ABSTRACT
We have semi-synthesized a natural product 7-acetylhorminone from crude extract of Premna obtusifolia (Indian headache tree), which is active against colorectal cancer after probation through computational screening methods as it passed through the set parameters of pharmacokinetics (most important nonblood-brain barrier permeant) and drug likeliness (e.g., Lipinski's, Ghose's, Veber's rule) which most other phytoconstituents failed to pass combined with docking with EGFR protein which is highly upregulated in the colorectal carcinoma cell. The structure of 7-acetylhorminone was confirmed by single crystal X-ray diffraction studies and 1H NMR, 13C NMR, and COSY studies. To validate the theoretical studies, first, in vitro experiments were carried out against human colorectal carcinoma cell lines (HCT116) which revealed the potent cytotoxic efficacy of 7-acetylhorminone and verified preliminary investigation. Second, the drugability of 7-acetylhorminone interaction with serum albumin proteins (HSA and BSA) is evaluated both theoretically and experimentally via steady-state fluorescence spectroscopic studies, circular dichroism, isothermal titration calorimetry, and molecular docking. In summary, this study reveals the applicability of 7-acetylhorminone as a potent drug candidate or as a combinatorial drug against colorectal cancer.
Subject(s)
Colorectal Neoplasms , Serum Albumin, Bovine , Humans , Colorectal Neoplasms/drug therapy , Colorectal Neoplasms/metabolism , Colorectal Neoplasms/pathology , Serum Albumin, Bovine/metabolism , Serum Albumin, Bovine/chemistry , Drug Screening Assays, Antitumor , Biological Products/chemistry , Biological Products/pharmacology , Molecular Structure , Materials Testing , Biocompatible Materials/chemistry , Biocompatible Materials/pharmacology , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , HCT116 Cells , Cell Proliferation/drug effects , Molecular Docking Simulation , Cell Survival/drug effects , Serum Albumin, Human/chemistry , Serum Albumin, Human/metabolismABSTRACT
This study aims to develop a multigrain probiotic biscuit and evaluate the effect of erythritol as a sugar replacer on the rheological properties of dough, along with the physicochemical and organoleptic properties of biscuits. The higher viscoelasticity of dough was observed at a 25% sugar replacement level with erythritol, and the calorific value of biscuits was significantly (p < 0.05) reduced from 415.12 to 404.69 Cal/100 g with increasing in the sugar replacement from 0% to 75%. The biscuits with higher concentrations of erythritol showed reduced water activity (aw) and higher hardness values. From Pearson's correlation analysis, it was observed that the probiotic viability had a positive relation with moisture, fat, energy, aw, and diameter and a negative association with the protein and fiber content of biscuits. The 25% replacement of sugar with erythritol showed a higher probiotic count (> 7 log CFU/g) and improved physicochemical and sensory properties during the storage period, which was further confirmed by the principal component analysis. So, it was recommended that the partial replacement of sugar with erythritol up to 25% is desirable for developing low-calorie bakery products without any alteration in the functional groups and improving the internal structure of the biscuits.
ABSTRACT
From the past few decades, consumers' demand for probiotic-based functional and healthy food products is rising exponentially. Encapsulation is an emerging field to protect probiotics from unfavorable conditions and to deliver probiotics at the target place while maintaining the controlled release in the colon. Probiotics have been encapsulated for decades using different encapsulation methods to maintain their viability during processing, storage, and digestion and to give health benefits. This review focuses on novel microencapsulation techniques of probiotic bacteria including vacuum drying, microwave drying, spray freeze drying, fluidized bed drying, impinging aerosol technology, hybridization system, ultrasonication with their recent advancement, and characteristics of the commonly used polymers have been briefly discussed. Other than novel techniques, characterization of microcapsules along with their mechanism of release and stability have shown great interest recently in developing novel functional food products with synergetic effects, especially in COVID-19 outbreak. A thorough discussion of novel processing technologies and applications in food products with the incorporation of recent research works is the novelty and highlight of this review paper.
