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1. (+)-Strebloside-Induced Cytotoxicity in Ovarian Cancer Cells Is Mediated through Cardiac Glycoside Signaling Networks

Author:
Chen Wei-Lun; Ren Yulin; Ren Jinhong; Erxleben Christian; Johnson Michael E.; Gentile Saverio; Kinghorn A. Douglas; Swanson Steven M.; Burdette Joanna E.
Source:
Journal of natural products 2017 v.80 no.3 pp. 659-669
ISSN:
1520-6025
Subject:
Streblus asper; adverse effects; anticarcinogenic activity; antineoplastic activity; antineoplastic agents; apoptosis; bark; cytotoxicity; digitoxin; digoxin; humans; in vitro studies; interphase; mitogen-activated protein kinase; molecular models; mutants; neoplasm cells; ouabain; ovarian neoplasms; transcription factor NF-kappa B; Vietnam
Abstract:
... (+)-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 ...
DOI:
10.1021/acs.jnatprod.6b01150
PubMed:
28234008
PubMed Central:
PMC5768141

2. (-)-7(S)-hydroxymatairesinol protects against tumor necrosis factor-α-mediated inflammation response in endothelial cells by blocking the MAPK/NF-κB and activating Nrf2/HO-1

Author:
Di Yang; Chen-Xi Xiao; Zheng-Hua Su; Meng-Wei Huang; Ming Qin; Wei-Jun Wu; Wan-Wan Jia; Yi-Zhun Zhu; Jin-Feng Hu; Xin-Hua Liu
Source:
Phytomedicine 2017 v.32 pp. 15-23
ISSN:
0944-7113
Subject:
Western blotting; anti-inflammatory activity; antineoplastic activity; antioxidants; cardiovascular diseases; drugs; endothelial cells; fluorescent antibody technique; gene expression regulation; heme oxygenase (biliverdin-producing); inducible nitric oxide synthase; inflammation; interleukin-6; lignans; messenger RNA; mitogen-activated protein kinase; necrosis; pathogenesis; phosphorylation; quantitative polymerase chain reaction; reverse transcriptase polymerase chain reaction; signal transduction; superoxide dismutase; transcription factor NF-kappa B; tumor necrosis factor-alpha
Abstract:
... Endothelial inflammation is an increasingly prevalent condition in the pathogenesis of many cardiovascular diseases. (-)-7(S)-hydroxymatairesinol (7-HMR), a naturally occurring plant lignan, possesses both antioxidant and anti-cancer properties and therefore would be a good strategy to suppress tumor necrosis factor-α (TNF-α)-mediated inflammation in vascular endothelial cells (VECs).: The objecti ...
DOI:
10.1016/j.phymed.2017.04.005

3. (3,3’-Methylene)bis-2-hydroxy-1,4-naphthoquinones induce cytotoxicity against DU145 and PC3 cancer cells by inhibiting cell viability and promoting cell cycle arrest

Author:
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
Source:
Molecular biology reports 2021 v.48 no.4 pp. 3253-3263
ISSN:
0301-4851
Subject:
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 ...
DOI:
10.1007/s11033-021-06406-w

4. (Poly-cyanoacrylate) nanomedicines for cancer and beyond: Lessons learned

Author:
P. Couvreur
Source:
Journal of controlled release 2021 v.334 pp. 318-326
ISSN:
0168-3659
Subject:
antineoplastic activity; biodegradability; chemical bonding; drugs; encapsulation; fluorescent dyes; hepatoma; humans; lipids; lysosomes; multiple drug resistance; nanocapsules; nanomedicine; polyacrylamide; squalene; therapeutics
Abstract:
... This « Magnum Opus » emphasizes that serendipity is a corner stone in research. The paths of discovery and innovation often result from the interdisciplinarity of scientific areas that are a priori disconnected from each other. In the 1970s, fundamental discoveries in cell biology led to unexpected advances in galenic pharmacy with the emergence of nanotechnologies for the intracellular delivery o ...
DOI:
10.1016/j.jconrel.2021.04.028

5. (−)-Neocaryachine, an Antiproliferative Pavine Alkaloid from Cryptocarya laevigata, Induces DNA Double-Strand Breaks

Author:
Suzuki Yuki; Saito Yohei; Goto Masuo; Newman David J.; O’Keefe Barry R.; Lee Kuo-Hsiung; Nakagawa-Goto Kyoko
Source:
Journal of natural products 2017 v.80 no.1 pp. 220-224
ISSN:
1520-6025
Subject:
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 ...
DOI:
10.1021/acs.jnatprod.6b01153
PubMed:
28099003
PubMed Central:
PMC5516478

6. (−)-Oleocanthal Combined with Lapatinib Treatment Synergized against HER-2 Positive Breast Cancer In Vitro and In Vivo

Author:
Abu Bakar Siddique; Hassan Y. Ebrahim; Mohamed R. Akl; Nehad M. Ayoub; Amira A. Goda; Mohamed M. Mohyeldin; Suresh K. Nagumalli; Wael M. Hananeh; Yong-Yu Liu; Sharon A. Meyer; Khalid A. El Sayed
Source:
Nutrients 2019 v.11 no.2 pp. -
ISSN:
2072-6643
Subject:
Western blotting; antibodies; antineoplastic activity; breast neoplasms; breasts; cell lines; enzyme inhibitors; epidermal growth factor receptors; epithelium; erbB-2 receptor; extra-virgin olive oil; mice; models; neoplasm cells; non-specific protein-tyrosine kinase; non-specific serine/threonine protein kinase; therapeutics; tyrosine
Abstract:
... Dysregulation of epidermal growth factor receptor (EGFR)/human epidermal growth factor-2 (HER2) family is a hallmark of aggressive breast cancer. Small-molecule tyrosine kinase inhibitors are among the most effective cancer targeted treatments. (−)-Oleocanthal (OC) is a naturally occurring phenolic secoiridoid lead from extra-virgin olive oil with documented anti-cancer activities via target ...
DOI:
10.3390/nu11020412
PubMed:
30781364
PubMed Central:
PMC6412724

7. 1,2,3,4,6-Pentakis[-O-(3,4,5-trihydroxybenzoyl)]-α,β-D-glucopyranose (PGG) analogs: design, synthesis, anti-tumor and anti-oxidant activities

Author:
Qurat-ul-ain Shaikh; Meiting Yang; Khadim Hussain Memon; Mehreen Lateef; Du Na; Shengbiao Wan; Deslandes Eric; Lijuan Zhang; Tao Jiang
Source:
Carbohydrate research 2016 v.430 pp. 72-81
ISSN:
0008-6215
Subject:
antineoplastic activity; antioxidant activity; antioxidants; benzoic acid; cinnamic acid; colon; cytotoxicity; drug therapy; humans; hydrogenation; inhibitory concentration 50; neoplasms
Abstract:
... 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 ...
DOI:
10.1016/j.carres.2016.04.021

