ABSTRACT
A rapid RP-HPLC method was developed for the detection and quantitation of nigerloxin, a fungal metabolite active against diabetic complications, in rat plasma. The method was validated and employed to analyze samples obtained from a pharmacokinetic study after oral administration of the nigerloxin at 100 mM/kg body weight to wistar rats. The assay exhibited a dose-dependent response in a linear range from 2-500 µg/mL in rat plasma. The Cmax, AUC, and t1/2 were found to be 10.68±2.05, 49.01±8.23, 6.5±1.4, respectively. In another study, nigerloxin was fed to rats over a period of 14, 28, and 90 days at 100 mM/kg body weight. The results showed that nigerloxin fed rats were not adversely affected, based on the evaluation of various toxicological parameters. Thus, the results of the present study and the preliminary pharmacokinetic profile of the metabolite indicated the absence of any toxicity and promised its possible future application as a molecule against diabetic complications without any side effects.
ABSTRACT
Background: OSF is a potentially malignant condition affecting the oral cavity and oropharynx. MMP-3 also known as Stromelysin -I is a key member of the MMP family which is responsible for degradation of collagen type II,IV,V,IX and X, proteoglycans, gelatins, fibronectin, laminin and elastin. It plays an important role in activation of pro MMP-1 into the active form of MMP-1 in malignant tissues. MMP-3 expression is low in normal tissues but it is altered during tumour formation, where remodeling of ECM is required. Purpose of the study: To assess the association of single-nucleotide polymorphisms, Adenosine (Insertion/Deletion) in -1171 5A > 6A in the MMP-3 promoter regions of patients with oral submucous fibrosis and in healthy individuals (controls). Methods: Thirty cases of OSF were categorized according to Khanna et al classification into four groups and Twenty age and sex matched controls were included in the study. Blood samples were collected in EDTA coated vacutainers and PCR restriction analysis was done. A statistical analysis was done using Chi-square test and Fisher's exact test to assess the frequency and association of the alleles in the case-control group. Results: The result showed a statistical significance difference between the duration of habit and disease severity with polymorphisms. The result also showed a higher frequency of the 5A allele in the study group as compared to the controls. Conclusion: A long-term follow up of these patients is mandatory to see the prognosis and their susceptibility to malignancy. The positive outcome of an association of the disease with polymorphisms would result in the development of potential diagnostic and therapeutic possibilities in potentially malignant and malignant lesions (AU)