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1.
Foods ; 13(15)2024 Jul 23.
Article in English | MEDLINE | ID: mdl-39123499

ABSTRACT

Antispasmodic agents are crucial in managing gastrointestinal motility disorders by modulating muscle contractions and reducing symptoms like cramping and diarrhea. This study investigated the antispasmodic potential of different coffee bean extracts, including light coffee (LC), medium coffee (MC), and dark coffee (DC), on ileum contractions induced by potassium chloride (KCl), and elucidated their mechanisms of action using in vitro isolated tissue techniques. The results demonstrated that all coffee extracts reduced spontaneous contractions of rat ileum tissue in a dose-dependent manner. Among these, LC showed the most significant reduction in ileum contractions, particularly at higher concentrations. The key findings reveal that LC at 5 mg/mL significantly reduced CaCl2-induced contractions in isolated rat ileum tissue, indicating that LC may inhibit calcium influx or interfere with calcium signaling pathways. The presence of nifedipine, propranolol, and N-nitro-L-arginine methyl ester (L-NAME) have been confirmed in their involvement; they block calcium influx and calcium channels and activate ß-adrenergic pathways as part of LC's mechanism of action. The presence of their active compounds, particularly chlorogenic acid and caffeine, likely contributes to the observed antispasmodic effects. These findings suggest that LC exerts its antispasmodic effects by targeting key mechanisms involved in muscle spasms and intestinal motility, providing a potential for managing such conditions.

2.
Foods ; 13(15)2024 Aug 02.
Article in English | MEDLINE | ID: mdl-39123636

ABSTRACT

BACKGROUND: Coffee leaves are a major source of bioactive components and are used as ethnomedicine. However, despite their traditional medicinal use, information about their effects on antihyperlipidemia remains limited. METHODS: The aims of this study were to evaluate the main components of leaf extracts from Arabica and Robusta coffees and to examine the potential of these coffee leaves in reducing lipid digestion and absorption in vitro. RESULTS: Coffee leaf extracts from Arabica coffee contain a high amount of caffeine, whereas extracts from Robusta coffee contain high amounts of chlorogenic acid (CGA) and caffeine. Additionally, leaf extracts from Arabica and Robusta coffee demonstrated the inhibition of pancreatic lipase, decreased micellar cholesterol solubility, and reduced bile acid binding. Furthermore, these extracts resulted in a reduction in cholesterol uptake in Caco-2 cells. Molecular docking experiments supported this discovery, showing CGA and caffeine binding to Niemann-Pick C1-like 1 (NPC1L1), a key protein in cholesterol absorption. The results indicated that CGA and caffeine can competitively bind to NPC1L1 at the cholesterol binding pocket, reducing its cholesterol binding rate. These findings suggest that coffee leaves might help suppress lipid absorption and digestion, highlighting their potential use in preventing and treating hyperlipidemia.

3.
Article in English | MEDLINE | ID: mdl-39126576

ABSTRACT

Nanoparticulate drug delivery systems (NDDS) based nanoformulations have emerged as promising drug delivery systems. Various NDDS-based formulations have been reported such as polymeric nanoparticles (NPs), nanoliposomes, solid lipid NPs, nanocapsules, liposomes, self-nano emulsifying drug delivery systems, pro liposomes, nanospheres, microemulsion, nanoemulsion, gold NPs, silver NPs and nanostructured lipid carrier. They have shown numerous advantages such as enhanced bioavailability, aqueous solubility, permeability, controlled release profile, and blood-brain barrier (BBB) permeability. This advantage of NDDS can help to deliver pure drugs to the target site. However, the formulation of nanoparticles is a complex process that requires optimization to ensure product quality and efficacy. Quality by Design (QbD) is a systemic approach that has been implemented in the pharmaceutical industry to improve the quality and reliability of drug products. QbD involves the optimization of different parameters like zeta potential (ZP), particle size (PS), entrapment efficiency (EE), polydispersity index (PDI), and drug release using statistical experimental design. The present article discussed the detailed role of QbD in optimizing nanoformulations and their advantages, advancement, and applications from the industrial perspective. Various case studies of QbD in the optimization of nanoformulations are also discussed.