8. 1,25-Dihydroxyvitamin D3 suppresses gastric cancer cell growth through VDR- and mutant p53-mediated induction of p21

Author:
Mingxing Li; Longfei Li; Lin Zhang; Wei Hu; Jing Shen; Zhangang Xiao; Xu Wu; Franky Leung Chan; Chi Hin Cho
Source:
Life sciences 2017 pp. -
ISSN:
0024-3205
Subject:
antineoplastic activity; calcitriol; calcitriol receptors; cell cycle checkpoints; cell growth; cyclin-dependent kinase; flow cytometry; humans; mutants; neoplasm cells; precipitin tests; risk; small interfering RNA; staining; stomach; stomach neoplasms; vitamin D deficiency
Abstract:
... Previous studies have indicated that vitamin D deficiency correlates with cancer risk and vitamin D potentiates antitumor effects in a variety of cancers. The antitumor effect of vitamin D on gastric cancer was rarely studied. We aimed to investigate the antitumor effect of vitamin D on gastric cancer and underlying mechanisms.We investigated the antitumor activity of the active form of vitamin D, ...
DOI:
10.1016/j.lfs.2017.04.021

9. 1,25‐Dihydroxyvitamin D3 and its analogues increase catalase at the mRNA, protein and activity level in a canine transitional carcinoma cell line

Author:
R. P. Middleton; R. Nelson; Q. Li; A. Blanton; J. A. Labuda; J. Vitt; N. Inpanbutr
Source:
Veterinary and comparative oncology 2015 v.13 no.4 pp. 452-463
ISSN:
1476-5810
Subject:
bladder; messenger RNA; protein synthesis; catalase; mitogen-activated protein kinase; dogs; reactive oxygen species; antineoplastic activity; superoxide dismutase; gene expression; calcitriol; neoplasm cells; enzyme activity
Abstract:
... Antioxidant enzymes, such as catalase, superoxide dismutases (SOD), MnSOD and Cu/ZnSOD, protect cells by scavenging reactive oxygen species (ROS). Numerous studies have reported the anti‐cancer effects of 1,25‐dihydroxyvitamin D₃ (calcitriol) and its related analogues, seocalcitol and analogue V. In this study, canine bladder transitional cell carcinoma (cbTCC) cells were used to determine effects ...
DOI:
10.1111/vco.12066

10. 1-Butylimidazole-derived ionic liquids: synthesis, characterisation and evaluation of their antibacterial, antifungal and anticancer activities

Author:
Prabodh Ranjan; Bheru Singh Kitawat; Man Singh
Source:
RSC advances 2014 v.4 no.96 pp. 53634-53644
ISSN:
2046-2069
Subject:
Bacillus subtilis; Escherichia coli; Fourier transform infrared spectroscopy; Pseudomonas aeruginosa; Staphylococcus aureus; antifungal properties; antineoplastic activity; carbon; cell growth; cell lines; doxorubicin; ionic liquids; nuclear magnetic resonance spectroscopy; organic halogen compounds; stable isotopes
Abstract:
... A series of new 1-butylimidazole-based ionic liquids (3a–h) have been synthesised by the quaternisation reaction of 1-butylimidazole with different alkyl- and alkoxy-substituted aryl halides using a microwave solvent-free approach with ≈82–95% yield. The solvent-free approach allows the preparation of a variety of ILs with better yields and purities, making any further purification unnecessary. Th ...
DOI:
10.1039/c4ra08370a

11. 13-Acetoxysarcocrassolide Exhibits Cytotoxic Activity against Oral Cancer Cells through the Interruption of the Keap1/Nrf2/p62/SQSTM1 Pathway: The Need to Move Beyond Classical Concepts

Author:
Yi-Chang Liu; Bo-Rong Peng; Kai-Cheng Hsu; Mohamed El-Shazly; Shou-Ping Shih; Tony Eight Lin; Fu-Wen Kuo; Yi-Cheng Chou; Hung-Yu Lin; Mei-Chin Lu
Source:
Marine drugs 2020 v.18 no.8 pp. -
ISSN:
1660-3397
Subject:
DNA; Western blotting; acetylcysteine; animal models; antineoplastic activity; antineoplastic agents; antioxidant enzymes; apoptosis; cell viability; corals; cytotoxicity; enzyme activity; flow cytometry; fluorescent antibody technique; immunostimulants; mechanism of action; membrane potential; mitochondrial membrane; mouth neoplasms; neoplasm cells; precipitin tests; proteins; reactive oxygen species; small interfering RNA; toxicity testing; transfection; xenotransplantation
Abstract:
... 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 ...
DOI:
10.3390/md18080382

12. 1550 nm excitation-responsive upconversion nanoparticles to establish dual-photodynamic therapy against pancreatic tumors

Author:
Khang-Yen Pham; Liu-Chun Wang; Chia-Ching Hsieh; Ya-Ping Hsu; Li-Chan Chang; Wen-Pin Su; Yi-Hsin Chien; Chen-Sheng Yeh
Source:
Journal of materials chemistry B 2021 v.9 no.3 pp. 694-709
ISSN:
2050-7518
Subject:
antineoplastic activity; chemistry; chlorins; irradiation; marriage; nanocarriers; singlet oxygen
Abstract:
... The second near-infrared biological window b (NIR-IIb, 1500–1700 nm) is recently considered as the promising region for deeper tissue penetration. Herein, a nanocarrier for 1550 nm light-responsive dual-photodynamic therapy (PDT) is developed to efficiently boost singlet oxygen (¹O₂) generation. The dual-photosensitizers (PSs), rose bengal (RB) and chlorin e6 (Ce6), are carried by the silica-coate ...
DOI:
10.1039/d0tb02655g

13. 16-Hydroxycleroda-3, 13-dien-15, 16-olide inhibits the proliferation and induces mitochondrial-dependent apoptosis through Akt, mTOR, and MEK-ERK pathways in human renal carcinoma cells

