Antiemetic activity of trans-ferulic acid possibly through muscarinic receptors interaction pathway: In vivo and in silico study

Bhuia, Md. Shimul; Kamli, Hossam; Islam, Tawhida; Sonia, Fatema Akter; Kazi, Md. Azim; Siam, Md. Sajjad Hossain; Rahman, Naimur; Bappi, Mehedi Hasan; Mia, Md. Nayem; Hossen, Md. Munnaf; Lucetti, Daniel Luna; Oliveira, Paulo Leonardo Celestino; Coutinho, Henrique D.M.; Islam, Muhammad Torequl

doi:10.1016/j.rechem.2023.101014

Cited by 24 publications

(13 citation statements)

References 73 publications

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“…Crystallographic investigations of ligands bound to specific proteins (macromolecules) play a key function in structurebased drug design (SBDD). [67] Pharmacological results indicated that our plant extract has an immerging effect against hepatic and renal disordered rats. From HPLC analysis, we found that the extract is rich in polyphenolic compounds, especially ellagic acid, gallic acid, kaemferol, quercetin hydrate, and rutin hydrate.…”

Section: Discussionmentioning

confidence: 90%

Longevity Spinach (Gynura procumbens) Ameliorated Oxidative Stress and Inflammatory Mediators in Cisplatin‐Induced Organ Dysfunction in Rats: Comprehensive in vivo and in silico Studies

Chandra Shill,

El‐Nashar,

Prova Mollick

et al. 2024

Chemistry & Biodiversity

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This study aimed to investigate the efficacy of Gynura procumbens (GP) leaf extract against cisplatin (CP)‐induced hepatorenal complications in Wister albino rats. Additionally, it aims to detect pol‐yphenolic compounds using high‐performance liquid chromatography with diode‐array detection (HPLC‐DAD). The rats were treated intraperitoneally with CP (7.5mg/kg) to mediate hepatorenal damage. They were then treated with GP extract (75 and 150mg/kg, P.O.) for 7 consecutive days. CP‐mediated hepatorenal biomarkers like alkaline phosphatase, alanine aminotransferase, aspar‐tate aminotransferase, creatinine and blood urea nitrogen levels were normalized by GP extract in a dose‐dependent manner. Similarly, it significantly reduced CP‐induced oxidative stress inducers including nitric oxide and advanced oxidative protein products. Besides, it enhanced the antioxi‐dant enzymes, and glutathione levels. Histopathological studies showed that CP caused collagen accumulation in the liver and kidney tissues. GP extract drained the collagen mass and acted against hepatorenal damage. Ellagic acid, gallic acid, quercetin hydrate, kaempferol, and rutin hydrate were revealed in GP extract. In‐silico modelling showed good docking scores of the polyphenolic compounds with molecular targets including CYP4502E1, NF‐κB, caspase‐3, and TNF‐α. GP could be an effective therapeutic option for management of anticancer drugs’ complications like CP‐induced organ damage, although clinical studies are required to establish herbal formulation.

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Section: Discussionmentioning

confidence: 90%

Longevity Spinach (Gynura procumbens) Ameliorated Oxidative Stress and Inflammatory Mediators in Cisplatin‐Induced Organ Dysfunction in Rats: Comprehensive in vivo and in silico Studies

Chandra Shill,

El‐Nashar,

Prova Mollick

et al. 2024

Chemistry & Biodiversity

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“…The mother solution was then diluted at concentrations of 20 and 40 mg/kg. In contrast, doses of the referral drugs were chosen by converting human doses to animal doses supported by animal dose calculation protocol and literature procedures 8 , 36 . The reference drug’s solutions were also prepared by thoroughly mixing them into DW (where a small amount of Tween 80 was used as a co-solvent) at concentrations of 16, 6, 10, 21, and 5 mg/kg for the drugs APT, DOM, DHM, HYS and OND, respectively.…”

Section: Methodsmentioning

confidence: 99%

“…In addition, several adverse reactions to radiation therapy and cancer treatment can cause emesis 5 . There is evidence that emesis and GI disturbances can be induced by microbes and their secretions 6 – 8 . However, emesis is a very complex process, initiated by sending emetogenic stimuli to the vomiting center (VC) in the medulla oblongata 9 .…”

Section: Introductionmentioning

confidence: 99%

Antiemetic activity of abietic acid possibly through the 5HT3 and muscarinic receptors interaction pathways