4.
Pathol Res Pract ; 261: 155490, 2024 Jul 25.
Article in English | MEDLINE | ID: mdl-39126977

ABSTRACT

Pyroptosis is an inflammatory programed cell death process that plays a crucial role in cancer therapeutic, while Gasdermin-D is a critical effector protein for pyroptosis execution. This review discusses the intricate interactions between Gasdermin-D and some non-coding RNAs (lncRNA, miRNA, siRNA) and their potential application in the regulation of pyroptosis as an anticancer therapy. Correspondingly, these ncRNAs significantly implicate in Gasdermin-D expression and function regarding the pyroptosis pathway. Functioning as competing endogenous RNAs (ceRNAs), these ncRNAs might regulate Gasdermin-D at the molecular level, underlying fatal cell death caused by cancer and tumor propagation. Therefore, these interactions appeal to therapeutics, offering new avenues for cancer treatment. It address this research gap by discussing the possible roles of ncRNAs as mediators of gasdermin-D regulation. It suggest therapeutic strategies based on the current research findings to ensure the interchange between the ideal pyroptosis and cancer cell death.

5.
Food Chem X ; 23: 101580, 2024 Oct 30.
Article in English | MEDLINE | ID: mdl-39027685

ABSTRACT

The aims of this study are the phytochemical exploration and food valorization of Schinus molle L. (S. molle) and Schinus terebinthifolia Raddi (S. terebinthifolia) from the Rabat, Morocco. Gas chromatography (GC) and high-performance liquid chromatography (HPLC) were used to analyze the chemical composition of the oils extracted from both species by soxhlet and maceration. Moreover, physicochemical characteristics such as lipid quality indexes such as thrombogenic index (TI), atherogenic index (AI), oxidation susceptibility (OS), and calculated oxidability (Cox) were determined. These characteristics included percentage acidity, peroxide, saponification, iodine, specific extinction values, chlorophyll, and carotenoid pigments. As results, the oil yields varied from 7% (S. molle) to 13% (S. terebinthifolia). In addition, unsaturated fatty acids represented the major fraction for S. terebinthifolia (79%) and S. molle (81%). However, S. terebinthifolia contains more saturated fatty acids (20%) than S. molle (16%) with a predominance of linoleic acid (59.53% and 55%, C18,2), oleic acid (19.29% and 21.69%, C18,1), and palmitic acid (12.56% and 15.48%, C16,0) in S. molle and S. terebinthifolia, respectively. Moreover, the main sterols are ß-sitosterol followed by campesterol and then Δ-5-avenasterol, while ß-sitosterol varies according to the species and the extraction method. Results revealed also that campesterol is influenced by the extraction results in a content of 179.66 mg/kg (soxhlet) and 63.48 mg/kg (maceration) for S. molle, while S. terebinthifolia yeilds concentrations of 170 mg/kg and 138 mg/kg, then Δ-5-avenasterol, which present with (117 mg/kg and 136 mg/kg), (34 mg/kg and 80 mg/kg) of the total amount of sterols for the oils extracted by soxhlet and maceration, respectively. In addition, there are favorable physicochemical properties for all oils, such as chlorophylls (0.4 to 0.8 mg/kg) and carotenoids (0.7 to 2 mg/kg). However, further investigations are needed to determine other chemical compounds of both extracts as well as to evaluate their biological and health benefits.

6.
Colloids Surf B Biointerfaces ; 241: 114051, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38954935

ABSTRACT

There has been a surge in effort in the development of various solid nanoparticles as Pickering emulsion stabilizers in the past decades. Regardless, the exploration of stabilizers that simultaneously stabilize and deliver bioactive has been limited. For this, liposomes with amphiphilic nature have been introduced as Pickering emulsion stabilizers but these nano-sized vesicles lack targeting specificity. Therefore in this study, superparamagnetic iron oxide nanoparticles (SPION) encapsulated within liposomes (MLP) were used as Pickering emulsion stabilizers to prepare pH and magnetic-responsive Pickering emulsions. A stable MLP-stabilized Pickering emulsion formulation was established by varying the MLP pH, concentration, and oil loading during the emulsification process. The primary stabilization mechanism of the emulsion under pH variation was identified to be largely associated with the MLP phosphate group deprotonation. When subjected to sequential pH adjustment to imitate the gastrointestinal digestion pH environment, a recovery in Pickering emulsion integrity was observed as the pH changes from acidic to alkaline. By incorporating SPION, the Pickering emulsion can be guided to the targeted site under the influence of a magnetic field without compromising emulsion stability. Overall, the results demonstrated the potential of MLP-stabilized Pickering emulsion as a dual pH- and magnetic-responsive drug delivery carrier with the ability to co-encapsulate hydrophobic and hydrophilic bioactive.


