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Respirantins are 18-membered antimycin-type depsipeptides produced by Streptomyces sp. and Kitasatospora sp. These compounds have shown extraordinary anticancer activities against a panel of cancer cell lines with nanomolar levels of IC50 values. However, further investigation has been impeded by the low titers of the natural producers and the challenging chemical synthesis due to their structural complexity. The biosynthetic gene cluster (BGC) of respirantin was previously proposed based on a bioinformatic comparison of the four members of antimycin-type depsipeptides. In this study, we report the first successful reconstitution of respirantin in Streptomyces albus using a synthetic BGC. This heterologous system serves as an accessible platform for the production and diversification of respirantins. Through polyketide synthase pathway engineering, biocatalysis, and chemical derivatization, we generated nine respirantin compounds, including six new derivatives. Cytotoxicity screening against human MCF-7 and Hela cancer cell lines revealed a unique biphasic dose-response profile of respirantin. Furthermore, a structure-activity relationship study has elucidated the essential functional groups that contribute to its remarkable cytotoxicity. This work paves the way for respirantin-based anticancer drug discovery and development.

Developing novel, efficient, and safe peptide drugs from sea anemones has aroused great interest in countries around the world today. Sea anemones contain complex protein and peptide toxins, which determine the diversity of their biological activities. In this study, a variety of activities were assessed for crude venom extracted from five species of South China Sea anemones, including hemolytic, enzyme inhibition, anticancer, insecticidal, analgesic and lethal activities. The most toxic sea anemone was found to be Heteractis magnifica , which has high lethal activity in mice with an LD50 of 11.0 mg/kg. The crude venom of H. magnifica also exhibited a range of the most potent activities, including hemolytic, trypsin inhibitory, cytotoxic activity against U251 and A549 cells, insecticidal and analgesic activities. In addition, the crude venom of Stichodactyla haddoni was the most effective inhibitor of pepsin, and the crude venom of Heteractis crispa was extremely strong toxicity to HepG2 cells. These findings are of great significance for exploring the potential and application of South China Sea anemone resources, and are expected to provide new directions and possibilities for the development of novel anticancer drugs, analgesics and biopesticides. [ABSTRACT FROM AUTHOR]

A metagenomic library consisting of 15,000 clones was constructed from the mangrove sediment. An antimicrobially active clone from the metagenomic library PS49 was identified by function- based screening. This paper presents the results of the biochemical characterization and metagenomic library screening of the marine-derived antibiotic, 8-demethoxy-10-deoxysteffimycin. Plasmid libraries were constructed, and clones were produced using a metagenomic approach. Out of 15,000 clones, 81 clones were screened for antimicrobial activity, and five potential clones were selected. The activity of one clone was characterized and named as PS49. The bioactive compounds from the selected clone were checked for antimicrobial, antioxidant, and anticancer activities. The clone PS49 was tested against various pathogens including bacteria and fungi and it showed inhibitory effects against all the tested pathogens. The antimicrobially active fractions were then crystallized and subjected to spectroscopic analysis such as FTIR, NMR and LC–MS analysis. The substance from clone PS49 has finally been recognized, and the compound from clone PS49 has been identified as 8-demethoxy-10-deoxysteffimycin. The substances isolated from the PS49 clone exhibited strong anticancer activity against skin cancer-cell lines SK-MEL2. The compounds showed a reduction in cell viability with an increase in the compound concentration. The compounds obtained from clone PS49 showed an IC50 value of 85 µg/ml. [ABSTRACT FROM AUTHOR]

Background: Curcumin (CUR) is a natural polyphenol and one of the key phytoconstituents found in the rhizomes of Curcuma Longa. It exhibits various pharmacological properties, encompassing antioxidant, anticancer effects, antiseptic, and anti-inflammatory, among several others. A significant drawback of using CUR is its limited bioavailability, which primarily depends on gut microorganisms responsible for converting it into its bioavailable form. Therefore, the contemporary study intended to formulate a novel PLAROsomal vesicular delivery of CUR, i.e., CUR-PLAROsomes employing a design of experiments approach to examine the influence of various process parameters, such as particle size and drug percentage release. Result: The prepared CUR-PLAROsomes were characterized for their physicochemical properties using various hyphenated tools. The CUR-PLAROsomes exhibited sizes ranging from 40 to 300 nm, and the optimized batch demonstrated a drug entrapment of 86.38 ± 0.22%. In-vitro anticancer studies were conducted using human colorectal adenocarcinoma cells (COLO320DM) and human breast adenocarcinoma (MCF-7). CUR-PLAROsomes exhibited significant in-vivo anti-inflammatory potential against carrageenan-induced paw edema. CUR-PLAROsomes were more potent against COLO320DM and MCF-7 cell lines, even at lower concentrations, than pure CUR. Conclusion: Furthermore, based on the observations, it exhibits potential as an anti-inflammatory agent, suggesting that PLAROsomes are an effective vesicular drug delivery system. Highlights: Newly introduced PLARosome is a next generation of Liposomes which have gain popularity owing to its better adaptability to overcome leakage problem of vesicular drug delivery system. This is the pioneer attempt to prepare Curcumin-loaded PLARosome as an anti-cancer and anti-inflammatory activity. Nano size of the PLAROsomes may contribute to enhance the efficacy of Curcumin as a target specific drug delivery system. Site specific delivery of phytoconstituents is possible by use of PLAROsomes as a novel drug delivery system. [ABSTRACT FROM AUTHOR]

Symphorema polyandrum belongs to the Lamiaceae family and is locally known as Badichang or mahasindhu. In this study, we performed Soxhlet extraction to prepare methanolic and hydromethanolic extracts, followed by quantification of their total phenolic content and total flavonoid content. Qualitative analysis of both the extracts was conducted to determine the presence of different phytochemicals. In addition, we aimed to identify the important phytochemical constituents in the methanolic extracts of S. polyandrum (SPM) using ultra-performance liquid chromatography hyphenated with high-resolution mass spectrometry (UPLC–ESI–QTOF–MSE). Furthermore, this study investigated the antioxidant, anticancer and anti-inflammatory properties of SPM and its safety profile in the normal fibroblast cell line L929. A colony proliferation assay and a Griess assay were performed to evaluate the effects of SPM on colony formation and nitric oxide (NO) production. A total of 13 important phytochemicals were identified and reported. The methanolic extract of SPM demonstrated significant antioxidant activity. SPM also showed substantial antiproliferative activity on MDA-MB-231 triple-negative breast cancer cells, with an IC50 value of 45.53 ± 1.63 µg/ml, and also reduced the survival of these cancer cells by promoting nuclear fragmentation and condensation without causing harm to normal cells. SPM inhibits the colony formation and reduces the nitric oxide (NO) production. The anti-inflammatory potential of SPM was assessed utilizing the murine alveolar macrophages (J774.A.1) as an in vitro model, and SPM effectively lowered the levels of proinflammatory cytokines such as TNF-α and IL-6. These findings emphasized the antiproliferative potential of SPM to cancer cells, along with its anti-inflammatory, and antioxidant capabilities, indicating the therapeutic efficacy of this medicinal plant. [ABSTRACT FROM AUTHOR]

The synthesis and characterization of a series of 5-nitro-N-phenyl-3-(phenylamino)-1H-indazole-1-carboxamide 5-NPIC derivatives (5a– 5v) have been reported as anticancer agents in this study. These derivatives were synthesized by reacting 3-chloro-5-nitro-N-phenyl-1H-indazole-1-carboxamide (4) with a variety of aniline derivatives in isopropanol. FT-IR, 1H-NMR, 13C-NMR and mass spectral methods were employed to confirm the structures of analogues (5a– 5v). The anticancer activity evaluation of compounds 5a– 5v revealed that 3-((3-methoxyphenyl) amino)-5-nitro-N-phenyl-1H-indazole-1-carboxamide (5j) exhibited good efficacy. The stability of ligand–protein complexes was systematically evaluated using molecular dynamics simulations (MDS), which demonstrated a consistent and robust binding of the most potent compound within the binding sites of target proteins. The results confirmed the anticancer activity, which was further substantiated by comprehensive molecular docking analyses that revealed complex interactions involving hydrophobic contacts, electrostatic forces and hydrogen bonds. Our results would collectively provide invaluable insights into the intricate molecular structure and dynamics of receptor target sites, thereby establishing a solid foundation for the development of novel and potent anticancer agents with optimistic pharmaceutical implications in near future. [ABSTRACT FROM AUTHOR]

