1.Research progress on the structure of HIV envelope glycoprotein and related HIV entry inhibitors
Chenglai XIA ; Shibo JIANG ; Shuwen LIU
Chinese Pharmacological Bulletin 2003;0(08):-
HIV-1 envelope glycoprotein gp120 and gp41 are considered as two important parts in viral entry.In the process of virus entry,CD4 first binds to gp120 and causes the conformation of gp120 to change.Furthermore the conformation of gp41 has also been changed.Many peptides,macromolecular compounds and small molecule compounds which bind to gp120 or gp41 can deter the progress of virus entry.These compounds can play an important role in halting the spread of HIV-1 in this way.The structure and interaction of gp120 and gp41 are reviewed here,as well as the anti-HIV agents blocking the HIV entry by targeting the HIV-1 envelope glycoprotein.
2.Peptidic HIV fusion inhibitors targeting envelope glycoprotein transmembrane subunit gp41
Shuwen LIU ; Shuguang WU ; Shib JIANG
Chinese Pharmacological Bulletin 2003;0(11):-
HIV envelope glycoprotein transmembrane subunit gp41 plays a major role in the fusion of viral and target cell membranes. The extracellular region of gp41 consists of N-terminal fusion peptide and downstream N- and C-heptad repeat (NHR and CHR) regions. The peptidesderived from the NHR and CHR regions, designated N- and C-peptides, respectively, have potent inhibitory activity on the HIV mediated cell fusion. C-peptide T-20 has just got the approval of U.S. FDA, which became the first success of one new class anti-HIV agents, named HIV-fusion inhibitors. However, a relatively long peptide such as T-20 suffers from several limitations including proteolytic sensitivity, large dosage, therefore it is unable to produced by gene engineering. Alternately, shorter peptidic fusion inhibitors and active peptides suitable for gene engineering are pursued. In the recent years, this kind of peptide modifications are hot spots in HIV research field and contribute a lot to the inhibitory mechanism of N- and C-peptide.
3.The application of magnetic resonance cholangiopancreatography in diagnosis of obstructive jaundice
Dongxin JIANG ; Lihua CAI ; Shuwen YUAN
Journal of Chinese Physician 2000;0(12):-
Objective To investigate the clinical application of magnetic resonance cholangiopancreatography(MRCP) in diagnosis of obstructive jaundice.Methods Thirty-three patients with obstructive jaundice were examined by MRCP and the accurate rate of MRCP was evaluated according to the result of operation and pathology examination.Results The positive rate of the orientation diagnosis of MRCP in obstruction was 100%(33/33).The accurate rates of qualitative diagnosis for benign disease and malignant obstructive jaundice were 87.5%(21/24) and 90%(9/10) respectively.The general qualitative diagnose accordance rate was 87.9%(29/33).Conclusion MRCP is simple,hurtless and safe for the diagnosis of obstructive jaundice and it deserves generalization in the clinical application.
4.Development of peptidic MERS-CoV entry inhibitors.
Shuai XIA ; Qian WANG ; Shuwen LIU ; Lu LU ; Shibo JIANG
Acta Pharmaceutica Sinica 2015;50(12):1513-9
In 2012, a new SARS-like coronavirus emerged in the Middle East, namely the Middle East respiratory syndrome coronavirus (MERS-CoV). It has caused outbreaks with high mortality. During infection of target cell, MERS-CoV S protein S1 subunit binds to the cellular receptor (DPP4), and its S2 subunit HR1 and HR2 regions intact with each other to form a stable six-helix bundle to mediate the fusion between virus and target cell membranes. Hence, blocking the process of six-helix bundle formation can effectively inhibit MERS-CoV entry into the target cells. This review focuses on the recent advance in the development of peptidic entry inhibitors targeting the MERS-CoV S2 subunit.
5.Small molecular agents against MERS-CoV infection.
