MCF-7 Human Breast Carcinoma Cells Research Articles

New pyranopyrazole based derivatives: Design, synthesis, and biological evaluation as potential topoisomerase II inhibitors, apoptotic inducers, and antiproliferative agents

A new series of pyranopyrazole-based derivatives were designed and synthesized. The synthesized compounds were assessed for their cytotoxic efficacy against A549 human lung carcinoma and MCF-7 human breast carcinoma cell lines. Three compounds (1b, 4b, and 7b) exhibited 1.3- to 2.3-fold more antiproliferative activity than that of doxorubicin against the A549 cell line. In comparison to doxorubicin, compounds 1d and 3b were 4.1- and 1.04-fold, respectively more powerful against MCF-7 cancer cells. All the synthesized compounds were found to be more selective toward A549 cancer cells than the normal human fibroblast BJ cells. Of interest, compounds 1b and 7b exhibited promising cytotoxicity and SIs of 27.72 and 25.30, respectively, towards A549 cancer cells, higher than that of doxorubicin (SI 4.81). The most potent compounds 1b, 1d, 3b, 4b, and 7b were then subjected to in vitro Topo II inhibition assay. They showed IC50 values in the range of 2.07 to 8.86 µM. Of particular interest, compound 7b (IC50 = 2.07 µM), exhibited higher Topo II inhibitory activity than that of doxorubicin (IC50 = 2.56 µM). The significant Topo II inhibition of compound 7b was explained by molecular docking simulations into the Topo II active site. Compound 7b halted the cell cycle in the S phase in A549 cancer cells. It induced total apoptosis and necrosis of 20.73- and 4-fold, respectively, greater than the control. This evidence was supported by a 3.59-fold increase in the level of apoptotic caspase-9 and a remarkable elevation of the Bax/BCL-2 ratio. The physiochemical parameters of compound 7b were aligned with Lipinski’s rule of five.

Functionalized Carbon Nanotubes for Delivery of Ferulic Acid and Diosgenin Anticancer Natural Agents.

It was investigated whether loading multi-wall carbon nanotubes (CNTs) with two natural anticancer agents: ferulic acid (FUA) and diosgenin (DGN), may enhance the anticancer effect of these drugs. The CNTs were functionalized with carboxylic acid (CNTCOOH) or amine (CNTNH2), loaded with the above pro-drugs, as well as both combined and coated with chitosan or chitosan-stearic acid. Following physicochemical characterization, the drug-loading properties and kinetics of the drug's release were investigated. Their effects on normal human skin fibroblasts and MCF-7 breast carcinoma cells, HepG2 hepatocellular carcinoma cells, and A549 non-small-cell lung cancer cells were evaluated in vitro. Their actions at the molecular level were evaluated by assessing the expression of lncRNAs (HULC, HOTAIR, CCAT-2, H19, and HOTTIP), microRNAs (mir-21, mir-92, mir-145, and mir-181a), and proteins (TGF-β and E-cadherin) in HepG2 cells. The release of both pro-drugs depended on the glutathione concentration, coating, and functionalization. Release occurred in two stages: a no-burst/zero-order release followed by a sustained release best fitted to Korsmeyer-Peppas kinetics. The combined nanoformulation cancer inhibition effect on HepG2 cancer cells was more pronounced than for A549 and MCF7 cells. The combined nanoformulations had an additive impact followed by a synergistic effect, with antagonism demonstrated at high concentrations. The nanoformulation coated with chitosan and stearic acid was particularly successful in targeting HepG2 cells and inducing apoptosis. The CNT functionalized with carboxylic acid (CNTCOOH), loaded with both FUA and DGN, and coated with chitosan-stearic acid inhibited the expression of lncRNAs and modulated both microRNAs and proteins. Thus, nanoformulations composed of functionalized CNTs dual-loaded with FUA and DGN and coated with chitosan-stearic acid are a promising drug delivery system that enhances the activity of natural pro-drugs.

Bisphenol A prevents MCF-7 breast cell apoptosis via the inhibition of progesterone receptor transactivation.

