1.The synthesis of purine derivatives and its inhibitory activity on CD38 NADase.
Na LI ; Wenjie ZHU ; Xiwen XUE ; Yongjuan ZHAO ; Honcheung LEE ; Liangren ZHANG ; Lihe ZHANG
Acta Pharmaceutica Sinica 2015;50(8):1013-20
CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
2.Novel Mutation of SLC26A3 Gene Observed in Congenital Chloride Diarrhea
Ji Hye CHEON ; Na Li YU ; Na Mi LEE
Neonatal Medicine 2023;30(3):75-78
Congenital chloride diarrhea (CLD) is a rare autosomal recessive disease caused by mutations in the solute carrier family 26 member 3 (SLC26A3) gene on chromosome 7q31. Affected neonates are vulnerable to dehydration, electrolyte imbalance in the form of hyponatremia, metabolic alkalosis, failure to thrive, or even death if left untreated. Genetic testing for mutations should be considered if the clinical diagnosis remains uncertain because early diagnosis and appropriate management are critical to the disease course in CLD. Several mutations have been reported in Korean patients with CLD, with the most common being the c.2063-1G>T mutation. Here, we report the case of a neonate with prenatally suspected CLD with confirmed novel mutations in the SLC26A3 gene (c.2147C>G; p.Ala716Gly).
3.The synthesis of purine derivatives and its inhibitory activity on CD38 NADase.
Na LI ; Wen-jie ZHU ; Xi-wen XUE ; Yong-juan ZHAO ; Hon-cheung LEE ; Liang-ren ZHANG ; Li-he ZHANG
Acta Pharmaceutica Sinica 2015;50(8):1013-1020
CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
ADP-ribosyl Cyclase 1
;
antagonists & inhibitors
;
Enzyme Inhibitors
;
chemical synthesis
;
chemistry
;
Humans
;
Purines
;
chemical synthesis
;
chemistry
4.Influence of Reflex Sympathetic Dystrophy on Functional Outcomes of the Upper Extremity in Stroke Patients.
Hee Kyu KWON ; Sang Ryong LEE ; Dae Won YOON ; Li Na KIM ; Su Han CHAE ; Hang Jae LEE
Journal of the Korean Academy of Rehabilitation Medicine 2003;27(4):480-484
OBJECTIVE: To assess the influence of reflex sympathetic dystrophy (RSD) on functional status and recovery of the hemiplegic upper extremity in stroke patients. METHOD: Retrospective chart review was performed in 561 patients. Among 561 stroke patients, 116 subjects were recruited and classified into two groups: patient group, 43 cases with RSD; control group, 73 cases without RSD. Upper extremity function was assessed based on feeding, dressing and personal hygiene scores of the modified Barthel index at the beginning of rehabilitation treatment and at the time of discharge. Causes of stroke and length of stay were recorded. Median nerve-somatosensory evoked potential studies were performed and assessed. RESULTS: The incidence of RSD was 7.7% and the time to development of RSD was 62.3+/-34.1 days after the onset of stroke. There was no significant difference in functional status between two groups at initial and final evaluation. The upper extremity function had improved in both groups although the length of stay was longer in patient group. SSEP abnormalities were more frequent in the patient group. CONCLUSION: The presence of well-managed RSD affected neither the functional status nor the functional recovery of upper extremity in stroke patients.
