anticancer drug
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2022 ◽  
Vol 12 (2) ◽  
pp. 879
Author(s):  
Suleiman Nafiu ◽  
Vitus Atanga Apalangya ◽  
Abu Yaya ◽  
Edward Benjamin Sabi

The electrical properties and characteristics of the armchair boron nitride nanotube (BNNT) that interacts with the curcumin molecule as an anticancer drug were studied using ab initio calculations based on density functional theory (DFT). In this study, a (5,5) armchair BNNT was employed, and two different interactions were investigated, including the interaction of the curcumin molecule with the outer and inner surfaces of the BNNT. The adsorption of curcumin molecules on the investigated BNNT inside the surface is a more favorable process than adsorption on the outside surface, and the more persistent and stronger connection correlates with curcumin molecule adsorption in this case. Furthermore, analysis of the HOMO–LUMO gap after the adsorption process showed that the HOMO value increased marginally while the LUMO value decreased dramatically in the curcumin-BNNT complexes. As a result, the energy gaps between HOMO and LUMO (Eg) are narrowed, emphasizing the stronger intermolecular bonds. As a result, BNNTs can be employed as a drug carrier in biological systems to transport curcumin, an anticancer medication, and thereby improve its bioavailability.


Author(s):  
Ahmet Cetinkaya ◽  
Leyla Karadurmus ◽  
S. Irem Kaya ◽  
Goksu Ozcelikay ◽  
Sibel A. Ozkan

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Naresh Kumar ◽  
Nidhi Goel

Abstract Cancer, one of the key health problems globally, is a group of related diseases that share a number of characteristics primarily the uncontrolled growth and invasive to surrounding tissues. Chemotherapy is one of the ways for the treatment of cancer which uses one or more anticancer agents as per chemotherapy regimen. Limitations of most anticancer drugs due to a variety of reasons such as serious side effects, drug resistance, lack of sensitivity and efficacy etc. generate the necessity towards the designing of novel anticancer lead molecules. In this regard, the synthesis of biologically active heterocyclic molecules is an appealing research area. Among heterocyclic compounds, nitrogen containing heterocyclic molecules has fascinated tremendous consideration due to broad range of pharmaceutical activity. Imidazoles, extensively present in natural products as well as synthetic molecules, have two nitrogen atoms, and are five membered heterocyclic rings. Because of their countless physiological and pharmacological characteristics, medicinal chemists are enthused to design and synthesize new imidazole derivatives with improved pharmacodynamic and pharmacokinetic properties. The aim of this present chapter is to discuss the synthesis, chemistry, pharmacological activity, and scope of imidazole-based molecules in anticancer drug development. Finally, we have discussed the current challenges and future perspectives of imidazole-based derivatives in anticancer drug development.


Author(s):  
Shervin Dokht Farhangfar ◽  
Farzaneh Fesahat ◽  
Sayed Mohsen Miresmaeili ◽  
Hadi Zare-Zardini

Background: Gensenoside Rh2 is an anticancer drug with low toxicity and stability in the body. The aim of this study was to evaluate the blood toxicity of functionalized graphene-arginine with anticancer drug ginsenoside Rh2 in balb/c mouse model with breast cancer. Materials and Methods: Graphene-Arginine (G-Arg) and Graphene-Arginine-ginsenoside Rh2 (G-Arg-Rh2) were synthesized using microwave method. For evaluation of blood toxicity, 32 mice with breast tumors were randomly divided into 4 groups: control (3mg/kg 6 mg / kg PBS sterile), group 1 (6 mg / kg ginsenoside), group 2 (3 mg / kg G-Arg), and group 3 (3 mg / kg G-Arg-Rh2). Treatment was done intravenously once every three days for 32 days. Finally, blood factors were also examined by sampling from the heart. Results: Complete functionalization was proven by FTIR and Raman. Examination of blood factors showed that white blood cells had a very small increase. Anova test showed significant difference among four groups in term of WBC count (p=0.016). Pair sample T test showed that there was significant difference between control and group 1(p=0.036) and control and group 2 (p=0.036). There was no significant difference between control and group 3 (p=0.051). Other blood factors had no significant difference among examined groups (p>0.05). Conclusion: Based on results, after treatment with all designed nanostructures, only white blood cells had a very small increase and inflammatory reactions were statistically similar in all groups. This indicates the high efficiency of designed drug.


Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 169
Author(s):  
Javier Pérez Quiñones ◽  
Cornelia Roschger ◽  
Aitziber Iturmendi ◽  
Helena Henke ◽  
Andreas Zierer ◽  
...  

The design and study of efficient polymer-based drug delivery systems for the controlled release of anticancer drugs is one of the pillars of nanomedicine. The fight against metastatic and invasive cancers demands therapeutic candidates with increased and selective toxicity towards malignant cells, long-term activity and reduced side effects. In this sense, polyphosphazene nanocarriers were synthesized for the sustained release of the anticancer drugs camptothecin (CPT) and epirubicin (EPI). Linear poly(dichloro)phosphazene was modified with lipophilic tocopherol or testosterone glycinate, with antioxidant and antitumor activity, and with hydrophilic Jeffamine M1000 to obtain different polyphosphazene nanocarriers. It allowed us to encapsulate the lipophilic CPT and the more hydrophilic EPI. The encapsulation process was carried out via solvent exchange/precipitation, attaining a 9.2–13.6 wt% of CPT and 0.3–2.4 wt% of EPI. CPT-loaded polyphosphazenes formed 140–200 nm aggregates in simulated body physiological conditions (PBS, pH 7.4), resulting in an 80–100-fold increase of CPT solubility. EPI-loaded polyphosphazenes formed 250 nm aggregates in an aqueous medium. CPT and EPI release (PBS, pH 7.4, 37 °C) was monitored for 202 h, being almost linear during the first 8 h. The slow release of testosterone and tocopherol was also sustained for 150 hours in PBS (pH 7.4 and 6.0) at 37 °C. The co-delivery of testosterone or tocopherol and the anticancer drugs from the nanocarriers was expected. Cells of the human breast cancer cell line MCF-7 demonstrated good uptake of anticancer-drug-loaded nanocarriers after 6 hours. Similarly, MCF-7 spheroids showed good uptake of the anticancer-drug-loaded aggregates after 72 hours. Almost all anticancer-drug-loaded polyphosphazenes exhibited similar or superior toxicity against MCF-7 cells and spheroids when compared to raw anticancer drugs. Additionally, cell-cycle arrest in the G2/M phase was increased in response to the drug-loaded nanocarriers. Almost no toxicity of anticancer-drug-loaded aggregates against primary human lung fibroblasts was observed. Furthermore, the aggregates displayed no hemolytic activity, which is in contrast to the parent anticancer drugs. Consequently, synthesized polyphosphazene-based nanocarriers might be potential nanomedicines for chemotherapy.


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