Characterization by HPLC of p-Hydroxybenzyl Alcohol Biotransformation to Gastrodin In Vivo

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110350
Author(s):  
Lijun Cheng ◽  
Yang Deng

Gastrodin (GAS) and its aglycone, p-hydroxybenzyl alcohol (HBA), are both bioactive compounds extracted from Gastrodia elata Blume (GEB). In the current Chinese pharmacopoeia, they are regarded as quality control markers for GEB. In this study, we developed a high-performance liquid chromatography method coupled with a diode array detector to quantify GAS and HBA concentrations in plasma following oral ingestion by rats. For the first time, GAS was detected in vivo after HBA administration. GAS and HBA both had similar pharmacological effects, but the influence of the glucose moiety resulted in different pharmacokinetic characteristics. In this study, the effects of GAS and HBA at different administration durations were investigated in zebrafish larvae. These compounds were found to induce a sedative effect but had different onset times. In conclusion, a biotransformation of HBA to GAS could be observed in the rats. This may be a new insight into the pharmacokinetic characteristics of these bioactive compounds and also relates to the different ways in which they take effect.

1995 ◽  
Vol 269 (2) ◽  
pp. R287-R293 ◽  
Author(s):  
N. Yamaguchi

The aim of the present study was to investigate if either dihydropyridine-sensitive L-type Ca2+ channels or cholinergic receptor-mediated mechanisms are implicated in endothelin-1 (ET)-induced adrenal catecholamine (CA) secretion in anesthetized dogs. ET was locally administered to the left adrenal gland via the left adrenolumbar artery. Plasma CA concentrations in adrenal venous and aortic blood were determined by a high-performance liquid chromatography method. In the control group, local infusion (1 min, 0.5 ml/min) of ET (the fixed total dose of 0.5 microgram given to the gland or approximately 0.0197 microgram/kg of body weight) resulted in a sharp increase in the basal CA output, followed by a rapid decline, and a relatively slow secondary response lasted over a period of 15-30 min. In the second group treated with nifedipine (5 micrograms or approximately 0.207 microgram/kg) similarly administered 10 min before ET infusion, the ET-induced first steep increase in CA output was significantly attenuated by approximately 75% (P < 0.05, n = 6). In dogs similarly receiving either pentolinium (1 mg or approximately 0.041 mg/kg) or atropine (0.5 mg or approximately 0.018 mg/kg), the ET-induced CA response remained unchanged. The results indicate that ET-induced adrenal CA release was largely mediated by the activation of dihydropyridine-sensitive L-type Ca2+ channels. Furthermore, neither nicotinic nor muscarinic receptors were functionally implicated in the CA response to ET. The study suggests the existence of noncholinergic mechanisms involved in the secretory action of ET on the adrenal medulla in the dog in vivo.


Author(s):  
M. V. Sycheva ◽  
A. S. Vasilchenko ◽  
E. A. Rogozhin ◽  
T. M. Pashkova ◽  
L. P. Popova ◽  
...  

Aim. Isolation and study ofbiological activity of antimicrobial peptides from chickens thrombocytes. Materials and methods. Peptides from chickens thrombocytes, obtained by reverse-phase high-performance liquid chromatography method with stepped and linear gradients of concentration increase of the organic solvent were used in the study. Their antimicrobial activity was determined by microtitration method in broth; mechanism of biological effect - by using fluorescent spectroscopy method with DNA-tropic dyes. Results. Individual fractions of peptides were isolated from chickens thrombocytes, that possess antimicrobial activity against Staphylococcus aureus P209 and Escherichia coli K12. A disruption of integrity of barrier structures of microorganisms under the effect of thrombocyte antimicrobial peptides and predominance of cells with damaged membrane in the population of E. coli was established. Conclusion. The data obtained on antimicrobial activity and mechanism of bactericidal effect of the peptide fractions from chickens thrombocytes isolated for the first time expand the understanding of functional properties of chickens thrombocytes and open a perspective for their further study with the aim of use as antimicrobial means.


Planta Medica ◽  
2018 ◽  
Vol 84 (15) ◽  
pp. 1118-1126 ◽  
Author(s):  
Izabela Nawrot-Hadzik ◽  
Sebastian Granica ◽  
Krzysztof Domaradzki ◽  
Łukasz Pecio ◽  
Adam Matkowski

