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Antitumor activity

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Histone deacetylase inhibitor panobinostat induces antitumor activity in epithelioid sarcoma and rhabdoid tumor by growth factor receptor modulation

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Histone deacetylase inhibitor panobinostat induces antitumor activity in epithelioid sarcoma and rhabdoid tumor by growth factor receptor modulation. Methods: In this study, we investigated the activity of a panel of epigenetic modulators and receptor tyrosine kinase inhibitors in vitro on respective cell lines as well as on primary patient-derived epithelioid sarcoma cells, and in vivo on xenografted mice.

Toxicity assessment of green synthesized Cu nanoparticles by cell-free extract of Pseudomonas silesiensis as antitumor cancer and antimicrobial

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Determination coefficient (R 2 ) between the CuNPs (MLC) and the spectrum activity of P. silesiensis strain A3 CuNPs have a high antitumor activity.. Biosynthesis, characterization and antimicrobial activity of copper oxide nanoparticles (CONPs) produced using brown alga extract (Bifurcaria bifurcata). (B) Microscopic examination images (800×) presented the morphological changes in A549 carcinoma cell line after exposure to various concentrations of CuNPs.

Prodigiosin purification from serratia marcescens M10 and its antitumor activities

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In this study, we report an efficient purification of Pg by using toluene:ethyl acetate ratio 9:1 (v/v) and chloroform:ethyl acetate ratio 1:1 (v/v) solvents as well as its promising antitumor activity tested in benign induced BALB/c mice..

Antitumor properties of vegetable oil extract from green microalga coelastrella sp.

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Recent studies pointed that the antitumor activity of astaxanthin may be exerted through several different mechanisms of action and influence on a multitude of molecular and cellular processes (Zhanget al., 2015). The anti- proliferative effect of astaxanthin against CBRH-7919 (human hepatoma), SHZ- 88 (rat breast), Lewis (mouse lung) cells and human HCT-116 colon cancer cells (Song et al., 2011. Palozza et al., 2011) was reported.

A phase I study of the safety and activity of K-001 in patients with advanced pancreatic ductal adenocarcinoma

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Based on those prior studies, we conducted the current study which focused on the safety and antitumor activity of oral drug K-001 in patients with advanced PDAC.

Novel 3-substituted-2-oxoindoline-based N-hydroxypropenamides as Histone Deacetylase Inhibitors and Antitumor Agents

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Inhibition of HDAC activity and cytotoxicity of the compounds synthesized against several cancer cell lines.. of the 5-methoxy substituent and methoxime on the indoline ring even decreased cytotoxicity (compound 6f). Histone deacetylases (HDACs): characteriza- tion of the classical HDAC family. Prodrugs of 4- demethyl-4-deoxypodophyllotoxin: synthesis and evaluation of the antitumor activity

Antiangiogenic antibody BD0801 combined with immune checkpoint inhibitors achieves synergistic antitumor activity and affects the tumor microenvironment

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Notably, the combination of BD0801 with an ICI reveals synergistic antitumor effects in both lung cancer and colorectal cancer mouse models.

Anti-proliferative and pro-apoptotic activity of glycosidic derivatives of lawsone in melanoma cancer cell

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The global impact caused by the high incidence rates and prevalence of cancer, associated with the heterogen- eity of the disease, which presents different forms and specificities and the chemoresistance developed by tumor cells to antineoplastic treatment reveal the im- portance of the search for new bioactive compounds with potential antitumor activity [6].

Investigation of the structural and physicochemical requirements of quinoline-arylamidine hybrids for the growth inhibition of K562 and Raji leukemia cells

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The negative sign of DIPX in model (2) implies that an enhanced value of DIPX is favorable for the antitumor activity of CQArA compounds. Dipole moments of the two most active compounds (15, 22) and the two least active compounds (17, 18).. Antitumor activities of the proposed compounds are logGI 50calc = 0.02 and –0.29 for 29 and 30, respectively.

Synthesis and in vitro cytotoxic activity of novel pyrazolo[1,5-a]pyrimidines and related Schiff bases

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Pyrazolo[1,5- a ]pyrimidines 5a–c and 9a–c and Schiff bases 11b–f were investigated for their cytotoxicity against four human cancer cell lines (colon HCT116, lung A549, breast MCF-7, and liver HepG2) according to SRB assay and the structure–activity relationship was discussed.. Key words: 5-Aminopyrazole, pyrazolopyrimidines, ferrocenyl-2-carboxaldehyde, Schiff bases, antitumor activity.

A better approach to economic development for indigenous medicine in Myanmar: The leaves of Tadehagi triquetrum (L). H. Ohashi (Lauk-thay)

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The antitumor behaviours screening of different crude extracts (PE, EtOAC, EtOH and watery extracts) of the leaves of Lauk-thay were carried out against Agrobacterium tumefaciens by Potato Crown Gall test or Potato Disc Assay method.. Among the tested crude extracts of the leaves of Lauk- thay, only pet ether crude extracts exhibited antitumor activity against A. beliefs on the action of medicinal plants.