Author:
Cheng Liu; Wei-Chang Lee; Bu-Miin Huang; Yi-Chen Chia; Yu-Chi Chen; Yung-Chia Chen
Source:
Phytomedicine 2017 v.36 pp. 95-107
ISSN:
0944-7113
Subject:
B-cell lymphoma; NAD ADP-ribosyltransferase; Polyalthia longifolia; Western blotting; acridine orange; antineoplastic activity; apoptosis; caspase-3; cell proliferation; cytochrome c; drug therapy; ethidium; fluorescent dyes; heat-shock protein 70; humans; hypoxia; iodides; membrane potential; mitochondria; mitochondrial membrane; mitogen-activated protein kinase; phosphorylation; pro-apoptotic proteins; radiotherapy; reactive oxygen species; renal cell carcinoma; staining
Abstract:
... Renal cell carcinoma (RCC) is well known that it cannot be treated with traditional chemotherapy or radiotherapy. 16-Hydroxycleroda-3,13-dien-15,16-olide (CD), isolated from Polyalthia longifolia Benth. & Hook. f. var. pendula had been reported to display significant efficacy against cancer cell lines.To determine the anti-tumour activities of CD in two clear cell type RCC (ccRCC) cell lines (A-49 ...
DOI:
10.1016/j.phymed.2017.09.021

14. 16-Tigloyl linked barrigenol-like triterpenoid from Semen Aesculi and its anti-tumor activity in vivo and in vitro

Author:
Yiren Yang; Liping Long; Xinxin Zhang; Kairu Song; Da Wang; Xin Xiong; Huiyuan Gao; Luping Sha
Source:
RSC advances 2019 v.9 no.54 pp. 31758-31772
ISSN:
2046-2069
Subject:
antineoplastic activity; apoptosis; breasts; doxorubicin; glycosides; hemolysis; human cell lines; humans; hydrolysates; lungs; metastasis; mice; neoplasm cells; neoplasm progression; toxicity; triterpenoids; uterine cervical neoplasms
Abstract:
... Barrigenol-like triterpenoids (BATs) showed promising anti-tumor, anti-inflammatory and anti-Alzheimer's activities, while, the inhibitory strength was usually affected by their states with aglycones or glycosides. In order to find more BATs as new anti-tumor agents with much more efficiency, the chemical and pharmaceutical studies were carried out on the acid hydrolysate product (AHP) of Semen Ae ...
DOI:
10.1039/c9ra06015d

15. 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells

Author:
Xu Ya-ming; Bunting Daniel P.; Liu Manping X.; Bandaranayake Hema A.; Gunatilaka A. A. Leslie
Source:
Journal of natural products 2016 v.79 no.4 pp. 821-830
ISSN:
1520-6025
Subject:
Physalis; adenocarcinoma; aeroponics; antineoplastic activity; breasts; cytotoxicity; lung neoplasms; neoplasm cells; prostatic neoplasms; spectral analysis; spectroscopy; structure-activity relationships
Abstract:
... 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 ...
DOI:
10.1021/acs.jnatprod.5b00911

16. 17β-estradiol exerts anticancer effects in anoikis-resistant hepatocellular carcinoma cell lines by targeting IL-6/STAT3 signaling

Author:
Seulki Lee; Minjong Lee; Jong Bin Kim; Ara Jo; Eun Ju Cho; Su Jong Yu; Jeong-Hoon Lee; Jung-Hwan Yoon; Yoon Jun Kim
Source:
Biochemical and biophysical research communications 2016 v.473 pp. 1247-1254
ISSN:
0006-291X
Subject:
antineoplastic activity; blood serum; cadherins; cell cycle checkpoints; cell growth; cell proliferation; cisplatin; doxorubicin; drug therapy; estradiol; fluorouracil; gene expression regulation; hepatoma; human cell lines; interleukin-6; metastasis; mitogen-activated protein kinase; neoplasm cells; phosphorylation; protective effect; signal transduction; transactivators; vimentin
Abstract:
... 17β-Estradiol (E2) has been proven to exert protective effects against HCC; however, its mechanism on HCC proliferation and suppression of invasion remains to be further explored.Because HCC up-regulates serum Interleukin-6 (IL-6) levels and Signal Transducer and Activator of Transcription 3 (STAT3), molecular agents that attenuate IL-6/STAT3 signaling can potentially suppress HCC development. In ...
DOI:
10.1016/j.bbrc.2016.04.049

17. 18-Des-hydroxy Cytochalasin: an antiparasitic compound of Diaporthe phaseolorum-92C, an endophytic fungus isolated from Combretum lanceolatum Pohl ex Eichler

Author:
Elson Rudimar Brissow; Igor Pereira da Silva; Kátia Aparecida de Siqueira; Jaqueline Alves Senabio; Leticia Pereira Pimenta; Ana Helena Januário; Lizandra Guidi Magalhães; Ricardo Andrade Furtado; Denise Crispim Tavares; Policarpo Ademar Sales Junior; Jane Lima Santos; Marcos Antônio Soares
Source:
Parasitology research 2017 v.116 no.7 pp. 1823-1830
ISSN:
0932-0113
Subject:
Combretum; Diaporthe; Leishmania; Schistosoma mansoni; Trypanosoma cruzi; adults; amastigotes; antineoplastic activity; antioxidant activity; antiparasitic agents; breast neoplasms; cytotoxicity; endophytes; ethyl acetate; fibroblasts; fungi; humans; inhibitory concentration 50; neoplasm cells; promastigotes; roots; trypomastigotes; viability
Abstract:
... 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 ...
DOI:
10.1007/s00436-017-5451-9

18. 18β-glycyrrhetinic acid inhibits migration and invasion of human gastric cancer cells via the ROS/PKC-α/ERK pathway

Author:
Hongke Cai; Xi Chen; Jianbo Zhang; Jijian Wang
Source:
Natural medicines 2018 v.72 no.1 pp. 252-259
ISSN:
1340-3443
Subject:
antineoplastic activity; bioactive compounds; cadherins; chemoprevention; dose response; humans; licorice; metastasis; mitogen-activated protein kinase; neoplasm cells; phosphorylation; protein kinase C; signal transduction; stomach neoplasms; vimentin
Abstract:
... 18β-glycyrrhetinic acid (18β-GA) is a bioactive component of licorice root which exerts pharmacological activities including anti-inflammatory, antiviral, anti-oxidative and anti-cancer effects. The current study further investigated the molecular mechanisms associated with the inhibitory effects of 18β-GA on tumor metastasis in human gastric cancer cells. The results indicated that 18β-GA signifi ...
DOI:
10.1007/s11418-017-1145-y

19. 1‐O‐alkylglycerols from the hepatopancreas of the crab Paralithodes camtschaticus, liver of the squid Berryteuthis magister, and liver of the skate Bathyraja parmifera, and their anticancer activity on human melanoma cells

Author:
Nikolay A. Latyshev; Svetlana P. Ermakova; Ekaterina V. Ermolenko; Andrey B. Imbs; Sergey P. Kasyanov; Ruslan M. Sultanov
Source:
Journal of food biochemistry 2019 v.43 no.5 pp. e12828
ISSN:
0145-8884
Subject:
Bathyraja; Paralithodes camtschatica; antineoplastic activity; aquatic organisms; crabs; cytotoxicity; hepatopancreas; human cell lines; inhibitory concentration 50; lipids; liver; melanoma; squid; therapeutics
Abstract:
... 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 ...
DOI:
10.1111/jfbc.12828

