Search Results (31)

This study aimed to determine the chemical composition of the essential oils (EOs) of Ocimum basilicum L., as well as to evaluate the antibacterial, antidiabetic, dermatoprotective, and anti-inflammatory properties, and the EOs and aqueous extracts of O. basilicum. The antibacterial activity was evaluated against bacterial strains, Gram-positive and Gram-negative, using the well diffusion and microdilution methods, whereas the antidiabetic activity was assessed in vitro using two enzymes involved in carbohydrate digestion, α-amylase and α-glucosidase. On the other hand, the dermatoprotective and anti-inflammatory activities were studied by testing tyrosinase and lipoxygenase inhibition activity, respectively. The results showed that the chemical composition of O. basilicum EO (OBEO) is dominated by methyl chavicol (86%) and trans-anethol (8%). OBEO exhibited significant antibacterial effects against Gram-negative and Gram-positive strains, demonstrated by considerable diameters of the inhibition zones and lower MIC and MBC values. In addition, OBEO exhibited significant inhibition of α-amylase (IC₅₀ = 50.51 ± 0.32 μg/mL) and α-glucosidase (IC₅₀ = 39.84 ± 1.2 μg/mL). Concerning the anti-inflammatory activity, OBEO significantly inhibited lipoxygenase activity (IC₅₀ = 18.28 ± 0.03 μg/mL) compared to the aqueous extract (IC₅₀ = 24.8 ± 0.01 μg/mL). Moreover, tyrosinase was considerably inhibited by OBEO (IC₅₀ = 68.58 ± 0.03 μg/mL) compared to the aqueous extract (IC₅₀ = 118.37 ± 0.05 μg/mL). The toxicological investigations revealed the safety of O. basilicum in acute and chronic toxicity. The finding of in silico analysis showed that methyl chavicol and trans-anethole (main compounds of OBEO) validate the pharmacokinetics of these compounds and decipher some antibacterial targets. Full article

Alzheimer’s disease remains one of the most widespread neurodegenerative reasons for dementia worldwide and is associated with considerable mortality and morbidity. Therefore, it has been considered a priority for research. Indeed, several risk factors are involved in the complexity of the therapeutic ways of this pathology, including age, traumatic brain injury, genetics, exposure to aluminum, infections, diabetes, vascular diseases, hypertension, dyslipidemia, and obesity. The pathophysiology of Alzheimer’s disease is mostly associated with hyperphosphorylated protein in the neuronal cytoplasm and extracellular plaques of the insoluble β-amyloid peptide. Therefore, the management of this pathology needs the screening of drugs targeting different pathological levels, such as acetylcholinesterase (AchE), amyloid β formation, and lipoxygenase inhibitors. Among the pharmacological strategies used for the management of Alzheimer’s disease, natural drugs are considered a promising therapeutic strategy. Indeed, bioactive compounds isolated from different natural sources exhibit important anti-Alzheimer effects by their effectiveness in promoting neuroplasticity and protecting against neurodegeneration as well as neuroinflammation and oxidative stress in the brain. These effects involve different sub-cellular, cellular, and/or molecular mechanisms, such as the inhibition of acetylcholinesterase (AchE), the modulation of signaling pathways, and the inhibition of oxidative stress. Moreover, some nanoparticles were recently used as phytochemical delivery systems to improve the effects of phytochemical compounds against Alzheimer’s disease. Therefore, the present work aims to provide a comprehensive overview of the key advances concerning nano-drug delivery applications of phytochemicals for Alzheimer’s disease management. Full article

