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Copyright of Boletín Latinoamericano y del Caribe de Plantas Medicinales y Aromáticas is the property of Universidad de Santiago de Chile and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Pitaya flower, a medicinal and edible plant commonly used in tropical and subtropical regions, was the focus of this study, which compared the effects of hot-air drying (HAD) and vacuum drying (VD) on phytochemical profiles and biological activities of its four parts: calyx, petals, stamens, and pistils. Both drying methods significantly increased the total phenolic content (TPC) of pitaya flowers, with values ranging from 1.86 to 3.24 times higher than those of fresh samples. Twelve flavonoid compounds were identified in pitaya flowers, with the glycoside derivatives of three flavonols (kaempferol, isorhamnetin, and quercetin) being the most abundant. VD resulted in 1.15 times higher total flavonoid glycoside content than HAD, whereas in petals, HAD yielded a total flavonoid glycoside content 1.21 times higher than VD. Both HAD and VD effectively increased the antioxidant capacities of pitaya flowers, though the difference between the two methods was not significant. Additionally, both drying methods enhanced the antiproliferative activity of pitaya flowers, with HAD showing a more significant effect than VD. The present study emphasized the efficacy of drying methods for enhancing flavonoids in pitaya flowers and provided insights for functional products' innovation with different parts of pitaya flowers. [ABSTRACT FROM AUTHOR]

Cancer remains a formidable global health challenge, with current treatment modalities such as chemotherapy, radiotherapy, surgery, and targeted therapy often hindered by low efficacy and adverse side effects. The indole scaffold, a prominent heterocyclic structure, has emerged as a promising candidate in the fight against cancer. This review consolidates recent advancements in developing natural and synthetic indolyl analogs, highlighting their antiproliferative activities against various cancer types over the past five years. These analogs are categorized based on their efficacy against common cancer types, supported by biochemical assays demonstrating their antiproliferative properties. In this review, emphasis is placed on elucidating the mechanisms of action of these compounds. Given the limitations of conventional cancer therapies, developing targeted therapeutics with enhanced selectivity and reduced side effects remains a critical focus in oncological research. [ABSTRACT FROM AUTHOR]

Given the malignancy of gastric cancer, developing highly effective and low‐toxic targeted drugs is essential to prolong patient survival and improve patient outcomes. In this study, we conducted structural optimizations based on the benzimidazole scaffold. Notably, compound 8 f presented the most potent antiproliferative activity in MGC803 cells and induced cell cycle arrest at the G0/G1 phase. Further mechanistic studies demonstrated that compound 8 f caused the apoptosis of MGC803 cells by elevating intracellular reactive oxygen species (ROS) levels and activating the mitogen‐activated protein kinase (MAPK) signaling pathway, accompanied by corresponding markers change. In vivo investigations additionally validated the inhibitory effect of compound 8 f on tumor growth in xenograft models bearing MGC803 cells without obvious toxicity. Our studies suggest that compound 8 f holds promise as a potential and safe lead compound for developing anti‐gastric cancer agents. [ABSTRACT FROM AUTHOR]

Lung cancer is one of the most common causative cancers worldwide. Particularly, non-small cell lung cancer (NSCLC) accounts for approximately 85% of all lung cancer cases. NSCLC is a serious form of lung cancer that requires prompt diagnosis, and the 5-year survival rate for patients with this disease is only 24%. Gibbosic acid H (GaH), a natural lanostanoid obtained from the Ganoderma species (Ganodermataceae), has antiproliferative activities against colon and lung cancer cells. The aim of the present study was to evaluate the antiproliferative activity of GaH in NSCLC cells and to elucidate the underlying molecular mechanisms. GaH was found to induce G0/G1 cell cycle arrest and autophagy by activating adenosine monophosphate-activated protein kinase in A549 and H1299 cells. The induction of this cell cycle arrest was associated with the downregulation of cyclin E1 and CDK2. Additionally, the induction of autophagy by GaH was correlated with the upregulation of LC3B, beclin-1, and p53 expression. GaH also induced apoptosis by upregulating cleaved caspase-3 and Bax in the lung cancer cells. These findings suggest that GaH has a potential in the growth inhibition of human lung cancer cells.

Tibetan Tea (TT), traditionally esteemed by indigenous communities on the Qinghai-Tibet Plateau for over thirteen centuries, is a post-fermented tea recognized for its wide spectrum of biological functions. These include antioxidant capabilities, hypocholesterolemic effects, anti-hyperglycemic properties, and immune system enhancement. Nevertheless, additional medicinal potentials of TT, including its anticancer effects, remain to be unveiled in empirical studies. We aimed to evaluate the antiproliferative and chemotherapy-enhancing effects of TT extract on human hepatocellular carcinoma (HCC) cells, thereby initiating an inquiry into the potential molecular mechanisms involved. In this study, it was observed that TT extract suppressed the proliferation of HCC cells and triggered significant apoptosis. This apoptotic induction was facilitated through the activation of caspase-3, caspase-8, and caspase-9, along with decreased expression ratio of Bcl-2/Bax protein in HCC cells. Moreover, the combinational treatment of TT extract and Paclitaxel (Taxol) was found to enhance the anticancer effect. The expression level of P-glycoprotein (P-gp) encoded by the MDR1 (Multiple Drug Resistance) gene was remarkably decreased, revealing that TT extract might have the potential to be utilized as an adjuvant to promote HCC treatment. In conclusion, the Tibetan Tea extract exhibits cytotoxic, anticancer, and chemosensitization properties. [ABSTRACT FROM AUTHOR]

Abstract Background Type I interferons (IFN-I)—a group of cytokines with immunomodulatory, antiproliferative, and antiviral properties—are widely used as therapeutics for various cancers and viral diseases. Since IFNs are proteins, they are highly susceptible to degradation by proteases and by hydrolysis in the strong acid environment of the stomach, and they are therefore administered parenterally. In this study, we examined whether the intestinal bacterium, enteropathogenic Escherichia coli (EPEC), can be exploited for oral delivery of IFN-Is. EPEC survives the harsh conditions of the stomach and, upon reaching the small intestine, expresses a type III secretion system (T3SS) that is used to translocate effector proteins across the bacterial envelope into the eukaryotic host cells. Results In this study, we developed an attenuated EPEC strain that cannot colonize the host but can secrete functional human IFNα2 variant through the T3SS. We found that this bacteria-secreted IFN exhibited antiproliferative and antiviral activities similar to commercially available IFN. Conclusion These findings present a potential novel approach for the oral delivery of IFN via secreting bacteria.

