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Polyethylene Glycol Polyester Block Copolymers: Biocompatible Carriers for Nanoparticulate Drug Delivery
Published in Dan Peer, Handbook of Harnessing Biomaterials in Nanomedicine, 2021
David S. Hart, Yunqi Zhao, M. Laird Forrest
Flory–Huggins interaction parameters have been employed to evaluate the thermodynamic affinity of geldanamycin prodrugs, among other anti-cancer agents for PCL cores [33]. Geldanamycin (GA) (Figure 3.3) is known to inhibit the ATP binding pocket of Hsp90, which reduces a cancer cells ability to refold essential proteins and eventually survive. The interaction parameter analysis facilitated the design of a novel type of prodrug, and illustrated how increasing lipophilicity of a target drug can increase the micelle loading capacity, and ultimately the aqueous solubility. Using functional group contributions of the drug and PCL chain, partial solubility parameters were estimated, and Flory–Huggins interaction parameter was calculated. When this interaction parameter approaches zero, the PCL chain is completely solvated with drug. A series of GA derivatives were synthesized with varying lengths of aliphatic chains at the 17′ position, and were evaluated with MCF-7 breast cancer cells to gauge the potency relative to GA. Most of these derivatives cytotoxicity was reduced at least an order of magnitude, however one bromoester derivative, 17-(ethylamino-2-bromododeconate)-17-demethoxygeldanamycin (GA 17′ C16Br) (Figure 3.3) IC50 reduced by only a factor of 5 (110 nM). As shown in Figure 3.3b, the ethylamine ester at the 17′ position will hydrolyze in vivo to activate the drug, and the addition of the electron withdrawing group (Br) increases the lability of the ester bond, decreasing the half-life.
Green synthesis of silver nanoparticles using Macrolepiota procera extract and investigation of their HSP27, HSP70, and HSP90 inhibitory potentials in human cancer cells
Published in Particulate Science and Technology, 2023
Aykut Özgür, Özlem Kaplan, Nazan Gökşen Tosun, İbrahim Türkekul, İsa Gökçe
MP-AgNPs showed a potent cytotoxic effect against MCF-7, A549, Saos-2, and HT-29 cell lines in a dose-dependent manner. Geldanamycin is benzoquinone-containing annamycin antibiotic which has anticancer potentials by inhibiting HSP90 chaperone activity in cancer cells. In the literature, geldanamycin exhibited anti-proliferative activity in wide variety of cancer cells and IC50 values were calculated range from 10 to 410 ng/ml (Li et al. 2019). When the IC50 values of the MP-AgNPs and geldanamycin were compared, the synthesized MP-AgNPs showed potential anticancer properties against MCF-7, A549, Saos-2, and HT-29 cell lines at nM concentrations.