Molecular Docking and Antihypertensive Activity of Eupalitin 3-O-β-D-galactopyranoside Isolated from Boerhavia diffusa Linn

<b>Background:</b> Angiotensin-converting enzyme (ACE) is a key regulator of blood pressure, and ACE inhibition is an essential part of the treatment of hypertension. We used a molecular docking approach to find the interaction of ACE with an active flavonoid isolated from <i>Boerhavia diffusa</i> Linn, <i>eupalitin 3-O-β-D-galactopyranoside</i>, which leads to potential antihypertensive effects in methyl predenisolone-induced hypertensive rats. Additionally, the pharmacokinetic parameters of this compound are assessed. <b>Methods:</b><i>eupalitin-3-O-β-D-galactopyranoside</i> was isolated from leaves of <i>Boerhavia diffusa</i> by sedimentation method. The compound was characterized by UPLC-MSMS, NMR, and UV spectroscopy to confirm the identity of the compound. Hypertension was induced in rats with methyl predenisolone (5 mg/kg/day) for 14 days. Systolic and diastolic blood pressure effects of <i>eupalitin 3-O-β-D-galactopyranoside</i> were assessed using a tail-cuff method. The blood plasma data for oral administration were used to determine various pharmacokinetic parameters from the bioavailability and serum concentration. <b>Results:</b> In methyl predenisolone-induced hypertensive rats, both systolic and diastolic blood pressures were significantly lower than that of the vehicle with treatment from <i>eupalitin 3-O-β-D-galactopyranoside</i> (<i>p</i> < 0.01). <b>Conclusions:</b> The pharmacokinetic process showed the moderate bioavailability of the compound; <i>eupalitin 3-O-β-D-galactopyranoside</i> induces powerful antihypertensive activity in methyl predenisolone-induced hypertensive rats, implying potential clinical application as a new therapeutic drug for hypertension.

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Publication Details

Journal
Pharmaceutics
Published
2024-12-23
DOI
https://doi.org/10.3390/pharmaceutics16121628
Citations
1
Primary Topic
Natural product bioactivities and synthesis
Type
article
Field-Weighted Citation Impact
0.23

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article

Molecular Docking and Antihypertensive Activity of Eupalitin 3-O-β-D-galactopyranoside Isolated from Boerhavia diffusa Linn

Saad Ali Alshehri, Kamal YT, Mohammed Muqtader Ahmed, Ilyas Uoorakkottil et al.
1 citations
Pharmaceutics
Natural product bioactivities and synthesis
0.23
article

Molecular Docking and Antihypertensive Activity of Eupalitin 3-O-β-D-galactopyranoside Isolated from Boerhavia diffusa Linn

Saad Ali Alshehri, Kamal YT, Mohammed Muqtader Ahmed, Ilyas Uoorakkottil, Rashid Koottangodan
article en
1 citations

Abstract

<b>Background:</b> Angiotensin-converting enzyme (ACE) is a key regulator of blood pressure, and ACE inhibition is an essential part of the treatment of hypertension. We used a molecular docking approach to find the interaction of ACE with an active flavonoid isolated from <i>Boerhavia diffusa</i> Linn, <i>eupalitin 3-O-β-D-galactopyranoside</i>, which leads to potential antihypertensive effects in methyl predenisolone-induced hypertensive rats. Additionally, the pharmacokinetic parameters of this compound are assessed. <b>Methods:</b><i>eupalitin-3-O-β-D-galactopyranoside</i> was isolated from leaves of <i>Boerhavia diffusa</i> by sedimentation method. The compound was characterized by UPLC-MSMS, NMR, and UV spectroscopy to confirm the identity of the compound. Hypertension was induced in rats with methyl predenisolone (5 mg/kg/day) for 14 days. Systolic and diastolic blood pressure effects of <i>eupalitin 3-O-β-D-galactopyranoside</i> were assessed using a tail-cuff method. The blood plasma data for oral administration were used to determine various pharmacokinetic parameters from the bioavailability and serum concentration. <b>Results:</b> In methyl predenisolone-induced hypertensive rats, both systolic and diastolic blood pressures were significantly lower than that of the vehicle with treatment from <i>eupalitin 3-O-β-D-galactopyranoside</i> (<i>p</i> < 0.01). <b>Conclusions:</b> The pharmacokinetic process showed the moderate bioavailability of the compound; <i>eupalitin 3-O-β-D-galactopyranoside</i> induces powerful antihypertensive activity in methyl predenisolone-induced hypertensive rats, implying potential clinical application as a new therapeutic drug for hypertension.

PharmaceuticsVol. 16(12)
Prince Sattam Bin Abdulaziz University (SA), Moulana Hospital (IN), King Khalid University (SA)
King Khalid University
Openalex Percentile: Top 40%
Natural product bioactivities and synthesis
0.23
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