Mini Reviews in Medicinal Chemistry - Volume 21, Issue 14, 2021

Diabetes mellitus is a disease that presents great challenges for healthcare systems worldwide, and the identification of alternative therapies for the treatment of this disease is of vital importance. Metallic nanoparticles (gold, silver, and selenium) and metallic oxide (ZnO) have been studied in different areas such as medicine, biotechnology, the environment, and the food industry with promising results. In medicine, current research has revealed these nanoparticles' anti-diabetic properties thanks to the implementation of animal models. This review will address the existing antecedents and the effects of gold, silver, selenium, and zinc oxide nanoparticles in diabetes administered alone, functionalized with other molecules, or combined with drugs that have shown promising therapeutic effects. The anti-diabetic effects of these nanoparticles are related to the regulation of glucose, insulin, and lipid profiles. In addition, oxidative stress markers, liver and kidney markers, the reduction of inflammation, apoptosis of the pancreas, and the restoration of normal liver and kidney histology are also reported in the literature after using these nanoparticles. However, the therapeutic effects that these nanoparticles provide are limited due to the lack of specific protocols dictated by international organizations to evaluate the risks of using these nanoparticles.

Limonene and perillyl alcohol are natural monoterpenes that have attracted the attention of medicinal chemists due to their promising anticancer activities. Considering this, both compounds were explored as scaffolds to obtain various derivatives with anticancer activity. In this review, the data are organized for the first time, with a focus on the synthetic methods and strategies to obtain the derivatives throughout the period from 2000 to 2020. A brief discussion regarding the structure and activity relationships of the most active derivatives, stereoisomers, and their mechanisms of action is presented. Among the active compounds, a series of limonenes with thiosemicarbazone groups and perillyl alcohol hybrids with glycosides or drugs are illustrated. Taking all of this into account, this review may help researchers develop new promising anticancer candidates based on the structures of limonene and perillyl alcohol.

Cholesterol, steroid alcohol, was discovered by M.E. Chevreul in 1815. Cholesterol and its derivatives showed a large variety of biological properties such as anticancer activity, anticardiac activity, anti-inflammatory activity, antimicrobial activity, anti-psychotic activity, antioxidant activity, drug-loaded activity, etc. In this mini-review, the advances of structural modification of cholesterol from 2014 to 2020 are summarized. In addition, the bioactivities, mechanisms of action and structureactivity relationships of cholesterol and its related derivatives are also discussed.

Styrylquinoline is a quinoline molecule linked to phenyl rings with an unsaturated ethylene linker, resulting in a flat and rigid conformation. The synthesis of the molecule was reported almost a century ago but was not much explored due to its adverse toxicity and poor selectivity. In the last two decades, a plethora of work was reported related to the synthesis and antiretroviral activity of several styrylquinoline derivatives. Later, other activities such as antimicrobial and anticancer abilities of these derivatives were also reported. In this review, we summarize the diverse steps of the development and analyze the spectrum of the activity of styrylquinolines and their utilization in drug design. Styrylquinolines are extensively explored for new pharmacological activities in recent years and this makes the moiety gain more visibility as a potential drug candidate and lead molecule in medicinal chemistry. The data obtained in vitro and ex vivo shed light on their different mechanism of action. Styrylquinoline has proved to be a potential lead molecule in medicinal chemist’s toolkit due to the exploration of a variety of avenues of its activity as a drug candidate.

Background: Organocalcogens are a class of organic compounds obtained by the synthesis experiments to include S, Se, or Te. Among the elements that comprise this class, Se is characterized as an essential mineral and nutrient for humans. Se has been widely studied in many aspects. Organic synthesis of organoselenides is used for obtaining new potential drug candidates and may be highly beneficial from the use of computational approaches to reduce time and cost of the experiments. Thus, the goal of our study is to evaluate the computational approaches used in the organoselenides research from 1999 to 2019. Methods: A literature review was performed by searching the database “Web of Sciences”. Results: Most of the theoretical studies included structural elucidation or structure-property analysis. We also found research regarding molecular docking approaches and Quantitative Structure-Activity Relationship (QSAR) studies. Conclusions: Computational studies have been widely applied to organoselenides. They demonstrated promising results and resulted in reduced the cost of research, increased efficacy, and, ultimately, novel organoselenides with desired properties.

