1.Genetic Subtypes and Pretreatment Drug Resistance in the Newly Reported Human Immunodeficiency Virus-Infected Men Aged≥50 Years Old in Guangxi.
Ning-Ye FANG ; Wen-Cui WEI ; Jian-Jun LI ; Ping CEN ; Xian-Xiang FENG ; Dong YANG ; Kai-Ling TANG ; Shu-Jia LIANG ; Yu-Lan SHAO ; Hua-Xiang LU ; He JIANG ; Qin MENG ; Shuai-Feng LIU ; Qiu-Ying ZHU ; Huan-Huan CHEN ; Guang-Hua LAN ; Shi-Xiong YANG ; Li-Fang ZHOU ; Jing-Lin MO ; Xian-Min GE
Acta Academiae Medicinae Sinicae 2023;45(3):399-404
		                        		
		                        			
		                        			Objective To analyze the genetic subtypes of human immunodeficiency virus (HIV) and the prevalence of pretreatment drug resistance in the newly reported HIV-infected men in Guangxi. Methods The stratified random sampling method was employed to select the newly reported HIV-infected men aged≥50 years old in 14 cities of Guangxi from January to June in 2020.The pol gene of HIV-1 was amplified by nested reverse transcription polymerase chain reaction and then sequenced.The mutation sites associated with drug resistance and the degree of drug resistance were then analyzed. Results A total of 615 HIV-infected men were included in the study.The genetic subtypes of CRF01_AE,CRF07_BC,and CRF08_BC accounted for 57.4% (353/615),17.1% (105/615),and 22.4% (138/615),respectively.The mutations associated with the resistance to nucleoside reverse transcriptase inhibitors (NRTI),non-nucleoside reverse transcriptase inhibitors (NNRTI),and protease inhibitors occurred in 8 (1.3%),18 (2.9%),and 0 patients,respectively.M184V (0.7%) and K103N (1.8%) were the mutations with the highest occurrence rates for the resistance to NRTIs and NNRTIs,respectively.Twenty-two (3.6%) patients were resistant to at least one type of inhibitors.Specifically,4 (0.7%),14 (2.3%),4 (0.7%),and 0 patients were resistant to NRTIs,NNRTIs,both NRTIs and NNRTIs,and protease inhibitors,respectively.The pretreatment resistance to NNRTIs had much higher frequency than that to NRTIs (2.9% vs.1.3%;χ2=3.929,P=0.047).The prevalence of pretreatment resistance to lamivudine,zidovudine,tenofovir,abacavir,rilpivirine,efavirenz,nevirapine,and lopinavir/ritonavir was 0.8%, 0.3%, 0.7%, 1.0%, 1.3%, 2.8%, 2.9%, and 0, respectively. Conclusions CRF01_AE,CRF07_BC,and CRF08_BC are the three major strains of HIV-infected men≥50 years old newly reported in Guangxi,2020,and the pretreatment drug resistance demonstrates low prevalence.
		                        		
		                        		
		                        		
		                        			Male
		                        			;
		                        		
		                        			Humans
		                        			;
		                        		
		                        			Middle Aged
		                        			;
		                        		
		                        			Reverse Transcriptase Inhibitors/therapeutic use*
		                        			;
		                        		
		                        			HIV Infections/drug therapy*
		                        			;
		                        		
		                        			Drug Resistance, Viral/genetics*
		                        			;
		                        		
		                        			China/epidemiology*
		                        			;
		                        		
		                        			Mutation
		                        			;
		                        		
		                        			HIV-1/genetics*
		                        			;
		                        		
		                        			Protease Inhibitors/therapeutic use*
		                        			;
		                        		
		                        			Genotype
		                        			
		                        		
		                        	
2.Clinical value of intracranial pressure monitoring combined with target temperature management in acute anterior circulation ischemic stroke
Ming ZHANG ; Jihui GE ; Yanru LI ; Zhiqiang REN ; Ju WANG ; Jinghe ZHAO ; Guang FENG
Chinese Journal of Neuromedicine 2023;22(8):772-779
		                        		
