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Chen Wei-Lun; Ren Yulin; Ren Jinhong; Erxleben Christian; Johnson Michael E.; Gentile Saverio; Kinghorn A. Douglas; Swanson Steven M.; Burdette Joanna E.
... (+)-Strebloside, a cardiac glycoside isolated from the stem bark of Streblus asper collected in Vietnam, has shown some potential for further investigation as an antineoplastic agent. A mechanistic study using an in vitro assay and molecular docking analysis indicated that (+)-strebloside binds and inhibits Na⁺/K⁺-ATPase in a similar manner to digitoxin. Inhibition of growth of different high-grad ...
Paula Priscilla de Freitas; Ruan Carlos Busquet Ribeiro; Isabella dos Santos Guimarães; Caroline S. Moreira; David R. Rocha; Fernando de Carvalho da Silva; Vitor Francisco Ferreira; Etel Rodrigues Pereira Gimba
antineoplastic activity; apoptosis; cell cycle checkpoints; cell viability; cytotoxicity; drug resistance; drug therapy; flow cytometry; metastasis; molecular biology; prostatic neoplasms
Abstract:
... We developed a novel method for the synthesis of bis-naphthoquinones (BNQ), which are hybrids of lawsone (2-hydroxy-1,4-naphthoquinone) and 3-hydroxy-juglone (3,5-dihydroxy-1,4-naphthoquinone). The anticancer activity of three synthesized compounds, named 4 (RC10), 5 (RCDFC), and 6 (RCDOH) was evaluated in vitro against two metastatic prostate cancer (PCa) cell lines, DU145 and PC3, using MTT assa ...
Cryptocarya; DNA damage; alkaloids; antineoplastic activity; bark; cytotoxicity; fractionation; humans; inhibitory concentration 50; mechanism of action; multiple drug resistance; neoplasm cells
Abstract:
... Twelve benzylisoquinoline alkaloids, including pavine and phenanthroindolizidine types, were isolated from a MeOH/CH₂Cl₂ extract of Cryptocarya laevigata (stem bark) through bioactivity-guided fractionation for antitumor effects. Selected compounds were evaluated for antiproliferative activity against five human tumor cell lines, including a multidrug-resistant subline. Since more common 2,3,8,9-t ...
... 1,2,3,4,6-Pentakis[-O-(3,4,5-trihydroxybenzoyl)]-α,β-D-glucopyranose (PGG) 12 has been reported for its antioxidant activities, where the free OH groups in PGG seem to be critical for activities. To explore PGG-based compounds as chemotherapeutic agents and to analyze the contribution of specific OH groups in PGG for anti-cancer activities, we designed and synthesized a series of 27 benzoic and ci ...
... 13-Acetoxysarcocrassolide (13-AC), a marine cytotoxic product isolated from the alcyonacean coral Lobophytum crassum, exhibited potent antitumor and immunostimulant effects as reported in previous studies. However, the 13-AC antitumor mechanism of action against oral cancer cells remains unclear. The activity of 13-AC against Ca9-22 cancer cells was determined using MTT assay, flow cytometric anal ...
... When cultivated under aeroponic growth conditions, Physalis crassifolia produced 11 new withanolides (1–11) and seven known withanolides (12–18) including those obtained from the wild-crafted plant. The structures of the new withanolides were elucidated by the application of spectroscopic techniques, and the known withanolides were identified by comparison of their spectroscopic data with those re ...
... Chemical investigation of the ethyl acetate extract from the endophytic fungus Diaporthe phaseolorum-92C (92C) isolated from the roots of Combretum lanceolatum led to the isolation of 18-des-hydroxy Cytochalasin H (compound 1). The trypanocidal and schistosomicidal activity and cytotoxicity of the extract from 92C were evaluated. The schistosomicidal, leishmanicidal, antimicrobial, and antioxidant ...
... 1‐O‐alkylglycerols (AKG) are a class of natural ether lipids derived from 1‐O‐alkyl‐2,3‐diacyl‐sn‐glycerols by deacylation. In this study, 1‐O‐alkylglycerol (AKG) composition was investigated in the hepatopancreas lipids of the crab Paralithodes camtschaticus and the liver lipids of the squid Berryteuthis magister and the skate Bathyraja parmifera. One of the principal AKG in marine organisms was ...
