Biological activity of Xanthium strumarium seed extracts on different cancer cell lines and Aedes caspius , Culex pipiens (Diptera: Culicidae)

We synthesized five novel tryptamine derivatives characterized by the presence of an azelayl chain or of a 1,1,1-trichloroethyl group, in turn connected to another heterocyclic scaffold. The combination of tryptamin-, 1,1,1-trichloroethyl- and 2-aminopyrimidinyl- moieties produced compound 9 identified as the most active compound in hematological cancer cell lines (IC50 = 0.57–65.32 μM). Moreover, keeping constant the presence of the tryptaminic scaffold and binding it to the azelayl moiety, the compounds maintain biological activity. Compound 13 is still active against hematological cancer cell lines and shows a selective effect only on HT29 cells (IC50 = 0.006 µM) among solid tumor models. Compound 14 loses activity on all leukemic lines, while showing a high level of toxicity on all solid tumor lines tested (IC50 0.0015–0.469 µM).

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Synthesis, conformational preferences, and biological activity of conformational analogues of the microtubule-stabilizing agents, (−)-zampanolide and (−)-dactylolide

MedChemComm ◽

10.1039/c9md00164f ◽

2019 ◽

Vol 10 (5) ◽

pp. 800-805 ◽

Cited By ~ 2

Author(s):

Jeffrey L. Henry ◽

Matthew R. Wilson ◽

Michael P. Mulligan ◽

Taylor R. Quinn ◽

Dan L. Sackett ◽

...

Keyword(s):

Biological Activity ◽

Cell Lines ◽

Cancer Cell ◽

Cancer Cell Lines ◽

Stabilizing Agents ◽

Conformational Preferences

Zampanolide and dactylolide are microtubule-stabilizing polyketides possessing potent cytotoxicity towards a variety of cancer cell lines.

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Synthesis of Novel Class of N-Alkyl-isatin-3-iminobenzoic Acid Derivatives and Their Biological Activity in Zebrafish Embryos and Human Cancer Cell Lines

Biological and Pharmaceutical Bulletin ◽

10.1248/bpb.b17-00674 ◽

2018 ◽

Vol 41 (3) ◽

pp. 350-359 ◽

Cited By ~ 7

Author(s):

Muhammad Farooq ◽

Zainab Mohammed Al Marhoon ◽

Nael Abu Taha ◽

Almohannad Abdulrahman Baabbad ◽

Mohammed Ahmed Al-Wadaan ◽

...

Keyword(s):

Biological Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Zebrafish Embryos ◽

Human Cancer Cell ◽

Human Cancer Cell Lines

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Synthesis, Expression and Biological Activity of the Prohormone for Gastrin Releasing Peptide (ProGRP)

Endocrinology ◽

10.1210/en.2005-0574 ◽

2006 ◽

Vol 147 (1) ◽

pp. 502-509 ◽

Cited By ~ 24

Author(s):

Chelsea Dumesny ◽

Oneel Patel ◽

Shamilah Lachal ◽

Andrew S. Giraud ◽

Graham S. Baldwin ◽

...

Keyword(s):

Colon Cancer ◽

Biological Activity ◽

Cell Lines ◽

Cancer Cell ◽

Inositol Phosphate ◽

Cancer Cell Lines ◽

Colon Cancer Cell ◽

Biologically Active ◽

Gastrin Releasing Peptide ◽

End Products

Gastrin-releasing peptide (GRP) has a widespread distribution and multiple stimulating effects on endocrine and exocrine secretions and metabolism. The prohormone for GRP (ProGRP, 125 amino acids) is processed to the amidated, biologically active end products GRP1–27 and GRP18–27. Amidated forms of GRP are putative autocrine or paracrine growth factors in a number of cancers including colorectal cancer. However, the potential role and biological activity of proGRP has not been investigated. Using a newly developed antisera directed to the N terminus of human proGRP, proGRP immunoreactivity was detected in all of the endometrial, prostate, and colon cancer cell lines tested and in nine of 10 resected colorectal carcinomas. However, no amidated forms were detected, suggesting an attenuation of processing in tumors. Recombinant proGRP was expressed as a His-tag fusion protein and purified by metal affinity chromatography and HPLC. ProGRP stimulated proliferation of a colon cancer cell line and activated MAPK, but unlike GRP18–27amide had no effect on inositol phosphate production. ProGRP did not compete with iodinated bombesin in binding assays on Balb-3T3 cells transfected with the known GRP receptors, GRP-R or BRS-3. We conclude that proGRP is present in a number of cancer cell lines and in resected colorectal tumors and is biologically active. Our results suggest that antagonists to GRP precursors rather than the amidated end products should be developed as a treatment for colorectal and other cancers that express proGRP-derived peptides.

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Synthesis, structure, magnetic and biological activity studies of bis-hydrazone derived Cu(ii) and Co(ii) coordination compounds

Dalton Transactions ◽

10.1039/c6dt01496h ◽

2016 ◽

Vol 45 (29) ◽

pp. 11849-11863 ◽

Cited By ~ 16

Author(s):

Upendarrao Golla ◽

Amit Adhikary ◽

Amit Kumar Mondal ◽

Raghuvir Singh Tomar ◽

Sanjit Konar

Keyword(s):

Biological Activity ◽

Cell Lines ◽

Cancer Cell ◽

Coordination Compounds ◽

Linear Chain ◽

Nuclease Activity ◽

Cancer Cell Lines ◽

Magnetic Studies ◽

Synthetic Strategy ◽

Chain Compound

Three double stranded helicates and one linear chain compound have been synthesized following similar synthetic strategy with change in the coordination of the ligands. Magnetic studies, nuclease activity and cytotoxicity on mammalian cancer cell lines have been investigated.