Hasan,

Alshammari,

Albekairi

et al. 2024

Sci Rep

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The present study was designed to evaluate the antiemetic activity of abietic acid (AA) using in vivo and in silico studies. To assess the effect, doses of 50 mg/kg b.w. copper sulfate (CuSO4⋅5H2O) were given orally to 2-day-old chicks. The test compound (AA) was given orally at two doses of 20 and 40 mg/kg b.w. On the other hand, aprepitant (16 mg/kg), domperidone (6 mg/kg), diphenhydramine (10 mg/kg), hyoscine (21 mg/kg), and ondansetron (5 mg/kg) were administered orally as positive controls (PCs). The vehicle was used as a control group. Combination therapies with the referral drugs were also given to three separate groups of animals to see the synergistic and antagonizing activity of the test compound. Molecular docking and visualization of ligand-receptor interaction were performed using different computational tools against various emesis-inducing receptors (D2, D3, 5HT3, H1, and M1–M5). Furthermore, the pharmacokinetics and toxicity properties of the selected ligands were predicted by using the SwissADME and Protox-II online servers. Findings indicated that AA dose-dependently enhances the latency of emetic retching and reduces the number of retching compared to the vehicle group. Among the different treatments, animals treated with AA (40 mg/kg) exhibited the highest latency (98 ± 2.44 s) and reduced the number of retching (11.66 ± 2.52 times) compared to the control groups. Additionally, the molecular docking study indicated that AA exhibits the highest binding affinity (− 10.2 kcal/mol) toward the M4 receptors and an elevated binding affinity toward the receptors 5HT3 (− 8.1 kcal/mol), M1 (− 7.7 kcal/mol), M2 (− 8.7 kcal/mol), and H1 (− 8.5 kcal/mol) than the referral ligands. Taken together, our study suggests that AA has potent antiemetic effects by interacting with the 5TH3 and muscarinic receptor interaction pathways. However, additional extensive pre-clinical and clinical studies are required to evaluate the efficacy and toxicity of AA.

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“…The primary objective is to identify a clinical candidate that demonstrates the desired efficacy and safety outcomes with an optimal concentration-time profile within the body. Thus, PK helps support drug discovery efforts by enabling the design and optimization of drug candidates with optimal ADME features, [64][65][66][67] whereas pharmacodynamics (PD) refers to the connection between drug concentrations at the target sites and the consequent effects. [68] Limitations associated with achieving appropriate pharmacokinetic profiles and addressing potential toxicity concerns are among the most critical factors limiting the oral ingestion of anticancer drugs.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 99%

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

Bhuia,

Chowdhury,

Sonia

et al. 2024

Chemistry & Biodiversity

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Rotundic acid (RA) is a naturally occurring pentacyclic triterpene with a multitude of pharmacological activities. The primary emphasis of this study is on summarizing the anticancer properties with the underlying mechanisms of RA and its derivatives, as well as the pharmacokinetic features. Data was collected (up to date as of November 10, 2023) from various reliable and authentic literatures by searching in different academic search engines, including PubMed, Springer Link, Scopus, Wiley Online, Web of Science, ScienceDirect, and Google Scholar. The findings imply that RA and its synthetic derivatives possess promising anti‐cancer properties against breast, colorectal, liver, and cervical cancers in various preclinical pharmacological test systems. The results also indicate that RA and its derivatives demonstrated anticancer effects via a number of cellular mechanisms, including apoptotic cell death, inhibition of oxidative stress, anti‐inflammatory effect, cytotoxicity, cell cycle arrest, anti‐proliferative effect, anti‐angiogenic effect, and inhibition of cancer cell migration and invasion. It has been proposed that RA and its derived compounds have the capability to serve as a hopeful chemotherapeutic agent, so further extensive clinical research is necessary.

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Antiemetic activity of trans-ferulic acid possibly through muscarinic receptors interaction pathway: In vivo and in silico study

Cited by 24 publications

References 73 publications

Longevity Spinach (Gynura procumbens) Ameliorated Oxidative Stress and Inflammatory Mediators in Cisplatin‐Induced Organ Dysfunction in Rats: Comprehensive in vivo and in silico Studies

Longevity Spinach (Gynura procumbens) Ameliorated Oxidative Stress and Inflammatory Mediators in Cisplatin‐Induced Organ Dysfunction in Rats: Comprehensive in vivo and in silico Studies

Antiemetic activity of abietic acid possibly through the 5HT3 and muscarinic receptors interaction pathways

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

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