... Breast cancer is a leading cause of women mortality worldwide. Diverse analogues of 2-benzylidene tetralone have been synthesized and evaluated for anti-cancer activity against a panel of cancer cell lines. Among these, compounds 13, 15 and 19 exhibited potent anti-cancer activity (IC₅₀ = 1–3 μM) against human breast cancer cells, MDA-MB-231 and non-toxic towards non-malignant cell line, HEK-293. ...
Juglans; Western blotting; antineoplastic activity; antineoplastic agents; apoptosis; bark; caspase-3; caspase-9; cell cycle checkpoints; cytotoxicity; dose response; flow cytometry; hepatoma; human cell lines; humans; in vivo studies; interphase; mice; mitochondria; models; neoplasm cells; propidium; proteins; shrinkage; staining
Abstract:
... In order to discover anticancer agents from natural sources, an ethanol-soluble extract of the root bark of Juglans cathayensis was investigated and showed cytotoxic effects against various human cancer cell lines. A subsequent phytochemical study on the EtOAc-soluble fraction determined 2-methoxyjuglone (1) as one of the main active constituents. Compound 1 was shown to be cytotoxic against HepG2 ...
Western blotting; antineoplastic activity; apoptosis; arabinose; caspase-3; cell cycle; chemical reactions; chemical structure; cytotoxicity; flow cytometry; humans; neoplasm cells; organic compounds; xylose
Abstract:
... Tiazofurin analogues bearing a 5-hydroxymethyl-2-methyl-tetrahydrofuro[2,3-d][1,3]dioxol-6-ol moiety as a sugar mimic (2 and 3), and two novel thiazole-based acyclo-C-nucleosides 4 and 16 have been synthesized in multistep sequences starting from d-xylose (compounds 2 and 3) or from d-arabinose (compounds 4 and 16). All synthesized analogues showed potent in vitro antitumour activities against a p ...
... Sesquiterpene lactones having α-methylene-γ-lactone moiety are promising natural metabolites showing various biological activity. One of the major metabolites isolated from Pulicaria undulata, 2α-hydroxyalantolactone (PU-1), has not been investigated in detail yet. Multidrug resistance (MDR) represents a major obstacle for cancer chemotherapy and the capability of novel natural products to overcom ...
Western blotting; antineoplastic activity; apoptosis; breast neoplasms; caspase-3; cell proliferation; cyclins; cytotoxicity; humans; mechanism of action; methylene blue; mitogen-activated protein kinase; neoplasm cells; proliferating cell nuclear antigen; signal transduction
Abstract:
... The mechanisms of action of 2α-hydroxyursolic acid in inhibiting cell proliferation and inducing apoptosis in MDA-MB-231 human breast cancer cells were investigated. The antiproliferative activity and cytotoxicity were determined by the methylene blue assay. The expression of proteins was determined using Western blot. 2α-Hydroxyursolic acid significantly inhibited MDA-MB-231 cell proliferation, a ...
antineoplastic activity; antipyrine; breasts; chemical reactions; chemical structure; colon; colorectal neoplasms; cytotoxicity; humans; liver; liver neoplasms; neoplasm cells; nuclear magnetic resonance spectroscopy; sodium; spectral analysis
Abstract:
... A convenient method for the synthesis of antipyrine, pyrazolopyrimidine and pyrazolopyridine thioglycosides was developed. This study reports a novel and efficient method for the synthesis of thioglycosides of a novel class of 4-aminoantipyrines 6a,b; 13a,b and their corresponding pyrazolopyrimidine thioglycosides 7a,b; 9a,b and pyrazolopyridine thioglycosides 14a,b; 16a,b. These series of compoun ...
... Context: 4-Nerolidylcatechol (4-NRC) has showed antitumor potential through apoptosis. However, its apoptotic mechanisms are still unclear, especially in leukemic cells. Objectives: To evaluate the cytotoxic potential of 4-NRC and its cell death pathways in p53-null K562 leukemic cells. Materials and methods: Cytotoxicity of 4-NRC (4.17–534.5 μM) over 24 h of exposure was evaluated by MTT assay. 4 ...