Background: Type I interferons (IFN-I)—a group of cytokines with immunomodulatory, antiproliferative, and antiviral properties—are widely used as therapeutics for various cancers and viral diseases. Since IFNs are proteins, they are highly susceptible to degradation by proteases and by hydrolysis in the strong acid environment of the stomach, and they are therefore administered parenterally. In this study, we examined whether the intestinal bacterium, enteropathogenic Escherichia coli (EPEC), can be exploited for oral delivery of IFN-Is. EPEC survives the harsh conditions of the stomach and, upon reaching the small intestine, expresses a type III secretion system (T3SS) that is used to translocate effector proteins across the bacterial envelope into the eukaryotic host cells. Results: In this study, we developed an attenuated EPEC strain that cannot colonize the host but can secrete functional human IFNα2 variant through the T3SS. We found that this bacteria-secreted IFN exhibited antiproliferative and antiviral activities similar to commercially available IFN. Conclusion: These findings present a potential novel approach for the oral delivery of IFN via secreting bacteria. [ABSTRACT FROM AUTHOR]

Excavatolide C (EXCC), a marine coral-derived compound, exhibits an antiproliferation effect on bladder cancer cells. The present study evaluated the improvement in the antiproliferation ability of EXCC by co-treatment with cisplatin in bladder cancer cells. EXCC/cisplatin (12.5 and 1 μg/mL) showed higher antiproliferation effects on bladder cancer cells than single treatments (EXCC or cisplatin alone) in the 48 h ATP assay. EXCC/cisplatin also enhanced the increase in subG1, annexin V-mediated apoptosis, and activation of poly (ADP-ribose) polymerase (PARP) and several caspases (caspases 3, 8, and 9) compared to the single treatments. Cellular and mitochondrial oxidative stress was enhanced with EXCC/cisplatin compared to the single treatments according to analyses of reactive oxygen species (ROS), mitochondrial superoxide, and mitochondrial membrane potential; in addition, cellular antioxidants, such as glutathione (GSH), and the mRNA expressions of antioxidant signaling genes (catalase and NFE2-like bZIP transcription factor 2) were downregulated. EXCC/cisplatin treatment produced more DNA damage than the single treatments, as indicated by γH2AX and 8-hydroxy-2′-deoxyguanosine levels. Moreover, several DNA repair genes for homologous recombination (HR) and non-homologous end joining (NHEJ) were downregulated in EXCC/cisplatin compared to others. The addition of the GSH precursor N-acetylcysteine, which has ROS scavenging activity, attenuated all EXCC/cisplatin-induced changes. Notably, EXCC/cisplatin showed lower antiproliferation, apoptosis, ROS induction, GSH depletion, and γH2AX DNA damage in normal cells than in bladder cancer cells. Therefore, the co-treatment of EXCC/cisplatin reduces the proliferation of bladder cancer cells via oxidative stress-mediated mechanisms with normal cell safety. [ABSTRACT FROM AUTHOR]

A binuclear La(III) complex {[La2(HA)4(H2O)4(C2H5OH)2Cl2]Cl4 (C1)} with 2-aminobenzoic acid (HA) was prepared from the ligand and heptahydrated lanthanum chloride. The complex was characterised by X-ray crystallography that revealed anti-prismatic geometry around both of the lanthanum. In the complex, the four 2-aminobenzoic acid ligands are zwitter ionic and the two lanthanum(III) ions net charge is only counterbalanced by chloride ions. The complex cytotoxicity was determined against human breast (MDA-MB-231), prostate (PC-3) and bladder (T-24) cancer cells. This complex afforded cytotoxicity towards the T-24 bladder cancer cells with an IC50 value of 383.5 µg/mL (319 µM). In contrary, activities by the lanthanum complex with IC50 values of 1124 µg/mL (934 µM) and 739 µg/mL (614 µM) were, respectively, shown against the MDA-MB-231 and PC-3 cancer cells. This means the complex is more cytotoxic against the T-24 cells, despite that its activity is less compared with activities shown by classical drugs. [ABSTRACT FROM AUTHOR]

Curcumin loaded in micelles of block copolymers of ω-methoxypoly(ethylene glycol) and N-(2-hydroxypropyl) methacrylamide modified with aliphatic dilactate (CD) or aromatic benzoyl group (CN) were previously reported to inhibit human ovarian carcinoma (OVCAR-3), human colorectal adenocarcinoma (Caco-2), and human lymphoblastic leukemia (Molt-4) cells. Myeloblastic leukemia cells (K562) are prone to drug resistance and differ in both cancer genotype and phenotype from the three mentioned cancer cells. In the present study, CD and CN micelles were prepared and their effects on K562 and normal cells were explored. The obtained CD and CN showed a narrow size distribution with diameters of 63 ± 3 and 50 ± 1 nm, respectively. The curcumin entrapment efficiency of CD and CN was similarly high, above 80% (84 ± 8% and 91 ± 3%). Both CD and CN showed suppression on WT1-expressing K562 and high cell-cycle arrest at the G2/M phase. However, CD showed significantly higher cytotoxicity to K562, with faster cellular uptake and internalization than CN. In addition, CD showed better compatibility with normal red blood cells and peripheral blood mononuclear cells than CN. The promising CD will be further investigated in rodents and possibly in clinical studies for leukemia treatment. [ABSTRACT FROM AUTHOR]

Despite decades of study, the antiproliferation and molecular processes of the biomolecular elements of honeybee venom (i.e., melittin) as anticancer agents remain largely unclear. This study illustrated the antiproliferation effect of melittin by regulating IL-1ß, COX-2 and TNF-a in human colorectal cancer cells WiDr. In order to assess the antiproliferation, various concentrations of melittin were contacted to the WiDr cell through MTT assay. Moreover, the ability of melittin to regulate the expression of IL-1ß, COX-2 and TNF-a was determined by ELISA. The cytotoxic effect showed the inhibition of the WiDr cell in a dosedependent manner, with the IC10, IC25 and IC50 values of 0.095 ± 0.001, 0.147 ± 0.002 and 0.207 ± 0.004, respectively. Additionally, in further investigations, melittin markedly inhibited the IL-1ß and COX-2 expression but induced the TNF-a, demonstrating significant (p < 0.05) elevations compared to the control group. These findings point to the antiproliferative properties of melittin in WiDr cells. Therefore, as a unique natural treatment for colorectal cancer, melittin may have a lot of potential. [ABSTRACT FROM AUTHOR]

