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Research Paper on Evaluation of the Pharmacokinetic, Metabolism, and Pharmacological Activity of Caesalpinia decapetala Protosappanoside D

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Research Paper on Evaluation of the Pharmacokinetic, Metabolism, and Pharmacological Activity of Caesalpinia decapetala Protosappanoside D

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Title: Evaluation of the Pharmacokinetic, Metabolism, and Pharmacological Activity of Caesalpinia decapetala Protosappanoside D

Abstract: For the first time, a new substance called protosappanoside D (PTD) was isolated from the Caesalpinia decapetala extract. The protosappanin B-3-O-b-D-glucoside was determined to be its structure by 1HNMR, 13C-NMR, 2D-NMR, and MS methods. PTD’s pharmacological effects, metabolism, or pharmacokinetics have not yet been documented. As a result, the LPS-induced RAW264.7 cell model was used in this study to investigate the anti-inflammatory activity of PTD. In parallel, we investigated PTD’s metabolites and pharmacokinetics using the UHPLC/Q Enactive Plus MS and UPLC-MS/MS techniques, and we first determined its bioavailability. The outcomes demonstrated that PTD could suppress the release of pro-inflammatory cytokines. Four metabolites were found in the metabolic study, and desaturation, oxidation, methylation, alkylation, dehydration, degradation, and desugarization were the main in vivo degradative pathways. After oral and intravenous administration, PTD and its primary metabolite protosappanin B (PTB) were measured in the pharmacokinetic study. PTD’s Tomax was 0.49 hours after oral administration, and its t1/2z and MRT(0-t) were 3.47 and 0.78 hours and 3.06 and 0.63 hours, respectively. It demonstrates that PTD was rapidly absorbed into plasma and that it might be quickly eliminated in the body. Its bioavailability is approximately 0.65%.

Keywords: Protosappanoside D; structure elucidation; metabolites; pharmacokinetics; anti-inflammation

Paper Quality: SCOPUS / Web of Science Level Research Paper

Subject: Chemistry

Writer Experience: 20+ Years

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