2,2-Bis(4-hydroxyphenyl)propane (bisphenol A; BPA) is an environmental endocrine-disrupting chemical. It mimics the effects of estrogen at multiple levels by activating estrogen receptors (ERs); however, BPA also affects the proliferation of human breast cancer cells independent of ERs. Although BPA inhibits progesterone (P4) signaling, the toxicological significance of its effects remain unknown. Tripartite motif-containing 22 (TRIM22) has been identified as a P4-responsive and apoptosis-related gene. Nevertheless, it has not yet been established whether exogenous chemicals change TRIM22 gene levels. Therefore, the present study investigated the effects of BPA on P4 signaling and TRIM22 and TP53 expression in human breast carcinoma MCF-7 cells. In MCF-7 cells incubated with various concentrations of P4, TRIM22 messenger RNA (mRNA) levels increased in a dose-dependent manner. P4 induced apoptosis and decreased viability in MCF-7 cells. The knockdown of TRIM22 abolished P4-induced decreases in cell viability and P4-induced apoptosis. P4 increased TP53 mRNA expression and p53 knockdown decrease the basal level of TRIM22 and P4 increased TRIM22 mRNA expression independent of p53 expression. BPA attenuated P4-induced increases in the ratio of cell apoptosis in a concentration-dependent manner, and the P4-induced decreases in cell viability was abolished in the presence of 100 nM and higher BPA concentrations. Furthermore, BPA inhibited P4-induced TRIM22 and TP53 expression. In conclusion, BPA inhibited P4-induced apoptosis in MCF-7 cells via the inhibition of P4 receptor transactivation. TRIM22 gene has potential as a biomarker for investigating the disruption of P4 signaling by chemicals.

The cancer preventive activity and mechanisms of prenylated resveratrol and derivatives

Resveratrol is regarded as neutraceuticals with multiple health benefits. The introduction of prenyl can enhance the bioactivity. In this work, the cancer preventive activities and mechanisms of 18 prenylated reseveratrol and derivatives were investigated. The results showed that prenyl increased the antiproliferative activities of resveratrol, oxyresveratrol and piceatannol against cancer cells, and their antiproliferative activities were time- and dose-dependent. 4-C-prenylation was important for the antiproliferative activity of stilbenoids. The 4-C-prenyl stilbenoids showed better antiproliferative activities than other prenylated stilbenoids. 4-C-prenyl piceatannol showed the best antiproliferative activity. Human hepatoellular carcinomas (HepG2) cell was more sensitive to prenylated stilbenoids than human MCF-7 breast carcinoma cell. 4-C-prenyl piceatannol had high affinities to Caspase-3, Caspase-9, CDK2 and Cyclin A2. The possible amino acids involved in binding 4-C-prenyl piceatannol were revealed. The expression of Caspase-3 and Caspase-9 were upregulated by 4-C-prenyl piceatannol and the expression of CDK2 and Cyclin A2 in HepG2 cells were downregulated, which contributed to apoptosis. The above results eludicated the possible antiproliferative mechanisms of prenylated stilbenoids.

Copper (II) complexes with N, S donor pyrazole-based ligands as anticancer agents.

A group of bidentate nitrogen and sulfur donor pyrazole derivative ligands abbreviated as Na[RNCS(Pz)], Na[RNCS(PzMe2)], Na[RNCS(PzMe3)], Na[RNCS(PzPhMe)], Na[RNCS(PzPh2)], where (R = Et, Ph), and their Cu (II) complexes were synthesized and characterized by spectroscopic and physicochemical methods. The crystal structure of [Cu(PhNCSPzMe3)2] was determined by X-ray crystallography analysis and the results described a distorted square planar coordination geometry for this complex. Also, the cyclic voltammetry investigations indicated that the synthesized copper complex is an electrochemically active species. Moreover, the cytotoxic activity of all of the twenty synthesized compounds was evaluated using MTT assay against the MCF-7 (human breast carcinoma) cell lines, in vitro. Cu (II) complexes indicate significant cytotoxicity against the MCF-7 cell lines as compared with the free ligands. The docking studies showed that the copper complexes have better interactions with EGFR and CDK2 proteins, compared to the free ligands, and most of the studied compounds have a higher value of binding energy relative to the studied controls. The results of QSAR analysis suggest that dipole moment is in direct correlation with the obtained IC50 values, and it strongly impact the anticancer effects generated by the compounds. Our findings suggest that the developed copper complexes can be good candidates for further evaluations as chemotherapeutic agents in the treatment of cancer.

