Pomegranate marc is a major, underutilized juice industry by-product rich in lipophilic polyunsaturated fatty acids-notably conjugated α-linolenic acids (CLnAs)-and hydrophilic polyphenols with potent antioxidant and anti-inflammatory properties. Despite its potential for nutraceutical, cosmetic, and pharmaceutical applications, this matrix remains largely unexploited. This study presents a novel, sequential in-line extraction strategy combining supercritical CO2 (ScCO2) and subcritical water (scW) to recover complementary bioactive fractions. Both extraction steps were optimized via Response Surface Methodology (RSM). Box-Behnken optimization of ScCO2 (43 MPa, 76 °C, 6.4 L min-1, 124 min) yielded 30 g kg-1 dry weight (dw) of oleoresin, achieving a 68% recovery of total oil. Subsequent scW extraction was optimized at 149 °C, with a 40 L kg-1 water-to-solute ratio and 73 min extraction time, yielding 47 g kg-1 dw of total phenolics (58% recovery). Strong agreement between experimental and predicted values confirmed the robustness of the models. Comprehensive profiling revealed a diverse phytocomplex including fatty acids, tocopherols, flavonoids, soluble sugars, and polysaccharides. Antioxidant assays confirmed that both γ-tocopherol and polyphenols significantly contribute to the extracts' bioactivity. To improve physical handling, the aqueous fractions were converted into solid dispersions via spray drying with maltodextrin. Preliminary in vitro biological assessments on HEK-293 (human embryonic kidney) and MCF-7 (Michigan Cancer Foundation-7) cell lines suggested that the maltodextrin-based formulations may modulate the cytotoxic profile compared to the free extract, with exploratory results showing dosage-dependent variations in cell viability across the two lines. This work suggests a potentially scalable and sustainable biorefinery approach for the integral valorisation of pomegranate marc, offering a basis for a pathway to produce solvent-free bioactives.

Cancer remains a major global health challenge, driving the search for novel anticancer agents from natural sources. Endophytic fungi associated with medicinal plants, particularly red ginger (Zingiber officinale Roscoe var. rubrum), represent promising reservoirs of bioactive metabolites with cytotoxic potential. In this study, the cytotoxic activity of ethyl acetate extracts obtained from endophytic fungi isolated from red ginger was evaluated. Preliminary screening using the brine shrimp lethality test identified potent extracts with lethal concentration values below 100 ppm. These active extracts were subsequently assessed for cytotoxicity against the human breast cancer cell line Michigan Cancer Foundation-7 using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. Among the tested isolates, ZOBT1 exhibited notable cytotoxicity, with an inhibitory concentration value of 20.103 μg/ml. Molecular characterization confirmed the fungal isolate as Aspergillus niger ZOBT1. Furthermore, molecular docking analysis revealed that Fonsecinone A, a compound derived from this isolate, demonstrated stable interactions with key residues at the estrogen receptor (ER) binding site. Specifically, Fonsecinone A interacted with Trp393, a residue adjacent to the canonical ER binding site, yielding a docking score of −5.3536 kcal/mol and a root mean square deviation_refine of 1.7373 Å, suggesting a plausible mechanism for its anticancer activity. Overall, these findings highlight the potential of red ginger-associated endophytic fungi as promising sources of bioactive metabolites with anticancer properties, emphasizing the need for further pharmacological and mechanistic studies to validate their therapeutic relevance.

Natural-derived chemicals, particularly secondary metabolites from plants, are gaining attention for their potential as innovative and less harmful anticancer treatments, advancing cancer therapy and developing new medicinal herbs. The present study aimed to investigate the antimitotic, antiproliferative, and anticancer activities of various extracts from the leaves, bark, and fruits of Cleistanthus collinus using the Allium cepa root tip assay, yeast cell model, and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against Henrietta Lacks (HeLa) and Michigan Cancer Foundation-7 (MCF-7) cancer cell lines. For the MTT assay, crude methanol extract was used, while methanol, ethyl acetate, chloroform, aqueous, and petroleum ether extracts were employed for the antimitotic and antiproliferative assays. In the antimitotic assay, the methanol bark extract exhibited the highest activity, with a mitotic index of 15±0.57% at 500μg/mL, significantly reducing cell division compared to the control (97±1.23%). The methanol bark fraction showed the strongest activity in the antiproliferative assay, with only 26.41±0.57% viable cells at 500μg/mL. The extracts reduced cell viability and increased cytotoxicity in a dose-dependent manner. The anticancer activities (half-maximal inhibitory concentration, IC50 values) ranged from 186.43±2.7μg/mL to 885.69±6.77μg/mL against the MCF-7 cell line and from 228.5±3.7μg/mL to 550.85±4.67μg/mL against the HeLa cell line, with the highest activity observed for the crude methanol extract of bark against MCF-7 cells. These findings suggest that methanol extracts of C. collinus could be a promising source of plant-based anticancer agents with antimitotic, antiproliferative, and antioxidant activities.