In this study, we have synthesized a series of novel quinoxaline based bisspirooxindoles through green protocol using ionic liquid [Bmim]BF4. All the compounds were well characterized by spectroscopic methods like FT‐IR, 1H NMR, 13C NMR, mass and finally the structures were authenticated by single crystal X‐ray diffraction (SCXRD) (4e). The target compounds were evaluated for their anticancer activity with different cancer cell lines like MDAMB‐231, MCF‐7, MCF‐10A, HCC‐1395, Molt‐4, and FaDU. The compounds 4d, 4g, 4m, and 4n showed 42.0%, 43.3%, 52.7%, and 56.0 percentage of growth inhibition respectively with the T cell acute lymphoblastic Molt‐4 cell line. The compounds 4b, 4c, 4 h, 4k, and 4m have shown 30%–39% of growth inhibition against FaDU cell line. Further, anticancer activity was validated with in silico molecular docking and molecular dynamics simulations. The outcomes of dynamics simulations exclusively emphasize that the compounds bind to HIS862 and TYR896 residues which are among the catalytic triad of PARP1. Finally, the results of ADME is also used to assess the drug likeness, which clearly shows that our target compounds are adaptable as potential drug pathways for medicinal chemists. [ABSTRACT FROM AUTHOR]

In this study, we present a green synthesis approach for synthesis of silver nanoparticles (Ag NPs) using Grewia Asiatica L. berries through a phytosynthesis method. In this synthesis procedure the Grewia Asiatica L. berry extract served as a natural reducing agent in the phytosynthesis of GA‐Ag NPs. The synthesized Ag NPs were characterized using various physico‐chemical techniques, revealing their spherical morphology of average size of ∼20 nm. These Ag NPs exhibited significant antibacterial activity against both Gram‐negative and Gram‐positive bacterial strains. Additionally, the GA‐Ag NPs demonstrated anticancer properties, with an IC50 value of approximately 5 µM. The study highlights the potential of Grewia Asiatica L. berry extract as a novel, nontoxic, eco‐friendly, and cost‐effective method for synthesizing silver nanoparticles with promising antibacterial and anticancer activities. [ABSTRACT FROM AUTHOR]

Compounds that can induce oxidative stress in cancer cells while remaining nontoxic to healthy cells are extremely promising for potential anticancer drugs. 2,2′:6′,2′′-terpyridine-metal complexes possess these properties. The high level of activity (IC50 = 0.605 µM) of 2,2′:6′,2′′-terpyridine-metal complexes on lung, breast, pancreatic, and glioblastoma multiforme cancer lines and their selectivity (SI > 41.32) on human normal fibroblasts were confirmed and presented in this paper. The mechanism of action of these compounds is associated with the generation of reactive oxygen species, which affects several cellular pathways and signals. The results demonstrate that 2,2′:6′,2′′-terpyridine-metal complexes affect cell cycle inhibition in the G0/G1 phase as well as the activation of apoptosis and autophagy cell death. These results were confirmed in several independent studies, including experiments measuring the fluorescence levels of reactive oxygen species, flow cytometry, and gene and protein analysis. [ABSTRACT FROM AUTHOR]

Cancer is a major disease that affects millions of people around the world every year. It affects individuals of all ages, races, and backgrounds. Since drugs used to treat cancer cannot distinguish between cancerous and healthy cells, they cause systemic toxicity along with serious side effects. Recently, controlled drug-release systems have been developed to reduce the side effects caused by anticancer drugs used for treatment. Morin is an anticancer drug with a flavonol structure. It has been extensively researched for its antioxidant, anti-inflammatory, antitumoral, and antibacterial properties, especially found in Chinese herbs and fruits, and its multiple positive effects on different diseases. In this study, a nanocomposite with magnetic properties was synthesized by coating biocompatible activated carbon obtained using the fruits of the Celtis tournefortii plant on the surface of iron oxide magnetic nanoparticles. Characterization of the synthesized activated carbon-coated iron oxide magnetic nanocomposite was confirmed by Fourier transform infrared, scanning electron microscopy, energy-dispersive X-ray spectrometry, X-ray diffraction, dynamic light scattering, zeta potential, and vibrating sample magnetometry. The cytotoxic effects of the drug-loaded magnetic nanocomposite were examined in HT-29 (colorectal), T98-G (glioblastoma) cancer cell lines, and human umbilical vein endothelial cell (HUVEC) healthy cell line. The morin loading and release behavior of the activated carbon-coated iron oxide magnetic nanocomposite were studied, and the results showed that up to 60% of the adsorbed morin was released within 4 h. In summary, activated carbon-coated iron oxide magnetic nanocomposite carriers have shown promising results for the delivery of the morin drug. [ABSTRACT FROM AUTHOR]

A novel series of six [1,2,4]triazolo[3,4-a]isoquinolin-3-yl)-3-(1,3-diphenyl-1H-pyrazol-4-yl)prop-2-en-1-ones (3a–3f) was designed and synthesized. They were characterized based on spectral and elemental analyses. In silico studies were also committed to provide insights and a better understanding of their structural features. The six compounds were screened for their antiproliferative activity using the MTT assay against five human cancer cell lines, namely, A549, HCT116, PC3, HT29, and MCF-7 in parallel with the non-cancerous human lung cell line WI-38. The results showed that 3e and 3f have potential cytotoxic activities, especially on A549 cells with IC50 = 2.3 µM and 1.15 µM, respectively. Meanwhile, they recorded a minimal cytotoxic effect on WI-38 cells. Concerning the molecular mechanism of action, the present study showed the inhibitory effect of the six compounds against total EGFR. The most potent EGFR inhibitors were 3e and 3f with IC50 = 0.031 µM and 0.023 µM, respectively. The selectivity index of 3f for EGFRT790M was 1.81 times more selective than that of lapatinib. In addition, 3e and 3f initiated cell cycle arrest at the G2/M and pre-G1 phases along with the downregulation of anti-apoptotic protein Bcl2 and the upregulation of pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. Further studies are recommended to evaluate animal models' promising anticancer activity and molecular mechanism of triazolo[3,4-a]isoquinoline derivatives 3e and 3f. [ABSTRACT FROM AUTHOR]

Nanobiotechnology is a field of science with tremendous promising applications in cancer chemotherapy, targeted drug delivery, molecular diagnosis, and molecular imaging. Selenium, one of the critical trace elements, participates in the structure of selenocysteine protein, which plays an important role in maintaining redox balance due to its oxidoreductase activity. Elemental selenium (Se0) has significantly lower toxicity values than its oxyanions, selenite, and selenate forms. For this reason, it is important to convert elemental selenium into atomic form in biological studies. In particular, their role in regulating the immune system makes selenium nanoparticles (SeNPs) superior to others. SeNPs have been discussed effectively in the literature in anticancer activity applications. SeNPs green synthesis is focused on a more economical, biocompatible, and environmentally friendly application by using, reducing, and stabilizing agents in plants. The aim of this review is to highlight the anticancer activity applications of SeNPs synthesized with plant extracts in the last 6 years (i.e., between 2019 and 2024). In addition, it aims to shed light on the green synthesis mechanism of NPs by using plant extracts and to highlight the factors affecting green synthesis and its advantages and disadvantages. [ABSTRACT FROM AUTHOR]

In this work, we synthesized a series of new 1,3‐oxazole derivatives comprising the sulfonylamide group and tested their activity against the human tumor cell line panel. This study further explores the stereoelectronic characteristics of 1,3‐oxazol‐5‐sulfonylamides and new 1‐(1,3‐oxazol‐5‐yl)piperidine‐4‐sulfonylamides to connect their anticancer activity to the molecular structure. Combining in vitro and in silico methods, we analyzed how the proximity of the sulfonylamide group to the heterocyclic ring affects the structure–activity interplay. Herein, our assessment is based on the purported complexation of 1,3‐oxazoles with targeted biomolecular fragments involving the π‐stacking interaction and hydrogen bonding within the prospective complexes. Defining the probability of the prospective drug–target interactions, we detail conformational properties, donor/acceptor capabilities, electronic characteristics, and thermodynamic preference of produced sulfanylamide group containing 1,3‐oxazoles toward biomolecular fragments, identifying the nature of variations in anticancer activity. [ABSTRACT FROM AUTHOR]

