1.Remission and remission-related factors in lupus nephritis patients: a cohort study
Yi YANG ; Ming KU ; Ran LUO ; Rui ZENG ; Shuwang GE ; Gang XU
Chinese Journal of Nephrology 2017;33(8):567-572
Objective To explore prognosis and remission-related factors in lupus nephritis (LN) patients.Methods Patients diagnosed as LN by renal biopsy in Tongji Hospital Affiliated to Tongji Medical College,Huazhong University of Science and Technology between Jan 1,2011 and July 31,2016 were enrolled.All related baseline clinical data was recorded and regular follow-up was performed.Kaplan-Meier curves was used to analyze partial remission and complete remission rates.Log-rank test was performed to compare remission rates of patients with nephrotic-range proteinuria (24-hour proteinuria≥3.5 g) and without nephrotic-range proteinuria (24-hour proteinuria<3.5 g).Univariate and muhivariate Cox regression analyses were performed to evaluate the remission-related factors in different periods.Results A total of 115 patients,with 88.7% female and (31.5±9.5)years mean age,were followed up for up to 5 years.During follow-up period 2 patients died and 1 dialyzed.The 6-,12-,24-and 36-and 48-month renal partial remission and complete remission rates were 33.3%,58.2%,71.5%,84.0%,89.6%,and 18.9%,40.5%,67.3%,79.4%,87.0%,respectively.Patients without nephrotic-range proteinuria had higher complete remission than patients with nephrotic -range proteinuria (HR=2.01,95%CI 1.15-3.34,P=0.014),but there was no difference in their partial remission (HR=1.33,95% CI 0.74-2.43,P=0.341).Multivariate Cox regression model indicated that every 1 g/L increase in baseline level of serum albumin was associated with increased 8% and 9% risk,respectively,in partial remission (HR=1.08,95%CI 1.01-1.15,P=0.024) and complete remission (HR=1.09,95%CI 1.01-1.07,P=0.038).Conclusions Around half of LN patients reach remission during 1 year.Patients without nephrotic-range proteinuria have higher complete remission,and serum albumin is a remission-related factors.
2.Improving the positional adaptability: structure-based design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Kaijun JIN ; Minjie LIU ; Chunlin ZHUANG ; Erik DE CLERCQ ; Christophe PANNECOUQUE ; Ge MENG ; Fener CHEN
Acta Pharmaceutica Sinica B 2020;10(2):344-357
In order to improve the positional adaptability of our previously reported naphthyl diaryltriazines (NP-DATAs), synthesis of a series of novel biphenyl-substituted diaryltriazines (BP-DATAs) with a flexible side chain attached at the C-6 position is presented. These compounds exhibited excellent potency against wild-type (WT) HIV-1 with EC values ranging from 2.6 to 39 nmol/L and most of them showed low nanomolar anti-viral potency against a panel of HIV-1 mutant strains. Compounds and had the best activity against WT, single and double HIV-1 mutants and reverse transcriptase (RT) enzyme comparable to two reference drugs (EFV and ETR) and our lead compound NP-DATA (). Molecular modeling disclosed that the side chain at the C-6 position of DATAs occupied the entrance channel of the HIV-1 reverse transcriptase non-nucleoside binding pocket (NNIBP) attributing to the improved activity. The preliminary structure-activity relationship and PK profiles were also discussed.
3.Analysis of clinical and endoscopic characteristics of colorectal polyps in children.
Feng Fan WANG ; Ying FANG ; Xiao Xia REN ; Hong Bin YANG ; Ku Ku GE ; Han Hua ZHANG ; Hua WANG ; Li Na SUN
Chinese Journal of Preventive Medicine 2022;56(9):1327-1332
To analyze the clinical and endoscopic characteristics of colorectal polyps in children, and to explore the detection rate, age and gender distribution characteristics, endoscopic treatment effect and follow-up monitoring of colorectal polyps in children, so as to provide reference for disease management of colorectal polyps in children. The clinical and endoscopic characteristics of children with colorectal polyps in Xi 'an Children's Hospital from January 2019 to December 2019 were retrospectively analyzed. The patients were divided into 5 groups according to age (y): 0
Child
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Child, Preschool
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Colonic Polyps
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Colonoscopy
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Female
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Gastrointestinal Hemorrhage/complications*
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Humans
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Intestinal Polyps/surgery*
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Male
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Retrospective Studies
4.A new phenylpropanoid glycoside from fruit of Cornus officinalis.