Arborinine, a plant-derived alkaloid, has shown potential cytotoxic effects against various cancer cell lines. This study aims to evaluate the cytotoxicity and apoptosis effects of arborinine on breast cancer (Michigan Cancer Foundation-7 (MCF-7)) and human embryonic kidney (HEK293) as normal cell lines. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was used to assess the inhibitory concentration of 50% (IC50) after 24 and 48 hours of treatment of HEK293 and MCF-7 cell lines with arborinine. Apoptosis was evaluated through Annexin V/PI staining, and gene expressions including BAX, BCL-2, P53, PARP, and caspases (i.e., 3, 8, and 9) were analyzed via quantitative real-time polymerase chain reaction (qRT-PCR). Additionally, intracellular reactive oxygen species (ROS) levels were measured using 2',7'-dichlorodihydrofluorescein diacetate (DCFH-DA) fluorescence. The MTT assay results indicated a dose-dependent reduction in cell viability for both HEK293 and MCF-7 cells following treatment with arborinine. The viability of HEK293 cells decreased significantly (P=0.038) at concentrations above 150 µg/mL, while IC50 for MCF-7 cells was 50µg/mL and 25 µg/mL for 24 and 48 hours, respectively. Annexin V staining revealed apoptosis rates of 9.36% in untreated MCF-7 cells, increasing to 52.3% post-treatment. Arborinine treatment upregulated pro-apoptotic factors, including BAX, PARP, and P53, while downregulating BCL-2. Additionally, arborinine increased ROS levels by approximately 1.3-fold and decreased glutathione(GSH) levels, while enhancing superoxide dismutase(SOD) activity. This study shows that arborinine reduces cell viability and induces apoptosis in MCF-7 breast cancer cells by modulating key apoptotic pathways. Its effectiveness at lower concentrations in cancerous cells highlights its potential as a promising therapeutic agent in oncology.

In traditional medicine, Cyrtostachys renda has been used for its many bioactive components that are good for people's health. This research assessed the cytotoxic effects of extracts and fractions against Michigan Cancer Foundation-7 (MCF-7) and Henrietta Lacks (HeLa) cell lines. The extracts and fractions of root and fruit assess cytotoxic activities and inhibitory mechanisms against the MCF-7 and HeLa cancer cell lines, respectively. The fruit and roots of C. renda were extracted using the liquid-liquid method. The sample concentrations evaluated included extracts 31.5-1000 μg/mL, fractions 15.625-500 μg/mL, and doxorubicin 2-0.0625 μg/mL. Cytotoxicity was evaluated on MCF-7 and HeLa cells using an MTT assay. Morphological alterations were subsequently discovered utilizing an inverted microscope. Flow cytometry was utilized to find out the cell cycle's distribution and the apoptosis characteristics. The different parts and extracts showed cytotoxic effects on HeLa and MCF-7 cells, with IC50 values ranging from 30.69 ± 0.47 to 787.89 ± 1.77 µg/mL. Cell cycle studies showed that fraction A4 inhibited the cell cycle in MCF-7 cells at the G1 phase followed by the G2/M and S phases, while fraction B5 inhibited the cell cycle in HeLa cells at the G2/M phase. Both fractions showed the ability to induce apoptosis against MCF-7 and HeLa cells. The results showed that the fractions A4 and B5 showed cytotoxic activity against MCF-7 and HeLa cells by cell cycle arrest and apoptosis induction.

