Search Results (60)

Strophanthus sarmentosus is recognised for various ethnomedicinal applications, including treatment after snakebites. However, only limited scientific evidence exists on its antivenomous capabilities. This study investigates the efficacy of methanol and ethylacetate extracts from S. sarmentosus leaves and roots against Echis ocellatus venom. A non-toxic range for the extracts was determined in rats, and assays were performed to test their anti-hemorrhagic and anti-hemolytic activity as well as their influence on venom-induced blood clotting. In all of these experiments, the extracts demonstrated significant positive effects equal to or better than antivenom. Moreover, the extracts strongly inhibited and even abolished the digestion of the vasoactive neuropeptide bradykinin by snake venom metalloproteinases. Strophantus plants are known for their high content of cardiac glycosides, one of which is the commercially available ouabain, that by itself also considerably inhibited venom-induced bradykinin cleavage. Although ouabain is only present in low amounts in S. sarmentosus when compared to other cardenolides of similar structure, it can be hypothesized that members of this substance class may also have inhibitory properties against venom proteases. S. sarmentosus additionally contains bioactive substances such as flavonoids, terpenoids, tannins, saponins, and alkaloids, which contribute to its protective effects. The study provides scientific data to explain the success of the traditional use of S. sarmentosus plant extracts as a first aid against envenomation in rural Africa. Full article

Nosocomial fungal infections caused by Candida auris pose a threat to public health due to their increased resistance to common antifungal drugs. Four thiourea derivatives of 2-thiophenecarboxylic acid were evaluated for their antifungal and antioxidant activity. The antifungal activity of the compounds was tested against strains of C. auris isolated from a hospital in Romania. With a notable inhibitory effect on C. auris biofilm growth and microbial adherence, the ortho-methylated derivative (SB2) showed the highest antifungal activity. Furthermore, emphasizing the impact of structural factors on the electron-donating capacity of these compounds, antioxidant activity assays (DPPH, FRAP, TEAC and CUPRAC) identified the SB2 compound as having the highest antihemolytic and antioxidant effects. The low cytotoxicity validated by hemocompatibility assays makes these compounds options for antifungal treatment. The results show that antifungal and antioxidant action is greatly influenced by structural modifications, especially the position of the methyl group on the aromatic ring. The possible clinical uses of these molecules as drugs for the treatment of multidrug-resistant C. auris infections needs further investigation. Full article

The use of nanoparticles is becoming increasingly apparent in a growing number of medical fields. To exploit the full potential of these particles, it is essential to examine their behavior in the blood and their possible interactions with blood cells. Dendritic core multi-shell DendroSol™ nanoparticles (DS-NPs) are able to penetrate into viable layers of human skin, but nothing is known about their interaction with blood cells. In the present study, we analyze the effect of DS-NPs on red blood cells (RBCs) using confocal laser scanning microscopy (CLSM), flow cytometry, sedimentation rate analysis, spectrophotometry, and hemolysis assays. DS-NPs labeled with Nile red (NR) were added to RBC suspensions and their accumulation in the area of the RBC membranes was demonstrated by CLSM as well as by flow cytometry. In the presence of DS-NPs, the RBCs show an increased sedimentation rate, which also confirms the binding of the NPs to the cells. Interestingly, in the presence of DS-NPs, the RBCs are stabilized against hypotonic hemolysis as well as against the hemolytic action of Triton X-100. This proven anti-hemolytic effect could be utilized to enhance the circulation time of RBCs loaded with drugs for prolonged sustained release and drug delivery with enhanced bioavailability. Full article

(1) Background: Lippia sidoides Cham is a Brazilian aromatic plant rich in phenolic compounds. In traditional medicine, its leaves are used to treat diseases of the Central Nervous System such as stress and anxiety. This study evaluates the capacity of the aqueous extract of L. sidoides as an anticonvulsant, anticholinesterase and antihemolytic agent. (2) Methods: The extract was obtained from the leaves using water as a solvent, then dried in a spray dryer. The anticonvulsant effect was evaluated in zebrafish models using the pentylenetetrazol (PTZ) method. The anticholinesterase effect was determined using the acetylcholinesterase enzyme and physostigmine as a positive control. The antihemolytic action was evaluated by exposing erythrocytes to different concentrations of NaCl in the presence and absence of the extract. (3) Results: The anticonvulsant effect was observed at a concentration of 400 mg/kg, delaying convulsive crises. In the anticholinesterase assay, a dose-dependent action and variation in the effect over time were observed, demonstrating a reversible effect of the extract. For the osmotic fragility test, the extract showed satisfactory results, providing cellular protection across all variations of NaCl concentration. (4) Conclusions: These results demonstrate the promising potential of L. sidoides extract for the development of drugs that act in the treatment of diseases that affect the Central Nervous System. Full article

