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1.
Plant Biotechnol (Tokyo) ; 37(4): 471-474, 2020 Dec 25.
Artigo em Inglês | MEDLINE | ID: mdl-33850436

RESUMO

The mechanical strength of a plant stem (a load-bearing organ) helps the plant resist drooping, buckling and fracturing. We previously proposed a method for quickly evaluating the stiffness of an inflorescence stem in the model plant Arabidopsis thaliana based on measuring its natural frequency in a free-vibration test. However, the relationship between the stiffness and flexural rigidity of inflorescence stems was unclear. Here, we compared our previously described free-vibration test with the three-point bending test, the most popular method for calculating the flexural rigidity of A. thaliana stems, and examined the extent to which the results were correlated. Finally, to expand the application range, we present an example of a modified free-vibration test. Our results provide a reference for improving estimates of the flexural rigidity of A. thaliana inflorescence stems.

2.
J Pharm Pharmacol ; 61(8): 1029-35, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19703346

RESUMO

OBJECTIVES: The P-glycoprotein (P-gp) efflux pump plays an important role in paclitaxel detoxification. However, hepatic uptake of paclitaxel mediated by a solute-linked carrier transporter family is still poorly understood in animals and humans. Freshly isolated hepatocyte suspensions are a well established in-vitro model for studying drug transport and xenobiotic metabolism. Therefore, the hepatic uptake of paclitaxel and its P-gp-insensitive prodrug, 2'-ethylcarbonate-linked paclitaxel (TAX-2'-Et), has been characterized using freshly isolated and pregnenolone-16-alpha-carbonitrile (PCN)-treated hepatocytes in rats. METHODS: Paclitaxel and TAX-2'-Et were incubated with rat hepatocyte suspensions in the presence or absence of inhibitors. KEY FINDINGS: Paclitaxel and TAX-2'-Et showed concentration-dependent uptake in rat hepatocytes. The intrinsic transport capacity was two-fold higher for paclitaxel uptake than for TAX-2'-Et uptake. Rifampicin (a potent inhibitor of organic anion transporting polypeptide (Oatp) 2), but not indometacin (a representative inhibitor of organic anion transporter (Oat) 2 and Oatp1) treatment, significantly inhibited the uptake of paclitaxel and TAX-2'-Et. We characterized the rifampicin-sensitive uptake of paclitaxel and TAX-2'-Et using rat hepatocytes treated with PCN, which dramatically enhances hepatic Oatp2 protein levels. PCN-treated hepatocytes displayed a 1.6-fold greater uptake of paclitaxel and TAX-2'-Et than the vehicle-treated hepatocytes. The uptake of the two compounds was significantly reduced by rifampicin but not by indometacin treatment. These findings demonstrated that the rat Oatp2, but not Oatp1 or Oat2, was a candidate transporter for the hepatic uptake of paclitaxel and TAX-2'-Et. CONCLUSIONS: The findings have provided an important step towards identifying a key transporter in hepatic detoxification of paclitaxel and TAX-2'-Et in small animals.


Assuntos
Antineoplásicos Fitogênicos/farmacocinética , Hepatócitos/metabolismo , Proteínas de Transporte de Cátions Orgânicos/metabolismo , Paclitaxel/análogos & derivados , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Relação Dose-Resposta a Droga , Masculino , Transportadores de Ânions Orgânicos Sódio-Independentes/metabolismo , Paclitaxel/administração & dosagem , Paclitaxel/farmacocinética , Carbonitrila de Pregnenolona/farmacologia , Pró-Fármacos , Ratos , Ratos Wistar
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