The objectives of this work were to determine the phytochemical composition and antioxidant, anti-diabetic, antibacterial, anti-inflammatory, and anti-acetylcholinesterase properties of Arbutus unedo L. and Laurus nobilis L. EOs. The antioxidant effects were estimated using four complementary methods. In addition, the anti-diabetic activity was assessed by targeting three carbohydrate-hydrolyzing enzymes, namely α-amylase, α-glucosidase, and lipase. The anti-inflammatory and anti-acetylcholinesterase effects were evaluated by testing the inhibitory potential of both plants on lipo-oxygenase and acetylcholinesterase (AChE), respectively. The antimicrobial activity of these oils was evaluated using disc-diffusion, minimum inhibitory concentration (MIC), and minimum lethal concentration (MLC) tests. The chemical composition of L. nobilis essential oil (EO) was dominated by eucalyptol (36.40%), followed by α-terpineole (13.05%), α-terpinyl acetate (10.61%), linalool (10.34%), and northujane (5.74%). The main volatile compounds of A. unedo EOs were decenal (13.47%), α-terpineol (7.8%), and palmitic acid (6.00%). L. nobilis and A. unedo EOs inhibited α-amylase with IC₅₀ values of 42.51 ± 0.012 and 102 ± 0.06 µg/mL, respectively. Moreover, both oils inhibited the activity of α-glucosidase (IC₅₀ = 1.347 ± 0.021 µg/mL and IC₅₀ = 76 ± 0.021 µg/mL) and lipase (IC₅₀ = 21.23 ± 0.021 µg/mL and IC₅₀ = 97.018 ± 0.012 µg/mL, respectively). In addition, L. nobilis EO showed an anti-AChE activity (IC₅₀ = 89.44 ± 0.07 µg/mL) higher than that of A. unedo EO (IC₅₀ = 378.57 ± 0.05 µg/mL). Regarding anti-inflammatory activity, in vitro assays showed that L. nobilis significantly inhibits (IC₅₀ = 48.31 ± 0.07 μg/mL) 5-lipoxygenase compared to A. unedo (IC₅₀ = 86.14 ± 0.05 μg/mL). This was confirmed in vivo via a notable inhibition of inflammation recorded after 6 h of treatment in both plants at a dose of 50 mg/kg. The microbiological results revealed that EOs from both plants inhibited the growth of all tested organisms except P. aeruginosa, with the highest antimicrobial effect for L. nobilis. The results of these tests showed that these two plants possess remarkable biological and pharmacological properties, explaining their medicinal effects and suggesting them as promising sources of natural drugs. Full article

The mammalian target of rapamycin (mTOR) is a highly conserved serine/threonine-protein kinase, which regulates many biological processes related to metabolism, cancer, immune function, and aging. It is an essential protein kinase that belongs to the phosphoinositide-3-kinase (PI3K) family and has two known signaling complexes, mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2). Even though mTOR signaling plays a critical role in promoting mitochondria-related protein synthesis, suppressing the catabolic process of autophagy, contributing to lipid metabolism, engaging in ribosome formation, and acting as a critical regulator of mRNA translation, it remains one of the significant signaling systems involved in the tumor process, particularly in apoptosis, cell cycle, and cancer cell proliferation. Therefore, the mTOR signaling system could be suggested as a cancer biomarker, and its targeting is important in anti-tumor therapy research. Indeed, its dysregulation is involved in different types of cancers such as colon, neck, cervical, head, lung, breast, reproductive, and bone cancers, as well as nasopharyngeal carcinoma. Moreover, recent investigations showed that targeting mTOR could be considered as cancer therapy. Accordingly, this review presents an overview of recent developments associated with the mTOR signaling pathway and its molecular involvement in various human cancer types. It also summarizes the research progress of different mTOR inhibitors, including natural and synthetised compounds and their main mechanisms, as well as the rational combinations with immunotherapies. Full article

Given the stochastic complexity of cancer diseases, the development of chemotherapeutic drugs is almost limited by problems of selectivity and side effects. Furthermore, an increasing number of protective approaches have been recently considered as the main way to limit these pathologies. Natural bioactive compounds, and particularly dietary phenolic compounds, showed major protective and therapeutic effects against different types of human cancers. Indeed, phenolic substances have functional groups that allow them to exert several anti-cancer mechanisms, such as the induction of apoptosis, autophagy, cell cycle arrest at different stages, and the inhibition of telomerase. In addition, in vivo studies show that these phenolic compounds also have anti-angiogenic effects via the inhibition of invasion and angiogenesis. Moreover, clinical studies have already highlighted certain phenolic compounds producing clinical effects alone, or in combination with drugs used in chemotherapy. In the present work, we present a major advance in research concerning the mechanisms of action of the different phenolic compounds that are contained in food medicinal plants, as well as evidence from the clinical trials that focus on them. Full article

