Pharmacokinetics and bioavailability of ginsenoside Rb1 and Rg1 from Panax notoginseng in rats

Xu, Qing; Fang, Xiao; Chen, Dao Feng

doi:10.1016/s0378-8741(02)00317-3

Cited by 271 publications

(186 citation statements)

References 6 publications

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“…168,169 Although these compounds play a critical role in reducing oxidative stress, their activities are lower than those of some other compounds in several in vivo studies. 170,171 To increase the activity and bioavailability of these compounds or crude extracts, nanosizing the formulation is an alternative for an enhanced protective effect against PD. The nanoginsenosides Rg1 and Rb1 with 19.9 nm particles synthesized using a nanoemulsion technique have enhanced bioavailability in the brain.…”

Section: Nanoginsenosidesmentioning

confidence: 99%

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Ganesan¹,

Ko²,

Kim³

et al. 2015

IJN

108

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Oxidative stress plays a very critical role in neurodegenerative diseases, such as Parkinson’s disease (PD), which is the second most common neurodegenerative disease among elderly people worldwide. Increasing evidence has suggested that phytobioactive compounds show enhanced benefits in cell and animal models of PD. Curcumin, resveratrol, ginsenosides, quercetin, and catechin are phyto-derived bioactive compounds with important roles in the prevention and treatment of PD. However, in vivo studies suggest that their concentrations are very low to cross blood–brain barrier thereby it limits bioavailability, stability, and dissolution at target sites in the brain. To overcome these problems, nanophytomedicine with the controlled size of 1–100 nm is used to maximize efficiency in the treatment of PD. Nanosizing of phytobioactive compounds enhances the permeability into the brain with maximized efficiency and stability. Several nanodelivery techniques, including solid lipid nanoparticles, nanostructured lipid carriers, nanoliposomes, and nanoniosomes can be used for controlled delivery of nanobioactive compounds to brain. Nanocompounds, such as ginsenosides (19.9 nm) synthesized using a nanoemulsion technique, showed enhanced bioavailability in the rat brain. Here, we discuss the most recent trends and applications in PD, including 1) the role of phytobioactive compounds in reducing oxidative stress and their bioavailability; 2) the role of nanotechnology in reducing oxidative stress during PD; 3) nanodelivery systems; and 4) various nanophytobioactive compounds and their role in PD.

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Section: Nanoginsenosidesmentioning

confidence: 99%

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Ganesan¹,

Ko²,

Kim³

et al. 2015

IJN

108

View full text Add to dashboard Cite

show abstract

“…The pharmacokinetics and bioavailability of ginsenosides from P. notoginseng in rats were studied by Xu et al (2003a) and Li et al (2004b). Its excretion profile was reported by .…”

Section: Pharmacokinetics and Bioavailabilitymentioning

confidence: 99%

Pharmacological activity of sanchi ginseng (Panax notoginseng)

2006

Journal of Pharmacy and Pharmacology

362

223

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The pharmacological activity and constituents of the sanchi ginseng Panax notoginseng have been reviewed. The bulk of pharmacological findings have been based on the saponins or steryl glycosides, although polysaccharides with immunopotentiating activity, proteins with antifungal, ribonuclease and xylanase activity, and a triacylglycerol (trilinolein) with antioxidant activity have been reported. Protective actions against cerebral ischaemia, beneficial effects on the cardiovascular system, and haemostatic, antioxidant, hypolipidaemic, hepatoprotective, renoprotective and estrogen-like activities have been described. Various methods for authentication of P. notoginseng are available.

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“…A major barrier to extending the clinical use of ginseng or ginsenosides is their low oral bioavailabilities, usually Ͻ5% in rodents (Xu et al, 2003;Qian et al, 2005;Joo et al, 2010). Low oral bioavailability may cause large variations in systemic exposure during clinical trials, which may lead to ambiguous results in the trials unless an extraordinarily large number of patients are enrolled.…”

Section: Introductionmentioning

confidence: 99%

Inhibition of P-Glycoprotein Leads to Improved Oral Bioavailability of Compound K, an Anticancer Metabolite of Red Ginseng Extract Produced by Gut Microflora

Yang

Wang²,

Niu³

et al. 2012

Drug Metab Dispos

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ABSTRACT:Ginsenosides are hydrolyzed extensively by gut microflora after oral administration, and their metabolites are pharmacologically active against lung cancer cells. In this study, we measured the metabolism of various ginsenosides by gut microflora and determined the mechanisms responsible for the observed pharmacokinetic behaviors of its active metabolite, Compound K (C-K). The results showed that biotransformation into C-K is the major metabolic pathway of ginsenosides after the oral administration of the red ginseng extract containing both protopanaxadiol and protopanaxatriol ginsenosides. Pharmacokinetic studies in normal mice showed that C-K exhibited low oral bioavailability. To define the mechanisms responsible for this low bioavailability, two P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporine A, were used, and their presence substantially decreased C-K's efflux ratio in Caco-2 cells (from 26.6 to <3) and significantly increased intracellular concentrations (by as much as 40-fold). Similar results were obtained when transcellular transport of C-K was determined using multidrug resistance 1 (MDR1)-overexpressing Madin-Darby canine kidney II cells. In MDR1a/b(؊/؊) FVB mice, its plasma C max and AUC 0-24h were increased substantially by 4.0-and 11.7-fold, respectively. These increases appear to be due to slower elimination and faster absorption of C-K in MDR1a/b(؊/؊) mice. In conclusion, C-K is the major active metabolite of ginsenosides after microflora hydrolysis of primary ginsenosides in the red ginseng extract, and inhibition/deficiency of P-gp can lead to large enhancement of its absorption and bioavailability.

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Pharmacokinetics and bioavailability of ginsenoside Rb1 and Rg1 from Panax notoginseng in rats

Cited by 271 publications

References 6 publications

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Pharmacological activity of sanchi ginseng (Panax notoginseng)

Inhibition of P-Glycoprotein Leads to Improved Oral Bioavailability of Compound K, an Anticancer Metabolite of Red Ginseng Extract Produced by Gut Microflora

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Pharmacokinetics and bioavailability of ginsenoside Rb1 and Rg1 from Panax notoginseng in rats

Cited by 271 publications

References 6 publications

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson&rsquo;s disease models

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson&rsquo;s disease models

Pharmacological activity of sanchi ginseng (Panax notoginseng)

Inhibition of P-Glycoprotein Leads to Improved Oral Bioavailability of Compound K, an Anticancer Metabolite of Red Ginseng Extract Produced by Gut Microflora

Contact Info

Product

Resources

About

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models