.01.001

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In order to realize the combination of chemotherapy and immunotherapy, a reduction-responsive paclitaxel (PTX) prodrug PEG-SS-PTX was synthesized and used as a carrier to encapsulate IDO inhibitor CY-1-4 for preparing PEG-SS-PTX/CY-1-4 NPs. PEG-SS-PTX/CY-1-4 NPs were evaluated by cytotoxicity, immunogenic cell death (ICD) induction ability and anti-tumor efficacy. Dynamic light scattering (DLS) results showed that the size of PEG-SS-PTX/CY-1-4 NPs was about 149 nm. In vitro experiments indicated that its cytotoxicity was in a concentration-dependent manner, and it induced the ICD of B16-F10 cells. In vivo studies in melanoma mouse model indicated that PEG-SS-PTX/CY-1-4 NPs significantly inhibited the tumor growth and reduced the expression of IDO in tumor tissues. Moreover, it increased the rate of CD8⁺ T cells in the spleen. In summary, PEG-SS-PTX/CY-1-4 NPs achieved good anti-tumor effects and reduced the dose of chemotherapy drugs, which was a safe and effective combined delivery system.

Fabrication of deoxycholic acid-modified polymeric micelles and their transmembrane transport

Qi Liu, Leqi Wang, Xinping Hu, Chuhang Zhou, Yingwei Tang, Yining Ma, Xiaoxiao Wang, Yan Liu

2021, 30(1): 17-26. DOI: 10.5246/jcps.2021.01.002

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Oral administration is the best way for the most patients due to the good compliance, and intestinal epithelium is the main barrier of oral drug absorption. In order to overcome the small intestine epithelial barrier to orally deliver water-insoluble drugs, deoxycholic acid (DA), a substrate of the intestinal bile acid transporters, conjugated poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) (DA-PEOz-PLA) was designed and synthesized, and deoxycholic acid-modified polymeric micelles composed of DA-PEOz-PLA and mPEG-PLA were fabricated to encapsulate model drug coumarin 6 (C6) based on intestinal bile acid pathway. The structure of DA-PEOz-PLA was confirmed using 1H NMR and TLC, and the molecular weight measured by GPC was 10 034 g/mol with a PDI of 1.51. The C6-loaded polymeric micelles with drug loading content of 0.085% were characterized to have 40.11 nm in diameter and uniform spherical morphology observed by TEM. Furthermore, the deoxycholic acid-modified polymeric micelles were demonstrated to further enhance the transmembrane transport efficiency. The mechanic study evidenced that anchorage of deoxycholic acid onto the micelles surface enriched their transcellular transport pathway. Therefore, the designed deoxycholic acid-modified polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.

The antidepressive effect of the complex consisting of Radix Pseudostellariae, Radix Pueraria and Herba Epimedii: the involvement of NRSF/NRSE-TPH2 signaling

Xuan Yu, Xinpei Wang, Fan Lei, Yugang Wang, Wei Wang, Yi Ding, Dongming Xing, Zhiyi Yuan, Hong Sun, Lijun Du

2021, 30(1): 27-41. DOI: 10.5246/jcps.2021.01.003

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Depression is a psychological disease with no particularly effective therapy currently available. In the present study, we aimed to examine the antidepressive activity of a pharmaceutical Chinese medicine called TaiZi (TZ) capsule, consisting of total polysaccharides of Radix Pseudostellariae and total flavonoids of both Radix Pueraria and Herba Epimedii. A tail suspension test and forced swimming test were performed to assess the effect of TZ in vivo. A plasmid of TPH2 (tryptophan hydroxylase-2) was constructed to determine the exact target of TZ in vitro. In addition, mRNA expression was detected using a real-time PCR assay, and the protein expression was investigated using a Western blotting analysis. The results showed that TZ had an anti-depression effect in mouse and rat models with increased serotonin in the brain, and in the upregulation of mRNA and protein expression of TPH2 in the brain simultaneously by inhibition of NRSF (neuron restrictive silencer factor) expression because NRSF could bind to NRSE (neuron restrictive silencer element) to repress TPH2 transcription during the depression conditions. Icariin could bind to NRSE directly and block NRSF protein toward to NRSE for TPH2 inhibition. Therefore, we concluded that TZ had potential antidepressive effects because it could ameliorat the depression-like behavior in the animals, and the underlying mechanism of the effect was involved in NRSF/NRSE-TPH2 signaling. Icariin was identified as the active component of TZ. This study provided a new perspective for the development of antidepression drugs (Chinese medicines) based on NRSF/NRSE -TPH2 signaling.

