Quantitative LC/MS/MS method and <i>in vivo</i> pharmacokinetic studies of vitexin rhamnoside, a bioactive constituent on cardiovascular system from hawthorn

Liang, Mingzhu; Xu, Wen; Zhang, Weidong; Zhang, Chuan; Liu, Runhui; Shen, Yun‐Heng; Li, Hui‐Liang; Wang, Xiaolin; Wang, Xiangwei; Pan, Qiongqun; Chen, Chunlin

doi:10.1002/bmc.777

Cited by 31 publications

(22 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…These findings, suggest not only a higher biodisposition in plasma but also that L7G remains for a longer period of time in the organism. These data are in accordance with previous works regarding the plasma pharmacokinetics of similar compounds, such as vitexin 2''-O-rhamnoside, vitexin 4''-O-glucoside, luteolin 3'-O-glucuronide, apigenin 7-O-glucuronide and acacetin 7-O-glucuronide [28,30,42]. As for the L3'S, it was already reported as being a major ISO metabolite in rats [43].…”

Section: Pharmacokinetics Of Cymbopogon Citratus Infusion In Rats Aftsupporting

confidence: 92%

“…High recovery of administered vitexin 4''-O-glucoside and 2''-O-rhamnoside in faeces indicated that the efficient absorption of these molecules from the gastrointestinal tract of rats was low. In fact, it was reported that vitexin 2''-O-rhamnoside has limited gastrointestinal absorption with an oral bioavailability of only 3.57% [28,30]. A recent work investigated the pharmacokinetic and excretion profile of Swertia pseudochinensis extract after its oral administration to rats and determined three secoiridoid glycosides and three flavonoid glycosides in plasma, bile, urine and faeces [25].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Pharmacokinetics of Cymbopogon Citratus Infusion in Rats after Single Oral Dose Administration

Costa¹,

Fortuna²,

Gonçalves³

et al. 2017

SOJPPS

View full text Add to dashboard Cite

Cymbopogon citratus, commonly known as lemongrass, is a tropical herb used in worldwide traditional medicine for centuries. Studies previously conducted by our team demonstrated its antioxidant and anti-inflammatory effects, and recently, the antiinflammatory potential was also observed in vivo. However, little is known about its pharmacokinetics. The current study aimed at obtaining, for the first time, the pharmacokinetic profile of lemongrass infusion after a single dose oral administration to rats.All in vivo experimental procedures were approved by the Portuguese Veterinary General Division. Male Wistar rats were administered with a single oral dose of lemongrass infusion (68.24 mg/kg) and aliquots of plasma were collected at 0.5, 1, 1.5, 2, 4, 8, 12 and 24 h post-dosing. Liver and kidney samples were collected at 1, 2, 4, 8 and 24 h post-dosing. Plasma and tissues homogenates were processed and luteolin (LUT), luteolin 7-O-glucuronide (L7G), chrysoeriol (CHR), diosmetin (DIO) and luteolin 3'-O-sulphate (L3'S) were quantified employing a RP-HPLC-DAD method. The mean concentration-time profiles obtained were analyzed by a noncompartmental pharmacokinetic analysis using the WinNonlin ® .The pharmacokinetic studies revealed the presence of LUT, L7G, CHR, DIO and L3'S. L7G and L3'S were rapidly detected, with maximum plasma concentrations at 30 min after oral administrations. The concentration-time profile of liver samples evidenced compounds undetected in plasma: LUT, CHR and DIO. L7G, CHR and L3'S were detected in the liver from the first hour and stayed in the tissue until at least 24h.The kidney concentration-time profile revealed the presence of the same compounds detected in plasma.The pharmacokinetic analysis showed that the compounds present in lemongrass infusion are not present in plasma, liver or kidneys. On the other hand, L7G and L3'S were the major metabolites found in plasma and tissues, suggesting that lemongrass polyphenols are promptly metabolized in vivo and their metabolites may be the ones responsible for the anti-inflammatory activity of C. citratus, when orally administered.

show abstract

Section: Pharmacokinetics Of Cymbopogon Citratus Infusion In Rats Aftsupporting

confidence: 92%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of Cymbopogon Citratus Infusion in Rats after Single Oral Dose Administration

Costa¹,

Fortuna²,

Gonçalves³

et al. 2017

SOJPPS

View full text Add to dashboard Cite

show abstract

“…No studies in this area on human tissue appear to have been conducted to date. The pharmacodynamic profile of hawthorn extracts has been examined in animal studies,[2930] but no studies appear to have been performed on human subjects.…”

