Development of efficient SPE-TLC method and evaluation of biological interactions of contraceptives with progesterone receptors

被引：6

作者：

Ali, Imran ^{[1
]}

Hussain, Iqbal ^{[1
]}

Saleem, Kishwar ^{[1
]}

Aboul-Enein, Hassan Y. ^{[2
]}

机构：

[1] Cent Univ, Jamia Millia Islamia, Dept Chem, New Delhi 110025, India

[2] Natl Reasearch Ctr, Pharmaceut & Med Chem Dept, Pharmaceut & Drug Ind Res Div, Cairo 12311, Egypt

来源：

ARABIAN JOURNAL OF CHEMISTRY | 2012年 / 5卷 / 02期

关键词：

Norethindrone acetate; Dydrogesterone; TLC; SPE; Plasma; PyMOL; Autodoc4; softwares; Protein bindings; DYDROGESTERONE; NORETHINDRONE;

D O I：

10.1016/j.arabjc.2010.09.010

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

TLC-SPE methodologies were developed to ascertain biological interactions of norethindrone acetate and dydrogesterone contraceptives with plasma progesterone receptor proteins. TLC solvent system for plain and Cu(II) impregnated silica gel plates was n-hexanc-n-butanol (90:10, v/v), which took 20 min to run up to 10.0 cm. The best separation was on Cu(II) impregnated plates due to maximum difference in R-r values and compact spots. The optimized SPE conditions were pH 2.0 and 3.0 of phosphate buffer (50 mM) for norethindrone acetate and dydrogesterone, respectively. The flow rate of plasma and eluting solvent (methanol) through C-18 cartridge was 0.10 mL/min. The interactions of these contraceptives with progesterone receptor proteins were analysed by TLC-SPE results, which were supported by modelling using PyMOL and Autodoc4 softwares. The dydrogesterone was found to be bound strongly than norethindrone acetate. Attempts have been made to discuss the drugs' interactions at chemo-supramolecular level. (c) 2010 King Saud University. Production and hosting by Elsevier B.V. All rights reserved.

引用

页码：235 / 240

页数：6

共 15 条

[1] Hyphenation in sample preparation: Advancement from the micro to the nano world [J].

Ali, Imran ;

Gupta, Vinod. K. ;

Aboul-Enein, Hassan Y. ;

Hussain, Afzal .

JOURNAL OF SEPARATION SCIENCE, 2008, 31 (11) :2040-2053

[2]

[Anonymous], 1969, THIN LAYER CHROMATOG, DOI DOI 10.1007/978-3-642-88488-7

[3] Use of dydrogesterone as a progestogen for oral contraception [J].

Bennink, HJTC ;

Boerrigter, PJ .

STEROIDS, 2003, 68 (10-13) :927-929

[4] A comparative molecular modeling study of dydrogesterone with other progestational agents through theoretical calculations and nuclear magnetic resonance spectroscopy [J].

Colombo, D ;

Ferraboschi, P ;

Prestileo, P ;

Toma, L .

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 2006, 98 (01) :56-62

[5]

Fried B., 1996, PRACTICAL THIN LAYER

[6]

Fried B., 1991, HDB THIN LAYER CHROM, V55

[7] High-performance liquid chromatographic optimization study for the separation of natural and synthetic anabolic steroids. Application to urine and pharmaceutical samples [J].

Gonzalo-Lumbreras, R ;

Izquierdo-Hornillos, R .

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 2000, 742 (01) :1-11

[8] Simultaneous determination of norethindrone ethinyl estradiol in human plasma by high performance liquid chromatography with tandem mass spectrometry-experiences on developing a highly selective method using derivatization reagent for enhancing sensitivity [J].

Li, WK ;

Li, YH ;

Li, AC ;

Zhou, SL ;

Weng, ND .

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 2005, 825 (02) :223-232

[9] Progesterone receptor ligand binding pocket flexibility: Crystal structures of the norethindrone and mometasone furoate complexes [J].

Madauss, KP ;

Deng, SJ ;

Austin, RJH ;

Lambert, MH ;

McLay, I ;

Pritchard, J ;

Short, SA ;

Stewart, EL ;

Uings, IJ ;

Williams, SP .

JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (13) :3381-3387

[10]

Mansour D., 2005, WOMENS HLTH MED, V2, P6

← 1 2 →