A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M<sub>27</sub> in human plasma and application to a human pharmacokinetic study

Valluri, Venkat Rao; Katari, Naresh Kumar; Khatri, Chirag; Kasar, Pankaj; Polagani, Srinivasa Rao; Jonnalagadda, Sreekantha B.

doi:10.1039/d1ra09026g

Cited by 7 publications

(5 citation statements)

References 11 publications

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“…The RP-HPLC purified sample was analyzed with LCMS/MS (16)(17) and the synthesized antimicrobial peptide (AMP) sample exhibited a wide range of antimicrobial activity against Staphylococcus aureus-ATCC 25923/ MCC 2408, Pseudomonas aeruginosa-ATCC 27853/ MCC 2080, Aspergillus niger-MTCC 9983 and Candida albicans-MTCC 183 which represent Gram-positive, Gram-negative, and fungal pathogens. High-performance liquid chromatography authorizes us to separate the peptide mixture, and protein sequence was identified with potential antimicrobial peptide from MS/MS data through de novo sequencing.…”

Section: Discussionmentioning

confidence: 99%

Characterization and biochemical activities of novel functional antimicrobial peptide (AMP) from Trichogramma chilonis

Sunil¹,

Kumar²,

Pramod³

et al. 2022

Biomedicine

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Introduction and Aim: The antimicrobial peptides (AMPs) are generally found in invertebrates, mammals, birds, plants and insects. AMPs produced by insect parasitoids contribute to innate immunity to resist infection due to lack of adaptive immunity. T. chilonis is one of the most effective endoparasitoid wasps for controlling lepidopterous insects. Several attempts have been made to isolate, characterize and develop a commercially viable product of AMPs from various insect sources. The present study aimed to characterize AMP from T. chilonis for potential antimicrobial and anti-cancer properties. Methods: AMP was identified through T. chilonis transcriptome sequence and designed in silico and synthesized. Its purity was quantified using RP-HPLC, and the mass identified by mass spectrophotometry. LC/MS-MS was employed to predict the sequence and the BLAST program used to compare the sequence. AMP was tested for haemolytic activity and antimicrobial activity. Two pathogenic bacteria and fungal strains were used and IC50 values and MIC values were predicted against microbial strains. Results: Synthetic peptide was found to be 95% homogenous with molecular weight of 3.48 kD. The peptide was identified to be a novel antimicrobial peptide consisting of 33 amino acid residues, and has a low computed instability index of -0.1.55 with high hydrophobic ratio of 27.27%. The antimicrobial activity revealed that T. chilonis antimicrobial peptide (TC-AMP) strongly inhibits the growth of selected human bacterial and fungal pathogens. While the haemolytic assay showed that the peptide did not obliterate human RBC in vitro. TC-AMP also showed an efficient inhibition of angiogenesis by in vivo model as evident by inhibition of vascularization. Conclusions: AMP derived from the parasitoid has a potent antibiotic and anti-angiogenesis property. The peptide can be used as a potential antimicrobial and anticancer drug in near future with more detailed studies on its targeted applications.

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Section: Discussionmentioning

confidence: 99%

Characterization and biochemical activities of novel functional antimicrobial peptide (AMP) from Trichogramma chilonis

Sunil¹,

Kumar²,

Pramod³

et al. 2022

Biomedicine

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“…This method effectively decreased the amount of phospholipids compared to PPT (Figure 3), hereby reducing the matrix effect and enabling accurate quantification of target drugs. Other pretreatments include protein removal through the addition of heavy metal ions (zinc sulfate solution) [29] and liquid-liquid extraction (LLE) using t-butyl methyl ether (TBME) [15,35], ethyl acetate [31], and TBME-ethyl acetate [19].…”

Section: Pretreatment and Matrix Effectmentioning

confidence: 99%

“…According to the Food and Drug Administration, at least 7% of the study sample size should be reanalyzed [39], and the percentage of difference should be within 80 % to 120 % of the mean of original and repeat concentrations. ISR has been evaluated as an index of reproducibility and validity in several studies involving the bioanalysis of MTDs [7,17,35].…”

Section: Applications Other Than Pharmacokinetic Analysis Incurred Sa...mentioning

confidence: 99%

Current Bioanalysis of Molecularly Targeted Drugs Using Liquid Chromatography–Tandem Mass Spectrometry