Pomegranate and its by-products contain a broad spectrum of phytochemicals, such as flavonoids, phenolic acids and tannins, having pleiotropic preventive and prophylactic properties in health disorders related to oxidative stress and microbial contamination. Here, we examined the biological effects of a pomegranate peel ellagitannins-enriched (>90%) extract, PETE. In vitro studies revealed that PETE has a strong antiradical action towards synthetic radicals and biologically relevant ROS surpassing or comparable to that of Trolox. In cellular models, it showed concentration-dependent (25–100 µg/mL) yet opposing effects depending on the cell membrane type and exposure conditions. In erythrocytes, PETE protected membrane integrity in the presence of the strong oxidant HClO and restored reduced glutathione levels to up to 85% of the control value while having much weaker acute and long-term intrinsic effects. Such protection persisted even after the removal of the extract from cells, indicating strong membrane interaction. In HeLa cancer cells, and at concentrations lower than those used for red blood cells, PETE induced robust potentiation of ROS production and mitochondrial potential dissipation, leading to autophagy-like membrane morphology changes and cell death. In S. aureus, the growth arrest and bacterial death in the presence of PETE (with MIC = 31.25 µg/mL and MBC = 125 µg/mL, respectively) can be linked to the tripled ROS induction by the extract in the same concentration range. This study indicates a specificity of ROS production by the pomegranate extract depending on the type of cell, the concentration of the extract and the time of incubation. This specificity witnesses a strong potential of the extract components as candidates in antioxidant and pro-oxidant therapy. Full article

Plant extracts of fifteen plants of ethnomedicinal use in Mexico were analyzed to provide scientific knowledge of their medicinal properties through the evaluation of different biological activities such as anti-hemolytic, antioxidant, and cytotoxic effects in normal cells. Therefore, methanolic extracts were obtained from each of the plants by the Soxhlet extraction. The hemolytic activity in human erythrocytes was evaluated, as was their potential to protect the erythrocyte membrane against the 2,2′-azobis (2-methylpropionamidine) dihydrochloride (AAPH) and 1,1–diphenyl–2–picryl hydrazyl (DPPH) radicals. Finally, the toxicity of the extracts in normal cell cultures of African green monkey kidney cells (Vero) and peripheral blood mononuclear cells (PBMC) was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction method. Most of the extracts showed low hemolytic activity and high anti-hemolytic activity as well as high selectivity indices (SI) and antioxidant effects. Extracts of H. inuloides, J. dioica, and J. spicigera induced cell proliferation of the Vero cells. K. daigremontiana, A. adstringens, S. mexicanum, J. spicigera, L. tridentata, and M. tenuiflora extracts showed PBMC cell proliferation. In the present study, it was observed that the evaluated extracts did not present hemolytic activity, and some presented low toxicity when Vero and PBMC cell cultures were exposed. In conclusion, traditionally used plants possess beneficial health properties, and it is hoped that this study will serve as a basis for understanding the biological effects of traditionally used plants and may complement future studies. Full article

Staphylococcus aureus biofilm formation is a pivotal mechanism in the development of drug resistance, conferring resilience against conventional antibiotics. This study investigates the inhibitory effects of Actinostemma lobatum (A. lobatum) Maxim extracts on S. aureus biofilm formation and their antihemolytic activities, with a particular focus on identifying the active antibiofilm and antihemolysis compound, quercetin. Seven solvent extracts and twelve sub-fractions were evaluated against four S. aureus strains. The ethyl acetate fraction (10 to 100 μg/mL) significantly hindered biofilm formation by both methicillin-sensitive and -resistant strains. Bioassay-guided isolation of the ethyl acetate extract identified quercetin as the major antibiofilm compound. The ethyl acetate extract was found to contain 391 μg/mg of quercetin and 30 μg/mg of kaempferol. Additionally, the A. lobatum extract exhibited antihemolytic activity attributable to the presence of quercetin. The findings suggest that quercetin-rich extracts from A. lobatum and other quercetin-rich foods and plants hold promise for inhibiting resilient S. aureus biofilm formation and attenuating its virulence. Full article

