Efficient transport and biotransformation of dipeptide-like tyrosine/phenylalanine-conjugated phenolic amide esters in THP-1 cells and PBMCs: A potential means for transporting compounds inside monocytes/macrophages

Background: Recent studies suggest that dipeptide-like tyrosine/phenylalanine-conjugated phenolic amide compounds may contain several biological activities including anti-inflammatory activity. However, there is currently no information about their transport and biotransformation in monocytes/macrophages involved in inflammation process. Objective: The objective of this study was to investigate cell transport and biotransformation of the phenolic amides and esters in monocyte/macrophage-like cells. Methods: Cell transport and biotransformation of the phenolic amides and esters (N-coumaroylphenylalanine, N-caffeoylphenylalanine, N-feruloylphenylalanine, N-coumaroyltyrosine, N-caffeoyltyrosine, N-feruloyltyrosine and their O-methyl esters) were investigated in THP-1 cells and PBMCs using HPLC, cellular and kinetics methods Results: In THP-1 cells, the phenolic amides were not transported significantly, but their O-methyl esters were transported significantly (P < 0.02). Also, the transport of the esters was found to be sodium-independent and pH-dependent. Among the tested esters, N-feruloylphenylalanine-O-methyl ester showed the highest uptake (Km of 25 µM), and the uptake was inhibited by PepT1/2 substrate and blocker (GlySar and enalapril) in THP-1 cells. Particularly, enalapril competitively inhibited the uptake with Ki of 560 µM. The data also showed that N-feruloylphenylalanine-O-methyl ester and N-feruloyltyrosine-O-methyl ester could be biotransformed into parent phenolic amides in THP-1 cells. Similarly, the ester compounds were also found to be transported and biotransformed in PBMCs. Conclusion: The data suggest that dipeptide-like tyrosine/phenylalanine-conjugated phenolic amide esters may be transported and biotransformed in THP-1 cells and PBMCs.

Essential oils of basil cultivars selectively affect the activity of antioxidant enzymes in murine glial cells

Aims: The aim of this work was to reveal some mechanisms of influence of three basil EO on the microglial cells, as recent-years research data state that these oils have anti-aging and neuroprotective action, and as it is supposed, against also some forms of neurodegenerations. Background: The microglial cells play a pivotal role as the neuroprotective agents against neuroinflammation. Ocimum subspecies are a rich source of essential oils (EO) and used to be applied since antiquity for different purposes, including the prevention and treatment of various diseases. Objective: We decided to evaluate the influence of the essential oils extracted from three basil cultivars (O. basilicum var. purpureum, O. basilicum var. thyrsiflora, and O. x citriodorum), possessing remarkable antioxidant capacity on the activity of the main antioxidant enzymes in microglial BV-2 wild type (WT) and Acetyl-CoA oxidase deficient cell lines (Acox1-/-). Method: All manipulations were carried out using murine microglial BV-2 cell lines (BV-2, Acyl-CoA oxidase type 1 (ACOX1) deficient mutants (Acox1-/-) and WT cells). Result: Different data included in the present article are stating that plant origin substances can play a role of regulators of enzymatic antioxidant capacity of cells. EOs extracted from the Ocimum different cultivars are able to trigger the activity of acetyl-CoA oxidase type 1 (or palmytoil-CoA oxidase type 1), which can serve as a basis of regulation of redox deviation in WT cells. Conclusion: So, it can be suggested them to be applied for the prevention of some processes, which can influence on the aging, as the process of ageing is commonly associated with mitochondrial dysfunction, oxidative stress caused by the increased level of free radical production, dysfunction of the microglia, high blood pressure and so on.

Effects of Nigella Sativa (Black seeds) Supplementation on Plasma Lipid Profile in Human Subjects – A review

: Dyslipidemia is the major risk factor for atherosclerotic cardiovascular disease (ASCVD), cerebrovascular disease and peripheral artery disease (PAD). It is characterized by higher plasma concentrations of total cholesterol (TC), low density lipoprotein-cholesterol (LDL-c), apolipoprotein B (apoB), very low density lipoprotein-cholesterol (VLDL-c), triglycerides (TGs) and low levels of high density lipoprotein-cholesterol (HDL-c). Herbal medicines are preferred by many across the globe particularly to manage chronic conditions such as dyslipidemia, hypertension, type 2 diabetes, cancer, and plenty of others. Nigella sativa (Black seeds or Black cumin seeds) is a miracle herb employed within the management of many sicknesses for centuries. Hence, this review focuses on the ameliorative effects of N. sativa on the plasma lipid concentrations of human subjects. Numerous randomized controlled clinical trials (RCTs) and different clinical studies demonstrated that N. sativa possess potential anti-dyslipidemic activity. The patients with dyslipidemia may well be benefited by using N. sativa along with healthy lifestyle changes and statin and other antihyperlipidemic medications as adjuvant therapy if needed.

Anti-infective and Antineoplastic properties of Green Tea Catechins: Examining the Therapeutic Risk-Benefit ratio

Background: Green tea is a commonly used dietary supplement and food product. Green tea contains many polyphenolic compounds known as green tea catechins (GTCs). There are numerous reports exploring the potential benefit of using green tea catechins as chemotherapeutic agents to treat neoplastic disorders and infectious processes. The prevalence of cancer diagnoses, bacterial infections, and viral diseases that include SARS-CoV-2 have led to increased interest in GTCs as a therapeutic option in patients suffering from these conditions. Objective: This concise review explores the evidence related to the therapeutic use of GTCs to treat neoplastic disorders as well as bacterial and viral infections. Methods: PubMed, NIH, OVID online databases were utilized to retrieve relevant scientific literature that address GTCs role in treating cancer and infectious disease. Results: While there are preliminary data indicating potentially adventitious properties of GTCs, there is a paucity of large prospective clinical trial data to support the use of GTCs in a therapeutic capacity to treat these disease processes. There are documented instances of GTCs interacting with medications indicated to treat neoplastic diseases. Conclusions: Currently, it appears the therapeutic benefit of using GTCs is outweighed by the potential risks.

