Cancer Cell Line A549 Research Articles

Cytotoxic tirucallanes from Dysoxylum alliaceum stem barks in human cancer and normal cells lines

The Dysoxylum genus that belongs to the Meliaceae family is widely distributed from India and Sri Lanka throughout Malaysia and Indonesia to Australia and New Zealand. Numerous types of compounds have been reported, including sesquiterpenoids, limonoids, triterpenoids, and alkaloids. One of the members of this genus is Dysoxylum alliaceum. Reports on the phytochemical constituents of this species are limited. During our search for naturally occurring tropical plant compounds with intriguing structures and biological properties, the stembark of D. alliaceum, which showed cytotoxic activity against MCF-7, A549 and CV-1 cell lines, was investigated. This paper also describes the chemical structure of the isolated compounds using HR-ESI-MS, FTIR, and NMR. As a result, eight triterpenoid compounds belonging to tirucallane-type (1-8) were identified, including cneorin-NP36 (1) toonapubesin A (2), toonapubesin B (3), chisopanin M (4), 21 α-methylmelianodiol (5), 21 β-methylmelianodiol (6), hispidone (7), and odoratone (8). These compounds are newly discovered in this plant. Furthermore, toonapubesin A (2) showed the highest selectivity against A549 cancer cell lines with IC50 value of 7.81±0.02 μM, resulting in no activity towards CV-1 cells. The current result could indicate that this plant produces potential natural product compounds with anticancer properties.

Synthesis of novel cyanopyridine compounds as potential EGFR inhibitors targeting A549 and PC3 cancer cell lines: In vitro, In vivo and ADME pharmacokinetics studies

Developing new leads for fighting cancer is a challenge for organic and medicinal chemists; hence, new functionalized pyridines have been synthesized via several transformations, including new amide bond formation, cyclization, and hydrazone synthesis. Aminolysis of the ethyl ester 2 with benzylamine affords the benzyl amide 3. Hydrazinolysis of the ester 2 afforded hydrazide 4. Hydrazide 4 used as precursor to obtain new hydrazino- and cyclized derivatives 5–10. Moreover, new series of hydrazone derivatives 11–17 were synthesized by condensation 2-((3-Cyano-4,6-dimethylpyridin-2-yl)oxy)acetohydrazide 4 with aromatic aldehydes and ketones. The synthesized compounds were subjected to cytotoxic screening against A549 and PC3 cells. Compounds 6 and 15 exhibited remarkable cytotoxic activities with IC50 values of 0.85 μM and 1.88 μM against A549 cells and IC50 values of 3.63 μM and 1.58 μM against PC-3 cells. Compounds 6, 8, and 15 exhibited promising EGFR inhibition with IC50 values of 42.6, 60.36, and 89.6 nM, respectively, compared to Erlotinib (93.7 %, IC50 = 78.6 nM). Moreover, compound 6 significantly activated apoptotic cell death in A549 cells, increasing the cell apoptosis by 76.7-fold (37.6 % in treated compared to 0.48 % for control) and arresting the cell cycle at S-phase by 32.56 % compared to control 24.03 %. Additionally, compound 6 caused tumor inhibition by 50.1 % of solid tumor in the SEC-bearing mice by interfering with EGFR enzymatic activity via considerable apoptosis-induction, which make it an attractive lead compound for the development of a chemotherapeutics to treat lung cancer.

Comprehensive Analysis of 11 Species of Euodia (Rutaceae) by Untargeted LC-IT-TOF/MS Metabolomics and In Vitro Functional Methods.

The Euodia genus comprises numerous untapped medicinal plants that warrant thorough evaluation for their potential as valuable natural sources of herbal medicine or food flavorings. In this study, untargeted metabolomics and in vitro functional methods were employed to analyze fruit extracts from 11 significant species of the Euodia genus. An investigation of the distribution of metabolites (quinolone and indole quinazoline alkaloids) in these species indicated that E. rutaecarpa (Euodia rutaecarpa) was the most widely distributed species, followed by E. compacta (Euodia compacta), E. glabrifolia (Euodia glabrifolia), E. austrosinensis (Euodia austrosinensis), and E. fargesii (Euodia fargesii). There have been reports on the close correlation between indole quinazoline alkaloids and their anti-tumor activity, especially in E. rutaecarpa fruits which exhibit effectiveness against various types of cancer, such as SGC-7901, Hela, A549, and other cancer cell lines. Additionally, the E. rutaecarpa plant contains indole quinazoline alkaloids, which possess remarkable antibacterial properties. Our results offer novel insights into the utilization of Euodia resources in the pharmaceutical industry.

