scholarly journals Antitumor activity of a fungal glucan tylopilan and Propionibacterium acnes preparation

2014 ◽  
Vol 63 (3-4) ◽  
pp. 293-298 ◽  
Author(s):  
Jan Grzybek ◽  
Izabella Zgórniak-Nowosielska ◽  
Andrzej Kasprowicz ◽  
Barbara Zawilińska ◽  
Stanisław Kohlmunzer

The study evaluated the antitumor activity of tylopilan, aβ- (1→3) (1→6) linked glucan isolated from fruiting bodies of <i>Tylopilus felleus</i> (Bull.: Fr.) P. Karst. (<i>Boletaceae</i>), and <i>Propionibacterium acnes</i> (<i>P.a.</i>) preparation. The antitumor effect of tylopilan and <i>P.a.</i> used alone or in combination was studied in NMRI mice inoculated i.p. with 106 180-TG Crocker tumor cells. All experiments were based on a pretreatment with tylopilan and/or <i>P.a.</i> 5 days and/or 2 h before tumor cell inoculation. Mean survival time (MST) of tumor - bearing mice was significantly prolonged in comparison to control mice by a single injection of tylopilan (25 µg/mouse or 50 µg/mouse) or <i>P.a.</i> (1 mg/mouse). MST was 23.6; 22.8 days in the tylopilan injected mice and 17.5 in the control animals. Tylopilan injected in conjunction with <i>P.a.</i> prolonged signifi-cantly MST in comparison to control mice as well as to tylopilan alone treated mice. We have found that <i>P.a.</i> which stimulate immune response enhanced significantly antitumor activity of tylopilan. The cytotoxicity of tylopilan at concentrations of 300, 150, 75 and 37.5 µg/ml towards 180-TG Crocker cells in vitro studies was evaluated. All examined tylopilan concentrations showed cytotoxic activity.

Nanomedicine ◽  
2021 ◽  
Vol 16 (29) ◽  
pp. 2587-2604
Author(s):  
Chaoqi Li ◽  
Xiangbo Gou ◽  
Hui Gao

Aim: The authors aimed to develop Dox@Rg1 nanoparticles with decreased cardiotoxicity to expand their application in cancer. Materials & methods: Dox@Rg1 nanoparticles were developed by encapsulating doxorubicin (Dox) in a self-assembled Rg1. The antitumor effect of the nanoparticles was estimated using 4T1 tumor-bearing mice and the protective effect on the heart was investigated in vitro and in vivo. Results: Different from Dox, the Dox@Rg1 nanoparticles induced increased cytotoxicity to tumor cells, which was decreased in cardiomyocytes by the inhibition of apoptosis. The study in vivo revealed that the Dox@Rg1 nanoparticles presented a perfect tumor-targeting ability and improved antitumor effects. Conclusion: Dox@Rg1 nanoparticles could enhance the antitumor effects and decrease the cardiotoxicity of Dox.


1982 ◽  
Vol 14 (1) ◽  
Author(s):  
V. Silobrcic ◽  
G. Fredrickson ◽  
R. Sedlacek ◽  
H.D. Suit ◽  
G. Wolberg

MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2224-2231 ◽  
Author(s):  
Hai-Rong Zhang ◽  
Yan-Cheng Liu ◽  
Ting Meng ◽  
Qi-Pin Qin ◽  
Shang-Feng Tang ◽  
...  

A zinc(ii) complex of HBrQ showed higher in vitro antitumor activity. It induced cell apoptosis in BEL-7404 cells via G2 phase arrest, led to mitochondria dysfunction and activation of caspase cascade. The central zinc(ii) should play a key role to enhance the antitumor effect


2015 ◽  
Vol 15 (1) ◽  
Author(s):  
Jonas Christian Schupp ◽  
Sandrine Tchaptchet ◽  
Niklas Lützen ◽  
Peggy Engelhard ◽  
Joachim Müller-Quernheim ◽  
...  

2018 ◽  
Vol 2 (23) ◽  
pp. 3516-3525 ◽  
Author(s):  
Kyle Runckel ◽  
Matthew J. Barth ◽  
Cory Mavis ◽  
Juan J. Gu ◽  
Francisco J. Hernandez-Ilizaliturri

