Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate
Delicaflavone (DF), a natural active ingredient from Selaginella doederleinii Hieron, has been reported to have favorable anticancer effects and is thus considered a potential anticancer agent. However, its pharmacokinetics and plasma protein binding properties remain unknown. Here, we investigated...
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Frontiers Media S.A.
2021
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oai:doaj.org-article:5284f8860df641daaa96a14b61050e522021-11-17T05:46:25ZPharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate1663-981210.3389/fphar.2021.761884https://doaj.org/article/5284f8860df641daaa96a14b61050e522021-11-01T00:00:00Zhttps://www.frontiersin.org/articles/10.3389/fphar.2021.761884/fullhttps://doaj.org/toc/1663-9812Delicaflavone (DF), a natural active ingredient from Selaginella doederleinii Hieron, has been reported to have favorable anticancer effects and is thus considered a potential anticancer agent. However, its pharmacokinetics and plasma protein binding properties remain unknown. Here, we investigated the pharmacokinetic profile of DF in rats using a validated HPLC-MS/MS methods, as well as its human serum albumin (HSA) binding properties through multi-spectroscopic and in silico methods. The results showed that DF was rapidly eliminated and had a widespread tissue distribution after intravenous administration. DF showed linear dynamics in the dose range of 30–60 mg/kg and poor oral bioavailability. The major distribution tissues of DF were the liver, lungs, and kidneys. Ultraviolet and fluorescence spectroscopy and molecular docking demonstrated that DF had a static quenching effect on HSA, with one binding site, and relatively strong binding constants. Thermodynamic analysis of the binding data revealed that hydrogen bonding and van der Waals interactions played major roles in binding. The results of this study further our understanding of the pharmacokinetic and plasma protein binding properties of the potential anticancer agent DF and shed light on pharmacological strategies that may be useful for the development of novel cancer therapeutics.Bing ChenBing ChenHongbin LuoHongbin LuoWeiying ChenWeiying ChenQishu HuangKaifan ZhengDafen XuShaoguang LiAilin LiuLiying HuangYanjie ZhengXinhua LinXinhua LinHong YaoHong YaoFrontiers Media S.A.articledelicaflavonepharmacokineticstissue distributionhuman serum albuminplasma binding propertyantitumor candidate 2Therapeutics. PharmacologyRM1-950ENFrontiers in Pharmacology, Vol 12 (2021) |
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| topic |
delicaflavone pharmacokinetics tissue distribution human serum albumin plasma binding property antitumor candidate 2 Therapeutics. Pharmacology RM1-950 |
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delicaflavone pharmacokinetics tissue distribution human serum albumin plasma binding property antitumor candidate 2 Therapeutics. Pharmacology RM1-950 Bing Chen Bing Chen Hongbin Luo Hongbin Luo Weiying Chen Weiying Chen Qishu Huang Kaifan Zheng Dafen Xu Shaoguang Li Ailin Liu Liying Huang Yanjie Zheng Xinhua Lin Xinhua Lin Hong Yao Hong Yao Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate |
| description |
Delicaflavone (DF), a natural active ingredient from Selaginella doederleinii Hieron, has been reported to have favorable anticancer effects and is thus considered a potential anticancer agent. However, its pharmacokinetics and plasma protein binding properties remain unknown. Here, we investigated the pharmacokinetic profile of DF in rats using a validated HPLC-MS/MS methods, as well as its human serum albumin (HSA) binding properties through multi-spectroscopic and in silico methods. The results showed that DF was rapidly eliminated and had a widespread tissue distribution after intravenous administration. DF showed linear dynamics in the dose range of 30–60 mg/kg and poor oral bioavailability. The major distribution tissues of DF were the liver, lungs, and kidneys. Ultraviolet and fluorescence spectroscopy and molecular docking demonstrated that DF had a static quenching effect on HSA, with one binding site, and relatively strong binding constants. Thermodynamic analysis of the binding data revealed that hydrogen bonding and van der Waals interactions played major roles in binding. The results of this study further our understanding of the pharmacokinetic and plasma protein binding properties of the potential anticancer agent DF and shed light on pharmacological strategies that may be useful for the development of novel cancer therapeutics. |
| format |
article |
| author |
Bing Chen Bing Chen Hongbin Luo Hongbin Luo Weiying Chen Weiying Chen Qishu Huang Kaifan Zheng Dafen Xu Shaoguang Li Ailin Liu Liying Huang Yanjie Zheng Xinhua Lin Xinhua Lin Hong Yao Hong Yao |
| author_facet |
Bing Chen Bing Chen Hongbin Luo Hongbin Luo Weiying Chen Weiying Chen Qishu Huang Kaifan Zheng Dafen Xu Shaoguang Li Ailin Liu Liying Huang Yanjie Zheng Xinhua Lin Xinhua Lin Hong Yao Hong Yao |
| author_sort |
Bing Chen |
| title |
Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate |
| title_short |
Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate |
| title_full |
Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate |
| title_fullStr |
Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate |
| title_full_unstemmed |
Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate |
| title_sort |
pharmacokinetics, tissue distribution, and human serum albumin binding properties of delicaflavone, a novel anti-tumor candidate |
| publisher |
Frontiers Media S.A. |
| publishDate |
2021 |
| url |
https://doaj.org/article/5284f8860df641daaa96a14b61050e52 |
| work_keys_str_mv |
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