Haberlea rhodopensis Friv., known also as Rhodope silivryak and the Orpheus flower, is a Balkan endemic "resurrecting" plant belonging to the Gesneriaceae family. In folk medicine, the leaves of Haberlea rhodopensis Friv. were widely used to treat wounds and some infectious diseases of stock such as foot-and-mouth disease and hoof rot, while the herb of Haberlea rhodopensis Friv. is still used to cleanse the stomach, liver, kidneys, and blood vessels. Because of the content of myconoside, during the last decade, Haberlea rhodopensis Friv. extracts have been recognized as valuable cosmetic ingredients. In the present study, we aim to (i) evaluate the cytotoxic and antiproliferative activity of two herb extracts of Haberlea rhodopensis Friv. that are commercially used for the preparation of cosmetic ingredients on different cancer cells, with one normal cell line used as a reference, and (ii) compare the investigated effects with those observed for the reference anticancer, non-selective compound doxorubicin. Herein, we observed a decrease in the inhibitory activity of both extracts compared to those of doxorubicin against all tested cell lines. However, the myconoside-enriched Haberlea rhodopensis Friv. plant Extract 2 (designated also as M2) showed increased inhibitory activity (cytotoxicity and antiproliferative effects) compared to the Haberlea rhodopensis Friv. plant Extract 1 (designated also as E1). Moreover, the Haberlea rhodopensis Friv. plant Extract 2 showed a significant increase in cytotoxicity (at 24 h) and antiproliferative activity (at 48 and 72 h post-treatment) at its highest-tested concentration of 100 µg/mL compared to Haberlea rhodopensis Friv. plant Extract 1. [ABSTRACT FROM AUTHOR]

Cherry kernels are a by-product of cherries that are usually discarded, leading to waste and pollution. In this study, the chemical composition of 21 batches of cherry kernels from two different cherry species was analyzed using untargeted metabolomics. The in vitro antioxidant activity, cellular antioxidant activity, and antiproliferative activity of these kernel extracts were also determined, and a correlation analysis was conducted between differential compounds and biological activity. A total of 49 differential compounds were screened. The kernels of Prunus tomentosa were found to have significantly higher total phenol, total flavonoid content, and biological activity than those of Prunus pseudocerasus (P

An effective approach to 5‐triazolyl‐substituted 6,7‐dihydrobenzo[d]isoxazol‐4(5H)‐ones and 4,5,6,7‐tetrahydrobenzo[d]isoxazoles was developed. The approach included α‐keto bromination of 6,7‐dihydrobenzo[d]isoxazol‐4(5H)‐one followed by nucleophilic substitution of bromine with the azide group. For the preparation of 5‐azido‐6,7‐dihydrobenzo[d]isoxazol‐4(5H)‐one, the carbonyl group at position 4 was reduced to a methylene group under ionic hydrogenation conditions using triethylsilane as a reducing agent. Cu(I)‐catalyzed [2+3] cycloaddition of terminal alkynes to both obtained azides was used for the synthesis of two series of triazolyl derivatives. Compounds, which contain in their structures common for some Hsp90 inhibitors 2,4‐dihydroxy‐5‐isopropylphenyl fragment, were evaluated as antiproliferative agents against two breast cancer cell lines: hormone‐dependent MCF7 and HER2‐positive HCC1954. The lead compound showed half‐maximal inhibitory concentration (IC50) values below 5 μM and induced significant changes in the Hsp90 signaling pathways in HER2‐positive HCC1954 cells. It increased the expression of Hsp70 (used as a pharmacodynamic marker of Hsp90 inhibition) and inhibited the expression of HER2, p‐c‐Met, c‐Met, and p‐AKT. The combination of the selected isoxazole‐triazole hybrid molecule and the earlier described apoptosis inducer LCTA‐3344 demonstrated a significant antiproliferative effect against HCC1954 cells. The lead compound was revealed to be a promising candidate for future anticancer drug design, particularly against aggressive breast cancer positive for HER2. [ABSTRACT FROM AUTHOR]

The PEG-coated ferrite nanoparticles Co0.2Mn0.6Zn0.2Fe2O4 (X1), Co0.4Mn0.4Zn0.2Fe2O4 (X2), and Co0.6Mn0.2Zn0.2Fe2O4 (X3) were synthesized by the coprecipitation method. The nanoparticles were characterized by XRD, Raman, VSM, XPS, and TEM. The magnetic hyperthermia efficiency (MH) was determined for PEG-coated nanoparticles using an alternating magnetic field (AMF). X2 nanoparticles displayed the highest saturation magnetization and specific absorption rate (SAR) value of 245.2 W/g for 2 mg/mL in a water medium. Based on these properties, X2 nanoparticles were further evaluated for antiproliferative activity against HCT116 cells at an AMF of 495.25 kHz frequency and 350 G strength, using MTT, colony formation, wound healing assays, and flow cytometry analysis for determining the cell viability, clonogenic property, cell migration ability, and cell death of HCT116 cells upon AMF treatment in HCT116 cells, respectively. We observed a significant inhibition of cell viability (2% for untreated control vs. 50% for AMF), colony-forming ability (530 cells/colony for untreated control vs. 220 cells/colony for AMF), abrogation of cell migration (100% wound closure for untreated control vs. 5% wound closure for AMF), and induction of apoptosis-mediated cell death (7.5% for untreated control vs. 24.7% for AMF) of HCT116 cells with respect to untreated control cells after AMF treatment. Collectively, these results demonstrated that the PEG-coated (CoMnZn-Fe2O4) mixed ferrite nanoparticles upon treatment with AMF induced a significant antiproliferative effect on HCT116 cells compared with the untreated cells, indicating the promising antiproliferative potential of the Co0.4Mn0.4Zn0.2Fe2O4 nanoparticles for targeting colorectal cancer cells. Additionally, these results provide appealing evidence that ferrite-based nanoparticles using MH could act as potential anticancer agents and need further evaluation in preclinical models in future studies against colorectal and other cancers. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Ganoderma, often hailed as a holistic "health package", comprises an array of nutritional components and active compounds, contributing to its esteemed status in the realm of healthy foods. In this study, a comprehensive analysis was performed to elucidate the diverse nutritional profiles, bioactive components, and antiproliferative activities between two Ganoderma species: G. lucidum (GLU) and G. leucocontextum (GLE). The results showed that GLE possessed a higher level of nutritional constituents, except for dietary fiber. Fatty acid analysis revealed comparable profiles rich in unsaturated fatty acids for both species. The ethanol extract of GLU and GLE exhibited potent antioxidant capabilities and remarkable inhibition of tumor cell proliferation via apoptosis induction, with greater potency in GLE. The heightened triterpene levels in GLE potentially contribute to its augmented antitumoral effects. The exploration emphasized the significance of comprehending the varied chemical compositions of Ganoderma species, providing insights into their potential health benefits applications in the food and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