Virus is a type of noncellular organism, which is simple in structure, small in size and contains only one kind of nucleic acid (RNA or DNA). It must be parasitized in living cells and proliferates by replication. Viruses can infect plants or animals, which leads to many epidemic diseases, such as the current pandemic COVID-19. Viral infectious diseases have brought serious threats to the health of people around the world. Natural products are chemical substances that are usually produced by living organisms and have biological or pharmacological activity. Many of these natural products show antiviral activity. Based on the increasing importance of antiviral research, this paper focuses on the discovery and development of antiviral natural products since 2010.

Vanadium is considered to be biologically significant and several vanadium IV & V complexes have successfully been studied as chemotherapeutic agents like insulin mimetic, antibacterial, antioxidant, and anticancer activities. The divergent ligand systems also play a pivotal role in designing the metal complex with desired properties. Thus, the combination of both with their synergistic advantages results in a potential drug candidate. Different mechanistic pathways have been proposed to explain the antitumor effects of vanadium complexes, including induction of tyrosine residues phosphorylation, inhibition of key protein tyrosine phosphatases (PTPases), which in turn promote the activation of the extracellular regulated kinase cascading (ERK) pathway. In the current review, we have summarized the work on vanadium (V) complexes based on different ligand systems and their biological significance as an anticancer lead compound.

Background: Adhatoda vasica (Nees.) of the family Acanthaceae has been used in the Southeast tropical zone as it is efficacious against headache, colds, cough, whooping cough, fever, asthma, dyspnea, phthisis, jaundice, chronic bronchitis, and diarrhea. It exhibits commendable pharmacological activities. Objective: The aim of the review is to provide a systematic overview of pharmacological activities with toxicity and clinical assessment, phytochemistry of A. vasica along with its characterization, geographical observation, phenology, traditional uses, as well as an organized representation of the findings. Method: The overall information of A. vasica was collected from various resources, including books, review papers, research papers, and reports which were obtained from an online search of globallyaccepted scientific databases. ChemDraw software was used to draw the compound’s structure. Results: Phytochemical review on A. vasica has led to the collection of 233 compounds of different types such as alkaloids, flavonoids, essential oils, terpenoids, fatty acids, phenols, etc. It is a promising source of potential phytopharmaceutical agent that exhibits diverse pharmacological activities, including antibacterial, antifungal, hepatoprotective, anti-ulcer, abortifacient, antiviral, antiinflammatory, thrombolytic, hypoglycemic, anti-tubercular, antioxidant, and antitussive activities. Conclusions: Sufficient number of studies on ethnopharmacology, traditional uses, and pharmacological activities of A. vasica are conducted. Furthermore, it is necessary to study the activity of chemical constituents for new drug design and discovery from natural products.

Introduction: Herb, Zanthoxylum armatum DC., commonly called Indian prickly ash, and Nepal pepper (family Rutaceae), is widely utilized in the traditional medicinal system. Objective: The current review provides requisite data for collecting descriptive information on the organoleptic, microscopical, ethnobotanical use, and phytochemicals and pharmacological properties of Z. armatum; therefore, it may help in forming a bridge between research gaps and the upcoming future findings for most of the researches. Materials and Methods: The systematic literature survey was conducted using the PRISMA methodology. The collective information was gathered from books, renowned journals, and electronic databases including Science Direct, Web of Science, Scopus and PubMed from 1966 to 2020. Results: Most of the bioactive metabolites are isolated and characterized till date, such as monoterpenes in essential oil and lignan components are reported to be present in the herbs. Several in vitro and in vivo pharmacological bioassays revealed the potential of Z. armatum having as possessing antimicrobial, antifungal, antibacterial, and hepatoprotective effects and so on. Conclusion: Therefore, the current review summarizes the organoleptic, microscopy, phytochemistry and biological activities of Z. armatum, providing more emphasis on in vitro as well as in-vivo studies along with clinical research, helpful in exploring the potential efficacy of the plant.