scholarly journals Cyclodextrin Polymers as Delivery Systems for Targeted Anti-Cancer Chemotherapy

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 6046
Author(s):  
Noemi Bognanni ◽  
Maurizio Viale ◽  
Alessia Distefano ◽  
Rita Tosto ◽  
Nadia Bertola ◽  
...  

In the few last years, nanosystems have emerged as a potential therapeutic approach to improve the efficacy and selectivity of many drugs. Cyclodextrins (CyDs) and their nanoparticles have been widely investigated as drug delivery systems. The covalent functionalization of CyD polymer nanoparticles with targeting molecules can improve the therapeutic potential of this family of nanosystems. In this study, we investigated cross-linked γ- and β-cyclodextrin polymers as carriers for doxorubicin (ox) and oxaliplatin (Oxa). We also functionalized γ-CyD polymer bearing COOH functionalities with arginine-glycine-aspartic or arginine moieties for targeting the integrin receptors of cancer cells. We tested the Dox and Oxa anti-proliferative activity in the presence of the precursor polymer with COOH functionalities and its derivatives in A549 (lung, carcinoma) and HepG2 (liver, carcinoma) cell lines. We found that CyD polymers can significantly improve the antiproliferative activity of Dox in HepG2 cell lines only, whereas the cytotoxic activity of Oxa resulted as enhanced in both cell lines. The peptide or amino acid functionalized CyD polymers, loaded with Dox, did not show any additional effect compared to the precursor polymer. Finally, studies of Dox uptake showed that the higher antiproliferative activity of complexes correlates with the higher accumulation of Dox inside the cells. The results show that CyD polymers could be used as carriers for repositioning classical anticancer drugs such as Dox or Oxa to increase their antitumor activity.

2020 ◽  
Vol 17 ◽  
Author(s):  
W. Abd El-Fattah

: In this work, 1,2,4-triazine derivatives were synthesized and evaluated for anticancer activities. Series of 1,2,4-triazine derivatives (4a, b) were prepared via the reaction of N-benzoyl glycine (1) with aromatic aldehydes in presence of fused sodium acetate and acetic anhydride to give 1,3-oxazolinone derivatives (2a, b), followed by condensation with 1-(ethoxycarbonyl) hydrazine (3) in glacial acetic acid. Compounds (4a, b) then reacted with acetic anhydride, ethyl chloroacetate and 2,4-dinitrophenyl hydrazine yielded the corresponding to N-acetyl derivatives (5a, b), N-(ethoxycarbonyl) methyl derivative (6) and 1,2-disubstituted hydrazine (7), respectively. The structures of the 1,2,4-triazine derivatives were confirmed by IR, 1H, 13C NMR, MS and elemental analyses. Anticancer activity of some 1,2,4-triazine derivatives (4-7) have been investigated. The results revealed that compounds 4a (IC50= 2.7μM), 5a (IC50= 1.5μM), and 5b (IC50= 3.9μM) show promising inhibitory growth efficacy compared to a standard antitumor drug (IC50= 4.6μM). These three compounds can be considered as potential agents against human hepatocellular carcinoma cell lines (HepG-2).


2021 ◽  
Author(s):  
Malini Devi Raman Ramarao ◽  
Ong Ming Thong ◽  
Sunderasan Elumalai

Exploration of the constituents of rubber for medicinal application is very limited due to the concern of allergenicity. However, the recent discovery of the ability of latex sera to exert specific antiproliferative activity against cancer-origin cell lines has paved a light of utilising rubber latex as therapeutics. Rubber latex and its seed oil show many potentials in various biological activities such as antifungal, antioxidant, anti-melanogenesis as well as a biomaterial in relation to angiogenesis. This review describes the current scientifically reported progress on the potential use of rubber in the field of medical research plus positive side concerning latex allergenicity.


2009 ◽  
Vol 44 (6) ◽  
pp. 2736-2740 ◽  
Author(s):  
Sau Hing Chan ◽  
Kim Hung Lam ◽  
Chung Hin Chui ◽  
Roberto Gambari ◽  
Marcus Chun Wah Yuen ◽  
...  

2011 ◽  
Vol 285 (4) ◽  
pp. 1145-1151 ◽  
Author(s):  
Sibylle Abarzua ◽  
Tatsuo Serikawa ◽  
Marlen Szewczyk ◽  
Dagmar-Ulrike Richter ◽  
Birgit Piechulla ◽  
...  

2017 ◽  
Vol 4 (S) ◽  
pp. 86
Author(s):  
John Paul Tosoc

C. olitorius are used as herbal medicine and eaten as vegetable by local people in Philippines.  The T’boli tribe commonly uses this plant to treat common illnesses such as pimples, wounds, boils, and inflammations. According to studies, the leaves of C. olitorius has properties to treat demulcent, diuretic, febrifuge, chronic cystitis, dysuria and even tumor. The aim of this study is to evaluate the cytotoxicity properties of the crude aqueous extract of C. olitorius leaf against colon (HCT116), breast (MCF-7), and liver (HepG2) carcinoma cell-lines using the MTT cell proliferation assay. The results showed that the aqueous extract has potential cytotoxicity activity against the three-carcinoma cell-lines. The aqueous extract was most bioactive in the colon carcinoma cell-line (HCT116) with cell viability percentage of 23.53 and 32.48 in 100 and 10 µg/mL, respectively. It was then followed by the breast carcinoma cell-line (MCF7) with cell viability percentage of 16.23 and 30.25 in 100 and 10 µg/mL, respectively. The extract was least but still bioactive in the liver carcinoma cell-line (HepG2) with cell viability percentage of 91.20 and 132.76 in 100 and 10 µg/mL, respectively. This study illustrates the importance of toxicological screening to confirm the safety and efficacy of the medicinal plant commonly used in the traditional medicine system in the treatment and management of illnesses by the T’boli tribe in South Cotabato


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