Plants have very important chemical components, known as secondary metabolites, for the pharmaceutical industry, as well as for the chemical, cosmetics, and agricultural control industries. These secondary metabolites isolated from essential oils are used to obtain the raw material or fragrance component of the drug by semi-synthesis. For this reason, plants have been used to treat many diseases in the past, and their active ingredients are still used in medicine today. Each plant, each drug, contains differences owing to their natural structure. However, making the drug obtained from a plant a standard product is important in terms of using it as a medicine in treatment. Therefore, in our study, both the characterization of secondary metabolites and the antioxidant, antimicrobial and antiproliferative potential of Melissa officinalis were investigated. β-Citral (30.900%) was the main component of the essential oil. Total phenolic and flavonoid contents of M. officinalis were found to be 923.33 μg/mL gallic acid equivalent and 1.650 μg/mL quercetin equivalent. The free radical scavenging percentage of M. officinalis was 42.17%. M. officinalis had antimicrobial activity against Enterococcus faecalis, Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, and Candida parapsilosis. In mouse fibroblast cells, the cell viability was found to be 87.50%, 88.235%, and 94.118% respectively, at low doses. In a human breast cancer cell line, it was observed that the cell viability at low concentrations was 77.861%, 85.40%, and 89.474% respectively. The inhibitory concentrations IC50 of M. officinalis calculated for mouse fibroblast and human breast cancer cells in the GraphPad Prism 9.1.1 program were found to be 6229 and 4417 μg/mL respectively. In conclusion, M. officinalis has high bioactive secondary metabolites such as β-citral, β-caryophyllene, 6-methyl-5-hepten-2-one, and cis-1,2-dihydroperillaldehyde, has strong antimicrobial activity, and inhibits viability on breast cancer cells. [ABSTRACT FROM AUTHOR]

Background: Artemisia vulgaris, a medicinal aromatic plant, is widely used as a food item, tonic pharmaceutical, and cosmetic industry additive owing to its antibacterial, antihypertensive, hepatoprotective, antioxidant, and antispasmodic properties. But the effect of different geographic locations on the chemical composition and bioactivities of its extracts is unclear. Methods: Biological activities of essential oils and ethanol extracts of three varieties of Artemisia vulgaris leaves, which are grown in Shanxi province China, were studied. Results: Gas chromatography-mass spectrometry analysis revealed that the main components of essential oils were terpenes and ketones. Essential oils and ethanol extract of Artemisia vulgaris leaves possessed good antioxidant activities, and their half maximal inhibitory concentrations determined using 1,1-diphenyl-2-picrylhydrazyl and 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonate) assays were 57.0 and 22.9 µg/mL, respectively. The essential oils also exhibited remarkable antibacterial activity against three foodborne pathogenic bacterial strains. The ethanol extract presented a high anticancer activity against the MGC-803 human gastric cancer cell line. Conclusion: These biological activities were well correlated with the composition of the extract and EOs, which in turn is affected by the genetic composition of Artemisia vulgaris and geographic location and diverse climatic condition under which it is grown. These findings demonstrate the remarkable potential of Artemisia vulgaris as a valuable source of antioxidant, antibacterial, and anticancer agents. [ABSTRACT FROM AUTHOR]

Pitaya flower, a medicinal and edible plant commonly used in tropical and subtropical regions, was the focus of this study, which compared the effects of hot-air drying (HAD) and vacuum drying (VD) on phytochemical profiles and biological activities of its four parts: calyx, petals, stamens, and pistils. Both drying methods significantly increased the total phenolic content (TPC) of pitaya flowers, with values ranging from 1.86 to 3.24 times higher than those of fresh samples. Twelve flavonoid compounds were identified in pitaya flowers, with the glycoside derivatives of three flavonols (kaempferol, isorhamnetin, and quercetin) being the most abundant. VD resulted in 1.15 times higher total flavonoid glycoside content than HAD, whereas in petals, HAD yielded a total flavonoid glycoside content 1.21 times higher than VD. Both HAD and VD effectively increased the antioxidant capacities of pitaya flowers, though the difference between the two methods was not significant. Additionally, both drying methods enhanced the antiproliferative activity of pitaya flowers, with HAD showing a more significant effect than VD. The present study emphasized the efficacy of drying methods for enhancing flavonoids in pitaya flowers and provided insights for functional products’ innovation with different parts of pitaya flowers.

Cancer remains a formidable global health challenge, with current treatment modalities such as chemotherapy, radiotherapy, surgery, and targeted therapy often hindered by low efficacy and adverse side effects. The indole scaffold, a prominent heterocyclic structure, has emerged as a promising candidate in the fight against cancer. This review consolidates recent advancements in developing natural and synthetic indolyl analogs, highlighting their antiproliferative activities against various cancer types over the past five years. These analogs are categorized based on their efficacy against common cancer types, supported by biochemical assays demonstrating their antiproliferative properties. In this review, emphasis is placed on elucidating the mechanisms of action of these compounds. Given the limitations of conventional cancer therapies, developing targeted therapeutics with enhanced selectivity and reduced side effects remains a critical focus in oncological research.

Background/Aim: Hepatocellular carcinoma (HCC) is a prevalent type of cancer worldwide. Although sorafenib is the only chemotherapy agent used for HCC, there is a need to discover a more potent anticancer agent with reduced side-effects. The compound, (S)-3-(3-fluoro-4-methoxybenzyl)-5,6,7-trimethoxychroman-4-one (FMTC), was designed to inhibit tubulin assembly but its specific mechanisms of action have not been previously investigated. Herein, we investigated the regulation mechanisms by which FMTC affects the proliferation of the HCC cell line, Huh7. Materials and Methods: The effects of FMTC on cell viability and growth were analyzed in the HCC cell line, Huh7. Cell cycle and apoptosis regulated by FMTC were analyzed using flow cytometry. To verify the regulation of mRNA and protein expression of cell proliferation-related factors by FMTC in Huh7 cells, RT-qPCR and western blot analyses were employed. Results: FMTC suppressed cell division dose-dependently by triggering cell cycle arrest at the G2/M phase via p21 up-regulation. The increased phosphorylation of histone H3 on Ser-10 and the condensation of chromatin in FMTC-treated cells indicated mitotic arrest. Prolonged FMTC-induced cell cycle arrest triggered apoptosis. Conclusion: FMTC inhibits the proliferation of human liver cancer cells by up-regulating p21, thereby inducing cell cycle arrest at the G2/M phase. These findings highlight FMTC as a novel agent for HCC treatment. [ABSTRACT FROM AUTHOR]

