Simultaneous Determination of α- and γ-Mangostins in Mouse Plasma by HPLC–MS/MS Method: Application to a Pharmacokinetic Study of Mangosteen Extract in Mouse

Han, Sang-Hoon; Chin, Young‐Won; Kim, Do Yeun; Choi, Young Hee

doi:10.1007/s10337-013-2437-3

Cited by 8 publications

(22 citation statements)

References 20 publications

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“…11) 27 , gambogic acid (6) 44 , and its major metabolite 10-hydroxygambogic acid (10-OHGA) 113 , polygalaxanthone (32, added to a blank matrix sample submitted to the same conditions 27,44,112 . Afterwards, the samples were analyzed in LC-ESI-MS/MS 27,35,69 , UFLC-MS/MS 112 or HPLC-UV 44 . Results obtained revealed that these compounds are stable 27,44,69,111,113,114 or did not exhibited significant degradation 7,35,112 under the studied conditions.…”

Section: Extreme Temperatures Stabilitymentioning

confidence: 99%

Drug-like Properties and ADME of Xanthone Derivatives: The Antechamber of Clinical Trials

Gomes¹,

Brandão²,

Fernandes³

et al. 2016

CMC

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Xanthone derivatives have been described as compounds with a privileged scaffold exhibiting diverse biological/pharmacological activities, what directed the interest to pursue the development of these derivatives into drug candidates. Nevertheless, to achieve this purpose it is crucial to study their pharmacokinetics and toxicity (PK/tox) properties as decision endpoints to continue or interrupt the development investment. This review aims to expose the most relevant analytical methods used in the physicochemical and PK/tox studies in order to detect, quantify, and identify different bioactive xanthones. Analyzing the main results from in vitro and in vivo systems towards ADME properties such as solubility, lipophilicity, pKa, chemical and metabolic stability, permeability, transporters modulation, and plasma protein binding, it is possible to uncover some threats governing the PK properties and to understand the bioavailability and drugability of xanthone derivatives. The last section of this review focuses on a case-study of the development of the drug candidate DMXAA, which has reached clinical trials, to provide the paths and the importance of PK/tox parameters of this scaffold. The data assembled in this review intends to guide for tackling issues in the design of potential lead compounds and drug candidates with a xanthone scaffold.

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Section: Extreme Temperatures Stabilitymentioning

confidence: 99%

Drug-like Properties and ADME of Xanthone Derivatives: The Antechamber of Clinical Trials

Gomes¹,

Brandão²,

Fernandes³

et al. 2016

CMC

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confidence: 99%

“…13,14) Above all, the validated analytical method and an accurate and minimum blood sampling technique using mice are necessary to achieve the pharmacokinetic profiles in herbal products. [6][7][8] In light of a small volume of blood in mouse, only <10 µL of blood collecting at each time looks appropriate and a microsampling system make it possible the sequential multiblood sampling with accurate time point and blood volume from each mouse. Also an advanced analytical methods using high-performance liquid chromatography tandem mass-spectrometry (HPLC-MS/MS) allow to analyze a parent compound and probable metabolites in these biological samples with sufficient limit of quantitation.…”

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confidence: 99%

“…Also an advanced analytical methods using high-performance liquid chromatography tandem mass-spectrometry (HPLC-MS/MS) allow to analyze a parent compound and probable metabolites in these biological samples with sufficient limit of quantitation. [6][7][8]15) Sauchinone is a biologically active lignan found in Saururus chinensis HORT. ex LOUDON (Saururaceae), a plant with a long history of medical use for treating fever, jaundice, edema, and inflammatory disease.…”

mentioning

confidence: 99%

“…[4][5][6][7] In addition, the tissue distribution and metabolism studies are meaningful to elucidate the pharmacological effects relying on the specific delivery and affinity of compounds to various tissues, extensive metabolizing organs, tentative metabolites identification. [7][8][9][10] At these points, the inevitable and integral reasons for pharmacokinetic investigations using mice, not like rats, are as followings: it is arduous to secure a sufficient amount of herbal product using rats and the use of various knockout or xenografted mouse models to demonstrate the pharmacological activities of herbal compounds is increasing in preclinical investigations 11,12) in terms of the different physiological and pathological conditions between mice and rats. 13,14) Above all, the validated analytical method and an accurate and minimum blood sampling technique using mice are necessary to achieve the pharmacokinetic profiles in herbal products.…”

mentioning

confidence: 99%

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Pharmacokinetics, Tissue Distribution, and Tentative Metabolite Identification of Sauchinone in Mice by Microsampling and HPLC-MS/MS Methods