Xiaoyun ZENG ; Lu LU ; Shibo JIANG ; Shuwen LIU
Acta Pharmaceutica Sinica 2015;50(12):1520-6
Middle East respiratory syndrome coronavirus (MERS-CoV) has caused outbreaks of SARS-like disease with 35% case-fatality rate, mainly in the Middle East. A more severe outbreak of MERS occurred recently in the Republic of Korea, where 186 people contracted the infections, causing great concern worldwide. So far, there has been no clinically available drug for the treatment of MERS-CoV infection. The potential drugs against MERS-CoV mainly consist of monoclonal antibodies, peptides and small molecular agents. Small molecular agents have an advantage of easier synthesis, lower cost in production and relatively higher stability. There is better chance for those candidates to gain a quick development. This article reviews the progress of developing small molecular MERS-CoV agents.
6.Discuss the unconventional bariatric surgery in China from the revisional bariatric surgery
Ruixiang HU ; Zhiyong DONG ; Shuwen JIANG ; Cunchuan WANG
International Journal of Surgery 2021;48(5):356-360
At present, the formal bariatric surgery approved by the American Society for Metabolic and Bariatric Surgery (ASMBS) includes adjustable gastric banding (AGB), sleeve gastrectomy (Sleeve gastrectomy, SG). ), Roux-en-Y gastric bypass (Roux-en-Y gastric bypass, RYGB), biliopancreatic diversion with duodenal switch (BPD-DS), mini gastric bypass (Mini-gastric bypass, MGB), single anastomosis gastric bypass (OAGB) and partial endoscopic surgery. According to the Chinese Society for Metabolic and Bariatric Surgery (CSMBS), the Chinese Obesity and Metabolic Surgery Database (COMES Database), and the Chinese Obesity and Metabolic Surgery Database (COMES Database), the Chinese Society for Metabolic and Bariatric Surgery (CSMBS) Chinese Obesity and Metabolic Surgery Collaborative, COMES Collaborative), Shanghai Weight Loss and Diabetes Surgery Data Management System, Shandong Province Weight Loss and Metabolic Surgery Case Registration System, Jiangsu Province Weight Loss and Metabolic Surgery Data Registration System, Great North China Weight Loss and Metabolic Surgery Statistics from the clinical data database and the Greater China Weight Loss and Metabolic Surgery Database. The domestically developed and approved bariatric surgery methods include RYGB, SG, MGB, OAGB, BPD-DS, AGB, combined sleeve gastrectomy (SG Plus), Jejunoileal Bypass (Jejunoileal Bypass, JJB), single stoma duodenal transposition (SADI-S), intragastric balloon (Balloon). However, there are still some irregular bariatric surgeries in China, which will cause some uncommon complications and bring great pain to patients. At the same time, it is also a huge challenge for regular bariatric surgeons who perform corrective surgeries. This article will review the revision surgery after bariatric surgery in China in the past 20 years, discusses a series of problems caused by non-standard bariatric surgery and the development of regular bariatric surgery.
7.The anti-HIV-1 entrance activity and mechanism of action of myriceric acid B from Rhoiptelea chiliantha Diels et Hand-Mazz
Chenglai XIA ; Qinchao MAO ; Runming LI ; Shibo JIANG ; Zhihong JIANG ; Shuwen LIU
Chinese Pharmacological Bulletin 2010;26(4):447-452
Aim To investigate the HIV-1 entry inhibitory activities of myriceric acid B and C isolated from Rhoiptelea chiliantha Diels et Hand-Mazz and their mechanism of action.Method The plasmids encoding envelope proteins of HIV-1 (pHXB2) and VSV (pVSV-G) were cotransfected 293T cells with pNL4-3.Luc.R-E- to produce HIV-1 Env pseudovirus and VSV-G pseudovirus,respectively,which were used for testing the antiviral activities of these compounds.ELISA and molecular docking were used to study the mechanism of action of the active compounds.Results Myriceric acid B could significantly inhibit the infection of HIV-1 Env pseudovirus with an IC_(50) of(8.3±0.2)mg·L~(-1).The carbonoxyl group at C-28 position and the hydroxyl group at the C-3 position of myriceric acid B are important for its anti-HIV-1 activity.Like other HIV-1 entry inhibitors targeting gp41 (eg,ADS-J1 and NB-64), myriceric acid B could also block the gp41 six-helix bundle formation.Molecular docking analysis suggests that myriceric acid B may bind to the hydrophobic cavity of the gp41 N-trimeric coiled coil.Conclusion Myriceric acid B is a potent HIV-1 entry inhibitor targeting gp41 and can serve as a lead compound for developing novel anti-HIV-1 drug.
