Kwangdong Pharmaceutical

Probiotic therapies, mainly live bacteria, have been proven to be effective in treating atopic dermatitis (AD) with some controversies. Killed probiotics or postbiotics would have immunomodulatory effect in allergic diseases including AD. This study was performed to evaluate the therapeutic effect and safety of tyndallized Lactobacillus rhamnosus (IDCC 3201, isolated from the feces of a Korean breastfed infant, repeated heat-treated and incubated, RHT3201) in children with AD. In a randomized, double-blind, placebo-controlled study, RHT3201 at a dose of 1.0×1010 CPU/d or placebo was given in children (aged 1-12years) with moderate AD for 12weeks. SCORing of AD (SCORAD) scores, allergic inflammatory markers, and safety parameters were evaluated. For evaluating the therapeutic effects of RHT3201, 33 subjects in each group were analyzed. The change of SCORAD total score at 12weeks (primary outcome) from baseline was significantly greater in the RHT3201 group (-13.89±10.05) compared to the control group (-8.37±9.95). Levels of eosinophil cationic protein (ECP) and interleukin (IL)-31 showed tendency to decrease in the RHT3201 group and significant decreases in subgroup analysis in AD for ≥50months. For safety analysis, a total of 100 subjects (50 in the treated group and 50 in the control group) were evaluated, and there were no significant differences in safety parameters between two groups. In children with moderate AD, oral administration of RHT3201 showed the therapeutic effect on AD, the effects in part correlated with decrement of ECP and IL-31, and the effect was more remarkable in subgroup analysis.

The aim of this study was to develop 'Koreans Gut Quotient Measurement Scales (GQ)', in which Koreans respond to questionnaires about the subjective feelings and symptoms of their intestinal health status. Among 66 items pooled from previous studies and 4 items that were added following a focus group interview, 15 items were chosen using the Delphi survey. The content validity was evaluated using the content validity ratio. Data collected from 1,120 people from the general public in Korea were analyzed to verify the reliability and validity of GQ. The finalized GQ consisted of 17 items (including two exploratory measurement items) that were classified into three independent factors based on exploratory factor analysis (EFA): 'perceived intestine discomfort', 'bowel movement discomfort', and 'bowel movement control discomfort'. The discriminant and convergent validity of GQ were identified using EFA, reliability test, and confirmatory factor analysis. In addition, the criterion-related validity of GQ was identified using correlation and multiple regression analysis. The GQ, which is a simplified intestinal health index developed based on an easy questionnaire for the public to understand, can be used as a tool for the public to evaluate their own intestinal health and determine when to visit clinics.

Nepalese sumac (Rhus parviflora) is a wild edible fruit used for the treatment of various ailments including neurological complications and stomach disorders in the traditional medicinal system of south Asia (Ayurveda). Four flavonoids were isolated from ethyl acetate (EtOAc) fraction of Nepalese sumac fruits and their chemical structures were determined on the basis of NMR, fast atom bombardment mass spectrometry (FAB/MS), and IR. The efficiency of isolated compounds in attenuating glutamateinduced cell death in an immortalized mouse hippocampal cell line (HT-22) and inhibition of cycline dependent kinase 5 (Cdk5) were investigated. Among the compounds, flavanols, fustin (1) and taxifolin (2), an aurone, aureusidin (3), and a biflavonoid, agathisflavone (4) were found to have protective effect against glutamate induced oxidative injury in HT22 cells. Aureusidin (3), a Cdk5/p25 inhibitor (IC50 3.5 μM), was the most potent neuroprotector with an EC50 value of 11.90 μM.

Comparative quantitative structure-activity relationship (QSAR) analyses of peptide deformylase (PDF) inhibitors were performed with a series of previously published (British Biotech Pharmaceuticals, Oxford, UK) reverse hydroxamate derivatives having antibacterial activity against Escherichia coli PDF, using 2D and 3D QSAR methods, comparative molecular field analysis (CoMFA), comparative molecular similarity indices analysis (CoMSIA), and hologram QSAR (HQSAR). Statistically reliable models with good predictive power were generated from all three methods (CoMFA r (2) = 0.957, q (2) = 0.569; CoMSIA r (2) = 0.924, q (2) = 0.520; HQSAR r (2) = 0.860, q (2) = 0.578). The predictive capability of these models was validated by a set of compounds that were not included in the training set. The models based on CoMFA and CoMSIA gave satisfactory predictive r (2) values of 0.687 and 0.505, respectively. The model derived from the HQSAR method showed a low predictability of 0.178 for the test set. In this study, 3D prediction models showed better predictive power than 2D models for the test set. This might be because 3D information is more important in the case of datasets containing compounds with similar skeletons. Superimposition of CoMFA contour maps in the active site of the PDF crystal structure showed a meaningful correlation between receptor-ligand binding and biological activity. The final QSAR models, along with information gathered from 3D contour and 2D contribution maps, could be useful for the design of novel active inhibitors of PDF.