Antihemolytic Activity Research Articles

Synthesis of spherical carbon nanoparticles from orange peel and their surface modification with chitosan: Evaluation of optical properties, biocompatibility, antioxidant and anti-hemolytic activity

Synthesis of spherical carbon nanoparticles from orange peel and their surface modification with chitosan: Evaluation of optical properties, biocompatibility, antioxidant and anti-hemolytic activity

Extract from Psidium guineense Sw leaves: An alternative against resistant strains of Staphylococcus aureus

Psidium guineense SW., commonly known as sour guava, is used in traditional medicine to address diverse health issues, such as inflammation, infections, and gastrointestinal disorders. Although previous research has highlighted the antimicrobial properties of the root extract and the antioxidant potential of its fruits, information regarding the activities associated with the leaf extract is lacking. The aim of the study was to use the traditional knowledge of the biological properties of P. guineense and investigate its antimicrobial activity, mechanism of action, synergistic effects, and antivirulence activity against Staphylococcus aureus. Minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined for S. aureus, including antibiotic-resistant isolates. The synergy between the extract and antibiotics was evaluated. A growth curve was constructed for S. aureus treated with the extract. The anti-hemolytic activity was assessed by inhibiting hemolysis in human blood, and the inhibition of staphyloxanthin (STX) was examined. The extract effectively inhibited all strains with MIC and MBC values ranging from 256 to 512 µg/mL and 512 to 1024 µg/mL, respectively. Antimicrobial synergy experiments demonstrated the enhanced effectiveness of antibiotics, especially ciprofloxacin, when combined with the P. guineense extract, especially with ciprofloxacin, resulting in complete synergy against all S. aureus strains. In growth curve tests, the extract inhibited growth at MIC of 256 µg/mL within 8 h and significantly delayed it at MIC/2 (128 µg/mL) within 12 h. In antivirulence tests, the extract effectively reduced hemolysis and STX production by S. aureus at MIC and MIC/2, indicating its potential as an antimicrobial agent with antivirulence properties. The extract effectively inhibited S. aureus, including drug-resistant strains with low MIC and MBC values, exhibiting strong antimicrobial and synergistic properties with antibiotics. also In addition, the extract accelerated recovery by limiting bacterial growth and exhibiting antivirulence capabilities, reducing the severe symptoms of S. aureus infections.

Green-synthesis of silver nanoparticles AgNPs from Podocarpus macrophyllus for targeting GBM and LGG brain cancers via NOTCH2 gene interactions

Brain tumors, particularly Glioblastoma Multiforme (GBM) and Low-Grade Gliomas (LGG), present significant clinical challenges due to their aggressive nature and resistance to conventional treatments. Traditional therapies such as surgery, chemotherapy, and radiation are often limited in efficacy, necessitating novel therapeutic strategies. Nanotechnology, particularly the use of silver nanoparticles (Ag NPs), offers a targeted and potentially more effective approach. This study focuses on the green synthesis of Ag NPs using Podocarpus macrophyllus leaf extract as a reducing agent. The synthesized Ag NPs were characterized for their physicochemical properties, demonstrating a controlled particle size of 13 nm as determined by scanning electron microscopy (SEM). Fourier-transform infrared (FTIR) spectroscopy confirmed the presence of functional groups, and energy-dispersive X-ray (EDX) spectroscopy revealed that silver constituted approximately 90% of the nanoparticle composition. The Ag NPs exhibited promising biological activity, including 90% free radical scavenging (antioxidant) activity, 99.15% inhibition of protein denaturation (anti-inflammatory activity), and 90.56% inhibition of alpha-amylase (anti-diabetic activity). Additionally, the nanoparticles displayed significant anti-hemolytic (89.9% inhibition) and antimicrobial activities, with a 20 mm inhibition zone against Staphylococcus species. Computational analyses further indicated that the NOTCH2 gene, which is upregulated in LGG and GBM, may interact with Ag NPs, suggesting their potential in brain cancer therapy. The green synthesis approach offers a sustainable and bioactive method for producing Ag NPs, underscoring their therapeutic promise for treating GBM and LGG.

