Evaluation of Pharmacokinetics, Antibacterial and Anti-Inflammatory Activities of Chrysin in Rat

Modi, Falguni D.; Bhavsar, Shailesh K.; Patel, Jatin H.; Varia, Raseshkumar D.; Modi, L. C.; Kale, Nitin V.

doi:10.20546/ijcmas.2018.709.179

Cited by 5 publications

(6 citation statements)

References 20 publications

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“…Most of ferulic acid was finally excreted through kidney mainly as conjugated ferulic acid (Zhoa et al, 2003;Zhoa et al, 2004). It is observe that phytochemicals relatively cleared very fast form the body and interaction with standard drug and other phytochemical are observed (Modi et. al., 2018;Gondaliya et.…”

Section: Discussionmentioning

confidence: 99%

“…The clean supernatant was transferred into inserts of automatic sampler vial, from which 20 µl of supernatant was injected into high performance liquid chromatography (HPLC) system. Plasma samples were analyzed to quantify ferulic acid using HPLC system by using procedure as described by Adam et al (2002), Cheng et al (2012 ab ) and Patel et al (2018) with minor modifications. In brief, the HPLC apparatus of Shimadzu (Japan) comprised of binary gradient delivery pump (model LC 20AP), diode array detector (model SPD M20A), auto sampler (model SIL 20A) and reverse phase C18 column (250×4.6 mm ID).…”

Section: Hplc Analysis Of Ferulic Acid From Plasma Samplesmentioning

confidence: 99%

“…Research report shows that absorption of ferulic acid after oral administration is quite rapid but bioavailability and mean residence time of it is low in rats (Rondini et al, 2002). So, in order to improve bioavailability, esterification of ferulic acid is one way (Biasutto et al, 2007) and to decrease in vivo metabolism, piperine can be favourable agent as bioenchaner (Singh et al, 2009;Chauhan et al, 2017;Patel et al, 2018). Ethyl ferulate is (ethyl-3hydroxy-4-methoxycinnamate) phenyl propanoid, alkyl ester derivative of ferulic acid.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics of ferulic acid following oral administration ethyl ferulate alone and in combination with piperine in rats

Modi¹,

Kale²,

Patel³

et al. 2019

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The present study was undertaken to evaluate pharmacokinetics of ferulic acid following oral administration of ethyl ferulate alone and in combination with piperine in rats. Following oral administration of ethyl ferulate and in combination with piperine, the mean peak plasma ferulic acid concentration of 18.38  1.38 vs 15.27  1.18 g/ ml was achieved at 0.25 h. Plasma concentration of ferulic acid at 0.5 h differ significantly (p <0.05) and plasma concentration of ferulic acid at 0.08 h, 0.25 h, 0.75 h and 1 h did not differ significantly. All pharmacokinetic parameter of ferulic acid did not differ significantly except volume of distribution (1.25 ± 0.12 vs 2.85 ± 0.57 L/ kg) and total body clearance (7.35 ± 0.57 vs 17.19 ± 1.59 L/h/kg).The study indicates rapid absorpti on and clearance of ferulic acid from body following oral administration of ethyl ferulate alone and in combination with piperine in rats.

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Section: Discussionmentioning

confidence: 99%

Section: Hplc Analysis Of Ferulic Acid From Plasma Samplesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics of ferulic acid following oral administration ethyl ferulate alone and in combination with piperine in rats

Modi¹,

Kale²,

Patel³

et al. 2019

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“…Compared with Lopinavir and Nelfinavir that are proteases inhibitors recommended for the treatment of SARS and MERS [31], the binding affinities of the four top compounds, both flavonoids, are very close to those of two anti-HIV drugs, and even a bit higher to that of the ligand reference. Indeed, the ligand 1 or chrysin has anti-inflammatory, antibacterial and antioxidant activities [57][58], while ligand 2 or kaempferol exhibits antitumor, antioxidant and anti-inflammatory capabilities [59]. In fact, our previous study showed that Aloe vera represents a potential treatment for COVID-19 [60], and three of its phytochemicals were identified as potential inhibitors of SARS-CoV-2 main protease, in which two compounds exhibit antiinflammatory effect [8].…”

Section: Scrutiny Of Toxicity Outcomes In Tablementioning

confidence: 99%

Facing COVID-19 Via Anti-Inflammatory Mechanism of Action: Molecular Docking and Pharmacokinetic Studies of Six Anti-Inflammatory Compounds Derived from Passiflora edulis

