Determination of alpha-mangostin in rat plasma by HPLC-MS and its application to pharmacokinetic studies

Li, L; Brunner, I.; Han, Aixia; Hamburger, Matthias; Kinghorn, D; Butterweck, Veronika

doi:10.1055/s-0030-1264636

Cited by 5 publications

(5 citation statements)

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“…More than 50 saponins have been isolated from Rhizoma Panacis Japonici (Chan et al, 2011;Zou et al, 2002aZou et al, , 2002bMorita et al, 1985) and are mainly classified as oleanolic acid-type saponins. SRPJ exhibited hepatoprotection activity (Li et al, 2010a), protection of heart from damage by acute myocardial ischemia injury (He et al, 2012), and anti-ulcer (Yamahara et al, 1987), anti-fatigue (Qian et al, 2008) and antiobesity (Han et al, 2005) activities. Chikusetsusaponin V and chikusetsusaponin IV are phytochemicals and representative markers of SRPJ (Hu et al, 2010; Fig.…”

Section: Introductionmentioning

confidence: 99%

Determination of chikusetsusaponin V and chikusetsusaponin IV in rat plasma by liquid chromatography–mass spectrometry and its application to a preliminary pharmacokinetic study

Yang

Chen

et al. 2013

Biomedical Chromatography

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A sensitive liquid chromatography-electrospray ionization-mass spectrometry method has been developed and validated for determination of two major bioactive saponins in rat plasma after oral administration of saponins extracted from Rhizoma Panacis Japonici, including chikusetsusaponin V and chikusetsusaponin IV for the first time. Akebia saponin D was used as the internal standard (IS). Plasma samples were prepared by protein precipitation with methanol. A Phenomenex C18 column (150 × 4.6 mm, 4 µm) was used as the analytical column with a mobile phase of acetonitrile and 0.05% aqueous formic acid. Mass spectrometric detection was achieved by single quadrupole mass spectrometer equipped with an electrospray ionization interface operating in negative ionization mode. Calibration curves showed good linearity over the concentration range of 5-500 ng/mL for the two analytes in rat plasma. The lower limit of quantification was 5 ng/mL. The intra- and inter-batch precisions were within 10.3% and accuracy ranged from -3.9 to 5.4%. The method was validated and successfully applied to the preliminary pharmacokinetic study of chikusetsusaponin V and chikusetsusaponin IV in rat plasma after oral administration of saponins extracted from Rhizoma Panacis Japonici.

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Section: Introductionmentioning

confidence: 99%

Determination of chikusetsusaponin V and chikusetsusaponin IV in rat plasma by liquid chromatography–mass spectrometry and its application to a preliminary pharmacokinetic study

Yang

Chen

et al. 2013

Biomedical Chromatography

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“…Although the oral bioavailabilities were not determined, the area under the plasma concentration-time curve (AUC) values were quite low, ranging from 0.56 to 138.3 lg*h/mL, and thus, it is expected that their corresponding oral bioavailabilities also will be low. Double peaks were observed in the plasma-concentration time curves for asperosaponin VI, which suggested that it may undergo enterohepatic recirculation (Li et al, 2010).…”

Section: Appendicies B-i Can Be Found In the Online Version Of This Omentioning

confidence: 99%

“…Pharmacokinetic parameters were also investigated for asperosaponin VI, BTS-1 and hederacolchiside E (Yoo et al, 2008;Li et al, 2010;Luo et al, 2013). Although the oral bioavailabilities were not determined, the area under the plasma concentration-time curve (AUC) values were quite low, ranging from 0.56 to 138.3 lg*h/mL, and thus, it is expected that their corresponding oral bioavailabilities also will be low.…”

Section: Appendicies B-i Can Be Found In the Online Version Of This Omentioning

confidence: 99%

Re‐evaluation of Quillaia extract (E 999) as a food additive and safety of the proposed extension of use