Subject(s)
Emulsions , Liposomes , Magnetic Iron Oxide Nanoparticles , Emulsions/chemistry , Liposomes/chemistry , Hydrogen-Ion Concentration , Magnetic Iron Oxide Nanoparticles/chemistry , Particle Size , Magnetite Nanoparticles/chemistry
7.
J Tradit Complement Med ; 14(4): 355-380, 2024 Jul.
Article in English | MEDLINE | ID: mdl-39035692

ABSTRACT

Dittrichia viscosa is a perennial herb that has been used for generations in traditional medicine to address a variety of diseases, including diabetes, hypertension, cancer, microbial disorders, inflammatory conditions, and wound healing. The objective of this review is to provide an overview of existing knowledge on D. viscosa with regards to its botanical description, ethnomedicinal uses, and pharmacological properties. Databases such as Scopus, Wiley-Online, PubMed, Springer, Google Scholar, and ScienceDirect were used to select relevant articles based on their title and abstract. The reviewed studies found a strong correlation between D. viscosa's traditional uses and its observed biological effects. Pharmacological research has shown that the essential oils and extracts from D. viscosa possess a variety of biological activities, such as anti-inflammatory, anticancer, antibacterial, antifungal, analgesic, and antioxidant properties. The chemical compounds found in D. viscosa include sesquiterpenes, monoterpenes, flavonoids, and phenolic acids; some of these compounds, such as tometosin and inuviscolide, have been isolated and displayed promising cytotoxic and anti-inflammatory activity. The present review suggests that the pharmacological properties of D. viscosa align well with its ethnomedicinal uses. These findings support the traditional use of D. viscosa in treating various illnesses. Additionally, toxicological examinations of D. viscosa extracts and essential oil have demonstrated the plant's safety, which supports the need for comprehensive pharmacological studies, in vivo studies, and clinical trials to evaluate the best doses for optimal medicinal effects. This work underscores the medicinal value of D. viscosa and its potential in developing new pharmacological agents to address major health challenges like antibiotic resistance and cancers.

8.
Health Sci Rep ; 7(6): e2120, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38831777

ABSTRACT

Background and Aims: Natural products are widely used in the pharmaceutical and cosmetics industries due to their high-value bioactive compounds, which make for "greener" and more environmentally friendly ingredients. These natural compounds are also considered a safer alternative to antibiotics, which may result in antibiotic resistance as well as unfavorable side effects. The development of cosmeceuticals, which combine the cosmetic and pharmaceutical fields to create skincare products with therapeutic value, has increased the demand for unique natural resources. The objective of this review is to discuss the biological properties of extracts derived from larvae of the black soldier fly (BSF; Hermetia illucens), the appropriate extraction methods, and the potential of this insect as a novel active ingredient in the formulation of new cosmeceutical products. This review also addresses the biological actions of compounds originating from the BSF, and the possible association between the diets of BSF larvae and their subsequent bioactive composition. Methods: A literature search was conducted using PubMed and Google Scholar to identify and evaluate the various biological properties of the BSF. Results: One such natural resource that may be useful in the cosmeceutical field is the BSF, a versatile insect with numerous potential applications due to its nutrient content and scavenging behavior. Previous research has also shown that the BSF has several biological properties, including antimicrobial, antioxidant, anti-inflammatory, and wound healing effects. Conclusion: Given the range of biological activities and metabolites possessed by the BSF, this insect may have the cosmeceutical potential to treat a number of skin pathologies.