... 5,6-Dihydroxy-3,7,4′-trimethoxyflavonol (AH5), 5,6,3′-trihydroxy-3,7,4′-trimethoxyflavonol (AH22), artemetin, and oroxylin A are four flavonoids with the same 2-phenyl-chromone skeleton isolated from the Chinese herb Aster himalaicus . The aim of this study was to evaluate the structure–activity relationship of these four analogs and the mediation of AH5 cytotoxicity via G2/M arrest and apoptosis ...
... Different size and morphology monodispersed chitosan (CS) microspheres loaded with the anticancer drug of 5-fluorouracil (5-Fu) were prepared by the microfluidic method assisted by a crosslinking unit with crosslinkers of tripolyphosphate (TPP) and glutaraldehyde (GTA). The sizes, morphologies, drug loading, encapsulation efficiency, drug release and cytotoxicity of 5-Fu loaded CS microspheres wer ...
antineoplastic activity; beta-cyclodextrin; cytotoxicity; energy-dispersive X-ray analysis; ferrimagnetic materials; fluorouracil; magnetic fields; magnetic properties; nanocarriers; nanoparticles; neoplasms; polymers; samarium; spectroscopy
Abstract:
... Drug-loading on magnetic nanoparticles coated with biocompatible polymers are intriguing nanostructures for targeted delivery of anticancer drugs with the application of a magnetic field. In this paper, we report the preparation of SmFeO₃ nanoparticles and loading of the anticancer drug 5-fluorouracil on the carrier by forming host–guest complex with β-cyclodextrin. The material and the polymer ar ...
... Thirty six 5,8-dimethoxy-1,4-naphthoquinone derivatives, which bear unsaturated alkyl side chain with ester bond, were synthesized and tested cytotoxic activity on L1210 cells and antitumor activity against ICR mice bearing S-180 cells. It could be recognized that the cytotoxicities of naphthoquinones with R₁ being methyl and propyl (IV1∼24) were not enhanced by replacing the alkanoyls with alkeno ...
... In the body, alcohol dehydrogenase rapidly converts ethanol to its toxic metabolite, acetaldehyde, which is further metabolized to non-toxic acetic acid by aldehyde dehydrogenase (ALDH). 6-(methylsulfinyl)hexyl isothiocyanate (6-MSITC), a major bioactive compound in Wasabi (Wasabia japonica) has various physiological effects such as anti-oxidative, anti-inflammatory and anti-cancer effects. Howeve ...
Western blotting; anti-inflammatory activity; antineoplastic activity; apoptosis; autophagy; colorectal neoplasms; cytotoxicity; drug therapy; fluorouracil; ginger; glucose; hypoxia; metastasis; neoplasm cells; neoplasm progression; signal transduction; starvation
Abstract:
... BACKGROUND: The development and growth of colorectal cancer based on constitutive activation of numerous signaling pathways that stimulate proliferation and metastasis. Plant-derived agents excel by targeting multiple aspects of tumor progression. Previous investigations have shown that ginger derivatives- shogaols possess anti-cancer and anti-inflammatory effects. In the present study, we have ex ...
... 6‐Gingerol, a potent nutraceutical, has been shown to have antitumor activity in different tumors, although its mechanism of action is not well understood. In this study, we evaluated antitumor activities of 6‐gingerol on human oral (SCC4, KB) and cervical cancer (HeLa) cell lines with or without wortmannin, rapamycin, and cisplatin. Tumor cell proliferation was observed using 3‐(4,5‐dimethylthiaz ...
... To investigate the antitumor effects of 7-O-geranylquercetin (GQ), a novel O-alkylated derivative of quercetin, against non-small cell lung cancer (NSCLC) cell lines A549 and NCI-H1975 and the corresponding mechanisms.Cell viability was assessed using MTT assay. The expression of proteins involved in apoptosis and autophagy was measured using western blotting. Besides, apoptosis was determined wit ...
... Cancer is a diverse class of diseases characterized by uncontrolled cell growth that constitutes the greatest cause of mortality and morbidity worldwide. Despite steady progress, the treatment modalities of cancer are still insufficient. Several new concepts have emerged for therapeutic intervention in malignant diseases with the goal of identifying specific targets and overcoming resistance again ...