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6-Substituted imidazo[1,2-a]pyridines: Synthesis and biological activity against colon cancer cell lines HT-29 and Caco-2

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2011.07.036 ◽

2011 ◽

Vol 46 (9) ◽

pp. 4573-4583 ◽

Cited By ~ 58

Author(s):

Nurit Dahan-Farkas ◽

Candice Langley ◽

Amanda L. Rousseau ◽

Dharmendra B. Yadav ◽

Hajierah Davids ◽

...

Keyword(s):

Colon Cancer ◽

Biological Activity ◽

Cell Lines ◽

Cancer Cell ◽

Cancer Cell Lines ◽

Colon Cancer Cell ◽

Colon Cancer Cell Lines ◽

Ht 29

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Targeting plasma membrane phosphatidylserine content to inhibit oncogenic KRAS function

Life Science Alliance ◽

10.26508/lsa.201900431 ◽

2019 ◽

Vol 2 (5) ◽

pp. e201900431 ◽

Cited By ~ 6

Author(s):

Walaa E Kattan ◽

Wei Chen ◽

Xiaoping Ma ◽

Tien Hung Lan ◽

Dharini van der Hoeven ◽

...

Keyword(s):

Biological Activity ◽

Plasma Membrane ◽

Cell Lines ◽

Cancer Cell ◽

Cancer Cell Lines ◽

Lipid Binding ◽

Small Gtpase ◽

Membrane Anchor ◽

Normal Cells

The small GTPase KRAS, which is frequently mutated in human cancers, must be localized to the plasma membrane (PM) for biological activity. We recently showed that the KRAS C-terminal membrane anchor exhibits exquisite lipid-binding specificity for select species of phosphatidylserine (PtdSer). We, therefore, investigated whether reducing PM PtdSer content is sufficient to abrogate KRAS oncogenesis. Oxysterol-related binding proteins ORP5 and ORP8 exchange PtdSer synthesized in the ER for phosphatidyl-4-phosphate synthesized in the PM. We show that depletion of ORP5 or ORP8 reduced PM PtdSer levels, resulting in extensive mislocalization of KRAS from the PM. Concordantly, ORP5 or ORP8 depletion significantly reduced proliferation and anchorage-independent growth of multiple KRAS-dependent cancer cell lines, and attenuated KRAS signaling in vivo. Similarly, functionally inhibiting ORP5 and ORP8 by inhibiting PI4KIIIα-mediated synthesis of phosphatidyl-4-phosphate at the PM selectively inhibited the growth of KRAS-dependent cancer cell lines over normal cells. Inhibiting KRAS function through regulating PM lipid PtdSer content may represent a viable strategy for KRAS-driven cancers.

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Anticancer effect of the fruit and seed extracts of Momordica charantia L. (Cucurbitaceae) on human cancer cell lines

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v18i10.9 ◽

2021 ◽

Vol 18 (10) ◽

pp. 2057-2065

Author(s):

Hatice Güneş ◽

Mehlika Alper ◽

Nevin Çelikoğlu

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

A549 Cells ◽

K562 Cells ◽

Cancer Cell Lines ◽

Fruit Extract ◽

Human Cancer Cell Lines ◽

Seed Extracts ◽

Mcf 7

Purpose: To investigate anticancer effects of Momordica charantia L. (M. charantia) fruit and seed extracts on some cancer cell lines. Methods: Human cancer cell lines, including lung cancer (A549), breast cancer (MCF-7), chronic myeloid leukemia (K562) and T cell leukemia (Jurkat) were incubated with the extracts (0 - 0.8 mg/mL) for 72 h. The cytotoxic effects of the extracts were determined using 3-(4,5-dimethylthiazol-2-yl)-2,5- dipenyltetrazolium bromide (MTT) assay. A549 and MCF-7 cells were treated with the ethanol fruit extract (FE) for 24 h and stained with propidium iodide (PI) for the analysis of cell cycle arrest using flow cytometry. Annexin V-FITC/PI staining along with flow cytometry analysis and caspase-3 assays were carried out to determine the apoptosis of the cells treated with FE extract for 24 h. Vascular endothelial growth factor (VEGF) secretion of the cells exposed to FE extract for 1 h was determined using enzyme-linked immunosorbent assay (ELISA). Cell invasion assay was applied to detect cell migration after treatment with FE extract for 48 h. Results: Ethanol fruit extract (FE) resulted in 90, 92, 85 and 87 % cytotoxicity against K562, A549, MCF-7 and Jurkat cell lines, respectively. However, ethanol seed extract of seed (SE) was less effective (≤42 %) on cytotoxicity against cancer cells. Acetone fruit extract (FA) caused 82, 75 and 59 % cytotoxicity on MCF-7, Jurkat and K562 cells, respectively, whereas 20 % cytotoxicity was observed on A549 cells. Dose analyses of FE extract indicated that K562 cells had the lowest IC50 value (0.082 mg/mL). In addition, FE extract treatment caused accumulation of A549 and MCF-7 cells in the S phase of the cell cycle. Moreover, apoptotic cell death was observed in A549 or MCF-7 cells treated with the FE extract. While the treatment of A549 cells with LPS for 24 h resulted in 19-fold increase in VEGF secretion, combination of FE with LPS caused 9.6-fold decrease in VEGF secretion, indicating the antiangiogenic activity of FE extract. Furthermore, FE extract treatment led to a significant decrease in the invasive properties of A549 and PC-3 cells when compared to untreated cells. Conclusion: Among the M. charantia extracts, FE extract displayed the highest anticancer potency against cancer cell lines, indicating that M. charantia FE extract may be a potential source for development of anticancer compounds in future.

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