The δ isoform of class I PI3K (PI3Kδ) has been shown as a promising target for the treatment of hematologic malignancies and immune diseases. Herein, a series of pyrido[3,2‐d]pyrimidine derivatives were designed, synthesized and evaluated for the preliminary bioactivity. Compared with idelalisib, compound S5 exhibited excellent enzyme activity against PI3Kδ (IC50 = 2.82 nM) and strong antiproliferation activity against SU‐DHL‐6 cells (IC50 = 0.035 μM). Besides, S5 inhibited the phosphorylation of Akt, which is downstream of PI3Kδ, in concentration‐dependent manner. In view of the significant improvement in potency of PI3Kδ and selectivity over other PI3K isoforms, Compound S5 deserved further investigation as a promising PI3Kδ inhibitor. [ABSTRACT FROM AUTHOR]

Researchers have become increasingly interested in nanoparticles made from plants because of their stability and large surface area. In the current study, iron oxide and iron dioxide nanoparticles were synthesized using aerial parts of the E. tirucalli as a reducing agent. The nanoparticles were analyzed using various techniques, including Ultraviolet-visible spectroscopy, Fourier Transform Infrared spectroscopy, X-ray diffractometer, X-ray photoelectron spectroscopy, X-ray energy dispersive spectroscopy, Scanning electron Microscopy, and Transmission Electron Microscopy. The nanoparticles were then investigated for their antiproliferative effect against MCF-7, SK-BR-3, MDA-MB231, and Vero cell lines. The results confirmed the formation of FeO and FeO2 nanoparticles by color change and a UV absorbance peak between 220–390 nm. EDS analysis showed traces of Fe and O, while TEM confirmed the nanoparticle size of 100 nm. FTIR showed a peak at 514 nm. The FeO-RT NPs demonstrated over 80% antiproliferative activity against the MCF-7 cell line at a concentration of 10 μg/mL. while doxorubicin, FeO-RT NPs, and DCM extract showed similar activity against the MDA-MB231 cell line at 10 and 1 g/mL concentrations. However, Vero and SK-BR-3 cell lines showed decreased antiproliferative activity. This study highlights the environmentally friendly use and safe application of iron oxide NPs in cancer therapy. [ABSTRACT FROM AUTHOR]

Thiazole and its derivatives have received a lot of attention from researchers due to its wide biological, pharmacological, and anticancer properties. A novel series of 2-[2-[4-Hydroxy-3-substituted benzylidene hydrazinyl]-thiazole-4[5H]-ones (4a–c) and acetoxy derivative (5) were synthesized via using thiosemicarbazones (2a–c). The structure of the thiazole derivatives (4a–c) and 5 in these compounds was confirmed by spectroscopic techniques (IR and NMR), as well as elemental investigations. The synthesized derivatives biological activity was assessed based on their capacity to suppress the growth of the cancer cell lines MCF-7 and HepG2, as well as to halt the cell cycle and trigger apoptosis. Among the synthesized thiazole derivatives, compound 4c was found the most active derivative, with inhibitory concentrations IC50 = 2.57 ± 0.16 and 7.26 ± 0.44 µM in MCF-7 and HepG2, respectively, compared to Staurosporine as the standard drug with IC50 6.77 ± 0.41 and 8.4 ± 0.51 µM, respectively. Additionally, compound 4c blocked vesicular endothelial growth factor receptor-2 (VEGFR-2), according to our results (IC50 = 0.15 µM), compared to Sorafenib (IC50 = 0.059 µM) as the standard drug. Moreover, compound 4c induced cell cycle arrest at the G1/S phase, increasing the percentage and accumulation of cancer cells (DNA content) in the pre-G1 phase by 37.36% in MCF-7 cancer cells compared to untreated MCF-7 cells at 2.02%. Also, compound 4c increased the percentage of early and late apoptosis from 0.51% and 0.29%, respectively, in the case of the MCF-7 untreated control sample to 22.39% and 9.51%, respectively, in the MCF-7 treated sample. Furthermore, molecular docking studies of compounds 4a–c and 5 were conducted with four key proteins (aromatase, epidermal growth factor receptor (EGFR), cyclin-dependent kinase 2 (CDK2), and B-cell lymphoma 2 (Bcl-2)) that stimulate the growth, proliferation, and development of cancer cells. Compound 4c exhibited good docking scores with a promising and potential binding affinity toward the active site of selected docked proteins. According to these results, compound 4c showed efficient cytotoxic activity against the tested cancer cells. [ABSTRACT FROM AUTHOR]

Chinese olives (Canarium album L.) are rich in phenolic compounds, exhibiting a broad spectrum of potential clinical applications. This study is the first report on the isolation and elucidation of bioactive compounds with high anti- proliferative activity from the ethyl acetate fraction of a Chinese olive fruit methanolic extract (CO-EtOAc). We used the WST-1 assay to determine which subfractions of CO-EtOAc had significant antiproliferative activity using the murine colon cancer cell line CT26. Subsequently, the functional compounds were characterized by the hyphenated technique and high-performance liquid chromatography-diode array detector-solid phase extraction-transfer tube-nuclear magnetic resonance (HPLC-DAD-SPE-TT-NMR). Thirteen phenolic constituents were identified from the antiproliferation-enhancing subfractions of CO-EtOAc, including two new compounds, 2,4-didehydrochebulic acid 1,7-dimethyl ester (5) and 1-hydroxybrevifolin (7), which were further purified and found to exhibit marked antiproliferative activity. Chebulic acid dimethyl ester (2), which was isolated from C. album for the first time, also possessed antiproliferative activity. [ABSTRACT FROM AUTHOR]

It is evident that zinc supplementation is essential for maintaining good health and preventing disease. In this study, a novel oyster peptide–zinc complex with an average molecular weight of 500 Da was prepared from oyster meat and purified using ultrafiltration, ultrasound, a programmed cooling procedure, chelating, and dialysis. The optimal chelating process parameters obtained through a response surface methodology optimization design are a peptide/zinc ratio of 15, pH of 6.53, reaction time of 80 min, and peptide concentration of 0.06 g/mL. Then, the structure of a peptide–zinc complex (named COP2-Zn) was investigated using the UV and infrared spectrums. The results showed that the maximum absorption peak was redshifted from 224.5 nm to 228.3 nm and the main difference of the absorption peaks was 1396.4 cm−1. The cytotoxicity and antiproliferative effects of COP2-Zn were evaluated. The results showed that COP2-Zn had a better antiproliferative effect than the unchelated peptide against HepG2 cells. A DNA flow cytometric analysis showed that COP2-Zn induced S-phase arrest in HepG2 cells in a dose-dependent manner. Additionally, the flow cytometer indicated that COP2-Zn significantly induced HepG2 cell apoptosis. [ABSTRACT FROM AUTHOR]

