The Assessment of Bioreductive Drug Toxicity in vitro and in Experimental Tumours in vivo

Author(s):  
I. J. Stratford ◽  
G. E. Adams ◽  
J. C. M. Bremner ◽  
S. Cole ◽  
Li Ding ◽  
...  
2011 ◽  
Vol 145 (2_suppl) ◽  
pp. P77-P78
Author(s):  
Joseph Knowles ◽  
Anna Sorace ◽  
C. Hope Heath ◽  
Will Lancaster ◽  
Eben L. Rosenthal ◽  
...  

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 202
Author(s):  
Lan Zhang ◽  
Min Yan ◽  
Kun Chen ◽  
Qikang Tian ◽  
Junying Song ◽  
...  

A new platform for triptolide (TP) delivery was prepared by conjugating TP to a carboxylmethyl chitosan (CMCS). Compared with the natural TP, the TP-conjugate (TP-CMCS) containing TP of ~5 wt% exhibited excellent aqueous solubility (>5 mg/mL). Results of in vitro experiments showed that TP-CMCS could relieve TP-induced inhibition on RAW264.7 cells and apoptosis, respectively. Compared with the TP group, TP-CMCS could effectively alleviate the toxicity injury of TP and decreased the mortality rate of the mice (p < 0.05). TP-CMCS did not cause much damage to the liver (AST and ALT) and kidney (BUN and CRE) (p < 0.05). After administration, the levels of IL-6, IL-1β, and TNF-α decreased, and the arthritis detumescence percentages increased significantly, and the bony erosion degree was distinctly decreased in the TP-CMCS groups and TP group. Our results suggested that TP-CMCS was a useful carrier for the treatment of RA, which enhanced aqueous solubility of free TP and reduced drug toxicity in vitro and in vivo.


Author(s):  
Ya-Nan Li ◽  
Ni Ning ◽  
Lei Song ◽  
Yun Geng ◽  
Jun-Ting Fan ◽  
...  

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.


1987 ◽  
Vol 14 (3) ◽  
pp. 166-167
Author(s):  
D. Arenholt-Bindslev ◽  
P. Hørsted-Bindslev ◽  
H.P. Philipsen

The aim of the present study was to compare the toxicity in vitro with the toxicity in vivo of two commercial chemicals marketed for use in the oral cavity (GLUMA BondR and 3M Etching LiquidR). Confluent cultures of human buccal epithelial cells were exposed to graded concentrations of GLUMA Bond or 3M Etching Liquid for 5 minutes. The cytotoxic effects induced by this treatment were observed (cytomorphology, proliferation rate). In vivo, monkey buccal epithelium was exposed to GLUMA Bond or 3M Etching Liquid for 5 minutes. Biopsies were taken after 24 hours, and the buccal epithelium processed for light microscopical examination. In both models, the toxic reactions to GLUMA Bond were far more extensive than those caused by 3M Etching Liquid.


2021 ◽  
pp. 088532822110038
Author(s):  
Mohammad Yousef Memar ◽  
Mina Yekani ◽  
Hadi Ghanbari ◽  
Edris Nabizadeh ◽  
Sepideh Zununi Vahed ◽  
...  

The aims of the present study were the determination of antimicrobial and antibiofilm effects of meropenem-loaded mesoporous silica nanoparticles (MSNs) on carbapenem resistant Pseudomonas aeruginosa ( P. aeruginosa) and cytotoxicity properties in vitro. The meropenem-loaded MSNs had shown antibacterial and biofilm inhibitory activities on all isolates at different levels lower than MICs and BICs of meropenem. The viability of HC-04 cells treated with serial concentrations as MICs and BICs of meropenem-loaded MSNs was 92–100%. According to the obtained results, meropenem-loaded MSNs display the significant antibacterial and antibiofilm effects against carbapenem resistant and biofilm forming P. aeruginosa and low cell toxicity in vitro. Then, the prepared system can be an appropriate option for the delivery of carbapenem for further evaluation in vivo assays.


2016 ◽  
pp. 2663 ◽  
Author(s):  
Qianqian Liang ◽  
Li Zhang ◽  
Tengteng Wang ◽  
Qiang Li ◽  
Jing Huang ◽  
...  

2017 ◽  
Vol 2017 ◽  
pp. 1-16 ◽  
Author(s):  
Lígia N. M. Ribeiro ◽  
Ana C. S. Alcântara ◽  
Gustavo H. Rodrigues da Silva ◽  
Michelle Franz-Montan ◽  
Silvia V. G. Nista ◽  
...  

The use of biomaterials composed of organic pristine components has been successfully described in several purposes, such as tissue engineering and drug delivery. Drug delivery systems (DDS) have shown several advantages over traditional drug therapy, such as greater therapeutic efficacy, prolonged delivery profile, and reduced drug toxicity, as evidenced by in vitro and in vivo studies as well as clinical trials. Despite that, there is no perfect delivery carrier, and issues such as undesirable viscosity and physicochemical stability or inability to efficiently encapsulate hydrophilic/hydrophobic molecules still persist, limiting DDS applications. To overcome that, biohybrid systems, originating from the synergistic assembly of polymers and other organic materials such as proteins and lipids, have recently been described, yielding molecularly planned biohybrid systems that are able to optimize structures to easily interact with the targets. This work revised the biohybrid DDS clarifying their advantages, limitations, and future perspectives in an attempt to contribute to further research of innovative and safe biohybrid polymer-based system as biomaterials for the sustained release of active molecules.


2021 ◽  
Author(s):  
Guofang Zhang ◽  
Yalin Cong ◽  
Guoli Cao ◽  
Liang Li ◽  
Peng Yu ◽  
...  

The global emergency caused by the SARS-CoV-2 pandemics can only be solved with adequate preventive and therapeutic strategies, both currently missing. The electropositive Receptor Binding Domain (RBD) of SARS-CoV-2 spike protein with abundant β-sheet structure serves as target for COVID-19 therapeutic drug design. Here, we discovered that ultrathin 2D CuInP2S6 (CIPS) nanosheets as a new agent against SARS-CoV-2 infection, which also able to promote viral host elimination. CIPS exhibits extremely high and selective binding capacity with the RBD of SARS-CoV-2 spike protein, with consequent inhibition of virus entry and infection in ACE2-bearing cells and human airway epithelial organoids. CIPS displays nano-viscous properties in selectively binding with spike protein (KD < 1 pM) with negligible toxicity in vitro and in vivo. Further, the CIPS-bound SARS-CoV-2 was quickly phagocytosed and eliminated by macrophages, suggesting CIPS could be successfully used to capture and facilitate the virus host elimination with possibility of triggering anti-viral immunization. Thus, we propose CIPS as a promising nanodrug for future safe and effective anti-SARS-CoV-2 therapy, as well as for use as disinfection agent and surface coating material to constrain the SARS-CoV-2 spreading.


1994 ◽  
Vol 102 ◽  
pp. 247 ◽  
Author(s):  
Nobuyuki Susa ◽  
Shunji Ueno ◽  
Yoshinori Furukawa

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