Folic acid-decorated PEGylated magnetite nanoparticles as efficient drug carriers to tumor cells overexpressing folic acid receptor

The improved drug delivery systems (DDS) are needed for the targeted delivery of their therapeutic cargo (biologically active protein/peptide molecules, nucleic acids, vaccines, etc.) to diseased cells. Thus, we aimed to develop magnetite nanoparticles (Fe3O4), stabilized with polyethylene glycol (PEG) and decorated (surface-functionalized) with folic acid (FA) (Fe3O4@PEG@FA) to ensure targeted internalization in cells expressing the folic acid receptors (FR). The Fe3O4@PEG@FA nanoparticles were synthesized by co-precipitation in a one-pot methodology. Curcumin (Curc), a polyphenol with anti-tumoral activity, was loaded on the nanoparticles, and FA-targeted (Fe3O4@PEG@FA@Curc) and non-targeted (Fe3O4@PEG@Curc) systems were obtained. The internalization of Fe3O4@PEG@FA@Curc and Fe3O4@PEG@Curc nanoparticles was determined in two tumor cell lines, the FR-positive MCF-7 human breast carcinoma cell line and A549 human lung adenocarcinoma cell line, expressing a low level of FR. The results showed that MCF-7 cells internalize FA-functionalized nanoparticles to a greater extent than non-targeted ones and also than A549 cells. The competitive studies performed in the presence of FA in excess suggested that internalization is an FR-dependent process. The increased internalization of Fe3O4@PEG@FA@Curc nanoparticles in MCF-7 cells is correlated with increased cytotoxicity in this cell line compared to A549 cells. In conclusion, the FA-functionalized magnetic systems can ensure a better internalization of the nanoparticles and can be used to deliver various therapeutic agents, both in cancer treatment and also in the treatment of other inflammation-associated diseases such as rheumatoid arthritis, systemic lupus erythematosus, osteoarthritis, Crohn's disease or atherosclerosis.

Dithiocarbazate based oxidomethoxidovanadium(V) and mixed-ligand oxidovanadium(IV) complexes: Study of solution behavior, DNA binding, and anticancer activity

In this work, one oxidomethoxidovanadium(V) [VVO(L)(OMe)] (1) and two mixed-ligand oxidovanadium(IV) [VIVO(L)(phen)] (2), and [VIVO(L)(bipy)] (3) complexes have been synthesized using a tridentate bi-negative ONS donor dithiocarbazate as main ligand, H2L [where, H2L = S-benzyl-3-(2-hydroxy-3-ethoxyphenyl)methylenedithiocarbazate] along with 1,10-phenanthroline (phen) (for 2) and 2,2′-bipyridine (bipy) (for 3) as co-ligands. The ligand and complexes have been characterised by FT-IR, UV–vis, NMR, and HR-ESI-MS techniques. Distorted square pyramidal for 1, and distorted octahedral geometry for 2 and 3 was confirmed by single crystal X-ray crystallography. The behavior of 1–3 in solution medium has been investigated through various physicochemical techniques. It is observed that 1 completely and 2–3 partially decomposes and converts into a penta-coordinated species, [VIVO(L)(DMSO/H2O)] after the release of the methoxido group (1) or breaking of the diimine based co-ligands (2 and 3) in DMSO/aqueous solution. Interestingly, in DMSO/aqueous solution, 1 gets completely reduced and converted into the corresponding oxidovanadium(IV) species. Interaction of 1–3 with calf thymus DNA (CT-DNA) was investigated and the results show, complex 2 exhibited the maximum binding constants, Kb = 7.12 × 104 M−1. The anticancer potential of 1–3 was evaluated by cell viability assay against human breast carcinoma cell, MCF-7, and noncancerous mouse embryonic cell, NIH-3T3 and 2 was found to be the most cytotoxic complex (IC50 = 6.73 ± 0.36 μM) in the series. In addition, 2 selectively inhibit colony formation compared to the rest complexes. Also, the cell cycle studies of the complexes were performed using flow cytometry analysis.

