Vildagliptin (VDG)is a frontier drug for diabetes mellitus. It is prescribed both in the monotherapy as well as in an amalgamation with other antidiabetic drugs. Drug-serum protein binding is an essential parameter which influences ADME properties of the drug. In current study, binding of VDG with serum protein (bovine serum albumin: BSA) was investigated using multi-spectroscopic techniques. A computational approach was also employed to identify the binding affinity of VDG with BSA at both Sudlow I and II sites. An enzyme activity assay specific for esterase was also investigated to know the post-binding consequences of VDG with BSA. Fluorescence spectra of BSA samples treated with VDG shows static quenching with binding parameters for VDG-BSA complex show single class of equivalent binding stoichiometry(n = 1.331) and binding constant 1.1 x 104M−1 at 298.15 K. The binding constant indicates important role of non-polar interactions in the binding process. Fluorescence resonance energy transfer (FRET) analysis of VDG absorption spectra and emission spectrum of BSA confirmed no significant resonance in energy transfer. Synchronous fluorescence of BSA after binding with VDG show maximum changes in emission intensity at tryptophan (Trp) residues. Post binding with VDG, BSA conformation changes as suggested by circular dichorism (CD) spectra of BSA and this lead to enhanced protein stability as indicated by a thermal melting curve of BSA. Communicated by Ramaswamy H. Sarma
Background: Cancer is a frightful disease and it is the second leading cause of death worldwide. Naturally derived compounds are gaining interest of research workers as they have less toxic side effects as compared to currently used treatments, such as chemotherapy. Plants are the pool of chemical compounds, which provide a promising future for research on cancer.Objective: This review paper provides updated information gathered on medicinal plants and isolated phytoconstituents used as anticancer agents and summarises the plant extracts and their isolated chemical constituents exhibiting anticancer potential on clinical trials.Methods: An extensive bibliographic investigation was carried out by analysing worldwide established scientific databases like SCOPUS, PUBMED, SCIELO, ScienceDirect, Springerlink, Web of Science, Wiley, SciFinder and Google Scholar etc. In the next few decades, herbal medicine may become a new epoch of medical system.Results: Many researches are going on medicinal plants for the treatment of cancer but it is a time to increase further experimental studies on plant extracts and their chemical constituents to find out their mechanism of action at molecular level.Conclusion: The article may help many researchers to start off further experimentation that might lead to the drugs for the cancer treatment.
Limiting starch bioavailability by modifying food matrix dynamics has evolved over the decade, which further envisions low glycemic starch prototypes to tackle chronic hyperglycemia. The dense matrix of whole grain foods like millets and cereals act as a suitable model to understand the dynamics of binary food matrix interactions between starch-lipid, starch-protein & starch-fiber. The state and types of matrix component (lipid/protein/fiber) which interact at various scales alters the starch micro configuration and limits the digestibility, but the mechanism is largely been ignored. Various in-vitro and in-vivo studies have deciphered the varied dimensions of physical interactions through depletion or augmentation studies to correlate towards a natural matrix and its low glycemic nature. The current chapter briefly encompasses the concept of food matrix types and binary interactions in mediating the glycemic amplitude of starch. We comprehensively elaborated and conceptually explained various approaches, which investigated the role of food matrices as complex real food systems or as fundamental approaches to defining the mechanisms. It’s a fact that multiple food matrix interaction studies at a time are difficult but it’s critical to understand the molecular interaction of matrix components to correlate in-vivo processes, which will assist in designing novel food prototypes in the future.