A series of tetrasubstituted pyrimidine derivatives containing methyl phenyl sulfone structure were designed, synthesized and evaluated for antiproliferative activity against four human cancer cell lines of MGC-803, Eca-109, PC-3 and MCF-7 using methyl thiazolyl tetrazolium (MTT) assay. Most of the compounds displayed moderate to excellent antiproliferative activity against the four human tumor cell lines, among which the compound 27g showed the best antiproliferative activity on MGC-803 cells, with IC50 value of (2.98 ± 0.13) μM, which is significantly better than that of the positive control 5-FU. Further studies on the anti-tumor mechanism showed that compound 27g significantly inhibited colony formation and migration of MGC-803 cells, blocked the cell cycle in GO/G1 phase, and induced apoptosis. [ABSTRACT FROM AUTHOR]

In the current study, a series of pyrimidine derivatives containing the 4-hydroxypiperidine group were designed and synthesized, and the antiproliferative activity of these compounds against four human tumor cell lines (MGC-803, PC-3, A549, H1975) was evaluated by MTT method in vitro. Most of the compounds have moderate anti-proliferative activities, among which compound 17i displayed the most excellent anti-proliferative activity, with IC50 value of 3.89 ± 0.57 µM against H1975 cell. Preliminary antitumor mechanism studies revealed that compound 17i could inhibit colony formation and cell migration of H1975 cells. Furthermore, compound 17i induced H1975 cells apoptosis in a dose-dependent manner and H1975 cell cycle arrest in S phase to inhibit cell proliferation. These results indicates that compound 17i could be a promising lead for further studies. [ABSTRACT FROM AUTHOR]

Abundant polyphenols make chokeberry have beneficial antioxidant and antiproliferative activity. In order to explore the contribution of different polyphenols in chokeberry to these activities, this study was conducted to determine polyphenol composition from 7 chokeberry varieties produced in China. Totally, 11 kinds of main polyphenol monomers were identified and quantified by UPLC-Q-TOF-MS and UPLC-PDA. HepG2 cells were used to evaluate their cellular antioxidant and antiproliferative activities. Partial least squares method was utilized to analyze multivariate correlations between proportion of different composition and monomers in total polyphenols with these activities. The results showed that the highest proportion in chokeberry polyphenols was proanthocyanidins. In comparing the bioactivities of 7 varieties of chokeberry, ‘Viking’ and purple chokeberry had the strongest antioxidant activity, while ‘Fukangyuan 1#’ had the strongest antiproliferative activity. In terms of the contribution sources of these bioactivities, the total antioxidant activity of chokeberry mainly depended on the contribution of free polyphenols. As the main source of cellular antioxidant activity, anthocyanins and neochlorogenic acid can provide more contribution. The antiproliferative activity mainly depended on the proportion of free polyphenols and proanthocyanidins in total polyphenols. The results may provide some new possibilities for the comprehensive utilization of polyphenols from chokeberry.

Two cytotoxic sesquiterpene lactones, 17-epichlorohyssopifolin A (1) and chlorjanerin (2), and a monoterpene lactone, loliolide (3) were isolated from Centaurea pseudosinaica. The cytotoxicity of the total extract and terpenoids 1–3 were evaluated against three human cancer cells (HepG2, PC-3, and HT-29), along with the human normal primary epidermal keratinocytes (HEKa) cells. With IC50 values ranging between 0.6 ± 0.04 and 5.0 ± 0.61 μg/mL against HepG2; 0.2 ± 0.01 and 11.9 ± 1.31 μg/mL against PC-3, and 0.04 ± 0.013 and 8.9 ± 0.97 μg/mL against HT-29, the total extract, and lactones 1–3 demonstrated cytotoxic effects. Compound 1 displayed the strongest impact on all cancer cells and a slightly safe effect on the normal cells HEKa. Compound 1 caused accumulation of HepG2 and HT-29 cells in G1 phase as displayed cell cycle analysis. On the other hand, the cell distributions were increased in the S phase in PC-3 cells. Furthermore, 1 caused apoptosis in PC-3 and HePG2 cells with 91.50%, and 79.72 %, respectively. A higher fraction of necrotic cells was observed in HT-29 cells amounting to 23.60%. These results suggested that the promising cytotoxicity exhibited by 1 is brought by the apoptosis induction in the cancer cells, which were evaluated. As the compounds showed antiproliferative effect against the HT-29 cells, the docking simulation was performed aiming at determining how they would interact with the EGFR enzyme, whose PDB: 4I23 is considered one of the two distinct wild types of EGFR enzymes. The antibacterial activity results revealed that 3 showed the most remarkable antibacterial effects, especially against the examined Gram-positive bacteria. The total extract exhibited potent activity against all examined bacteria. The total extract showed a potent antifungal effect against two Candida and two Aspergillus pathogens. The antioxidant activity revealed the potency of the total extract and 3 as antioxidant candidates. The obtained results refer to the importance of Centaurea pseudosinaica as a source of potent antiproliferative agents and the whole plant as an antipathogenic and antioxidant agent.

Abstract Background Seagrasses are unique marine flowering plants. Enhalus acoroides (L.f.) Royle (family Hydrocharitaceae), a new record for the Egyptian coast of the Red Sea, was the grass of choice. A comparative study on Enhalus acoroides (L.f.) Royle (leaves, roots and rhizomes) was done to determine the plant organ that shows the highest antiproliferative and antioxidant activities. The total phenolic content was determined using the Folin–Ciocalteu method. The total flavonoid content was estimated by the aluminum chloride assay. Fourier transform infrared (FT-IR) analysis was performed to detect the chemical functional groups in the extract. High-performance liquid chromatography (HPLC) was done for the qualitative and quantitative evaluation of phenolic compounds. UPLC-ESI-TOF–MS was performed for metabolomics profiling of the extract. Antioxidant activity was determined using the DPPH scavenger percentage method. Antiproliferation assay against hepatocellular carcinoma HepG2, human breast cancer cell lines MCF-7, MDA-MB-231 was performed for the three seagrass organs. Mitochondrial membrane potential (ΔΨm) was measured after treatment with three extracts against MCF-7 cell line. Results The highest phenolic content is found in the leaves, while roots exhibited the highest DPPH scavenger percentage. The total concentration of phenolic compounds detected by HPLC was leaves > rhizomes > roots. Also leaves exhibit the highest antiproliferative activity and mitochondrial membrane potential depletion effect against MCF-7 cell line tested. UPLC-ESI-TOF–MS metabolite profiling of leaves detected different secondary and primary metabolites to which the activity was retained. Leaves are a new candidate to be used in the treatment of cancer. Conclusion Enhalus acoroides (L.f.) Royle leaves extract is a new nutraceutical candidate. Further in-depth studies are required on Enhalus acoroides (L.f.) Royle leaves. Graphical abstract