Abstract Clinical observations suggest the existence of shared resistance pathways between rituximab and chemotherapy agents. To explore the mechanisms of rituximab resistance, our group created rituximab-resistant cell lines (RRCLs), which display altered expression of several inhibitor of apoptosis (IAP) family proteins. Here, we provide evidence to support pharmacologically targeting IAPs in lymphoma with LCL-161, a small molecule mimetic of the second mitochondria-derived activator of caspases (SMAC). The antitumor effect of LCL-161 was determined using luminescent adenosine triphosphate assays, flow cytometry, SCID mouse xenografts, and ex vivo patient biopsy sample studies. In vitro exposure to LCL-161 also resulted in a dose-dependent decrease in IAP levels, along with synergistic enhancement of the antitumor effect of cytotoxic chemotherapy, in rituximab-sensitive cell lines and RRCLs. In addition, LCL-161 increased the cytotoxic effect of the proteasome inhibitor carfilzomib in ex vivo lymphoma patient samples. The combination of LCL-161 with the chemotherapy regimen rituximab, gemcitabine, and vinorelbine (RGV) improved in vivo survival compared with RGV alone in severe combined immunodeficient mice implanted with RRCLs but not in animals implanted with rituximab-sensitive cell lines. In summary, LCL-161 exhibits synergistic antitumor activity in both in vitro and in vivo models of resistant lymphoma. Our data support further preclinical investigation of LCL-161 as a novel antilymphoma agent.


2015 ◽  
Vol 4 (11) ◽  
pp. 1767-1780 ◽  
Author(s):  
Narayanan K. Narayanan ◽  
Kazuhiro Kunimasa ◽  
Yukio Yamori ◽  
Mari Mori ◽  
Hideki Mori ◽  
...  

2018 ◽  
Vol 19 (9) ◽  
pp. 2594 ◽  
Author(s):  
Jephesson Santos ◽  
Monalisa Brito ◽  
Rafael Ferreira ◽  
Ana Moura ◽  
Tatyanna Sousa ◽  
...  

Natural products have an important role as prototypes in the synthesis of new anticancer drugs. Piperine is an alkaloid amide with antitumor activity and significant toxicity. Then, the N-(p-nitrophenyl)acetamide piperinoate (HE-02) was synthesized, and tested for toxicological and antitumor effects. The toxicity was evaluated in vitro (on RAW 264.7 cells and mice erythrocytes) and in vivo (acute toxicity in mice). The Ehrlich ascites carcinoma model was used to evaluate the antitumor activity of HE-02 (6.25, 12.5 or 25 mg/kg, intraperitoneally, i.p.), as well as toxicity. HE-02 induced only 5.01% of hemolysis, and reduced the viability of RAW 264.7 cells by 49.75% at 1000 µg/mL. LD50 (lethal dose 50%) was estimated at around 2000 mg/kg (i.p.). HE-02 reduced Ehrlich tumor cell viability and peritumoral microvessels density. There was an increase of Th1 helper T lymphocytes cytokine profile levels (IL-1β, TNF-α, IL-12) and a decrease of Th2 cytokine profile (IL-4, IL-10). Moreover, an increase was observed on reactive oxygen species and nitric oxide production. Weak in vivo toxicological effects were recorded. Our data provide evidence that the piperine analogue HE-02 present low toxicity, and its antitumor effect involves modulation of immune system to a cytotoxic Th1 profile.


2020 ◽  
Vol 15 (4) ◽  
pp. 341-359
Author(s):  
Moloud Kazemi ◽  
Jaber Emami ◽  
Farshid Hasanzadeh ◽  
Mohsen Minaiyan ◽  
Mina Mirian ◽  
...  

Background: The development of biocompatible tumor-targeting delivery systems for anticancer agents is essential for efficacious cancer chemotherapy. Nanoparticles, as drug delivery cargoes for cancer therapy, are rapidly improving to overcome the limitations of conventional chemotherapeutic agents. Heparin–modified nanoparticles are currently being considered as one of the favorable carriers for the delivery of chemotherapeutics to cancer tissues. Objective: This study was aimed at evaluating the in vitro and in vivo antitumor activity of a novel targeted, pH-sensitive, heparin-based polymeric micelle loaded with the poorly water-soluble anticancer drug, docetaxel (DTX). The micelles could overcome the limited water solubility, non-specific distribution, and insufficient drug concentration in tumor tissues. Methods: DTX-loaded folate targeted micelles were prepared and evaluated for physicochemical properties, drug release, in vitro cellular uptake and cytotoxicity in folate receptor-positive and folate receptor-negative cells. Furthermore, the antitumor activity of DTX-loaded micelles was evaluated in the tumor-bearing mice. Some related patents were also studied in this research. Results: The heparin-based targeted micelles exhibited higher in vitro cellular uptake and cytotoxicity against folate receptor over-expressed cells due to the specific receptor-mediated endocytosis. DTX-loaded micelles displayed greater antitumor activity, higher anti-angiogenesis effects, and lower systemic toxicity compared with free DTX in a tumor-induced mice model as confirmed by tumor growth monitoring, immunohistochemical evaluation, and body weight shift. DTX-loaded targeting micelles demonstrated no considerable toxicity on major organs of tumor-bearing mice compared with free DTX. Conclusion: Our results indicated that DTX-loaded multifunctional heparin-based micelles with desirable antitumor activity and low toxicity possess great potential as a targeted drug delivery system in the treatment of cancer.


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