Kim

Han

Seo

et al. 2015

Biological & Pharmaceutical Bulletin

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Sauchinone, a biologically active lignan found in Saururus chinensis (Saururaceae), exerts various biological activities against jaundice, inflammatory disease, hepatic steatosis, and oxidative injury. Despite its diverse applications, there exists some information about sauchinone's pharmacokinetics but its tissue distribution, metabolism, and tentative metabolites have not been reported yet. Thus we investigated the pharmacokinetics of sauchinone in mice using microsampling and HPLC-MS/MS methods. Sauchinone presented linear pharmacokinetics at intravenous doses 7.5-20 mg/kg and oral doses 20-500 mg/kg. However, the metabolism of sauchinone was saturated and this agent presented nonlinear pharmacokinetics at 50 mg/ kg in the intravenous study. At sauchinone 20 mg/kg the F of sauchinone was 7.76% of the oral dose despite that 77.9% of sauchinone was absorbed. This might be due to extensive metabolism of sauchinone in S9 fractions of liver and small intestine. Tentative metabolites of sauchinone by oxidation, dioxidation, methylation, demethylation, dehydrogenation, or bis-glucuronide conjugation were detected in plasma and S9 fractions of liver, intestine, and kidney. The distribution of sauchinone was considerably high (tissue-to-plasma (T/P) ratios, >1) in liver, small intestine, kidney, lung, muscle, fat, or mesentery after intravenous and oral administration and in stomach and large intestine only after oral administration. The protein binding value of sauchinone was 53.0%. These pharmacokinetic data of sauchinone provide an important basis for preclinical applications and experimental methods can be adjusted to evaluate the pharmacokinetics of natural products in mice.Key words sauchinone; pharmacokinetics; metabolite identification; Saururus chinensis; mouse Pharmacokinetic studies to investigate the absorption, distribution, metabolism, and excretion (ADME) of pharmacologically active compounds of interest are essential in the preclinical and clinical process 1,2) because ADME of compounds are fundamental to therapeutic outcome in relation with the efficacy and safety.3) Along with the usages of a large number of herbal products as adjuvant or alternative medicines, the investigation of pharmacokinetic properties in herbal products has been demanding. [4][5][6][7] In addition, the tissue distribution and metabolism studies are meaningful to elucidate the pharmacological effects relying on the specific delivery and affinity of compounds to various tissues, extensive metabolizing organs, tentative metabolites identification.7-10) At these points, the inevitable and integral reasons for pharmacokinetic investigations using mice, not like rats, are as followings: it is arduous to secure a sufficient amount of herbal product using rats and the use of various knockout or xenografted mouse models to demonstrate the pharmacological activities of herbal compounds is increasing in preclinical investigations 11,12) in terms of the different physiological and pathological conditions between mice and rats. 13,14) Abo...

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Absorption, tissue distribution, tissue metabolism and safety of α-mangostin in mangosteen extract using mouse models

Choi

Han

Kim

et al. 2014

Food and Chemical Toxicology

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Simultaneous Determination of α- and γ-Mangostins in Mouse Plasma by HPLC–MS/MS Method: Application to a Pharmacokinetic Study of Mangosteen Extract in Mouse

Cited by 8 publications

References 20 publications

Drug-like Properties and ADME of Xanthone Derivatives: The Antechamber of Clinical Trials

Drug-like Properties and ADME of Xanthone Derivatives: The Antechamber of Clinical Trials

Pharmacokinetics, Tissue Distribution, and Tentative Metabolite Identification of Sauchinone in Mice by Microsampling and HPLC-MS/MS Methods

Absorption, tissue distribution, tissue metabolism and safety of α-mangostin in mangosteen extract using mouse models

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