scholarly journals Syntheses of l-Rhamnose-Linked Amino Glycerolipids and Their Cytotoxic Activities against Human Cancer Cells

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 566
Author(s):  
Makanjuola Ogunsina ◽  
Pranati Samadder ◽  
Temilolu Idowu ◽  
Mark Nachtigal ◽  
Frank Schweizer ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Drug Resistant ◽  
Ether Lipids ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Synthetic Procedure ◽  
Major Impediment

A major impediment to successful cancer treatment is the inability of clinically available drugs to kill drug-resistant cancer cells. We recently identified metabolically stable l-glucosamine-based glycosylated antitumor ether lipids (GAELs) that were cytotoxic to chemotherapy-resistant cancer cells. In the absence of commercially available l-glucosamine, many steps were needed to synthesize the compound and the overall yield was poor. To overcome this limitation, a facile synthetic procedure using commercially available l-sugars including l-rhamnose and l-glucose were developed and the l-GAELs tested for anticancer activity. The most potent analog synthesized, 3-amino-1-O-hexadecyloxy-2R-(O–α-l-rhamnopyranosyl)-sn- glycerol 3, demonstrated a potent antitumor effect against human cancer cell lines derived from breast, prostate, and pancreas. The activity observed was superior to that observed with clinical anticancer agents including cisplatin and chlorambucil. Moreover, like other GAELs, 3 induced cell death by a non-membranolytic caspase-independent pathway.

Rhodium(i) N-heterocyclic carbene complexes: synthesis and cytotoxic properties

2021 ◽  
Vol 45 (11) ◽  
pp. 5176-5183
Author(s):  
Ichraf Slimani ◽  
Serap Şahin-Bölükbaşı ◽  
Mustafa Ulu ◽  
Enes Evren ◽  
Nevin Gürbüz ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Mtt Assay ◽  
Incubation Time ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Carbene Complexes ◽  
Human Cancer Cells ◽  
Benzimidazolium Salts ◽  
Ht 29

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.

scholarly journals Antioxidant and Cytotoxic Activities of Myrtaceae Essential Oils Rich in Terpenoids From Brazil

2021 ◽  
Vol 16 (2) ◽  
pp. 1934578X2199615
Author(s):  
Lucas Botelho Jerônimo ◽  
Jamile S. da Costa ◽  
Laine C. Pinto ◽  
Raquel C. Montenegro ◽  
William N. Setzer ◽  
...  
Keyword(s):  
Essential Oils ◽  
Cancer Cells ◽  
Antioxidant Activities ◽  
Human Cancer ◽  
Psidium Guajava ◽  
Cytotoxic Activities ◽  
Chemical Compositions ◽  
Main Compound ◽  
Human Cancer Cells ◽  
High Concentrations

This work analyzed the chemical compositions and evaluated the antioxidant and cytotoxic activities of essential oils (EO) of Eugenia patrisii (Epat), Eugenia stipitata (Esti), Myrcia splendens (Mspl), Myrcia sylvatica (Msyl), Psidium guajava (Pgua), and Psidium guineense (Pgui-1 and Pgui-2) from the Brazilian Amazon. Sesquiterpenoids were found in high concentrations in the oils of E. patrisii and M. splendens, which were rich in E-caryophyllene (32.0% and 45.8%); E. stipitata and M. sylvatica, which displayed germacrene D (11.8%) and germacrene B (24.5%); and P. guajava that showed epi-β-bisabolol (16.1%) as the main compound. However, P. guineense samples (Pgui-1 and Pgui-2) were rich in monoterpenoids such as limonene (Pgui-1: 30.2%; Pgui-2 30.4%) and α-pinene (Pgui-1: 22.5%; Pgui-2: 17.7%). The samples showed a weak and moderate antioxidant activities in the DPPH assay, displaying inhibition rates from 11.5% to 38.6% (at 10 mg/mL). All samples were cytotoxic against human cancer cells by the MTT method. Epat oil showed higher activity against melanoma (SKMEL-19, IC505.8 µg/mL), gastric (AGP01, IC503.2 µg/mL), and colon (HCT116, IC506.7 µg/mL). Meanwhile, the samples Pgua and Pgui were more active against breast cancer cells (MCF7, IC5012.4 µg/mL and 11.6 µg/mL, respectively).

