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

2012 ◽  
Vol 40 (8) ◽  
pp. 1538-1544 ◽  
Author(s):  
Zhen Yang ◽  
Jing-Rong Wang ◽  
Tao Niu ◽  
Song Gao ◽  
Taijun Yin ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Gut Microflora ◽  
Red Ginseng ◽  
Compound K ◽  
Ginseng Extract ◽  
P Glycoprotein

Korean red ginseng extract enhances paclitaxel distribution to mammary tumors and its oral bioavailability by P-glycoprotein inhibition

Xenobiotica ◽  
2016 ◽  
Vol 47 (5) ◽  
pp. 450-459 ◽  
Author(s):  
Jin Kyung Bae ◽  
You-Jin Kim ◽  
Hee-Sung Chae ◽  
Do Yeun Kim ◽  
Han Seok Choi ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Mammary Tumors ◽  
Red Ginseng ◽  
Korean Red Ginseng ◽  
Ginseng Extract ◽  
P Glycoprotein ◽  
Glycoprotein Inhibition

scholarly journals Chemoprevention of Lung Carcinogenesis by Red Ginseng and Ginsenoside Rg3 in A/J mice

2020 ◽  
Author(s):  
Jie Xiong ◽  
Hongmei Yuan ◽  
Shihong Fei ◽  
Hongge Wu ◽  
Jing Cheng ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Lung Tumor ◽  
Tumor Formation ◽  
Mass Spectrometry Analysis ◽  
Lung Carcinogenesis ◽  
Red Ginseng ◽  
Ginsenoside Rg3 ◽  
Preventive Effect ◽  
Korean Red Ginseng ◽  
P Glycoprotein

Abstract Background: Red ginseng has long been used as a traditional medicine for a variety of maladies. Ginsenosides are the active components of ginseng but are limited by their low oral bioavailability. Methods: We evaluated several types of red ginseng extracts for their ability to inhibit lung tumor formation and growth induced by the carcinogen benzo(a)pyrene [B(a)P] in A/J mice. The concentrations of various ginsenosides were quantified in these ginseng extracts using the methods of ultra-performance liquid chromatography tandem mass spectrometry analysis to identify the ginsenosides that may contribute to cancer prevention. We next explored whether inhibition of P-glycoprotein by verapamil could increase the oral bioavailability of ginsenoside by using CaCo-2 cell transcellular transport and in situ mouse intestinal perfusion models. The plasma and intestine concentration of ginsenoside and cancer preventive effect of ginsenoside combined with verapamil in A/J mice were also detected by using B(a)P-induced mouse cancer model.Results: We found that treatment with one type of red ginseng (Korean red ginseng B, KRGB) led to a significant reduction of tumor load compared with other types of red ginseng. KRGB contained the highest concentration of ginsenoside Rg3 among these red ginseng extracts, suggested that Rg3 may play an important role in its preventive efficacy. Our study showed that Rg3 had a relatively poor bioavailability, and co-administration of verapamil decreased the efflux ratio of Rg3 in Caco-2 cells, increased the absorption rate of Rg3 in rat small intestine, increased the plasma and intestine concentration of Rg3 in A/J mice, and enhanced the cancer preventive effect of Rg3 against B(a)P induced lung tumorigenesis. Conclusions: Ginsenosides Rg3 is one of the key components of read ginseng that may be responsible for its efficacy against lung carcinogenesis in mice. Rg3 appears to be the substrate of P-glycoprotein, and inhibition of P-glycoprotein could enhance its oral bioavailability.

scholarly journals Detection of 13 Ginsenosides (Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg3, Rh2, F1, Compound K, 20(S)-Protopanaxadiol, and 20(S)-Protopanaxatriol) in Human Plasma and Application of the Analytical Method to Human Pharmacokinetic Studies Following Two Week-Repeated Administration of Red Ginseng Extract

Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2618 ◽  
Author(s):  
Sojeong Jin ◽  
Ji-Hyeon Jeon ◽  
Sowon Lee ◽  
Woo Youl Kang ◽  
Sook Jin Seong ◽  
...  
Keyword(s):  
Human Plasma ◽  
Analytical Method ◽  
Plasma Concentrations ◽  
Repeated Administration ◽  
Pharmacokinetic Studies ◽  
Red Ginseng ◽  
Compound K ◽  
Ginseng Extract ◽  
Limit Of Quantitation ◽  
Liquid Chromatography Tandem Mass

