Table of Content

28 November 2021, Volume 30 Issue 11

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Original articles

Synthesis of a series of novel homo- and hetero-glycoclusters and their binding activities to DC-SIGN

Xueni Cai, Ge Fu, Martin Lepšík, Emanuele Paci, Yuan Guo, Zhongjun Li, Qing Li

2021, 30(11):  859-873.  DOI: 10.5246/jcps.2021.11.074

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As a dendritic cell-specific C-type lectin receptor, DC-SIGN plays an important role in the early stages of many viral infections, including HIV and Ebola, making it an interesting therapeutic target. It has been found that DC-SIGN can recognize both highly mannosylated and branched fucosylated oligosaccharides. Herein, we synthesized a new series of homo- and Man-Fuc heteroglycoclusters with diverse structures. The binding properties of these compounds to tetrameric extracellular DC-SIGN were assessed by surface plasmon resonance (SPR). Heteroglycocluster 17b showed high DC-SIGN-binding activity (K_D = 2.6 μM). The structural determinants of this high affinity of 17b were rationalized by docking and compared with its much less potent isomer 17a. Therefore, 17b might serve as a base for the development of potent inhibitors of DC-SIGN-dependent viral infection.



Syntheses of phenyl benzoate compounds and their bioactivity investigation

Beidou Zhou, Jiali Li, Baocheng Huang, Zihan Yu, Zetong Ma, Zhipeng Ruan, Qihong Cai, Dongbao Hu

2021, 30(11):  874-882.  DOI: 10.5246/jcps.2021.11.075

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Eight phenyl benzoate compounds were synthesized in one step, and then their antioxidant, anti-tyrosinase, and anti-pancreatic lipase activities were evaluated in the present study. The total yields ranged from 31% to 85%. Compound 4c exhibited a stronger antioxidant activity compared with Trolox, with half maximal inhibitory concentrations (IC₅₀) of approximately 13.06 μM, and the antioxidant mechanism was further studied using computational chemistry. Compounds 1c–5c exhibited minimal anti-tyrosinase activity. Compounds 4c, 5d, 6c and 6d exhibited weak anti-pancreatic lipase activity, with an inhibition rate of 33.52%, 15.76%, 18.37% and 20.77%, respectively. These results demonstrated that all compounds had reference significance, especially compound 4c.



Ela tablets improve sexual performance in mice with erectile dysfunction caused by repeated restraint stress

Zeyu Gao, Jun Chen, Ayinuer Reheman, Yi Sun, Tao Wu, Xirali Tursun, Xiaoping Pu, Haji Akber Aisa, Xin Zhao

2021, 30(11):  883-894.  DOI: 10.5246/jcps.2021.11.076

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Ela tablets contain an optimized extract of a Chinese herbal prescription. The original prescription has been used to treat erectile dysfunction (ED), while the detailed indications and specific treatment mechanisms of Ela tablets remain unclear. In the present study, we aimed to investigate whether Ela tablets could protect mice from ED caused by repeated restraint stress and to explore the possible mechanisms. Mice were restrained daily in centrifuge tubes with venting holes for 14 consecutive days and administered Ela tablets at 1 h before restraining. On the 14^th night, mating experiments were conducted. Thereafter, blood, testicular, and penile samples were collected. Serum testosterone levels were measured using a kit. Testicular tissue morphology was observed by H&E staining. The PDE5 expression in the corpus cavernosum was measured by Western blotting analysis. The results indicated that Ela tablets significantly shortened the sexual arousal time, increased the number of sexual encounters, maintained the normal morphology of testicular tissue, increased the serum testosterone levels, and decreased the PDE5 expression in the corpus cavernosum. Our data showed that Ela tablets elicited protective effects on the sexual ability of mice exposed to repeated restraint stress. Moreover, the underlying mechanism was related to the preservation of testicular tissue morphology, maintenance of testosterone levels, and inhibition of penile PDE5 expression.



Teasaponin induces reactive oxygen species-mediated mitochondrial dysfunction in Candida albicans

Shihui Li, Kemeng Guo, Nining Yin, Mingzhu Shan, Yao Zhu, Ying Li

2021, 30(11):  895-903.  DOI: 10.5246/jcps.2021.11.077

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Candida albicans is the most prevalent commensal fungus and readily causes invasive fungal infection in immunocompromised individuals. Teasaponin (TS), a natural product generally regarded as safe, has been reported to inhibit filamentation of C. albicans. This study found that TS could exert moderate fungicidal activity against C. albicans, and the mode of action was further explored. The minimum fungicidal concentration (MFC) was determined by the broth microdilution method. The colony counting method was used to determine the time-killing curve of TS against C. albicans in every 2 h. The effect of TS on the content of intracellular reactive oxygen species (ROS) in C. albicans was analyzed by 2′,7′-dichlorofluorescin diacetate (DCFH-DA) staining, and the mitochondrial membrane potential (mtΔψ) was determined by rhodamine123 (RH123) staining. An ATP assay kit was utilized to determine the intracellular ATP levels after TS treatment. Results showed that TS-induced ROS accumulation and mitochondrial dysfunction contributed to the death of C. albicans cells. Further research demonstrated that VC could reinforce the fungicidal ability of TS. On the contrary, VE could antagonize the function of TS against C. albicans, which might guide the clinical application of TS. The results preliminarily elucidated the potential mechanisms of TS against C. albicans and might provide a potential option for the treatment of clinical Candida.