Synthesis, antimicrobial and cytotoxic activities, and structure–activity relationships of gypsogenin derivatives against human cancer cells

2014 ◽  
Vol 82 ◽  
pp. 565-573 ◽  
Author(s):  
Safiye Emirdağ-Öztürk ◽  
Tamer Karayıldırım ◽  
Aysun Çapcı-Karagöz ◽  
Özgen Alankuş-Çalışkan ◽  
Ali Özmen ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Structure Activity Relationships ◽  
Human Cancer Cells ◽  
Structure Activity

scholarly journals Selective vulnerability of aneuploid human cancer cells to inhibition of the spindle assembly checkpoint

2020 ◽  
Author(s):  
Yael Cohen-Sharir ◽  
James M. McFarland ◽  
Mai Abdusamad ◽  
Carolyn Marquis ◽  
Helen Tang ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cellular Response ◽  
Large Scale ◽  
Spindle Assembly Checkpoint ◽  
Human Cancer ◽  
Spindle Assembly ◽  
Selective Vulnerability ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Diploid Cells

AbstractSelective targeting of aneuploid cells is an attractive strategy for cancer treatment. Here, we mapped the aneuploidy landscapes of ~1,000 human cancer cell lines and classified them by their degree of aneuploidy. Next, we performed a comprehensive analysis of large-scale genetic and chemical perturbation screens, in order to compare the cellular vulnerabilities between near-diploid and highly-aneuploid cancer cells. We identified and validated an increased sensitivity of aneuploid cancer cells to genetic perturbation of core components of the spindle assembly checkpoint (SAC), which ensures the proper segregation of chromosomes during mitosis. Surprisingly, we also found highly-aneuploid cancer cells to be less sensitive to short-term exposures to multiple inhibitors of the SAC regulator TTK. To resolve this paradox and to uncover its mechanistic basis, we established isogenic systems of near-diploid cells and their aneuploid derivatives. Using both genetic and chemical inhibition of BUB1B, MAD2 and TTK, we found that the cellular response to SAC inhibition depended on the duration of the assay, as aneuploid cancer cells became increasingly more sensitive to SAC inhibition over time. The increased ability of aneuploid cells to slip from mitotic arrest and to keep dividing in the presence of SAC inhibition was coupled to aberrant spindle geometry and dynamics. This resulted in a higher prevalence of mitotic defects, such as multipolar spindles, micronuclei formation and failed cytokinesis. Therefore, although aneuploid cancer cells can overcome SAC inhibition more readily than diploid cells, the proliferation of the resultant aberrant cells is jeopardized. At the molecular level, analysis of spindle proteins identified a specific mitotic kinesin, KIF18A, whose levels were drastically reduced in aneuploid cancer cells. Aneuploid cancer cells were particularly vulnerable to KIF18A depletion, and KIF18A overexpression restored the sensitivity of aneuploid cancer cells to SAC inhibition. In summary, we identified an increased vulnerability of aneuploid cancer cells to SAC inhibition and explored its cellular and molecular underpinnings. Our results reveal a novel synthetic lethal interaction between aneuploidy and the SAC, which may have direct therapeutic relevance for the clinical application of SAC inhibitors.

scholarly journals System-Wide Analysis of Protein Acetylation and Ubiquitination Reveals a Diversified Regulation in Human Cancer Cells

Biomolecules ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 411 ◽  
Author(s):  
Hiroko Kozuka-Hata ◽  
Aya Kitamura ◽  
Tomoko Hiroki ◽  
Aiko Aizawa ◽  
Kouhei Tsumoto ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cancer Cell ◽  
Translational Control ◽  
Large Scale ◽  
Human Cancer ◽  
Initiation Factor ◽  
Protein Acetylation ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Lysine Modification

Post-translational modifications are known to be widely involved in the regulation of various biological processes, through the extensive diversification of each protein function at the cellular network level. In order to unveil the system-wide function of the protein lysine modification in cancer cell signaling, we performed global acetylation and ubiquitination proteome analyses of human cancer cells, based on high-resolution nanoflow liquid chromatography–tandem mass spectrometry, in combination with the efficient biochemical enrichment of target modified peptides. Our large-scale proteomic analysis enabled us to identify more than 5000 kinds of ubiquitinated sites and 1600 kinds of acetylated sites, from representative human cancer cell lines, leading to the identification of approximately 900 novel lysine modification sites in total. Very interestingly, 236 lysine residues derived from 141 proteins were found to be modified with both ubiquitination and acetylation. As a consequence of the subsequent motif extraction analyses, glutamic acid (E) was found to be highly enriched at the position (−1) for the lysine acetylation sites, whereas the same amino acid was relatively dispersed along the neighboring residues of the lysine ubiquitination sites. Our pathway analysis also indicated that the protein translational control pathways, such as the eukaryotic initiation factor 2 (EIF2) and the ubiquitin signaling pathways, were highly enriched in both of the acetylation and ubiquitination proteome data at the network level. This report provides the first integrative description of the protein acetylation and ubiquitination-oriented systematic regulation in human cancer cells.