... Disulfiram, which exhibits marked tumor inhibition mediated by copper, was encapsulated in lipid nanocapsules modified with TAT peptide (TATp) and pH-triggered sheddable PEG to target cancer cells on the basis of tumor environmental specificity. PEG-shedding lipid nanocapsules (S-LNCs) were fabricated from LNCs by decorating short PEG chains with TATp (HS-PEG₁ₖ–TATp) to form TATp-LNCs and then cov ...
antineoplastic activity; cell lines; chemical reactions; computational methodology; copper; cytotoxicity; mice; models; multiple drug resistance; neoplasms
Abstract:
... A new Cu-based anticancer metallodrug which targets the translocator protein is reported. [CuBr₂(TZ6)] elicits a remarkable in vitro cytotoxicity in sensitive and multidrug resistant cell lines and induces a 98% reduction of tumor mass in a murine tumor model. Target binding was studied by experimental and computational methods. ...
... The combination of photodynamic therapy (PDT) and enzyme therapy is a highly desirable approach in malignant tumor therapies as it takes advantage of the spatial-controlled PDT and the effective enzyme-catalyzed bioreactions. However, it is a challenge to co-encapsulate hydrophilic enzymes and hydrophobic photosensitizers, and these two agents often interfere with each other. In this work, a proto ...
Cercopithecus aethiops; Haliclona; antineoplastic activity; breast neoplasms; carcinoma; cytotoxicity; hepatoma; humans; inhibitory concentration 50; kidneys; metabolites; nuclear magnetic resonance spectroscopy; spectral analysis; stable isotopes; Red Sea
Abstract:
... Three acetylenic brominated derivatives were isolated from a Red Sea sponge, Haliclona sp. One of them, 18-bromooctadeca-9(E),17(E)-dien-7,15-diynoic acid (), is a known metabolite, and the other two are new compounds, (1E,5E,12E,19E)-1,22-dibromodocosa- 1,5,12,19-tetraen-3,14,21-triyne (1) and methyl 18-bromooctadeca-9(E),17(E)-dien-7,15- diynoate (2) which was isolated for the first time as a na ...
... Curcumin is a dominating active component of Curcuma longa and has been studied widely because of its prominent biological activities. The extremely low aqueous solubility, stability, and bioavailability of curcumin limit its application in the field of medicine. In this study, we developed pectin–curcumin (PEC–CCM) conjugates that could self-assemble water-soluble nanomicelles in aqueous solution ...
... To target a response to a high oxidative stress environment of inflammatory or tumor sites, various reactive oxygen species (ROS) sensitive polymers have been developed as drug delivery systems. In this study, a novel oxidation sensitive copolymer, phenylboronic acid pinacol ester-functionalized methoxyl poly(ethylene glycol)-block-poly(phthalic anhydride-alter-glycidyl propargyl ether) (mPEG-b-P( ...
... The development of more efficient photosensitizers with minimal damage to surrounding normal tissues has been a valuable and challenging subject during photodynamic therapy (PDT). Herein, a stimuli-activated porphyrinic photosensitizer (PEG-TPP-DNB; PEG = poly(ethylene glycol); TPP = 5,10,15,20-tetraphenylporphyrin; DNB = 2,4-dinitrobenzene) with capabilities of fluorescence and, remarkably, singl ...
adverse effects; antineoplastic activity; antineoplastic agents; bone resorption; breast neoplasms; catechol; cytotoxicity; dendrimers; ligands; metastasis; models; moieties; nanomedicine; neoplasm cells; pH; peripheral nervous system diseases; pharmacokinetics; polyethylene glycol; proteasome inhibitors
Abstract:
... Bortezomib is a boronate proteasome inhibitor widely used as an efficient anticancer drug; however, the clinical use of bortezomib is hampered by its adverse effects such as hematotoxicity and peripheral neuropathy, and low efficacy on solid tumors due to unfavorable pharmacokinetics and poor penetration in the solid tumors. In this study, we developed a tripeptide Arg–Gly–Asp (RGD)-targeted dendr ...
