Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Advance online publication
Displaying 1-3 of 3 articles from this issue
  • Kou Nakamura, Masako Yamasaki, Hirofumi Ohashi, Shiki Saito, Koudai As ...
    Article ID: c23-00243
    Published: 2023
    Advance online publication: May 26, 2023

    Although aryl hydrocarbon receptors (AhRs) are related to the metabolic pathway of xenobiotics, recent studies have revealed that this receptor is also associated with the life cycle of viruses and inflammatory reactions. For example, flutamide, used to treat prostate cancer, inhibits hepatitis C virus proliferation by acting as an AhR antagonist, and methylated-pelargonidin, an AhR agonist, suppresses pro-inflammatory cytokine production. To discover a novel class of AhR ligands, we screened 1000 compounds derived from fungal metabolites using a reporter assay and identified methylsulochrin as a partial agonist of the aryl hydrocarbon receptor. Methylsulochrin was found to inhibit the production of hepatitis C virus (HCV) in Huh-7.5.1 cells. Methylsulochrin also suppressed the production of interleukin-6 in RAW264.7 cells. Furthermore, a preliminary structure–activity relationship study using sulochrin derivatives was performed. Our findings suggest the use of methylsulochrin derivatives as anti-HCV compounds with anti-inflammatory activity.

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  • Shiyi Tang, Rui Feng, Yanlei Kang, Jianbo Cheng, Jianguang Zhou
    Article ID: c22-00881
    Published: 2023
    Advance online publication: April 26, 2023

    The efficiency of pharmacotherapy is significantly influenced by the crystal habit and polymorphic form of the drugs. Especially due to the anisotropy of different facets in crystalline material, crystal habit impacts the physicochemical properties and behaviors of a drug, which has been rarely reported. This paper describes a facile method for online monitoring of crystal plane orientation of favipiravir(T-705) by Raman spectroscopy. Firstly, we investigated the synergy of multiple physicochemical fields (solvation, agitated flow fields, etc.), and then prepared favipiravir crystals with different orientations in a controllable manner. Secondly, to establish the connection between crystal planes and Raman spectra, the favipiravir crystals were theoretically analyzed at the molecular and structural levels using density functional theory (DFT) and 3D visualization tools. Finally, we based on standard samples and applied it to 12 actual samples to evaluate the crystal habit of favipiravir. The results are similar to the classical XRD method. Additionally, the XRD method is difficult to be monitored online, while the Raman method is non-contact, fast, and requires no sample preparation, showing a great application prospect in the pharmaceutical process.

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  • Yusuke Imayoshi, Shuji Ohsaki, Hideya Nakamura, Satoru Watano
    Article ID: c23-00168
    Published: 2023
    Advance online publication: April 22, 2023

    A rotary tableting machine is used for the continuous tableting process. Tableting conditions often result in capping, leading to serious problems during production. Several studies have been conducted to predict the tablet capping tendency. However, as most previous studies were conducted using a compaction simulator, there is a lack of technology that can be readily applied during actual production. Therefore, the present study aimed to develop a novel method for predicting tablet capping in a rotary tableting machine. We hypothesized that capping occurs when residual stress of the tablet inside a die exceeds the critical stress immediately before ejection. Residual stress was evaluated by measuring the in-line die-wall pressure in a rotary tableting machine. Additionally, critical stress was estimated from the tablet strength inside the die using the Rumpf’s equation. The critical and residual stresses were compared to determine the capping tendency to some extent. The findings of this study will substantially contribute to the rapid detection of tablet capping during tablet production.

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