Synthesis, characterization and evaluation of antibacterial activity of copper(ii) curcumin complex against staphylococcus aureus

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Wang, et al., Two copper(II) complexes of curcumin derivatives: synthesis, crystal structure and in vitro antitumor activity, Transition Metal Chemistry, 39, pp . Ng, Curcumin interaction with copper and iron suggests one possible mechanism of action in Alzheimer's disease animal models, Journal of Alzheimer's disease, 6, pp . Dutta, et al., Enhanced antioxidant activities of metal conjugates of curcumin derivatives, Metal-based drugs, 8, pp .

Nghiên cứu khảo sát một số yếu tố ảnh hưởng tới quá trình tách chiết beta- glucan từ Lentinula edodes.

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Chihara, G., et al., Fractionation and purification of the polysaccharides with marked antitumor activity, especially lentinan, from Lentinus edodes (Berk.) Sing. Chihara, G., et al., Antitumor and metastasis-inhibitory activities of lentinan as an immunomodulator: an overview. Chihara, G., et al., Inhibition of mouse sarcoma 180 by polysaccharides from Lentinus edodes (Berk.) sing. Ikekawa, T., et al., Antitumor action of some Basidiomycetes, especially Phllinus linteus.

The epigenetic immunomodulator, HBI8000, enhances the response and reverses resistance to checkpoint inhibitors

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HBI-8000 is a novel, orally bioavailable class I selective histone deacetylase inhibitor that directly modifies antitumor activity by inducing apoptosis, cell cycle arrest, and. We hypothesized that HBI-8000 functions as an epigenetic immunomodulator to reprogram the tumor microenvironment from immunologically cold. Results: HBI-8000 augmented the activity of ICI antibodies targeting either PD-1, PD-L1 or CTLA-4, and significantly increased tumor regression ( p <.

New sandwich-type polymeric potassium-dicyanoargentate(I) complex: Synthesis, characterization and enzymatic activity

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The structural characterizations of these complexes, catalysis applications, EPR properties of the d 9 structure, as well as biological properties, have been determined [4–16].. compounds containing silver that exhibited antitumor activity have also been reported in the literature [27–32]. Elemental analysis of the sample was taken according to the standard (C, N, H, and O values) method.

Bortezomib potentiates antitumor activity of mitoxantrone through dampening Wnt/ β-catenin signal pathway in prostate cancer cells

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In this study, MTX increased proteasome activity in prostate cancer cells, in- dicating that proteasome activity may be required for MTX-induced apoptosis. BZM and MG132 attenuated MTX-induced apoptosis, which may be due to a de- crease in proteasome activity.. This study demonstrates that BZM enhances MTX- induced anti-tumor effects by inhibiting the Wnt/ β - Catenin signaling pathway in prostate cancer cells..

An insight into the therapeutic potential of piperazine-based anticancer agents

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Compound 92 showed encouraging activity against the HL60 cell line, having an IC 50 value of 0.6 µM. Upon screening for cytotoxic potential, compound 93 (Figure 8) was found to have good activity against PC-3, having an IC 50 value of 16 µM. Compound 95 showed good antitumor activity against DU145 and KBvin (vincristine-resistant KB subline), having GI 50 values of 0.91 µM. Compounds 96 and 97 displayed prominent activity against A549, having GI 50 values of 9.07 µM and 12.22 µM.

Chapter 080. Cancer Cell Biology and Angiogenesis (Part 9)

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Drugs that block the enzymatic activity of HDAC are being developed. A number of different chemical classes of HDAC inhibitors have demonstrated antitumor activity in clinical studies against cutaneous T cell lymphoma (e.g., vorinostat) and some solid tumors. HDAC inhibitors may target cancer cells via a number of mechanisms including upregulation of death receptors (DR4/5, FAS, and their ligands) and p21 Cip1/Waf1 , as well as inhibition of cell cycle checkpoints..

Chapter 080. Cancer Cell Biology and Angiogenesis (Part 20)

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Sunitinib, FDA approved for the treatment of GIST (see above and Table 80-2), has activity directed against mutant c-Kit receptors, but also targets VEGFR and PDGFR, and has shown significant antitumor activity against metastatic RCC, presumably on the basis of its antiantiogenic activity.. Similarly, sorafenib, originally developed as a Raf kinase inhibitor but with potent activity against VEGF and PDGF receptors, increases progression-free survival in RCC.

Extracellular glutaminase-free l-asparaginase from trichoderma viride F2: Purification, biochemical characterization and evaluation of its potential in mitigating acrylamide formation in starchy fried food

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Purification, characterization and antitumor activity of L- asparaginase from Penicillium brevicompactum NRC 829. https://doi.org/10.9734/bmrj/2012/1735. Imada, A., Igarasi, S., Nakahama, K., &. Kalyanasundaram, I., Nagamuthu, J., Srinivasan, B., Pachayappan, A., &. Kamble, V.P., Rao, R.S., Borker, P.S., Khobragade, C.N., &. https://doi.org/10.1007/s y. Kotzia, G.A., &. https://doi.org/10.1016/j.jbiotec .