Synthesis, Biological Investigation, and Molecular Docking of Novel Benzimidazole‐Hydrazone Hybrids as Potential Anticancer Agent Candidates

AbstractIn this study, six novel Benzimidazole‐hydrazone derivatives starting from the commercially available 1H‐benzo[d]imidazole‐2‐amine were synthesized, and the molecular structure of the obtained compounds were confirmed by NMR, FTIR and MS spectroscopic techniques. The anticancer activities of the synthesized compounds were investigated against HT29 (Human colon adenocarcinoma) and A549 (Human non‐small cell lung cancer) cancer cell lines using xCELLigence real‐time cell analysis. Cell apoptosis was determined by DNA laddering assay and Annexin V/FITC flow cytometer. Compound 4 c exhibited the best anticancer potency against both cancer cell lines (A549 and HT29) with IC50 values of 0.0019 μM and 0.0093 μM, respectively. Compound 4 c reduced the growth of A549 and HT29 cells in vitro and induced early apoptosis of A549 and HT29 cells. Additionaly, all compounds demonstrated favorable pharmacokinetics properties compared to Paclitaxel (reference compound) and the best docking scores were obtained for compounds 4 e and 4 b among the compounds.

Phytochemical Investigation of Tecoma capensis Flower Aqueous Extract and In Vitro Biological Studies: Anti‐Bacterial and Anti‐Proliferative Activities of its Silver Nanoparticles

AbstractIn this study, we report the synthesis of silver nanoparticles (AgNPs) from Tecoma capensis flower aqueous extract (TcAqFE). The impact of AgNPs on microstructural, optical, antibacterial and antiproliferative properties have been investigated through UV‐visible spectroscopy, X‐ray diffraction, transmission electron microscopy (TEM), fourier infra‐red spectroscopy (FTIR), agar well diffusion technique assay and MTT. The particles size estimated from TEM and XRD is in the range of 1–10 nm. The XRD pattern reveals that the Tecoma capensis silver nanoparticles (TcAgNPs) have a cubic crystal structure. FTIR spectra showed band positions at 1071, 1358, 1620, 1962, 2150, 2920 and 3361 cm−1. Surface plasmon resonance (SPR) in AgNPs became evident with an absorption peak at 407 nm. GC‐MS analysis of ethanolic flower extract revealed the presence of major phytochemical constituents, including Butanal (57.14 %), Propanol (20.23 %), Ethanone (4.88 %), Mesitylene (3.70 %), Hexanal (3.33 %), 4‐Cyclopentene‐1,3‐diol, trans (3.16 %), Furan (2.94 %), 5‐Hepten‐2‐one (2.58 %), and Acetic acid (1.68 %). The antibacterial assay results clearly indicate that the TcAgNPs exhibited the maximum activity against Salmonella typhi, with inhibition zone (IZ) values of (40±1.4 mm), followed by Bacillus subtilis (35.66±2.0 mm), Staphylococcus aureus (32.6±0.64 mm), Escherichia. coli (29.66±2.05 mm), Listeria monocytogenes (27±1.63 mm), and Klebsiella pneumoniae exhibiting the least IZ values (23±1.6 mm). Minimum inhibitory concentration (MIC) values ranged from 0.20 to 2.81 mg/mL. The highest MIC value 2.81 mg/mL was observed in case of Salmonella typhi, while Staphylococcus aureus (0.20 mg/mL), displayed the lowest MIC values. The MIC of Gentamycin also ranged from 0.012 to 0.024 mg/mL. MTT assay demonstrated that the aqueous extract was potent against the cancer cell line A549, with a GI50 of 71.79 μg/mL. These results suggest that TcAgNPs have therapeutic potential and can serve as antibacterial and antiproliferative agents to protect against several ailments.