20. 2,4-Dihydroxy-3′-methoxy-4′-ethoxychalcone suppresses cell proliferation and induces apoptosis of multiple myeloma via the PI3K/akt/mTOR signaling pathway

Author:
FengChen Zhu; DianMing Jiang; MingHua Zhang; Bo Zhao
Source:
Pharmaceutical biology 2019 v.57 no.1 pp. 641-648
ISSN:
1744-5116
Subject:
Caragana; NAD ADP-ribosyltransferase; Western blotting; antineoplastic activity; apoptosis; cell proliferation; cytochrome c; flow cytometry; fluorescence microscopes; in vivo studies; inhibitory concentration 50; insulin-like growth factor I; myeloma; phosphatidylinositol 3-kinase; rapamycin; signal transduction; traditional medicine
Abstract:
... Context: Caragana pruinosa Kom. (Fabaceae), a commonly used folk medicine, has been found to possess antitumor effects. However, the antiproliferative effect of 2,4-dihydroxy-3′-methoxy-4′-ethoxychalcone (DMEC) derived from C. pruinosa against multiple myeloma (MM) has never been investigated. Objective: This study systematically evaluates the antiproliferative effect of DMEC against MM cells. Mat ...
DOI:
10.1080/13880209.2019.1662814
PubMed:
31564190
PubMed Central:
PMC6781472

21. 2-(3′,4′-Dimethoxybenzylidene)tetralone induces anti-breast cancer activity through microtubule stabilization and activation of reactive oxygen species

Author:
Yashveer Gautam; Sonam Dwivedi; Ankita Srivastava; Hamidullah; Arjun Singh; D. Chanda; Jyotsna Singh; Smita Rai; Rituraj Konwar; Arvind S. Negi
Source:
RSC advances 2016 v.6 no.40 pp. 33369-33379
ISSN:
2046-2069
Subject:
acetylcysteine; acute oral toxicity; adverse effects; antineoplastic activity; apoptosis; breast neoplasms; cell lines; cytotoxicity; inhibitory concentration 50; interphase; mammary neoplasms (animal); microtubules; mitosis; models; mortality; neoplasm cells; polymerization; rats; reactive oxygen species; tubulin; women
Abstract:
... 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. ...
DOI:
10.1039/c6ra02663j

22. 2-Ethoxystypandrone, a novel small-molecule STAT3 signaling inhibitor from Polygonum cuspidatum, inhibits cell growth and induces apoptosis of HCC cells and HCC Cancer stem cells

Author:
Wuguo Li; Qing Zhang; Kaotan Chen; Zhenhua Sima; Jingli Liu; Qiang Yu; Jiawei Liu
Source:
BMC complementary and alternative medicine 2019 v.19 no.1 pp. 38
ISSN:
1472-6882
Subject:
Reynoutria japonica; Western blotting; alternative medicine; antineoplastic activity; antineoplastic agents; apoptosis; cell cycle; cell growth; cell viability; chemical structure; dose response; drug resistance; ethyl acetate; flow cytometry; gels; hepatoma; high performance liquid chromatography; humans; inhibitory concentration 50; juglone; luciferase; metastasis; nuclear magnetic resonance spectroscopy; oncogenes; phosphorylation; physicochemical properties; relapse; reporter genes; roots; signal transduction; spectral analysis; stem cells; transactivators; transcription (genetics); tyrosine
Abstract:
... BACKGROUND: Signal transducer and activator of transcription 3 (STAT3) is an oncogene constitutively activated in hepatocellular carcinoma (HCC) cells and HCC cancer stem cells (CSCs). Constitutively activated STAT3 plays a pivotal role in holding cancer stemness of HCC CSCs, which are essential for hepatoma initiation, relapse, metastasis and drug resistance. Therefore, STAT3 has been validated a ...
DOI:
10.1186/s12906-019-2440-9
PubMed:
30709346
PubMed Central:
PMC6359800

23. 2-Methoxyjuglone Induces Apoptosis in HepG2 Human Hepatocellular Carcinoma Cells and Exhibits in Vivo Antitumor Activity in a H22 Mouse Hepatocellular Carcinoma Model

Author:
Yu Heng-Yi; Zhang Xiao-Qiong; Li Xue-; Zeng Fan-Bo; Ruan Han-Li
Source:
Journal of natural products 2013 v.76 no.5 pp. 889-895
ISSN:
1520-6025
Subject:
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 ...
DOI:
10.1021/np400025b

24. 2-Methylpyridine-1-ium-1-sulfonate as an Inducer of Apoptosis and Cell Cycle Arrest: A comparative in vitro and Computational Study

Author:
Hamid-Reza Mohammadi-Motlagh; Reza Yarani; Mona Sadeghalvad; Elham Adham; Hassan Rasouli; Ali Mostafaie
Source:
Nutrition and cancer 2019 v.71 no.4 pp. 643-656
ISSN:
1532-7914
Subject:
Allium; DNA fragmentation; antineoplastic activity; apoptosis; bulbs; cell cycle checkpoints; computer simulation; cyclins; dose response; gastrointestinal neoplasms; human cell lines; mechanism of action; medicinal plants; medicine; neoplasm cells; phosphotransferases (kinases)
Abstract:
... “Let food be thy medicine and thy medicine be thy food” was expressed by Hippocrates and the health benefits of medicinal plants and natural products have been considered by humans since historic times. The current study aims to investigate the anti-cancer activity of 2-Methylpyridine-1-ium-1-sulfonate (MPS) isolated from bulbs of Allium hirtifolium. The MPS compound (in a dose-dependent manner) i ...
DOI:
10.1080/01635581.2018.1506495

25. 2-Substituted thiazole-4-carboxamide derivatives as tiazofurin mimics: synthesis and in vitro antitumour activity

Author:
Mirjana Popsavin; Vesna Kojić; Saša Spaić; Miloš Svirčev; Gordana Bogdanović; Dimitar Jakimov; Lidija Aleksić; Velimir Popsavin
Source:
Tetrahedron 2014 v.70 pp. 2343-2350
ISSN:
0040-4020
Subject:
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 ...
DOI:
10.1016/j.tet.2014.02.035

26. 2-fluoro-RNA oligonucleotide CD40 targeted aptamers for the control of B lymphoma and bone-marrow aplasia

