Current Topics in Medicinal Chemistry - Volume 22, Issue 2, 2022

As a traditional Chinese medicine (TCM), Shuang-Huang-Lian (SHL) has been widely used for treating infectious diseases of the respiratory tract such as encephalitis, pneumonia, and asthma. During the past few decades, considerable research has focused on pharmacological action, pharmacokinetic interaction with antibiotics, and clinical applications of SHL. A huge and more recent body of pharmacokinetic studies support the combination of SHL and antibiotics have different effects such as antagonism and synergism. SHL has been one of the best-selling TCM products. However, there is no systematic review of SHL preparations, ranging from protection against respiratory tract infections to interaction with antibiotics. Since their important significance in clinical therapy, the pharmacodynamics, pharmacokinetics, and interactions with antibiotics of SHL were reviewed and discussed. In addition, this review attempts to explore the possible potential mechanism of SHL preparations in the prevention and treatment of COVID-19. We are concerned about the effects of SHL against viruses and bacteria, as well as its interactions with antibiotics in an attempt to provide a new strategy for expanding the clinical research and medication of SHL preparations.

Urease is an attractive drug target for designing anti-infective agents against pathogens such as Helicobacter pylori, Proteus mirabilis, and Ureaplasma urealyticum. In the past century, hundreds of medicinal chemists focused their efforts on explorations of urease inhibitors. Despite the FDA’s approval of acetohydroxamic acid as a urease inhibitor for the treatment of struvite nephrolithiasis and the widespread use of N-(n-butyl)thiophosphoric triamide as a soil urease inhibitor as nitrogen fertilizer synergists in agriculture, urease inhibitors with high potency and safety are urgently needed. Exploration of novel urease inhibitors has therefore become a hot research topic recently. Herein, inhibitors identified worldwide from 2016 to 2021 have been reviewed. They structurally belong to more than 20 classes of compounds such as urea/thioure analogues, hydroxamic acids, sulfonamides, metal complexes, and triazoles. Some inhibitors showed excellent potency with IC50 values lower than 10 nM, having 10000-fold higher potency than the positive control thiourea.

Background: Allium sativum L., or garlic, is one of the most studied plants worldwide within the field of traditional medicine. Current interests lie in the potential use of garlic as a preventive measure and adjuvant treatment for viral infections, e.g., SARS-CoV-2. Even though it cannot be presented as a single treatment, its beneficial effects are beyond doubt. The World Health Organization has deemed it an essential part of any balanced diet with immunomodulatory properties. Objective: The aim of the study was to review the literature on the effects of garlic compounds and preparations on immunomodulation and viral infection management, with emphasis on SARS-CoV- -2. Methods: Exhaustive literature search has been carried out on electronic databases. Conclusion: Garlic is a fundamental part of a well-balanced diet which helps maintain general good health. The reported information regarding garlic’s ability to beneficially modulate inflammation and the immune system is encouraging. Nonetheless, more efforts must be made to understand the actual medicinal properties and mechanisms of action of the compounds found in this plant to inhibit or diminish viral infections, particularly SARS-CoV-2. Based on our findings, we propose a series of innovative strategies to achieve such a challenge in the near future.

Bergenin, 4-O-methyl gallic acid glucoside, is a bioactive compound in various plants belonging to different families. The present work compiles scattered information on pharmacology, structure-activity relationship and nanotechnological aspects of bergenin, collected from various electronic databases such as Sci Finder, PubMed, Google Scholar, etc. Bergenin has been reported to exhibit hepatoprotective, anti-inflammatory, anticancer, neuroprotective, antiviral, and antimicrobial activities. Molecular docking studies have shown that isocoumarin pharmacophore of bergenin is essential for its bioactivities. Bergenin holds a great potential to be used as a lead molecule and also as a therapeutic agent for the development of more efficacious and safer semisynthetic derivatives. Nanotechnological concepts can be employed to overcome the poor bioavailability of bergenin. Finally, it is concluded that bergenin can emerge as clinically potential medicine in modern therapeutics.

Background: The pecan nutshell contains phytochemicals with various biological activities that are potentially useful in the prevention or treatment of diseases, such as cancer, diabetes, and metabolic imbalances associated with heart diseases. Objective: The aim of this study is to update this topic by means of a literature review and include those studies that contribute to the knowledge of the chemical composition and biological activities of pecan nutshell, particularly those related to the therapeutic potential against some chronic degenerative diseases associated with oxidative stress. Methods: Exhaustive and detailed review of the existing literature was conducted using electronic databases. Conclusion: The pecan nutshell is a promising natural product with pharmaceutical uses in various diseases. However, additional research related to the assessment of efficient extraction methods and characterization, particularly the evaluation of the mechanisms of action in new in vivo models, is necessary to confirm these findings and development of new drugs with therapeutic use.