Plasma-Binding of Virginiamycin in vitro and in vivo

Inflamasi merupakan keadaan yang cenderung merugikan sebagai respon perlindungan tubuh untuk mengurangi dan menghilangkan pemicu terjadinya cedera dan infeksi.1 Salah satu mediator yang berperan dalam peradangan adalah Enzim siklooksigenase (COX).3 Penelitian in vitro menunjukan bahwa daun asam jawa (Tamarindus indica L.) memiliki aktivitas sebagai antiinflamasi.4,5 Penelitian ini menggunakan metode uji in silico dengan melakukan skrinning virtual terhadap senyawa-senyawa aktif di dalam asam jawa. Skrining virtual dilakukan untuk memprediksi senyawa aktif dalam asam jawa yang memiliki aktivitas sebagai antiinflamasi terhadap selektif inhibitor COX-2. Pengujian yang dilakukan meliputi skrining pharmacopore, molecular docking, pengujian lipinsky’s rules of five dan pengujian Pre-ADMET. Dari hasil identifikasi farmakofor dan penambatan molekul diperoleh satu senyawa aktif daun asam jawa sebagai senyawa pemandu terhadap COX-2 yaitu Linalool yang memiliki nilai pharmacophore fit score sebesar 52.11% dan memiliki nilai ikatan energi bebas (∆G) sebesar -9.21 kkal/mol, lebih rendah dibandingkan dengan ligan alaminya yaitu Celecoxib (-7.98 kkal/mol). Dengan residu asam amino ligan alami yang sama terikat pada Linalool yaituTYR371. Dari hasil prediksi parameter absorbsi dan distribusi menunjukkan bahwa senyawa Linalool memiliki nilai Caco-2 cell sebesar 37.4763 nmsec-1, HIA (%) sebesar 96.0055 dan Protein Plasma Binding (%) 95.0547. Kata kunci: antiinflamasi, asam jawa, inhibitor selektif COX-2, penambatan molekul, skrining farmakofor.

Download Full-text

Afaltoxin B1 transport in rat blood plasma. Binding to albumin in vivo and in vitro and spectrofluorimetric studies into the nature of the interaction

Biochimica et Biophysica Acta (BBA) - General Subjects ◽

10.1016/0304-4165(86)90030-9 ◽

1986 ◽

Vol 881 (3) ◽

pp. 383-390 ◽

Cited By ~ 17

Author(s):

Heini W. Dirr ◽

Johan C. Schabort

Keyword(s):

Blood Plasma ◽

Plasma Binding ◽

Rat Blood

Download Full-text

In Vitro Plasma Binding of Verapamil

InPharma ◽

10.1007/bf03304849 ◽

1985 ◽

Vol 469 (1) ◽

pp. 15-15

Keyword(s):

Plasma Binding

Download Full-text

Importance of blood-collection tubes in plasma lidocaine determinations.

Clinical Chemistry ◽

10.1093/clinchem/25.4.617 ◽

1979 ◽

Vol 25 (4) ◽

pp. 617-619 ◽

Cited By ~ 20

Author(s):

W W Stargel ◽

C R Roe ◽

P A Routledge ◽

D G Shand

Keyword(s):

Binding Sites ◽

Clinical Samples ◽

Therapeutic Drug ◽

Blood Collection ◽

Plasma Binding ◽

Sample Concentration ◽

Plasma Lidocaine ◽

Collection Tube ◽

Blood Collection Tubes

Abstract In 25 clinical samples serum lidocaine concentrations fell from a mean of 6.5 +/- 2.1 mg/L (mean +/- SD) to 4.9 +/- 1.8 mg/L (p less than 0.001) when the blood sample was allowed to make contact with the stopper of the Vacutainer collection tube. In vitro experiments showed that this effect of the stopper occurred only with whole blood and was dependent on sample concentration. The plasma binding of lidocaine decreased from a normal value of 56% +/- 2.2 (mean +/- SD) to 28% +/- 2.2 (p less than 0.001) when exposed to the Vacutainer stopper. We conclude that a chemical leached from such stoppers displaces lidocaine from its plasma-binding sites and that the drug is then redistributed into the erythrocytes, producing spuriously low lidocaine concentrations in plasma or serum. Such artifacts are important in therapeutic drug monitoring and can lead to erroneous clinical decisions.

Download Full-text

Do nonesterified fatty acids displace thyroxin from its plasma binding sites in severe nonthyroidal illnesses?

Clinical Chemistry ◽

10.1093/clinchem/35.6.931 ◽

1989 ◽

Vol 35 (6) ◽

pp. 931-934 ◽

Cited By ~ 9

Author(s):

R E Nicolson ◽

C P Reilly ◽

P R Pannall ◽

L Esposito ◽

M L Wellby

Keyword(s):

Fatty Acids ◽

Binding Sites ◽

Binding Proteins ◽

The Other ◽

Plasma Binding ◽

Plasma Nefa ◽

Nonesterified Fatty Acids ◽

Very High

Abstract Severe nonthyroidal illnesses have been associated with increases in nonesterified fatty acids (NEFA) and the dialyzable fraction of thyroxin (T4) in plasma. We have further investigated their possible relationship in severe nonthyroidal illnesses as well as in induced in vivo and in vitro situations involving increased NEFA. We demonstrate that there is no relationship between NEFA and the dialyzable fraction of T4, either in severe nonthyroidal illnesses or in the other situations, unless plasma NEFA concentrations exceed 5 mmol/L in normal persons or 1.7 mmol/L in nonthyroidal illnesses, and that this concentration was not reached in the patients we studied, with one exception. We conclude that NEFA are unlikely to contribute to an inhibition of the binding of T4 to the binding proteins that might be present in plasma of patients with severe nonthyroidal illnesses unless their NEFA concentrations are very high.

Download Full-text

Characteristics of Dolutegravir and Bictegravir Plasma Protein Binding: a First Approach for the Study of Pharmacologic Sanctuaries

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00895-20 ◽

2020 ◽

Vol 64 (11) ◽

Author(s):

Thibaut Gelé ◽

Hélène Gouget ◽

Valérie Furlan ◽

Pierre-Hadrien Becker ◽

Anne-Marie Taburet ◽

...

Keyword(s):

Human Serum Albumin ◽

Serum Albumin ◽

Protein Binding ◽

Plasma Binding ◽

Acid Glycoprotein ◽

Binding Rate ◽

Preferential Binding ◽

High Protein Binding ◽

Nonlinear Binding

ABSTRACT This study aimed to characterize in vitro dolutegravir (DTG) and bictegravir (BIC) binding. They had a preferential binding to human serum albumin (HSA) with two classes of albumin sites. Human alpha-1-acid glycoprotein (HAAG) binding of DTG and BIC showed an atypical nonlinear binding. The low-affinity site on HSA, the main plasma binding protein, suggests that the high protein binding rate should not impair passive diffusion.

Download Full-text