Trichostatin A (TSA), a natural derivative of dienohydroxamic acid derived from a fungal metabolite, exhibits various biological activities. It exerts antidiabetic activity and reverses high glucose levels caused by the downregulation of brain-derived neurotrophic factor (BDNF) expression in Schwann cells, anti-inflammatory activity by suppressing the expression of various cytokines, and significant antioxidant activity by suppressing oxidative stress through multiple mechanisms. Most importantly, TSA exhibits potent inhibitory activity against different types of cancer through different pathways. The anticancer activity of TSA appeared in many in vitro and in vivo investigations that involved various cell lines and animal models. Indeed, TSA exhibits anticancer properties alone or in combination with other drugs used in chemotherapy. It induces sensitivity of some human cancers toward chemotherapeutical drugs. TSA also exhibits its action on epigenetic modulators involved in cell transformation, and therefore it is considered an epidrug candidate for cancer therapy. Accordingly, this work presents a comprehensive review of the most recent developments in utilizing this natural compound for the prevention, management, and treatment of various diseases, including cancer, along with the multiple mechanisms of action. In addition, this review summarizes the most recent and relevant literature that deals with the use of TSA as a therapeutic agent against various diseases, emphasizing its anticancer potential and the anticancer molecular mechanisms. Moreover, TSA has not been involved in toxicological effects on normal cells. Furthermore, this work highlights the potential utilization of TSA as a complementary or alternative medicine for preventing and treating cancer, alone or in combination with other anticancer drugs. Full article

Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmasterol has been examined via in vitro and in vivo assays and molecular docking for its various biological activities on different metabolic disorders. The findings indicate potent pharmacological effects such as anticancer, anti-osteoarthritis, anti-inflammatory, anti-diabetic, immunomodulatory, antiparasitic, antifungal, antibacterial, antioxidant, and neuroprotective properties. Indeed, stigmasterol from plants and algae is a promising molecule in the development of drugs for cancer therapy by triggering intracellular signaling pathways in numerous cancers. It acts on the Akt/mTOR and JAK/STAT pathways in ovarian and gastric cancers. In addition, stigmasterol markedly disrupted angiogenesis in human cholangiocarcinoma by tumor necrosis factor-α (TNF-α) and vascular endothelial growth factor receptor-2 (VEGFR-2) signaling down-regulation. The association of stigmasterol and sorafenib promoted caspase-3 activity and down-regulated levels of the anti-apoptotic protein Bcl-2 in breast cancer. Antioxidant activities ensuring lipid peroxidation and DNA damage lowering conferred to stigmasterol chemoprotective activities in skin cancer. Reactive oxygen species (ROS) regulation also contributes to the neuroprotective effects of stigmasterol, as well as dopamine depletion and acetylcholinesterase inhibition. The anti-inflammatory properties of phytosterols involve the production of anti-inflammatory cytokines, the decrease in inflammatory mediator release, and the inhibition of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Stigmasterol exerts anti-diabetic effects by reducing fasting glucose, serum insulin levels, and oral glucose tolerance. Other findings showed the antiparasitic activities of this molecule against certain strains of parasites such as Trypanosoma congolense (in vivo) and on promastigotes and amastigotes of the Leishmania major (in vitro). Some stigmasterol-rich plants were able to inhibit Candida albicans, virusei, and tropicalis at low doses. Accordingly, this review outlines key insights into the pharmacological abilities of stigmasterol and the specific mechanisms of action underlying some of these effects. Additionally, further investigation regarding pharmacodynamics, pharmacokinetics, and toxicology is recommended. Full article