Bandages
;
Evoked Potentials
;
Evoked Potentials, Somatosensory
;
Humans
;
Hygiene
;
Incidence
;
Length of Stay
;
Reflex Sympathetic Dystrophy*
;
Reflex*
;
Rehabilitation
;
Retrospective Studies
;
Stroke*
;
Upper Extremity*
5.Predictive Factors for Severe Thrombocytopenia and Classification of Causes of Thrombocytopenia in Premature Infants
Hoon Bum SHIN ; Na Li YU ; Na Mi LEE ; Dae Yong YI ; Sin Weon YUN ; Soo Ahn CHAE ; In Seok LIM
Neonatal Medicine 2018;25(1):16-22
PURPOSE: This study investigated predictive factors for severe neonatal thrombocytopenia, which greatly increases the need for intensive care and is associated with a high mortality rate in premature infants. Factors adopted for prompt identification of at-risk newborns include blood test results and birth history. This study analyzed the relationship between the presence of severe neonatal thrombocytopenia and the mortality rate. The causes of thrombocytopenia in premature infants were also examined. METHODS: This retrospective study evaluated 625 premature infants admitted to the neonatal intensive care unit (NICU) at Chung-Ang University Medical Center. The neonates were classified into 3 groups according to the severity of thrombocytopenia: mild (100×10⁹/L≤platelet < 150×10⁹/L), moderate (50×10⁹/L≤platelet < 100×10⁹/L), or severe (platelet < 50×10⁹/L). Analysis of blood samples obtained at the onset of thrombocytopenia included platelet count, white blood cell (WBC) count, hemoglobin level, hematocrit level, absolute neutrophil count, and high-sensitivity C-reactive protein level. RESULTS: Of the 625 premature infants admitted to our NICU, 214 were detected with thrombocytopenia. The mortality rate in thrombocytopenic neonates was 18.2% (39/214), whereas a mortality rate of only 1.0% was observed in non-thrombocytopenic neonates. The major causes of thrombocytopenia were perinatal insufficiency and sepsis in premature infants. Severe thrombocytopenia was noted more frequently in premature infants with higher WBC counts and in those with a younger gestational age. CONCLUSION: Platelet count, WBC count, and gestational age are reliable predictors for severe neonatal thrombocytopenia. The major causes of thrombocytopenia were perinatal insufficiency and sepsis in premature infants.
Academic Medical Centers
;
C-Reactive Protein
;
Classification
;
Critical Care
;
Gestational Age
;
Hematocrit
;
Hematologic Tests
;
Humans
;
Infant, Newborn
;
Infant, Premature
;
Intensive Care, Neonatal
;
Leukocytes
;
Mortality
;
Neutrophils
;
Platelet Count
;
Reproductive History
;
Retrospective Studies
;
Sepsis
;
Thrombocytopenia
;
Thrombocytopenia, Neonatal Alloimmune
6.The Effect of Glenohumeral Internal Rotation Deficit on the Isokinetic Strength, Pain, and Quality of Life in Male High School Baseball Players.
Jinyoung LEE ; Li Na KIM ; Hongsun SONG ; Sunghwan KIM ; Seungseok WOO
Annals of Rehabilitation Medicine 2015;39(2):183-190
OBJECTIVE: To investigate the effects of glenohumeral internal rotation deficit (GIRD) on the isokinetic strength, body pain, and the quality of life in male high school baseball players of Korea. METHODS: Fifty-six male high school baseball players were divided into either group A (GIRD> or =20degrees, n=12) or group B (GIRD<20degrees, n=44). The range of motion in the shoulder and the isokinetic strength were measured. Questionnaires were administered regarding the body pain location by using the visual analogue scale, and the quality of life was measured by using the SF-36 Form. RESULTS: All subjects had increased external rotation range of motion and decreased internal rotation in the throwing shoulder. The incidence of GIRD (> or =20degrees) was 21.43% in the present study. In the isokinetic strength test, a significantly weaker muscular state at an angular velocity of 180degrees/s was observed in group A, compared to group B. For the comparison of the pain, the frequency of shoulder pain was higher (33.93%) than other body pain, among the study subjects. CONCLUSION: GIRD is one of the main risk factors of glenohumeral joint damage, and it is correlated with reduced isokinetic strength and quality of life. High school baseball players will need appropriate shoulder rehabilitation programs for the improvement in their quality of life and performance.
Baseball*
;
Humans
;
Incidence
;
Korea
;
Male
;
Quality of Life*
;
Range of Motion, Articular
;
Rehabilitation
;
Risk Factors
;
Shoulder
;
Shoulder Joint
;
Shoulder Pain
;
Surveys and Questionnaires
7.A Study on the Prevalence and Associated Factors of Falls in Some Rural Elderly.