8.Acid native polyacrylamide gel electrophoresis:a method for studying the mechanism of action of HIV entry inhibitor ADS-J1
Qinchao MAO ; Hongtao WANG ; Xugui LI ; Chenglai XIA ; Shibo JIANG ; Shuwen LIU
Chinese Pharmacological Bulletin 2010;26(1):25-28
Aim ADS-J1 is a low molecular HIV entry inhibitor targeting HIV transmembrane subunit gp41 through virtual screening from a compound library containing 20 000 molecules.This study is to investigate the binding sites of ADS-J1 on gp41.Methods Acid native polyacrylamide gel electrophoresis (AN-PAGE) assay was applied to test the binding ability of ADS-J1 with the peptides derived from gp41 N-terminal heptad repeat (NHR) region.Results It was reported previously that ADS-J1 could block the gp41 six-helix bundle (6-HB) formation using native polyacrylamide gel electrophoresis (N-PAGE).However,the binding sites could not be found because positive charged N-peptides derived from gp41 NHR could not show bands on the gel.In the present study,the AN-PAGE assay which could show N-peptides in the gel was established,and it was found that ADS-J1 could inhibit the gp41 6-HB formation.Moreover,ADS-J1 bound directly to the gp41 cavity region of NHR.The positively charged residue (K574) located in this region was critical for the binding of ADS-J1.Conclusions ADS-J1 inhibits HIV entry by targeting the cavity region of gp41 NHR,whereas K574 in the cavity plays a critical role for the binding.Furthermore,the AN-PAGE assay provides a simple method for studying the mechanism of action of virus entry inhibitors targeting the transmembrane protein of type I enveloped virus.
9.A Clinical Study on the Co-infection of Other Sexually Transmitted Infectionsin Patients with Genital Herpes
Weihong LAI ; Guozhu HAN ; Qianqiu WANG ; Wenhua JIANG ; Chuanfu ZHANG ; Huazhong XUE ; Shuwen ZHANG
Chinese Journal of Dermatology 1995;0(03):-
ObjectiveTostudytheincidenceandclinicalcharacteristicsoftheco-infectedsexuallytransmittedinfections(STI)inpatientswithgenitalherpes.MethodsTheclinicaldataof287caseswithherpeticlesionsorpatientswithsuspectedherpeslesionswerecollected,andthepathogensofsexuallytransmittedinfectionsweredetected.ResultsGenitalherpeswasconfirmedin64.8%(186/287)oftherecruitedcases.HIVantibodiesweredetectedin68cases,andnoHIVantibodywasdetected.Theco-infectionssuchascondylomaacuminatum,activeorlatentsyphilis,genitalcandidiasisandotherSTIswerediscoveredin23.1%(43/186)ofpatientswithgenitalherpes.Allgenitalherpescasesco-infectedwithotherSTIswerecausedbyHSV-2.ConclusionTheco-infectionsarecommoninpatientswithgenitalherpes,andthefeaturesofthelesionsmaybechangedbytheseco-infections.
10.Studies on a high-throughput screening method for identification of HIV fusion inhibitors targeting gp41
Shuwen LIU ; Shibo JIANG ; Beiyi LIU ; Zhihua WU ; Lin LV ; Jiajie ZHANG ; Ning FU ; Shuguang WU ;
Chinese Pharmacological Bulletin 1986;0(05):-
AIM To modify and improve a screening assay so that it becomes more convenient, economic and adaptable in China for high throughput screening of HIV fusion inhibitors targeting gp41. METHODS The original screening method reported by Jiang et al (J Virol. Methods 1999;80:85 96) was modified by: ① using a conformation specific monoclonal antibody to replace a polyclonal antibody for coating plates; ②simplifying the procedures; ③using parts of the reagents produced in China. RESULTS The modified screening assay is simpler, more convenient, and more economic than the original assay, but its sensitivity is comparable to and specificity is a little better than the original method. CONCLUSIONS The modified screening assay is more convenient and economic and can be used in China for high throughput screening of HIV fusion inhibitors from complex sample, such as phage display peptide libraries, microorganism fermentation liquids, herbs and other natural products.