ABSTRACT
A case who revealed the longest duration of viral shedding (67 days) in current reports, presented complicated characteristic on the relapse of COVID-19 due to the inconsistent performance of chest radiography and SARS-CoV-2-RNA detection after discharge. Lopinavir-interferon α2b boosted ribavirin following with lopinavir boosted budesonide might be a potent treatment for viral clearance.
Subject(s)
COVID-19/virology , SARS-CoV-2/physiology , Aftercare , COVID-19/diagnostic imaging , COVID-19/physiopathology , Female , Hospitalization , Humans , Lopinavir/therapeutic use , Middle Aged , Patient Discharge , RNA, Viral/genetics , RNA, Viral/isolation & purification , Recurrence , Ribavirin/therapeutic use , SARS-CoV-2/genetics , Thorax/diagnostic imaging , Virus Shedding/drug effects , COVID-19 Drug TreatmentABSTRACT
The evidence of long-term clinical dynamic on Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) RNA re-positive case are less. We performed a 108 days follow-up on dynamic clinical presentations in a case, who hospitalized three times due to the positive recurrence of SARS-CoV-2 RNA after discharge, to understand the prognosis of the 2019-Coronavirus disease (COVID-19). In this case, positive SARS-CoV-2 recurred even after apparent recovery (normal CT imaging, no clinical symptoms, negative SARS-CoV-2 on stool sample and negative serum IgM test) from COVID-19, viral shedding duration lasted for 65 days, the time from symptom onset to disappearance was up to 95 days. Erythrocyte-associated indicators, liver function and serum lipid metabolism presented abnormal throughout during the observation period. Awareness of atypical presentations such as this one is important to prompt the improvement of the management of COVID-19.
Subject(s)
Betacoronavirus/pathogenicity , Coronavirus Infections/blood , Coronavirus Infections/virology , Pneumonia, Viral/blood , Pneumonia, Viral/virology , RNA, Viral/genetics , Virus Shedding , Adult , Alanine Transaminase/blood , Antiviral Agents/therapeutic use , Aspartate Aminotransferases/blood , Betacoronavirus/drug effects , Betacoronavirus/genetics , Biomarkers/blood , COVID-19 , Cholesterol, HDL/blood , Coronavirus Infections/diagnostic imaging , Coronavirus Infections/drug therapy , Hospitalization , Humans , Interferon alpha-2/therapeutic use , Lopinavir/therapeutic use , Male , Methylprednisolone/therapeutic use , Pandemics , Pneumonia, Viral/diagnostic imaging , Pneumonia, Viral/drug therapy , RNA, Viral/isolation & purification , Recurrence , SARS-CoV-2 , Tomography, X-Ray Computed , gamma-Glutamyltransferase/bloodABSTRACT
A series of novel 3-(thiophen-2-ylthio)pyridine derivatives as insulin-like growth factor 1 receptor (IGF-1R) inhibitors was designed and synthesized. IGF-1R kinase inhibitory activities and cytotoxicities against HepG2 and WSU-DLCL2 cell lines were tested. For all of these compounds, potent cancer cell proliferation inhibitory activities were observed, but not through the inhibition of IGR-1R. Selected compounds were further screened against various kinases. Typical compound 22 (50% inhibitory concentration [IC50 ] values, HepG2: 2.98 ± 1.11 µM and WSU-DLCL2: 4.34 ± 0.84 µM) exhibited good inhibitory activities against fibroblast growth factor receptor-2 (FGFR2), FGFR3, epidermal growth factor receptor, Janus kinase, and RON (receptor originated from Nantes), with IC50 values ranging from 2.14 to 12.20 µM. Additionally, the cell-cycle analysis showed that compound 22 could arrest HepG2 cells in the G1/G0 phase. Taken together, all the experiments confirmed that the compounds in this series were multitarget anticancer agents worth further optimizing.
Subject(s)
Antineoplastic Agents/pharmacology , Drug Design , Protein Kinase Inhibitors/pharmacology , Pyridines/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , ErbB Receptors/antagonists & inhibitors , ErbB Receptors/metabolism , Hep G2 Cells , Humans , Janus Kinases/antagonists & inhibitors , Janus Kinases/metabolism , Molecular Structure , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/chemistry , Pyridines/chemical synthesis , Pyridines/chemistry , Receptor Protein-Tyrosine Kinases/antagonists & inhibitors , Receptor Protein-Tyrosine Kinases/metabolism , Receptor, Fibroblast Growth Factor, Type 2/antagonists & inhibitors , Receptor, Fibroblast Growth Factor, Type 2/metabolism , Receptor, Fibroblast Growth Factor, Type 3/antagonists & inhibitors , Receptor, Fibroblast Growth Factor, Type 3/metabolism , Receptor, IGF Type 1/antagonists & inhibitors , Receptor, IGF Type 1/metabolism , Structure-Activity RelationshipABSTRACT
This study aims to investigate the preparation process and in vitro release behavior of artesunate polylactic acid microspheres, in order to prepare an artesunate polylactic acid (PLA) administration method suitable for hepatic arterial embolization. With PLA as the material and polyvinyl alcohol (PVA) as the emulsifier, O/W emulsion/solvent evaporation method was adopted to prepare artesunate polylactic acid microspheres, and optimize the preparation process. With drug loading capacity, encapsulation efficiency and particle size as indexes, a single factor analysis was made on PLA concentration, PVA concentration, drug loading ratio and stirring velocity. Through an orthogonal experiment, the optimal processing conditions were determined as follows: PLA concentration was 9. 0% , PVA concentration was 0. 9% , drug loading ratio was 1:2 and stirring velocity was 1 000 r x min(-1). According to the verification of the optimal process, microsphere size, drug loading and entrapment rate of artesunate polylactic acid microspheres were (101.7 +/- 0.37) microm, (30.8 +/- 0.84)%, (53.6 +/- 0.62)%, respectively. The results showed that the optimal process was so reasonable and stable that it could lay foundation for further studies.