... Failure of current chemotherapeutic drugs leads to the recurrence of tumor pathology and mortality in lung cancer patients. This study aimed to evaluate the anticancer activity and related mechanisms of 4,5,4′-trihydroxy-3,3′-dimethoxybibenzyl (TDB), a bibenzyl extracted from Dendrobium ellipsophyllum Tang and Wang, in human lung cancer cells. Cytotoxicity of TDB (0–300 µM) in different types of h ...
... In an attempt to improve the therapeutic indices of gemcitabine (GEM), a prodrug was designed by conjugating GEM with a stimuli-responsive dendritic polyHPMA copolymer (dendritic polyHPMA-GEM) and synthesized using the one-pot method of RAFT polymerization. The prodrug with dendritic architectures was able to aggregate and form stable nanoscale systems in the order of 46 nm. The high molecular wei ...
... Rosemary extracts have exhibited potential cytostatic or cytotoxic effects in several cancer cell models but their bioactive compounds are yet to be discovered. In this work, the anticancer activity of a rosemary-leaf extract and its fractions were assayed to identify the phenolic compounds responsible for their antiproliferative/cytotoxic effects on a panel of human colon cancer cell lines. Biogu ...
antineoplastic activity; apoptosis; biocompatible materials; cell cycle; coordination polymers; cytotoxicity; dimensional stability; drug carriers; drug resistance; drug therapy; fluorouracil; human cell lines; metastasis; mice; near infrared radiation; neoplasms; photothermotherapy; polyethylene glycol; thermal stability
Abstract:
... Chemotherapy is a conventional treatment method for metastatic bone cancer, but it has limitations, such as lower drug-targeting of bone tissues and serious side effects. Bone metastasis almost always occurs in advanced cancer, and most patients in this period have strong drug resistance, which further worsens the curative effect. To address the above-mentioned difficulties, a drug delivery platfo ...
DNA damage; DNA replication; adhesion; antineoplastic activity; apoptosis; breast neoplasms; cell adhesion; cell cycle checkpoints; cell proliferation; chalcone; cytotoxicity; drugs; flow cytometry; fluorescence microscopy; hybrids; neoplasm cells; non-specific protein-tyrosine kinase; phosphorylation; relapse; sequence analysis; signal transduction; transactivators; transcriptome
Abstract:
... Although triple-negative breast cancer (TNBC) accounts for only 15% of breast cancer cases, it is associated with a high relapse rate and poor outcome after standard treatment. Currently, the effective drugs and treatment strategies for TNBC remain limited, and thus, developing effective treatments for TNBC is pressing. Several studies have demonstrated that both chalcone and syringaldehyde have a ...
DNA damage; antineoplastic activity; apoptosis; bark; breast neoplasms; caspase-3; cell cycle checkpoints; cytotoxicity; human cell lines; neoplasm cells; phosphotransferases (kinases); procyanidins; research; spectral analysis; tamoxifen
Abstract:
... Albezia odoratissima has many health benefits. The present study investigated the isolation, characterization and anticancer activity of procyanidin C1 from A. odoratissima bark. Procyanidin C1 was isolated and characterized by IR, ¹³C NMR, ¹H NMR and LC-MS spectroscopic studies. Anticancer property of procyanidin C1 was explored by studying the expression of checkpoint kinases, Bcl-2 and BAX, cel ...
... Little is known about anticancer capability of wild-growing mushrooms belonging to Agaricus spp. in comparison with their cultivated counterparts. The present study was done to evaluate in vitro antiproliferative effects of dichloromethane-methanol (1:1, v/v) extracts obtained from several Iranian wild strains of Agaricus spp. in comparison with the cultivated white button mushroom, A. bisporus. T ...
... Angel's trumpet or Brugmanisa suaveolens (B. suaveolens), belonging to the family Solanaceae, distributed in Africa, America, Europe, Australia and Asia, has been used traditionally for the treatment of arthritis, sores, pain, inflammation, ulcers, abscesses, dermatitis, wounds, dysmenorrhea, fungal infections of the skin and as vaginal antiseptic in white secretions. Phytochemical studies of B. s ...
... The cytotoxicity of targeted combinational chemotherapy is significantly more significant than that of other approaches. This study aimed to develop compostable poly(caprolactone)-poly(ethylene glycol)-poly(-caprolactone) (PCECs) nanomaterials (NMs) for the delivery of irinotecan (SN38) and paclitaxel (PTX) to examine the anticancer effect of (PTX@SN38-NMs) against glioma carcinoma cells in vivo a ...