Pure CeO2 and Ce1‐xMnxO2, where x = 0, 2, 4 and 6% w/w, were synthesized by sol‐gel method using Acacia Concinna fruit extract as a surfactant and stabilizing agent. The synthesized particles were subjected to various characterization techniques, including XRD, HRTEM, FESEM, FTIR, Raman and UV‐Visible spectroscopy. The XRD pattern of the samples demonstrated single phase of CeO2, with cubic fluorite type structure and crystallite size of 6–7 nm. The morphology of the nanoparticles (NPs) was analyzed by FESEM and HRTEM which illustrated an aggregate of irregular spherical nanoparticles and the average particle size is around 18 nm. Raman spectroscopy validated the phase purity and indicated about the structural defects caused by the dopants. The bandgap energy of CeO2 NPs is calculated to be 3.00 eV from the Tauc plot of UV‐Visible spectroscopy, which gradually decreased to 2.43 eV with increase in manganese doping. Cytotoxicity studies signified the role of Mn‐doped CeO2 NPs as a potential nanotherapeutic agent for cancer treatment. The cell viability assay showed that 200 µg/mL of 6% Mn‐doped CeO2 nanoparticles exhibited remarkable cytotoxic effect by inhibiting 50% of cancer cells both in breast and colon cancer cell lines without affecting the healthy cell lines. [ABSTRACT FROM AUTHOR]

Hepatocellular carcinoma (HCC) is a leading cause of cancer‐related mortality worldwide, driven mainly by chronic hepatitis infections and metabolic disorders, which highlights the urgent need for novel therapeutic strategies. Sirtuins, particularly SIRT1 are crucial in HCC pathogenesis, making it a promising drug target. Indole‐based molecules show potential as therapeutic agents by interacting with key proteins like sirtuins involved in cancer progression. In this study, we designed and synthesized novel indole‐based small molecules and investigated their potential sirtuin inhibitory action and anticancer activity on HCC cell lines. Four of the twenty‐eight tested small molecules on different cancer types were selected (4 g, 4 h, 4o, and 7j) based on their structure–activity relationship and studied on a panel of HCC cell lines. Compounds had active drug‐target interactions with SIRT1 or SIRT2 based on DEEPScreen DTI predictions and docking studies which confirmed that 4o, 4 g, and 7j were most potent in their interaction with SIRT1. Compound 4 g caused the highest sirtuin activity inhibition in vitro and induced G1 arrest and apoptosis in HCC cell lines. [ABSTRACT FROM AUTHOR]

Chalcone is an aromatic ketone that forms the central core of many important biological compounds. Chalcone derivatives show various biological activities, especially anti-inflammatory, antibacterial, antioxidant, and anticancer activities, and also inhibit melanoma cell growth. In this study, we synthesized chalcone compounds with bis-chalcone's chemical structure under microwave (MW) and microwave–ultrasound (MW-US) conditions and compared them to chalcones produced using the classical synthesis method. All bis-chalcones were synthesized with terephthalaldehyde and an appropriate aromatic ketone as substrates in Claisen–Schmidt condensation. All the obtained compounds were tested regarding their roles as potential anticancer agents. The cytotoxic effect of the bis-chalcones against human MeWo and A375 melanoma cell lines was investigated through colorimetric MTT and SRB assays. The data were analyzed statistically. In the case of the synthesis of bis-chalcones, it was determined that the use of green conditions supported by the MW or MW-US factors led to an increase in the yield of the final products and a reduction in the reaction time compared to the classic method. The biological results showed the high cytotoxic effect of bis-chalcones. The present results show the compounds' high antiproliferative and cytotoxic potential, especially for the two selected bis-chalcone derivatives (3b and 3c), in particular, at concentrations of 50 μM–200 μM at 24, 48 h, and 72 h of incubation. The use of MW and US for the synthesis of bis-chalcones significantly improved the process compared to the classical method. The derivatives containing two hydroxy and two methoxy groups were the most effective against the tested cancer cells. [ABSTRACT FROM AUTHOR]

• Anticancer activity of C. campestris on MDA-MB-231, RL-95-2, MCF-7, SH-SY5Y cells. • C. campestris extract has antioxidant activity through DPPH, ABTS, and FRAP tests. • Phenolic profile of the extract was determined HPLC-DAD analysis. • C. campestris extract has in vivo antitumoral effect on breast cancer model of mice. Globally, the mortality rate attributed to cancer is on a concerning upward trajectory. Cancer, characterized by aberrations in the normal cell cycle, excessive proliferation, and abnormal differentiation, poses a formidable health challenge. Notably, breast cancer, constituting over one-third of all cancers in women, stands out as a prevalent malignancy. While diverse treatment modalities are deployed in the battle against cancer, herbal remedies emerge as a compelling option for those seeking treatments with minimal side effects. Cuscuta campestris Yunck , a staple in traditional medicine renowned for its efficacy in addressing cancer and various ailments, assumes a pivotal role in herbal medicine. Our investigation delved into assessing the anticancer potential of ethanol extracts from Cuscuta campestris Yunck, employing MDA-MB-231 (triple negative breast cancer cells), RL-95-2 (endometrium cancer cells), MCF-7 (ER positive breast cancer cells), SH-SY5Y (Neuroblastoma cancer cells), COLO 205 (Colon cancer cells), and A-549 (lung cancer cells) cell lines. Additionally, the antioxidant activity of the ethanol extract was gauged through DPPH, ABTS, and FRAP tests. Phenolic compounds of the extract was determined HPL-DAD analysis. The research delved further into the practical implications of Cuscuta campestris Yunck extract by employing a solid Ehrlich Ascites Tumor (EAT) model in mice. Furthermore, our study extended to scrutinizing the ethanol extractʼs anticancer efficacy across distinct phases (proliferation phase: 0–14 days, plateau phase: 14–28 days) of the solid Ehrlich Ascites Tumor (EAC) model in mice. Isorhamnetin was found the highest flavonol amount as 16.97 ± 1.27 mg.g−1 in the Cuscuta campestris Yunck extract. DPPH SC 50 values of 0.021 ± 0.001 mg/mL, ABTS SC 50 values of as 0.653 ± 0.071 mg/mL and FRAP values of as 20.122 ± 0.708 (µmol trolox/g ext), respectively. Cuscuta campestris Yunck extract significantly decreased the cell viability beginning from the 1 mg/ml concentration at the MDA-MB-231 (triple negative breast cancer) and RL-95-2 (endometrial cancer) cell lines. The research delved further into the practical implications of Cuscuta campestris Yunck extract by employing a solid Ehrlich Ascites Tumor (EAT) model in mice. Here, the extract exhibited a significant reduction in tumor volumes compared to the control group, pointing towards its tangible efficacy in impeding tumor growth. This multifaceted study not only sheds light on the intricate phenolic composition and antioxidant capabilities of Cuscuta campestris Yunck but also underscores its promising role as a botanical source for potential cancer treatment. [ABSTRACT FROM AUTHOR]

A new series of 1,2,3-triazole skeleton incorporated pyrrole derivatives (11a–j) were developed and their chemical structures were confirmed by analytical data. Further, the anticancer profile of these newly derived compounds 11a–j was assessed against four types of human cancer cell lines such as human breast cancer (MCF-7), lung cancer (A549), colon cancer (Colo-205) and ovarian cancer (A2780) by employing of the MTT method and was compared with etoposide used as a positive control. Most of the examined derivatives displayed moderate to good activity compared with the positive control. Among them, five compounds 11a, 11b, 11c, 11d, and 11e showed more potent activity. Particularly, compound 11a showed superior activity. [ABSTRACT FROM AUTHOR]

In this study, new Cu (II) and Zn (II) chelates (3–6) of 3‐/or 4‐ethyl and azo chromophore groups (NN) containing Schiff base ligands (2‐{(E)‐[(4‐ethylphenyl)imino]methyl}‐4‐[(E)‐phenyldiazenyl]phenol, HL1 (1) and 2‐{(E)‐[(3‐ethylphenyl)imino]methyl}‐4‐[(E)‐phenyldiazenyl]phenol, HL2 (2) were prepared and characterized by the analytical and spectroscopic methods. Crystal structures of chelates 3, 4 and 6 were determined by single‐crystal X‐ray diffraction studies. The ligands behaved as bidentates, coordinating through the nitrogen atom of the azomethine group (CHN) and the oxygen atom of the α‐hydroxyl group (OH). The metal:ligand ratio in the prepared copper (II) and zinc (II) chelates was found to be 1:2 by analytical and spectral analysis. The bands in the infrared spectra of the metal chelates in the region of 522–504 cm−1 and 467–455 cm−1 are attributed to ν(MO) and ν(MN) vibrations, respectively. When the DNA binding activities of the compounds were examined, it was determined that compound 4 had the highest binding constant. Fluorescence and viscosity data showed that the compounds interact with DNA through minor grove binding mode. Furthermore, anticancer properties of the compounds were investigated. Ligand 2 was found to be highly effective against the HepG2 cell with an IC50 of 0.31 μM. In addition, structural analysis, frontier molecular orbitals, molecular electrostatic potential maps, Hirshfeld surface analysis of the synthesized compounds using computational chemistry methods and anticancer activity studies were carried out by molecular docking. [ABSTRACT FROM AUTHOR]

