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DQAsomes as Mitochondria-Targeted Nanocarriers for Anti-Cancer Drugs
Published in Mansoor M. Amiji, Nanotechnology for Cancer Therapy, 2006
Shing-Ming Cheng, Sarathi V. Boddapati, Gerard G. M. D’Souza, Volkmar Weissig
Dequalinium is a dicationic compound resembling “bola”-form electrolytes, i.e., it is a symmetrical molecule with two charge centers separated at a relatively large distance. Such symmetric bola-like structures are well known from archaeal lipids that usually consist of two glycerol backbones connected by two hydrophobic chains.85,86 The self-assembly behavior of bipolar lipid from Archaea has been extensively studied (reviewed in Gambacorta, Gliozi, and De Rosa 1995). Generally, it has been shown that these symmetric bipolar archaeal lipids can self-associate into mechanically, very stable monolayer membranes. The most striking structural difference between dequalinium and archaeal lipids lies in the number of bridging hydrophobic chains between the polar head groups. Contrary to the common arachaeal lipids, in dequalinium there is only one carbohydrate chain that connects the two cationic hydrophilic head groups. Therefore, this type of bola lipids has been named single-chain bola-amphiphile.87,88 The self-association behavior of this single-chain cationic bola amphiphile was investigated using Monte Carlo computer simulations (Figure 38.1c, left panel),83 several electron microscopic (EM) techniques (Figure 38.1c, right panel) as well as dynamic laser light scattering.84
Dequalinium chloride use in adult Spanish women with bacterial vaginosis: an observational study
Published in Journal of Obstetrics and Gynaecology, 2022
Jordi Antoni Vives, María Jesús Cancelo, Miguel Ángel Losada, Alejandro Doménech
Current treatment guidelines recommend the use of antibiotics metronidazole and clindamycin, which have proven efficient in the short-term control of BV symptoms (Centers for Disease Control and Prevention 2015; Spanish Gynecology and Obstetrics Society 2018). In the current setting of a rational use of antibiotics, antiseptic agents such as dequalinium chloride (DQC) are considered an effective option in treating different vaginal infections, including BV (Verstraelen et al. 2012; Donders et al. 2014; Mendling et al. 2016). DQC is a compound that exerts a broad bactericidal (both gram-positive and gram-negative) and fungicidal activity. Its mechanism of action is based on its ability to disrupt cell permeability and its effects on protein denaturation, mitochondrial electron transport chain and protein synthesis. This multiple mechanism of action implies that pathogen resistance is not to be expected as is the case of antibiotics. It is also well tolerated and safe due to a low systemic absorption.
Mitochondrial delivery of microRNA mimic let-7b to NSCLC cells by PAMAM-based nanoparticles
Published in Journal of Drug Targeting, 2020
Niloufar Maghsoudnia, Reza Baradaran Eftekhari, Alireza Naderi Sohi, Parisa Norouzi, Hamid Akbari, Mohammad Hossein Ghahremani, Masoud Soleimani, Mohsen Amini, Hamed Samadi, Farid Abedin Dorkoosh
In a similar study, HA was electrostatically capped to mesoporous silica nanoparticles (MSN) containing doxorubicin to target CD44 receptors in cancer cells resulting in efficient uptake by CD44 receptor-mediated endocytosis. TPP was also grafted to MSN to provide mitochondria targeting of doxorubicin for effective therapy [31]. In another work, liposomes containing paclitaxel were decorated with HA using electrostatic absorption. Dequalinium as mitochondrial targeting moiety was employed to specifically guide the liposomes to the mitochondria in A549 cells. The results revealed that HA could specifically bind the overexpressed CD44 on A549 cells and increased the cellular uptake of the lipososmes [32]. Similar results were observed in a study conducted by Kaili Wang et al. in which drug-loaded nanoparticles, composed of HA and TPP were demonstrated to specifically target CD44 receptors and accumulate within the cells mitochondria [33]
Functional paclitaxel plus honokiol micelles destroying tumour metastasis in treatment of non-small-cell lung cancer
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Xin Wang, Lan Cheng, Hong-Jun Xie, Rui-Jun Ju, Yao Xiao, Min Fu, Jing-Jing Liu, Xue-Tao Li
Dequalinium (DQA) is a quaternary ammonium cation. As a kind of mitochondrial-targeted drug, DQA can selectively accumulated in the mitochondria of cancer cells. Some previous studies had demonstrated that the modification of DQA on the liposomal surface could increase the cellular uptake by electrostatic interactions [14,15]. Honokiol is an active natural extract of traditional Chinese herb Magnolia offcinalis, and it is widely used as a supplementary functional drug in treatment of cancer for the various biological properties such as inhibiting the VM channels, suppressing the invasion of cancer cells and reducing the adhesion rate between cancer cells and body environment [16,17]. Paclitaxel is one of the most effective chemotherapy drugs for treating various kinds of cancer. The underlying mechanism for the cytotoxicity of paclitaxel is mainly from binding tubulin and stabilizing microtubules. These stable microtubules inhibit the division of cancer cells at the G2/M phase of cell cycle [18,19]. Therefore, the combination of paclitaxel plus honokiol was considered for the preparation of micelles. In this way, the proliferation of lung cancer cells was restricted by paclitaxel, and cellular metastases and VM channels were suppressed by honokiol in the meanwhile. This combination fundamentally solved the problem of tumor metastasis which was inevitable for traditional chemotherapy when killing cancer cells.