Marine Macrolides to Tackle Antimicrobial Resistance of Mycobacterium tuberculosis.

Tuberculosis has become a major health problem globally. This is worsened by the emergence of resistant strains of Mycobacterium tuberculosis showing ability to evade the effectiveness of the current antimycobacterial therapies. Therefore, the efforts carried out to explore new entities from many sources, including marine, are critical. This review summarizes several marine-derived macrolides that show promising activity against M. tuberculosis. We also provide information regarding the biosynthetic processes of marine macrolides, including the challenges that are usually experienced in this process. As most of the studies reporting the antimycobacterial activities of the listed marine macrolides are based on in vitro studies, the future direction should consider expanding the trials to in vivo and clinical trials. In addition, in silico studies should also be explored for a quick screening on marine macrolides with potent activities against mycobacterial infection. To sum up, macrolides derived from marine organisms might become therapeutical options for tackling antimycobacterial resistance of M. tuberculosis.

Cruciferous vegetables as a treasure of functional foods bioactive compounds: Targeting p53 family in gastrointestinal tract and associated cancers.

In the past few years, phytochemicals from natural products have gotten the boundless praise in treating cancer. The promising role of cruciferous vegetables and active components contained in these vegetables, such as isothiocyanates, indole-3-carbinol, and isothiocyanates, has been widely researched in experimental in vitro and in vivo carcinogenesis models. The chemopreventive agents produced from the cruciferous vegetables were recurrently proven to affect carcinogenesis throughout the onset and developmental phases of cancer formation. Likewise, findings from clinical investigations and epidemiological research supported this statement. The anticancer activities of these functional foods bioactive compounds are closely related to their ability to upregulate p53 and its related target genes, e.g., p21. As the "guardian of the genome," the p53 family (p53, p63, and p73) plays a pivotal role in preventing the cancer progression associated with DNA damage. This review discusses the functional foods bioactive compounds derived from several cruciferous vegetables and their use in altering the tumor-suppressive effect of p53 proteins. The association between the mutation of p53 and the incidence of gastrointestinal malignancies (gastric, small intestine, colon, liver, and pancreatic cancers) is also discussed. This review contains crucial information about the use of cruciferous vegetables in the treatment of gastrointestinal tract malignancies.

Terpenes and terpenoids as main bioactive compounds of essential oils, their roles in human health and potential application as natural food preservatives.

Essential oils (EOs) are volatile and concentrated liquids extracted from different parts of plants. Bioactive compounds found in EOs, especially terpenes and terpenoids possess a wide range of biological activities including anticancer, antimicrobial, anti-inflammatory, antioxidant, and antiallergic. Available literature confirms that EOs exhibit antimicrobial and food preservative properties that are considered as a real potential application in food industry. Hence, the purpose of this review is to present an overview of current knowledge of EOs for application in pharmaceutical and medical industries as well as their potential as food preservatives in food industry.

Molecular Docking of Phytochemical Compounds of Momordica charantia as Potential Inhibitors against SARS-CoV-2.

BACKGROUND: Coronavirus disease 2019 (COVID-19) has been recently declared as a global public health emergency, where the infection is caused by SARS-CoV-2. Nowadays, there is no specific treatment to cure this infection. The main protease (Mpro) of SARS-CoV-2 and SARS spike glycoprotein- human ACE2 complex have been recognized as suitable targets for treatment, including COVID-19 vaccines. OBJECTIVE: In our current study, we identified the potential of Momordica charantia as a prospective alternative and a choice in dietary food during a pandemic. MATERIALS AND METHODS: A total of 16 bioactive compounds of Momordica charantia were screened for activity against 6LU7 and 6CS2 with AutoDockVina. RESULTS: We found that momordicoside B showed the lowest binding energy compared to other compounds. In addition, kuguaglycoside A and cucurbitadienol showed better profiles for drug-like properties based on Lipinski's rule of five. CONCLUSION: Our result indicates that these molecules can be further explored as promising candidates against SARS-CoV-2 or Momordica charantia can be used as one of the best food alternatives to be consumed during the pandemic.

Pharmaceutical Prospects of Bee Products: Special Focus on Anticancer, Antibacterial, Antiviral, and Antiparasitic Properties.

Bee products have long been used in traditional healing practices to treat many types of disorders, including cancer and microbial-related diseases. Indeed, several chemical compounds found in bee products have been demonstrated to display anticancer, antibacterial, antiviral, and antiparasitic properties. With the improvement of research tools and in view of recent advances related to bee products, this review aims to provide broad yet detailed insight into the pharmaceutical prospects of bee products such as honey, propolis, bee pollen, royal jelly, bee bread, beeswax, and bee venom, in the domain of cancer and infectious disease management. Available literature confirms the efficacy of these bee products in the alleviation of cancer progression, inhibition of bacterial and viral proliferation, and mitigation of parasitic-related symptoms. With such potentials, bioactive components isolated from the bee products can be used as an alternative approach in the long-run effort to improve humans' health at a personal and community level.

Molecular modeling and phenoloxidase inhibitory activity of arbutin and arbutin undecylenic acid ester.

Excessive melanin formation has been linked to various skin disorders such as hyperpigmentation and skin cancer. Tyrosinase is the most prominent target for inhibitors of melanin production. In this study, we investigated whether arbutin and its prodrug, arbutin undecylenic acid ester, might inhibit phenoloxidase (PO), a tyrosinase-like enzyme. Molecular docking simulation results suggested that arbutin and arbutin undecylenic acid ester can bind to the substrate-binding pocket of PO. Arbutin undecylenic acid ester with an IC50 6.34 mM was effective to inhibit PO compared to arbutin (IC50 29.42 mM). In addition, arbutin undecylenic acid ester showed low cytotoxicity in Drosophila S2 cells and the compound inhibited the melanization reaction. Therefore, the results of this study have demonstrated that arbutin undecylenic acid ester as a potential inhibitor of PO. We successfully designed a new platform utilizing Drosophila melanogaster and Bombyx mori as animal models propounding fast, cheap, and high effectiveness in method to screen tyrosinase inhibitors.

Molecular and Functional Analysis of Pore-Forming Toxin Monalysin From Entomopathogenic Bacterium Pseudomonas entomophila.

Pseudomonas entomophila is a highly pathogenic bacterium that infects insects. It is also used as a suitable model pathogen to analyze Drosophila's innate immunity. P. entomophila's virulence is largely derived from Monalysin, a ß-barrel pore-forming toxin that damages Drosophila tissues, inducing necrotic cell death. Here we report the first and efficient purification of endogenous Monalysin and its characterization. Monalysin is successfully purified as a pro-form, and trypsin treatment results in a cleaved mature form of purified Monalysin which kills Drosophila cell lines and adult flies. Electrophysiological measurement of Monalysin in a lipid membrane with an on-chip device confirms that Monalysin forms a pore, in a cleavage-dependent manner. This analysis also provides a pore-size estimate of Monalysin using current amplitude for a single pore and suggests lipid preferences for the insertion. Atomic Force Microscope (AFM) analysis displays its structure in a solution and shows that active-Monalysin is stable and composed of an 8-mer complex; this observation is consistent with mass spectrometry data. AFM analysis also shows the 8-mer structure of active-Monalysin in a lipid bilayer, and real-time imaging demonstrates the moment at which Monalysin is inserted into the lipid membrane. These results collectively suggest that endogenous Monalysin is indeed a pore-forming toxin composed of a rigid structure before pore formation in the lipid membrane. The endogenous Monalysin characterized in this study could be a desirable tool for analyzing host defense mechanisms against entomopathogenic bacteria producing damage-inducing toxins.