Remifentanil induces apoptosis and G1-phase cell cycle arrest in human MCF-7 breast cancer cellsB reast cancer represents one of the most prevalent female malignant tumors globally [1].According to a recently published statistic in 2023, thirteen percent of malignancies in women are caused by breast cancer, and the greatest number of deaths from breast cancer among women has been reported [1].However, the global mortality of breast cancer is falling as a better indicator of progress due to early diagnosis through the established system of mammography screening, increased awareness, and improvements in comprehensive treatment options such as adjuvant chemotherapies [1].The available options include surgery, radiation, chemotherapy, immunother-apy, or hormonal therapies, depending on the stage and subtype of breast cancer [2].Despite significant advancements in diagnostic and therapeutic approaches against breast cancer, the treatment still remains a challenging endeavor due to the high relapse and lethality rate of the disease, significant side effects, and the lower effectiveness of therapeutic strategies [3].Patients with breast cancer are most commonly diagnosed as hormone receptor-positive [4].The MCF-7 (Michigan Cancer Foundation-7) cell line is characterized as the Luminal A subtype of breast cancer, which is an estrogen and progesterone receptor-positive tumor [5].A primary care approach for the Objectives: Remifentanil, a fentanyl-derivative opioid analgesic acting as a -opioid receptor agonist, is a crucial drug in anesthesia due to its numerous benefits during surgical procedures.This study aimed to explore whether remifentanil effectively induced apoptosis in MCF-7 breast cancer cells via possible mechanisms.Methods: Flow cytometry was performed for Annexin V/7-aminoactinomycin (7-AAD) and DAPI staining, cell cycle assays, and to measure reactive oxygen species (ROS) levels.Immunoassays for lactate dehydrogenase (LDH) and interleukin (IL)-6, as well as a chorioallantoic membrane (CAM) test, were also performed.Results: Remifentanil effectively suppressed cell proliferation and led to the induction of cell cycle arrest at the G1 phase in MCF-7 cells.Compared with the control group, MCF-7 cells treated with remifentanil had a higher apoptotic rate with nuclear fragmentation, increased LDH release, and lower IL-6 concentrations.Overgeneration of ROS and decreased angiogenic activity were also observed in remifentanil-treated MCF-7 cells.Conclusion: Remifentanil led to G1-phase arrest and apoptosis in MCF-7 cells.The mechanism of action of remifentanil likely involves the suppression of IL-6 production and angiogenesis, along with enhanced ROS levels and LDH generation.This preliminary study highlighted the need for further experimental evidence from future research to clearly support the significant potential of remifentanil as an anticancer agent for breast cancer.

Background: Cancer is a term refer to a group of diseases which is characterized by cell-growth in uncontrolled manner. It is considered one of the major global challenges, due to difficulty in cancer management, and this difficulty which also associated with their treatment. Therefore, the current study aimed to assess the impact of cyclophosphamide on the cell viability of Michigan Cancer Foundation-7 (MCF-7) breast cancer and H9 lymphoma cancer cell lines and the detection of gene expression. Materials and Method: Cancer cell lines MCF7 and H9 were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS), 50 g/ml for ampicillin and streptomycin, and assessed the cytotoxic effect of cyclophosphamide therapy with concentration (50 g/ml) for serial dilution (50, 25, 12.5, 6.25 and 3.125 g/ml) for 48 and 72 hours using 3-(4,5-dimethylthiazol2-yl)-2,5 diphenyl tetrazolium bromide (MTT) assay. Additionally, a real-time polymerase chain reaction (PCR) test was conducted to identify the expression of related genes, including EPCAM and of Keratin type I cytoskeletal 19 (KRT19). Results: The highest significant inhibition rates were obtained at the doses (50 and 25 μg/ml) after 48 and 72 hours compared to other concentrations in the same treated period. According to sensitivity, MCF7 were more sensitive to cyclophosphamide than H9 cells for 48 and 72 hours. Also, our results observed the down-regulation of the GAPDH, and ERBB2 gene at 72 hours after treatment in MCF-7 and H9 cells. Meanwhile, KRT19 gene expression was up-regulated in MCF-7 and H9 cells after exposure to Chemotherapy for 72 hours. Conclusion: The current in vitro study showed that cyclophosphamide has a concentration- and time-dependent harmful effect on the MCF7 and H9 cell lines.