9.
Drug Deliv Transl Res ; 14(9): 2325-2344, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38758498

ABSTRACT

Skin cancer remains one of the most prominent types of cancer. Melanoma and non-melanoma skin cancer are commonly found together, with melanoma being the more deadly type. Skin cancer can be effectively treated with chemotherapy, which mostly uses small molecular medicines, phytoceuticals, and biomacromolecules. Topical delivery of these therapeutics is a non-invasive way that might be useful in effectively managing skin cancer. Different skin barriers, however, presented a major obstacle to topical cargo administration. Transferosomes have demonstrated significant potential in topical delivery by improving cargo penetration through the circumvention of diverse skin barriers. Additionally, the transferosome-based gel can prolong the residence of drug on the skin, lowering the frequency of doses and their associated side effects. However, the choice of appropriate transferosome compositions, such as phospholipids and edge activators, and fabrication technique are crucial for achieving improved entrapment efficiency, penetration, and regulated particle size. The present review discusses skin cancer overview, current treatment strategies for skin cancer and their drawbacks. Topical drug delivery against skin cancer is also covered, along with the difficulties associated with it and the importance of transferosomes in avoiding these difficulties. Additionally, a summary of transferosome compositions and fabrication methods is provided. Furthermore, topical delivery of small molecular drugs, phytoceuticals, and biomacromolecules using transferosomes and transferosomes-based gel in treating skin cancer is discussed. Thus, transferosomes can be a significant option in the topical delivery of drugs to manage skin cancer efficiently.


Subject(s)
Antineoplastic Agents , Liposomes , Skin Neoplasms , Humans , Skin Neoplasms/drug therapy , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/therapeutic use , Antineoplastic Agents/chemistry , Animals , Administration, Cutaneous , Drug Delivery Systems , Skin Absorption
10.
Cytotherapy ; 26(8): 785-789, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38775774

ABSTRACT

In recent years, Malaysia has seen a surge in stem cell therapy for various medical conditions. However, the regulation of stem cell research and therapy in Malaysia faces several challenges such as the emergence of unregulated clinics and a lack of specific legislation. Some urgent measures, including enactment of specific laws, strengthened monitoring, as well as increased public awareness and education, are crucial. Therefore, stem cell therapy regulation requires concerted efforts by the policymakers, regulator bodies and healthcare professionals. This commentary discusses the current guidelines and challenges in Malaysian stem cell therapy regulation and proposes some future recommendations that could pave the way for responsible progress of stem cell research and therapy globally.


Subject(s)
Stem Cell Research , Stem Cell Transplantation , Humans , Stem Cell Research/legislation & jurisprudence , Stem Cell Transplantation/legislation & jurisprudence , Stem Cell Transplantation/methods , Malaysia , Guidelines as Topic , Stem Cells/cytology , Cell- and Tissue-Based Therapy/methods
11.
Biomed Pharmacother ; 176: 116744, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38810399

ABSTRACT

Cancer is one of the major leading causes of mortality globally and chemo-drug-resistant cancers pose significant challenges to cancer treatment by reducing patient survival rates and increasing treatment costs. Although the mechanisms of chemoresistance vary among different types of cancer, cancer cells are known to share several hallmarks, such as their resistance to apoptosis as well as the ability of cancer stem cells to produce metastatic daughter cells that are resistant to chemotherapy. To address the issue of chemo-drug resistance in cancer cells, a tetracistronic expression construct, Ad-MBR-GFP, encoding adenovirus-mediated expression of MOAP-1, Bax, RASSSF1A, and GFP, was generated to investigate its potential activity in reducing or inhibiting the chemo-drug resistant activity of the human breast cancer cells, MCF-7-CR and MDA-MB-231. When infected by Ad-MBR-GFP, the cancer cells exhibited round cell morphology and nuclei condensation with positive staining for annexin-V. Furthermore, our results showed that both MCF-7-CR and MDA-MB-231 cells stained positively for CD 44 and negatively for CD 24 (CD44+/CD24-) with high levels of endogenous ALDH activity whereas SNU-1581 breast cancer cells were identified as CD 44-/CD 24- cells with relatively low levels of endogenous ALDH activity and high sensitivity toward chemo-drugs, suggesting that both CD 44 and ALDH activity contribute to chemo-drug resistance. Moreover, both MCF-7-CR and MDA-MB-231 cells showed strong chemo-drug sensitivity to cisplatin when the cells were infected by Ad-MBR-GFP, leading to 9-fold and 2-fold reduction in the IC 50 values when compared to cisplatin treatment alone, respectively. The data were further supported by 3D (soft agar) and spheroid cell models of MCF-7-CR and MDA-MB-231 cells which showed a 2-fold reduction of a number of cell colonies and spheroid size when treated with both Ad-MBR-GFP and cisplatin, and compared to control. Other than chemo-sensitivity, Ad-MBR-GFP-infected cancer cells retarded cell migration. Flow cytometry analysis showed that the mechanism of action of Ad-MBR-GFP involved cell cycle arrest at the G1 phase and inhibition of cellular DNA synthesis. Taken together, our investigation showed that Ad-MBR-GFP mediated chemo-drug sensitization in the infected cancer cells involved the activation of apoptosis signaling, cell cycle arrest, and inhibition of DNA synthesis, suggesting that Ad-MBR-GFP is potentially efficacious for the treatment of chemo-drug resistant cancers.