... The escalating demand for secondary metabolites in international markets poses a severe threat to many plant species. An unscrupulous collection is also the immediate challenge to the survival of many unthreatened as well as vulnerable plants. Fungal endophytes have emerged in recent years as a promising substitute for sources of plant secondary metabolites. Many appealing secondary metabolites wi ...
Petiveria alliacea; adenosine triphosphate; antineoplastic activity; breast neoplasms; cell proliferation; cell viability; cytotoxicity; glycolysis; leaf extracts; leukemia; mice; mitochondria; models; neoplasm cells; nutrients; oxidative phosphorylation; oxygen; oxygen consumption; traditional medicine
Abstract:
... Metabolic plasticity in cancer cells assures cell survival and cell proliferation under variable levels of oxygen and nutrients. Therefore, new anticancer treatments endeavor to target such plasticity by modifying main metabolic pathways as glycolysis or oxidative phosphorylation. In American traditional medicine Petiveria alliacea L., Phytolaccacea, leaf extracts have been used for leukemia and b ...
... Epidemiological studies have shown that hepatocellular carcinoma (HCC) is a main cause of tumor death worldwide. Accumulating data indicate that ginsenoside CK is an effective compound for preventing HCC growth and development. However, improvement of pharmaceutical effect of the ginsenoside CK is still needed. In our study, we performed acetylation of ginsenoside CK (CK-3) and investigated the an ...
... Reduction-responsive nano-carriers have been confirmed to be promising for intracellular drug delivery. To develop multifunctional polymer-based drug delivery system, a novel dextran–Pt(iv) conjugate was synthesized by conjugating Pt(iv) to the side chains of the hydrophilic dextran and used for doxorubicin (DOX) delivery. Pt(iv) conjugation could change the hydrophilicity of dextran, leading to t ...
... Graphene nanosheets were prepared by the direct exfoliation of graphite in an aqueous lysozyme solution using ultrasonication. Atomic force microscopy studies indicated that the nanosheets possessed small lateral dimensions of less than three layers. Raman spectroscopy suggested that defects were introduced by the sonication process. These defects were primarily edge defects, not basal-plane defec ...
antineoplastic activity; chemical reactions; chemical structure; cisplatin; cytotoxicity; humans; in vitro studies; lung neoplasms; neoplasm cells; organic compounds; prostatic neoplasms
Abstract:
... A new methodology was developed for the synthesis of hexahydro-1H-pyrido[2,3-b]indol-2-one scaffolds via a sequential Michael addition/amidation/reductive cyclization process. A wide variety of products bearing a hexahydro-1H-pyrido[2,3-b]indol-2-one core with varying degrees of substitution around it, which is a key structural skeleton found in a large number of biologically active natural produc ...
... A facile and efficient methodology was developed for the synthesis of multifunctional polycyclic spiropyrrolidine oxindoles bearing mesityl oxide unit via a three-component 1,3-dipolar cycloaddition reaction of dienones 2 with azomethine ylides (thermally generated in situ from isatin derivatives and proline or thioproline). Products bearing adjacent four chiral carbon centers were smoothly obtain ...
... In situ syntheses and X-ray structures of three novel cationic–anionic complexes: [CoL¹Br][ZnL²L³ZnBr₅] (1), and [CoL¹Cl][ZnL³Br₃] (2) and [CoL¹Cl][ZnL³Cl₃] (3) L¹ = N,N,N-tris(3,5-dimethylpyrazol-1-ylmethyl)amine, L² = hexamethylenetetramine (urotropine), L³ = 3,5-dimethylpyrazole, have been reported. The presence of three different organic ligands (L¹, L² and L³) in isolated complexes results fr ...
... 16-Hydroxy-cleroda-3,13-dien-16,15-olide (HCD) which is extracted from a medicinal plant, Polyalthia longifolia, was shown to exhibit anticancer activity through apoptosis and FAK inhibition in our previous study. To improve its solubility and efficacy, a novel HCD delivery system using copper-substituted mesoporous silica nanoparticles (MSNs) was designed as a delivery vehicle, and the outer surf ...