Introduction. Studies have shown that natural compounds from various plants including berries can have antitumor activity. We examined Phlojodicarpus sibiricus extract as well as homogenates of wild berries such as hawthorn, cranberry, brier; all these plants contain a variety of biologically active compounds: flavonoids, carotenoids, anthocyanins and other polyphenols.Aim. To evaluate cytotoxicity of wild berries and Phlojodicarpus sibiricus growing in Northwestern Siberia in Michigan Cancer Foundation-7 (MCF-7) breast cancer cell line using the МТТ assay.Materials and methods. We examined homogenates of wild berries including Dahurian hawthorn (Crataegus dahurica Koehne), bog cranberry (Oxycoccus microcarpus Turcz.), Yakut brier (Rosa jacutica Juz.) and extract of the above-ground part (leaves, stems) of Phlojodicarpus sibiricus. Cytotoxicity of the prepared homogenates was evaluated on the MCF-7 cell line. For homogenate screening, colorimetric assay for assessing cell metabolic activity МТТ was used.Results. Dahurian hawthorn, bog cranberry and Yakut brier have statistically significant cytotoxic effect on tumor cells at concentration of 100 mg/mL in incubation medium. Among the evaluated berries, Yakut brier demonstrated the highest suppression of MCF-7 cell line growth: at dose 100 mg/mL it decreased it by 80.19 % compared to control. Extract of Phlojodicarpus sibiricus at concentration 10 mg/mL left only 4.95 % of the MCF-7 cells alive.Conclusion. Therefore, wild berries have antiproliferative potential. Being edible, they can be helpful in prevention of oncological diseases. High antiproliferative activity of Phlojodicarpus sibiricus demonstrated by us in this and previous studies indicate that it can be considered a source of effective antitumor compounds.

Novel inhibitors of epidermal growth factor receptor (EGFR)T790M/vascular endothelial growth factor receptor-2 (VEGFR-2) were synthesized based on the iodoquinazoline scaffold linked to different heteroaromatic, aromatic, and/or aliphatic moieties. The novel derivatives were in vitro examined for anticancer activities against A549, HCT116, michigan cancer foundation-7 (MCF-7), and HepG2 cells. Molecular modeling was applied to discover their orientation of binding with both VEGFR-2 and EGFR active sites. Compounds 8d, 8c, 6d, and 6c indicated the highest cytotoxicity with IC50 = 6.00, 6.90, 6.12 and 6.24 µM, 7.05, 7.35, 6.80, and 6.80 µM, 5.75, 7.50, 6.90, and 6.95 µM, and 6.55, 7.88, 7.44, and 7.10 µM against the A549, HepG2, HCT116, and MCF-7 cell lines, correspondingly. The cytotoxicity against normal VERO (normal african green monkey kidney cells) of the extremely active eight compounds 6a-d and 8a-d was evaluated. Our compounds exhibited low toxicity concerning normal VERO cells with IC50 = 45.66-51.83 μM. Furthermore, inhibition assays for both the EGFRT790M and VEGFR-2 enzymes were done for all compounds. Remarkable inhibition of EGFRT790M activity was achieved with compounds 6d, 8d, 6c, and 8c at IC50 = 0.35, 0.42, 0.48, and 0.50 µM correspondingly. Moreover, remarkable inhibition of VEGFR-2 activity was achieved with compounds 8d, 8c, 6d, and 6c at IC50 = 0.92, 0.95, 1.00, and 1.20 µM correspondingly. As planned, derivatives 6d, 8d, 6c, and 8c presented exceptional inhibition of both EGFRT790M/VEGFR-2 activities. Finally, in silico absorption, distribution, metabolism, excretion and toxicity (ADMET) studies were made for the highly active four compounds 6c, 6d, 8c, and 8d in comparison with erlotinib and sorafenib as reference standards.