Subject(s)
Adenoviridae , Breast Neoplasms , Drug Resistance, Neoplasm , Neoplastic Stem Cells , Tumor Suppressor Proteins , bcl-2-Associated X Protein , Humans , Neoplastic Stem Cells/metabolism , Neoplastic Stem Cells/drug effects , Neoplastic Stem Cells/pathology , Breast Neoplasms/genetics , Breast Neoplasms/pathology , Breast Neoplasms/drug therapy , Breast Neoplasms/metabolism , Adenoviridae/genetics , Tumor Suppressor Proteins/genetics , Tumor Suppressor Proteins/metabolism , Female , bcl-2-Associated X Protein/metabolism , bcl-2-Associated X Protein/genetics , MCF-7 Cells , Cell Line, Tumor , Biomarkers, Tumor/metabolism , Biomarkers, Tumor/genetics , Apoptosis/drug effects , Antineoplastic Agents/pharmacology , Cisplatin/pharmacology
12.
Nat Prod Bioprospect ; 14(1): 27, 2024 May 09.
Article in English | MEDLINE | ID: mdl-38722432

ABSTRACT

Until recently, the main pharmaceuticals used to control cholesterol and prevent cardiovascular disease (CVD) were statin-related drugs, known for their historical side effects. Therefore, there is growing interest in exploring alternatives, such as nutritional and dietary components, that could play a central role in CVD prevention. This review aims to provide a comprehensive understanding of how natural phytosterols found in various diets combat CVDs. We begin with a description of the overall approach, then we explore in detail the different direct and indirect mechanisms that contribute to reducing cardiovascular incidents. Phytosterols, including stigmasterol, ß-sitosterol, ergosterol, and fucosterol, emerge as promising molecules within nutritional systems for protection against CVDs due to their beneficial effects at different levels through direct or indirect cellular, subcellular, and molecular mechanisms. Specifically, the mentioned phytosterols exhibit the ability to diminish the generation of various radicals, including hydroperoxides and hydrogen peroxide. They also promote the activation of antioxidant enzymes such as superoxide dismutase, catalase, and glutathione, while inhibiting lipid peroxidation through the activation of Nrf2 and Nrf2/heme oxygenase-1 (HO-1) signaling pathways. Additionally, they demonstrate a significant inhibitory capacity in the generation of pro-inflammatory cytokines, thus playing a crucial role in regulating the inflammatory/immune response by inhibiting the expression of proteins involved in cellular signaling pathways such as JAK3/STAT3 and NF-κB. Moreover, phytosterols play a key role in reducing cholesterol absorption and improving the lipid profile. These compounds can be used as dietary supplements or included in specific diets to aid control cholesterol levels, particularly in individuals suffering from hypercholesterolemia.

