1.Synthesis of phenylacetamide derivatives and their protective effects on islet cell damage induced by palmitic acid
Ai-Yun LI ; Li GUAN ; Wan-Zhen SU ; Yang-Yang LU ; Sheng-Jie ZHANG ; Wei-Ze LI ; Xiang-Ying JIAO
Chinese Pharmacological Bulletin 2024;40(6):1130-1136
Aim To design and synthesize a series of phenylacetamide derivatives with different substituted phenylacetic acid as raw materials,and to investigate the protective effects of the compound on the damage of pancreatic β cells induced by palmitate acid(PA).Methods Min6 cells were cultured and divided into B blank control group,PA treatment group and PA+compounds group.The viability of Min6 cells was de-tected by CCK-8.The protein expressions of TXNIP and NLRP3 were observed by Western blot.MDA con-tent and SOD activity were detected by MDA and SOD kit.The insulin secretion of Min6 islet cells was meas-ured with insulin ELISA kit.Results A total of 10 phenylacetamide derivatives were designed and synthe-sized.Their structures were confirmed by 1H NMR and ESI-MS.Pharmacological activity study showed that most of the compounds had protective effects on islet βcells,among which LY-6 and LY-8 had stronger pro-tective effects than PA model group,with the cell via-bility of 61.4%,and LY-6 had the highest cell activi-ty,reaching to 104.9%.Compared with PA group,the protein expression of TXNIP and NLRP3 decreased in LY-6 and LY-8 groups,MDA content decreased and SOD activity increased,and insulin secretion of Min6 cell increased.Conclusions LY-6 and LY-8 inhibit TXNIP expression and decrease the activation of NL-RP3 inflammasome,and decrease the production of MDA and increase SOD activity,and thus reducing is-let β cells apoptosis and increasing insulin secretion.Therefore,the compound LY-6 could serve as a poten-tial anti-diabetic new chemical entity.
2.Impact of pumpkin polysaccharides on hypoxia/reoxygenation-induced myocardial cell injury by regulating Nrf2/γ-GCS pathway
Wan ZHENG ; Shanshan YANG ; Yun LIN ; Junping WEI ; Yani YAN
Chinese Journal of Immunology 2024;40(9):1871-1875
Objective:To investigate the impact of pumpkin polysaccharide(PP)on hypoxia/reoxygenation(H/R)-induced myocardial cell(H9C2)injury by regulating Nrf2/γ-GCS pathway.Methods:HR cell models were established,and the concentration of pumpkin polysaccharide(PP)was determined.H9C2 cells were grouped into Control group,H/R group,pumpkin polysaccharide group(PP group,2 mg/L PP),Nrf2 inhibitor group(ML385 group,2.0 μmol/L ML385),and PP+ML385 group(2.0 mg/L PP+2.0 μmol/L ML385),the apoptosis,mitochondrial membrane potential changes,oxidative stress(LDH,MDA,SOD,ROS),the lev-els of inflammatory factors(TNF-α,IL-6,IL-1β)and the protein expressions of Nrf2 and γ-GCS in H9C2 cells were detected,respec-tively.Results:Compared with Control group,H/R group had changes in cell morphology,the cell injury and mitochondrial membrane potential decreased,the H9C2 cell viability,SOD and protein expression levels of Nrf2 and γ-GCS were significantly decreased,while the apoptosis rate,LDH,MDA,ROS,and levels of TNF-α,IL-6 and IL-1β were significantly increased(P<0.05);compared with H/R group,the cell injury in PP group was reduced,the mitochondrial membrane potential was restored,the H9C2 cell viability,SOD and protein expression levels of Nrf2 and γ-GCS were significantly increased,and the apoptosis rate,LDH,MDA,ROS,and levels of TNF-α,IL-6 and IL-1β were significantly decreased(P<0.05),the effect of ML385 was opposite to that of PP,and ML385 could reverse the antioxidant and anti-inflammatory effects of PP.Conclusion:PP up-regulates the Nrf2/γ-GCS pathway to exert antiox-idant and anti-inflammatory effects,and reduces H/R-induced H9C2 cell injury.
