scholarly journals Antimalarial drugs lose their activity with a slight drop in pH

2020 ◽  
Author(s):  
Tomohisa Kitagawa ◽  
Atsushi Mastumoto ◽  
Ichiro Terashima ◽  
Yukifumi Uesono
Keyword(s):  
Antimicrobial Activity ◽  
Glucose Uptake ◽  
Falciparum Malaria ◽  
Pharmacological Activity ◽  
Antimalarial Drugs ◽  
Normal Blood ◽  
Glucose Starvation ◽  
Amphiphilic Drug ◽  
Blood Ph ◽  
Ph Dependent

AbstractAntimalarial drugs have antimicrobial, antiviral, antimalarial and immunosuppressive activities, although the mechanisms remain unknown. Quinacrine (QC) increases the antimicrobial activity against yeast exponentially with a pH-dependent increase in the cationic amphiphilic drug (CAD) structure. CAD-QC localizes in membranes and induces glucose starvation by noncompetitively inhibiting glucose uptake. A logarithmic increase in antimicrobial activity with pH-dependent CAD formation was also observed for chloroquine, indicating that the CAD structure is crucial for its pharmacological activity. A decrease in CAD structure with a slight decrease in pH from 7.4 greatly reduced their effects; namely, these drugs would inefficiently act on falciparum malaria and COVID-19 pneumonia patients with acidosis, resulting in resistance. Recovering normal blood pH or using pH-insensitive quinoline drugs might be effective.

scholarly journals PENGARUH PEMBERIAN TERAPI OKSIGEN DENGAN MENGGUNAKAN NON-REBREATHING MASK (NRM) TERHADAP NILAI TEKANAN PARSIAL CO2 (PaCO2) PADA PASIEN CEDERA KEPALA SEDANG (MODERATE HEAD INJURY) DI RUANG INTENSIVE CARE UNIT (ICU) RSUP H ADAM MALIK MEDAN TAHUN 2016

2018 ◽  
Vol 11 (1) ◽  
pp. 33-38
Author(s):  
Marlisa Marlisa
Keyword(s):  
Head Injury ◽  
Ph Value ◽  
Sampling Technique ◽  
Normal Blood ◽  
P Value ◽  
Youth Health ◽  
Series Design ◽  
Blood Ph ◽  
Injury Treatment ◽  
Adequate Oxygenation

Head injury is any cases that caused high disability and mortallity rate. In neurology, head injury occupies the first squence and become the main of health problem to most youth, health and productive peoples. The treatment of head injury treatment is to prevent damage of brain cells by adequate oxygenation. The objective of the research was to find out the influence of giving oxygent therapy by using non-rebreathing mask (NRM) towards changing of partial pressure CO2 (PaCO2) value to head injury patients in ICU room of H. Adam Malik Hospital Medan. The research used the quasi experiment method with time series design. The samples were 10 respondents, taken by purpossive sampling technique. The instrument of the research was observation sheet. The result of the research showed that before given the oxygent therapy by using nonrebreathing mask (NRM), 5 respondents (50%) had normal blood pH value, 6 respondents (60%) had low blood HCO3- value, and 6 respondents (60%) had normal blood PaCO2 value. After given oxygent therapy found that 5 respondents (50%) had low blood pH value, 6 respondents (60%) had low blood HCO3- value, and 7 respondents (70%) had low blood PaCO2 value. The result of statistic analyze with T-Test was found significant influence of changing PaCO2 value with p value = 0,000 (p<0,05). The reduction of PaCO2 value is followed by increasing of blood pH value and reduction of blood HCO3- value. Using of non-rebreathing mask (NRM) is only effective for head injury patients with high blood PaCO2.

scholarly journals A New Pathway Promotes Adaptation of Human Glioblastoma Cells to Glucose Starvation

Cells ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 1249
Author(s):  
Alberto Azzalin ◽  
Francesca Brambilla ◽  
Eloisa Arbustini ◽  
Katia Basello ◽  
Attilio Speciani ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Membrane Trafficking ◽  
Adaptor Protein ◽  
Glucose Starvation ◽  
Glioblastoma Cells ◽  
Glucose Addition ◽  
Human Glioblastoma ◽  
Human Glioblastoma Cells ◽  
Inducible Protein

Adaptation of glioblastoma to caloric restriction induces compensatory changes in tumor metabolism that are incompletely known. Here we show that in human glioblastoma cells maintained in exhausted medium, SHC adaptor protein 3 (SHC3) increases due to down-regulation of SHC3 protein degradation. This effect is reversed by glucose addition and is not present in normal astrocytes. Increased SHC3 levels are associated to increased glucose uptake mediated by changes in membrane trafficking of glucose transporters of the solute carrier 2A superfamily (GLUT/SLC2A). We found that the effects on vesicle trafficking are mediated by SHC3 interactions with adaptor protein complex 1 and 2 (AP), BMP-2-inducible protein kinase and a fraction of poly ADP-ribose polymerase 1 (PARP1) associated to vesicles containing GLUT/SLC2As. In glioblastoma cells, PARP1 inhibitor veliparib mimics glucose starvation in enhancing glucose uptake. Furthermore, cytosol extracted from glioblastoma cells inhibits PARP1 enzymatic activity in vitro while immunodepletion of SHC3 from the cytosol significantly relieves this inhibition. The identification of a new pathway controlling glucose uptake in high grade gliomas represents an opportunity for repositioning existing drugs and designing new ones.

Abnormal circulatory control in falciparum malaria: the effects of antimalarial drugs

1993 ◽  
Vol 44 (4) ◽  
pp. 325-329 ◽  
Author(s):  
W. Supanaranond ◽  
T. M. E. Davis ◽  
S. Pukrittayakamee ◽  
B. Nagachinta ◽  
N. J. White
Keyword(s):  
Falciparum Malaria ◽  
Antimalarial Drugs ◽  
Circulatory Control

scholarly journals Susceptibility of Chlamydia trachomatis to the Excipient Hydroxyethyl Cellulose: pH and Concentration Dependence of Antimicrobial Activity

2008 ◽  
Vol 52 (7) ◽  
pp. 2660-2662 ◽  
Author(s):  
Ali A. Abdul Sater ◽  
David M. Ojcius ◽  
Matthew P. Meyer
Keyword(s):  
Antimicrobial Activity ◽  
Chlamydia Trachomatis ◽  
Epithelial Cells ◽  
Concentration Dependence ◽  
Hydroxyethyl Cellulose ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Sexually Transmitted ◽  
Calcium Sequestration ◽  
Ph Dependent

ABSTRACT Hydroxyethyl cellulose (HEC) is used as a neutral excipient in microbicides used against sexually transmitted pathogens. However, HEC inhibits the infection of cervical epithelial cells by Chlamydia trachomatis at pH 5 in a concentration-dependent manner. At pH 7, infection is inversely dependent on the concentration of HEC, possibly due to pH-dependent calcium sequestration.

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