Design, synthesis of anticancer and anti-inflammatory 4-(1-methyl-1H-indol-3-yl)-6-(methylthio) pyrimidine-5-carbonitriles

A novel series of 4-(1-methyl-1H-indol-3-yl)-6-(methylthio) pyrimidine-5-carbonitriles (4a–i) was synthesized and evaluated for anticancer potential against cell lines for breast cancer. Compounds 4b, 4e, and 4h exhibited prominent cytotoxicity against human breast carcinoma MCF-7 cell line with GI50 of 2.0, 0.5, and 0.5 µM, respectively. Molecular docking study against EGFR tyrosine kinase could provide valuable insights into the plausible mechanism of action. The compounds could bind with significantly high binding affinity and their binding affinity scores could correlate well with the observed anticancer activity. Furthermore, compounds 4a, 4c, 4e, 4g, and 4i exhibited significant inflammatory activities as well which could expand the therapeutic domain of this novel series.

Synthesis of New 1,2,4-Triazole Derivatives with Expected Biological Activities

To further study novel N-aceyl, N-thiourea and imidazole derivatives were synthesized. We used a multi-step reaction protocol that began with symmetrical 4-amino- 1,2,4-Triazole [I]. The new Schiff base [II] was derived by condensation of compound [I] with 4-aminoacetophenone in Ethanol and some drops from glacial acetic acid as a catalyst, whereas the Schiff base [III] was synthesized by reacting compound [II] with 4-hydroxyacetophenone in ethanol. N- acyl derivative [IV] was prepared by addition reaction of acetyl chloride to azomethine group of Schiff base [III] in dry benzene. Then, N-thiourea derivative [V] was prepared from reaction of thiourea with N-aceyl derivative [IV] in alkaline solution. The third step involved cyclization reaction of derivative [V] with 2-hydroxy-1,2-diphenylethan-1-one in dimethyl formamide (DMF) to obtain new imidazole derivative [VI]. The synthesized compounds were characterized on the spectroscopic data and their physical properties. Also, we studied the anti-bacterial activity of the prepared compounds against three types of bacteria: Staphylococcus aureus, Klebsiella pneumoniae and Pseudomonas aeruginosa, some of which showed best antibacterial activity comparable with Ampicillin, as standard antibiotic. Furthermore, the cytotoxic effect of various concentrations of the prepared compounds [II] and [VI] was investigated against MCF-7 (human breast carcinoma cells), Hep G2 (human liver cancer cell line) and WRL-68 (human hepatic cell line), revealing a moderate activity at 400 μl/ml, which had no effect on the growth of normal WRL-68 cells, and confirmed the safety of using this type of molecules in medications.

Sustained doxorubicin delivery system to breast tumor cancer cell based on a novel cationic molecularly imprinted polymer

In this study, Poly(methacrylic acid-co-diallyldimethylammonium chloride) or Poly(MAA-PDDA) was synthesized as a cationic molecularly imprinted nano-polymer. After in vitro assays such as cytotoxicity assay and hemolysis activity test, this imprinted nano-polymer was examined for targeted Doxorubicin (DOX) delivery in BALB/c mice bearing MCF7 human breast carcinoma cells. In vivo studies of synthesized nanoparticles on BALB/c mice showed their selectivity. Also, it was found that tumor growth delay (TGD) improved from 1.11 in DOX treated group to 2.82 in cationic polymer combined with DOX. Imprinted cationic polymer provides remarkable prevention of tumor growth. Investigating drug deposition in various tissues showed that DOX concentration was considerably more in tumors than in other tissues.

Design and Characterization of Maltoheptaose-b-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen.

Tamoxifen citrate (TMC), a non-steroidal antiestrogen drug used for the treatment of breast cancer, was loaded in a block copolymer of maltoheptaose-b-polystyrene (MH-b-PS) nanoparticles, a potential drug delivery system to optimize oral chemotherapy. The nanoparticles were obtained from self-assembly of MH-b-PS using the standard and reverse nanoprecipitation methods. The MH-b-PS@TMC nanoparticles were characterized by their physicochemical properties, morphology, drug loading and encapsulation efficiency, and release kinetic profile in simulated intestinal fluid (pH 7.4). Finally, their cytotoxicity towards the human breast carcinoma MCF-7 cell line was assessed. The standard nanoprecipitation method proved to be more efficient than reverse nanoprecipitation to produce nanoparticles with small size and narrow particle size distribution. Moreover, tamoxifen-loaded nanoparticles displayed spherical morphology, a positive zeta potential and high drug content (238.6 ± 6.8 µg mL−1) and encapsulation efficiency (80.9 ± 0.4 %). In vitro drug release kinetics showed a burst release at early time points, followed by a sustained release profile controlled by diffusion. MH-b-PS@TMC nanoparticles showed higher cytotoxicity towards MCF-7 cells than free tamoxifen citrate, confirming their effectiveness as a delivery system for administration of lipophilic anticancer drugs.