3.Distribution Characteristics of Rh Phenotype and Feasibility of Compatible Blood Transfusion in Pregnant and Postpartum Women
Gui-Lin YANG ; Tao ZHANG ; Chun-Li LI ; Hong-Peng ZHANG ; Ying-Ying WU ; Sheng-Lan LI ; Kuai WAN ; Yun-Ping YANG
Journal of Experimental Hematology 2024;32(3):868-874
Objective:To analyze the distribution characteristics of Rh phenotype in pregnant and postpartum women in Chongqing area,and to explore the clinical significance of Rh phenotype in pregnant and postpartum women and the feasibility of Rh phenotype compatible blood transfusion.Methods:The ABO blood group and Rh phenotype of 65 161 pregnant and postpartum women were detected by microcolumn gel method,and 48 122 males in the same period were taken as controls.The data were analyzed by Chi-square test.Results:There were 112 870 cases(99.64%)of RhD+in 113 283 samples.In RhD+cases,CCDee(48.39%)and CcDEe(32.88%)were the main phenotypes.The first case of D--phenotype in Chongqing area was detected.413 cases(0.36%)of RhD-were detected,with ccdee(52.78%)and Ccdee(33.41%)as the main phenotypes.Compared with RhD-group,RhD+group showed statistically significant difference in Rh phenotype distribution(P<0.01).Among 65 161 maternal samples,the positive rate of 5 antigens of Rh blood group from high to low was D>e>C>c>E,and there was no significant difference compared with male samples(P>0.05).There was no significant difference in the distribution of Rh phenotype between males and pregnant/postpartum women,as well as between pregnant/postpartum women with different ABO blood groups(P>0.05).In pregnant and postpartum women,there was no significant difference in distribution of Rh phenotype among the normal pregnancy population,the population with adverse pregnancy history,the population using human assisted reproductive technology(ART)and the population with infertility(P>0.05).There was no significant difference in the distribution of Rh phenotype between the 4 populations mentioned above and the inpatients in the local general Grade A hospitals and the blood donors(P>0.05).In RhD positive pregnant and postpartum women,the probability of finding compatible blood for CcDEe phenotype was 100%,the probability of finding compatible blood for CCDee,CcDee and CCDEe phenotypes was 45%-60%,the probability of finding compatible blood for ccDEE,ccDEe and CcDEE phenotypes was 5%-10%,and the probability of finding compatible blood for other phenotypes was lower than 0.5%.The supply of blood with CCDee and ccDEE phenotypes can meet the compatible transfusions requirements of 7 Rh phenotypes in more than 99%of patients.Conclusion:Rh phenotype detection should be carried out for pregnant and postpartum women,and it is feasible to carry out Rh phenotype-matched or compatible blood transfusion for pregnant and postpartum women who need blood transfusion.
4. Network pharmacology-based study on mechanism of Zhi-Huang-Zhi-Tong powder in rheumatoid arthritis treatment
Xiao-Yun TIAN ; Ying-Jie YANG ; Wan-Ting ZHENG ; Ming-Qing HUANG ; Li-Hong NAN ; Jian-Yu CHEN ; Hai-Yu ZHAO
Chinese Pharmacological Bulletin 2024;40(2):381-389
Aim To discover the potential active compounds and possible mechanisms in rheumatoid arthritis (RA) treatment with Zhi-Huang-Zhi-Tong powder (ZHZTP) by using network pharmacology and in vitro study. Methods The active ingredient targets and disease targets of Zhihuang Zhitong Powder were searched and screened by database; they intersected to get a common target; and the "drug-component-target" relationship network diagram was constructed for GO and KEGG enrichment analysis of the overlapping genes; then the core components were docked with the core targets. Finally, based on the inflammation model of HUVECs in vitro, the efficacy and mechanism of Zhihuang Zhitong powder were verified by MTT method, plate scratch test and Western blot. Results Active compounds involved in RA treatment were screened in the present study, and the top two were ursolic acid and emodin, all playing crucial roles in RA treatment with ZHZTP. Additionally, the key target was AKTA, TNF and IL-6. GO and KEGG enrichment analysis revealed that ZHZTP regulated BP, MF and CC, and also focused on regulating AKTA, TNF and IL-6 signaling pathway. Molecular docking showed that interactions between key active compounds and key targets were stable. In vitro ZHZTP significantly inhibited cell viability and migration of TNF-a-stimulated HUVECs, and the involved mechanism may be associated with PI3K/AKT/m-TOR signaling. Conclusions The present study reveals that the potential active compounds of ZHZTP are ursolic acid and emodin, and moreover, the involved mechanisms of ZHZTP for RA treatment are associated with PI3 K/AKT/m-TOR signaling.