Flavourings¹,

Younes²,

Aquilina³

et al. 2019

EFS2

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The EFSA Panel on Food Additives and Nutrient Sources added to Food (ANS) provides a scientific opinion on Quillaia extract (E 999) when used as a food additive and the evaluation of the safety of its proposed extension of use as a food additive in flavourings. The Scientific Committee for Food (SCF) in 1978 established an acceptable daily intake (ADI) of 0–5 mg spray‐dried extract/kg body weight (bw) per day for E 999. The Joint FAO/WHO Expert Committee on Food Additives (JECFA) established in its latest evaluation a group ADI of 0–1 mg/kg bw per day, expressed as quillaia saponins, for Quillaia extract for Type 1 and Type 2. The Panel considered it likely that intact Quillaia extract saponins are absorbed to a low extent, are hydrolysed in the gastrointestinal (GI) tract and that the aglycone is absorbed only to a limited extent. The Panel considered that the genotoxicity data available did not indicate a concern for genotoxicity. Taking into account the available toxicological database, various no observed adverse effect levels (NOAELs) relevant for the derivation of an ADI were identified. The Panel considered that the 2‐year study in rats was the most robust and that the NOAEL of 1,500 mg Quillaia extract/kg bw per day could be used to derive the ADI for E 999. Considering that the adverse effects reported were due to the presence of saponins in the extract, that saponins were present in Quillaia extract Type 1 (around 20%) and using an uncertainty factor of 100, the Panel derived a ADI of 3 mg saponins/kg bw per day for E 999. None of the exposure estimates for the different population groups of the refined brand‐loyal scenario exceeded the ADI of 3 mg saponins/kg bw per day. The proposed extension of use also would not result in an exceedance of this ADI for the refined scenario. The Panel proposed some recommendations for the European Commission to consider, in particular revising the EU specifications for E 999 in order to differentiate the extracts of Quillaia according to the saponins content and to include other parameters to better characterise the food additive.

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“…AM has demonstrated potential therapeutic benefits for many types of cancer cells, with antitumor effects inhibiting key phases of cancer development [8][9][10][11], increasing cell cycle arrest and death in breast cancer cells [10,11], and growing selectivity [12]. However, AM's hydrophobic nature, poor water solubility, limited bioavailability [6,[13][14][15], and accumulation in target organs pose significant challenges [16,17]. Folate-conjugated chitosan nanoparticles (F-CS-NPs) have been developed to enhance AM cytotoxicity and to selectively target MCF-7 breast cancer cells.…”

Section: Introductionmentioning

confidence: 99%

Cytotoxicity Enhancement of α-Mangostin with Folate-Conjugated Chitosan Nanoparticles in MCF-7 Breast Cancer Cells

Herdiana,

Wathoni,

Shamsuddin

et al. 2023

Molecules

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α-mangostin (AM) is a promising natural anticancer agent that can be used in cancer research. However, its effectiveness can be limited by poor solubility and bioavailability. To address this issue, chitosan-based nanoparticles (CSNPs) have been investigated as a potential delivery system to enhance the cytotoxicity to cancer cells and improve selectivity against normal cells. In this study, we developed folate-conjugated chitosan nanoparticles (F-CS-NPs) using a carbodiimide-based conjugation method to attach folate to chitosan (CS), which have different molecular weights. The NPs were crosslinked using tripolyphosphate (TPP) via ionic gelation. To characterize the F-CS-NPs, we utilized various analytical techniques, including transmission electron microscopy (TEM) to evaluate the particle size and morphology, Fourier-transform infrared spectroscopy (FTIR) to confirm the presence of functional groups, and ultraviolet-visible spectroscopy (UV-Vis) to measure the absorption spectrum and confirm the presence of folate. The particle size of AM-F-CS-NPs ranged from 180 nm to 250 nm, with many having favorable charges ranging from +40.33 ± 3.4 to 10.69 ± 1.3 mV. All NPs exhibited the same spherical morphology. The use of F-CS-NPs increased drug release, followed by a sustained release pattern. We evaluated the cytotoxicity of AM, AM-F-CS-HMW, and AM-F-CS-LMW NPs against MCF-7 cells and found IC50 values of 8.47 ± 0.49, 5.3 ± 0.01, and 4.70 ± 0.11 µg/mL, respectively. These results confirm the improved cytotoxicity of AM in MCF-7 cells when delivered via F-CS-NPs. Overall, our in vitro study demonstrated that the properties of F-CS-NPs greatly influence the cytotoxicity of AM in MCF-7 breast cancer cells (significantly different (p < 0.05)). The use of F-CS-NPs as a drug-delivery system for AM may have the potential to develop novel therapies for breast cancer.

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Determination of alpha-mangostin in rat plasma by HPLC-MS and its application to pharmacokinetic studies

Cited by 5 publications

References 0 publications

Determination of chikusetsusaponin V and chikusetsusaponin IV in rat plasma by liquid chromatography–mass spectrometry and its application to a preliminary pharmacokinetic study

Determination of chikusetsusaponin V and chikusetsusaponin IV in rat plasma by liquid chromatography–mass spectrometry and its application to a preliminary pharmacokinetic study

Re‐evaluation of Quillaia extract (E 999) as a food additive and safety of the proposed extension of use

Cytotoxicity Enhancement of α-Mangostin with Folate-Conjugated Chitosan Nanoparticles in MCF-7 Breast Cancer Cells

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