Novel Co2+ and Cd2+ Complexes Derived From a New N‐Donor Pyridyl‐Functionalized Thiophosphoric Triamide Ligand: Structural Investigation, DNA/COVID‐19/Monkeypox Molecular Docking, and Biological Assays

ABSTRACTA thiophosphoric triamide (SPT) ligand P(S)[NH‐2Py]3 was synthesized and utilized as a ligand to make novel binuclear and mononuclear Co2+ and Cd2+ complexes. The compounds are the first examples of discrete chelate SPT complexes with a [N]3P(S)‐based backbone in which the SPT acts as a flexible tridentate N,N,N‐donor or N,N,O‐donor ligand. The metal cation features a hexacoordinate environment M(N)3(Cl)3/M(N)4(O)2 adopting a distorted octahedral geometry. Hirshfeld surface analysis affirms that the pyridinyl nitrogen is a more dominant H‐bond acceptor than the thiophosphoryl sulfur atom. The inhibitory activity against the MDA‐MB‐231 cancer cell line in vitro indicated a good inhibitory effect for all compounds. The mononuclear Co2+ complex showed a stronger inhibitory activity against cancer cells than other studied compounds with an IC50 of 62 ± 1.4 nM. Antioxidant and antihemolytic activity of the compounds showed appreciable performance with the highest activities for the Cd2+ complex. A computational DNA binding study by molecular docking indicated a good affinity of the compounds with the DNA receptor by a mixed mode of interactions. Docking was also performed on SARS‐CoV‐2 and monkeypox (Mpox), resulting in binding energies (−5.5 to −8.9 kcal/mol) that are competitive with current effective drugs.

Evaluation of the in vitro toxicity and anti-inflammatory activity of the methanolic extract of the leaves of Pistacia lentiscus L. harvested from northwestern Algeria.

Medicinal and aromatic plants have been used for thousands of years for their therapeutic properties, to treat various ailments and maintain health. This study was carried out to test the in vitro toxicity and anti-inflammatory activity of the methanolic extract of the leaves of Pistacia lentiscus L., native to the north-western region of Algeria. Toxicity was studied in vitro by the hemolysis test and anti-hemolytic activity on human red blood cells, while anti-inflammatory activity was assessed in vitro by the protein denaturation method. The study of toxicity by hemolysis of red blood cells showed a high rate of hemolysis at a dose of 200 mg/mL, with a hemolytic percentage of around 88.64%, while a high rate of anti-hemolysis was observed at a dose of 25 mg/mL, with an inhibition percentage of around 83.17%. Evaluation of anti-inflammatory activity revealed a high percentage of inhibition of ovalbumin denaturation, reaching 63.53% at the 2000 ug/mL dose, while the lowest percentage was obtained at the 3500 ug\mL concentration with 10.16%. This extract has a toxic substance but does not exceed the toxicity threshold which achieves significant anti-inflammatory activity with depandant doses.

Antisickling, hemolytic activities and toxicological evaluation of three plants species from the Nigerien Pharmacopoeia: Annona senegalensis Linné. Boscia senegalensis (Pers) Lam. and Ampelocissus afr

The aim of this study consits to evaluate the antisickling and antihemolytic activities and to determine the subacute toxicity of three plants Annona senegalensis L.; Boscia senegalensis (Pers) Lam.; and Ampelocissus africana (Lour) Merr.. The plant material contains leaves and bark of Annona senegalensis roots, leaves and bark root of Boscia senegalensis and the roots of Ampelocissus africana. A single method (80% ethanol maceration) is used to extract the five samples. The antisickleemic and antihemolytic effects are established with sickle cells disease (SCD) in the presence of sodium metabisulfite. Subacute toxicity is tested on Wistar strain rats. All samples showed an antisickling effect but leaves of Annona senegalensis (LAS) showed the highest percentage of antisickling activity (89.55%) at 50mg/ml. The anti-hemolytic effect was demonstrated in all samples by inhibition of hemolysis in the presence of a hemolysant. The toxicity results showed that the aqueous extracts of Annona senegalensis leaves and Boscia senegalensis root bark have non-toxic effects to wistar strain rats. However, some manifestations including fatigue, stretching and slight dyspenea were observed at doses of 150mg/mL and 300mg/mL. This work can contribute as a starting point towards the development of an improved traditional medicine (ITM) method which can help to treat the sickle cell disease. Keywords: Annona senegalensis L., Boscia senegalensis (pers) Lam and Ampelocissus Africana (Lour) Merr. Antisickness activity, Toxicity.