AbstractResearchers have become increasingly interested in nanoparticles made from plants because of their stability and large surface area. In the current study, iron oxide and iron dioxide nanoparticles were synthesized using aerial parts of the E. tirucalli as a reducing agent. The nanoparticles were analyzed using various techniques, including Ultraviolet-visible spectroscopy, Fourier Transform Infrared spectroscopy, X-ray diffractometer, X-ray photoelectron spectroscopy, X-ray energy dispersive spectroscopy, Scanning electron Microscopy, and Transmission Electron Microscopy. The nanoparticles were then investigated for their antiproliferative effect against MCF-7, SK-BR-3, MDA-MB231, and Vero cell lines. The results confirmed the formation of FeO and FeO2 nanoparticles by color change and a UV absorbance peak between 220–390 nm. EDS analysis showed traces of Fe and O, while TEM confirmed the nanoparticle size of 100 nm. FTIR showed a peak at 514 nm. The FeO-RT NPs demonstrated over 80% antiproliferative activity against the MCF-7 cell line at a concentration of 10 μg/mL. while doxorubicin, FeO-RT NPs, and DCM extract showed similar activity against the MDA-MB231 cell line at 10 and 1 g/mL concentrations. However, Vero and SK-BR-3 cell lines showed decreased antiproliferative activity. This study highlights the environmentally friendly use and safe application of iron oxide NPs in cancer therapy.

In this study, a series of derivatives of thiazolyl-pyrazole hybrid structures were designed to search for new heterocyclic compound-based antitumor agents. The designed target structures were synthesized with easy, practical, and efficient procedures. The antiproliferative effect of the synthesized compounds against cancer cell lines A549, MCF-7, and HepG2 was evaluated regarding inhibition concentration and selectivity index against healthy cell line CCD-34Lu. The results overall showed that the compounds had high antiproliferation against cancer cells compared to the doxorubicin-positive control. In particular, compound 11 A549 (SI: 3.58) and HepG2 (SI: 12.36) had high selectivity in cancer cell lines, while compounds 10h and 10o had high selectivity (SI: 10.74 for both) in MCF-7 cancer cell lines. The calculated theoretical pharmacokinetic properties revealed that they could be suitable drug candidates. In addition, in vitro test results indicate a correlation between the structure-activity relationships of the compounds. The various molecular modifications of thiazolyl-pyrazole hybrid compounds are promising for developing new anticancer drug candidates. [ABSTRACT FROM AUTHOR]

MSN8C, an analog of mansonone E, has been identified as a novel catalytic inhibitor of human DNA topoisomerase II that induces tumor regression and differs from VP-16(etoposide). Treatment with MSN8C showed significant antiproliferative activity against eleven human tumor cell lines in vitro. It was particularly effective against the HL-60/MX2 cell line, which is resistant to Topo II poisons. The resistance factor (RF) of MSN8C for Topo II in HL-60/MX2 versus HL-60 was 1.7, much lower than that of traditional Topo II poisons. Furthermore, in light of its potent antitumor efficacy and low toxicity, as demonstrated in the A549 tumor xenograft model, MSN8C has been identified as a promising candidate for antitumor applications. [ABSTRACT FROM AUTHOR]

Two new oleanane-type triterpene glycosides, phytolasides A (1) and B (2), and six known ones (3–8), were isolated from Phytolacca acinosa fruit fermentation broth. Their structures were elucidated by HR-ESI-MS and 1 D- and 2 D-NMR spectroscopic methods. Antiproliferation of compounds 1 and 2 against HepG2 cells was examined by using CCK8 assays. [ABSTRACT FROM AUTHOR]

Baccaurea motleyana Mull. Arg (Baccaurea) is a tall plant whose fruit is consumed as food in Indonesia. This study aims to evaluate the antioxidant activity of the B. motleyana extracts and their antiproliferative effect on PANC-1 cancer cells. The ethanolic (EBM), ethyl acetate (EABM), and n-hexane (HBM) extracts of B. motleyana leaf were evaluated for their in vitro antiproliferative activity on pancreas cancer (PANC-1) cell lines. Mechanisms of extracts through p53 and Bcl-2 proteins expression using immunocytochemistry. Cell viability assays were performed by calculating the percentage of viable cells and used to determine the IC50 of extracts at 72 h. Spectrophotometrically measuring its antioxidant DPPH and ABTS radical scavenging activities. The phytochemicals profile of extracts was carried out using qualitative tests to identify alkaloids, flavonoids, saponins, triterpenoids/steroids, and tannins. Differences were considered as statistically significant at p<0.05 according to one way ANOVA test followed by Tukey's test. EBM contains more phytochemicals compound than EABM and HBM. The IC50 of EBM, EABM, and HBM were 41.36±1.79 μg/mL, 62.02±2.52 μg/mL, and 124.33±6.04 μg/mL, respectively (DPPH method, p<0.05). In addition, 34.07±2.51 μg/ml, 89.33±4.21 μg/ml, and 202.53±6.81 μg/ml, respectively (ABTS method, p<0.05). The extracts can inhibit the proliferation of PANC-1 cells at 24 h and 72 h. EBM has the strongest IC50 compared to EABM and HBM was 20.75±2.13 μg/mL, 94.63±5.32 μg/mL, and 176±7.10 μg/mL, respectively (p<0.05). Furthermore, EBM could exhibit antiproliferation via modulating the p53 and Bcl-2. EBM, EABM, and HBM have antioxidant and antiproliferative activity against PANC-1 cells. [ABSTRACT FROM AUTHOR]

Non-small cell lung cancer (NSCLC) is one of the leading cancer killers. Apigenin (Api) and Naringenin (Nar) are natural bioactive substances obtained in various vegetables and fruits, possessing anti-tumor effects across multiple studies. This study investigated the latent synergistic antiproliferative functions of Api and Nar in A549 and H1299 NSCLC cells. Cell viability was determined after incubating with different concentrations of Api, Nar, or the combination of Api and Nar (CoAN) for 24 h. Analysis using the CompuSyn software revealed that the CI value of each combined dose was < 1, depicting that the two drugs had a synergistic inhibitory effect. The CoAN (A:N = 3:2) group with the lowest CI value was selected for subsequent experiments. The IC50 of CoAN (A:N = 3:2) was used to determine the cell cycle, the expression ratio of Bax to Bcl2, Caspase 3 activity, and mitochondrial function to assess oxidative stress and apoptosis. The results established that CoAN treatment caused significant cytotoxicity with cell cycle arrest at G2/M phases. Furthermore, CoAN significantly enhanced mitochondria dysfunction, elevated oxidative stress, and activated the apoptotic pathway versus Api or Nar alone groups. Thus, the CoAN chemotherapy approach is promising and deserves further research. [ABSTRACT FROM AUTHOR]

