IUji penghambatan senyawa etil 4-{4-okso-2-[(E

Perpustakaan Universitas Indonesia >> UI - Skripsi (Open)
IUji penghambatan senyawa etil 4-{4-okso-2-[(E)-2-{4sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat terhadap
aktivitas siklooksigenase-2 = Inhibition test of ethyl 4-{4-oxo-2-[(E)-2{4- sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3- yl]}benzoate
compound for cyclooxygenase-2 activity
Titik Nurdayani
Deskripsi Dokumen: http://lib.ui.ac.id/opac/themes/libri2/detail.jsp?id=20313771&lokasi=lokal
-----------------------------------------------------------------------------------------Abstrak
Senyawa Etil 4-{4-okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin3-il]}benzoat merupakan senyawa baru yang mempunyai kemiripan struktur
dengan senyawa diarilheterosiklik, sedangkan sebagian besar inhibitor selektif
siklooksigenase-2 merupakan senyawa diarilheterosiklik, sehingga senyawa
tersebut diprediksi mempunyai aktivitas menghambat konversi asam arakhidonat
menjadi prostaglandin melalui jalur siklooksigenase. Penelitian ini bertujuan
untuk menguji efek penghambatan siklooksigenase-2 (COX-2) oleh senyawa etil
4-{4-okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat.
Uji aktivitas penghambatan COX-2 dilakukan dengan menggunakan kit COX
(ovine) inhibitor screening assay. Prostaglandin yang terbentuk ditentukan
menggunakan metoda Enzyme Immunoassay dan intensitas warna yang dihasilkan
diukur serapannya menggunakan plate reader pada panjang gelombang 415 nm.
Dari hasil uji didapatkan nilai IC50 senyawa etil 4-{4-okso-2-[(E)-2-{4sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat adalah 16,91 μM.
Sebagai pembanding, pengujian juga dilakukan terhadap asetosal dan selekoksib.
Hasil yang diperoleh untuk nilai IC50 asetosal dan selekoksib berturut-turut yaitu
24,97 μM dan 0,43 μM. Hasil penelitian menunjukkan bahwa senyawa etil 4-{4okso-2-[(E)-2-{4-sulfamoilfeniletenil}-3,4-dihidrokuinazolin-3-il]}benzoat
mempunyai potensi inhibisi lebih kuat dibandingan asetosal tetapi masih lebih
rendah dibandingkan selekoksib.
<hr>
<b>Abstract</b><br>
Ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3yl]}benzoate compound is a new drug that has structural similarities with diaryl
heterocyclic compound, while some of cyclooxygenase-2 selective inhibitor is a
diaryl heterocyclic compound, so that the compound is predicted to have activity
inhibits the conversion of arachidonic acid into prostaglandins through the
cyclooxygenase. The aim of this study is to the test inhibitory effect of
cyclooxygenase-2 (COX-2) by the ethyl 4-{4-oxo-2-[(E)-2-{4sulfamoylphenyletenyl}-3,4-dihydroquinazolin-3-yl]}benzoate compound. Study
of COX-2 inhibitory activity carried out by using a kit COX (ovine) inhibitor
screening assay. Prostaglandins which were formed was determined using the
method of Enzyme Immunoassay and the resulting color intensity was measured
using a plate reader absorbance at a wavelength of 415 nm. From the test results
obtained IC50 value of ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4dihydroquinazolin-3-yl]}benzoate compound was 16.91 μM. For comparison, the
tests were also done on acetosal and celecoxib. The results obtained for acetosal
and celecoxib IC50 values were 24.97 μM and 0.43 μM, respectively. The results
showed that the ethyl 4-{4-oxo-2-[(E)-2-{4-sulfamoylphenyletenyl}-3,4dihydroquinazolin-3-yl]}benzoate compound has stronger inhibitory potency
compared to acetosal but still lower than celecoxib.