The diagnosis and treatment processes of cancer are among the main challenges of medical science in recent decades. The use of different therapeutic agents is one of the most common methods frequently utilized for cancer treatment. Accumulating evidence points to a potential effect of Obeticholic acid (OCA), a specific ligand for farnesoid X receptor, on the regulation of cancer-associated pathways. In spite of tremendous efforts to introduce OCA into the clinical setting, there is a great deal of uncertainty about its impact on breast cancer treatment. This study was performed to evaluate the effects of OCA on breast cancer. In this experiment, the MCF-7 (Michigan Cancer Foundation-7) cell line was treated with 0.1 µM OCA, and cancerous characteristics of the MCF-7 cell line was evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assay, gelatin zymography, western blot, Real-time PCR, flow cytometry, and ELISA techniques. The results indicated that OCA increased the rate of apoptosis and the expression levels of PPARα (Peroxisome proliferator-activated receptor alpha) and TIMP-1 (tissue inhibitor of metalloproteinase-1) genes in this cell line, while it reduced the mRNA levels of MMP7 (matrix metalloproteinase 7) and Bcl-2 (B-cell lymphoma 2) genes, as well as the protein levels of the active form of AKT (protein kinase B), Erk1/2 (extracellular signal-regulated kinase 1/2) and STAT3 (Signal transducers and activators of transcription-3). Also, OCA decreased the activity of MMP9, while it increased the secretion of VEGF-A (vascular endothelial growth factor-A). It seems that OCA can exert anti-cancer effects on the MCF-7 cells by reducing growth, proliferation, migration, invasion, and regulation of the expression of genes involved in cancer-associated pathways. However, it should be noted that further studies are warranted to establish this concept, especiallythe increase of VEGF-Acan be considered a challenge for the results of this study.

Abhrak Bhasma (Shatputi) is a time tested classical Ayurvedic formulation, prepared from mica, as well as the juices of numerous other indigenous substances. In this work, we focus on the efficacy of Abharak Bhasma on anticancer activity and immunomodulatory effects using breast cancer Michigan Cancer Foundation-7 cell line and macrophage cell line Robert Abelson leukemia virus 264.7. The in vitro anti-cancer activities of the formulation were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide assay. The percentage of cell death against Michigan Cancer Foundation-7 cell breast cancer cells increases with an increase in the concentration of Abhrak Bhasma. A high percentage of cell death (49.22±1.504 %) was observed at the concentration of 200 µg/ml of Abhrak Bhasma. The corresponding half-maximal inhibitory concentration value of Abhrak Bhasma was found to be 193.2±10.72 µg/ml. There was a dose-dependent decrease in the nitrite level in Robert Abelson leukemia virus 264.7 incubated with Abhrak Bhasma at the concentration ranges from 50 to 200 µg/ml. A significant reduction in nitrite level was found to be about 489.3±35.92 at 200 µg/ml. Lipopolysaccharide (1 µg/ml) treated was served as a control with a maximum nitrite level of about 1873±83.59 µg. The present study reveals that the percentage of cell viability in the macrophage cell line decreases with an increase in the concentration of Abhrak Bhasma. The least viability of the cell was observed at the concentration of 200 µg/ml showing 53.85±1.211 %. Our study highlights dual qualities of Abhrak Bhasma as a potential drug against breast cancer and as an immunomodulatory drug showing anti-inflammatory properties.

Designing and fabrication of colloidal nano-phytosomes with gamma-oryzanol and phosphatidylcholine for encapsulation and delivery of polyphenol-rich extract from pomegranate peel

Objectives:To evaluate the anti-cancer effect of resveratrol on Michigan cancer foundation-7 (MCF-7) and hepatoblastoma cell line (HepG2) cells.Methods:The study was carried out at the Department of Botany and Microbiology, Prince Sattam bin Abdulaziz University, Al-kharj, Saudi Arabia, from August 2022 to October 2022. Different concentrations of resveratrol were added to the MCF-7 and HepG2 cell lines. Cell death and proliferation were measured with MTT and Trypan blue exclusion assays. Apoptosis markers were assessed by using a quantitative PCR assay (qPCR).Results:The resveratrol was shown to suppress the proliferation of MCF-7 and HepG2 cells at dose- and time-dependent. The cytotoxic effect of resveratrol was observed even at 100 μM after 24 hours. In comparison to untreated cells, resveratrol treatment reduced the viability of MCF-7 cells to roughly 57.5% with a half maximal inhibitory concentration (IC50) of 51.18 μM and HepG2 cells to 56.2% with an IC50 of 57.4 μM. Furthermore, in the tested cell lines, resveratrol was able to induce apoptosis mediated by elevated apoptosis markers.Conclusion:Resveratrol appears to be an excellent candidate agent in anticancer therapy in various human cancers.