In Vitro Evaluation of Anti-Hemolytic and Cytotoxic Effects of Traditional Mexican Medicinal Plant Extracts on Human Erythrocytes and Cell Cultures.

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.

Evaluation of Antioxidant, Antibacterial, and Anti-hemolytic Properties of Ethanol Extract from Plectranthus barbatus Andrews (Lamiaceae) Leaves

Polyphenols can act as antioxidants, antibacterial, antifungal, or insecticidal agents. Given that microbial infections and arboviruses transmitted by Aedes aegypti significantly contribute to global morbidity and mortality, there is an urgent need to discover new antimicrobials and insecticides. This study investigated the ethanol extract (PbLE) of Plectranthus barbatus Andrews (Lamiaceae) leaves for its chemical constituents, antioxidant, antimicrobial, anti-hemolytic, and larvicidal activities. Qualitative analysis by Thin Layer Chromatography revealed cinnamic derivatives, flavonoids, terpenes, and steroids in PbLE. Quantitative analysis showed that PbLE contained 98.64 ± 0.87 mg EAG/g of total phenols, with flavonoids comprising 21.84 ± 0.34 mg EQ/g (c.a. 22%). PbLE demonstrated scavenging activity against ABTS+ (IC50 = 3246.00 ± 0.97 µg/mL) and DPPH (IC50 = 1371.75 ± 0.94 µg/mL) free radicals and exhibited reducing ability in the phosphomolybdenum method (IC50 = 899.33 ± 0.73 µg/mL). Although PbLE did not affect the growth or survival of pathogenic microorganisms, it significantly reduced (c.a. 80% for the extract at 256 mg/mL) the hemolysis caused by Staphylococcus aureus in human erythrocytes. Furthermore, PbLE (7 mg/mL) caused 40% mortality of A. aegypti third-instar larvae after 48-h exposure. In conclusion, PbLE, rich in phenolic compounds, acts as an antioxidant that mitigates S. aureus virulence to human erythrocytes and reduces the viability of A. aegypti larvae. The data reported herein contribute to the science by exploring P. barbatus, a medicinal plant with a long history of traditional use, as source of bioactive compounds with pharmacological and insecticidal properties. The determination of LC50 and mechanisms of PbLE larvicidal activity are underway.

Phytochemical Analysis and Evaluation of the Antioxidant, Anti-Inflammatory, Hemolytic, and Antibacterial Effects of Astragalus gombo (L.) Leaves.

The purpose of this study is to determine the phytochemical content and biological activities of the Astragalus gombo (endemic specie). While identification and quantification of individual secondary metabolites were performed by analysis HPLC. Antioxidant (DPPH and FRAP), anti-inflammatory, anti-hemolytic and antibacterial activities were evaluated. For analysis HPLC, we obtained 65 peaks and identified 6 major bioactive compounds. The total concentration in polyphenols, flavonoids and condensed tannins varied respectively from 66.306±0.88 mg GA eq/g, 34.312±1.4 mg Q eq/g and 5.343±2.74 mg Ca eq/g. In terms of antioxidant activity, we found that this extract had high inhibitory ratios equivalent to IC50=62.813±0.006 µg/mL for DPPH and IC50=19.375±0.041 µg/mL for FRAP. A high anti-inflammatory activity was estimated at 1615.81µg/mL, and a weak anti-hemolytic activity, the other hand the antibacterial activity is somewhat moderate against the five strains studied. This study demonstrated that the aqueous extract of A. gombo from El Oued region has tremendous antioxidant, anti-inflammatory and antibacterial abilities.

Antibiofilm and Antihemolytic Activities of Actinostemma lobatum Extract Rich in Quercetin against Staphylococcus aureus.

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.