Jun HE ; Jie-Kun XU ; Xue-Ge PAN ; Xian-Sheng YE ; Ying-Ying LIANG ; Ge-Fan YANG ; Wei-Ku ZHANG
China Journal of Chinese Materia Medica 2018;43(21):4264-4266
To investigate the chemical compounds from the ripe fruit of Cornus officinalis, a new phenylpropanoid glycoside 1-O-(6'-O-p-hydroxybenzoyl-β-D-glucopyranosyl)-p-phenylpropanol, named cornuphenylpropanoid A (1), were separated and purified by D101 macroporous resin, silica gel and ODS column chromatography. Its structure was extensively determined on basis of ¹H-NMR, ¹³C-NMR, DEPT, HSQC, HMBC and HR-ESI-MS spectroscopic data.
Cornus
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chemistry
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Fruit
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chemistry
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Glycosides
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chemistry
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isolation & purification
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Molecular Structure
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Phytochemicals
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chemistry
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isolation & purification
5.Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: Boosting the safety and metabolic stability.
Xin JIN ; Shuai WANG ; Limin ZHAO ; Wenjuan HUANG ; Yinxiang ZHANG ; Christophe PANNECOUQUE ; Erik DE CLERCQ ; Ge MENG ; Huri PIAO ; Fener CHEN
Acta Pharmaceutica Sinica B 2023;13(3):1192-1203
Our recent studies for nonnucleoside reverse transcriptase inhibitors identified a highly potent compound JK-4b against WT HIV-1 (EC50 = 1.0 nmol/L), but the poor metabolic stability in human liver microsomes (t 1/2 = 14.6 min) and insufficient selectivity (SI = 2059) with high cytotoxicity (CC50 = 2.08 μmol/L) remained major issues associated with JK-4b. The present efforts were devoted to the introduction of fluorine into the biphenyl ring of JK-4b, leading to the discovery of a novel series of fluorine-substituted NH2-biphenyl-diarylpyrimidines with noticeable inhibitory activity toward WT HIV-1 strain (EC50 = 1.8-349 nmol/L). The best compound 5t in this collection (EC50 = 1.8 nmol/L, CC50 = 117 μmol/L) was 32-fold in selectivity (SI = 66,443) compared to JK-4b and showed remarkable potency toward clinically multiple mutant strains, such as L100I, K103N, E138K, and Y181C. The metabolic stability of 5t was also significantly improved (t 1/2 = 74.52 min), approximately 5-fold higher than JK-4b in human liver microsomes (t 1/2 = 14.6 min). Also, 5t possessed good stability in both human and monkey plasma. No significant in vitro inhibition effect toward CYP enzyme and hERG was observed. The single-dose acute toxicity test did not induce mice death or obvious pathological damage. These findings pave the way for further development of 5t as a drug candidate.
6.Chemical constituents from ripe fruit of Cornus officinalis.
Xian-Sheng YE ; Jun HE ; Jia-Lin ZHANG ; Xiao-Bin PANG ; Lei ZHANG ; Hao-Yi QIAO ; Xue-Ge PAN ; Jia ZHANG ; Shu-Na LIU ; Wei-Ku ZHANG ; Jie-Kun XU
China Journal of Chinese Materia Medica 2016;41(24):4605-4609
To investigate the chemical compounds from the fruit of Cornus officinalis, six compounds were isolated and determined by extensive spectroscopic analysis as 6'-O-acetyl-7α-O-ethyl morroniside (1), (-)-isolariciresinol 3α-O-β-D-glucopyranoside(2), apigenin (3), cirsiumaldehyde(4), p-coumaric acid (5), caffeic acid (6). Compound 1 was a new iridoid glucoside,and compounds 2-4 were obtained from the Cornus genus for the first time. Compounds 2-6 were evaluated for the viability of PC12 cells when exposed in conditions of oxygen and glucose deprivation. The MTT results showed that compound 4 increased cell viability moderately in OGD/R treated PC12 cells at the concentration of 1.0 μmol•L⁻¹.