5.Progress in delivering biotechnology drugs on microneedles
Han LIU ; Guo-zhong YANG ; Wan-ren DU ; Suo-hui ZHANG ; Ze-quan ZHOU ; Yun-hua GAO
Acta Pharmaceutica Sinica 2024;59(10):2751-2762
As a new transdermal drug delivery system, microneedles can significantly improve skin permeability, enhance drug transdermal delivery, and demonstrate unique advantages in breaking stratum corneum barrier of skin. This feature enables microneedles to demonstrate enormous potential in delivering biotechnology drugs. The traditional delivery method for biotechnology drugs is mainly injection, which brings problems such as pain and skin redness to patients, leading to poor patient compliance. In addition, the production, transportation, and storage of biotechnology drugs require strict low-temperature conditions to maintain their activity and increase cost output. Microneedles, by contrast, have many benefits, providing new avenues and solutions for biomolecular delivery. Accordingly, this review introduced the microneedle drug delivery system for delivery biotechnology drugs, and summarized the research progress of microneedle systems in biotechnology drugs.
6.2023 Clinical Practice Guidelines for Diabetes Management in Korea: Full Version Recommendation of the Korean Diabetes Association
Jun Sung MOON ; Shinae KANG ; Jong Han CHOI ; Kyung Ae LEE ; Joon Ho MOON ; Suk CHON ; Dae Jung KIM ; Hyun Jin KIM ; Ji A SEO ; Mee Kyoung KIM ; Jeong Hyun LIM ; Yoon Ju SONG ; Ye Seul YANG ; Jae Hyeon KIM ; You-Bin LEE ; Junghyun NOH ; Kyu Yeon HUR ; Jong Suk PARK ; Sang Youl RHEE ; Hae Jin KIM ; Hyun Min KIM ; Jung Hae KO ; Nam Hoon KIM ; Chong Hwa KIM ; Jeeyun AHN ; Tae Jung OH ; Soo-Kyung KIM ; Jaehyun KIM ; Eugene HAN ; Sang-Man JIN ; Jaehyun BAE ; Eonju JEON ; Ji Min KIM ; Seon Mee KANG ; Jung Hwan PARK ; Jae-Seung YUN ; Bong-Soo CHA ; Min Kyong MOON ; Byung-Wan LEE
Diabetes & Metabolism Journal 2024;48(4):546-708
7.Development of parenting behavior scale for caregivers of children aged 2 to 6 years and analysis for its reliability and validity.
Ni Na XIONG ; Rui Yun SHEN ; Ying WANG ; Ming ZHAO ; Zhuang WEI ; Wan Xia ZHANG ; Yan Jie CHEN ; Yang MA ; Wen Jing JI ; Ai Min LIANG
Chinese Journal of Preventive Medicine 2023;57(1):58-62
To develop a caregiver parenting behavior scale for children aged 2 to 6 years, and to verify its reliability and validity. This study recruited 1 350 caregivers of children aged 2 to 6 years. The item discrimination analysis and exploratory factor analysis were used to analyze the structure, dimensions and items of the scale. Homogeneity reliability, split-half reliability and test-retest reliability were used to analyze the reliability of the scale. Content validity and construct validity were used to analyze the validity of the scale. The results showed that the final scale contained 7 dimensions and 45 items. Cronbach's α coefficient of the total scale was 0.945; the coefficient of split half was 0.899; the test-retest reliability analysis showed that the correlation coefficients between the two tests were 0.893 (total score), 0.854 (social), 0.832 (language), 0.871 (gross motor), 0.893 (fine motor), 0.862 (cognitive), 0.832 (self-care), and 0.872 (sensory). The content validity analysis was carried out by two rounds of expert argumentation using Delphi expert consultation method. The Kendall coefficient of the items score in two rounds of Delphi expert consultation was 0.813 (P<0.01). The structure validity analysis showed that there were significant correlations between each dimension and the total scale, also between each dimension of the scale, and the extracted average variance values of each dimension was greater than the correlation coefficients between this dimension and other dimensions. In conclusion, the reliability and validity of the scale are qualified. It can be used as a tool to evaluate and guide the parenting behavior of caregivers of children aged 2 to 6 years.
Humans
;
Child
;
Caregivers/psychology*
;
Reproducibility of Results
;
Parenting
;
Surveys and Questionnaires
;
Factor Analysis, Statistical
;
Psychometrics/methods*
8.Chemical constituents from leaves of Craibiodendron yunnanense.