Assessment of phytochemicals, antioxidant, anti-hemolytic, anti-inflammatory and anti-cancer potential of flowers, leaves and stem extracts of.

To evaluate phytochemicals and in vitro biological potential of flowers, leaves and stem extracts of Rosa arvensis. Presence of twenty secondary metabolites was confirmed and then phenolic and flavonoid contents were quantified spectrophotometrically. Fourier Transform Infrared spectroscopy was conducted to ascertain functional groups and antioxidant potential was examined using 2,2-diphenyl-1-picrylhydrazyl scavenging activity, total antioxidant capacity and total reducing power assays. Human erythrocytes were used to assess anti-hemolytic activity and five bacterial strains were examined to determine antibacterial potential of plant extracts. Radish seeds were used to perform phytotoxic activity and cytotoxic potential was evaluated via brine shrimps and PC3 cell lines. Highest phenolic contents were detected in the methanolic extract of Rosa arvensis flower (RAFM) [(151.635 ± 0.005) gallic acid equivalent mg/g] and highest flavonoid contents in the chloroform leaf extract (RALC) [(108.228 ± 0.004) quercetin equivalent mg/g]. Fourier-transform infrared spectroscopy analysis showed the presence of wide range of functional groups. The antioxidant assays indicated highest DPPH scavenging activity [IC50 (23.5 ± 0.6) μg/mL] in the methanolic stem extract (RASM), highest total antioxidant capacity [(265.1 ± 0.9) μg/mL] in RAFM and highest reducing potential [(209.9 ± 0.6) μg/mL] in leaf extract (RALM). Highest anti-hemolytic activity [(90.0 ± 0.5) μg/mL] was recorded in RAFM and brine shrimp cytotoxicity potential [(52.3 ± 0.3) μg/mL] in RASM. The antimicrobial activity was detected highest [(21.1 ± 0.5) mm inhibition zones] in RALM against Streptococcus aureus. In the end, anti-inflammatory and anti-cancer activity results depicted less than 50 % inhibition in the methanolic extracts. CONCLUSIONS: Our findings will be helpful in designing pharmaceutical regimens and therefore, more studies can be recommended to isolate and characterize compounds associated with the biological activities of Rosa arvensis.

Assessment of Multifunctional Activity of a Postbiotic Preparation Derived from Lacticaseibacillus paracasei Postbiotic-P6.

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.

Biosynthesis and Characterization of Aeonium arboreum-Derived Silver Nanoparticles: Antimicrobial Activity, Biofilm Inhibition, Antihemolytic Activity, and In Silico Studies.

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.

Antibacterial, cytotoxic and antioxidant effect of green leaf extract of Anacardium occidentale L.

Anacardium occidentale has pharmacological potential of anti-inflammatory, healing, antimicrobial and gastroprotective characteristics. Thus, the objective of this study was to evaluate the antibacterial, cytotoxic and antioxidant effects of the green leaf extract of Anacardium occidentale against clinical and ATCC collection bacteria. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of selected strains of clinical importance and ATCC were determined. The effect of the association with licensed antibiotics reported in the literature was evaluated, as well as their influence on the formation and pre-formation of biofilms. Human blood samples A, B and O were subjected to cytotoxicity evaluation at concentrations of 250μg/mL-1000μg/mL in assays for hemolytic and antihemolytic activity. The oxidant and antioxidant activities on human hemoglobin were determined at different concentrations of the test extract. The test product presented MIC=1000µg/mL and MBC= 1300µg/mL, respectively, for Streptococcus viridans and Streptococcus pyogenes, demonstrating a bacteriostatic nature. In the association study of the extract with azithromycin against the Streptococcus viridans strain, the effect was indifferent, while in Streptococcus pyogenes the effect was antagonistic. The test extract at a concentration of 1000µg/mL prevented biofilm formation for both strains tested, but was unable to destroy pre-formed biofilm. In terms of hemolytic and anti-hemolytic activity, the product showed low activity on human erythrocytes in both tests. The green leaf extract did not show oxidizing activity. Regarding the antioxidant potential, a 65% reduction was observed compared to phenylhydrazine. The extract from the green leaves of Anacardium occidentale is safe for possible therapeutic applications, demonstrating effective antibacterial activity and low toxicological potential.