Two new sesquiterpene glycosides from Dendrobium findleyanum

One new ylangene-type sesquiterpene glycoside, findlayanoside C (1), and one new picrotoxane-type sesquiterpene glycoside, findlayanoside D (3), together with five known sesquiterpene glycosides, dendrofindlayanoside C (2), dendronobiloside B (4), dendronobiloside A (5), dendroside F (6) and dendromoniliside D (7), have been isolated from the stems of Dendrobium findleyanum. The structures of compounds 1 and 3 were elucidated by means of extensive spectroscopic analyses, and their absolute configuration were confirmed by electronic circular dichroism (ECD) calculations. Cytotoxic activity assays against SMMC-7721, A-549 and MCF-7 human cancer cell lines revealed IC50 values of 10.12, 12.32 and 14.13 μM for compound 1, and of 9.25, 13.16 and 16.26 μM for compound 2. This study enriches the anti-tumour sesquiterpenoids composition of D. findleyanum.

Anticancer Potential of a Synthetic Quinoline, 9IV-c, by Inducing Apoptosis in A549 Cell and In vivo BALB/c Mice Models.

In a previous work from the author of this study, the compound of 9IV-c, ((E)-2-(3,4- dimethoxystyryl)-6,7,8-trimethoxy-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine) was synthesized, and the effects of potent activity on the multiple human tumor cell lines were evaluated considering the spindle formation together with the microtubule network. Accordingly, cytotoxic activity, apoptotic effects, and the therapeutic efficiency of compound 9IV-c on A549 and C26 cell lines were investigated in this study. The compound 9IV-c demonstrated high cytotoxicity against A549 and C26 cell lines with IC50 = 1.66 and 1.21 μM, respectively. The flow cytometric analysis of the A549 cancer cell line treated with compound 9IVc showed that This compound induced cell cycle arrest at the G2/M phase and apoptosis. Western blotting analysis displayed that compound 9IV-c also elevated the Bax/Bcl-2 ratio and increased the activation of caspase-9 and -3 but not caspase-8. These data presented that the intrinsic pathway was responsible for 9IV-c -induced cell apoptosis. In vivo studies demonstrated that treatment with the compound of 9IV-c at 10 mg/kg dose led to a decrease in tumor growth compared to the control group. It was found that there was not any apparent body weight loss in the period of treatment. Also, in the vital organs of the BALB/c mice, observable pathologic changes were not detected.

Synergistic inhibitory actions of resveratrol, epigallocatechin-3-gallate, and diallyl trisulfide against skin cancer cell line A431 through mitochondrial caspase dependent pathway: a combinational drug approach.

The harmful effect of chemotherapeutic side effects has paid a way to discover a novel with curative way for skin cancer treatment. Skin cancer prevention is more viable with the use of combination of bioactive agents than using of single bioactive compounds. Present work was demonstrated to evaluate the interaction of Resveratrol (Res), Epigallocatechin-3-gallate (EGCG), and diallyl trisulfide (DATS) with each other as a binary combination on A431 cells. Nuclear fragmentation analysis of combination of bioactive agents using DAPI analysis, detection of apoptosis, analysis of cell cycle, ROS assay, antimigration assays, and western blotting were implemented to study the combination of bioactive compounds on A431 cell line. Among the selected combination EGCG + DATS had a synergetic effect reducing cellular migration, increased intercellular reactive oxygen species generation, condensation, cell phagocytosis induced by phosphatidylserine externalization, rise in sub-G1 DNA content, and S-phase were cell cycle arrest. The combinations EGCG + DATS induced apoptotic proteins in A431 cells by upregulation of proapoptotic Bax and Bad proteins, a downmodulation of anti-apoptotic proteins Bcl2 and caspases (caspase-3, and -9) activity got triggered by intrinsic pathway. The combination of EGCG + DATS showed good anticancer potential against A431 skin cancer cell line via the mitochondrial caspase dependent pathway with very strong synergism. This finding will help to produce a novel combination/chemoprevention using dietary bioactive agents (EGCG + DATS) for the treatment of skin cancer after clinical trial.