In the present study, new oxalamide-based compounds were designed from thalidomide and synthesized easily and with high yields (from 69% up to 93%) by a two-step method. The antiproliferative effects of synthesized 6a-d and 7a-d compounds on (ER+) MCF-7 and (ER-) MDA-MB-231 breast cancer cell line and human fibroblast WI-38 healthy cell line were investigated by the MTT method. The results showed that compound 7d was the most potent candidate against both MCF-7 and MDA-MB-231 cell lines with IC50 = 4.72 µM and 6.37 µM, respectively. To investigate whether antiproliferative effect of the compounds on breast cancer cell lines is dependent on COXs, expressions of COX-1/2 on the MCF-7 cell line were investigated by the Western-Blot technique. Among synthesized compounds, compound 7d increased the expression of both COX-1 and COX-2. The inhibition potential of compounds on COX-1/2 enzymes was investigated by molecular docking compared to inhibitor co-ligand celecoxib in crystal structures of COX-1 (PDB ID: 3KK6) and COX-2 (PDB ID: 3LN1). Docking results indeed showed that compound 7d had a higher binding affinity for both COX-1 and COX-2 active sites. Consequently, the novel oxalamide-based compounds presented here may be important candidate molecules for the development of new COX-dependent antiproliferative agents. [ABSTRACT FROM AUTHOR]

Carrageenans are polysaccharide constituents of red seaweed cell walls used in food and medicine as well as thickening agents and excipients in cosmetics and skincare products. Carrageenans have antioxidants, anti-inflammatory and pro-apoptotic properties that could potentially cause antiproliferative effects against cancer cells. The primary aim of this study was to assess the antiproliferative effect of iota (ι) and kappa (κ)-carrageenan as well as their combination with α-tocopherol on epidermoid carcinoma (A431NS) cells concerning DNA synthesis and translationally-controlled tumour protein (TPT1) gene expression. Carrageenans exhibited cytotoxic effects against A431NS cells with CD50

Haberlea rhodopensis Friv., known also as Rhodope silivryak and the Orpheus flower, is a Balkan endemic “resurrecting” plant belonging to the Gesneriaceae family. In folk medicine, the leaves of Haberlea rhodopensis Friv. were widely used to treat wounds and some infectious diseases of stock such as foot-and-mouth disease and hoof rot, while the herb of Haberlea rhodopensis Friv. is still used to cleanse the stomach, liver, kidneys, and blood vessels. Because of the content of myconoside, during the last decade, Haberlea rhodopensis Friv. extracts have been recognized as valuable cosmetic ingredients. In the present study, we aim to (i) evaluate the cytotoxic and antiproliferative activity of two herb extracts of Haberlea rhodopensis Friv. that are commercially used for the preparation of cosmetic ingredients on different cancer cells, with one normal cell line used as a reference, and (ii) compare the investigated effects with those observed for the reference anticancer, non-selective compound doxorubicin. Herein, we observed a decrease in the inhibitory activity of both extracts compared to those of doxorubicin against all tested cell lines. However, the myconoside-enriched Haberlea rhodopensis Friv. plant Extract 2 (designated also as M2) showed increased inhibitory activity (cytotoxicity and antiproliferative effects) compared to the Haberlea rhodopensis Friv. plant Extract 1 (designated also as E1). Moreover, the Haberlea rhodopensis Friv. plant Extract 2 showed a significant increase in cytotoxicity (at 24 h) and antiproliferative activity (at 48 and 72 h post-treatment) at its highest-tested concentration of 100 µg/mL compared to Haberlea rhodopensis Friv. plant Extract 1.

Curcumin loaded in micelles of block copolymers of ω-methoxypoly(ethylene glycol) and N-(2-hydroxypropyl) methacrylamide modified with aliphatic dilactate (CD) or aromatic benzoyl group (CN) were previously reported to inhibit human ovarian carcinoma (OVCAR-3), human colorectal adenocarcinoma (Caco-2), and human lymphoblastic leukemia (Molt-4) cells. Myeloblastic leukemia cells (K562) are prone to drug resistance and differ in both cancer genotype and phenotype from the three mentioned cancer cells. In the present study, CD and CN micelles were prepared and their effects on K562 and normal cells were explored. The obtained CD and CN showed a narrow size distribution with diameters of 63 ± 3 and 50 ± 1 nm, respectively. The curcumin entrapment efficiency of CD and CN was similarly high, above 80% (84 ± 8% and 91 ± 3%). Both CD and CN showed suppression on WT1-expressing K562 and high cell-cycle arrest at the G2/M phase. However, CD showed significantly higher cytotoxicity to K562, with faster cellular uptake and internalization than CN. In addition, CD showed better compatibility with normal red blood cells and peripheral blood mononuclear cells than CN. The promising CD will be further investigated in rodents and possibly in clinical studies for leukemia treatment.

The PEG-coated ferrite nanoparticles Co0.2Mn0.6Zn0.2Fe2O4 (X1), Co0.4Mn0.4Zn0.2Fe2O4 (X2), and Co0.6Mn0.2Zn0.2Fe2O4 (X3) were synthesized by the coprecipitation method. The nanoparticles were characterized by XRD, Raman, VSM, XPS, and TEM. The magnetic hyperthermia efficiency (MH) was determined for PEG-coated nanoparticles using an alternating magnetic field (AMF). X2 nanoparticles displayed the highest saturation magnetization and specific absorption rate (SAR) value of 245.2 W/g for 2 mg/mL in a water medium. Based on these properties, X2 nanoparticles were further evaluated for antiproliferative activity against HCT116 cells at an AMF of 495.25 kHz frequency and 350 G strength, using MTT, colony formation, wound healing assays, and flow cytometry analysis for determining the cell viability, clonogenic property, cell migration ability, and cell death of HCT116 cells upon AMF treatment in HCT116 cells, respectively. We observed a significant inhibition of cell viability (2% for untreated control vs. 50% for AMF), colony-forming ability (530 cells/colony for untreated control vs. 220 cells/colony for AMF), abrogation of cell migration (100% wound closure for untreated control vs. 5% wound closure for AMF), and induction of apoptosis-mediated cell death (7.5% for untreated control vs. 24.7% for AMF) of HCT116 cells with respect to untreated control cells after AMF treatment. Collectively, these results demonstrated that the PEG-coated (CoMnZn-Fe2O4) mixed ferrite nanoparticles upon treatment with AMF induced a significant antiproliferative effect on HCT116 cells compared with the untreated cells, indicating the promising antiproliferative potential of the Co0.4Mn0.4Zn0.2Fe2O4 nanoparticles for targeting colorectal cancer cells. Additionally, these results provide appealing evidence that ferrite-based nanoparticles using MH could act as potential anticancer agents and need further evaluation in preclinical models in future studies against colorectal and other cancers.