Analytical methods for the quantification of selenium species in biological matrix: Where are we?

Objective: Over the years, scientific investigations have proven the importance of selenium as an essential element for mammals, emphasizing its activity against many diseases and even its prophylactic effects. It is also established now that a malconsumption of selenium can be harmful. Therefore, the nature and the concentration of selenium and its derivatives found in the diet, the body, and even in the environment, for example, in the soil, should be determined carefully. Methods: In this review, analytical methods for speciation and determination of selenium concentrations in biological samples are summarized. Results: Methods ranging from routine to cutting-edge are explored, focusing on their analytical characteristics, such as specificity for discrete selenium species, sensitivity, accuracy, reproducibility, and skills required. Conclusion: There are already numerous studies regarding the analysis of selenium species. Beyond the method employed for actual measurements, we propose to review the preanalytic steps for sample handling in biological matrices, which directly affect results that will be more accurate with careful pretreatment. Furthermore, to reach better outcomes in terms of the identification of selenium species, different combinations of techniques might be the answer. We highlight here the last and the cutting-edge methods to identify and quantify selenium such as, high-performance liquid chromatography combined to inductively coupled plasma mass spectrometry (HPLC-ICP-MS), hydride generation atomic absorption spectrometry (HG-AAS), hydride-generation combined to atomic fluorescence spectrometry (HG-AFS), or to inductively coupled plasma optical emission spectrometry (HG-ICP-OES). This review emphasizes the importance of such investigations and the need to achieve reliable, safe, and effective quantification and methods of determination.

The antimitotic Podophyllotoxin and its derivatives- recent synthetic advances

: The substantial antimitotic potential of podophyllotoxin and its derivatives has attracted both synthetic and medicinal chemists to expand the chemical space for the subsequent biological evaluation of these compounds. The interest ranges from total synthesis, hemi-synthesis, one-pot synthetic approaches and structure-activity relationship studies. In the first segment of the review, we present recent development in the synthesis of podophyllotoxin and also describe its mode of action. The second section covers the synthesis and the structure-activity relationships of podophyllotoxin derivatives, along with the discussion of important structural features required by the molecule for displaying antimitotic activity. The last part describes the synthesis and biological evaluation of potent 4-aza podophyllotoxin derivatives. This review is of interest to chemists who study natural and synthetic compounds for drug discovery.

Recent Reports of Plants as DNA Protection Agents

: DNA damage induced by reactive oxygen species (ROS) leads to cell death, tissue damage and may contribute towards the onset of several chronic diseases. Plants carry a cocktail of compounds like flavonoids, polyphenolics, tannins, saponins, terpenoids, and alkaloids that have shown promising pharmacological potential in treatingvarious illnessesresponsible for high mortality.Some of the plant-derived compounds carry the potential to shield the DNA fromdamage induced byreactive oxygen species(ROS). The objective of this article is to presentrecent reports of plant extracts and natural products as DNA protecting agents in one place. This review summarizes the plant-based extracts and isolated compounds with promising DNA protection activities against ROS induced damage. The antioxidant potential of plants is assessed using various antioxidant assays like DPPH assay, FRAP assay, and H2O2 assay. Further, the DNA protection of the extract is validated by using a plasmid protection assay. The mechanism of protection generally involves the scavenging of ROS by the antioxidants present in plant extracts. This review summarizes the work done on plant-based compounds for their antioxidant and DNA protection abilities invitro. However invivo evaluation of promising plants is the need of time.

Optimising Conditions for Encapsulation of Salacia chinensis Root Extract enriched with Phenolic Compounds

Background: S. chinensis extract contains bioactive compounds, which exhibit high antioxidant activities. However, for commercial uses, it is necessary to encapsulate the extract to protect it from degradation. Objective: This study aimed to optimise spray-drying conditions and then compare with freeze-drying to identify the most suitable conditions for encapsulation of Salacia chinensis L. root extract. Method: Three factors of spray-drying encapsulation, including maltodextrin concentration, inlet temperature and feed rate, have been tested for the impacts on the physical and phytochemical properties of S. chinensis root extract. Based on the optimal conditions, the spray-drying was then compared with freeze-drying. Results: The results showed that maltodextrin concentration, inlet temperature and feed rate had significant impacts on recovery yield, phenolics, mangiferin and antioxidant activity of the spray-dried extract. The optimal spray-drying encapsulation conditions were maltodextrin concentration of 20 %, inlet temperature of 130ºC and feed rate of 9 mL/min. Under these optimal conditions, the encapsulated extract had comparable solubility, total phenolics, mangiferin, and antioxidant activity, lower bulk density, moisture content, and water activity as compared to encapsulated extract made using the freeze-drying technique. These optimal spray-drying conditions are recommended to encapsulate the extract of S. chinensis root. Conclusion: Spray-drying was found to be more effective for encapsulation of S. chinensis root extract than freeze-drying. Therefore, spray-drying is recommended for further applications.