and delayed onset of seizure compared with PTZ group (p < 0.05). Therefore, they
concluded that the nanosuspensions preparation could significantly improve the
anti-epileptic effect piperine (Ren et al. 2019a).
22.25 In Vitro Cytotoxic and In Silico Activity
The obtained MTT values showed that piperine has a cytotoxic effect because the
IC 50 was recorded as 61.94 ± 0.054 µg/ml (Nimse and Pal 2015; Paarakh et al.
2015; Sannigrahi et al. 2012; Saha and Pal 2016). The tyrosine kinase receptors
have multidomain extracellular Ligands for specific Ligand, a signal pass transmembrane hydrophobic helix and tyrosine kinase domain. The receptor tyrosine
kinases are not only cell surfaces transmembrane receptors, but are also enzymes
having kinase activity (Bari et al. 2012). Angiogenesis in cancer is a significant
stage in which new capillaries form to supply a vasculature for nutrient supply and
waste material removal. Thus, the kinase inhibitor is a new cancer treatment as such
an anti-angiogenic agent. The trend nowadays is to develop herbal drugs and drug
candidates as inhibitors.
Low molecular weight entities originated in the extracellular part of the receptor
impede tyrosine kinase phosphorylation block signaling (Manley et al. 2002). Since
the type I receptor tyrosine kinase is a major regulator of several distinct and diverse
cellular pathways. They took Piperine and docked to get the superior conformer.
The docking demonstrates that piperine has a −7.6 kJ mol
−1 binding energy with
two hydrogen bonds formed. Molecular docking with EGFR tyrosine kinase
domain revealed that piperine has suppressive capability and thereby has interactions in active pockets one or the other amino acids. The topology of the active
position of EGFR tyrosine kinase was similar in all synthesized molecules, which is
Fig. 22.12 In vitro release
profiles of piperine
nanoparticles and
unformulated piperine in
phosphate buffer at 37 °C for
24 h. Each point represents
mean ± S.D (n = 3). With
copyright permission (Ren
et al. 2019a)
782
N. Sachan et al.
concluded that the nanosuspensions preparation could significantly improve the
anti-epileptic effect piperine (Ren et al. 2019a).
22.25 In Vitro Cytotoxic and In Silico Activity
The obtained MTT values showed that piperine has a cytotoxic effect because the
IC 50 was recorded as 61.94 ± 0.054 µg/ml (Nimse and Pal 2015; Paarakh et al.
2015; Sannigrahi et al. 2012; Saha and Pal 2016). The tyrosine kinase receptors
have multidomain extracellular Ligands for specific Ligand, a signal pass transmembrane hydrophobic helix and tyrosine kinase domain. The receptor tyrosine
kinases are not only cell surfaces transmembrane receptors, but are also enzymes
having kinase activity (Bari et al. 2012). Angiogenesis in cancer is a significant
stage in which new capillaries form to supply a vasculature for nutrient supply and
waste material removal. Thus, the kinase inhibitor is a new cancer treatment as such
an anti-angiogenic agent. The trend nowadays is to develop herbal drugs and drug
candidates as inhibitors.
Low molecular weight entities originated in the extracellular part of the receptor
impede tyrosine kinase phosphorylation block signaling (Manley et al. 2002). Since
the type I receptor tyrosine kinase is a major regulator of several distinct and diverse
cellular pathways. They took Piperine and docked to get the superior conformer.
The docking demonstrates that piperine has a −7.6 kJ mol
−1 binding energy with
two hydrogen bonds formed. Molecular docking with EGFR tyrosine kinase
domain revealed that piperine has suppressive capability and thereby has interactions in active pockets one or the other amino acids. The topology of the active
position of EGFR tyrosine kinase was similar in all synthesized molecules, which is
Fig. 22.12 In vitro release
profiles of piperine
nanoparticles and
unformulated piperine in
phosphate buffer at 37 °C for
24 h. Each point represents
mean ± S.D (n = 3). With
copyright permission (Ren
et al. 2019a)
782
N. Sachan et al.