Author:
Mario Martinez Soldevilla; Helena Villanueva; Maurizio Bendandi; Susana Inoges; Ascensión López-Díaz de Cerio; Fernando Pastor
Source:
Biomaterials 2015 v.67 pp. 274-285
ISSN:
0142-9612
Subject:
B-lymphocytes; abnormal development; agonists; antagonists; antibodies; antineoplastic activity; bone marrow; drug therapy; drugs; immunosuppression; immunotherapy; lymphoma; messenger RNA; neoplasm cells; oligonucleotides; patients; radiotherapy
Abstract:
... Recent studies have underscored the importance of immunomodulatory antibodies in the treatment of solid and hematological tumors. ODN-Aptamers are rising as a novel class of drugs that can rival therapeutic antibodies. The success of some of the current cancer immunotherapy approaches in oncological patients depends on the intrinsic antigenicity of each tumor as has recently been disclosed, and it ...
DOI:
10.1016/j.biomaterials.2015.07.020

27. 20 (S)-ginsenoside Rh2 inhibits colorectal cancer cell growth by suppressing the Axl signaling pathway in vitro and in vivo

Author:
Haibo Zhang; Jun-Koo Yi; Hai Huang; Sijun Park; Wookbong Kwon; Eungyung Kim; Soyoung Jang; Si-Yong Kim; Seong-kyoon Choi; Duhak Yoon; Sung-Hyun Kim; Kangdong Liu; Zigang Dong; Zae Young Ryoo; Myoung Ok Kim
Source:
Journal of Ginseng Research 2022 v.46 no.3 pp. 396-407
ISSN:
1226-8453
Subject:
Panax; Western blotting; antineoplastic activity; apoptosis; cell cycle checkpoints; cell growth; colorectal neoplasms; morbidity; mortality; neoplasm cells; research; toxicity; transfection; xenotransplantation
Abstract:
... Colorectal cancer (CRC) has a high morbidity and mortality worldwide. 20 (S)-ginsenoside Rh2 (G-Rh2) is a natural compound extracted from ginseng, which exhibits anticancer effects in many cancer types. In this study, we demonstrated the effect and underlying molecular mechanism of G-Rh2 in CRC cells in vitro and in vivo. Cell proliferation, migration, invasion, apoptosis, cell cycle, and western ...
DOI:
10.1016/j.jgr.2021.07.004

28. 20(S)-Ginsenoside Rh2 displays efficacy against T-cell acute lymphoblastic leukemia through the PI3K/Akt/mTOR signal pathway

Author:
Ting Xia; Jin Zhang; Chuanxin Zhou; Yu Li; Wenhui Duan; Bo Zhang; Min Wang; Jianpei Fang
Source:
Journal of Ginseng Research 2020 v.44 no.5 pp. 725-737
ISSN:
1226-8453
Subject:
Panax; T-lymphocytes; active ingredients; antineoplastic activity; apoptosis; autophagy; cell growth; cell proliferation; immunoblotting; interphase; lymphocytic leukemia; prognosis; reactive oxygen species; research; signal transduction; spleen; xenotransplantation
Abstract:
... T-cell acute lymphoblastic leukemia (T-ALL) is a kind of aggressive hematological cancer, and the PI3K/Akt/mTOR signaling pathway is activated in most patients with T-ALL and responsible for poor prognosis. 20(S)-Ginsenoside Rh2 (20(S)-GRh2) is a major active compound extracted from ginseng, which exhibits anti-cancer effects. However, the underlying anticancer mechanisms of 20(S)-GRh2 targeting t ...
DOI:
10.1016/j.jgr.2019.07.003

29. 2D-QSAR and docking study of a series of coumarin derivatives as inhibitors of CDK (anticancer activity) with an application of the molecular docking method

Author:
Rania Kasmi; Elghalia Hadaji; Oussama Chedadi; Abdellah El Aissouq; Mohammed Bouachrine; Abdelkrim Ouammou
Source:
Heliyon 2020 v.6 no.8 pp. e04514
ISSN:
2405-8440
Subject:
antineoplastic activity; cell lines; computer software; coumarin; drug design; drugs; hydrogen bonding; models; quantitative structure-activity relationships; regression analysis; synthesis
Abstract:
... Quantitative Structure Activity Relationship (QSAR) analysis techniques are tools largely utilized in many research fields, including drug discovery processes.In this work electronic descriptors are calculated with the Gaussian 03W software using the DFT method with the BecKe 3-parameters exchange functional and Lee-Yang-Parr correlation functional, with Kohn and Sham orbitals (KS) developed on a ...
DOI:
10.1016/j.heliyon.2020.e04514

30. 2α-Hydroxyalantolactone from Pulicaria undulata: activity against multidrug-resistant tumor cells and modes of action

Author:
Mohamed-Elamir F. Hegazy; Mona Dawood; Nuha Mahmoud; Mohamed Elbadawi; Yoshikazu Sugimoto; Sabine M. Klauck; Nagla Mohamed; Thomas Efferth
Source:
Phytomedicine 2021 v.81 pp. 153409
ISSN:
0944-7113
Subject:
DNA damage; P-glycoproteins; Pulicaria undulata; antineoplastic activity; apoptosis; cell cycle checkpoints; cytotoxicity; epidermal growth factor receptors; gene expression regulation; gene overexpression; human cell lines; leukemia; mechanism of action; medicinal plants; messenger RNA; microarray technology; multiple drug resistance; neoplasm cells; phosphatidylinositol 3-kinase; sesquiterpenoid lactones; transcriptome; transcriptomics
Abstract:
... 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 ...
DOI:
10.1016/j.phymed.2020.153409

31. 2α-Hydroxyursolic Acid Inhibited Cell Proliferation and Induced Apoptosis in MDA-MB-231 Human Breast Cancer Cells through the p38/MAPK Signal Transduction Pathway

Author:
Xue Jiang; Tong Li; Rui Hai Liu
Source:
Journal of agricultural and food chemistry 2016 v.64 no.8 pp. 1806-1816
ISSN:
0021-8561
Subject:
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 ...
DOI:
10.1021/acs.jafc.5b04852

32. 2′-Aminoanalogues of the cruciferous phytoalexins spirobrassinin, 1-methoxyspirobrassinin and 1-methoxyspirobrassinol methyl ether: Synthesis and anticancer properties

Author:
Mariana Budovská; Viera Tischlerová; Ján Mojžiš; Marianna Harvanová; Oleksandr Kozlov; Taťána Gondová; Nataša Tomášková
Source:
Tetrahedron 2017 pp. -
ISSN:
0040-4020
Subject:
aniline; antineoplastic activity; chemical reactions; enantiomers; high performance liquid chromatography; humans; neoplasms; nuclear magnetic resonance spectroscopy; phytoalexins; solvents
Abstract:
... A method for the synthesis of new 2′-aminoanalogues of spiroindoline phytoalexins is reported. 2′-Aminonalogues of spirobrassinin, 1-methoxyspirobrassinin and 2,2′-diamino analogues of 1-methoxyspirobrassinol methyl ether were prepared by substitution of the methylsulphanyl group on the dihydrothiazole ring of corresponding phytoalexins. Final products were obtained by heating the phytoalexins wit ...
DOI:
10.1016/j.tet.2017.09.033