Recent Development of a Traditional Herbal Medicine, Stixis suaveolens (Roxb.) Pierre: Its Botany, Ethnomedicine, Phytochemistry, Pharmacology, and Toxicology

Background/Objective Plant-based products and their isolated compounds have been utilized in traditional medicine since early times. In folk medicine, Stixis suaveolens (Roxb.) Pierre has been used to treat painful tendons and bones, rheumatism, eye infections, cough, malaria, asthma, and cardiovascular diseases. This study aims to summarize up-to-date botany, ethnomedicine, phytochemical components, pharmacological effects, and toxicology. Methods Information on S. suaveolens was collected from databases such as the Web of Science, Scopus, Google Scholar, PubMed, Science Direct, Springer, and others. Results S. suaveolens has been demonstrated to possess various pharmacological effects, including antioxidant, antimicrobial, anti-inflammatory, antidiabetic, antidepressant, antidiarrheal, hepatoprotective, analgesic, antihemolytic, and thrombolytic activities. Phytochemical studies of this species have revealed the presence of secondary metabolites, including lignans, phenolics, alkaloids, and volatile components. Conclusion The pharmacological effects of the extracts and bioactive compounds resulting from the experimental studies in the review support the traditional uses of S. suaveolens. They could be useful in developing novel pharmacological applications in the treatment of various acute and chronic human ailments. The efficacy, safety, and toxicity of S. suaveolens plant in enhancing therapeutic efficacy should be investigated widely in further studies.

INVESTIGATION OF POTENTIAL ACTIVITIES OF PEGANUM HARMALA SEEDS: IN SILICO AND IN VITRO ANALYSES

Seeds of Peganum harmala L. have been traditionally used in Algerian medicine. This study investigates whether the antioxidant, antihemolytic, and anti-inflammatory activities of Peganum harmala extracts (PHE) are attributed to polyphenolic compounds, which are abundant in methanol, chloroform, and ethyl acetate extracts. Extraction and fractionation of polyphenols involved solvents with different polarities, resulting in a crude extract (CrE), a chloroform extract (CHE), and an ethyl acetate extract (EAE). The antioxidant potential of CrE and its fractions was assessed using the ferrothiocyanate (FTC) and thiobarbituric acid (TBA) assays. The inhibition of mice erythrocyte hemolysis was evaluated for methanol, chloroform, and ethyl acetate extracts in the presence of the oxidant (AAPH). PMA-induced mouse ear edema was used as an in vivo model for inflammation. The FTC assay demonstrated the strong antioxidant effect of CrE (87.64 ± 0.003%). EAE showed potent antioxidant activity with low MDA absorption levels. Assessment of antihemolytic effects against AAPH-induced oxidative hemolysis revealed significant protective effects of CrE and EAE, with EAE showing the most pronounced effect. In the in vivo model, CrE (100 mg/kg) exhibited substantial anti-inflammatory activity, inhibiting the ear edema. Computational analyses using molecular docking simulations showed that chlorogenic acid, hesperetin, and rutin have promising potential as inhibitors of COX-2 protein, which is a key component in inflammatory pathways. This study highlights the potent antioxidant properties of P. harmala, particularly in CrE, and its anti-inflammatory effects. The bioactive compounds, such as chlorogenic acid, hesperetin, and rutin, exhibit potential as anti-inflammatory agents. P. harmala could be a valuable natural source for potential medical applications, suggesting the need for further exploration in medical treatments.

Assessment of Anticancer Properties of Argemone mexicana L. and Berberine: A Comparative Study.

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.