Betulin and α-lipoic acid are naturally occurring substances with different biological properties. Combining two phytochemical units into a conjugate is a frequently used method to obtain new compounds with better pharmacokinetic parameters. This research concerned the preparation of lipoate derivatives of betulin using the Steglich method. Experimental lipophilicity values were determined for target compounds 6–10 by reversed-phase thin-layer chromatography. In silico methods were used to calculate the physicochemical parameters and lipophilicity of new derivatives and to determine the probable directions of biological activity. α-Lipoic acid, betulin, and lipoate derivatives 6–10 were tested for antiproliferative activity against MV4-11, A549, MCF-7, PC-3, HCT116, MiaPaca-2, and Hs294T cancer cells. 3-(5-(1,2-Dithiolan-3-yl)pentanoyl))betulin 10 showed moderate anticancer activity against MV4-11, PC-3, and HCT116, with IC50 values in the range of 39.8–76.7 µM. The introduction of a dithiolate substituent at the C3 position in 28-acetylbetulin gave compound 9 the highest activity (IC50 = 37.9 µM), in the ratio of biphenotypic B myelomonocytic leukemia cells (MV4-11). All lipoate derivatives were inactive towards normal cells. [ABSTRACT FROM AUTHOR]

In this study, Mesosphaerum suaveolens extracts were used for the green fabrication of fluorescent Carbon Quantum Dots (CQDs) by the microwave-assisted method. This study unravels the effect of CQDs on improving the photocatalytic degradation of methylene blue (MB) and Rhodamine B (RhB) dyes followed by the anticancer activity against human breast cancer cells (MDA-MB-231). The bio-fabricated CQDs indicated various characteristics that were analyzed, including phase, structure, functional groups, and binding energies. The CQDs displayed notable photocatalytic performance in the removal of MB (80.73%) and RhB (92.3%) dye, after 200 min of sunlight irradiation. The highest catalytic degradation activity of the CQDs is accredited to their high electron transport at the edges, which is helpful to the efficient separation of electron–hole pairs. Furthermore, the anticancer activity of CQDs was demonstrated against human breast cancer cells (MDA-MB-231). This research suggests that bio-fabricated CQDs act as active photocatalysts and hold promise as a potentially ideal material for mitigating water pollution and exploring anticancer potentials in the future. [ABSTRACT FROM AUTHOR]

Commonly used antimicrobial agents are no longer effective due to their overuse or misuse. In addition, many medicinal plant extracts can combat infectious diseases due to their main active constituents or secondary metabolites. The current study aimed to assess the bioactivities of Launaea nudicaulis (LN) leaf extract (LE) against different multi-drug resistant (MDR) Pseudomonas aeruginosa (P. aeruginosa) isolates. The ethyl acetate extract of a Launaea nudicaulis (LN) leaf was analyzed using GC–MS, which identified 27 key bioactive compounds. The major constituents found were as follows: 7-acetyl-6-ethyl-1,1,4,4-tetramethyltetralin, isopropyl myristate, thiocarbamic acid, N,N-dimethyl, S-1,3-diphenyl-2-butenyl ester, hahnfett, cyclopentane acetic acid, 3-oxo-2-pentyl-, methyl ester, hexadecanoic acid, and dotriacontane. Our study demonstrated that the LN leaf was a rich source of other important phytochemicals, including phenolic acids, tannins, saponins, and steroids. The relative biosafety of the L. nudicaulis LE was determined from the elevated inhibitory concentration 50 (IC50) of 262  μg/mL, as calculated from the cytotoxicity assay against the Wi-38 normal cell line. Conversely, 12.7 and 24.5  μg/ mL were the recorded low IC50 values for the tested extract against the MCF-7 and Hep-G2 cancerous cell lines, respectively, reflecting its potent activity against the tested cancerous cell lines. Microbiologically, the susceptible P. aeruginosa isolates to the tested extract showed a growth inhibition zone diameter, in the well diffusion assay, ranging from 11.34  ±  0.47 to 26.67  ±  0.47  mm, and a percent inhibition (PI) value of 50–106.2%, reflecting its acceptable activity. In addition, the broth microdilution assay recorded minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) in the ranges of 15.625–1,000  μg/mL and 125–1,000  μg/mL, respectively. In conclusion, the L. nudicaulis LE revealed showed promising activity and high selectivity against P. aeruginosa. Moreover, the extract exhibited natural anticancer activities with safe low concentrations, indicating its potential as a superior candidate for future studies of its active constituents. [ABSTRACT FROM AUTHOR]

AbstractThis study aims to prepare, characterize, and evaluate zinc oxide nanoscaffolds (ZnO NSs) as a potential anticancer drug that selectively targets malignant cells while remaining non-toxic to normal cells. Electrospun NSs were fabricated and loaded with varying concentrations of ZnO nanoparticles (NPs). The uniform morphology of the fabricated samples was confirmed through Field Emission Scanning Electron Microscope (FESEM) imaging. Elemental composition was investigated using Energy Dispersive X-ray spectroscopy (EDX), Fourier Transform Infrared (FTIR), and X-ray diffraction (XRD) analyses. Biocompatibility and cytotoxicity were assessed using the (3-(4.5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay) (MTT) assay and flow cytometry. The water uptake and degradation properties of the electrospun NSs were also examined. Furthermore, a cumulative release profile was generated to assess the release behavior of ZnO NSs. The prepared ZnO NSs demonstrated negligible toxicity toward normal human dermal cells. Conversely, the four used concentrations of ZnO NSs displayed substantial cytotoxicity and induced apoptosis in various cancer cell lines. The observed effects were concentration-dependent. Notably, ZnO NSs 8% exhibited the most significant reduction in cell viability against the MCF7 cell line. The findings from this study indicate the potential of ZnO NSs as an effective anticancer agent, with the ZnO NSs 8% demonstrating the most pronounced impact. This research introduces a novel application of electrospun zinc oxide nanoscaffolds, demonstrating their capacity for selective anticancer activity, particularly against breast carcinoma, while preserving normal cell viability. The study presents a significant advancement in the use of nanomaterial for targeted cancer therapy. [ABSTRACT FROM AUTHOR]

Schiff bases have proven to be beneficial in medicine and have interesting complexation capabilities with transition metals. The +4, +5, and +6 oxidation states of schiff base metal complexes have been the subject of recent review, which have highlighted their notable cytotoxic effects against various colon cancer cell lines (HT-29, HCT-116, SW-480, Coco-2, CT-26, LT-174, LoVo). Extensive research has focused on schiff base metal complexes in the +4 and +6 oxidation states, exhibiting distinct geometries and significant thermodynamic stability. These studies provide IC50 values for these complexes in colon cancer cell lines along with comprehensive structural representations that shed light on how different substituents affect cytotoxicity. When compared to schiff base ligands alone, metal complexes of schiff bases have been shown to significantly reduce colon cancer cell invasion and proliferation. The studied literature emphasizes schiff base metal complexe’s potential in biological applications and suggests that more study may be necessary to fully comprehend their biology. To enable more sophisticated multidisciplinary study in this field, future investigations should focus on synthesizing novel complexes with enhanced bioavailability, solubility, and low toxicity. [ABSTRACT FROM AUTHOR]

ABSTRACT This article explains the synthesis of three Schiff base Cu(II) complexes derived from 3‐hydroxybenzaldehyde and ethylenediamine using three distinct copper anionic salts, and it explores the effects of those salts on the properties of the complexes. Elemental analysis, electronic spectra, FT‐IR, ESR, molar conductance, magnetic measurement, thermogravimetric analysis and PXRD were used to characterize the compounds. The anionic salt has been demonstrated to exhibit distinctive characteristics on Gram‐positive and Gram‐negative bacteria in terms of structure, DNA binding, cell viability, DNA breakage and activity. Furthermore, this ligand L1 and its derivatives indicated positive antifungal efficacy against Aspergillus niger and Trichophyton tonsurans. The study elucidates the manner in which distinct anion salts impacted the properties of complexes and their antifungal, anticancer and antibacterial outcomes. [ABSTRACT FROM AUTHOR]