Despite the significant advances and mechanistic understanding of tumor processes, therapeutic agents against different types of cancer still have a high rate of recurrence associated with the development of resistance by tumor cells. This chemoresistance involves several mechanisms, including the programming of glucose metabolism, mitochondrial damage, and lysosome dysfunction. However, combining several anticancer agents can decrease resistance and increase therapeutic efficacy. Furthermore, this treatment can improve the effectiveness of chemotherapy. This work focuses on the recent advances in using natural bioactive molecules derived from phenolic compounds isolated from medicinal plants to sensitize cancer cells towards chemotherapeutic agents and their application in combination with conventional anticancer drugs. Dietary phenolic compounds such as resveratrol, gallic acid, caffeic acid, rosmarinic acid, sinapic acid, and curcumin exhibit remarkable anticancer activities through sub-cellular, cellular, and molecular mechanisms. These compounds have recently revealed their capacity to increase the sensitivity of different human cancers to the used chemotherapeutic drugs. Moreover, they can increase the effectiveness and improve the therapeutic index of some used chemotherapeutic agents. The involved mechanisms are complex and stochastic, and involve different signaling pathways in cancer checkpoints, including reactive oxygen species signaling pathways in mitochondria, autophagy-related pathways, proteasome oncogene degradation, and epigenetic perturbations. Full article

The search for natural plant-based products as new pharmacological alternatives to treat various human pathologies has taken on great importance for researchers and research laboratories. In this context, research has intensified to extract and identify natural molecules endowed with biological effects. The objective of this study is to review the source and pharmacological properties of cirsimaritin. The identification and isolation of this flavonoid from various natural sources, including medicinal plants such as Artemisia judaica, Cirsium japonicum, Lithocarpus dealbatus, Microtea debilis, and Ocimum sanctum, has been carried out and verified using different spectral techniques. Biological effect investigations are carried out with a wide variety of experimental models in vitro and in vivo and laboratory techniques. The results of these research works showed the biological properties of cirsimaritin including anticancer, antimicrobial, antidiabetic, antiparasitic, antioxidant, and anti-inflammatory effects. The mechanisms involved in the multiple activities of this molecule are diverse and include sub-cellular, cellular, and molecular levels. Indeed, this bioactive induces anti-inflammatory and antiproliferative effects by inhibiting cell membrane receptors, interference with signaling pathways, and inhibiting transcriptional factors such as Nf-κB involved in cell promotion and proliferation. In the light of these results, cirsimaritin appears as a promising and viable alternative natural bioactive drug to treat many pathological conditions. Full article

This exploratory investigation aimed to determine the chemical composition and evaluate some biological properties, such as antioxidant, anti-inflammatory, antidiabetic, and antimicrobial activities, of Matricaria chamomilla L. essential oils (EOs). EOs of M. chamomilla were obtained by hydrodistillation and phytochemical screening was performed by gas chromatography–mass spectrophotometry (GC-MS). The antimicrobial activities were tested against different pathogenic strains of microorganisms by using disc diffusion assay, the minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) methods. The antidiabetic activity was performed in vitro using the enzyme inhibition test. The antioxidant activity of EOs was tested using the free radical scavenging ability (DPPH method), ferrous ion chelating (FIC) ability, and β-carotene bleaching assay. The anti-inflammatory effects were tested in vivo using the carrageenan-induced paw edema method and in vitro using the inhibition of the lipoxygenase test. The analysis of the phytochemical composition by GC-MS revealed that camphor (16.42%) was the major compound of EOs, followed by 3-carene (9.95%), β-myrcene (8.01%), and chamazulene (6.54%). MCEO, honey, and their mixture exhibited antioxidant activity against the DPPH assay (IC₅₀ ranging from 533.89 ± 15.05 µg/mL to 1945.38 ± 12.71 µg/mL). The mixture exhibited the best radical scavenging activity, with an IC₅₀ of 533.89 ± 15.05 µg/mL. As antidiabetic effect, EO presented the best values against α-glucosidase (265.57 ± 0.03 μg/mL) and α-amylase (121.44 ± 0.05 μg/mL). The EOs and honey mixture at a dose of 100 mg/kg exhibited a high anti-inflammatory effect, with 63.75% edema inhibition after 3 h. The impact of EOs on the studied species showed an excellent antimicrobial (Staphylococcus aureus ATCC 29213 (22.97 ± 0.16 mm)), antifungal (Aspergillus niger (18.13 ± 0.18 mm)) and anti-yeast (Candida albicans (21.07 ± 0.24 mm) effect against all the tested strains. The results obtained indicate that the EOs of M. chamomilla could be a potential drug target against diabetes, inflammation and microbial infections; however, further investigations to assess their bioactive molecules individually and in combination are greatly required. Full article