13.
Food Chem X ; 22: 101453, 2024 Jun 30.
Article in English | MEDLINE | ID: mdl-38803670

ABSTRACT

This study aimed to explore the possibility of enriching cold-pressed Virginia (VIO) and Valencia (VAO) peanut oils with omega-3 fatty acids (FAs) from walnut oil (WO) to produce blended oils with improved nutritional value. The oxidative stability of pure and blended oils was examined under accelerated conditions (60 °C) for 28 days. The FA and tocopherol profiles, as well as nutritional quality indices, were determined. As the proportion of WO increased in the blends, the levels of linoleic and α-linolenic essential FAs increased, while oleic acid content decreased. Furthermore, γ- and δ-tocopherol levels rose, whereas α-tocopherol declined. Among the studied blends, VIO:WO blends, especially at a (70:30) ratio, were nutritionally favorable with a balanced FA profile. During storage, notable changes were observed in tocopherol levels, along with subtle alterations in the FA profile of the blended oils. Hence, the oxidative stability of pure VIO and VAO decreased with WO incorporation.

14.
Sci Rep ; 14(1): 9195, 2024 04 22.
Article in English | MEDLINE | ID: mdl-38649707

ABSTRACT

The development of novel antioxidant compounds with high efficacy and low toxicity is of utmost importance in the medicine and food industries. Moreover, with increasing concerns about the safety of synthetic components, scientists are beginning to search for natural sources of antioxidants, especially essential oils (EOs). The combination of EOs may produce a higher scavenging profile than a single oil due to better chemical diversity in the mixture. Therefore, this exploratory study aims to assess the antioxidant activity of three EOs extracted from Cymbopogon flexuosus, Carum carvi, and Acorus calamus in individual and combined forms using the augmented-simplex design methodology. The in vitro antioxidant assays were performed using DPPH and ABTS radical scavenging approaches. The results of the Chromatography Gas-Mass spectrometry (CG-MS) characterization showed that citral (29.62%) and niral (27.32%) are the main components for C. flexuosus, while D-carvone (62.09%) and D-limonene (29.58%) are the most dominant substances in C. carvi. By contrast, ß-asarone (69.11%) was identified as the principal component of A. calamus (30.2%). The individual EO exhibits variable scavenging activities against ABTS and DPPH radicals. These effects were enhanced through the mixture of the three EOs. The optimal antioxidant formulation consisted of 20% C. flexuosus, 53% C. carvi, and 27% A. calamus for DPPHIC50. Whereas 17% C. flexuosus, 43% C. carvi, and 40% A. calamus is the best combination leading to the highest scavenging activity against ABTS radical. These findings suggest a new research avenue for EOs combinations to be developed as novel natural formulations useful in food and biopharmaceutical products.


Subject(s)
Acorus , Antioxidants , Carum , Cymbopogon , Oils, Volatile , Plant Extracts , Cymbopogon/chemistry , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Acorus/chemistry , Carum/chemistry , Gas Chromatography-Mass Spectrometry , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology
15.
Chem Biol Interact ; 394: 110978, 2024 May 01.
Article in English | MEDLINE | ID: mdl-38552766

ABSTRACT

Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by the accumulation of amyloid-ß (Aß) protein aggregates, leading to synaptic dysfunction and neuronal cell death. In this study, we used a comprehensive approach encompassing in vitro assays, computational analyses, and an in vivo Caenorhabditis elegans model to evaluate the inhibitory effects of various xanthones, focusing on Garcinone D (GD), on Aß42 oligomer formation. Dot blot analysis revealed concentration-dependent responses among xanthones, with GD consistently inhibiting Aß42 oligomer formation at low concentrations (0.1 and 0.5 µM, inhibitions of 84.66 ± 2.25% and 85.06 ± 6.57%, respectively). Molecular docking and dynamics simulations provided insights into the molecular interactions between xanthones and Aß42, highlighting the disruption of key residues involved in Aß42 aggregation. The neuroprotective potential of GD was established using transgenic C. elegans GMC101, with substantial delays in paralysis reported at higher concentrations. Our findings show that GD is a potent suppressor of Aß42 oligomer formation, suggesting its potential as a therapeutic candidate for AD. The concentration-dependent effects observed in both in vitro and in vivo models underscore the need for nuanced dose-response assessments. These findings contribute novel insights into the therapeutic landscape of xanthones against AD, emphasizing the multifaceted potential of GD for further translational endeavors in neurodegenerative disorder research.