Histidine triad nucleotide binding protein 1 (HINT1) is a haplo-insufficient tumor suppressor gene that plays a significant role in cell proliferation and survival. However, to date, no systematic pan-cancer analysis has been conducted to explore its function in prognosis, and its oncogenic and immunological roles. We also analyzed the role of HINT1 in breast cancer (BC) progression in vitro. An analysis of the HINT1 expression pattern was performed using the TIMER database. The infiltration of immune cells into several cancer types was also studied using the Xena Shiny tool. To determine the relationship between stemness and the expression of HINT1 mRNA, the Spearman correlation test was used with the SangerBox tool. The correlation between HINT1 and functional states in various cancers was determined from the CancerSEA database. The potential role of HINT1 in BC oncogenesis was also investigated by Western blot and Annexin V/PI assays. The Cancer Genome Atlas pan-cancer data analysis suggested that HINT1 was extensively altered in most tumor tissues but not in most adjacent normal tissues. A high expression of HINT1 was associated with the decreased infiltration of cluster of differentiation (CD)4+ T cells. Importantly, increased HINT1 expression was also associated with a large majority of tumors with high stemness and lower stromal, immune, and estimate scores. Further, the expression of HINT1 was significantly associated with the tumor mutational burden (TMB) and microsatellite instability (MSI) in certain tumor types. Finally, HINT1 overexpression was found to impair BC progression by promoting cell apoptosis. HINT1 upregulation also reduced the expression of microphthalmia transcription factor (MITF) and β-catenin in BC Michigan Cancer Foundation-7 (MCF-7) cells, and the phosphorylation of protein kinase B (p-Akt). The present study showed that HINT1 plays an oncogenic role in various cancers and could also be used as a biomarker for BC.

The medicinal plant Ipomoea aquatica belonging to convulvulaceae family is an effective natural herb for treatment of various ailments and possesses effective anticancer activity. The aim of the work is to characterize a secondary metabolite merromoside (a resin glycoside) for anti-breast cancer activity through down regulation of ROS species. The Extract of the whole plant has been prepared by maceration method using 50%v/v ethanol in distilled water to get a hydroalcoholic extract. The phytochemical evaluation reveals that the active secondary metabolite was isolated by using column chromatographic technique. The isolated compound was evaluated for its anticancer properties through invitro method such as 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay on Michigan Cancer Foundation-7 Cell lines. The purity and structural characterization were done by high-performance thin layer chromatography, Fourier Transform Infrared Spectroscopy, Proton and13C Nuclear Magnetic Resonance spectroscopy and Liquid Chromatography-Mass Spectrometry. The isolated compound (W04) from the derived extract showed Rf value of 0.79 that showed IC50 of 182.8μg/ml. The chemical structure of W04 has been confirmed as [4,5-dihydroxy-6-[5-hydroxy-2-methyl-4-(2-methylpropanoyloxy)-6-[(24,25,26-trihydroxy-5,23-dimethyl-9-oxo-19-pentyl-2,4,8,20,22-pentaoxatricyclo[19.2.2.13,7]hexacosan-6-yl)oxy]oxan-3-yl]oxy-2-methyloxan-3-yl] 2-methyl propanoate with the molecular weight of 979.15268. The isolated compound merromoside from hydroalcoholic extract of Ipomoea aquatica has been evaluated for anti-breast cancer properties. The down regulation of ROS species will prevent reverse signalling and angiogenesis. This indicates that merromoside will overcome MDR in breast cancer especially DOX-resistant.

Enhanced mitochondria destruction on MCF-7 and HeLa cell lines in vitro using triphenyl-phosphonium-labelled phthalocyanines in ultrasound-assisted photodynamic therapy activity.

Anti-hyaluronidase and cytotoxic activities of fucoxanthin cis/trans isomers extracted and characterized from 13 brown seaweeds

