Berberine Encapsulated PLGA-PEG Nanoparticles Modulate PCSK-9 in HepG2 Cells

Ochin, Chinedu; Garelnabi, Mahdi

doi:10.2174/1871529x18666180201130340

Cited by 26 publications

(17 citation statements)

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“…While the cytotoxicity in breast cancer cells (MDA-MB-231 and T47D lines) in vitro and in vivo in rats could be enhanced by up to 14-fold, the preparation has a far better transport in cultured Caco-2 cells and rat intestinal perfusion preparations due to improved permeability (5.5-fold) and reduced P-gl efflux (2-fold). In view of the antihypercholesterolaemic effect of berberine, Ochin and Garelnabi [45] also prepared berberine nanoparticles by encapsulating with PLGA-poly(ethylene glycol) (PEG). In cellular models using HepG2 cells, targeting proprotein convertase subtilisin/kexin type 9 (PCSK-9) by this nanoparticle preparation to lower low-density lipoprotein cholesterol (LDL-C) has been presented.…”

Section: Figurementioning

confidence: 99%

The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches

Habtemariam

2020

Biomedicines

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Berberine is a quaternary isoquinoline alkaloid that has been isolated from numerous plants which are still in use today as medicine and herbal supplements. The great deal of enthusiasm for intense research on berberine to date is based on its diverse pharmacological effects via action on multiple biological targets. Its poor bioavailability resulting from low intestinal absorption coupled with its efflux by the action of P-glycoprotein is, however, the major limitation. In this communication, the chemical approach of improving berberine’s bioavailability and pharmacological efficacy is scrutinised with specific reference to type-2 diabetes and associated diseases such as hyperlipidaemia and obesity. The application of modern delivery systems, research from combination studies to preparation of berberine structural hybrids with known biologically active compounds (antidiabetic, antihyperlipidaemic and antioxidant), as well as synthesis approaches of berberine derivative are presented. Improvement of bioavailability and efficacy through in vitro and ex vivo transport studies, as well as animal models of bioavailability/efficacy in lipid metabolism and diabetes targets are discussed.

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Section: Figurementioning

confidence: 99%

The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches

Habtemariam

2020

Biomedicines

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“…Numerous factors regulate PCSK9 expression. For example, statin treatment leads to an increased transcription of PCSK9 (7), in contrast to berberine treatment, which decreases PCSK9 expression (8). However, to date, whether H 2 S is involved in the regulation of hepatic PCSK9 expression remains unknown.…”

Section: Introductionmentioning

confidence: 99%

Hydrogen sulfide inhibits PCSK9 expression through the PI3K/Akt‑SREBP‑2 signaling pathway to influence lipid metabolism in HepG2 cells

et al. 2019

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Hydrogen sulfide (H 2 S) is an endogenous gaseous signaling molecule that plays important roles in the cardiovascular system. In our previous studies, we demonstrated that H 2 S regulates lipid metabolism. In the present study, we aimed to explore the mechanisms through which H 2 regulates lipid metabolism in HepG2 cells in vitro . Treatment of the HepG2 cells with H 2 S inhibited the expression of proprotein convertase subtilisin/kexin type 9 (PCSK9) and increased the level of low-density lipoprotein receptor (LDLR) in a time- and dose-dependent manner. The knockdown of PCSK9 by siRNA effectively increased the levels of LDLR and 1,1′-dioctadecyl-3,3,3′,3′-tetramethyl-indocarbocyanine perchlorate-labeled LDL (DiI-LDL) uptake in the H 2 S-treated HepG2 cells. Furthermore, the phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt)-sterol regulatory element binding proteins 2 (SREBP-2) signaling pathway was confirmed to be involved in H 2 S-regulated PCSK9 expression. Notably, the HepG2 cells were incubated with 30% serum and DiI-LDL for 24 h, and the results revealed that H 2 S increased lipid uptake, but caused no increase in lipid accumulation. On the whole, the findings of this study demonstrate that H 2 S is involved in the regulation of lipid metabolism in HepG2 cells through the regulation of the expression of PCSK9 via the PI3K/Akt-SREBP-2 signaling pathway. To the very best of our knowledge, this study is the first to report that H 2 S can regulate the expression of PCSK9.

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“…The results showed a decrease in ROS production, caspase activation, oxidative stress, and prohibition of depolarization of mitochondria in cells treated with NPs 99. Oral administration of the nanoformulation prepared by PLGA-PEG-PLGA block copolymers containing BBR chloride effectively modulated PCSK-9 mRNA for treatment of high LDL cholesterol 100…”

Section: Natural Product-based Nanoformulations For Metsmentioning

confidence: 95%

<p>Nanoformulations of natural products for management of metabolic syndrome</p>

Taghipour

Hajialyani

Naseri

et al. 2019

IJN

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Metabolic syndrome is a common metabolic disorder which has become a public health challenge worldwide. There has been growing interest in medications including natural products as complementary or alternative choices for common chemical therapeutics regarding their limited side effects and ease of access. Nanosizing these compounds may help to increase their solubility, bioavailability, and promisingly enhance their efficacy. This study, for the first time, provides a comprehensive overview of the application of natural-products-based nanoformulations in the management of metabolic syndrome. Different phytochemicals including curcumin, berberine, Capsicum oleoresin, naringenin, emodin, gymnemic acid, resveratrol, quercetin, scutellarin, stevioside, silybin, baicalin, and others have been nanosized hitherto, and their nanosizing method and effect in treatment and alleviating metabolic syndrome have been reviewed and discussed in this study. It has been discovered that there are several pathways or molecular targets relevant to metabolic disorders which are affected by these compounds. Various natural-based nanoformulations have shown promising effect in treatment of metabolic syndrome, and therefore can be considered as future candidates instead of or in conjunction with pharmaceutical drugs if they pass clinical trials successfully.

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Berberine Encapsulated PLGA-PEG Nanoparticles Modulate PCSK-9 in HepG2 Cells

Abstract: PCSK-9 modulation by oral administration of Berberine using nanotechnology approach can improve its pharmacokinetic profile. Further studies are needed to maximize its delivery efficiency.

Cited by 26 publications

References 0 publications

The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches

The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches

Hydrogen sulfide inhibits PCSK9 expression through the PI3K/Akt‑SREBP‑2 signaling pathway to influence lipid metabolism in HepG2 cells

<p>Nanoformulations of natural products for management of metabolic syndrome</p>

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