We aimed to develop a sensitive method for detecting 13 ginsenosides using liquid chromatography–tandem mass spectrometry and to apply this method to pharmacokinetic studies in human following repeated oral administration of red ginseng extract. The chromatograms of Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg3, Rh2, F1, compound K (CK), protopanaxadiol (PPD), and protopanaxatriol (PPT) in human plasma were well separated. The calibration curve range for 13 ginsenosides was 0.5–200 ng/mL and the lower limit of quantitation was 0.5 ng/mL for all ginsenosides. The inter- and intra-day accuracy, precision, and stability were less than 15%. Among the 13 ginsenosides tested, nine ginsenosides (Rb1, Rb2, Rc, Rd, Rg3, CK, Rh2, PPD, and PPT) were detected in the human plasma samples. The plasma concentrations of Rb1, Rb2, Rc, Rd, and Rg3 were correlated with the content in red ginseng extract; however, CK, Rh2, PPD, and PPT were detected although they are not present in red ginseng extract, suggesting the formation of these ginsenosides through the human metabolism. In conclusion, our analytical method could be effectively used to evaluate pharmacokinetic properties of ginsenosides, which would be useful for establishing the pharmacokinetic–pharmacodymic relationship of ginsenosides as well as ginsenoside metabolism in humans.

scholarly journals Tolerability and pharmacokinetics of ginsenosides Rb1, Rb2, Rc, Rd, and compound K after single or multiple administration of red ginseng extract in human beings

2020 ◽  
Vol 44 (2) ◽  
pp. 229-237 ◽  
Author(s):  
Min-Koo Choi ◽  
Sojeong Jin ◽  
Ji-Hyeon Jeon ◽  
Woo Youl Kang ◽  
Sook Jin Seong ◽  
...  
Keyword(s):  
Human Beings ◽  
Red Ginseng ◽  
Compound K ◽  
Ginseng Extract ◽  
Multiple Administration

scholarly journals Morphine dependence is attenuated by red ginseng extract and ginsenosides Rh2, Rg3, and compound K

2016 ◽  
Vol 40 (4) ◽  
pp. 445-452 ◽  
Author(s):  
Taddesse Yayeh ◽  
Kyunghwa Yun ◽  
Soyong Jang ◽  
Seikwan Oh
Keyword(s):  
Morphine Dependence ◽  
Red Ginseng ◽  
Compound K ◽  
Ginseng Extract

scholarly journals Enhanced Absorption Study of Ginsenoside Compound K (20-O-β-(D-Glucopyranosyl)-20(S)-protopanaxadiol) after Oral Administration of Fermented Red Ginseng Extract (HYFRG™) in Healthy Korean Volunteers and Rats

2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Il-Dong Choi ◽  
Ju-Hee Ryu ◽  
Dong-Eun Lee ◽  
Myoung-Hee Lee ◽  
Jae-Joong Shim ◽  
...  
Keyword(s):  
Oral Administration ◽  
Red Ginseng ◽  
Sprague Dawley ◽  
Compound K ◽  
Open Label ◽  
Ginseng Extract ◽  
Enhanced Absorption ◽  
Sprague Dawley Rats ◽  
Ginsenoside Compound K ◽  
The Mean

To evaluate the pharmacokinetics of compound K after oral administration of HYFRG and RG in humans, an open-label, randomized, single-dose, fasting, and one-period pharmacokinetic study was conducted. After oral administration of a single 3 g dose of HYFRG and RG to 24 healthy Korean males, the mean (±SD) ofAUC0–tandCmaxof compound K from HYFRG were 1466.83 ± 295.89 ng·h/mL and 254.45 ± 51.20 ng/mL, being 115.2- and 80-fold higher than those for RG (12.73 ± 7.83 ng·h/mL and 3.18 ± 1.70 ng/mL), respectively; in case of Sprague Dawley rats the mean (±SD) ofAUC0–tandCmaxof compound K from HYFRG was 58.03 ± 32.53 ng·h/mL and 15.19 ± 10.69 ng/mL, being 6.3- and 6.0-fold higher than those from RG (9.21 ± 7.52 ng·h/mL and 2.55 ± 0.99 ng/mL), respectively.Tmaxof compound K in humans and rats was 2.54 ± 0.92 and 3.33 ± 0.50 h for HYFRG and 9.11 ± 1.45 and 6.75 ± 3.97 hours for RG, respectively. In conclusion, the administration of HYFRG resulted in a higher and faster absorption of compound K in both humans and rats compared to RG.

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