Solubility of Piperine and Its Inclusion Complexes in Biorelevant Media and Their Effect on Attenuating Mouse Ileum Contractions
| Autor: | Masahiko Ogihara, Mitsutoshi Kimura, Hajime Moteki, Ikuo Kanamoto, Toshinari Ezawa, Namiko Matsumoto, Isamu Murata, Yukiko Inagaki, Kinami Kashiwaba, Yutaka Inoue |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Contraction (grammar)
Intestinal contractility Physical and chemical processes General Chemical Engineering General Chemistry Article Fluorescence Intestinal fluid chemistry.chemical_compound Chemistry Differential scanning calorimetry Solubility chemistry Piperine Contraction rate Mouse Ileum Particulate matter QD1-999 Dissolution Nuclear chemistry |
| Zdroj: | ACS Omega, Vol 6, Iss 10, Pp 6953-6964 (2021) ACS Omega |
| ISSN: | 2470-1343 |
| Popis: | This study evaluated the solubility of piperine (PP) in biorelevant media and the effect of its ground mixtures (GMs) and coprecipitates (CPs) on intestinal contractions when presented in inclusion complexes with α-, β-, and γ-cyclodextrins (CDs). In the powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) measurements, CP (PP/αCD) and CP (PP/γCD) suggest the formation of inclusion complexes. The 1H-nuclear magnetic resonance (NMR) analysis showed the integrated intensity ratios of CP (PP/αCD) and CP (PP/γCD) protons to be 1/2 and 1/1, the same as the respective molar ratios in the respective GM inclusion complexes. The intestinal contraction test confirmed that the intestinal contraction rate of carbachol (CCh) in the presence of 2.0 × 10–5 M PP was comparable to that in the absence of PP. On the other hand, CP (PP/αCD), GM (PP/αCD = 1/2), and GM (PP/βCD = 1/1) formed inclusion complexes that significantly suppressed the intestinal contractility at PP 1.0 × 10–8 M. No significant differences were observed between CP and GM. The solubility of the PP/αCD inclusion complex was 6–7 times higher than that of PP in the fasted-state-simulated intestinal fluid (FaSSIF, pH 6.5). PP functioned to suppress intestinal contraction by forming an inclusion complex. Based on this result, PP/αCD might be expected to be effective as an antidiarrheal. |
| Databáze: | OpenAIRE |
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