33. 2′-Hydroxyflavanone induced changes in the proteomic profile of breast cancer cells

Author:
Lokesh D. Nagaprashantha; Jyotsana Singhal; Shireen Chikara; Gabriel Gugiu; David Horne; Sanjay Awasthi; Ravi Salgia; Sharad S. Singhal
Source:
Journal of proteomics 2019 v.192 pp. 233-245
ISSN:
1874-3919
Subject:
antineoplastic activity; antineoplastic agents; breast neoplasms; breasts; citrus fruits; epithelial cells; flavonoids; metastasis; neoplasm cells; proteins; proteomics; therapeutics; women
Abstract:
... In spite of rapid advances in understanding of signaling networks associated with the incidence and therapeutic-sensitivity, breast cancer (BC) still remains the most commonly diagnosed and prevalent cancer in women. Emergence of resistance to hormonal interventions in estrogen-receptor (ER) positive BC coupled to loss of ER expression and activation of ER-independent growth factor, heat-shock, MY ...
DOI:
10.1016/j.jprot.2018.09.005

34. 3,5,7-Trimethoxyphenanthrene-1,4-dione: a new biologically relevant natural phenanthrenequinone derivative from Dioscorea prazeri and studies on its single X-ray crystallographic behavior, molecular docking and other physico-chemical properties

Author:
Goutam Brahmachari; Saktipada Das; Maya Biswas (Sinha); Abhishek Kumar; Ambrish Kumar Srivastava; Neeraj Misra
Source:
RSC advances 2016 v.6 no.9 pp. 7317-7329
ISSN:
2046-2069
Subject:
Dioscorea; X-radiation; X-ray diffraction; ambient temperature; antineoplastic activity; computer simulation; crystal structure; crystallization; data collection; geometry; least squares; physicochemical properties; prediction; quinones; spectral analysis; yams
Abstract:
... A naturally occurring new phenanthrenequinone derivative has been isolated from the yams of Dioscorea prazeri Prain and Burkil (Dioscoreaceae) and identified as 3,5,7-trimethoxyphenanthrene-1,4-dione (1) on the basis of its detailed spectral and single crystal X-ray analyses. The compound crystallizes in the triclinic space group P1̄ with the following unit-cell parameters: a = 7.7045(3), b = 8.50 ...
DOI:
10.1039/c5ra21490d

35. 3-Bromopyruvate and sodium citrate induce apoptosis in human gastric cancer cell line MGC-803 by inhibiting glycolysis and promoting mitochondria-regulated apoptosis pathway

Author:
Xingyu Guo; Xiaodong Zhang; Tingan Wang; Shulin Xian; Yunfei Lu
Source:
Biochemical and biophysical research communications 2016 v.475 pp. 37-43
ISSN:
0006-291X
Subject:
adenosine triphosphate; antineoplastic activity; apoptosis; caspase-3; cell growth; cytochrome c; glycolysis; hexokinase; humans; lactic acid; neoplasm cells; phosphofructokinases; pro-apoptotic proteins; sodium citrate; stomach neoplasms; viability
Abstract:
... Cancer cells are mainly dependent on glycolysis to generate adenosine triphosphate (ATP) and intermediates required for cell growth and proliferation. Thus, inhibition of glycolysis might be of therapeutic value in antitumor treatment. Our previously studies had found that both 3-bromopyruvate (BP) and sodium citrate (SCT) can inhibit tumor growth and proliferation in vitro and in vivo. However, t ...
DOI:
10.1016/j.bbrc.2016.04.151

36. 3-Formylchromone Counteracts STAT3 Signaling Pathway by Elevating SHP-2 Expression in Hepatocellular Carcinoma

Author:
Chakrabhavi Dhananjaya Mohan; Min Hee Yang; Shobith Rangappa; Arunachalam Chinnathambi; Sulaiman Ali Alharbi; Tahani Awad Alahmadi; Amudha Deivasigamani; Kam Man Hui; Gautam Sethi; Kanchugarakoppal S. Rangappa; Kwang Seok Ahn
Source:
Biology 2021 v.11 no.1 pp. -
ISSN:
2079-7737
Subject:
antineoplastic activity; cell movement; hepatoma; humans; lungs; metastasis; mice; phosphorylation; signal transduction; toxicity; transactivators; transportation; tyrosine
Abstract:
... Hepatocellular carcinoma (HCC) is one of the leading cancers that contribute to a large number of deaths throughout the globe. The signal transducer and activator of transcription 3 (STAT3) is a tumorigenic protein that is overactivated in several human malignancies including HCC. In the present report, the effect of 3-formylchromone (3FC) on the STAT3 signaling pathway in the HCC model was invest ...
DOI:
10.3390/biology11010029

37. 3-Hydroxyflavanone induces apoptosis in HeLa cells

Author:
Soon Young Shin; Young Han Lee
Source:
Han'guk Ŭngyong Saengmyŏng Hwahakhoe chi = 2013 v.56 no.1 pp. 113-116
ISSN:
1738-2203
Subject:
NAD ADP-ribosyltransferase; antineoplastic activity; apoptosis; cell cycle; cell proliferation; cyclins; flavonoids; flow cytometry; uterine cervical neoplasms
Abstract:
... Flavonoids and their derivatives exhibit many biological properties, including anti-inflammatory and antitumor activities. However, the antitumor action of 3′-hydroxyflavanone (3′-HF) is largely unknown. Antitumor efficacy of 3′-HF was assessed using cervical cancer (HeLa) cells. 3′-HF treatment resulted in a reduction in cell proliferation. A flow cytometric analysis demonstrated that 3′-HF dereg ...
DOI:
10.1007/s13765-012-2234-y

38. 3-Methyl-4-nitro-5-isatylidenyl-isoxazoles as 1,3-dipolarophiles for synthesis of polycyclic 3,3′-pyrrolidinyl-dispirooxindoles and their biological evaluation for anticancer activities