Secondary metabolites from a deep-sea-derived Aspergillus versicolor F77

Ying Kang, Chanjuan Zhang, He Zhang, Dong Liu

2021, 30(1): 42-48. DOI: 10.5246/jcps.2021.01.004

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Chemical examination of fermentation products of a deep-sea-derived fungus Aspergillus versicolor F77 led to the isolation of two new compounds acetyl-sydonol (1) and 2-hydroxydiorcinol D (2), a new natural product 1-(2,4-dimethoxyphenyl)-1,2-dihydro-3H-pyrazol-3-one (3), together with four known compounds sydonol (4), (S)-sydonic acid (5), aspergillusene A (6) and diorcinol D (7). Their structures were determined through the extensive spectroscopic analysis and comparison with the reported data in literature. Compound 6 showed moderate NF-κB inhibitory activity.

Pharmacodynamic comparison of two different source plants of Murrayae Folium et Cacumen

Mengqiu Lu, Haizhen Liang, Pengfei Tu, Yong Jiang

2021, 30(1): 49-57. DOI: 10.5246/jcps.2021.01.005

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A comparison of the pharmacodynamic effects of two source plants of Murrayae Folium et Cacumen (MFC), Murraya exotica L. and Murraya paniculata (L.) Jack, was performed in order to supply reference for its multi-source rationality and interchangeability in clinical practice. According to the traditional efficacy of MFC, the effects of promoting Qi, relieving pain, promoting blood circulation and removing blood stasis were systematically evaluated by the models of writhing response in mice, foot swelling in rats, gastric emptying and small intestine propulsion in mice, and acute blood stasis in rats, respectively. The results showed that both M. exotica and M. paniculata could significantly inhibit the writhing reaction induced by acetic acid in mice and the paw swelling induced by carrageenan in rats, reduce IL-6, TNF-α and PGE2 levels in plasma of paw-swelling rats and increase gastric empty rate and intestinal propulsive rate. The above-mentioned effects were dose-dependent, and there was no significant difference between M. exotica and M. paniculata at the same doses. Therefore, M. exotica and M. paniculata had the similar anti-inflammatory, analgesic and gastrointestinal motility promotion effects, which provided a support for the pharmacodynamic equivalence of the multi-source plants of MFC.

Quality evaluation of Farfarae Flos by ITS/ITS2 and HPLC fingerprint analysis

Zijuan Lu, Yan Jia, Jie Xing, Shuxian Xiao, Yulong Wang, Wenjie Qin, Xuemei Qin, Zhenyu Li

2021, 30(1): 58-68. DOI: 10.5246/jcps.2021.01.006

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The flower bud of Tussilago farfara L., also known as Farfarae Flos (FF), is commonly used in the traditional Chinese medicine (TCM) for the treatment of cough, bronchitis and asthmatic disorders. In this study, 26 samples from five provinces across northern China were collected, and internal transcribed spacer-polymerase chain reaction (ITS-PCR) coupled with high performance liquid chromatography (HPLC) fingerprint profiling was used for the quality evaluation of FF. The results of the ITS sequence analysis showed the high similarity values among these samples. ITS2 sequence exhibited less molecular diversity compared with ITS1, and no obvious correlation was found between the variation of ITS with the production areas or cultivation methods. The results of HPLC fingerprints in combination with the similarity analysis suggested that relative contents of phenylpropanoids and flavonoids varied among the 26 FF samples, and there was also no obvious difference among the different habitats. The phenylpropanoids and the flavonoids showed similar fluctuating patterns, and positive correlation among them was also observed. The results presented in this study suggested that FF from different habits showed high similarities, and ITS-PCR coupled with HPLC fingerprint profiling could be used as a valuable approach for the quality evaluation of FF.

Development and challenges of professional Master of pharmacy education in China

Jie Gu, Yanli Liu, Fengguo Xu, Yongze Zhang, Rong Shao, Tao Lu

2021, 30(1): 69-76. DOI: 10.5246/jcps.2021.01.007

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In the present work, we aimed to describe the current situation and developing trend of professional Master of pharmacy education in China. Systematic searches of websites for literatures related to the specialty of professional Master of pharmacy were conducted. E-mail or telephone inquires were made directly to 108 pharmacy institutions (schools and universities) in China offering the MPharm program. The MPharm program was established in China in 2010, which primarily focuses on cultivating professionals in fields, such as drug technology transformation, inspection and regulation of drugs, registration and distribution of drugs, and pharmaceutical services. After 9 years of development, it has almost completed the overall design of its higher education paradigm with Chinese characteristics. With the rapid development of the pharmaceutical industry in China, the professional degree of pharmacy education program at the master’s level is insufficient to meet social and market demand for qualified professionals. Therefore, doctoral-level programs are now being promoted.

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Journal of Chinese Pharmaceutical Sciences

2021, 30(1): 77-86.

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