New cassane-type alkaloids and diterpenoids from the pericarps of Caesalpinia bonduc

The phytochemical investigation of the pericarps of Caesalpinia bonduc led to the isolation and identification of five new cassane-type alkaloids: caesalminines C − G (1–5) and six new diterpenoids: caesalbonducin K − P (6–11), along with seven known compounds (12–18). Compounds 1–5 were identified as a group of rare alkaloids possessing a tetracyclic cassane-type diterpenoid skeleton with a lactam D-ring instead of a typical furan or lactone moiety. The structures of 1–11 were elucidated on the basis of 1D and 2D NMR including HSQC, HMBC, COSY and NOESY, and other spectroscopic analyses. The cytotoxic activities of the isolated compounds were evaluated in the A431, A549 and U87MG cancer cell lines.

Ruthenium-Cyclopentadienyl-Cycloparaphenylene Complexes: Sizable Multicharged Cations Exhibiting High DNA-Binding Affinity and Remarkable Cytotoxicity.

Two novel sizable multicharged cationic complexes, of the formulae [(η6--[12]CPP)[Ru(η5--Cp)]12]Χ12 and [(η6--[11]CPP)[Ru(η5--Cp)]11]Χ11, CPP = cycloparaphenylene, Cp = cyclopentadienyl, X = [PF6]-, (1), (3) and [Cl]-, (2), (4), were synthesized and characterized using NMR techniques, high-resolution mass spectrometry, and elemental analyses. Complexes (1) and (3) were stable in acetone and acetonitrile solutions over 48 h. In contrast, the water-soluble (2) and (4) begin to decompose in aqueous media after 1 h, due to the [Cl]- tendency for nucleophilic attack on ruthenium of the {Ru(η5--Cp)} units. Fluorescence quenching experiments conducted during the stability window of (2) with the d(5'-CGCGAATTCGCG-3')2-EtBr adducts revealed remarkably high values for Ksv = 1.185 × 104 ± 0.025 M-1 and Kb = 3.162 × 105 ± 0.001 M-1. Furthermore, the cytotoxic activity of (2) against A2780, A2780res, and MCF-7 cancer cell lines shows that it is highly cytotoxic with IC50 values in the range of 4.76 ± 1.85 to 16 ± 0.81 μΜ.

Clerodendrum chinense Stem Extract and Nanoparticles: Effects on Proliferation, Colony Formation, Apoptosis Induction, Cell Cycle Arrest, and Mitochondrial Membrane Potential in Human Breast Adenocarcinoma Breast Cancer Cells.

Breast cancer stands out as the most widespread form of cancer globally. In this study, the anticancer activities of Clerodendrum chinense (C. chinense) stem ethanolic extract were investigated. High-performance liquid chromatography (HPLC) analysis identified verbascoside and isoverbascoside as the major bioactive compounds in the C. chinense stem extract. Successfully developed nanoparticles exhibited favorable hydrodynamic diameter, polydispersity index, and surface charge, thus ensuring stability after four months of storage. The total phenolic content and total flavonoid contents in the nanoparticles were reported as 88.62% and 95.26%, respectively. The C. chinense stem extract demonstrated a dose-dependent inhibitory effect on MCF-7, HeLa, A549, and SKOV-3 cancer cell lines, with IC50 values of 109.2, 155.6, 206.9, and 423 µg/mL, respectively. C. chinense extract and NPs exhibited dose-dependent cytotoxicity and the highest selectivity index values against MCF-7 cells. A dose-dependent reduction in the colony formation of MCF-7 cells was observed following treatment with the extract and nanoparticles. The extract induced cytotoxicity in MCF-7 cells through apoptosis and necrosis. C. chinense stem extract and nanoparticles decreased mitochondrial membrane potential (MMP) and induced G0/G1 phase arrest in MCF-7 cells. In conclusion, use of C. chinense stem extract and nanoparticles may serve as a potential therapeutic approach for breast cancer, thus warranting further exploration.