The aim of this work was the determination of Pelargonium graveolens (aerial parts) volatile compounds at three developmental stages and the evaluation of their antioxidant, antidiabetic, dermaprotective, anti-inflammatory, and antibacterial effects. The aerial parts of Pelargonium graveolens were collected at three stages, namely the vegetative, beginning, and full flowering. Pelargonium graveolens essential oils were extracted from the dried materials of these aerial parts by hydrodistillation. The volatiles were analyzed by Gas Chromatography-Mass Spectrometry GC-MS, and the antioxidant activity was assessed by DPPH, ABTS, H₂O₂, and FRAP assays. The in vitro antidiabetic effect was evaluated by the inhibition of α-amylase, α-glucosidase, and lipase enzymes, while the antibacterial activity was assessed against six bacterial strains using an agar well diffusion assay and a microdilution method. The main constituents were menthol, menthene, eremophilene, isoborneol, isogeraniol, α-pinene, linalyl acetate, and 3-carene, with quantitative differences at the three phenological stages. The essential oil at the full flowering stage showed the best antioxidant activity, with IC₅₀ values of 83.26 ± 0.01, 116.42 ± 0.07, 132.25 ± 0.11, and 48.67 ± 0.04 μg/mL for DPPH, FRAP, ABTS, and H₂O₂ assays, respectively. This oil also exhibited significant effects against α-amylase (IC₅₀ = 43.33 ± 0.01 μg/mL), α-glucosidase (IC₅₀ = 19.04 ± 0.01 μg/mL), lipase (IC₅₀ = 24.33 ± 0.05 μg/mL), 5-lipoxygenase (IC₅₀ = 39.31 ± 0.01 μg/mL), and tyrosinase (IC₅₀ = 124.49 ± 0.07 μg/mL). The essential oil extracted at the full flowering stage showed the best antibacterial effect against a panel of microorganisms with diameter inhibition zones ranging between 11.00 ± 0.17 mm and 17.30 ± 0.17 mm and MIC values from 0.25% to 2% v/v. Overall, the results presented here suggest that the full flowering stage is the best optimal harvest time of Pelargonium graveolens for food and pharmaceutical applications. Full article

Salvia officinalis is a medicinal plant used to treat some diseases, including microbial infections and diabetes. Different studies showed the biological and pharmacological properties of this species. The aim of this study was the determination of the chemical compounds of S. officinalis essential oils and the investigation of their antimicrobial, antioxidant, antidiabetic, and anti-inflammatory properties. The chemical compounds of S. officinalis were determined by GC-MS analysis. The antioxidant activity was assessed by DPPH, ABTS, H₂O₂, and FRAP assays. The in vitro antidiabetic effect was evaluated by the inhibition of α-amylase, α-glucosidase, and lipase activities, and the anti-inflammatory effect was evaluated using the 5-lipoxygenase assay. Moreover, antibacterial activity was assessed against six bacterial strains using agar well diffusion assay and microdilution method. The main compounds in essential oils of S. officinalis at three phenological stages were naphthalenone, camphor, 1.8-cineole, and α-thujone. The full flowering stage essential oil showed the best antioxidant activity with different IC₅₀ values according to the used tests. This oil also exhibited important inhibitory effects at the full flowering stage against α-amylase (IC₅₀ = 69.23 ± 0.1 μg/mL), α-glucosidase (IC₅₀ = 22.24 ± 0.07 μg/mL), and lipase (IC₅₀ = 37.3 ± 0.03 μg/mL). The 5-lipoxygenase inhibitory effect was the best at the full flowering stage (IC₅₀ = 9.24 ± 0.03 μg/mL). The results of the antibacterial evaluation revealed that, at three seasonal periods, S. officinalis essential oil demonstrated strong antibacterial activity. Although the full flowering stage had the best antibacterial activity, there were no significant differences between the three stages. Additionally, the essential oils showed bactericidal effects on Listeria monocytogenes, Staphylococcus aureus, Bacillus subtilis, Proteus mirabilis, Escherichia coli, and Salmonella typhimurium, respectively. The findings of this work showed remarkably that S. officinalis synthesizes essential oils according to different developmental stages. Moreover, it has exhibited interesting biological and pharmacological properties justifying its medicinal effects and suggesting it as a very important source of natural drugs. Full article

