Pharmacokinetics and tissue distribution of resveratrol, emodin and their metabolites after intake of Polygonum cuspidatum in rats

Lin, Shiuan-Pey; Chu, Pei Yi; Tsai, Shu-Yao; Wu, Meng-Hao; Hou, Yu‐Chi

doi:10.1016/j.jep.2012.10.009

Cited by 54 publications

(32 citation statements)

References 38 publications

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“…Wang and Morris (2005) reported a method of precipitating plasma proteins for the quantification of quercetin and conjugated quercetin metabolites in human plasma using two volumes of acetone. Lin et al (2012) investigated the pharmacokinetic behavior and tissue distribution of resveratrol, emodin and their corresponding metabolites after the intake of Polygonum cuspidatum (PC) in rats, using methanol as the extraction solution for PPT. Furthermore, the method validation results revealed that the use of perchloric acid for PPT would neither affect recovery nor cause any detectable matrix effects (Liu et al, 2012;César et al, 2011).…”

Section: Protein Precipitationmentioning

confidence: 99%

“…Diosmin is subsequently absorbed and transformed to the sulfated and glucuronidated conjugates into the systemic circulation. Lin et al (2012) investigated the dose-dependent pharmacokinetics and tissue distribution of resveratrol and emodin after oral administration of PC in rats. To determine the concentrations of resveratrol and emodinin in tissue homogenates, samples were analyzed before and after the treatments with GLU and SULF, respectively.…”

Section: Applications To Pharmacokinetic Studiesmentioning

confidence: 99%

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Quantification of conjugated metabolites of drugs in biological matrices after the hydrolysis with β‐glucuronidase and sufatase: a review of bio‐analytical methods

Ding

Peng

Zhang

et al. 2013

Biomedical Chromatography

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Glucuronidation and sulfation represent two major pathways in phase II drug metabolism in humans and other mammalian species. The great majority of drugs, for example, polyphenols, flavonoids and anthraquinones, could be transformed into sulfated and glucuronidated conjugates simultaneously and extensively in vivo. The pharmacological activities of drug conjugations are normally decreased compared with those of their free forms. However, some drug conjugates may either bear biological activities themselves or serve as excellent sources of biologically active compounds. As the bioactivities of drugs are thought to be relevant to the kinetics of their conjugates, it is essential to study the pharmacokinetic behaviors of the conjugates in more detail. Unfortunately, the free forms of drugs cannot be detected directly in most cases if their glucuronides and sulfates are the predominant forms in biological samples. Nevertheless, an initial enzymatic hydrolysis step using β-glucuronidase and/or sulfatase is usually performed to convert the glucuronidated and/or sulfated conjugates to their free forms prior to the extraction, purification and other subsequent analysis steps in the literature. This review provides fundamental information on drug metabolism pathways, the bio-analytical strategies for the quantification of various drug conjugates, and the applications of the analytical methods to pharmacokinetic studies.

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Section: Protein Precipitationmentioning

confidence: 99%

Section: Applications To Pharmacokinetic Studiesmentioning

confidence: 99%

Quantification of conjugated metabolites of drugs in biological matrices after the hydrolysis with β‐glucuronidase and sufatase: a review of bio‐analytical methods

Ding

Peng

Zhang

et al. 2013

Biomedical Chromatography

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“…However, an understanding of the concentration of resveratrol in tissues, especially in human eyes, is lacking. Several studies have reported the pharmacokinetics and tissue distribution of resveratrol in the liver, kidneys, lungs, and heart [14, 15]. These studies were mostly based on animal models; few researchers have used human subjects for experimentation.…”

Section: Introductionmentioning

confidence: 99%

Tissue Distribution oftrans-Resveratrol and Its Metabolites after Oral Administration in Human Eyes

Wang

Yang

et al. 2017

Journal of Ophthalmology

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Purpose. This study was performed to measure the concentration of trans-resveratrol and its three metabolites in human eyes. Methods. The patients who underwent pars plana vitrectomy for rhegmatogenous retinal detachment were included. The participants were orally given trans-resveratrol-based supplement (Longevinex®). A suitable amount of conjunctiva, aqueous humor, and vitreous humor were obtained during the operation. High-performance liquid chromatography (HPLC) with mass spectrometry (LC/MS/MS) was used to detect the concentration of trans-resveratrol and its three metabolites in the various samples. Results. The average concentration of resveratrol in the conjunctiva was 17.19 ± 15.32 nmol/g (mean ± SD). The concentration of resveratrol in the aqueous humor was close to the limit of detection, but its metabolites could be quantified. The concentrations of resveratrol metabolites in the aqueous humor can be detected. In the vitreous humor, the average concentration of resveratrol-3-O-sulfate was 62.95 ± 41.97 nmol/L. The sulfate conjugations of resveratrol were recovered in the conjunctiva, aqueous humor, and vitreous humor. Conclusions. Resveratrol and its three metabolites can be detected in the ocular tissues after oral administration. Although the concentration of parent resveratrol was low in the eyes, its metabolites could be detected and may have a role in the treatment of ocular diseases.

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“…Moreover, emodin can induce apoptosis of colorectal cancer cells through activating p53/p38/Puma pathway by triggering ROS production (Liu et al, 2015). Pharmacokinetic study revealed that emodin was predominantly found in liver and brain after oral intake of Polygonum cuspidatum , which is a widely used in TCM (Lin et al, 2012). After intragastric administration at doses of 20 and 40 mg/kg, emodin rapidly underwent phase II metabolism to form its glucuronide derivative, and the parent form of emodin was almost undetectable in vivo (Shia et al, 2010).…”

Section: Components Isolated From Tcms That Inhibit Mapkmentioning

confidence: 99%

Development of Certain Protein Kinase Inhibitors with the Components from Traditional Chinese Medicine

et al. 2017

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Traditional Chinese medicines (TCMs) have been used in China for more than two thousand years, and some of them have been confirmed to be effective in cancer treatment. Protein kinases play critical roles in control of cell growth, proliferation, migration, survival, and angiogenesis and mediate their biological effects through their catalytic activity. In recent years, numerous protein kinase inhibitors have been developed and are being used clinically. Anticancer TCMs represent a large class of bioactive substances, and some of them display anticancer activity via inhibiting protein kinases to affect the phosphoinositide 3-kinase, serine/threonine-specific protein kinases, pechanistic target of rapamycin (PI3K/AKT/mTOR), P38, mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinases (ERK) pathways. In the present article, we comprehensively reviewed several components isolated from anticancer TCMs that exhibited significantly inhibitory activity toward a range of protein kinases. These components, which belong to diverse structural classes, are reviewed herein, based upon the kinases that they inhibit. The prospects and problems in development of the anticancer TCMs are also discussed.

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Pharmacokinetics and tissue distribution of resveratrol, emodin and their metabolites after intake of Polygonum cuspidatum in rats

Cited by 54 publications

References 38 publications

Quantification of conjugated metabolites of drugs in biological matrices after the hydrolysis with β‐glucuronidase and sufatase: a review of bio‐analytical methods

Quantification of conjugated metabolites of drugs in biological matrices after the hydrolysis with β‐glucuronidase and sufatase: a review of bio‐analytical methods

Tissue Distribution oftrans-Resveratrol and Its Metabolites after Oral Administration in Human Eyes

Development of Certain Protein Kinase Inhibitors with the Components from Traditional Chinese Medicine

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