Stimuli-responsive heparin-drug conjugates co-assembled into stable nanomedicines for cancer therapy

Fang, Zaixiang; Li, Gang; Li, Zhiqian; Gu, Ling; Pan, Dayi; Li, Yunkun; Chen, Jie; Ding, Haitao; Tian, Xiaohe; Gong, Qiyong; Luo, Kui

doi:10.1016/j.actbio.2023.04.016

Cited by 7 publications

(1 citation statement)

References 56 publications

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“…This chemical modification reduces the binding affinity of LMWHs for antithrombin and blocks angiogenic factors involved in the initial angiogenesis (VEGF and FGF2) and the primitive stabilization of the endothelial vascular network (platelet-derived growth factor subunit B) to inhibit multiple stages of angiogenesis, which directly leads to decreased blood perfusion throughout the tumor and inhibition of tumor growth. Due to the high expression of heparinase in tumor tissues and the fact that heparin can be specifically degraded in the tumor region, Zaixiang Fang et al synthesized heparin–paclitaxel and heparin–pyrophosphopyridine and then co-assembled the two couplings into a nanomedicine [ 101 ]. The nanoparticles increased the accumulation of pyrophosphopyridine by 11-fold in tumors and inhibited the tumor growth of 4T1-loaded tumor-bearing mice by up to 98.1%, with no systemic toxicity.…”

Section: Various Heparin Conjugates With Non-coagulant Effectsmentioning

confidence: 99%

Non-Anticoagulant Activities of Low Molecular Weight Heparins—A Review

Feng,

Wang,

Zhou

et al. 2023

Pharmaceuticals

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Low molecular weight heparins (LMWHs) are derived from heparin through chemical or enzymatic cleavage with an average molecular weight (Mw) of 2000–8000 Da. They exhibit more selective activities and advantages over heparin, causing fewer side effects, such as bleeding and heparin-induced thrombocytopenia. Due to different preparation methods, LMWHs have diverse structures and extensive biological activities. In this review, we describe the basic preparation methods in this field and compare the main principles and advantages of these specific methods in detail. Importantly, we focus on the non-anticoagulant pharmacological effects of LMWHs and their conjugates, such as preventing glycocalyx shedding, anti-inflammatory, antiviral infection, anti-fibrosis, inhibiting angiogenesis, inhibiting cell adhesion and improving endothelial function. LMWHs are effective in various diseases at the animal level, including cancer, some viral diseases, fibrotic diseases, and obstetric diseases. Finally, we briefly summarize their usage and potential applications in the clinic to promote the development and utilization of LMWHs.

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Section: Various Heparin Conjugates With Non-coagulant Effectsmentioning

confidence: 99%