Postbiotics possess various functional activities, closely linked to their source bacterial strains and preparation methods. Therefore, the functional activities of postbiotics need to be evaluated through in vitro and in vivo methods. This study aims to prepare a postbiotic and explore its antihemolytic, anti-inflammatory, antioxidant, and antibacterial activities. Specifically, a postbiotic preparation named PostbioP-6 was prepared by intercepting 1–5 kDa of Lacticaseibacillus paracasei Postbiotic-P6 fermentation broth. The results demonstrate that PostbioP-6 exhibited notable biological activities across multiple assays. It showed significant antihemolytic activity, with a 4.9–48.1% inhibition rate at 10–50% concentrations. Anti-inflammatory effects were observed both in vitro, where 8–40% PostbioP-6 was comparable to 259.1–645.4 μg/mL diclofenac sodium, and in vivo, where 3.5 and 4.0 μL/mL PostbioP-6 significantly reduced neutrophil counts in inflamed zebrafish (p < 0.05). Antioxidant properties were evident through increased reducing power (OD₇₀₀ increased from 0.279 to 2.322 at 1.25–12.5% concentrations), DPPH radical scavenging activity (38.9–92.4% scavenging rate at 2.5–50% concentrations), and hydroxyl radical scavenging activity (4.66–10.38% scavenging rate at 0.5–4% concentrations). Additionally, PostbioP-6 demonstrated antimicrobial activity against two Gram-positive bacteria, eight Gram-negative bacteria, and one fungus. Furthermore, PostbioP-6 significantly inhibited the increase in peroxide value and malondialdehyde content in cookies, highlighting its potential application in food preservation. In conclusion, we prepared a novel postbiotic, termed PostbioP-6, which proved to have prominent anti-hemolytic, anti-inflammatory, antioxidant, and broad-spectrum antimicrobial activities. The multifunctional properties of PostbioP-6 position it as a potentially effective functional food supplement or preservative. In the future, further research is necessary to elucidate the precise mechanisms of action, identify the active components, and validate its biological activities in animal models or clinical trials. Full article

Environmentally friendly biosynthesis of silver nanoparticles (AgNPs) from Aeonium arboreum (L.) Webb & Berthel is reported for the first time. The synthesized AgNPs were characterized using UV-Vis, FTIR, TEM, Zeta potential, and XRD analysis, revealing high stability (−29.1 mV), spherical shape, and an average size of 100 nm. The antimicrobial activity levels of both A. arboreum extract and biosynthesized AgNPs were evaluated against five uropathogens (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans). Both the extract and the AgNPs exhibited significant efficacy, particularly against E. coli, with inhibition zones of 27 mm and 30 mm, respectively. LC-MS analysis tentatively identified 11 secondary metabolites in the extract, including quercetin-3-O-glucoside, quercetin-3-O-rhamnoside, myricetin 3-glucoside, and daphneresinol. In silico docking studies revealed promising binding affinities of these metabolites in relation to key enzymes involved in bacterial folate synthesis (dihydrofolate reductase (DHFR) and dihydropteroate synthase (DHPS)) and DNA replication (DNA gyrase). These findings demonstrate the potential of A. arboreum-based AgNPs and their associated metabolites as a novel therapeutic approach for combating urinary tract infections. Their antimicrobial, antihemolytic, and antibiofilm properties warrant further investigation. Full article

