Cajanonic acid A (CAA), a prenylated stilbene derivative extracted from the leaves of pigeon pea (Cajanus cajan), has been reported to possess inhibitory activity on the peroxisome proliferator-activated receptor gamma (PPARγ) and protein tyrosine phosphatase 1B (PTP1B). Its hypoglycemic activity in rats is comparable to that of the approved antidiabetic agent rosiglitazone. Therefore, CAA is a potential candidate for the treatment of type 2 diabetes and a lead compound for the discovery of novel hypoglycemic drugs. To achieve a thorough understanding of the biological behavior of CAA in vivo, our current study was designed to investigate the pharmacokinetics, bioavailability, distribution, and excretion of CAA in rats by UPLC-MS/MS. Chromatographic separation was performed on BEHC18 column (2.1 mm × 50 mm, 1.7 µm). Quantification was performed under the negative ion mode by using single reaction monitoring (SRM) of the transitions of m/z 353.14 → 309.11 for CAA and m/z 269.86 → 224.11 for genistein, respectively. Standard calibration curve showed excellent linearity (r2 > 0.99) within the range of 2 - 800 ng/mL. The accuracies and precisions were within the acceptance limits (all < 20%). CAA was quickly absorbed into bloodstream and distributed rapidly and widely to various tissues. The excretion ratio of CAA in the 3 main pathways via bile, feces, and urine was only 5.17%. These results indicate that CAA was quickly and thoroughly metabolized in vivo and excreted mainly as metabolites.

中文翻译：

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UPLC-MS/MS对大鼠体内Cajanonic Acid A的药代动力学、组织分布和排泄研究

木豆酸 A (CAA) 是一种从木豆 (Cajanus cajan) 叶子中提取的异戊二烯衍生物，据报道对过氧化物酶体增殖物激活受体 γ (PPARγ) 和蛋白酪氨酸磷酸酶 1B (PTP1B) 具有抑制活性。其在大鼠中的降血糖活性与批准的抗糖尿病药物罗格列酮相当。因此，CAA 是治疗 2 型糖尿病的潜在候选药物，也是发现新型降血糖药物的先导化合物。为了深入了解 CAA 在体内的生物学行为，我们目前的研究旨在通过 UPLC-MS/MS 研究 CAA 在大鼠体内的药代动力学、生物利用度、分布和排泄。在 BEHC18 色谱柱（2.1 mm × 50 mm，1.7 µm）上进行色谱分离。在负离子模式下，分别使用单反应监测 (SRM) 对 CAA 的 m/z 353.14 → 309.11 和染料木黄酮的 m/z 269.86 → 224.11 的跃迁进行定量。标准校准曲线在 2 - 800 ng/mL 范围内显示出极好的线性 (r2 > 0.99)。准确度和精密度均在可接受范围内（均 < 20%）。CAA 被迅速吸收到血液中，并迅速广泛地分布到各种组织中。CAA在胆、粪、尿3条主要途径中的排泄率仅为5.17%。这些结果表明，CAA 在体内迅速而彻底地代谢并主要作为代谢物排出体外。标准校准曲线在 2 - 800 ng/mL 范围内显示出极好的线性 (r2 > 0.99)。准确度和精密度均在可接受范围内（均 < 20%）。CAA 被迅速吸收到血液中，并迅速广泛地分布到各种组织中。CAA在胆、粪、尿3条主要途径中的排泄率仅为5.17%。这些结果表明，CAA 在体内迅速而彻底地代谢并主要作为代谢物排出体外。标准校准曲线在 2 - 800 ng/mL 范围内显示出极好的线性 (r2 > 0.99)。准确度和精密度均在可接受范围内（均 < 20%）。CAA 被迅速吸收到血液中，并迅速广泛地分布到各种组织中。CAA在胆、粪、尿3条主要途径中的排泄率仅为5.17%。这些结果表明，CAA 在体内迅速而彻底地代谢并主要作为代谢物排出体外。17%。这些结果表明，CAA 在体内迅速而彻底地代谢并主要作为代谢物排出体外。17%。这些结果表明，CAA 在体内迅速而彻底地代谢并主要作为代谢物排出体外。