HIRAYAMA,

KUNO,

FURUSHO

et al. 2023

Chromatography

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Molecular targeted drugs (MTDs), such as tyrosine kinase inhibitors, have been actively developed and widely used in recent years due to their high selectivity and therapeutic efficacy compared to conventional cytotoxic chemotherapeutic agents. Bioanalysis of MTDs for therapeutic drug monitoring (TDM) is performed by many medical and clinical laboratories, and the implementation of TDM for MTDs can lead to better control of tumor progression, reduce tumor recurrence, and minimize side effects. Since bioanalysis of MTDs often requires high detection sensitivity with a limit of quantitation of 1 ng/mL or less, many of the reported analytical methods are performed by liquid chromatography-tandem mass spectrometry (LC-MS/MS). This review highlights recent bioanalytical methods for MTDs using LC-MS/MS. We selected articles on bioanalysis of MTDs of signal transduction inhibitors that (1) were published after 2017, (2) used human samples (whole blood, plasma, serum, urine), and (3) underwent analytical validation. Typical analytical conditions, notable pretreatment techniques, LC separations, and measurement techniques are outlined.

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“…In the literature, some methods to predict several pharmacokinetic parameters of different drugs have been used to determinate their biological activity (Nguyen et al, 2022;Valluri et al, 2022;Goutelle et al, 2022). For this reason, in this research, some pharmacokinetic factors for coumarin derivatives such as 2, 5, 7, 8, 9, 10 and 24 were determined using SwissADME software (Table 3).…”

Section: Pharmacokinetic Evaluationmentioning

confidence: 99%

Evaluation of coumarin and their derivatives as Janus Kinase-3 inhibitors using a theoretical model

et al. 2023

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For several years, cancer has increased in the population, being one of the main causes of death worldwide. This clinical pathology is associated with the activation/release of various biomolecules, including the Janus kinase family (JAKs). It is important to mention that some studies indicate that some JAK inhibitors (ruxolitinib and tofacitinib) may have a significant effect on some autoimmune diseases and cancer; however, some of these drugs can produce secondary effects such as herpes zoster, infectious, acute respiratory distress and others. The aim of this study was to evaluate the interaction of coumarin and its derivatives (compounds 2 to 24) with the JAK-3 surface. In this way, the Interaction of coumarin and their derivatives with JAK-3 was determined using the 3pjc protein and either decernotinib or tofacitinib drugs as theoretical tools on DockinServer program. The results showed differences in the aminoacid residues involved in the interaction of coumarin and their derivatives with 3pjc protein surface compared with decernotinib and tofacitinib. Besides, the inhibition constant (Ki) for coumarin derivatives 7, 9 and 10 was lower compared with tofacitinib. However, Ki was lower for 2, 5, 7, 8, 9, 10, and 24 compared with decernotinib. In conclusion, the coumarin derivatives 2, 5, 7, 8, 9, 10, and 24 could be good alternatives as JAK-3 inhibitors to decrease cancer cells growth.

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A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M₂₇ in human plasma and application to a human pharmacokinetic study

Abstract: A simple, specific, selective and accurate bioanalytical method was developed and validated for simultaneous estimation of acalabrutinib and its active metabolite in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS).

Cited by 7 publications

References 11 publications

Characterization and biochemical activities of novel functional antimicrobial peptide (AMP) from Trichogramma chilonis

Characterization and biochemical activities of novel functional antimicrobial peptide (AMP) from Trichogramma chilonis

Current Bioanalysis of Molecularly Targeted Drugs Using Liquid Chromatography–Tandem Mass Spectrometry

Evaluation of coumarin and their derivatives as Janus Kinase-3 inhibitors using a theoretical model

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A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M27 in human plasma and application to a human pharmacokinetic study

Abstract: A simple, specific, selective and accurate bioanalytical method was developed and validated for simultaneous estimation of acalabrutinib and its active metabolite in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS).

Cited by 7 publications

References 11 publications

Characterization and biochemical activities of novel functional antimicrobial peptide (AMP) from Trichogramma chilonis

Characterization and biochemical activities of novel functional antimicrobial peptide (AMP) from Trichogramma chilonis

Current Bioanalysis of Molecularly Targeted Drugs Using Liquid Chromatography–Tandem Mass Spectrometry

Evaluation of coumarin and their derivatives as Janus Kinase-3 inhibitors using a theoretical model

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A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M₂₇ in human plasma and application to a human pharmacokinetic study