Man WANG ; Ya-Nan WANG ; Hai-Qiang WANG ; Wan-Qi YANG ; Shuang-Gang MA ; Yong LI ; Jing QU ; Yun-Bao LIU ; Shi-Shan YU
China Journal of Chinese Materia Medica 2023;48(4):978-984
The present study investigated the chemical constituents from the leaves of Craibiodendron yunnanense. The compounds were isolated and purified from the leaves of C. yunnanense by a combination of various chromatographic techniques including column chromatography over polyamide, silica gel, Sephadex LH-20, and reversed-phase HPLC. Their structures were identified by extensive spectroscopic analyses including MS and NMR data. As a result, 10 compounds, including melionoside F(1), meliosmaionol D(2), naringenin(3), quercetin-3-O-α-L-arabinopyranoside(4), epicatechin(5), quercetin-3'-glucoside(6), corbulain Ib(7), loliolide(8), asiatic acid(9), and ursolic acid(10), were isolated. Compounds 1 and 2 were two new compounds, and compound 7 was isolated from this genus for the first time. All compounds showed no significant cytotoxic activity by MTT assay.
Quercetin
;
Ericaceae
;
Plant Leaves
;
Catechin
;
Chromatography, High Pressure Liquid
9.Study on the related factors of antiviral treatment in previously reported hepatitis C patients based on the Andersen model.
Peng XU ; Jie Jun YU ; Wan Yue ZHANG ; Dan Dan YANG ; Chuan Wu SUN ; Xing Yun CHEN ; Qing YUAN ; Shao Dong YE ; Liang ZHAO ; Zhong Fu LIU ; Jian LI
Chinese Journal of Hepatology 2023;31(1):49-55
Objective: To understand the basic characteristics of previously reported patients with hepatitis C and analyze the related factors affecting their antiviral treatment. Methods: A convenient sampling method was adopted. Patients who had been previously diagnosed with hepatitis C in the Wenshan Prefecture of Yunnan Province and Xuzhou City of Jiangsu Province were contacted by telephone for an interview study. The Andersen health service utilization behavior model and related literature were used to design the research framework for antiviral treatment in previously reported hepatitis C patients. A step-by-step multivariate regression analysis was used in previously reported hepatitis C patients treated with antiviral therapy. Results: A total of 483 hepatitis C patients, aged 51.73 ± 12.06 years, were investigated. The proportion of male, agricultural occupants who were registered permanent residents, farmers and migrant workers was 65.24%, 67.49%, and 58.18%, respectively. Han ethnicity (70.81%), married (77.02%), and junior high school and below educational level (82.61%) were the main ones. Multivariate logistic regression analysis results showed that married patients with hepatitis C (OR = 3.19, 95% CI: 1.93-5.25, compared with unmarried, divorced, and widowed patients) with high school education or above (OR = 2.54, 95% CI: 1.54-4.20, compared with patients with junior high school education or below) were more likely to receive antiviral treatment in the predisposition module. Patients with severe self-perceived hepatitis C in the need factor module (compared with patients with mild self-perceived disease, OR = 3.36, 95% CI: 2.09-5.40) were more likely to receive treatment. In the competency module, the family's per capita monthly income was more than 1,000 yuan (compared with patients with per capita monthly income below 1,000 yuan, OR = 1.59, 95% CI: 1.02-2.47), and the patients had a high level of awareness of hepatitis C knowledge (compared with patients with a low level of knowledge, OR = 1.54, 95% CI: 1.01-2.35), and the family members who knew the patient's infection status (compared with patients with an unknown infection status, OR = 4.59, 95% CI: 2.24-9.39) were more likely to receive antiviral treatment. Conclusion: Different income, educational, and marital statuses are related to antiviral treatment behavior in hepatitis C patients. Family support of hepatitis C patients receiving hepatitis C-related knowledge and their families knowing the infection status is more important in promoting the antiviral treatment of patients, suggesting that in the future, we should further strengthen the hepatitis C knowledge of hepatitis C patients, especially the family support of hepatitis C patients' families in treatment.
Humans
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Male
;
Antiviral Agents/therapeutic use*
;
China
;
Hepatitis C/drug therapy*
;
Hepacivirus
;
Logistic Models
10. The protective effect of orcinol glucoside on dexamethasone induced osteoblast cell damage through inhibition of glucocorticoid receptor nucleus translocation
Xin-Yun-Xi HE ; Wan-Lu ZHAO ; Yang YU ; Yan LIU ; Qiao-Yan ZHANG ; Quan-Long ZHANG ; Lu-Ping QIN
Chinese Pharmacological Bulletin 2023;39(7):1346-1353
Aim To investigate the protective effect of orcinol glucoside on dexamethasone(DEX)-induced osteoblast injury and its mechanism. Methods Primary osteoblasts were extracted from calvaria of neonatal mice and cultured in medium with DEX(1 μmol•L

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