AbstractGiant knotweeds of the genus Reynoutria (syn. Fallopia)–Reynoutria japonica, Reynoutria sachalinensis, and a hybrid of them, Reynoutria x bohemica–are noxious invasive plants in Europe and North America. R. japonica is a traditional East Asian (Japan and China) drug (Polygoni cuspidati rhizoma). Recently, it has been included in European Pharmacopoeia as one of the traditional Chinese medicinal herbs. In this study, a reversed-phase high performance liquid chromatography method with diode array detector and time-of-flight mass spectrometry was developed and validated for the profiling of rhizomes from European invasive populations and Polygoni cuspidati rhizoma purchased in China. Twenty-five compounds were identified, mainly stilbenes, anthraquinones, flavan-3-ols, and phenylpropanoid esters. Tatariside B, hydropiperoside, vanicoside C, a new compound (3,6-O-di-p-coumaroyl)-β-fructofuranosyl-(2 → 1)-(2′-O-acetyl-6′-O-feruloyl)-β-glucopyranoside) were reported for the first time in these raw materials. Six compounds from three phytochemical classes–stilbenes: piceid and resveratrol; anthraquinones: emodin and physcion; hydroxycinnamic sucrose esters: vanicosides A and B–were quantified using the validated method. R. japonica from China contained twice as many stilbenoids than samples from Poland (piceid 14.83 mg/g dm vs. 7.45 mg/g and resveratrol 1.29 mg/g vs. 0.65 mg/g). R. sachalinensis rhizomes contained lower quantities of anthraquinones and no detectable stilbenes, which together with higher amounts of hydroxycinnamic glycosides makes it easily distinguishable from the other two. The phytochemical profile of R. x bohemica was intermediate between the two parent species.


2006 ◽  
Vol 3 (1) ◽  
Author(s):  
Yahdiana Harahap ◽  
Umar Mansur ◽  
Theresia Sinandang

The aim of this research is to find the method for analyze glimepiride and itÂ’s metabolite. Glimepiride is the second generation of antidiabetic oral from the sulphonyl urea that works by stimulating the insulin secretion from beta cells of pancreas. Glimepiride is isolated from plasma the using chloroform. Using the high performance liquid chromatography method which include C18 reversed phase column, using mixture of methanol:water (50:50, v/v) as a mobile phase, flow rate 1.0 ml/minutes, detection at wavelenght 228 nm with photo diode array detector gives retention times of glimepiride in 17 minutes without any interference from endogen component of plasma and from itÂ’s metabolite. Linearity with added internal standard gliclazide was established for the range concentration 100-1000 ng/ml with coefficient of correlation (r) is 0.9977 and give the limit of quantitation of glimepiride in 50 ng/ml. The results of validation method fulfilled for the given criterias.


Author(s):  
Rajasekhar Reddy Alavala ◽  
Prathusha Katahala ◽  
Ganapathi Thipparapu ◽  
Umasankar Kulandaivelu ◽  
Shireesha Boyapati ◽  
...  

Objective: Tacrine is a potent acetylcholine esterase inhibitor (AChEI), and curcumin has been recently proven to possess AChEI, amyloid β aggregation inhibitory activity in addition to its diverse pharmacodynamic nature. Tacrine undergoes biological transformation by cytochrome P450 (CYP 1A2) to a hydroxy metabolite, which is hepatotoxic. Curcumin is known for its inhibitory nature for various metabolic enzymes along with CYP1A2. The present study was undertaken to evaluate the influence of curcumin on the disposition kinetics of tacrine and to assess its impact on dosage regimen.Methods: It was hypothesized that the simultaneous administration of curcumin and tacrine can minimize the toxicity along with increased absorption of tacrine and curcumin into the biological system during the treatment of Alzheimer’s patients.Results and Discussion: Hence, an attempt was made to develop a simple, precise, accurate, and cost-effective reversed-phase high-performance liquid chromatography method for simultaneous determination of curcumin and tacrine and also to estimate the effect of curcumin on absorption of tacrine, in rat plasma.Conclusion: Concomitant administration of curcumin with tacrine improved the parameters such as Cmax and AUC, which indicates that the curcumin would improve the absorption of tacrine.


2008 ◽  
Vol 52 (9) ◽  
pp. 3047-3051 ◽  
Author(s):  
Stephanie J. Wallace ◽  
Jian Li ◽  
Craig. R. Rayner ◽  
Kingsley Coulthard ◽  
Roger L. Nation

ABSTRACT Colistin methanesulfonate (CMS) has the potential to hydrolyze in aqueous solution to liberate colistin, its microbiologically active and more toxic parent compound. While conversion of CMS to colistin in vivo is important for bactericidal activity, liberation of colistin during storage and/or use of pharmaceutical formulations may potentiate the toxicity of CMS. To date, there has been no information available regarding the stability of CMS in pharmaceutical preparations. Two commercial CMS formulations were investigated for stability with respect to colistin content, which was measured by a specific high-performance liquid chromatography method. Coly-Mycin M Parenteral (colistimethate lyophilized powder) was stable (<0.1% of CMS present as colistin) for at least 20 weeks at 4°C and 25°C at 60% relative humidity. When Coly-Mycin M was reconstituted with 2 ml of water to a CMS concentration of 200 mg/ml for injection, Coly-Mycin M was stable (<0.1% colistin formed) for at least 7 days at both 4°C and 25°C. When further diluted to 4 mg/ml in a glucose (5%) or saline (0.9%) infusion solution as directed, CMS hydrolyzed faster at 25°C (<4% colistin formed after 48 h) than at 4°C (0.3% colistin formed). The second formulation, CMS Solution for Inhalation (77.5 mg/ml), was stable at 4°C and 25°C for at least 12 months, as determined based on colistin content (<0.1%). This study demonstrated the concentration- and temperature-dependent hydrolysis of CMS. The information provided by this study has important implications for the formulation and clinical use of CMS products.