Preparation and characterization of pH-sensitive calcium carbonate-chlorin e6 nanoparticles for photodynamic therapy

Jingru Wang, Shuang Zhang, Zhuoyue Li, Meiqi Xu, Guangxue Wang, Xuan Zhang

2021, 30(11):  904-911.  DOI: 10.5246/jcps.2021.11.078

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In the present study, we combined CaCO₃ NPs and Ce6 to construct CaCO₃-Ce6 nanoparticles (NPs). CaCO₃-Ce6 NPs were characterized in terms of particle size, zeta potential, UV-Vis absorption spectrum, fluorescence spectrum, FTIR spectrum, and pH-responsive behavior. The reactive oxygen species (ROS) generation in vitro was measured in 4T1 cells. The results showed that CaCO₃-Ce6 NPs were uniform-sized NPs with excellent fluorescence properties and pH-responsive behavior. The ability of ROS generation by CaCO₃-Ce6 NPs was stronger compared with Ce6 in 4T1 cells because Ca²⁺ could enhance the ROS generation, which could contribute to a stronger anti-tumor effect.



Determination of deferasirox particle size distribution via laser diffraction and its application in establishing a correlation between particle size and drug dissolution in vitro

Yuyuan Chen, Song Wu, Liqing Chen, Yuanyuan Zhang, Zhonggao Gao, Tianlei Li, Wei Huang, Qingyun Yang

2021, 30(11):  912-923.  DOI: 10.5246/jcps.2021.11.079

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Deferasirox is the first-line drug for iron overload due to thalassemia in adults and pediatric patients. It is classified as a type II compound in the Biopharmaceutics Classification System, and thus the particle size of its active pharmaceutical ingredient (API) should be strictly controlled during the manufacturing process. In the present study, laser diffraction was adopted to measure the particle size distribution of deferasirox API. We also developed and validated an accurate and convenient method by investigating important optical parameters and sample dispersing conditions. The relative standard deviation values, namely, d (0.1), d (0.5), d (0.9), and d (4,3), measured via methodology validation and actual sample measurement were < 3%. The dissolution curves of several batches of dispersible tablets prepared using deferasirox with different particle sizes were compared in the four dissolved media to investigate the influence of particle size on drug dissolution in vitro. Results indicated that the particle size distribution of deferasirox API significantly affected the release of its dispersible tablet.



Chemical constituents from the seeds of Capparis masaikai

Caicai Xi, Yunling Xu, Kang Feng, Renzhao Wu, Shihong Luo

2021, 30(11):  924-931.  DOI: 10.5246/jcps.2021.11.080

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A total of 21 compounds were isolated from the seeds of Capparis masaikai and identified as oxazolidine-2-thione (1), succinimide (2), catechol (3), octathiocane (4), monoethanolamine (5), 3-hydroxypropanenitrile (6), L-arabinose (7), 1,2,3-propanetriol (8), drummondol (9), spionoside B (10), adenosine (11), corchoionoside C (12), coniferin (13), syringin (14), cis-syringin (15), dihydrosyringin (16), indole-3-carboxylic acid (17), β-D-glucopyranosyl indole-3-carboxylic acid (18), 6-hydroxyindole-3-carboxylic acid β-D-glucopyranosyl ester (19), linoleis monoglyceride (20), and triolein (21). Their structures were identified based on physicochemical property and spectroscopic analysis, including MS, NMR, and single-crystal X-ray crystallographic data. Compounds 2–10 and 12–21 were isolated from C. masaikai for the first time.



News

The group of Professor Xiaoda Yang has made important progress in protein phosphatase inhibitors based on vanadium active groups

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2021, 30(11):  932-933. 

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The group of Professor Xiaoda Yang has made important progress in protein phosphatase inhibitors based on vanadium active groups.



The group of Professor Zhenjun Yang has made continuous progress in the research and development of RNA drugs and vaccines

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2021, 30(11):  934-936. 

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The group of Professor Zhenjun Yang has made continuous progress in the research and development of RNA drugs and vaccines.



The group of Professor Tao Liu has published noncanonical amino acids (ncAAs)-triggered therapeutic switch on Nature Chemical Biology

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2021, 30(11):  937-938. 

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The group of Professor Tao Liu has published noncanonical amino acids (ncAAs)-triggered therapeutic switch on Nature Chemical Biology.



The 4th International Conference on Nanomedicine was held

School of Pharmaceutical Sciences, Peking University Health Science Center

2021, 30(11):  939-940. 

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The 4th International Conference on Nanomedicine was held.