Background: The nature acts like a large “bio-laboratory” comprising plants, algae, fungi, yeast, etc., which are composed of biomolecules. These naturally occurring biomolecules have been identified to play an active role in the formation of nanoparticles. Methods: This research work mainly aims to investigate the anti-oxidant (diphenylpicrylhydrazyl assay) and anti-cancer (Michigan cancer foundation-7 cell line) capacities of biologically prepared copper oxide mediated from the hydroalcoholic extract of Justicia glauca by simple precipitation and also to identify the phytochemicals in the extract by qualitatively. Results: On screening test, the extract shows the presence of carbohydrate, phenolics, alkaloids, and terpenoids saponins which are chiefly act as a reducing, stabilizing, and capping agents in nanomaterial preparations. The medicinal plant Justicia glauca extract-mediated copper oxide materials were synthesized by lost cost, simple, effective, and eco-friendly precipitation method. The prepared copper nanomaterials were characterized by ultraviolet–visible, Fourier-transform infrared spectroscopy, energy dispersive X-ray analysis, X-ray diffraction, and scanning electron microscope. The obtained spectral results reveal that the prepared particles were found to be elliptical flat shapes of copper oxide with the average size of 19.72 nm with 51.11% of copper and 48.89% of oxygen elements. Especially, on anti-oxidant and anti-cancer activities the prepared Justicia glauca extract-mediated copper oxide revealed excellent potent while comparing the other green synthesized copper oxide particles. Conclusion: Overall results evidenced that the aqueous extract of Justicia glauca is a very good bioreductant for the synthesis of copper oxide nanoparticles.

IntroductionMurine double minute 2 (MDM2) is an oncogene that is important in tumorigenesis, tumor metastasis and chemotherapy resistance. We aimed to synthesize a molecular imaging probe, 99mTc-HYNIC-siRNA 1489, which could specifically bind to MDM2. The [99mTc]HYNIC-siRNA 1489 molecular probe provided an effective way of assessing MDM2 expression via single-photon emission computed tomography.MethodThree siRNAs were designed, and their inhibitory efficiencies were determined using western blots and qRT-PCR. The selected siRNA was labeled with the radionuclide technetium-99m (99mTc) through the chelator HYNIC. The bioactivity and properties of [99mTc]HYNIC-siRNA 1489 were evaluated prior to imaging in mice. Imaging and biodistribution of the probe were used to assess its targeting ability.ResultsSiRNA 1489, which was labeled with 99mTc, displayed a strong inhibitory effect in Michigan Cancer Foundation-7 cell lines. The radiochemical purity of [99mTc]HYNIC-siRNA 1489 was stable at various temperatures in phosphate-buffered serum and bovine serum. The tumor/muscle ratio in mice injected with [99mTc]HYNIC-siRNA 1489 was higher than that in those injected with the negative control, [99mTc]HYNIC-NC siRNA. The percentage injected dose per gram (%ID/g) of the tumors injected with 99mTc-HYNIC-siRNA 1489 was greater than that of the control group.ConclusionThe [99mTc]HYNIC-siRNA 1489 was taken up by the tumor, which had a high level of MDM2. The probe exhibited a sufficient retention time in the tumor. This probe may be an effective strategy for evaluating MDM2 expression and achieving early diagnosis in breast cancer.

Lack of new anti-cancer and anti-infective agents directed the pharmaceutical research to natural products' discovery especially from actinomycetes as one of the major sources of bioactive compounds. Metabolomics- and dereplication-guided approach has been used successfully in chemical profiling of bioactive actinomycetes. We aimed to study the metabolomic profile of five bioactive actinomycetes to investigate the interesting metabolites responsible for their antimicrobial and anti-cancer activities. Three actinomycetes, namely, Streptomyces sp. SH8, SH10 and SH13, were found to exhibit broad spectrum of antimicrobial activities, whereas isolate SH4 showed the broadest antimicrobial activity against all tested strains. In addition, isolates SH8, SH10 and SH12 displayed potent cytotoxicity against the breast cancer cell line Michigan Cancer Foundation-7 (MCF-7), whereas isolates SH4 and SH12 exhibited potent anti-cancer activity against the hepatoma cell line hepatoma G2 (HepG2) compared with their weak inhibitory properties on the normal breast cells MCF-10A and normal liver cells transformed human liver epithelial-2 (THLE2), respectively. All bioactive isolates were molecularly identified as Streptomyces sp. via 16S rRNA gene sequencing. Our actinobacterial dereplication analysis revealed putative identification of several bioactive metabolites including tetracycline, oxytetracycline and a macrolide antibiotic, novamethymycin. Together, chemical profiling of bioactive Streptomycetes via dereplication and metabolomics helped in assigning their unique metabolites and predicting the bioactive compounds instigating their diverse bioactivities.