		                        			
		                        			Objective:To observe the clinical value of intracranial pressure (ICP) monitoring combined with target temperature management (TTM) in patients with acute anterior circulation ischemic stroke after mechanical thrombectomy.Methods:A prospective analysis was performed. Ninety-two patients with acute anterior circulation ischemic stroke who received mechanical thrombectomy from March 2019 to June 2022 in Department of Neurosurgery, He'nan Provincial People's Hospital were enrolled. Within 1-5 d of mechanical thrombectomy, these patients were randomly divided into observation group ( n=46) and control group ( n=46). The patients in observation group received comprehensive management for neurological critical illness through multimodal monitoring such as ICP real-time monitoring combined with TTM (controlling the core temperature at 33℃-35℃), while patients in control group received simple ICP real-time monitoring. ICP monitoring for both groups lasted for 5-7 d, and routine symptomatic support treatment was given. Stepwise treatment was adopted based on real-time changes of ICP. The differences in clinical data, ICP at different times, incidence of adverse events, length of hospital stay, mortality rate, and prognoses were compared between the 2 groups. Results:On the 2 nd, 3 rd, 4 th, and 5 th d of monitoring, the observation group had significantly decreased ICP compared with the control group ( P<0.05). Both observation group and control group had significantly increased ICP on the 2 nd, 3 rd, 4 th, and 5 th d of monitoring compared with that on the 1 st d of monitoring ( P<0.05). Compared with the control group, the observation group had statistically higher incidences of shivers and electrolyte disorders, and statistically lower incidences of unstable blood pressure, cerebral heart syndrome, septic shock, and cerebral hernia during hospitalization ( P<0.05). Compared with the control group, the observation group had significantly shortened hospital stay, and statistically lower modified Rankin scale (mRS) scores, higher Glasgow outcome scale-extended (GOS-E) scores, higher good prognosis rate, and lower mortality rate 6 months after mechanical thrombectomy ( P<0.05). Compared with the control group, the observation group had statistically lower incidences of postoperative cerebral hemorrhage conversion and recurrent cerebral infarction ( P<0.05). Kaplan-Meier survival analysis showed that the survival rate in the observation group was significantly higher than that in the control group ( P<0.05). Conclusion:ICP monitoring combined with TTM can reduce early complications, shorten hospital stay, reduce mortality, and improve long-term prognosis in patients with acute anterior circulation ischemic stroke after mechanical thrombectomy.
		                        		
		                        		
		                        		
		                        	
3.Clinical treatment outcomes and their changes in extremely preterm twins: a multicenter retrospective study in Guangdong Province, China.
Bi-Jun SHI ; Ying LI ; Fan WU ; Zhou-Shan FENG ; Qi-Liang CUI ; Chuan-Zhong YANG ; Xiao-Tong YE ; Yi-Heng DAI ; Wei-Yi LIANG ; Xiu-Zhen YE ; Jing MO ; Lu DING ; Ben-Qing WU ; Hong-Xiang CHEN ; Chi-Wang LI ; Zhe ZHANG ; Xiao RONG ; Wei SHEN ; Wei-Min HUANG ; Bing-Yan YANG ; Jun-Feng LYU ; Hui-Wen HUANG ; Le-Ying HUO ; Hong-Ping RAO ; Wen-Kang YAN ; Xue-Jun REN ; Yong YANG ; Fang-Fang WANG ; Dong LIU ; Shi-Guang DIAO ; Xiao-Yan LIU ; Qiong MENG ; Yu WANG ; Bin WANG ; Li-Juan ZHANG ; Yu-Ge HUANG ; Dang AO ; Wei-Zhong LI ; Jie-Ling CHEN ; Yan-Ling CHEN ; Wei LI ; Zhi-Feng CHEN ; Yue-Qin DING ; Xiao-Yu LI ; Yue-Fang HUANG ; Ni-Yang LIN ; Yang-Fan CAI ; Sha-Sha HAN ; Ya JIN ; Guo-Sheng LIU ; Zhong-He WAN ; Yi BAN ; Bo BAI ; Guang-Hong LI ; Yue-Xiu YAN
Chinese Journal of Contemporary Pediatrics 2022;24(1):33-40
		                        		
