Parasuraman Subramani, Raveendran Ramasamy, Ardestani Mehdi Shafiee, Ananthakrishnan Ramesh, Jabbari-Arabzadeh Ali, Alavidjeh Mohammad Shafiee, Aghasadeghi Mohammad Reza, Elangovan Sundararajan, Dhanapathi Halanaik
Department of Pharmacology, Jawaharlal Institute of Postgraduate Medical Education and Research, Pondicherry, India.
Pharmacogn Mag. 2012 Apr;8(30):129-34. doi: 10.4103/0973-1296.96559.
To determine the biodistribution properties of cleistanthin A and cleistanthin B in rodents using magnetic resonance imaging (MRI).
Cleistanthins A and B, constituents of Cleistanthus collinus Roxb., were labelled with gadolinium (Gd(3+)) directly and injected into normal and tumoric nude mice. The tissue signal intensity was measured using MRI to perform a noninvasive kinetic assay. Wistar rats were used for determination of the grayscale intensity to observe the distribution patterns of of cleistanthins A and B.
Cleistanthin A is kinetically more attractive to the gastrointestinal tract than is cleistanthin B, which gets accumulated in muscular tissues of mice in greater concentrations compared with cleistanthin A. Cleistanthin B but not cleistanthin A showed tumoric affinity and exhibited a tumor kinetic attraction in tumoric mice. In rats, cleistanthin A showed greater grayscale intensities in the brain, liver, and skeletal muscles in immediate post contrast MRI images, whereas the gadolinium tagged cleistanthin B showed higher grayscale intensities in the cardiac muscle and skeletal muscles in delayed post contrast MRI images.
Cleistanthin A is more pharmacokinetically attractive to the gastrointestinal tract than cleistanthin B.
利用磁共振成像(MRI)确定啮齿动物体内铁屎米酮A和铁屎米酮B的生物分布特性。
将铁屎米酮A和铁屎米酮B(铁屎米属植物的成分)直接用钆(Gd(3+))标记,并注射到正常和患肿瘤的裸鼠体内。使用MRI测量组织信号强度以进行非侵入性动力学分析。使用Wistar大鼠测定灰度强度,以观察铁屎米酮A和铁屎米酮B的分布模式。
与铁屎米酮B相比,铁屎米酮A在动力学上对胃肠道更具吸引力,而铁屎米酮B在小鼠肌肉组织中的积累浓度高于铁屎米酮A。铁屎米酮B而非铁屎米酮A显示出对肿瘤的亲和力,并在患肿瘤的小鼠中表现出肿瘤动力学吸引力。在大鼠中,在造影后即刻的MRI图像中,铁屎米酮A在脑、肝和骨骼肌中显示出更高的灰度强度,而钆标记的铁屎米酮B在造影后延迟的MRI图像中在心肌和骨骼肌中显示出更高的灰度强度。
与铁屎米酮B相比,铁屎米酮A在药代动力学上对胃肠道更具吸引力。