1.The Inquiry Skills of Arthralgia
Xizhi LI ; Zhaoping LV ; Rui FENG ; Ruomei CUI
Journal of Kunming Medical University 2007;0(S2):-
Arthralgia is a common syndrome of joint and rheumatoid disease.Inquiry has significant value in diagnosis of joint disease.By thoroughly elaborative inquiry,we can obtain main information and made the primary diagnosis for most patients with arthralgia.Nevertheless it is much more difficult for the beginners to do inquiry considering the complex display and the numerous arthrosis.Inquiry of the following five main points may help the beginners to acquire the techniques quickly:(1)Time,degree of urgency and remote cause;(2)The numbers and location of arthritis affected;(3)Region appearance and joint function;(4)Simultaneous phenomenon;(5)Informations of diagnose and treat before.
2.Aspirin inhibition of expression of inflammatory proteins induced by oxidized low-density lipoprotein in HUVECs
Wei WU ; Ruomei QI ; Rui LI ; Xin GAO ; Li BAO
Chinese Pharmacological Bulletin 1986;0(04):-
Aim To evaluate the effects of aspirin on the expression of inflammatory proteins induced by oxidized low-density lipoprotein(ox-LDL) in human vascular endothelial cells (HUVECs). Methods HUVECs were stimulated with different concentrations of ox-LDL. The expression of inflammatory proteins was detected by Western blot.Intracellular ROS generation was measured by flow cytometry using perexide-sensitive flurscent probe 2′, 7′-dichrofluorescein diacetate(DCFH-DA).Results ① Aspirin inhibited COX-2 expression induced by ox-LDL. Cells were preincubated with 2.5 mmol?L-1, 5 mmol?L-1 of aspirin or without any treatment for 30 min and then stimulated by 0.3 g?L-1 ox-LDL for 16 h, COX-2 expression was reduced by treating of aspirin.COX-2 expression was enhanced after the stimulation with ox-LDL, and aspirin inhibited the increasing.② Aspirin suppressed ICAM-1 expression induced by ox-LDL in HUVECs. ICAM-1 expression was increased by ox-LDL stimulation for 16 h, and aspirin significantly down-regulated the expression. Similar results were obtained by immunofluorescence.③ Aspirin partially reduced ROS production induced by ox-LDL in HUVECs. After stimulation with 0.3 g?L-1 ox-LDL for 16 h, the intracellular level of ROS was increased, however, aspirin failed to fully inhibit the phenomenon.Conclusion Nonsteroidal anti-inflammatory drugs (NSAID) aspirin significantly down-regulated the expression of COX-2 and ICAM-1 induced by ox-LDL.The results suggested that aspirin could reduce the inflammation responses mediated by ox-LDL on HUVECs in atherosclerosis.
3.Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones as potential HIV-1 inhibitors.
Yumeng WU ; Chengrun TANG ; Ruomei RUI ; Liumeng YANG ; Wei DING ; Jiangyuan WANG ; Yiming LI ; Christopher C LAI ; Yueping WANG ; Ronghua LUO ; Weilie XIAO ; Hongbing ZHANG ; Yongtang ZHENG ; Yanping HE
Acta Pharmaceutica Sinica B 2020;10(3):512-528
A series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones were synthesized and their anti-HIV-1 activities were evaluated. Most of these compounds were highly active against wild-type (WT) HIV-1 strain (IIIB) with EC values in the range of 0.0038-0.4759 μmol/L. Among those compounds, had an EC value of 3.8 nmol/L and SI (selectivity index) of up to 25,468 indicating excellent activity against WT HIV-1. anti-HIV-1 activity and resistance profile studies suggested that compounds and displayed potential anti-HIV-1 activity against laboratory adapted strains and primary isolated strains including different subtypes and tropism strains (ECs range from 4.3 to 63.6 nmol/L and 18.9-219.3 nmol/L, respectively). On the other hand, it was observed that those two compounds were less effective with EC values of 2.77 and 4.87 μmol/L for HIV-1A (K103N + Y181C). The activity against reverse transcriptase (RT) was also evaluated for those compounds. Both and obtained sub-micromolar IC values showing their potential in RT inhibition. The pharmacokinetics examination in rats indicated that compound has acceptable pharmacokinetic properties and bioavailability. Preliminary structure-activity relationships and molecular modeling studies were also discussed.