Author:
Bing Lin; Wen-Hui Zhang; Dan-Dan Wang; Yi Gong; Qi-Di Wei; Xiong-Li Liu; Ting-Ting Feng; Ying Zhou; Wei-Cheng Yuan
Source:
Tetrahedron 2017 pp. -
ISSN:
0040-4020
Subject:
antineoplastic activity; chemical elements; chemical reactions; chemical structure; organic compounds; proline
Abstract:
... Developed herein is a diversity-oriented one-pot multicomponent synthesis of polycyclic 3,3′- pyrrolidinyl-dispirooxindoles 3via a multicomponent 1,3-dipolar cycloaddition event of 3-methyl-4-nitro-5-isatylidenyl-isoxazoles 2 with azomethine ylides (thermally generated in situ from isatins and proline or thioproline). Products bearing four consecutive stereocenters consist of two oxindole moieties ...
DOI:
10.1016/j.tet.2017.07.011

39. 3-Nitroacridine derivatives arrest cell cycle at G0/G1 phase and induce apoptosis in human breast cancer cells may act as DNA-target anticancer agents

Author:
Qian Zhou; Chaoqun You; Cong Zheng; Yawen Gu; Hongchao Gu; Rui Zhang; Hongshuai Wu; Baiwang Sun
Source:
Life sciences 2018 v.206 pp. 1-9
ISSN:
0024-3205
Subject:
DNA; DNA damage; adverse effects; antineoplastic activity; antineoplastic agents; apoptosis; bacteriophages; binding capacity; bioavailability; breast neoplasms; cell cycle checkpoints; cell growth; cell proliferation; circular dichroism spectroscopy; dose response; enzyme inhibition; fluorescence microscopes; growth retardation; humans; interphase; mechanism of action; neoplasm cells; therapeutics; ultraviolet-visible spectroscopy
Abstract:
... DNA is considered to be one of the most promising targets for anticancer agents. Acridine analogues have anticancer activity based on DNA binding and topoisomerases inhibition. However, due to the side effects, resistance and low bioavailability, a few have entered into clinical usage and the mechanisms of action are not fully understood. Novel acridine derivatives are needed for effective cancer ...
DOI:
10.1016/j.lfs.2018.05.010

40. 3-O-Methylquercetin from organic Nicotiana tabacum L. trichomes: Influence of the variety, cultivation and extraction parameters

Author:
Liege C. Schwingel; Geraldo O. Schwingel; Nirlei Storch; Fabiano Barreto; Valquiria L. Bassani
Source:
Industrial crops and products 2014 v.55 pp. 56-62
ISSN:
0926-6690
Subject:
Nicotiana tabacum; antineoplastic activity; antioxidants; byproducts; chromatography; ethanol; flavonoids; leaves; tobacco use; toxicity; trichomes
Abstract:
... The 3-O-methylquercetin (3-MQ) is a flavonoid aglycone with important antioxidant, antiviral, and anticancer properties. The presence of 3-MQ in Nicotiana tabacum L. trichomes is well known as the species’ response to environmental stress factors. Although 3-MQ has been synthesized, its yield has been low and toxic by-products are formed that are difficult to separate. The present work reports the ...
DOI:
10.1016/j.indcrop.2014.01.054

41. 3D cellular spheroids as tools for understanding carboxylated quantum dot behavior in tumors

Author:
Greta Jarockyte; Dominyka Dapkute; Vitalijus Karabanovas; Justinas V. Daugmaudis; Feliksas Ivanauskas; Ricardas Rotomskis
Source:
Biochimica et biophysica acta 2018 v.1862 pp. 914-923
ISSN:
0304-4165
Subject:
adverse effects; antineoplastic activity; carboxylation; cell culture; humans; in vivo studies; mathematical models; mice; nanomedicine; nanoparticles; neoplasms; phenotype; quantum dots; tissues; zinc sulfide
Abstract:
... Monolayer cell cultures have been considered the most suitable technique for in vivo cellular experiments. However, a lot of cellular functions and responses that are present in natural tissues are lost in two-dimensional cell cultures. In this context, nanoparticle accumulation data presented in literature are often not accurate enough to predict behavior of nanoparticles in vivo. Cellular sphero ...
DOI:
10.1016/j.bbagen.2017.12.014

42. 3D printed tablets containing oxaliplatin loaded alginate nanoparticles for colon cancer targeted delivery. An in vitro/in vivo study

Author:
Seyedeh Zahra Mirdamadian; Jaleh Varshosaz; Mohsen Minaiyan; Azade Taheri
Source:
International journal of biological macromolecules 2022 v.205 pp. 90-109
ISSN:
0141-8130
Subject:
alginates; antineoplastic activity; cancer therapy; colorectal neoplasms; drugs; extrusion; intestines; intravenous injection; oral administration; printers; stomach; three-dimensional printing
Abstract:
... This study aimed to develop a colon-targeted tablet of oxaliplatin (OP) using the combination of nanotechnology and fused deposition modeling (FDM) 3D printing to improve its antitumor activity, tumor targetability, and safety profile. Eudragit L100-55 filament containing OP loaded alginate nanoparticles (OP-NPs) were fabricated using hot-melt extrusion method and printed by an FDM printer to 3D p ...
DOI:
10.1016/j.ijbiomac.2022.02.080

43. 3D-QSAR models to predict anti-cancer activity on a series of protein P38 MAP kinase inhibitors

Author:
El Ghalia Hadaji; Mohamed Bourass; Abdelkarim Ouammou; Mohammed Bouachrine
Source:
Journal of Taibah University for Science 2017 v.11 no.3 pp. 392-407
ISSN:
1658-3655
Subject:
antineoplastic activity; antineoplastic agents; autoimmune diseases; correlation; energy; enzyme inhibitors; least squares; mechanics; mitogen-activated protein kinase; model validation; molecular models; neoplasms; neural networks; quantitative structure-activity relationships; signal transduction; therapeutics
Abstract:
... Protein kinases are essential components of various signaling pathways and represent attractive targets for therapeutic interventions. Kinase inhibitors are currently used to treat malignant tumors, as well as autoimmune diseases, due to their involvement in immune cell signaling. In this study, three-dimensional quantitative structure–activity relationship (3D-QSAR) analyses, including Multiple L ...
DOI:
10.1016/j.jtusci.2016.05.006

44. 3‐Bromopyruvate as a potent anticancer therapy in honor and memory of the late Professor André Goffeau

Author:
Young H. Ko; Katarzyna Niedźwiecka; Margarida Casal; Peter L. Pedersen; Stanisław Ułaszewski
Source:
Yeast 2019 v.36 no.4 pp. 211-221
ISSN:
0749-503X
Subject:
Cryptococcus neoformans; adenosine triphosphate; adverse effects; algae; animal models; antimicrobial properties; antineoplastic activity; apoptosis; bromination; cancer therapy; cell movement; fungi; glucose; glycolysis; hexokinase; lactic acid; mitochondria; neoplasm cells; neoplasms; oxygen; patients; pumps; pyruvic acid; transporters
Abstract:
... 3‐Bromopyruvate (3BP) is a small, highly reactive molecule formed by bromination of pyruvate. In the year 2000, the antitumor properties of 3BP were discovered. Studies using animal models proved its high efficacy for anticancer therapy with no apparent side effects. This was also found to be the case in a limited number of cancer patients treated with 3BP. Due to the “Warburg effect,” most tumor ...
DOI:
10.1002/yea.3367