		                        			OBJECTIVES:
		                        			To investigate the clinical treatment outcomes and the changes of the outcomes over time in extremely preterm twins in Guangdong Province, China.
		                        		
		                        			METHODS:
		                        			A retrospective analysis was performed for 269 pairs of extremely preterm twins with a gestational age of <28 weeks who were admitted to the department of neonatology in 26 grade A tertiary hospitals in Guangdong Province from January 2008 to December 2017. According to the admission time, they were divided into two groups: 2008-2012 and 2013-2017. Besides, each pair of twins was divided into the heavier infant and the lighter infant subgroups according to birth weight. The perinatal data of mothers and hospitalization data of neonates were collected. The survival rate of twins and the incidence rate of complications were compared between the 2008-2012 and 2013-2017 groups.
		                        		
		                        			RESULTS:
		                        			Compared with the 2008-2012 group, the 2013-2017 group (both the heavier infant and lighter infant subgroups) had lower incidence rates of severe asphyxia and smaller head circumference at birth (P<0.05). The mortality rates of both of the twins, the heavier infant of the twins, and the lighter infant of the twins were lower in the 2013-2017 group compared with the 2008-2012 group (P<0.05). Compared with the 2008-2012 group, the 2013-2017 group (both the heavier infant and lighter infant subgroups) had lower incidence rates of pulmonary hemorrhage, patent ductus arteriosus (PDA), periventricular-intraventricular hemorrhage (P-IVH), and neonatal respiratory distress syndrome (NRDS) and a higher incidence rate of bronchopulmonary dysplasia (P<0.05).
		                        		
		                        			CONCLUSIONS
		                        			There is a significant increase in the survival rate over time in extremely preterm twins with a gestational age of <28 weeks in the 26 grade A tertiary hospitals in Guangdong Province. The incidences of severe asphyxia, pulmonary hemorrhage, PDA, P-IVH, and NRDS decrease in both the heavier and lighter infants of the twins, but the incidence of bronchopulmonary dysplasia increases. With the improvement of diagnosis and treatment, the multidisciplinary collaboration between different fields of fetal medicine including prenatal diagnosis, obstetrics, and neonatology is needed in the future to jointly develop management strategies for twin pregnancy.
		                        		
		                        		
		                        		
		                        			Bronchopulmonary Dysplasia/epidemiology*
		                        			;
		                        		
		                        			Female
		                        			;
		                        		
		                        			Gestational Age
		                        			;
		                        		
		                        			Humans
		                        			;
		                        		
		                        			Infant
		                        			;
		                        		
		                        			Infant, Extremely Premature
		                        			;
		                        		
		                        			Infant, Newborn
		                        			;
		                        		
		                        			Pregnancy
		                        			;
		                        		
		                        			Respiratory Distress Syndrome, Newborn/epidemiology*
		                        			;
		                        		
		                        			Retrospective Studies
		                        			;
		                        		
		                        			Treatment Outcome
		                        			
		                        		
		                        	
