Current Topics in Medicinal Chemistry - Volume 21, Issue 29, 2021

Background: Traditionally, the Algerian medicinal plant Elaeosilenum thapsioides (Desf.) Maire has been used for many diseases. The present research work aims to explore the chemical and biological characterization of its essential oil. Methods: The essential oils were obtained by hydrodistillation of different Elaeosilenum thapsioides (Apiaceae) aerial parts samples collected from two different regions (Mahouane and Megres) from Setif, Eastern Algeria. The chemical characterization of the obtained essential oils is reported here for the first time. Besides, they were evaluated for their in vitro Acetylcholinesterase (AChE) inhibitory activity involved in Alzheimer’s disease using Ellman’s spectrophotometric method. Results: Additionally, their in vitro antimicrobial activity was assessed by the disc diffusion method. Both activities were performed at various oil concentrations. The GC/MS analysis of the essential oils from aerial parts (leaves, stems, flowers, and seeds) of E. thapsioides identified 47 constituents. Monoterpene hydrocarbons were the main components, ranging from 72.78 to 99.13%. Oxygenated monoterpenes and oxygenated sesquiterpenes ranged between 1.37 and 17.25% and 0.12 and 3.53% in essential oils from leaves and stems. Sesquiterpene hydrocarbons were present in small to large quantities in the essential oils of both populations, ranging from 0.69 to 13.44%. The presence of m-Methoxybenzyl isothiocyanate was recorded in stems essential oils from Mahouane and leaves essential oils from Merges, which was 9.73% and 3.72%, respectively. Conclusion: The stems essential oils obtained from plants collected in Mahouane showed the highest AChE inhibitory activity. The highest anti-bacterial activity was shown by the essential oil obtained from Megres leaves against Bacillus cereus ATCC 11778. The oils exhibited a moderate inhibitory activity in both tests.

Euglena, a microalga, has gained a great attention as it contains several bioactive compounds including food supplements, drugs and biofuels. The genus Euglena includes >300 species of unicellular, fresh water flagellates. The objective of this review article concerns the presentation of updated information on pharmacological and therapeutic properties and industrial implications of molecules isolated from Euglena species. A bibliographic search of scientific literature published till March, 2020 was made from scientific databases using different search engines. Euglena produces several antioxidant molecules, such as β-carotene, L-ascorbic acid, polymers of unsaturated fatty acids and phytotoxins useful in manufacturing many pharmaceutical, cosmetics, and nutraceutical compounds. It is a rich source of antimicrobial, anticancer, immunomodulatory compounds. Though, several studies have indicated its therapeutic applications, extensive research is needed to explore its efficacy against many pathophysiological conditions including toxicity assessment of compound(s). Nevertheless, the biotechnological influence on industrial production of Euglena has been less exploited.

Phytochemicals are the most valuable and comprehensive structures, which may have a broad range of protective benefits, from reducing inflammation and speeding healing to preventing infection and fighting cancer. Resveratrol (RSV) is a natural phenolic compound from the oligomeric stilbenoids group, which is usually found in daily human diet, such as grape, peanut, berries and grains. It exhibits anti-inflammatory, neuroprotective, antioxidant, and cancer prevention and treatment effects. RSV is thought to have an impressive outcome in colorectal cancer (CRC) treatment through the vital molecules and cancer signaling pathways, including SIRT1, P53, P21, AMPK, ROS, BMP7, COX-2, NO, caspases, Wnt, TNFs, NF-ΚB, EMT, and pentose phosphate pathway. Therefore, this paper reviews the current researches on the pharmacological effects and pharmacokinetics of resveratrol and its drug delivery system, as well as clinical studies involving CRC.

Cyclophosphamide (CP) is an extensively used anticancer drug, but its cardiotoxic manifestation is a major concern for its widespread clinical use. The observed cardiotoxic attributes have been reported at the therapeutic dose and often result into a high mortality rate and poor clinical outcome. Fall in the level of antioxidant enzymes catalase (CAT), reduced glutathione (GSH), superoxide dismutase (SOD) generation of reactive oxygen species (ROS), inflammatory cytokines nuclear factor kappa-light-chain enhancer of activated B cells (NF-kB), tumor necrosis factor-alpha (TNF-α), interleukin 1 beta (IL- 1β), apoptotic proteins (caspases) and direct damage to myocardial tissue (histological and ultrastructural damage) are some of the reported manifestations of cardiotoxicity. The observed clinical attributes of CP-induced cardiotoxicity are myocarditis, hemorrhage, thrombosis, myocardial infarction (MI), reduced ejection fraction, altered electrocardiogram (ECG) reading and heart failure. However, unlike Daxarazasone (an adjuvant to reduce doxorubicin-induced cardiotoxicity), no approved adjuvant is available to mitigate CPinduced cardiotoxicity. Thus, various natural bioactives have been explored for the possible cardioprotective effect against CP-induced cardiotoxicity. In the current manuscript, we have discussed the clinical and preclinical aspects of CP-induced cardiotoxicity, its clinically used combination with other anticancer drugs, and the available therapeutic regimen to mitigate this cardiotoxicity. Further, we discussed the limitations of available synthetic drugs used as an adjuvant and discussed various natural bioactive and their experimental details. This manuscript's overall goal is to throw light on CP-induced cardiotoxicity and summarize all the experimental data so that researchers working in this field may scientifically get up-to-date information in one place.

Gynura procumbens (Lour.) Merr. is a well-known plant used in folkloric medicine in tropical Asian countries. The plant is prevalently employed by traditional healers in the treatment of diabetes, cancer, hypertension, inflammation, fever, and skin disorders. Several scientific studies reported that Gynura procumbens possesses considerable therapeutic value for the development of emerging treatment options. The diverse pharmacological effects of this plant are attributed to its vast phytoconstituent content. Different chemical classes, including alkaloids, flavonoids, phenolics, steroids, proteins, and polysaccharides, have been isolated from this plant. In this review, we tried to explore the different aspects of Gynura procumbens as an established medicinal plant. The data gathered here give an indication that the plant Gynura procumbens is a good natural source of chemical compounds with different types of pharmacological actions, and these chemical compounds can be used as models for the development of de novo therapeutic agents.