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Improved Chiral Separation of (RS)-Goitrin by SFC: An Application in Traditional Chinese Medicine

机译:SFC改善(RS)-甲状腺素的手性分离:在中药中的应用

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摘要

Like chemical drugs, research and development of herbal medicine also have a need to resolve enantiomers. To help illustrating the antiviral bioactivity of Isatidis Radix, a widely used traditional Chinese medicine (TCM), supercritical fluid chromatography (SFC) was used for analytical and preparative separation of (R,S)-goitrin, which was reported as the active ingredient of the herbal. Improved resolution was achieved on Chiralpak IC column, using acetonitrile as the organic modifier, representing a tenfold increase in speed, compared to the previous normal phase HPLC (NPLC) method. The newly developed chromatographic method was validated in terms of linearity, precision, limit of detection (LOD), and limit of quantitation (LOQ). Scale-up purification of (R)-goitrin and (S)-goitrin was performed on a preparative column with >90% total recovery. The absolute stereochemical assignment of the purified isomers was determined through optical rotation study. This attempt explored SFC's application in chiral research of traditional Chinese medicine.
机译:像化学药物一样,草药的研究与开发也需要解析对映异构体。为了帮助说明Isatidis Radix(一种广泛使用的中药(TCM))的抗病毒生物活性,使用超临界流体色谱(SFC)进行分析和制备性分离(R,S)-goitrin的过程,据报道,goitrin是其有效成分。草药。与先前的正相HPLC(NPLC)方法相比,使用乙腈作为有机改性剂,在Chiralpak IC色谱柱上实现了更高的分离度,表示速度提高了十倍。新开发的色谱方法在线性,精密度,检出限(LOD)和定量限(LOQ)方面得到了验证。 (R)-goitrin和(S)-goitrin的放大纯化是在制备柱上进行的,总回收率> 90%。通过旋光研究确定了纯化的异构体的绝对立体化学分配。这项尝试探索了证监会在中药手性研究中的应用。

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