4.Effects of Human Immunodeficiency Virus-positive Mothers Receiving Antiretroviral Therapy to Prevent Mother-to-child Transmission on the Growth and Development of 18-month-old Children in Lingshan County of Guangxi.
Xian-Min GE ; Mei LIN ; Jin-Mei CHEN ; Jin-Hui ZHU ; Guang-Hua LAN ; Yu YAN ; Huan-Huan CHEN ; Liu-Hong LUO ; Shan-Shan LI ; Bin LI ; Guang-Hua HUANG ; Jia-Wei LI ; Yue-Qin DENG ; Ping-Jing WEN ; Yu-Man HUANG ; Qiu-Ying ZHU ; Qin MENG ; Shuai-Feng LIU ; Xiu-Ling WU ; Jing-Hua HUANG ; Hua-Xiang LU
Acta Academiae Medicinae Sinicae 2021;43(5):743-748
		                        		
		                        			
		                        			Objective To evaluate the effects of antiretroviral therapy(ART)for the prevention of mother-to-child transmission(PMTCT)of acquired immune deficiency syndrome(AIDS)on the growth and development of 18-month-old children born by human immunodeficiency virus(HIV)-positive pregnant women in Lingshan County,Guangxi Zhuang Autonomous Region,and provide scientific evidence for improving the ART medication plan for PMTCT.Methods Lingshan County,ranking the first in the HIV-epidemic counties of Guangxi,was selected as the research site.According to the design of retrospective case-control study,we assigned all the subjects into the case group and the control group:(1)The case group included the HIV-positive pregnant women who had received ART for PMTCT and their HIV-negative infants in Lingshan County from 2010 to 2017.The historical cards and PMTCT data of them were collected from the national PMTCT database.(2)The control group included the healthy pregnant women and their healthy babies born in the Lingshan Maternity and Infant Hospital in 2017,and the children's growth and development data were collected.The stunted growth in children was defined as at least one of the three main indicators of body height,body weight,and head circumference below the normal range.Results The number of HIV-positive mothers and their infants in the case group was 391 and 368,respectively,and 87.21%(341/391)and 95.38%(351/368)of mothers and infants respectively received ART medication.The HIV positive rate,mortality rate,and mother-to-child transmission rate of 18-month-old children were 1.36%(5/368),4.35%(16/368),and 2.01%(5/249),respectively.The incidence of stunted growth of 18-month-old children in the case group and the control group was 42.12%(155/368)and 23.06%(101/438),respectively,with significant difference(
		                        		
		                        		
		                        		
		                        			Case-Control Studies
		                        			;
		                        		
		                        			China/epidemiology*
		                        			;
		                        		
		                        			Female
		                        			;
		                        		
		                        			Growth and Development
		                        			;
		                        		
		                        			HIV
		                        			;
		                        		
		                        			HIV Infections/prevention & control*
		                        			;
		                        		
		                        			Humans
		                        			;
		                        		
		                        			Infant
		                        			;
		                        		
		                        			Infectious Disease Transmission, Vertical/prevention & control*
		                        			;
		                        		
		                        			Mothers
		                        			;
		                        		
		                        			Pregnancy
		                        			;
		                        		
		                        			Pregnancy Complications, Infectious/drug therapy*
		                        			;
		                        		
		                        			Retrospective Studies
		                        			
		                        		
		                        	
5.Coronavirus disease 2019 in pregnant and non-pregnant women: a retrospective study.
Ying ZHA ; Ge CHEN ; Xun GONG ; Yuan-Yuan WU ; Xing-Guang LIN ; Jian-Li WU ; Ya-Fei HUANG ; Yu-Qi LI ; Ying ZHANG ; Dong-Rui DENG ; Su-Hua CHEN ; Fu-Yuan QIAO ; Ling FENG ; Wan-Jiang ZENG ; Ke-Zhen LI ; Hai-Yi LIU
Chinese Medical Journal 2021;134(10):1218-1220
6.Inverted U-Shaped Associations between Glycemic Indices and Serum Uric Acid Levels in the General Chinese Population: Findings from the China Cardiometabolic Disease and Cancer Cohort (4C) Study.
Yuan Yue ZHU ; Rui Zhi ZHENG ; Gui Xia WANG ; Li CHEN ; Li Xin SHI ; Qing SU ; Min XU ; Yu XU ; Yu Hong CHEN ; Xue Feng YU ; Li YAN ; Tian Ge WANG ; Zhi Yun ZHAO ; Gui Jun QIN ; Qin WAN ; Gang CHEN ; Zheng Nan GAO ; Fei Xia SHEN ; Zuo Jie LUO ; Ying Fen QIN ; Ya Nan HUO ; Qiang LI ; Zhen YE ; Yin Fei ZHANG ; Chao LIU ; You Min WANG ; Sheng Li WU ; Tao YANG ; Hua Cong DENG ; Jia Jun ZHAO ; Lu Lu CHEN ; Yi Ming MU ; Xu Lei TANG ; Ru Ying HU ; Wei Qing WANG ; Guang NING ; Mian LI ; Jie Li LU ; Yu Fang BI
Biomedical and Environmental Sciences 2021;34(1):9-18
		                        		