This work presents a theoretical study of the antioxidant and anticancer properties of three flavonoid derivatives Isoquercitin, Ophioglonol, and Quercetin. DFT calculations were performed to analyze their electronic properties, providing insights into their reactivity and mechanism of action. Molecular docking and molecular dynamics simulations were conducted to examine the stability behavior of the protein‐ligand complexes, providing a detailed mechanism of the interactions at the atomic level. Additionally, some physicochemical and pharmacokinetic predictions were examined by using several web servers. Quercetin and isoquercetin show therapeutic properties, with MESP plots revealing interaction regions with SOD and hAPN targets. However, isoquercetin raises concerns related to AMES toxicity and hERG inhibition. The results of Molecular docking and MD simulations provide theoretical guidance for developing effective inhibitors to treat cancer, but further experimental validation is needed to optimize therapeutic efficacy. The MM/GBSA show that Ophioglonol has the strongest binding affinity with the protein, driven by many interactions. The Actionon also demonstrates strong binding, while Isoquercitin and Quercetin have moderate to weaker affinities. The PCA revealed distinct conformational changes in the protein upon binding with the ligand, highlighting specific regions of flexibility, which could be crucial for understanding their binding mechanisms and potential therapeutic effects. [ABSTRACT FROM AUTHOR]

This study aimed to explore the antioxidant potential of the ethyl acetate extract of Streptomyces coeruleofuscus SCJ strain, along with its inhibitory effects on the triple-negative human breast carcinoma cell line (MDA-MB-468). The ethyl acetate extract's total phenolic and flavonoid contents were quantified, and its antioxidant activity was investigated using DPPH (1,1-Diphenyl-2-picrylhydrazyl), ABTS (2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid), and FRAP (Ferric Reducing Antioxidant Power) assays. Furthermore, the cytotoxic effect of the organic extract from Streptomyces coeruleofuscus SCJ on MDA-MB-468 cancer cells was assessed via the crystal violet assay. In tandem, a thorough computational investigation was conducted to explore the pharmacokinetic properties of the identified components of the extract, utilizing the SwissADME and pKCSM web servers. Additionally, the molecular interactions between these components and Estrogen Receptor Beta, identified as a potential target, were probed through molecular docking studies. The results revealed that ethyl acetate extract of SCJ strain exhibited remarkable antioxidant activity, with 39.899 ± 1.56% and 35.798 ± 0.082% scavenging activities against DPPH and ABTS, respectively, at 1 mg/mL. The extract also displayed significant ferric reducing power, with a concentration of 1.087 ± 0.026 mg ascorbic acid equivalents per mg of dry extract. Furthermore, a strong positive correlation (p < 0.0001) between the antioxidant activity, the polyphenol and the flavonoid contents. Regarding anticancer activity, the SCJ strain extract demonstrated significant anticancer activity against TNBC MDA-MB-468 cancer cells, with an inhibition percentage of 62.76 ± 0.62%, 62.67 ± 0.93%, and 58.07 ± 4.82% at 25, 50, and 100 µg/mL of the extract, respectively. The HPLC-UV/vis analysis revealed nine phenolic compounds: gallic acid, sinapic acid, p-coumaric acid, cinnamic acid, trans-fereulic acid, syringic acid, chloroqenic acid, ellagic acid, epicatechin. Streptomyces coeruleofuscus SCJ showed promise for drug discovery, exhibiting antioxidant and anticancer effects. [ABSTRACT FROM AUTHOR]

Introduction: The method of encapsulating the drug molecule in a carrier, such as a magnetic nanoparticle, is a promising development that has the potential to deliver the medicine to the site where it is intended to be administered. Morin is a pentahydroxyflavone obtained from the leaves, stems, and fruits of various plantsmainly from the Moraceae family exhibiting diverse pharmacological activities such as anti-inflammatory, anti-oxidant, and free radical scavenging and helps treat diseases such as diabetes, myocardial infarction and cancer. Methods: In this study, we conducted the synthesis of a nanocomposite with magnetic properties by coating biocompatible activated carbon obtained from okra plant leaves with magnetic nanoparticles. Results: Characterization of the synthesized activated carbon-coated magnetic nanocomposite was confirmed by Fourier transform infrared, scanning electron microscopy, dynamic light scattering, and zeta potential. The cytotoxic effects of the drug-loaded magnetic nanocomposite were examined in HT-29 (Colorectal), MCF-7 (breast), U373 (brain), T98-G (Glioblastoma) cancer cell lines, and human umbilical vein endothelial cells healthy cell line. Discussion: We studied the loading and release behavior of morin hydrate in the activated carbon-coated magnetic nanocomposite. Activated carbon-coated magnetic nanocomposite carriers can show promising results for the delivery of Morin hydrate drugs to the targeted site. [ABSTRACT FROM AUTHOR]

Background: Solid tumors often develop hypoxic regions, leading to aggressive behavior and increased drug resistance. Methods: The chemical composition of Cymbopogon citratus essential oil (EO) was analyzed using GC-MS. Alginate nanoparticles containing the EO and its primary component, citral, were synthesized via the ionic gelation method. Encapsulation was confirmed using ATR-FTIR analysis. The anticancer efficacy of C. citratus EO, citral, and their respective alginate nanoparticles was evaluated under normoxic (21% oxygen) and hypoxic (1% oxygen) conditions on breast cancer (MDA-MB-231) and melanoma (A-375) cell lines. Additionally, qPCR and flow cytometry were used to assess apoptosis gene expression ratios (Bax/Bcl-2) and levels of apoptosis. Results: Citral (80.98%) was identified as the major component of the EO. Alginate nanoparticles containing C. citratus EO and citral (C. citratus-AlgNPs and citral-AlgNPs) were synthesized with particle sizes of 195 ± 4 nm and 222 ± 9 nm, and zeta potentials of -22 ± 3 mV and − 17 ± 1 mV, respectively. Both samples demonstrated significantly greater efficacy under hypoxic conditions. Citral and C. citratus-AlgNPs had IC50 values of 27 (19–39) µg/mL and 25 (4-147) µg/mL, respectively, against MDA-MB-231 and A-375 cells. Flow cytometry showed increased apoptosis under hypoxic conditions, with the highest rates observed for citral-AlgNPs and C. citratus-AlgNPs (84 ± 5 and 92 ± 5% in MDA-MB-231 and A-375 cells, respectively). Conclusion: This study demonstrates that alginate nanoparticles enhance the anticancer activity of C. citratus-AlgNPs and citral, particularly under hypoxic conditions, highlighting their potential for hypoxia-targeted cancer therapies. [ABSTRACT FROM AUTHOR]

ABSTRACT Twenty new substituted erlotinib analogs with anticancer activity were produced with good to excellent yields through the one‐step reaction of erlotinib, aromatic aldehydes, and cyclic secondary amines such as piperidine, morpholine, pyrrolidine, N‐methylpiperazine, or imidazole using nano‐CuO in choline chloride: urea (ChCl:urea) solvent under ultrasound irradiation at 80°C. MTT protocol was applied to investigate the cytotoxicity of all produced substituted erlotinib analogs in A431 (human epidermoid carcinoma cell) and HU02 (foreskin fibroblast) cell lines. The results illustrated that at a concentration of less than 10 μM, the growth of A431 cells could be inhibited by the produced compounds. Compared to erlotinib as positive control, the highest cytotoxic activity with IC50 equal to 2.58 ± 0.57 μM belonged to compound 4c carrying 4‐fluorobenzene with piperidine substitution. All of the synthesized compounds showed significant cytotoxic activity on A431, while showing no apparent cytotoxicity to HU02. The reasons for the stronger cytotoxic activity 4c can be most probably attributed to the two phenomena of greater solubility of the fluoro derivative and the flexibility of piperidine. Based on this study, compound 4c is the most promising compound with anticancer properties. [ABSTRACT FROM AUTHOR]

Ovarian cancer is the fifth most prevalent cancer in women. Chemotherapy is a major treatment option for patients with advanced ovarian cancer (OC). Quinoline-2-thione and its derivatives are potential candidates for tumor therapy. In this study, we investigated the anticancer activity of the quinoline-2-thione derivative KA3D against ovarian cancer. The effect of KA3D on the viability of ovarian cancer cells was evaluated using MTT assay, and its effects on apoptosis and the cell cycle were detected using flow cytometry. Western blotting was performed to identify apoptosis-and cell cycle-related proteins altered by KA3D treatment. A xenograft model was used to verify the inhibitory effect of KA3D in vivo. H&E staining, biochemical indicator detection, and blood cell counts were used to observe the toxicity and side effects of KA3D. KA3D treatment impeded cell viability, induced apoptosis, and impeded the G2 phase of the cell cycle in ovarian cancer cells. Mechanistically, we found that KA3D enhanced the expression of proapoptotic molecules such as BAX and Caspase 3, while antiapoptotic proteins such as BCL2 were inhibited. The G0/G1 phase-related protein cyclin D1 was reduced and the G2 phase-related protein cyclin B1 was upregulated. In vivo, KA3D displayed potent anticancer activity, with no apparent toxicity in BABLC/c nude mice bearing SKOV3 cells. KA3D demonstrated remarkable chemotherapeutic drug efficacy in terms of significant cancer suppression in vitro and in vivo with low toxicity. [ABSTRACT FROM AUTHOR]

