TY - JOUR A1 - Zhao, De-Wei A1 - Yu, Mang A1 - Hu, Kai A1 - Wang, Wei A1 - Yang, Lei A1 - Wang, Ben-Jie A1 - Gao, Xiao-Hong A1 - Guo, Yong-Ming A1 - Xu, Yong-Qing A1 - Wei, Yu-Shan A1 - Tian, Si-Miao A1 - Yang, Fan A1 - Wang, Nan A1 - Huang, Shi-Bo A1 - Xie, Hui A1 - Wei, Xiao-Wei A1 - Jiang, Hai-Shen A1 - Zang, Yu-Qiang A1 - Ai, Jun A1 - Chen, Yuan-Liang A1 - Lei, Guang-Hua A1 - Li, Yu-Jin A1 - Tian, Geng A1 - Li, Zong-Sheng A1 - Cao, Yong A1 - Ma, Li T1 - Prevalence of Nontraumatic Osteonecrosis of the Femoral Head and its Associated Risk Factors in the Chinese Population: Results from a Nationally Representative Survey JF - Chinese Medical Journal N2 - Background: Nontraumatic osteonecrosis of the femoral head (NONFH) is a debilitating disease that represents a significant financial burden for both individuals and healthcare systems. Despite its significance, however, its prevalence in the Chinese general population remains unknown. This study aimed to investigate the prevalence of NONFH and its associated risk factors in the Chinese population. Methods: A nationally representative survey of 30,030 respondents was undertaken from June 2012 to August 2013. All participants underwent a questionnaire investigation, physical examination of hip, and bilateral hip joint X-ray and/or magnetic resonance imaging examination. Blood samples were taken after overnight fasting to test serum total cholesterol, triglyceride, and high-density lipoprotein (HDL) and low-density lipoprotein (LDL) levels. We then used multivariate logistic regression analysis to investigate the associations between various metabolic, demographic, and lifestyle-related variables and NONFH. Results: NONFH was diagnosed in 218 subjects (0.725%) and the estimated NONFH cases were 8.12 million among Chinese people aged 15 years and over. The prevalence of NONFH was significantly higher in males than in females (1.02% vs. 0.51%, \(\chi^2\) = 24.997, P < 0.001). Among NONFH patients, North residents were subjected to higher prevalence of NONFH than that of South residents (0.85% vs. 0.61%, \(\chi^2\) = 5.847, P = 0.016). Our multivariate regression analysis showed that high blood levels of triglycerides, total cholesterol, LDL-cholesterol, and non-HDL-cholesterol, male, urban residence, family history of osteonecrosis of the femoral head, heavy smoking, alcohol abuse and glucocorticoid intake, overweight, and obesity were all significantly associated with an increased risk of NONFH. Conclusions: Our findings highlight that NONFH is a significant public health challenge in China and underscore the need for policy measures on the national level. Furthermore, NONFH shares a number of risk factors with atherosclerosis. KW - nontraumatic osteonecrosis of the femoral head KW - risk factors KW - idiopathic osteonecrosis KW - early-stage osteonecrosis KW - implantation KW - bone KW - marrow KW - follow-up KW - intake KW - avascular necrosis KW - occupational-status KW - cigarette smoking KW - alcohol KW - prevalence Y1 - 2015 U6 - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-138482 VL - 128 IS - 21 ER - TY - JOUR A1 - Tan, Aaron A1 - Babak, Maria V. A1 - Venkatesan, Gopalakrishnan A1 - Lim, Clarissa A1 - Klotz, Karl-Norbert A1 - Herr, Deron Raymond A1 - Cheong, Siew Lee A1 - Federico, Stephanie A1 - Spalluto, Giampiero A1 - Ong, Wei-Yi A1 - Chen, Yu Zong A1 - Loo, Jason Siau Ee A1 - Pastorin, Giorgia T1 - Design, Synthesis and Evaluation of New Indolylpyrimidylpiperazines for Gastrointestinal Cancer Therapy JF - Molecules N2 - Human A3 adenosine receptor hA3AR has been implicated in gastrointestinal cancer, where its cellular expression has been found increased, thus suggesting its potential as a molecular target for novel anticancer compounds. Observation made in our previous work indicated the importance of the carbonyl group of amide in the indolylpyrimidylpiperazine (IPP) for its human A2A adenosine receptor (hA2AAR) subtype binding selectivity over the other AR subtypes. Taking this observation into account, we structurally modified an indolylpyrimidylpiperazine (IPP) scaffold, 1 (a non-selective adenosine receptors’ ligand) into a modified IPP (mIPP) scaffold by switching the position of the carbonyl group, resulting in the formation of both ketone and tertiary amine groups in the new scaffold. Results showed that such modification diminished the A2A activity and instead conferred hA3AR agonistic activity. Among the new mIPP derivatives (3–6), compound 4 showed potential as a hA3AR partial agonist, with an Emax of 30% and EC50 of 2.89 ± 0.55 μM. In the cytotoxicity assays, compound 4 also exhibited higher cytotoxicity against both colorectal and liver cancer cells as compared to normal cells. Overall, this new series of compounds provide a promising starting point for further development of potent and selective hA3AR partial agonists for the treatment of gastrointestinal cancers. KW - gastrointestinal cancer KW - hA3AR KW - partial agonists KW - indolylpyrimidylpiperazines Y1 - 2019 U6 - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-193271 SN - 1420-3049 VL - 24 IS - 20 ER -