		                        			Objective:
		                        			The relationship between serum uric acid (SUA) levels and glycemic indices, including plasma glucose (FPG), 2-hour postload glucose (2h-PG), and glycated hemoglobin (HbA1c), remains inconclusive. We aimed to explore the associations between glycemic indices and SUA levels in the general Chinese population.
		                        		
		                        			Methods:
		                        			The current study was a cross-sectional analysis using the first follow-up survey data from The China Cardiometabolic Disease and Cancer Cohort Study. A total of 105,922 community-dwelling adults aged ≥ 40 years underwent the oral glucose tolerance test and uric acid assessment. The nonlinear relationships between glycemic indices and SUA levels were explored using generalized additive models.
		                        		
		                        			Results:
		                        			A total of 30,941 men and 62,361 women were eligible for the current analysis. Generalized additive models verified the inverted U-shaped association between glycemic indices and SUA levels, but with different inflection points in men and women. The thresholds for FPG, 2h-PG, and HbA1c for men and women were 6.5/8.0 mmol/L, 11.0/14.0 mmol/L, and 6.1/6.5, respectively (SUA levels increased with increasing glycemic indices before the inflection points and then eventually decreased with further increases in the glycemic indices).
		                        		
		                        			Conclusion
		                        			An inverted U-shaped association was observed between major glycemic indices and uric acid levels in both sexes, while the inflection points were reached earlier in men than in women.
		                        		
		                        		
		                        		
		                        			Aged
		                        			;
		                        		
		                        			Asian Continental Ancestry Group
		                        			;
		                        		
		                        			Blood Glucose/analysis*
		                        			;
		                        		
		                        			China/epidemiology*
		                        			;
		                        		
		                        			Cohort Studies
		                        			;
		                        		
		                        			Diabetes Mellitus/blood*
		                        			;
		                        		
		                        			Female
		                        			;
		                        		
		                        			Glucose Tolerance Test
		                        			;
		                        		
		                        			Glycated Hemoglobin A/analysis*
		                        			;
		                        		
		                        			Glycemic Index
		                        			;
		                        		
		                        			Humans
		                        			;
		                        		
		                        			Male
		                        			;
		                        		
		                        			Middle Aged
		                        			;
		                        		
		                        			Uric Acid/blood*
		                        			
		                        		
		                        	
7.Mechanisms exploration of Angelicae Sinensis Radix and Ligusticum Chuanxiong Rhizoma herb-pair for liver fibrosis prevention based on network pharmacology and experimental pharmacologylogy.
Jian-Zhi WU ; Ya-Jing LI ; Guang-Rui HUANG ; Bing XU ; Fei ZHOU ; Run-Ping LIU ; Feng GAO ; Jun-De GE ; Ya-Jie CAI ; Qi ZHENG ; Xiao-Jiaoyang LI
Chinese Journal of Natural Medicines (English Ed.) 2021;19(4):241-254
		                        		