Exploring Brilliant Blue FCF Assembly with Beta Cyclodextrin, Characterizations and Applications in Biological Systems Using Physicochemical and Computational Methods

AbstractThis research delvedinto the BrilliantBlue FCF (BB) dye encapsulation within the nano hydrophobic cavity of β‐cyclodextrin (β‐CD) utilizing various spectroscopic and physicochemical techniques. Job's plot using UV‐visible and Fluorescence spectroscopy, surface tension, and conductance study confirmed 1 : 1 stoichiometry of theinclusion complex (BBIC).1H NMR and FT‐IR studies demonstrated the possible binding mode of BB into the β‐CD cavity, which wasin good agreement withthe DFT study. The degree of affinity of β‐CD for BB in the ground state and excited state were estimatedfromUV‐visible andFluorescence spectroscopy(binding constant=8113.9451 M−1and10199.563 M−1), andthe negative free binding energyshowedthe encapsulation process to bethermodynamically feasible. PXRD analysis and SEM image studies revealed the formation of the BBIC. After complexation with β‐CD, the photostability of BB was found to be enhanced. The interaction study of BB and BBIC with CT‐DNA revealed the sustained release of BB from the complex. Furthermore, neither BBICnor free BB exhibited a significant cytotoxic effect on the normal cell line HEK‐293. However, BBIC complex (IC50=6.15 μM) showed significant in vitrocytotoxic activity compared to pure BB (IC50=8.90 μM) towards cancer cell line A549.

Acylation of Oleanolic Acid Oximes Effectively Improves Cytotoxic Activity in In Vitro Studies.

(1) Background: The aim of the presented work was to obtain a set of oleanolic acid derivatives with a high level of anticancer activity and a low level of toxicity by applying an economic method. Three types of oleanolic acid derivatives were obtained: (i) derivatives of methyl oleanonate oxime, (ii) derivatives of methyl oleanonate oxime with an additional 11-oxo function, and (iii) derivatives of morpholide of oleanonic acid oxime. (2) Methods: The above oximes were acylated with aliphatic or aromatic carboxylic acid. The newly obtained compounds were subjected to ADMETox analysis and were also tested for cytotoxicity activity on the HeLa, KB, MCF-7, A-549, and HDF cell lines with the MTT assay. (3) Results: Among the tested acylated oximes of oleanolic acid, some derivatives, particularly those with two nitro groups attached to the aromatic ring, proved to be the most potent cytotoxic agents. These triterpene derivatives significantly inhibited the growth of the HeLa, KB, MCF-7, and A-549 cancer cell lines in micromolar concentrations. (4) Conclusions: The introduction of different moieties, particularly the 3,5-dinitro group, resulted in the synthesis of highly potent cytotoxic agents with favorable SI and ADMETox parameters.

C-30 analogues of betulinic acid as potent cytotoxic agents: design, synthesis, biological evaluation and in-silico studies

In an endeavour to improve the anti-cancer activity of betulinic acid (BA), a series of C-30 derivatives were envisaged and synthesized with a novel synthetic approach. All the derivatives were evaluated for cytotoxic activity by MTT assay against six different human cancer cell lines: prostate (PC3), lung (A549), human hepatocellular carcinoma (HepG2), human leukemia (Molt-4), pancreatic (Panc-1) and breast (MCF-7). The data revealed that compound 16 was observed most promising cytotoxic agent with IC50 values of 7.43 μM, 9.1 μM, and 9.64 μM against A549, MCF-7, and PC3 cancer cell lines respectively. A further mechanistic study confirmed compound 16 showed significant cell death by arresting the cell cycle in the G1 phase and inducing apoptosis in A549 cells. Communicated by Ramaswamy H. Sarma

Development of new thieno[2,3-d]pyrimidines as dual EGFR and STAT3 inhibitors endowed with anticancer and pro-apoptotic activities