45. 3‐hydroxy‐3‐methyl glutaryl coenzyme A reductase: an essential actor in the biosynthesis of cantharidin in the blister beetle Epicauta chinensis Laporte

Author:
S. Lü; M. Jiang; T. Huo; X. Li; Y. Zhang
Source:
Insect molecular biology 2016 v.25 no.1 pp. 58-71
ISSN:
0962-1075
Subject:
Epicauta; RNA interference; antineoplastic activity; biosynthesis; cantharidin; chemical defenses; courtship; double-stranded RNA; gas chromatography; gene expression; genes; insects; juvenile hormones; males; messenger RNA; monoterpenoids; reverse transcriptase polymerase chain reaction; therapeutics
Abstract:
... Cantharidin (C₁₀H₁₂O₄) is a monoterpene defensive toxin in insects involved in chemical defence as well as in courtship and mating behaviours. It is relatively well known in the medical literature because of its high anticancer activity and as an effective therapy for molluscum contagiosum. However, little is known about its biosynthesis pathway in vivo, and no enzyme involved in cantharidin biosy ...
DOI:
10.1111/imb.12198

46. 3′-Hydroxy-4′-methoxy-β-methyl-β-nitrostyrene inhibits tumor growth through ROS generation and GSH depletion in lung cancer cells

Author:
Chun-Hao Tsai; Pei-Wen Hsieh; Yi-Chen Lee; Chie-Hong Wang; Wen-Chin Chiu; Chun-Wun Lu; Yen-Yun Wang; Stephen Chu-Sung Hu; Tain-Lu Cheng; Shyng-Shiou F. Yuan
Source:
Life sciences 2017 v.172 pp. 19-26
ISSN:
0024-3205
Subject:
Western blotting; antineoplastic activity; antineoplastic agents; apoptosis; caspases; cell viability; enzyme-linked immunosorbent assay; flow cytometry; glutathione; humans; lung neoplasms; membrane potential; mitochondria; mitochondrial membrane; neoplasm cells; reactive oxygen species; staining; thiols
Abstract:
... Members of the β-nitrostyrene family are known to suppress tumor growth, with the underlying mechanisms of β-nitrostyrene remain mostly unclear. Herein, we synthesized a β-nitrostyrene derivative, 3′-hydroxy-4′-methoxy-β-methyl-β-nitrostyrene (CYT-Rx20), and explored its anticancer activities in human lung cancer cells in vitro and in vivo.Cell viability was measured by XTT assay. Apoptosis was de ...
DOI:
10.1016/j.lfs.2016.12.009

47. 3′‐Desmethylarctigenin induces G2/M cell cycle arrest and apoptosis through reactive oxygen species generation in hepatocarcinoma cells

Author:
Enxiang Zhang; Xiuling Wang; Xiaoyi Liu; Min Liang; Hongbo Hu; Shutao Yin
Source:
Phytotherapy research 2019 v.33 no.12 pp. 3218-3227
ISSN:
0951-418X
Subject:
antineoplastic activity; apoptosis; cell cycle checkpoints; chemoprevention; hepatoma; human cell lines; mice; mitochondria; models; reactive oxygen species; therapeutics; toxicity
Abstract:
... Previous studies have shown that arctigenin is a promising chemopreventive or therapeutic agent against various cancers. However, less is known about anticancer activity of 3′‐desmethylarctigenin (3′‐DMAG), which is a biotransformed product from arctigenin or arctin. In this study, we compared the anticancer activity of 3′‐DMAG with its parent compound arctigenin and demonstrated that 3′‐DMAG exer ...
DOI:
10.1002/ptr.6496

48. 4,5-Dihydropyrazole derivatives containing oxygen-bearing heterocycles as potential telomerase inhibitors with anticancer activity

Author:
Yin Luo; Yang Zhou; Jie Fu; Hai-Liang Zhu
Source:
RSC advances 2014 v.4 no.45 pp. 23904-23913
ISSN:
2046-2069
Subject:
Western blotting; active sites; antineoplastic activity; apoptosis; autophagy; enzyme inhibition; enzyme inhibitors; flow cytometry; humans; inhibitory concentration 50; models; moieties; neoplasm cells; oxygen; pyrazoles; stomach neoplasms; telomerase; telomeres
Abstract:
... Telomere and telomerase were closely related to the occurrence and development of some cancers. After the key active site of telomerase was identified, to enhance the ability of dihydropyrazole derivatives to inhibit telomerase, we designed a series of novel 4,5-dihydropyrazole derivatives containing heterocyclic oxygen moiety based on previous studies. The telomerase inhibition assay showed that ...
DOI:
10.1039/c4ra02200a

49. 4,5-Diphenyl-2-methyl picolinate induces cellular senescence by accumulating DNA damage and activating associated signaling pathways in gastric cancer

Author:
Zhicong Zhao; Dongsheng Shang; Lipeng Qiu; Chang Guo; Yanyan Li; Hanqing Liu; Guoyue Yuan; Zhigang Tu
Source:
Life sciences 2019 v.238 pp. 116973
ISSN:
0024-3205
Subject:
DNA damage; antineoplastic activity; antineoplastic agents; cell senescence; drug therapy; enzymes; fluorescent antibody technique; heterocyclic nitrogen compounds; in vitro studies; in vivo studies; mice; screening; signal transduction; staining; stomach neoplasms; survival rate
Abstract:
... Gastric cancer (GC) is a common cancer with a relatively low survival rate. Cellular senescence, a potent anti-cancer mechanism, is naturally occurred, and can be induced by chemotherapeutic agents. We sought to explore new compounds against GC cells by inducing cellular senescence.Primary screening of a library of N-heterocyclic compounds identified some with potent inhibitory effects on GC cells ...
DOI:
10.1016/j.lfs.2019.116973

50. 4-Aminoantipyrine in carbohydrate research: Design, synthesis and anticancer activity of thioglycosides of a novel class of 4-aminoantipyrines and their corresponding pyrazolopyrimidine and pyrazolopyridine thioglycosides

Author:
Galal H. Elgemeie; Mamdouh A. Abu-Zaied; Samah A. Loutfy
Source:
Tetrahedron 2017 pp. -
ISSN:
0040-4020
Subject:
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 ...
DOI:
10.1016/j.tet.2017.08.024