		                        			
		                        			Angelicae Sinensis Radix (Danggui) and Ligusticum Chuanxiong Rhizoma (Chuan Xiong) herb-pair (DC) have been frequently used in Traditional Chinese medicine (TCM) prescriptions for hundreds of years to prevent vascular diseases and alleviate pain. However, the mechanism of DC herb-pair in the prevention of liver fibrosis development was still unclear. In the present study, the effects and mechanisms of DC herb-pair on liver fibrosis were examined using network pharmacology and mouse fibrotic model. Based on the network pharmacological analysis of 13 bioactive ingredients found in DC, a total of 46 targets and 71 pathways related to anti-fibrosis effects were obtained, which was associated with mitogen-activated protein kinase (MAPK) signal pathway, hepatic inflammation and fibrotic response. Furthermore, this hypothesis was verified using carbon tetrachloride (CCl
		                        		
		                        		
		                        		
		                        	
8.Comprehensive profiling and characterization of the absorbed components and metabolites in mice serum and tissues following oral administration of Qing-Fei-Pai-Du decoction by UHPLC-Q-Exactive-Orbitrap HRMS.
Wei LIU ; Jian HUANG ; Feng ZHANG ; Cong-Cong ZHANG ; Rong-Sheng LI ; Yong-Li WANG ; Chao-Ran WANG ; Xin-Miao LIANG ; Wei-Dong ZHANG ; Ling YANG ; Ping LIU ; Guang-Bo GE
Chinese Journal of Natural Medicines (English Ed.) 2021;19(4):305-320
		                        		
		                        			
		                        			Qing-Fei-Pai-Du decoction (QFPDD) is a Chinese medicine compound formula recommended for combating corona virus disease 2019 (COVID-19) by National Health Commission of the People's Republic of China. The latest clinical study showed that early treatment with QFPDD was associated with favorable outcomes for patient recovery, viral shedding, hospital stay, and course of the disease. However, the effective constituents of QFPDD remain unclear. In this study, an UHPLC-Q-Orbitrap HRMS based method was developed to identify the chemical constituents in QFPDD and the absorbed prototypes as well as the metabolites in mice serum and tissues following oral administration of QFPDD. A total of 405 chemicals, including 40 kinds of alkaloids, 162 kinds of flavonoids, 44 kinds of organic acids, 71 kinds of triterpene saponins and 88 kinds of other compounds in the water extract of QFPDD were tentatively identified via comparison with the retention times and MS/MS spectra of the standards or refereed by literature. With the help of the standards and in vitro metabolites, 195 chemical components (including 104 prototypes and 91 metabolites) were identified in mice serum after oral administration of QFPDD. In addition, 165, 177, 112, 120, 44, 53 constituents were identified in the lung, liver, heart, kidney, brain, and spleen of QFPDD-treated mice, respectively. These findings provided key information and guidance for further investigation on the pharmacologically active substances and clinical applications of QFPDD.
		                        		
		                        		
		                        		
		                        			Administration, Oral
		                        			;
		                        		
		                        			Alkaloids/analysis*
		                        			;
		                        		
		                        			Animals
		                        			;
		                        		
		                        			COVID-19
		                        			;
		                        		
		                        			Chromatography, High Pressure Liquid
		                        			;
		                        		
		                        			Drugs, Chinese Herbal/pharmacokinetics*
		                        			;
		                        		
		                        			Flavonoids/analysis*
		                        			;
		                        		
		                        			Mice
		                        			;
		                        		
		                        			SARS-CoV-2
		                        			;
		                        		
		                        			Saponins/analysis*
		                        			;
		                        		
		                        			Triterpenes/analysis*
		                        			
		                        		
		                        	
9.Effect of electroacupuncture on small airway function in patients with stable chronic obstructive pulmonary disease.
Ying HE ; Gui-Yuan LI ; Ze-Guang ZHENG ; Yi GAO ; Jun-Hui PAN ; Feng WANG ; Wan-Yi HUANG ; Yan GE ; Guang-En ZHONG ; Juan TONG
Chinese Acupuncture & Moxibustion 2021;41(8):861-865
		                        		
		                        			OBJECTIVE:
		                        			To observe the regulatory effect of electroacupuncture (EA) on small airway function and exercise tolerance in patients with stable chronic obstructive pulmonary disease (COPD).
		                        		