Bacillus velezensis iturins inhibit the hemolytic activity of Staphylococcus aureus

Bovine mastitis caused by S. aureus has a major economic impact on the dairy sector. With the crucial need for new therapies, anti-virulence strategies have gained attention as alternatives to antibiotics. Here we aimed to identify novel compounds that inhibit the production/activity of hemolysins, a virulence factor of S. aureus associated with mastitis severity. We screened Bacillus strains obtained from diverse sources for compounds showing anti-hemolytic activity. Our results demonstrate that lipopeptides produced by Bacillus spp. completely prevented the hemolytic activity of S. aureus at certain concentrations. Following purification, both iturins, fengycins, and surfactins were able to reduce hemolysis caused by S. aureus, with iturins showing the highest anti-hemolytic activity (up to 76% reduction). The lipopeptides showed an effect at the post-translational level. Molecular docking simulations demonstrated that these compounds can bind to hemolysin, possibly interfering with enzyme action. Lastly, molecular dynamics analysis indicated general stability of important residues for hemolysin activity as well as the presence of hydrogen bonds between iturins and these residues, with longevous interactions. Our data reveals, for the first time, an anti-hemolytic activity of lipopeptides and highlights the potential application of iturins as an anti-virulence therapy to control bovine mastitis caused by S. aureus.

Natural deep eutectic solvents-mediated extraction of rosmarinic acid from Lamiaceae plants: Enhanced extractability and anti-inflammatory potential

Species from the Lamiaceae family (mint, sage, savory, rosemary, etc.) are widely used as culinary spices and teas and are recognized as a rich source of bioactive phytochemicals, especially rosmarinic acid (RA). In recent years, there is a tendency to reduce the use of solvents and processes that may be toxic and harmful to the environment. This study investigates the potential of the use of eco-friendly natural deep eutectic solvents (NADES) and ultrasound-mediated approach in the extraction of rosmarinic acid from Lamiaceae species. The chromatographic analysis demonstrated the promising ability of choline chloride-based NADES as RA extraction solvents. The majority of the prepared ready-to-use NADES extracts protect the erythrocyte membrane from lyses and showed pronounced antioxidant activity. Principal component analysis (PCA) showed that the DPPH and FRAP activities of extracts were related to RA, while other extracted compounds were responsible for ORAC and antihemolytic activity. Interestingly, pure NADES reduced the level of inflammatory mediator PGE2 in lipopolysaccharide (LPS)-stimulated monocytes. A solubility study of pure RA indicates that NADES may serve as an alternative to organic solvents.

Physalin H, physalin B, and isophysalin B suppress the quorum-sensing function of Staphylococcus aureus by binding to AgrA.

The virulence of Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA), depends on the expression of toxins and virulence factors controlled by the quorum-sensing (QS) system, encoded on the virulence accessory gene regulator (agr) locus. The aim of this study was to identify a phytochemical that inhibits Agr-QS function and to elucidate its mechanism. We screened 577 compounds and identified physalin H, physalin B, and isophysalin B--phytochemicals belonging to physalins found in plants of the Solanaceae family--as novel Agr-QS modulators. Biological analyses and in vitro protein-DNA binding assays suggested that these physalins suppress gene expression related to the Agr-QS system by inhibiting binding of the key response regulator AgrA to the agr promoters, reducing the function of hemolytic toxins downstream of these genes in MRSA. Furthermore, although physalin F suppressed gene expression in the Agr-QS system, its anti-hemolytic activity was lower than that of physalins H, B, and isophysalin B. Conversely, five physalins isolated from the same plant with the ability to suppress Agr-QS did not reduce bacterial Agr-QS activity but inhibited AgrA binding to DNA in vitro. A docking simulation revealed that physalin interacts with the DNA-binding site of AgrA in three docking states. The carbonyl oxygens at C-1 and C-18 of physalins, which can suppress Agr-QS, were directed to residues N201 and R198 of AgrA, respectively, whereas these carbonyl oxygens of physalins, without Agr-QS suppression activity, were oriented in different directions. Next, 100-ns molecular dynamics simulations revealed that the hydrogen bond formed between the carbonyl oxygen at C-15 of physalins and L186 of AgrA functions as an anchor, sustaining the interaction between the carbonyl oxygen at C-1 of physalins and N201 of AgrA. Thus, these results suggest that physalin H, physalin B, and isophysalin B inhibit the interaction of AgrA with the agr promoters by binding to the DNA-binding site of AgrA, suppressing the Agr-QS function of S. aureus. Physalins that suppress the Agr-QS function are proposed as potential lead compounds in the anti-virulence strategy for MRSA infections.