Incorporation of electroendocytosis and nanosecond pulsed electric field in electrochemotherapy of breast cancer cells

ABSTRACT The study aimed to evaluate the possibility to perform electrochemotherapy using nanosecond pulsed electric field (nsPEF) and low electric field (LEF) monopolar electrical impulses to alleviate the problems of conventional electroporation. Two types of pulses have been used to treat MCF-7 human breast carcinoma cell line: very low voltage (electric field strength) long trains of short unipolar electric pulses, and low frequencies of extremely intense (40kV/cm), ultra-short (10ns) electric pulses. The electropermeabilization efficiency of the formed endocytotic vesicles was measured using the cloning efficacy test. The cell viability was decreased significantly at a repetition frequency begins from 0.01 Hz by ~35% and reached complete cell loss at 1 Hz of nanosecond pulses for cells treated before with monopolar pulses at 20 V/cm in the presence of BLM with 4 µM concentration. The uptake of non-permeant drugs has been done without plasma membrane permeabilization (classical electroporation), but by endocytosis. Nanosecond electric pulses can disrupt the membrane of endocytotic vesicles and release the cytotoxic drug bleomycin.

Synthesis, spectroscopic and biological activity evaluation of Ni(II), Cu(II) and Zn(II) complexes of schiff base derived from pyridoxal and 4-fluorobenzohydrazide

A novel Schiff base ligand, 4-fluoro-N-((3-hydroxy-5-(hydroxymethyl)-2-methylpyridin-4-yl)methylene)benzohydrazide (PLFBH) was synthesized by condensationof pyridoxal and 4-fluorobenzohydrazide. Its complexes with Ni(II), Cu(II), and Zn(II) metal ionswere prepared and characterized by spectroscopic IR, 1H-NMR, UV, LC-MS, ESR, and powder XRD studies and by elemental analysis and thermal analysis, molar conductance, and magnetic susceptibility measurements. The results indicate the geometry of the complexes to be hexa coordinate distorted octahedral. Based on the electronic absorption and fluorescence emission spectra and viscosity studies, an intercalative mode of binding of the complexes with CT-DNA was suggested, which was also supported by DNA docking studies. The docking studies of metal complexes with DNA were carried out using Autodock 4.2. The in vitro anticancer assay for the Cu(II)-PLFBH complex was performed to assess the ability of the complex to inhibit human cell proliferation on HeLa human cervical carcinoma cells, MCF-7 human breast carcinoma cells, and A549 human lung carcinoma cells. The Cu(II)-PLFBH complex exhibited moderate to good inhibitory effect on the cancer cell lines studied. The complexes showed good cleavageability toward plasmid pBR322 DNA. The metal complexes were found to show good antibacterial activity against gram positive bacteria, Staphylococcus aureus and Bacillus cereus and gram negative bacteria Escherichia coli and Pseudomonas aeruginosa cultures,while the ligand showed marginal activity. Supplemental data for this article is available online at https://doi.org/10.1080/15257770.2021.1961271 .

Studies on non-medicinal parts of plant materials: Triterpenes from the roots of Schisandra chinensis

Phytochemical study on a non-medicinal part of a plant material for herbal medicine, the roots of Schisandra chinensis, was conducted to isolate five new triterpenes, schinensins A–D (1–4) and 3-O-methylchangnanic acid (5), together with 21 known compounds including 10 triterpenes, one sterol, two sesquiterpenes, seven lignans, and one flavonoid. The structures of new triterpenes (1–5) were assigned on the basis of spectroscopic analyses aided with TDDFT ECD calculations. Schinensin A (1) was a dinortriterpene possessing 28-norschiartane skeleton, while schinensins B–D (2–4) were assigned as 3,4:9,10-disecocycloartane, 3,4-secocycloartane, and cycloartane triterpenes, respectively. In an evaluation of antiproliferative activities against human cancer cell lines, some triterpenes exhibited significant activities against human breast carcinoma MCF-7 cells as compared to the other cell lines (A549, HeLa, and RPMI8226).