Eucalyptus globulus is a plant widely used by the world population, including Morocco, in the treatment of several pathologies. The aim of this work is to evaluate the antioxidant, anti-inflammatory, dermatoprotective, and antimicrobial effects of essential oil and honey from E. globulus, as well as their combination. Chemical composition was determined by GC-MS analysis. The antioxidant activity was evaluated by three tests, namely, DPPH, reducing power, and the β-carotene/linoleic acid assay. The anti-inflammatory activity was investigated in vitro (5-lipoxygenase inhibition) and in vivo (carrageenan-induced paw edema model), while the dermatoprotective activity was tested in vitro (tyrosinase inhibition). Moreover, the antibacterial activity was assessed using agar well diffusion and microdilution methods. The results showed that eucalyptol presents the main compound of the essential oil of E. globulus (90.14%). The mixture of essential oil with honey showed the best antioxidant effects for all the tests used (0.07 < IC₅₀ < 0.19 mg/mL), while the essential oil was the most active against tyrosinase (IC₅₀ = 38.21 ± 0.13 μg/mL) and 5-lipoxygenase (IC₅₀ = 0.88 ± 0.01 μg/mL), which corroborated the in vivo test. Additionally, the essential oil showed the best bactericidal effects against all strains tested, with inhibition diameter values ranging from 12.8 to 21.6 mm. The findings of this work showed that the combination of the essential oil with honey showed important results in terms of biological activity, but the determination of the underlying mechanisms of action remains a major prospect to be determined. Full article

A flavone, chrysoeriol is synthetized in several plant species. It comes from several natural sources, especially medicinal plants. The identification and isolation of this compound has been carried out and verified by several research teams using different spectral methods. It seems that the concentration of this molecule is variable and fluctuating depending on the source, the part extracted, the region, and the methods of extraction and characterization. The aim of this paper is to highlight the in vitro and in vivo pharmacological properties of chrysoeriol and to provide insight into its pharmacokinetics. Anticancer, anti-inflammatory, antibacterial, antifungal, anti-osteoporosis, anti-insecticide, and neuroprotective actions have been shown in a number of studies on this chemical. Different mechanisms in theses pharmacological effects include subcellular, cellular, and molecular targets. In vivo pharmacokinetic analysis has proved the good stability of this molecule, showing its promising potential to prevent or treat diseases including cancer, diabetes, inflammation, osteoporosis, Parkinson’s disease, and cardiovascular diseases. Full article

Pinosylvin (3,5-dihydroxy-trans-stilbene), a natural pre-infectious stilbenoid toxin, is a terpenoid polyphenol compound principally found in the Vitaceae family in the heartwood of Pinus spp. (e.g., Pinus sylvestris) and in pine leaf (Pinus densiflora). It provides defense mechanisms against pathogens and insects for many plants. Stilbenoids are mostly found in berries and fruits but can also be found in other types of plants, such as mosses and ferns. This review outlined prior research on pinosylvin, including its sources, the technologies used for its extraction, purification, identification, and characterization, its biological and pharmacological properties, and its toxicity. The collected data on pinosylvin was managed using different scientific research databases such as PubMed, SciFinder, SpringerLink, ScienceDirect, Wiley Online, Google Scholar, Web of Science, and Scopus. In this study, the findings focused on pinosylvin to understand its pharmacological and biological activities as well as its chemical characterization to explore its potential therapeutic approaches for the development of novel drugs. This analysis demonstrated that pinosylvin has beneficial effects for various therapeutic purposes such as antifungal, antibacterial, anticancer, anti-inflammatory, antioxidant, neuroprotective, anti-allergic, and other biological functions. It has shown numerous and diverse actions through its ability to block, interfere, and/or stimulate the major cellular targets responsible for several disorders. Full article