Subject(s)
Amyloid beta-Peptides , Caenorhabditis elegans , Peptide Fragments , Xanthones , Animals , Humans , Alzheimer Disease/drug therapy , Alzheimer Disease/metabolism , Amyloid beta-Peptides/metabolism , Amyloid beta-Peptides/toxicity , Animals, Genetically Modified , Caenorhabditis elegans/drug effects , Caenorhabditis elegans/metabolism , Disease Models, Animal , Molecular Docking Simulation , Molecular Dynamics Simulation , Neuroprotective Agents/pharmacology , Neuroprotective Agents/chemistry , Peptide Fragments/toxicity , Peptide Fragments/metabolism , Protein Aggregates/drug effects , Xanthones/pharmacology , Xanthones/chemistry
16.
Front Biosci (Landmark Ed) ; 29(2): 55, 2024 Feb 05.
Article in English | MEDLINE | ID: mdl-38420797

ABSTRACT

Breast cancer (BC) is the second most common malignancy in the world. Numerous studies have demonstrated the association between human leukocyte antigen (HLA) and cancer. The occurrence and development of BC are closely linked to genetic factors. Human leukocyte antigens G and E (HLA-G and HLA-E) are non-classical major histocompatibility complex (MHC) class I molecules. These molecules play an important role in immune surveillance by inhibiting the cytotoxic and natural killer T cells responsible for immune escape. The expression of HLA-G and HLA-E has been associated with several diseases, including tumors. The HLA system plays a key role in the escape of tumor cells from immune surveillance. This review aims to determine the correlation between BC susceptibility and HLA markers specific HLA alleles such as HLA-B07, HLA-DRB111, HLA-DRB113, and HLA-DRB115 are associated with an increased risk of developing BC. Furthermore, HLA-G mutations have been attributed to an elevated likelihood of metastasis in BC patients. Understanding the complex associations between the HLA system and BC development is critical for developing novel cancer prevention, detection, and treatment strategies. This review emphasizes the importance of analyzing HLA polymorphisms in the management of BC patients, as well as the urgent need for further research in this area.


Subject(s)
Breast Neoplasms , HLA-G Antigens , Female , Humans , Breast Neoplasms/diagnosis , Breast Neoplasms/genetics , Histocompatibility Antigens Class II/genetics , HLA-E Antigens , HLA-G Antigens/genetics , Polymorphism, Genetic , Disease Susceptibility
17.
Chem Biol Interact ; 392: 110907, 2024 Apr 01.
Article in English | MEDLINE | ID: mdl-38395253

ABSTRACT

The regulation of gene expression is fundamental to health and life and is essentially carried out at the promoter region of the DNA of each gene. Depending on the molecular context, this region may be accessible or non-accessible (possibility of integration of RNA polymerase or not at this region). Among enzymes that control this process, DNA methyltransferase enzymes (DNMTs), are responsible for DNA demethylation at the CpG islands, particularly at the promoter regions, to regulate transcription. The aberrant activity of these enzymes, i.e. their abnormal expression or activity, can result in the repression or overactivation of gene expression. Consequently, this can generate cellular dysregulation leading to instability and tumor development. Several reports highlighted the involvement of DNMTs in human cancers. The inhibition or activation of DNMTs is a promising therapeutic approach in many human cancers. In the present work, we provide a comprehensive and critical summary of natural bioactive molecules as primary inhibitors of DNMTs in human cancers. The active compounds hold the potential to be developed as anti-cancer epidrugs targeting DNMTs.


Subject(s)
DNA (Cytosine-5-)-Methyltransferases , Neoplasms , Humans , DNA (Cytosine-5-)-Methyltransferases/genetics , Neoplasms/metabolism , DNA (Cytosine-5-)-Methyltransferase 1/genetics , CpG Islands , DNA Methylation , Epigenesis, Genetic
18.
Biomed Pharmacother ; 170: 115989, 2024 Jan.
Article in English | MEDLINE | ID: mdl-38103309