Worldwide, cancer ranks among the foremost contributors to mortality despite recent medical progress. Alternative approaches in controlling various forms of cancer are being highly explored by researchers. This study provides the global research trends in the utilization of medicinal plant-synthesized nanoparticles for cancer treatment over the span of 18 years using scientometric analysis. Recent research advances on medicinal plant-derived nanoparticles for cancer treatment and their possible mechanisms of action were described. Relevant articles published between 2005 and 2023 were retrieved from Scopus and Web of Science and analyzed using RStudio and VOSViewer. Scientometric indicators were employed to analyze the results. The initial search returned 5695 articles, with a publication growth rate of 3.71% annually. Countries from Asia contributed the most (61.37%) to the total number of publications. The therapeutic effects of nanoparticles derived from medicinal plants can be attributed to various mechanistic pathways, including induced apoptosis from reactive oxygen species generation, as well as mitochondrial and cell membrane disruption, amongst others. Although some reported studies demonstrated promising safety and efficacy against certain cancer cells in vivo and in vitro, the little to no clinical data on medicinal plant-synthesized nanoparticles hinder the ability to make informed decisions about their clinical potential in cancer treatment. [ABSTRACT FROM AUTHOR]

In this work, we reported the synthesis of honey bee (Apis mellifera) venom-derived nanoparticles via a hydrothermal method. This method not only ensures the preservation of the bee venom's bioactive components but also enhances their potential stability, thus broadening the scope for their applications in the biomedicinal field. The synthesis method started with the homogenization suspension of bee venom, followed by its hydrothermal process to synthesize bee venom nanoparticles (BVNPs). The successful synthesis of BVNPs was characterized using various characteristic techniques such as Ultraviolet–visible (UV–Vis) spectroscopy, Fourier Transforms Infrared (FTIR) Spectroscopy, Zeta Potential (ZP), Liquid Chromatography-Mass Spectrometry (LCMS), and Transmission Electron Microscopy (TEM). The synthesis of BVNPs through biosynthesis is shown by the visible violet-brown color development at 347 nm by UV–Vis spectroscopy. FTIR analysis revealed the presence of several functional groups in the BVNPs, including alcohols (–OH), phenols (C6H5–), carboxylic acids (–COOH), amines (–NH2, –NH–), aldehydes (–CHO), ketones (–CO–), nitriles (–CN), amides (–CO–N–), imines (–CNH–), esters (–COO–), and polysaccharides. These functional groups, as confirmed by their specific stretching and bending vibrational modes, contribute to the diverse biological activities of BVNPs, including cytotoxicity against MCF-7 breast cancer cells. The ZP of the BVNPs indicated good colloidal stability at − 45 mV. LCMS analysis confirmed the presence of major bioactive molecules, including melittin & apamin and TEM analysis shows the BVNPs exhibited a quasi-spherical shape with good dispersion, the average size was approximately 25 nm, with some being smaller (quantum dots) and interplanar spacing of 0.236 nm indicated a highly ordered crystalline structure. Moreover, the anticancer efficacy of the BVNPs was ascertained through in vitro assays against MCF-7 breast cancer cells, showing a dose-dependent cytotoxic effect. The findings of this study underscore the viability of hydrothermal synthesis in producing biologically active and structurally stable BVNPs, with a significant potential for anticancer activities. [ABSTRACT FROM AUTHOR]

A novel library of 4H‐chromene‐7‐azaindole‐1,2,3‐triazole hybrids (6 a‐n) utilizing 1‐(prop‐2‐yn‐1‐yl)‐1H‐pyrrolo[2,3‐b]pyridine‐3‐carbaldehyde, 5,5‐dimethylcyclohexane‐1,3‐dione and malononitrile as precursors involving multicomponent synthesis and click chemistry reactions. The title compounds were screened for their invitro anticancer activity against human breast adenocarcinoma (MCF‐7), human cervical cancer (HeLa) and prostate cancer (DU‐145) cells by using Doxorubicin as standard reference. The activities of all compounds could be more effecting against HeLa cells. Compound 6 g with 3‐nitro substitution on phenyl ring displayed outstanding activity against all three cell lines with IC50 value of 6.67±0.39 μM (MCF‐7), 4.49±0.32 μM (HeLa) and 10.38±0.42 μM (DU‐145) than reference drug. The compound 6 h with methyl group in ortho position of phenyl ring showed best activity with IC50 value of 7.32±0.62 μM, 6.87±0.33 μM and 15.40±0.60 μM against MCF‐7, HeLa and DU‐145 cells respectively. Performed molecular docking study against crystal structure of EGFR obtained favorable binding interactions showing consistency with experimental results. [ABSTRACT FROM AUTHOR]

Cancer is a devastating disease, with female breast cancer becoming the leading cause of global cancer morbidity. Sorafenib is a multiple kinase inhibitor, and exhibits activity against a wide spectrum of tumor types, however, in some cases it proves insufficient. Synthesis of sorafenib analogs can be an efficient way to discover potent cancer therapeutic agents. In this work, we intended to design sorafenib analogs and determine their antiproliferative activity against five cancer cell lines (A549, HepG2, HCT116, MDA‐MB‐231, and PC‐3) using MTS method. As a result, we synthesized a sorafenib analog 1 A and its base‐promoted arranged compound 1 A2. Their in‐vitro cytotoxicity and potencies in the epidermal growth factor receptor (EGFR) inhibition study revealed that compound 1 A displayed higher inhibition activity than cisplatin in MDA‐MB‐231 (breast cancer) cells with an IC50 value of 16.18±1.42 μM. The structure of 1 A2 was explicitly confirmed by the single‐crystal X‐ray diffraction analysis. [ABSTRACT FROM AUTHOR]

The core structure is an aromatic heterocyclic organic compound i.e. Isoquinoline. Both the structures of Isoquinoline and quinoline contain a fused ring structure of benzene and pyridine. Isoquinoline, the pyridine counterpart, has a pKb of 8.6 and a pKa of 5.14, making it a weak basic. When it comes into contact with Lewis acids, such BF3, it protonates and becomes a salt. This process produces adducts. The liquid form of Isoquinoline is colorless, hygroscopic, and it has an unpleasant smell. Isoquinoline derivatives are a very significant group of natural and synthetic compounds which show various Pharmacological activities like anti-cancer, anti-oxidant, anti-microbial, anti-inflammatory, anti-microbial, analgesic, anti-fungal, anti-viral, antispasmodic and an enzyme inhibitor. Morphine and codeine are the most extensively characterized Isoquinoline alkaloids. They are made from either tyrosine or phenylalanine. Some of the Isoquinoline nucleus-containing drugs available in the market were Nelfinavir, Apomorphine, Quinapril, Praziquantel, Solifenacin, Papaverine, Metocurine, Tubocurarine. Isoquinoline alkaloids with anticancer properties may be therapeutically to target specific binding to nucleic acids, modulating polynucleic acid stability. These binds change the way that duplex B-form DNA interacts with proteins involved in DNA replication, repair, or transcription. [ABSTRACT FROM AUTHOR]

Tragopogon coelesyriacus is a pharmacotherapeutic herbaceous plant belonging to the Asteraceae family and consumed as a vegetable. Here, the methanolic and water extracts of T. coelesyriacus were obtained from its aboveground parts (stem, leaves, and flowers), and the phytochemical potentials were investigated by LC‐HRMS (liquid chromatography–high resolution mass spectrometry) analysis for the first time. The antibacterial, antifungal, and anticarcinogenic activities of T. coelesyriacus extracts were investigated using experimental and in silico methods. T. coelesyriacus methanol extract revealed remarkable inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumonia (MICs = 0.83, 1.67, and 1.67 mg/mL, respectively) compared to Escherichia coli and Enterobacter aerogenes (MIC = 53.3 mg/mL). Inhibitory effects of T. coelesyriacus methanolic extracts were also observed in all Candida species tested, with the highest inhibition on Candida krusei (MIC = 0.83 mg/mL), whereas no inhibitory effect was identified from the water extract. Additionally, both T. coelesyriacus methanolic (IC50 = 86 μg/mL) and water (IC50 = 92 μg/mL) extracts revealed significant selective anticarcinogenic effects on AR42J pancreatic cancer cells. HeLa and MDA‐MB‐231 cells were, however, more resilient to methanol and water extract, respectively. In silico analyses further elucidated the noteworthy antibacterial potential of keracyanin chloride on S. aureus MurB enzyme and the remarkable inhibitory potential of naringin on FYN kinase specific for pancreatic cancer (AR42J) development. In conclusion, T. coelesyriacus phytochemicals with antibacterial, antifungal, and anticancer properties were revealed for the first time, and molecular docking studies on potential targets confirmed good agreement with experimental findings. Therefore, the current studies on T. coelesyriacus provide the basis for investigating new pharmaceutical potentials of other Tragopogon members. [ABSTRACT FROM AUTHOR]