ChemInform Abstract: Sesquiterpenes from Rhizomes of Cyperus rotundus with Cytotoxic Activities on Human Cancer Cells in vitro.

ChemInform ◽  
2016 ◽  
Vol 47 (8) ◽  
pp. no-no ◽  
Author(s):  
Byeol Ryu ◽  
Hye Mi Kim ◽  
Jae-Seung Lee ◽  
Yoon Jin Cho ◽  
Myung Sook Oh ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cyperus Rotundus ◽  
Cytotoxic Activities ◽  
Human Cancer Cells

Sesquiterpene lactones from Carpesium rosulatum with potential cytotoxicity against five human cancer cell lines

2010 ◽  
Vol 30 (8) ◽  
pp. 1083-1087 ◽  
Author(s):  
Hyung-In Moon ◽  
Okpyo Zee
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Sesquiterpene Lactone ◽  
Cell Lines ◽  
Human Cancer ◽  
Sesquiterpene Lactones ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Whole Plant

In search for plant-derived cytotoxicity compound against human cancer cells (A549, SK-OV-3, SK-MEL-2, XF498, HCT15), it was found that the chloroform extracts obtained from the whole plant of Carpesium rosulatum MlQ. (Compositae) exhibited significant cytotoxic activity. Four sesquiterpene lactone, CRC1 (2α, 5-epoxy-5,10-dihydroxy-6-angeloyl-oxy-9β-isobutyloxy-germacran-8α,12-olide), CRC2 (2α,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide), CRC3 (2α,5-epoxy-5,10-dihydroxy-6α-angeloyloxy-9β-(3-methyl-butanoyloxy)-gemacran-8α,12-olide), CRC4 (2β,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide) were isolated from the whole parts of C. rosulatum. 2α,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide (CRC2) showed the most potent cytotoxicity with IC50 value of 6.01 μM against SK-MEL-2.

scholarly journals Compounds with Antiproliferative Activity on Five Human Cancer Cell Lines from South Korean Carpesium triste

2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Hyung-In Moon
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Sesquiterpene Lactones ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
South Korean ◽  
Whole Plant

In the search for antiproliferative compounds against human cancer cells (A549, SK-OV-3, SK-MEL-2, XF498, HCT15), it was found that the chloroform extracts obtained from the whole plant of Carpesium rosulatum Miq. (Compositae) exhibited significant cytotoxic activity. Two sesquiterpene lactones, CT-1 (2α,5-epoxy-5,10-dihydroxy-6-angeloyloxy-9β-isobutyloxy-germacran-8α,12-olide), and CT-2 (2β,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide) were isolated from the whole plant. CT-2 showed the most potent cytotoxicity with an IC50 value of 7.88 μM against SK-MEL-2.

scholarly journals Hydrazine-Containing Heterocycle Cytochalasan Derivatives From Hydrazinolysis of Extracts of a Desert Soil-Derived Fungus Chaetomium madrasense 375

2021 ◽  
Vol 9 ◽  
Author(s):  
Qingfeng Guo ◽  
Jinhua Chen ◽  
Yuwei Ren ◽  
Zhenhua Yin ◽  
Juanjuan Zhang ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cancer Cells ◽  
Human Cancer ◽  
Drug Resistant ◽  
Hydrazine Monohydrate ◽  
Chemical Libraries ◽  
Human Cancer Cells ◽  
First Time ◽  
Antiproliferative Activities ◽  
Positive Controls

“Diversity-enhanced extracts” is an effective method of producing chemical libraries for the purpose of drug discovery. Three rare new cytochalasan derivative chaetoglobosins B1-B3 (1–3) were obtained from chemically engineered crude broth extracts of Chaetomium madrasense 375 prepared by reacting with hydrazine monohydrate and four known metabolite chaetoglobosins (4–7) were also identified from the fungus. The structures were identified by NMR and MS analysis and electronic circular dichroism simulation. In addition, the antiproliferative activities of these compounds were also evaluated, and the drug-resistant activities of cytochalasans were evaluated for the first time. Compound 6 possessed potent activity against four human cancer cells (A549, HCC827, SW620, and MDA-MB-231), and two drug-resistant HCC827 cells (Gefitinib-resistant, Osimertinib-resistant) compared with the positive controls.

Enniatin Exerts p53-Dependent Cytostatic and p53-Independent Cytotoxic Activities against Human Cancer Cells

2007 ◽  
Vol 20 (3) ◽  
pp. 465-473 ◽  
Author(s):  
Rita Dornetshuber ◽  
Petra Heffeter ◽  
Majid-Reza Kamyar ◽  
Thomas Peterbauer ◽  
Walter Berger ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Human Cancer Cells
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