Augmentation of anti-proliferative, pro-apoptotic and oxidant profiles induced by piceatannol in human breast carcinoma MCF-7 cells using zein nanostructures

Piceatannol (PCT), a natural polyphenolic stilbene, has pleiotropic pharmacological potentials. It possesses cytotoxic activities toward variant cancerous cells. Zein nanospheres (ZN NSs) have been introduced as ideal nanostructures due to their natural origin, safety, histocompatibility. and convenient method of formulation. The purpose of this study was to explore the impact of PCT-ZN NSs formula on pharmacotherapy potential of PCT against human breast cancer MCF-7 cells. PCT-ZN NSs were formulated and characterized selectively to particle size, zeta potential, encapsulation efficiency and diffusion of PCT. The selected formula has a particle size of 84.4 ± 2.3 nm, zeta potential value of 33.8 ± 1.2 mV and encapsulation efficiency of 89.5 ± 4.1%. PCT-ZN NSs displayed significantly lower IC50 against MCF-7 cells by about 24 folds. Further, PCT-ZN NSs formula showed higher cellular uptake as compared to free PCT. Examination of cell cycle phases displayed cells accumulation in G2-M phase and increased percentage cells in pre-G1 phase indicating an apoptosis-enhancing activity. Annexin V staining indicated augmented early and late apoptosis. PCT-ZN NSs pro-apoptotic activity was confirmed by the observed significant increased mRNA expression of CASP3, p53, and Bax as well as decreased expression of Bcl2. In addition, PCT-ZN NSs induced oxidative stress as evidenced by depletion of glutathione reductase (GR) activity, increased generation of reactive oxygen species (ROS) and accumulation of lipid peroxidation products. Conclusively, ZN nanostructures of PCT revealed superior cell death-inducing activities against MCF-7 cells in comparison with free PCT. This is mediated, at least partly, by enhanced cellular uptake, pro-apoptotic activity, and oxidative stress potential.

Phenolic profiling and in vitro bioactivities of three medicinal Bryophyllum plants

Bryophyllum constitutes a subgenus within the genus Kalanchoe that contains several plant species used in traditional medicine worldwide for the treatment of several diseases. However, little is known about the phytoconstituents of Bryophyllum spp. and previous reports have pointed at their low in Planta concentrations of bioactive compounds. In this work, we take advantage of plant in vitro culture for the study of the phenolic compounds found in the aerial parts of Bryophyllum spp. and their associated bioactivities. Our results show that the induction of nutritional stress leads to an improved accumulation of phenolic compounds, mainly flavonols and anthocyanins, represented by myricetin and malvidin glycosides, respectively. This effect is mainly found for B. × houghtonii, whose hydroethanolic extracts promoted the highest antioxidant, cytotoxic and anti-inflammatory activities. In the case of cytotoxic activity, Bryophyllum extracts showed an enhanced activity against the MCF-7 human breast carcinoma cell line. Meanwhile, extracts from B. daigremontianum promoted a wide range of effectiveness against different bacterial and fungal strains. This study is committed to shed light about the phytochemical potential associated to this unexplored subgenus, with the aim of considering Bryophyllum spp. as a valuable source of bioactive compounds for their exploitation in food, cosmetic and pharmaceutical industries.

The effect of Rhus coriaria L. methanolic extract on cytotoxicity of Cladophora glomerata L. Kützing methanolic extract against human breast carcinoma MCF-7 cell line

The effect of Rhus coriaria L. methanolic extract on cytotoxicity of Cladophora glomerata L. Kützing methanolic extract against human breast carcinoma MCF-7 cell line

In vitro antimicrobial, antioxidant, cytotoxic activities, and wound healing potential of Thymbra capitata ethanolic extract

