Abstract

Berberine (BBR), a natural isoquinoline alkaloid derived from Chinese herbs, exerts many biological effects, including antiviral, antimicrobial, antidiarrhea, anti-inflammatory, and antitumor effects. In this study, a novel berberine nanoparticle (NP) consisting of heparin (HP) and BBR with or without being shelled with linear polyethyleneimine (LPEI) was developed to enhance its antitumor activity on osteosarcoma U-2 OS cells. With varying ratios of HP to BBR, HP/BBR NPs had a size ranging from 218.4 ± 3.9 to 282.0 ± 5.1 nm and zeta potential from −35.7 ± 0.4 to −51.9 ± 1.8 mV. After shelling with LPEI, the resultant NPs (HP/BBR/LPEI) possessed a size ranging from 226.3 ± 3.0 to 405.7 ± 85.2 nm and zeta potential from −46.5 ± 0.3 to −35.6 ± 0.5 mV; the encapsulation rate of BBR was close to 80%. The release profiles of both NPs were revealed to be slower than that of BBR solution. Results also showed that BBR and its two derived NPs reduced the viability of U-2 OS cells, and BBR NPs increased the cellular uptake of BBR. Cells were arrested at the G1 phase when treated individually with BBR and the two NPs (HP/BBR and HP/BBR/LPEI) and DNA condensation was induced. In addition, BBR and BBR NPs reduced the expression of mouse double minute 2 homolog (MDM2) but increased that of p53, and BBR NPs enhanced apoptotic effects. In short, heparin-based nanoparticles could be potential carriers for osteosarcoma treatment.

Highlights

  • Berberine (BBR) is a natural isoquinoline alkaloid derived from Chinese herb plants includingCoptis chinensis, Berberis aquifolium, Berberis vulgaris, and Coscinium fenestratum [1]

  • Silica nanoconjugates bearing a covalently linked BBR enhanced apoptosis cell death in a human cervical carcinoma cell line (HeLa), a human hepatocellular carcinoma cell line (Hep G2), and human embryonic kidney (HEK) 293T cell lines when compared with cells treated with BBR [23]

  • The HP/BBR/linear PEI (LPEI) NPs were designed to decrease the rate of drug release and enhance cellular uptake and apoptosis effects

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Summary

Introduction

Berberine (BBR) is a natural isoquinoline alkaloid derived from Chinese herb plants includingCoptis chinensis, Berberis aquifolium, Berberis vulgaris, and Coscinium fenestratum [1]. Berberine (BBR) is a natural isoquinoline alkaloid derived from Chinese herb plants including. BBR has been shown to inhibit the proliferation of cancer cells [10,11] and HER2-overexpressing breast cancer cells [12] and to induce cell cycle arrest [13,14]. The clinical applications of BBR are handicapped by its poor absorption and bioavailability. BBR is poorly absorbed in the gastrointestinal tract, resulting in poor bioavailability [1,17,18]. To overcome this shortcoming, nanoparticle-mediated delivery systems have been developed for new therapeutic strategies [19].

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