Cellular delivery and enhanced anticancer activity of berberine complexed with a cationic derivative of γ–cyclodextrin

Popiołek, Iwona; Niziołek, Anna; Kamiński, Kamil; Kwolek, Urszula; Nowakowska, Maria; Szczubiałka, Krzysztof

doi:10.1016/j.bmc.2019.02.042

Cited by 23 publications

(9 citation statements)

References 37 publications

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“…It is worth reiterating that poor intestinal absorption, extensive efflux by the action of P-gc and extensive degradation account to the rather poor bioavailability/pharmacokinetics profile of berberine. The various formulation approaches specifically designed to tackle this problem and improve berberine's anticancer efficacy are shown in Table 2 [106][107][108][109][110][111][112][113][114][115][116][117][118][119][120][121][122][123]. These include nanoparticles of various sizes and surface charges with some specifically targeting subcellular organelles, such as the mitochondria.…”

Section: Enhancement Of Berberine's Anticancer Effect Via Formulationmentioning

confidence: 99%

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Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization

Habtemariam

2020

Molecules

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Berberine is multifunctional natural product with potential to treat diverse pathological conditions. Its broad-spectrum anticancer effect through direct effect on cancer cell growth and metastasis have been established both in vitro and in vivo. The cellular targets that account to the anticancer effect of berberine are incredibly large and range from kinases (protein kinase B (Akt), mitogen activated protein kinases (MAPKs), cell cycle checkpoint kinases, etc.) and transcription factors to genes and protein regulators of cell survival, motility and death. The direct effect of berberine in cancer cells is however relatively weak and occur at moderate concentration range (10–100 µM) in most cancer cells. The poor pharmacokinetics profile resulting from poor absorption, efflux by permeability-glycoprotein (P-gc) and extensive metabolism in intestinal and hepatic cells are other dimensions of berberine’s limitation as anticancer agent. This communication addresses the research efforts during the last two decades that were devoted to enhancing the anticancer potential of berberine. Strategies highlighted include using berberine in combination with other chemotherapeutic agents either to reduce toxic side effects or enhance their anticancer effects; the various novel formulation approaches which by order of magnitude improved the pharmacokinetics of berberine; and semisynthetic approaches that enhanced potency by up to 100-fold.

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Section: Enhancement Of Berberine's Anticancer Effect Via Formulationmentioning

confidence: 99%

“…Popiołek et al [110] PLGA nanoparticles PLGA-doxorubicin conjugate used for encapsulation of berberine.…”

Section: Suganthi Et Al [109]mentioning

confidence: 99%

Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization

Habtemariam

2020

Molecules

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“…The experiment was carried out for 24 h after adding HBC to cell media. To assess cell viability, Crystal Violet (CV) assay was used (Popiołek et al, 2019). Briefly, cells were seeded into 24-well plates at the density of about 1.1•10 4 cells/cm 2 .…”

Section: Dynamic Light Scattering (Dls) Measurementsmentioning

confidence: 99%

Heparin-Binding Copolymer as a Complete Antidote for Low-Molecular-Weight Heparins in Rats

Kałaska

Mikłosz

Kamiński

et al. 2020

J Pharmacol Exp Ther

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Bleeding resulting from the application of low-molecular-weight heparins (LMWHs) may be treated with protamine sulfate but lacks efficiency; its action against anti-factor Xa activity is limited to ~60%. Moreover, protamine sulfate can cause life-threatening hypersensitivity reactions. We developed diblock heparin-binding copolymer (HBC) that can neutralize the anticoagulant activity of parenteral anticoagulants. In the present study, we explored the safety profile of HBC and its potential to reverse enoxaparin, nadroparin, dalteparin, and tinzaparin in human plasma and at in vivo conditions. HBC-LMWHs complexes were characterized using zeta potential, isothermal titration calorimetry, and dynamic light scattering. The rat cardiomyocytes and human endothelial cells were used for the assessment of in vitro toxicity. Male Wistar rats were observed for up to 4 days after HBC administration for clinical evaluation, gross necropsy, and biochemistry and histopathological analysis. Rats were treated with LMWHs alone or followed by short-time intravenous infusion of HBC, and bleeding time and anti-factor Xa activity were measured. HBC completely reversed anti-factor Xa activity prolonged in vitro by all LMWHs with an optimal weight ratio of 2.5:1. The complexes of HBC-LMWHs were below 5 µm. We observed no effects on the viability of cardiovascular cells treated with HBC at concentrations up to 0.05 mg/mL. Single doses up to 20 mg/kg of HBC were well-tolerated by rats. HBC completely reversed the effects of LMWHs on bleeding time and anti-factor Xa activity in vivo after 20 minutes, and retained ~80% and ~60% of reversal activity after 1 hour and 2 hours, respectively. Well-documented efficacy and safety of HBC both in vitro and in vivo make this polymer a promising candidate for LMWHs reversal.

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“…18 However, the poor oral bioavailability seriously limits the clinical utility of BBR. To overcome this shortcoming some preparations, such as the complex of BBR and γcyclodextrin, 19 the conjugate of BBR and baicalein, 20 the composition of BBR and 5-aminosalicylic acid, 21 as well as the supramolecule dendrimer-BBR, 22 were well documented. To enhance the antitumor activity the 13-position of BBR was modified by CH 2 CO-Cys(Bzl)-OBzl, CH 2 CO-Glu(OBzl)-OBzl, CH 2 CO-Ile-OBzl and CH 2 CO-Asp(OBzl)-OBzl.…”

Section: Introductionmentioning

confidence: 99%

<p>Development of 13-Cys-BBR as an Agent Having Dual Action of Anti-Thrombosis and Anti-Inflammation</p>

Wang

Zhang

et al. 2020

DDDT

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Background: There is a correlation between tumor and inflammation. The activity of 13-[CH 2 CO-Cys(Bzl)-OBzl]-berberine (13-Cys-BBR) slowing tumor growth is higher than that of BBR. Whether the anti-inflammation activity of 13-Cys-BBR is higher than that of BBR remains unknown. There is a correlation between thrombosis and inflammation. Whether 13-Cys-BBR is an inhibitor of thrombosis remains unknown. Purpose: The object of this investigation is to compare the activities of 13-Cys-BBR inhibiting thrombosis and inflammation to those of BBR. Methods: In vivo anti-thrombosis assay was performed on rat model of arterial and venous thrombosis. In vivo anti-inflammation assay was performed on mouse model of xylene induced ear edema. Results: At oral dose of 66.7 nmol/kg, 13-Cys-BBR, but not BBR, inhibited the rats to form both venous thrombus and arterial thrombus. At oral dose of 2 μmol/kg, 13-Cys-BBR, but not BBR, inhibited the ears of the mice to occur edema. Conclusion:The anti-venous thrombosis activity, anti-arterial thrombosis activity and antiinflammation activity of 13-Cys-BBR were significantly higher than those of BBR. 13-Cys-BBR is a promising preclinical candidate.

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Cellular delivery and enhanced anticancer activity of berberine complexed with a cationic derivative of γ–cyclodextrin

Cited by 23 publications

References 37 publications

Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization

Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization

Heparin-Binding Copolymer as a Complete Antidote for Low-Molecular-Weight Heparins in Rats

<p>Development of 13-Cys-BBR as an Agent Having Dual Action of Anti-Thrombosis and Anti-Inflammation</p>

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