Matondo

Kilembe

Mwanangombo

et al. 2021

JOCAMR

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Aim: In the most severe case of the COVID-19, there is an excessive production of proinflammatory cytokines, being the main cause of mortality and morbidity. The present study aims at assessing the potential inhibitor effect of six phytochemicals with anti-inflammatory activity derived from Passiflora edulis, against the SARS-CoV-2 main protease. Materials and Methods: Virtual screening by molecular docking (Autodock tool) was used to obtain the binding energies of ligand-protein complexes formed between each of the six ligands and the SARS-CoV-2 main protease. The six ligands were then submitted to ADME (absorption, distribution, metabolism and excretion) and toxicity analyses to understand their pharmacokinetic behavior, using SwissADME, preADMET and pkCSM webservers. Results: Four high-docking score compounds were identified (both flavonoids) as hits, with the trend: ligand 4 (quercetin, -8.2 kcal/mol ) > ligand 1 (chrysin, -8.0 kcal/mol) > ligand 2 (kaempferol, -7.9 kcal/mol) > ligand 3 (luteolin, -7.7 kcal/mol)> ligand 5 (harmol, -6.7 kcal/mol) > ligand 6 (harmine, -6.4 kcal/mol). The pharmacokinetic behavior of the six ligands revealed that they can be easily absorbed and have good permeability and bioavailability. The toxicity predictions of the six compounds from P. edulis which is an editable fruit confirm that they are safe. Conclusion: Several approaches are currently being used to tackle the COVID-19. Given the cytokine storm in the most severe case of the COVID-19, we adopted the strategy of combatting the disease by compounds that exhibit anti-inflammatory activity. The assessment of the efficiency of six phytochemicals from P. edulis against the SARS-CoV-2 Mpro and their pharmacokinetic profile revealed their potential inhibitor effect against the COVID-19 protein.

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“…Compared with Lopinavir and Nel navir that are protease inhibitors recommended for the treatment of SARS and MERS, the binding a nities of the four top compounds, both avonoids, are very close to those of two anti-HIV drugs, and even a bit higher to that of the ligand reference. Indeed, the ligand 1 or chrysin has anti-in ammatory, antibacterial and antioxidant activities [44][45], while ligand 2 or kaempferol exhibits antitumor, antioxidant and anti-in ammatory capabilities [46]. In fact, our previous studies showed that aloe vera represents potential treatment for COVID-19 [47], and three of its phytochemicals were identi ed as potential inhibitors of SARS-CoV-2 main protease, in which two compounds exhibit antiin ammatory effect [5].…”

Section: Scrutiny Of Toxicity Outcomes Inmentioning

confidence: 99%

Facing COVID-19 via anti-inflammatory mechanism of action: Molecular docking and Pharmacokinetic studies of six anti-inflammatory compounds derived from Passiflora edulis

Mpiana¹,

Matondo²,

Kilembe³

et al. 2020

Preprint

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SARS-CoV-2 is the causative agent of the COVID-19 disease. Pathophysiologically, high levels of proinflammatory cytokines in the serum of SARS-CoV-2 patients are reported, which is so-called the cytokine storm. In this study, molecular docking calculations of six bioactive compounds from Passiflora edulis with anti-inflammatory activity in interaction with the main protease of SARS-CoV-2 were performed, and their pharmacokinetic properties were predicted. The results of their molecular simulations and the ADME-T profiles of each ligand (Absorption, Distribution, Metabolism, Excretion and Toxicity) suggest their use as potential treatment for SARS-CoV-2. Among the six investigated compounds in which four flavonoids and two alkaloids, the best docked ligands are quercetin (-8.2 kcal/mol), chrysin (-8.0 kcal/mol), kaempferol (-7.9 kcal/mol) and luteolin (-7.7 kcal/mol), both flavonoids compounds. Their pharmacokinetic studies using SwissADME, preADMET and pkCSM Web servers establish the good ADMET profile for each ligand.

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Evaluation of Pharmacokinetics, Antibacterial and Anti-Inflammatory Activities of Chrysin in Rat

Cited by 5 publications

References 20 publications

Pharmacokinetics of ferulic acid following oral administration ethyl ferulate alone and in combination with piperine in rats

Pharmacokinetics of ferulic acid following oral administration ethyl ferulate alone and in combination with piperine in rats

Facing COVID-19 Via Anti-Inflammatory Mechanism of Action: Molecular Docking and Pharmacokinetic Studies of Six Anti-Inflammatory Compounds Derived from Passiflora edulis

Facing COVID-19 via anti-inflammatory mechanism of action: Molecular docking and Pharmacokinetic studies of six anti-inflammatory compounds derived from Passiflora edulis

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