In part due to the resilience of cellular feedback pathways that develop therapeutic resistance to targeting the EGFR alone, using EGFR inhibitors alone was demonstrated to be unsuccessful in clinical trials. The over-activation of the signal transducer/activator of transcription 3 (STAT3) during the administration of an EGFR inhibitor is expected to play a substantial part in the failure and resistance of EGFR inhibitor treatment. Therein, we proposed a hypothesis that induced STAT3-mediated resistance to EGFR inhibition therapy could be addressed by a dual inhibition of EGFR and STAT3 method. To this end, we tried to discover new thieno[2,3-d]pyrimidine derivatives “5a-o”. Results from the screening on A549 and MCF7 cancer cell lines revealed that compounds 5j and 5k showed two-digit nanomolar with appropriate safety towards the WI-38 cell line. The best molecules, 5j and 5k, were subjected to γ-radiation, and their cytotoxic efficacy didn’t change after irradiation, demonstrating that not having to use it avoided its side effects. Compounds 5j and 5k demonstrated the highest inhibition when their potency was tested as dual inhibitors on EGFR 67 and 41 nM, respectively, and STAT3 5.52 and 3.34 nM, respectively, proved with in silico molecular docking and dynamic simulation. In light of the results presented above, the capacity of both powerful compounds to alter the cell cycle and initiate the apoptotic process in breast cancer MCF7 cells was investigated. Caspase-8, Bcl-2, Bax and Caspase-9 apoptotic indicators were studied.

Triiron Complex with N-Ferrocenyl Aminocarbyne Ligand Bridging a Diiron Core: DFT, Electrochemical, and Biological Insights.

The first N-ferrocenyl aminocarbyne complex, [Fe2Cp2(CO)2(μ-CO){μ-CN(Me)(Fc)}]CF3SO3 ([2]CF3SO3), was synthesized with an 88% yield from [Fe2Cp2(CO)4], isocyanoferrocene (CNFc), and methyl triflate. The synthesis proceeded through the intermediate formation of [Fe2Cp2(CO)3(CNFc)], 1. Multinuclear NMR experiments revealed the presence of cis and trans isomers for [2]CF3SO3 in organic solvents, in agreement with DFT outcomes. Electrochemical and spectroelectrochemical studies demonstrated one reduction process occurring prevalently at the diiron core and one oxidation involving the ferrocenyl substituent. The oxidation process is expected to favor the redox activation of [2]+ in a biological environment. Both [2]CF3SO3 and its phenyl analogue [Fe2Cp2(CO)2(μ-CO){μ-CN(Me)(Ph)}]CF3SO3 ([3]CF3SO3), prepared for comparison, exerted moderate antiproliferative activity against the human cancer cell lines A431, HCT-15, PSN-1, 2008, and U1285. However, [2]CF3SO3 exhibited a higher cytotoxicity than [3]CF3SO3, showed a substantial ability to induce intracellular ROS production, and outperformed cisplatin in a three-dimensional SCLC cell model.

Dihydrophenanthro[b]furan derivatives from the tubers of Bletilla striata

Two pairs of new dihydrophenanthro[b]furan enantiomers blephebibnols G–H (1–2), one new dihydrophenanthro[b]furan derivative blephebibnol I (3), along with four known analogues (4–7), were isolated from the tubers of Bletilla striata. Their structures including the absolute configurations were determined by the combination of spectroscopic data analysis, ECD and NMR calculations. Compounds 1a, 1b, and 2b showed inhibition of NO production in LPS-stimulated BV-2 cells, with IC50 values ranging from 4.11 to 14.65 μM. Further mechanistic study revealed that 1a suppressed the phosphorylation of p65 subunit to regulate the NF-κB signaling pathway. In addition, some compounds displayed selective cytotoxic activities against HCT-116, HepG2, A549, or HGC27 cancer cell lines with IC50 values ranging from 0.1 to 8.23 μM.

Investigating the Medicinal Potential of Lavatera cashmeriana Leaf Extract: Phytochemical Profiling and In Vitro Evaluation of Antimicrobial, Antioxidant, and Anticancer Activities.