1997 ◽  
Vol 273 (4) ◽  
pp. R1339-R1345 ◽  
Author(s):  
Guoju Geng ◽  
Rania Gaspo ◽  
Fethi Trabelsi ◽  
Nobuharu Yamaguchi

The aim of the present study was to investigate whether the dihydropyridine-sensitive L-type Ca2+ channel is operative in adrenal catecholamine (CA) secretion induced by a novel neuropeptide, pituitary adenylate cyclase-activating polypeptide (PACAP), in anesthetized dogs. Plasma CA concentrations in adrenal venous and aortic blood were determined by a high-performance liquid chromatography method. All drugs tested were locally infused into the left adrenal gland via the left adrenolumbar artery. PACAP, with the isoform consisting of 27 (PACAP-27) and 38 (PACAP-38) amino acid residues, significantly increased CA output in a dose-dependent manner, with doses ranging from 5 to 500 ng and 7 to 700 ng, respectively. However, the amplitude of epinephrine response to PACAP-27 was three times greater than that obtained with PACAP-38 at the highest dose tested. In a separate group, a single dose of PACAP-27 (50 ng) induced highly reproducible CA responses when the same dose was repeated with an interval of 35 min. In dogs treated with nifedipine (50 μg), 5 min before the second administration of PACAP-27, the net CA response was significantly inhibited by ∼50% compared with that obtained in the presence of vehicle. A similar CA response to BAY K 8644 (5 μg) was completely abolished by the same dose of nifedipine. The present results indicate that both PACAP-27 and PACAP-38 have the direct local secretagogue effect on the adrenal medulla in vivo and that CA responses to PACAP-27 were greater than those observed with PACAP-38 at equivalent mole doses. The study suggests that the dihydropyridine-sensitive L-type Ca2+ channel is functionally involved in PACAP-induced adrenal CA secretion in the canine adrenal medulla in vivo.


1997 ◽  
Vol 272 (4) ◽  
pp. R1290-R1297 ◽  
Author(s):  
N. Yamaguchi

The present study was designed to test whether endothelin (ET) A and/or B receptors in the adrenal medulla are functionally involved in ET-1-induced catecholamine (CA) release in anesthetized dogs. ET-1 was locally infused into the gland via the left adrenolumbar artery. Plasma CA in adrenal venous and aortic blood was determined by a high-performance liquid chromatography method. In the control group, the local infusion of ET-1 (0.5 microg, 0.4 microM) resulted in a significant increase in CA output. In the presence of a low dose of BQ-123 (5 microg, 16.4 microM), the ET-1-induced CA response was significantly attenuated by approximately 80%. With a high dose of BQ-123 (50 microg, 164 microM), the CA response was further blocked by approximately 95%. This inhibition was significantly greater than that obtained with the low dose of BQ-123. By contrast, a low dose of BQ-788 (5 microg, 15.1 microM) did not significantly affect the CA response. With a high dose of BQ-788 (50 microg, 151 microM), the CA response was only partially inhibited by approximately 70%. The results indicate that BQ-123 significantly inhibited ET-1-induced adrenal CA release in a dose-dependent manner. With the low doses, the CA response was markedly inhibited by BQ-123 but remained unchanged in the presence of BQ-788. Moreover, the high dose of BQ-123 virtually abolished the CA response, whereas BQ-788 failed to do so within the dose range tested. The present study suggests that the ET(A) receptor may play a predominant role in mediating the ET-1-induced CA secretion in the canine adrenal gland in vivo, although the possible involvement of the ET(B) receptor could not completely be excluded under the present experimental conditions.


2011 ◽  
Vol 94 (4) ◽  
pp. 1076-1081 ◽  
Author(s):  
Fernando Rodríguez-Ramos ◽  
Víctor H Sánchez-Estrada ◽  
Alejandro Alfaro-Romero ◽  
Gabriela Rubí Tapia-Álvarez ◽  
Andrés Navarrete

Abstract An HPLC method was developed for the simultaneous determination of gnaphaliin A and B, active compounds of Gnaphalium liebmannii Sch. Bp ex Klatt. The HPLC separation was performed on an Inertsil ODS-3 (150 × 4.6 mm id, 5 μm) RP C18 column operated at 40°C; the isocratic mobile phase was 0.02% aqueous orthophosphoric acid– methanol–acetonitrile (50 + 30 + 20, v/v/v), with a run time of 20 min and flow rate of 1.5 mL/min. Detection with a photodiode array detector (PDAD) was at 270 nm. The method was validated for linearity, repeatability, LOD, and LOQ. The LOD and LOQ for gnaphaliin A and B were found to be in the range of 0.4–0.5 and 1.0–1.4 μg/mL, respectively. This is the frst report of an analytical method developed for the quantitative analysis of flavones from Gnaphalium species by HPLC-PDAD with applications for raw material and commercial products.


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