Abstract Objectives In this study, we aimed to detect the chemical compounds of Thymbra capitata ethanolic extract (TC-EtOH) as well as to evaluated its antimicrobial, antioxidant, cytotoxic activities, and in vivo wound healing effects. Methods The chemical composition of TC-EtOH was analyzed by Gas chromatography-mass spectrometry (GC-MS). Antioxidant and antimicrobial properties were determined with 2,2-diphenyl-1-picrylhydrazyl (DPPH), disc diffusion test and broth micro-dilution (minimal inhibitory concentration [MIC]) methods, respectively. Cytotoxic activity was tested on MG63 (human osteosarcoma) and MCF-7 (human breast carcinoma) cells by 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) assay. Tumor necrosis factor alpha (TNF-α) protein levels were determined by ELISA. Results The major components of TC-EtOH were tetratria contane (14.92%), camphor (12.50%), and terpineol (10.77%). TC-EtOH showed powerful antimicrobial activity in C. Tropicalis (0.03 mg/mL). The IC50 values of the TC-EtOH of the DPPH were determined 21.5 μg/mL. The IC50 values were calculated 37.28 and 44.40 μg/mL on the MG63 and MCF-7 cell lines, respectively. It was observed that the wounds treated with TC-EtOH showed a faster healing. Conclusions According to results, T. capitata species are thought to be natural antioxidants and a novel pharmaceutical compound for the pharmaceutical industry.

Fatty Acids and Other Chemical Compositions of Some Seagrasses Collected from the Saudi Red Sea with Potential of Antioxidant and Anticancer Agents

The fatty acids (FAs), amino acids (AAs), phenolic and polysaccharides from Cymodocea serrulata, Halodule uninervis, Halophila stipulacea and Thalassia hemprichii were studied, their antioxidant and anticancer activities were also investigated. The results showed that T. hemprichii and C. serrulata were rich in gallic acid and protocatechuic acid with values of 45.26 and 25.26 mg/g, respectively. The polysaccharides of T. hemprichii and H. stipulacea were mainly composed of galactose (~ 21%), mannose (~ 14.5%) and glucose (~ 12.5%). The protein contents ranged from 3.06% (H. stipulacea) to 9.56% (T. hemprichii). Palmitic acid (C16:0) percentage was more than half of the total FAs content of H. uninervis and T. hemprichii, while linoleic acid (C18:2) was 35.7 and 28.6%, respectively, in both seagrasses. The highest steroid content was found in C. serrulata at 92.67%, and triterpenes lupeol (15.51%) and β-amyrin (16.59%) in H. stipulacea as the major oxygenated-unsaponifiable matters. T. hemprichii extract demonstrated the highest effective antioxidant activity with IC50 value of 1.2 µg/ml, while H. uninervis extract displayed potential cytotoxic effect against human SKOV-3 ovarian and MCF-7 breast carcinoma cells with IC50 values of 0.52 and 2.3 µg/ml, respectively.

Evaluation of Antiviral, Antibacterial and Antiproliferative Activities of the Endophytic Fungus Curvularia papendorfii, and Isolation of a New Polyhydroxyacid.

An endophytic fungus isolated from Vernonia amygdalina, a medicinal plant from Sudan, was taxonomically characterized as Curvularia papendorfii. Ethyl acetate crude extract of C. papendorfii revealed an important antiviral effect against two viral pathogens, the human coronavirus HCoV 229E and a norovirus surrogate, the feline coronavirus FCV F9. For the last one, 40% of the reduction of the virus-induced cytopathogenic effect at lower multiplicity of infection (MOI) 0.0001 was observed. Selective antibacterial activity was obtained against Staphylococcus sp. (312 µg/mL), and interesting antiproliferative activity with half maximal inhibitory concentration (IC50) value of 21.5 ± 5.9 µg/mL was observed against human breast carcinoma MCF7 cell line. Therefore, C. papendorfii crude extract was further investigated and fractionated. Twenty-two metabolites were identified by gas chromatography coupled to mass spectrometry (GC–MS), and two pure compounds, mannitol and a new polyhydroxyacid, called kheiric acid, were characterized. A combination of spectroscopic methods was used to elucidate the structure of the new aliphatic carboxylic acid: kheiric acid (3,7,11,15-tetrahydroxy-18-hydroxymethyl-14,16,20,22,24-pentamethyl-hexacosa-4E,8E,12E,16,18-pentaenoic acid). Kheiric acid showed an interesting result with a minimum inhibitory concentration (MIC) value of 62.5 µg/mL against meticillin-resistant Staphylococcus aureus (MRSA). Hence, endophytes associated with medicinal plants from Sudan merit more attention, as they could be a treasure of new bioactive compounds.