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Bui, Dinh ; McWilliams, Lenora A ; Wu, Lei , et al. Cancers,2023,15(1):89. DOI: 10.3390/cancers15010089 PubMed ID: 36612086
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Abstract: This study reports the first clinical evidence of significantly high secretion of matrine in a multi-component botanical (Antitumor B, ATB) into human saliva from the systemic circulation. This is of high clinical significance as matrine can be used as a monitoring tool during longitudinal clinical studies to overcome the key limitation of poor patient compliance often reported in cancer chemoprevention trials. Both matrine and dictamine were detected in the saliva and plasma samples but only matrine was quantifiable after the oral administration of ATB tablets (2400 mg) in 8 healthy volunteers. A significantly high saliva/plasma ratios for Cmax (6.5 2.0) and AUC0–24 (4.8 2.0) of matrine suggested an active secretion in saliva probably due to entero-salivary recycling as evident from the long half-lives (t1/2 plasma = 10.0 2.8 h, t1/2 saliva = 13.4 6.9 h). The correlation between saliva and plasma levels of matrine was established using a population compartmental pharmacokinetic co-model. Moreover, a species-relevant PBPK model was developed to adequately describe the pharmacokinetic profiles of matrine in mouse, rat, and human. In conclusion, matrine saliva concentrations can be used as an excellent marker compound for mechanistic studies of active secretion of drugs from plasma to saliva as well as monitor the patient’s compliance to the treatment regimen in upcoming clinical trials of ATB.
Keywords: cancer chemoprevention ; OCT transporter ; PBPK modeling ; plasma-saliva correlation ; entero-salivary recycling ; pharmacokinetics ; saliva excretion marker ; patient compliance tracker
Purchased from AmBeed: 19908-48-6 ; 484-29-7
CAS No. : | 484-29-7 | MDL No. : | MFCD00221742 |
Formula : | C12H9NO2 | Boiling Point : | - |
Linear Structure Formula : | - | InChI Key : | WIONIXOBNMDJFJ-UHFFFAOYSA-N |
M.W : | 199.21 | Pubchem ID : | 68085 |
Synonyms : |
Dectamine;Dictamine
|
Chemical Name : | 4-Methoxyfuro[2,3-b]quinoline |
Signal Word: | Warning | Class: | N/A |
Precautionary Statements: | P261-P305+P351+P338 | UN#: | N/A |
Hazard Statements: | H302-H315-H319-H335 | Packing Group: | N/A |
GHS Pictogram: |
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* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.
Yield | Reaction Conditions | Operation in experiment |
---|---|---|
91% | With hydrogen bromide; In water; acetic acid; for 8.0h;Heating / reflux; | A mixture of <strong>[484-29-7]4-methoxyfuro[2,3-b]quinoline</strong> (compound 1; 0.20 g, 1 mmol), 48% HBr (10 ml), and AcOH (20 ml) was refluxed for 8 h. After cooling, the mixture was poured into an ice-cold sat. NaHCO3 solution (60 ml), and extracted with AcOEt (3×60 ml). The AcOEt extracts were combined, washed with H2O, dried on MgSO4, and evaporated to yield a residual solid, which was purified by flash column chromatography (FC; silica gel; AcOEt). The proper fractions were combined and evaporated to obtain compound 2 (0.17 g, 91%). Detected Properties of the Title Compound: M.p. 236-237 C. 1H-NMR (200 MHz, DMSO): 7.06 (d,J=2.4, H-C(3)) 7.29 (m,H-C(6)); 7.56-7.68 (m,H-C(2), H-C(7), H-C(8)); 8.28 (d,J)=7.6, H-C(5)). 13C-NMR (50 MHz, DMSO): 104.85; 105.84; 121.60; 122.12; 123.08; 124.60; 130.06; 140.04; 142.53; 160.70; 166.69. |