Section: Constituents and Their Mechanisms Of Actionmentioning

confidence: 99%

Hawthorn (Crataegus spp.) in the treatment of cardiovascular disease

Tassell¹,

Kingston²,

Gilroy³

et al. 2010

Phcog Rev

103

View full text Add to dashboard Cite

The medicinal properties of hawthorn (Crataegus spp., a genus comprising approximately 300 species) have been utilized by many cultures for a variety of therapeutic purposes for many centuries. In the Western world cardiovascular disease (CVD) has become one of the single most significant causes of premature death. Echoing this situation, more recent research into the therapeutic benefits of hawthorn preparations has focused primarily upon its cardiovascular effects. This review covers research into the various mechanisms of action proposed for Crataegus preparations, clinical trials involving Crataegus preparations, and the herb's safety profile.Clinical trials reviewed have been inconsistent in terms of criteria used (sample size, preparation, dosage, etc) but have been largely consistent with regard to positive outcomes. An investigation into data available to date regarding hawthorn preparations and herb/drug interactions reveals that theoretical adverse interactions have not been experienced in practice. Further, adverse reactions relating to the use of hawthorn preparations are infrequent and mild, even at higher dosage ranges. A recent retrospective study by Zick et al. has suggested a negative outcome for the long-term use of hawthorn in the prognosis of heart failure. These findings are examined in this paper.Although further research is needed in certain areas, current research to date suggests that hawthorn may potentially represent a safe, effective, nontoxic agent in the treatment of CVD and ischemic heart disease (IHD).

show abstract

“…Studies with the C ‐linked dihydrochalcone aspalathin from rooibos revealed that it is absorbed as intact C ‐glucoside from the small intestine in humans and pigs 6, 37, 38. Liang et al identified the intact vitexin rhamnoside in plasma after its oral administration to rats 39. Thus, the intestinal absorption of flavan‐3‐ol C ‐glycosides is as well considered to be possible.…”

Section: Discussionmentioning

confidence: 99%

Flavan‐3‐ol C‐glycosides – Preparation and model experiments mimicking their human intestinal transit

Hasslauer

Oehme

Locher

et al. 2010

Molecular Nutrition Food Res

View full text Add to dashboard Cite

In order to study the human intestinal transit of flavan-3-ol C-glycosides, several C-glycosyl derivatives were prepared by non-enzymatic reaction of (+)-catechin with α-D-glucose, α-D-galactose and α-D-rhamnose, respectively. In contrast to literature data, we propose that the reaction mechanism proceeds in analogy to the rearrangement of flavan-3-ols during epimerization under alkaline conditions. Four of the 12 synthesized flavan-3-ol C-glycosides were incubated under aerobic conditions at 37°C using saliva (2 min) and simulated gastric juice (3 h). To simulate human intestine, the C-glycosides were also incubated under anaerobic conditions at 37°C both in human ileostomy fluid (10 h) and colostomy fluid (24 h), respectively. The flavan-3-ol C-glycosides under study, i.e. (+)-epicatechin 8-C-β-D-glucopyranoside (1a), (+)-epicatechin 6-C-β-D-glucopyranoside (1d), (+)-catechin 6-C-β-D-galactopyranoside (2b), (+)-catechin 6-C-β-D-rhamnopyranoside (3b) were analyzed in the incubation samples by HPLC-DAD and HPLC-DAD-MS/MS. They were found to be stable in the course of incubation in saliva, simulated gastric juice and ileostomy fluid and underwent degradation in colostomy fluid. While the 6-C-β-D-glucopyranoside 1d was completely metabolized between 2 and 4 h, decomposition of the 6-C-β-D-galactopyranoside 2b reached only 16 ± 2% within 4 h of incubation. Linear degradation rates of 1d and 2b in colostomy fluid differed significantly. As microbial metabolism of flavan-3-ols is known not to be influenced by the stereochemistry of the aglycon, varying degradation rates are ascribed to the effect of the sugar moiety. Based on these results we assume that flavan-3-ol C-glycosides pass through the upper gastrointestinal tract (oral cavity, stomach and small intestine) unmodified and are then metabolized by the colonic microflora.

show abstract

Quantitative LC/MS/MS method and in vivo pharmacokinetic studies of vitexin rhamnoside, a bioactive constituent on cardiovascular system from hawthorn

Cited by 31 publications

References 26 publications

Pharmacokinetics of Cymbopogon Citratus Infusion in Rats after Single Oral Dose Administration

Pharmacokinetics of Cymbopogon Citratus Infusion in Rats after Single Oral Dose Administration

Hawthorn (Crataegus spp.) in the treatment of cardiovascular disease

Flavan‐3‐ol C‐glycosides – Preparation and model experiments mimicking their human intestinal transit

Contact Info

Product

Resources

About