Argemone mexicana L. has been used in traditional Mexican medicine. Among its bioactive constituents, berberine (BER) has garnered attention for its cytotoxic properties against different tumor cell lines. This study investigates the in vitro toxicity against HEP-G2 (human hepatocellular carcinoma) and murine lymphoma (L5178Y-R) cells using the MTT assay of the methanol extract (AmexM), sub-partitions of A. mexicana, and BER. Selectivity indices (SIs) were determined by comparing their cytotoxic effects on VERO (monkey kidney epithelial) and PBMC (human peripheral blood mononuclear) non-tumoral cells. Additionally, the anti-hemolytic effect of these treatments was assessed using the AAPH method. The treatment with the most promising activity against tumor cells and anti-hemolytic efficacy underwent further evaluation for toxicity in Artemia salina and antioxidant activities using DPPH, ABTS, and FRAP assays. BER demonstrated an IC₅₀ = 56.86 µg/mL in HEP-G2 cells and IC₅₀ < 5.0 µg/mL in L5178Y-R cells, with SI values of 15.97 and >5.40 in VERO and PBMC cells, respectively. No significant hemolytic effects were observed, although AmexM and BER exhibited the highest anti-hemolytic activity. BER also demonstrated superior antioxidant efficacy, with lower toxicity in A. salina nauplii compared to the control. Additionally, BER significantly attenuated nitric oxide production. This study highlights the antiproliferative effects of A. mexicana, particularly BER, against HEP-G2 and L5178Y-R tumor cell lines, along with its selectivity towards normal cells. Furthermore, its anti-hemolytic and antioxidant potentials were demonstrated, suggesting that BER is a promising candidate for potent chemotherapeutic agents. Full article

In this study, we investigated for the first time the anti-inflammatory and immunomodulatory properties of crude polysaccharide (PSHT) extracted from green marine algae Halimeda tuna. PSHT exhibited anti-oxidant activity in vitro through scavenging 1, 1-diphenyl-2-picryl hydroxyl free radical, reducing Fe³⁺/ferricyanide complex, and inhibiting nitric oxide. PSHT maintained the erythrocyte membrane integrity and prevented hemolysis. Our results also showed that PSHT exerted a significant anti-edematic effect in vivo by decreasing advanced oxidation protein products and malondialdehyde levels and increasing the superoxide dismutase and glutathione peroxidase activities in rat’s paw model and erythrocytes. Interestingly, PSHT increased the viability of murine RAW264.7 macrophages and exerted an anti-inflammatory effect on lipopolysaccharide-stimulated cells by decreasing pro-inflammatory molecule levels, including nitric oxide, granulocyte-macrophage colony-stimulating factor (GM-CSF) and tumor necrosis factor-alpha (TNF-α). Our findings indicate that PSHT could be used as a potential immunomodulatory, anti-inflammatory, anti-hemolytic, and anti-oxidant agent. These results could be explained by the computational findings showing that polysaccharide building blocks bound both cyclooxygenase-2 (COX-2) and TNF-α with acceptable affinities. Full article

The anti-lung cancer properties of the plant Medicago orbicularis have not been explored yet. Therefore, we identified its phytochemical composition and investigated the antioxidant, anti-hemolytic, and anti-cancerous properties of extracts of this plant in A549 human lung adenocarcinoma cells. The results show that all parts of M. orbicularis (stems, leaves, and fruits) exhibit remarkable hemolytic activities and modest antioxidant capacity. In addition, all extracts showed a dose-dependent anti-cancerous cytotoxic activity against A549 cells, with fruit extracts being the most potent. This cytotoxic effect could be related, at least partly, to the induction of apoptosis, where M. orbicularis fruit extracts reduced the ratio of anti-apoptotic BCL-2/pro-apoptotic BAX, thereby promoting cellular death. Furthermore, the use of M. orbicularis, in combination with a conventional chemotherapeutic agent, cisplatin, was assessed. Indeed, the combination of cisplatin and M. orbicularis fruit extracts was more cytotoxic and induced more aggregation of A549 cells than either treatment alone. GC-MS analysis and total polyphenol and flavonoid content determination indicated that M. orbicularis is rich in compounds that have anti-cancerous effects. We propose M. orbicularis as a potential source of anti-cancerous agents to manage the progression of lung cancer and its resistance to therapy. Full article