This study investigated the medicinal potential of Lavatera cashmeriana, a plant traditionally known for its therapeutic properties. The aim was to identify the phytocompounds in L. cashmeriana leaf extract and evaluate its antibacterial, antioxidant, and anticancer effects. Gas chromatography-mass spectrometry analysis was employed to characterize the phytochemical composition of the ethanol extract derived from L. cashmeriana leaves. The antimicrobial potential was assessed through the well diffusion technique, targeting Escherichia coli, Enterococcus faecalis, Pseudomonas aeruginosa, Staphylococcus aureus, and Candida albicans. The 2,2-diphenyl-1-picrylhydrazyl assay was conducted to assess antioxidant capabilities, while cytotoxicity against the A549 cancer cell line was determined via the MTT assay. GC-MS analysis identified ten different compounds, with phytol, 1-Eicosanol, and 2,6,10-trimethyl,14-ethylene-14-pentadecne being the most prevalent. The extract exhibited notable antimicrobial efficacy against all bacteria with MIC values ranging from 62.5 to 250 µg/mL. However, C. albicans did not respond. The extract exhibited antioxidative properties with an IC50 value of 86 µg/mL and cytotoxicity with an IC50 value of 69.95 µg/mL against the A549 cancer cell line. The results derived from this study supported the historical use of L. cashmeriana as a medicinal plant and suggested that it can potentially treat a wide range of medical ailments. The identified phytocompounds and the demonstrated antibacterial, antioxidant, and anticancer effects provide scientific evidence for its medicinal properties. However, further investigations are needed to fully understand its safety profile, efficacy, and mechanism of action before recommending it for therapeutic purposes.

Antimicrobial, antioxidant and antiproliferative activities of a galactose-binding seed lectin from Manilkara zapota

A seed lectin from Manilkara zapota (MZSL) was purified using ammonium sulphate precipitation and affinity chromatography. Hemagglutination activity, neutral sugar content and physicochemical properties of the lectin were determined and toxicity was checked by brine shrimp toxicity assay. Antimicrobial, antioxidant as well as in vitro anticancer activities of MZSL were also evaluated. Our findings showed the molecular weight of MZSL to be 33.0 ± 1 kDa. Minimum hemagglutination concentration of the lectin was 15.625 μg/ml. With a neutral sugar content of 6.32 %, the lectin was fully active at a temperature range of 30–50 °C and pH 7.0–8.0 and it was mildly toxic with an LC50 value of 107.93 μg/ml. The lectin demonstrated bacteriostatic activity against gram-positive bacteria in contrast to gram-negative bacteria at a concentration of 31.25 μg/ml, agglutinated Staphylococcus aureus and Shigella dysenteriae and exerted fungistatic activity against Aspergillus niger. MZSL dose-dependently reduced the formation of biofilm by E. coli. DPPH assay confirmed its antioxidant activity with an IC50 value of 96.42 μg/ml. MZSL showed 21.64 % growth inhibition against Ehrlich ascites carcinoma (EAC) cells at 80 μg/ml whereas its antiproliferative potential against MCF-7 and A-549 cancer cell lines became evident with IC50 values of 70.66 μg/ml and 107.64 μg/ml, respectively.

The Isolation of 5-Hydroxymethylfuran Metabolites from the Broth Extract of Fomitopsis meliae (Agaricomycetes)

This study aimed to identify antibacterial compounds from the broth extract of <i>Fomitopsis meliae</i> (MSUCC009). From small-scale fermentation, the broth extract of <i>F. meliae</i> showed antibacterial activity. Therefore, the fermentation of this fungal strain was scaled up and the broth extract was chemically investigated. Purification of the broth extract led to the isolation of two 5-hydroxymethylfuran metabolites, 5-hydroxymethyl-2- furoic acid methyl ester and 5-hydroxymethyl-2-furancarboxylic acid (HMFCA) together with a pyrimidine base, uracil. This is the first isolation report of 5-hydroxymethylfuran derivatives from the genus <i>Fomitopsis</i>. The structures of isolated compounds were elucidated based on nuclear magnetic resonance (NMR) and mass spectrometry (MS) spectroscopic methods, and comparison with previous reports. 5-Hydroxymethyl-2-furancarboxylic acid exhibited antibacterial activity against methicillin-susceptible <i>Staphylococcus aureus</i> with MIC and MBC values of > 0.25 mg/mL. 5-Hydroxymethyl-2-furoic acid methyl ester and 5-hydroxymethyl-2-furancarboxylic acid were also tested against A549 cancer cell lines. These two compounds were inactive in this cytotoxicity assay.