Simple Summary: Carbon dots (CDs) are carbon-based nanomaterials with versatile applications, including fluorescence imaging, drug and gene transport, drug delivery, medical diagnosis, and biosensing. In this study, we successfully synthesized various CDs without significantly impacting the cell viability of cancer cells, which suggests the potential for future bioimaging and drug delivery applications. These findings contribute to advancing the potential of CDs in various biomedical research contexts. Backgroung: The rising complexity and associated side effects of cancer treatments highlight the need for safer and more effective therapeutic agents. Carbon-based nanomaterials such as CDs have been gaining prominence for their unique characteristics, opening avenues for diverse applications such as fluorescence imaging, drug and gene transport, controlled drug delivery, medical diagnosis, and biosensing. Despite promising advancements in research, it remains imperative to scrutinize the properties and potential cytotoxicity of newly developed CDs, ensuring their viability for these applications. Methods: We synthesized four N-doped CDs through a hydrothermal method. Cell viability assays were conducted on A549 and UM-UC-5 cancer cells at a range of concentrations and incubation times, both individually and with the chemotherapeutic agent 5-fluorouracil (5-FU). Results: The obtained results suggest that the newly developed CDs exhibit suitability for applications such as bioimaging, as no significant impact on cell viability was observed for CDs alone. [ABSTRACT FROM AUTHOR]

ABSTRACT A total of 48 tetrahydrooxazolo‐[5′,4′:4,5]pyrimido[1,2‐a]azepinones were designed and synthesized from a scaffold hopping approach. All compounds were confirmed by analysis using 1H NMR, 13C NMR, and HRMS techniques. The synthesized compounds were evaluated against the human cancer cell lines (HeLa, MCF‐7, A549) in vitro, and the structure–activity relationships were summarized. The compound E43 exhibited the best inhibitory activity against HeLa, MCF‐7, A549, displaying IC50 values of 1.48 ± 0.13, 3.01 ± 0.09, and 5.11 ± 0.13 μM. Molecular docking indicated that compound E43 may bind to protein (PDB:6FEX) via hydrogen bond and π stacking. Further, molecular dynamics simulations indicated a relatively low binding free energy (−40.06 kJ·mol−1) of compound E43 with protein. In conclusion, these findings suggested that E43 is promising as a potential novel anticancer drug candidate worthy of further investigation. [ABSTRACT FROM AUTHOR]

Novel complexes of form (NHC)Au(SCOR) (NHC = N‐heterocyclic carbene, SCOR− = thiocarboxylate ligand) were synthesised and characterised by spectroscopic techniques and X‐ray diffraction studies. The results of NMR and X‐ray studies indicated that thiocarboxylate ligands are comparable with NHCs in their electron donor ability. The complexes were stable at room temperature in the solid state but in solution underwent disproportionation reactions to form equilibria with [Au(NHC)2]+ and [Au(SCOR)2]−. In solution, the thiocarboxylate ligand in (NHC)Au(SCOR) underwent rapid exchange with other thiocarboxylate or thiolate ligands. The (NHC)Au(SCOR) complexes showed toxicity against cisplatin‐resistant ovarian cancer cells (OVCAR‐8), with IC50 < 10 μM, in the range exhibited by cationic [Au(NHC)2]+ complexes well‐known for their promising anticancer activity. [ABSTRACT FROM AUTHOR]

A straightforward synthetic route to new N‐heterocyclic carbene (NHC)‐gold‐steroidyl complexes is reported. The desired complexes were obtained using a weak base (such as K2CO3) through a concerted‐metallation‐deprotonation (CMD) reaction mechanism occurring between [Au(NHC)Cl] and ethisterone as a model steroid‐based alkyne. Most complexes displayed good cytotoxicity against a panel of cancer cell lines with IC50 values in the low micromolar range. Cellular uptake of the most active complex 2a into MCF‐7 breast cancer cells was facilitated by the coordinated ethisterone ligand. [ABSTRACT FROM AUTHOR]

Three silver N‐heterocyclic carbene (NHC) complexes (Ag1–Ag3) were designed and synthesized using quinoline‐functionalized benzoimidazole salts (L1–L3). Both NHC precursors and resultant silver‐NHC complexes were characterized by NMR, FT‐IR spectroscopy, and elemental analysis. X‐ray diffraction analysis was additionally performed to investigate the crystal structures of these silver‐NHC complexes. The results showed that Ag1 is a dinuclear silver complex with a deviated linear geometry. Ag2 has a disilver core in which two silver atoms are coordinated by two quinoline‐functionalized carbene ligands and one acetonitrile molecule. The silver‐NHC complex Ag3 is composed of a silver‐triangle formed by three silver atoms and three carbene ligands. The in vitro cytotoxic studies revealed that silver‐NHC complexes had stronger antitumor activity than their corresponding NHC precursors. Notably, after a 24‐h exposure to cancer cells, Ag2 presented the highest cytotoxicity with a half maximal inhibitory concentration (IC50) at 1.74 ± 0.08 μM in A2780 cells, which was approximately 14‐fold lower than that of the clinically approved metallodrug cisplatin (IC50 = 24.74 ± 1.35 μM). Detailed mechanistic studies suggested that the complex Ag2 provoked intracellular reactive oxygen species (ROS) overproduction and mitochondrial membrane depolarization, which eventually resulted in mitochondrial dysfunction and cell potent necrosis. Overall, our studies show that NHC‐coordinated silver complexes can be readily constructed and used as an attractive class of anticancer agents, which is conductive for further investigation of their therapeutic potential for treating cisplatin‐resistant cancers. [ABSTRACT FROM AUTHOR]

The fungus Ophiocordyceps sinensis OS8 has been sourced from the wild variant of O. sinensis. In this study, the enriched β-D-glucan polysaccharide obtained from cultured mycelium of O. sinensis OS8 (OS8P) was examined for its potential to inhibit the growth of HepG2 liver cancer cells, and the IC 50 was 511.79 µg/mL. The study of cellular migration was analyzed by scratch assay. It was found that the HepG2 cell migration was significantly inhibited (P < 0.05) in the OS8P-treated group. The cell apoptotic feature's reliability was determined via DAPI staining to confirm the experimental results' reliability. The AO/PI double staining assay showed that HepG2 cells treated with OS8P (IC 50) had dead cells with condensed and shrieking nuclei that are late apoptotic. Morphological alterations were meticulously examined using scanning electron microscopy. The specific morphological characteristics of apoptotic cells, notably cell lysis, were distinctly observable. The damaged cells demonstrated severe structural disruption, loss of original shape, blebs formation, and apoptotic bodies' appearance. These findings provide pharmacological proof that the OS8P extract could be potentially employed in the food and medical industries for anticancer applications. [Display omitted] • Fungus O. sinensis OS8 as alternative source for biomedicine. • Its main bioactive compound is a β-D-glucan polysaccharide. • It has bioactivity against migration of liver cancer cells. • It has potential inducing liver cancer cell death via apoptosis. [ABSTRACT FROM AUTHOR]

Green synthesis of gold nanoparticles (AuNPs) using Ginkgo biloba leaf aqueous extract was optimized by response surface methodology to yield monodispersed, crystalline nanoparticles of 18 ± 4 nm diameter. Fourier transform infrared spectroscopy confirmed capping by flavonoids, terpenoids and polyphenols providing stability for over 6 months. The biosynthesized AuNPs exhibited promising in vitro dose and time-dependent antiproliferative effects against human nasopharyngeal carcinoma CNE1 cells with IC50 reducing from 65.7 to 39.2 μg/mL over 24–72 hrs. Distinct cytoplasmic damage was observed under microscope. Treatment with 50 μg/mL AuNPs for 48 hrs dramatically upregulated pro-apoptotic Bax, Caspase-3 and p53 by 8.7, 6.5 and 4.3 fold respectively while downregulating anti-apoptotic Bcl-2 by 11.2 fold, indicating apoptosis induction via mitochondrial intrinsic pathway. The green fabricated G. biloba AuNPs displayed preferential toxicity towards carcinoma cells compared to normal fibroblasts, indicating potential for targeted nasopharyngeal cancer therapy. [ABSTRACT FROM AUTHOR]