Nam Gu LIM ; Kyu Beom SHIM ; Yong Beom KIM ; Ju Li PARK ; Eun Young KIM ; Baek Ju NA ; Dae Kyeong KIM ; Moo Skik LEE
Journal of the Korean Geriatrics Society 2002;6(3):183-196
BACKGROUNDS: It is to find out ins and outs of falls, and then to study risky factors that are preventable. METHODS: Total 260 elderly people living in Nonsan who are 60 years old and over were analyzed for data. Stereotyped of those are populational, social specific, physical functions, and basis diseases. And concerning falls, it was analyzed if they have had experience of up to 5 times within 3 years recently. RESULTS: The analyzed are total 260 people, men 112(43%), and women 148(57%). And the ones who answered they have had experience of falls are 108(41.6%), men 31(28.7%), and women 77(71.3%), showing a distinguishable difference between two groups. Women have had more experience than men have(p<0.001), and according to their age, the average age of those experienced falls showed to be higher than the one of those who have not(p=0.036). And according to their education, the ones who did not go to any schools have had more experience than those who did, showing the education has something to do with falls(p<0.001). The mean mass index(p=0.043) and average weight(p=0.023) also showed a mere difference between the group of the people who have had experience and the one of those who have not. Taking into account the fact that there were more women in the group who have had experienced falls, it is shown that there is nothing practical to pay attention to. In Activity of Daily Living(ADL) the experienced is 10.8(+/-4.2), and the unexperienced 9.1(+/-3.1), showing a mere difference between two groups(p<0.000). Concerning chronic diseases, there was no difference between those two groups, but individual patient histories showed that the experienced group had less rheumatic trouble than the unexpedenced(p=0.033). Looking at the difference of the causes for the falls according to their gender, the range of their movements(p=0.043), illumination(p=0.012), influence of alcoho1(p=0.001), and the shoes when they were falling down(p<0.001), the first aid treatments after falls(p=0.014), and influence of medications(p<0.001) showed a mere difference between men and women, while did not show any difference in seasons, time of falls, places, and the descriptions of the surfaces of the places. The mean number of falls within recent 3 years of the experienced was 1.79 times, and the comparison of the relation between the frequency and the causes of falls was done between the ones with experience of I fall, and the ones with experience of more twice falls. The average height(p=0.046) was much higher thai those with experience of more than 2 falls. There was also a mere difference between two groups in movements(p=0.009), illumination(p=0.005), influence of alcohol(p=0.003), the shoes (p=0.048), and first aid treatments after falls(p<0.001). CONCLUSION: The group with higher risk rate includes women, age, poor education, skinny physical figures, and lack of ability to act in daily life. Therefore, those results should be considered when a preventive program of falls for elderly people is designed.
Aged*
;
Asian Continental Ancestry Group
;
Chronic Disease
;
Chungcheongnam-do
;
Education
;
Female
;
First Aid
;
Humans
;
Male
;
Middle Aged
;
Prevalence*
;
Seasons
;
Shoes
8.Inhibitory Effect of a Sesquiterpene from Artemisia iwayomogi on Expression of Inducible Nitric Oxide Synthase by Suppression of I-κBα Degradation in LPS-stimulated RAW 264.7 Cells.
Na Yeon KIM ; Hye Jin KOH ; Hua LI ; Hwa Jin LEE ; Jae Ha RYU
Natural Product Sciences 2017;23(2):92-96
A sesquiterpene was purified from Artemisia iwayomogi methanolic extract during the course of searching anti-inflammatory principle from medicinal plants. A sesquiterpene identified as armefolin inhibited the production of nitric oxide (NO) and attenuated inducible nitric oxide synthase (iNOS) protein level in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Armefolin also down-regulated mRNA expressions of iNOS and pro-inflammatory cytokines, interleukin-1β and interleukin-6 in LPS-activated macrophages. Moreover, armefolin suppressed the degradation of inhibitory-κBα (I-κBα) in LPS-activated macrophages. These data suggest that armefolin from A. iwayomogi can suppress the LPS-induced production of NO and the expression of iNOS gene through inhibiting the degradation of I-κBα. Taken together, armefolin from A. iwayomogi might be a candidate as promising anti-inflammatory agent.
Artemisia*
;
Cytokines
;
Interleukin-6
;
Macrophages
;
Methanol
;
Nitric Oxide
;
Nitric Oxide Synthase Type II*
;
Plants, Medicinal
;
RAW 264.7 Cells*
;
RNA, Messenger
9.Juvenile Obesity Aggravates Disease Severity in a Rat Model of Atopic Dermatitis.