ABSTRACT

Cyanobacteria and microalgae contain various phytochemicals, including bioactive components in the form of secondary metabolites, namely flavonoids, phenolic acids, terpenoids, and tannins, with remarkable anticancer effects. This review highlights the recent advances in bioactive compounds, with potential anticancer activity, produced by cyanobacteria and microalgae. Previous in vitro investigations showed that many of these bioactive compounds exhibit potent effects against different human cancer types, such as leukemia and breast cancers. Multiple mechanisms implicated in the antitumor effect of these compounds were elucidated, including their ability to target cellular, subcellular, and molecular checkpoints linked to cancer development and promotion. Recent findings have highlighted various mechanisms of action of bioactive compounds produced by cyanobacteria and microalgae, including induction of autophagy and apoptosis, inhibition of telomerase and protein kinases, as well as modulation of epigenetic modifications. In vivo investigations have demonstrated a potent anti-angiogenesis effect on solid tumors, as well as a reduction in tumor volume. Some of these compounds were examined in clinical investigations for certain types of cancers, making them potent candidates/scaffolds for antitumor drug development.


Subject(s)
Antineoplastic Agents , Cyanobacteria , Microalgae , Neoplasms , Humans , Microalgae/chemistry , Cyanobacteria/metabolism , Biological Factors , Antineoplastic Agents/chemistry , Neoplasms/drug therapy
19.
Heliyon ; 9(11): e21222, 2023 Nov.
Article in English | MEDLINE | ID: mdl-38053906

ABSTRACT

Lavandula stoechas, a Mediterranean plant, renowned in traditional medicine for its health benefits, is also arousing strong interest associated with its essential oils (EOs) with promising therapeutic properties. The aim of this study was to analyze the chemical composition of the plant, as well as to study its major activities, including antioxidant, anti-diabetic, dermatoprotective, anti-inflammatory, and antibacterial effects, focusing on its major molecules. Using the GC-MS method, the main compounds identified in L. stoechas EO (LSEO) were fenchone (31.81 %) and camphor (29.60 %), followed by terpineol (13.14 %) and menthone (8.96 %). To assess their antioxidant activity, three in vitro methods were used (DPPH, FRAP, and ABTS). The results revealed that LSEO exhibited the best antiradical property (54 ± 62 µg/mL) according to the DPPH test, while fenchone demonstrated the highest antioxidant capacity (87 ± 92 µg/mL) in the FRAP test, and camphor displayed the highest antioxidant capacity (96 ± 32 µg/mL) in the ABTS test. However, these results were lower than those obtained by Trolox used as a reference. In addition, study also explored the anti-diabetic potential of LSEO and its major compounds by evaluating their inhibitory activity towards two digestive enzymes, α-glucosidase and α-amylase. Camphor (76.92 ± 2.43 µg/mL) and fenchone (69.03 ± 2.31 µg/mL) exhibited the best inhibitory activities for α-amylase and α-glucosidase assays, respectively. Interestingly, all elements of the study exerted activities superior to those of acarbose, regardless of the test performed. In contrast, the evaluation of the dermatoprotective potential was carried out in vitro by targeting two enzymes involved in cutaneous processes, tyrosinase and elastase. In this light, fenchone (53.14 ± 3.06 µg/mL) and camphor (48.39 ± 1.92 µg/mL) were the most active against tyrosinase and elastase, respectively. It should be noted that the effect of both molecules, as well as that of LSEO, ranged between 53.14 ± 3.06 and 97.45 ± 5.22 µg/mL, which was significantly lower than the standard, quercetin (IC50 of 246.90 ± 2 0.54 µg/mL) against tyrosinase. Furthermore, the anti-inflammatory potential of these elements has been studied by evaluating their ability to inhibit lipooxygenase (LOX), a class of enzymes involved in the inflammatory process in the human body. As a result, the LSEO demonstrated a remarkable effect with an IC50 of 6.34 ± 1.29 µg/mL, which was almost comparable to the standard, quercetin (IC50 = 3.93 ± 0.45 µg/mL). Concerning the antibacterial potential, we carried out a quantitative analysis of the various products tested, revealing a bactericidal activity of the LSEO against the strain L. monocytogenes ATCC 13932 at a minimum effective concentration (MIC = CMB = 0.25). Overall, LSEOs offer significant potential as a source of natural antioxidants, and antidiabetic and anti-inflammatory agents, as well as dermatoprotective and antibacterial compounds. Its major molecules, fenchone and camphor, showed promising activity in these areas of study, making it a valuable candidate for future research and development in the field of natural medicine.

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