In this research, the study utilized the root, leaf, and petiole parts of in vitro grown Salvia hispanica plants as explants. Following UV‐C treatment applied to developing callus, methanol extracts were obtained and analyzed using liquid chromatography–mass spectrometry (LC/MS) to investigate their anticancer properties. First, the seeds of S. hispanica were soaked in commercial bleach for 6 min to ensure surface sterilization. The most effective antimicrobial activity on Gram‐negative bacteria, with a zone diameter (11 ± 0.82 mm), was noticed in callus extracts obtained from the petiole explant in the second protocol against Klebsiella pneumoniae EMCS bacteria. Anticancer activities on SH‐SY5Y human neuroblastoma cells were investigated by using 1000, 500, 250, 125, 62.5, 31.25, 15.62, and 78.12 μg/mL doses of the extracts, and the most effective cytotoxic activity was determined at the 1000 μg/mL dose of the extracts obtained from both protocols. The extracts were determined to inhibit hCAI, hCAII, AChE, and BChE enzymes. The content of 53 different phytochemical components of the extracts was analyzed by liquid chromatography with tandem mass spectrometry (LC–MS/MS). Rosmarinic acid, quinic acid, and caffeic acid were found in the highest concentration. The comprehensive LC–MS/MS analysis of S. hispanica extracts revealed a diverse array of phytochemical compounds, highlighting its potential for therapeutic applications. [ABSTRACT FROM AUTHOR]

Background/Objectives: This study investigated the anticancer potential of an aqueous extract of the fungus Fomitopsis betulina. Methods: The study assessed the effect of the extract on nine cancer cell lines, including melanoma (LM-MEL-75), lung cancer (A549), and colorectal cancer (HT29, LoVo), and four normal cell lines. The cytotoxicity of the extract was evaluated using MTT, sulforhodamine-B (SRB), and clonogenic viability assays. Additionally, the study examined the effect of the extract on plant model organisms, garden cress (Lepidium sativum) and common onion (Allium cepa), to further investigate its biological activity. Results: The assays demonstrated selective cytotoxicity of the extract toward cancer cells, while sparing normal cells. The extract induced significant cytotoxic effects at lower concentrations in lung cancer, melanoma, and colon cancer cells, showing promise as a potential anticancer agent. The results also revealed that the extract inhibited seed germination and root growth, suggesting its potential to disrupt cell cycles and induce apoptosis. Conclusions: This study highlights the therapeutic potential of F. betulina and highlights the need for further research to identify the active ingredients and mechanisms underlying its anticancer effects. [ABSTRACT FROM AUTHOR]

Breast cancer is the most prevalent form of cancer in women worldwide. Triple-negative breast cancer is the most unfavorable for patients, but it is also the most sensitive to chemotherapy. Triterpene glycosides from sea cucumbers possess a high therapeutic potential as anticancer agents. This study aimed to identify the pathways triggered and regulated in MDA-MB-231 cells (triple-negative breast cancer cell line) by the glycosides cucumarioside A0-1 (Cuc A0-1) and djakonovioside A (Dj A), isolated from the sea cucumber Cucumaria djakonovi. Using flow cytometry, fluorescence microscopy, immunoblotting, and ELISA, the effects of micromolar concentrations of the compounds on cell cycle arrest, induction of apoptosis, the level of reactive oxygen species (ROS), mitochondrial membrane potential (Δψm), and expression of anti- and pro-apoptotic proteins were investigated. The glycosides caused cell cycle arrest, stimulated an increase in ROS production, and decreased Δψm in MDA-MB-231 cells. The depolarization of the mitochondrial membrane caused by cucumarioside A0-1 and djakonovioside A led to an increase in the levels of APAF-1 and cytochrome C. This, in turn, resulted in the activation of caspase-9 and caspase-3 and an increase in the level of their cleaved forms. Glycosides also affected the expression of Bax and Bcl-2 proteins, which are associated with mitochondria-mediated apoptosis in MDA-MB-231 cells. These results indicate that cucumarioside A0-1 and djakonovioside A activate the intrinsic apoptotic pathway in triple-negative breast cancer cells. Additionally, it was found that treatment with Cuc A0-1 resulted in in vivo inhibition of tumor growth and metastasis of murine solid Ehrlich adenocarcinoma. [ABSTRACT FROM AUTHOR]

Management of cancer is challenging due to non-targeting and high side effect issues. Drug repurposing is an innovative method for employing medications for other disease therapy in addition to their original use. Simvastatin, a 3-hydroxy-3-methylglutaryl coenzyme-A reductase inhibitor, is a lipid-lowering drug that is being studied for the treatment of cancer in various in vitro and in vivo models. Nanotechnology offers a potential platform for incorporation of drugs with enhanced pharmaceutical (solubility, release characteristics, stability, etc.) and biological characteristics (targeting, pharmacokinetic, pharmacodynamic). Utilizing a variety of resources such as Scopus, Springer, Web of Science, Elsevier, Bentham Science, Taylor & Francis, and PubMed, a thorough literature search was carried out by looking through electronic records published between 2003 and 2024. The keywords used were simvastatin, drug repurposing, anti-cancer simvastatin, pharmaceutical properties of simvastatin, simvastatin nanoformulations, simvastatin patents, clinical trials, etc. Numerous articles were looked for, filtered, checked out, and incorporated. Pure simvastatin has been researched as a repurposed medication for the treatment of cancer in several in vitro and in vivo models, such as carcinoma of the lung, colon, liver, prostate, breast, and skin. Simvastatin also incorporated into different nanocarriers (nanosuspensions, microparticles/nanoparticles, liposomes, and nanostructured lipid carriers) and showed improvement in solubility, bioavailability, drug loading, release kinetics, and targeting. Clinical trial and patent reports suggest potential of simvastatin in cancer therapy. The preclinical studies of pure simvastatin in in vitro and in vivo models showed the potential for its ability to inhibit cancer cell growth and further incorporation into nanoformulations strengthened its preclinical and pharmaceutical characteristics. [ABSTRACT FROM AUTHOR]

Kombucha is a black tea fermented with sugar using yeasts and Acetobacter species. It indicates that fermented tea cultures vary geographically and can be readily comprehended through various studies on Kombucha cultures. Specifically, the fermentation process of Kombucha requires the symbiotic culture of bacteria and yeast (SCOBY) found in kombucha cultures. It is known for its beneficial qualities and high chemical content. This study aimed to determine the anticancer potential of Kombucha fermented tea against specific human cancer cell lines as well as its antioxidant activity utilizing the DPPH assay. The findings showed that Kombucha has significant antioxidant activity, which is explained by the high phenolic content and other bioactive ingredients created during fermentation. Additionally, the tea demonstrated encouraging anticancer efficacy with a dose-dependent suppression of cell proliferation, especially against cell lines. According to the study, Kombucha has the potential to operate as a natural antioxidant and anticancer agent because of its bioactive components. These results confirm the health benefits of Kombucha and call for more research into its modes of action and therapeutic uses. [ABSTRACT FROM AUTHOR]

The aim of this study was identification and characterization of highly efficient Exopolysaccharide (EPS) producing bacteria in marine sediment soil. To identify specific exopolysaccharide producing bacteria, observations were collected regarding their morphological, physiological, and biochemical characteristics. The findings indicated that Halomonas sp. is the genus to which this bacterium belongs. The following elements were present (carbon, hydrogen, nitrogen and sulfur) in EPS. Further, to confirm the biological potential, the antibacterial Shigella flexneri (MTCC 1457), Proteus mirabilis (MTCC 1429), Escherichia coli (MTCC 43) and Streptococcus pneumoniae (MTCC 655) and MIC properties of exopolysaccharide. MTT assay was used to assess the effect of EPS on growth of Hep G2 (Hepatocellular carcinoma) cell line. These cells were cultured under different concentrations rate of EPS. The inhibitory concentrations (IC50 value) of the tested EPS was found to be 21.188215 µl/ml. Annexin V/PI staining confirmed the apoptosis induced by EPS in Hep G2 cells. [ABSTRACT FROM AUTHOR]