The objective of our research was to examine the antioxidant and membrane-protective characteristics of a few medicinal plant extracts belonging to the Asteracea family, along with their flavonoid and polyphenolic content, in order to identify strategies for enhancing beverage composition and boosting the antioxidant capacity of green and black tea. The activity of aqueous-ethanolic extracts from the dried parts of plants, such as Arictum tomentosum Mill., Ghnapilum kasachstanicum Kirp. & Kuprian. ex Kirp., Artemisia schrenkiana Ledeb., A. rutifolia Steph. ex Spreng., A. cina O.Berg, and A. vulgaris L., were examined using a model of Wistar rats. Thiobarbituric acid-reacting substances (TBARS), a marker of malondialdehyde concentration, were used to measure the amount of lipid peroxidation (LPO) in liver microsomes. Considering the outcomes, the extracts from A. tomentosum, G. kasachstanicum, and A. vulgaris exhibit the strongest membrane-stabilizing action among those examined. At a concentration of 5 g/mL, the extracts of these plants demonstrated a significant anti-hemolitic impact, whereas the remaining extracts displayed a similar effect at doses above 10 g/mL. Accordingly, among the extracts studied, the A. tomentosum, G. kasachstanicum, A. schrenkiana, A. rutifolia, A. cina, and A. vulgaris extracts have significant antioxidant properties. The integrated antioxidant and antihemolytic qualities of A. tomentosum and green tea extracts were comparable to those of the individual plant extracts. When the extracts of A. schrenkiana and green tea were combined, similar outcomes were seen, suggesting that there was no appreciable synergistic interaction. Full article

Previous studies detail that different blood groups are associated with incidence of oxidative stress-related diseases such as certain carcinomas. Bioactive compounds represent an alternative for preventing this oxidative stress. The aim of this study was to elucidate the impact of blood groups on the erythroprotective potential of fucoxanthin, β-Carotene, gallic acid, quercetin and ascorbic acid as therapeutic agents against oxidative stress. The impact of ABO blood groups on the erythroprotective potential was evaluated via the antioxidant capacity, blood biocompatibility, blood susceptibility and erythroprotective potential (membrane stabilization, in vitro photostability and antihemolytic activity). All tested antioxidants exhibited a high antioxidant capacity and presented the ability to inhibit ROO•-induced oxidative stress without compromising the cell membrane, providing erythroprotective effects dependent on the blood group, effects that increased in the presence of antigen A. These results are very important, since it has been documented that antigen A is associated with breast and skin cancer. These results revealed a probable relationship between different erythrocyte antigens with erythroprotective potential, highlighting the importance of bio-targeted drugs for groups most susceptible to certain chronic-degenerative pathologies. These compounds could be applied as additive, nutraceutical or encapsulated to improve their bioaccessibility. Full article

Background: Eryptosis stimulated by anticancer drugs can lead to anemia in patients. β-caryophyllene oxide (CPO) is an anticancer sesquiterpene present in various plants; however, its effect on the structure and function of human red blood cells (RBCs) remains unexplored. The aim of this study was to investigate the hemolytic and eryptotic activities and underlying molecular mechanisms of CPO in human RBCs. Methods: Cells were treated with 10–100 μM of CPO for 24 h at 37 °C, and hemolysis, LDH, AST, and AChE activities were photometrically assayed. Flow cytometry was employed to determine changes in cell volume from FSC, phosphatidylserine (PS) externalization by annexin-V-FITC, intracellular calcium by Fluo4/AM, and oxidative stress by 2′,7′-dichlorodihydrofluorescein diacetate (H₂DCFDA). Cells were also cotreated with CPO and specific signaling inhibitors and antihemolytic agents. Furthermore, whole blood was exposed to CPO to assess its toxicity to other peripheral blood cells. Results: CPO induced concentration-responsive hemolysis with LDH and AST leakage, in addition to PS exposure, cell shrinkage, Ca²⁺ accumulation, oxidative stress, and reduced AChE activity. The toxicity of CPO was ameliorated by D4476, staurosporin, and necrosulfonamide. ATP and PEG 8000 protected the cells from hemolysis, while urea and isotonic sucrose had opposite effects. Conclusions: CPO stimulates hemolysis and eryptosis through energy depletion, Ca²⁺ buildup, oxidative stress, and the signaling mediators casein kinase 1α, protein kinase C, and mixed lineage kinase domain-like pseudokinase. Development of CPO as an anticancer therapeutic must be approached with prudence to mitigate adverse effects on RBCs using eryptosis inhibitors, Ca²⁺ channel blockers, and antioxidants. Full article