		                        			METHODS:
		                        			A total of 62 patients with stable COPD were randomized into an observation group (31 cases, 1 case dropped off) and a control group (31 cases, 5 cases dropped off). On the base of routine medication and aerobic exercise, the patients of the two groups all received EA at Danzhong (CV 17), Rugen (ST 18), Guanyuan (CV 4), Zhongwan (CV 12), Tianshu (ST 25) and Yingchuang (ST 16). In the observation group, filiform needles were used and inserted perpendicularly, 3 mm in depth. In the control group, the placebo needling method was performed, in which the needle was not inserted through skin at each point. In both groups, electric stimulation with low-frequency electronic pulse instrument was exerted, with continuous wave, 2 Hz in frequency, lasting 30 min each time in the two groups. The treatment was given once every other day, 3 times a week, for 14 treatments totally. Before and after treatment, the following indexes were compared in patients between the two groups, i.e. the lung function indexes (forced expiratory volume in first second [FEV1], forced vital capacity [FVC], the ratio of FEV1 to FVC [FEV1/FVC], maximal voluntary ventilation [MVV], the percentage of maximal expiratory flow [MEF] at 25% of FVC exhaled [MEF25], MEF50 and MEF75 in predicted value), cardiopulmonary exercise test indexs (metabolic equivalent [METS], oxygen uptake per kg body weight [VO
		                        		
		                        			RESULTS:
		                        			After treatment, FVC%, MVV%, MEF75%, MEF50%, VO
		                        		
		                        			CONCLUSION
		                        			Electroacupuncture can improve the respiratory function and exercise tolerance in COPD patients through removing small airway obstruction and increasing ventilation.
		                        		
		                        		
		                        		
		                        			Electroacupuncture
		                        			;
		                        		
		                        			Exercise Tolerance
		                        			;
		                        		
		                        			Forced Expiratory Volume
		                        			;
		                        		
		                        			Humans
		                        			;
		                        		
		                        			Pulmonary Disease, Chronic Obstructive/therapy*
		                        			;
		                        		
		                        			Respiratory Function Tests
		                        			
		                        		
		                        	
10.Pancreatic lipase inhibitory constituents from Fructus Psoraleae.
Xu-Dong HOU ; Li-Lin SONG ; Yun-Feng CAO ; Yi-Nan WANG ; Qi ZHOU ; Sheng-Quan FANG ; Da-Chang WU ; Shi-Zhu ZANG ; Lu CHEN ; Yue BAI ; Guang-Bo GE ; Jie HOU
Chinese Journal of Natural Medicines (English Ed.) 2020;18(5):369-378
		                        		
		                        			
		                        			Pancreatic lipase (PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae (FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL (IC < 10 μmol·L). Inhibition kinetic analyses demonstrated that isobavachalcone, bavachalcone and corylifol A acted as mixed inhibitors against PL-mediated 4-methylumbelliferyl oleate (4-MUO) hydrolysis, with the K values of 1.61, 3.77 and 10.16 μmol·L, respectively. Furthermore, docking simulations indicated that two chalcones (isobavachalcone and bavachalcone) could interact with the key residues located in the catalytic cavity of PL via hydrogen binding and hydrophobic interactions. Collectively, these finding provided solid evidence to support that Fructus Psoraleae contained bioactive compounds with lipid-lowering effects via targeting PL, and also suggested that the chalcones in Fructus Psoraleae could be used as ideal leading compounds to develop novel PL inhibitors.
		                        		
		                        		
		                        		
		                        	
            
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