Keun Yeong JEONG ; Jaehee LEE ; Chengjin LI ; Taeho HAN ; Sat Byol LEE ; Hyunkyoung LEE ; Seung Keun BACK ; Heung Sik NA
Allergy, Asthma & Immunology Research 2015;7(1):69-75
PURPOSE: There is increasing epidemiological evidence of an association between childhood obesity and atopic dermatitis, but little is known about the underlying mechanism(s). In the present study, we used a rat model of atopic dermatitis to assess whether juvenile obesity, induced by reduction of litter size, aggravated the signs of atopic dermatitis and, if so, whether this aggravation was associated with changes in plasma concentration of adipokines, such as leptin and adiponectin. METHODS: Dermatitis was induced by neonatal capsaicin treatment. Body weight, dermatitis score, serum IgE, skin nerve growth factor (NGF), serum leptin and adiponectin, and cytokine mRNA expression in the skin lesion were compared between small (SL, 5 pups) and large litters (LL, 15 pups). RESULTS: The body weight of juvenile rats up to 6 weeks of age was significantly heavier in the SL group, compared with those in the LL group. The SL group showed more robust development of dermatitis, and higher levels of serum IgE and skin NGF than the LL group. Additionally, the SL group demonstrated higher levels of leptin and pro-inflammatory cytokine mRNA but lower levels of adiponectin than the LL group. CONCLUSIONS: These results suggest a causal link between a decrease in immunological tolerance, induced by juvenile obesity, and aggravation of atopic dermatitis.
Adipokines
;
Adiponectin
;
Animals
;
Body Weight
;
Capsaicin
;
Dermatitis
;
Dermatitis, Atopic*
;
Immunoglobulin E
;
Leptin
;
Litter Size
;
Models, Animal*
;
Nerve Growth Factor
;
Obesity*
;
Pediatric Obesity
;
Plasma
;
Rats
;
RNA, Messenger
;
Skin
10.Flowers of Inula japonica Attenuate Inflammatory Responses.
Jeon Hyeun CHOI ; Young Na PARK ; Ying LI ; Mei Hua JIN ; Jiean LEE ; Younju LEE ; Jong Keun SON ; Hyeun Wook CHANG ; Eunkyung LEE
Immune Network 2010;10(5):145-152
BACKGROUND: The flowers of Inula japonica (Inulae Flos) have long been used in traditional medicine for the treatment of inflammatory diseases. In the present study, we investigated the anti-inflammatory properties of Inulae Flos Extract (IFE). METHODS: The anti-inflammatory effects of IFE against nitric oxide (NO), PGE2, TNF-alpha, and IL-6 release, as well as NF-kappa B and MAP kinase activation were evaluated in RAW 264.7 cells. RESULTS: IFE inhibited the production of NO and the expression of inducible nitric oxide synthase (iNOS) in LPS-stimulated RAW264.7 cells. In addition, IFE reduced the release of pro-inflammatory cytokines, such as TNF-alpha and IL-6. Furthermore, IFE inhibited the NF-kappa B activation induced by LPS, which was associated with the abrogation of I kappa B-alpha degradation and subsequent decreases in nuclear p65 and p50 levels. Moreover, the phosphorylation of ERK, JNK, and p38 MAP kinases in LPS-stimulated RAW 264.7 cells was suppressed by IFE in a dose-dependent manner. CONCLUSION: These results suggest that the anti-inflammation activities of IFE might be attributed to the inhibition of NO, iNOS and cytokine expression through the down-regulation of NF-kappa B activation via suppression of I kappa B alpha and MAP kinase phosphorylation in macrophages.
Cytokines
;
Dinoprostone
;
Down-Regulation
;
Flowers
;
I-kappa B Proteins
;
Interleukin-6
;
Inula
;
Macrophages
;
Medicine, Traditional
;
NF-kappa B
;
Nitric Oxide
;
Nitric Oxide Synthase Type II
;
Phosphorylation
;
Phosphotransferases
;
Tumor Necrosis Factor-alpha