Lechtenberg Matthias, Schepmann Dirk, Niehues Michael, Hellenbrand Nils, Wünsch Bernhard, Hensel Andreas
Institute for Pharmaceutical Biology and Phytochemistry, University of Münster, Münster, Germany.
Planta Med. 2008 Jun;74(7):764-72. doi: 10.1055/s-2008-1074535. Epub 2008 May 21.
Extracts from saffron, the dried stigmata from Crocus sativus L., are being used more and more in preclinical and clinical trials for the treatment of cancer and depression. Because of the known quality problems of saffron, HPLC methods on RP(18) 2.5 microm and monolithic RP(18) material have been developed and validated for quality control including the quantification of crocins 1 to 5, crocetin, picrocrocin and the degradation products, the CIS-crocins. Additionally, a GC-MS method has allowed detection and quantification of the volatile compounds from the pentane extract of saffron. Both systems together allowed the comprehensive characterisation of saffron herbal material and extracts for clinical/preclinical trials. For effective preparation of the respective reference standards, a fast centrifugal partition chromatography (FCPC) method was developed allowing the quick isolation of crocins 1, 2, 5 and picrocrocin in good yields. Using these chromatographic methods and the reference standards, a representative survey of saffron from the global market indicated a high variability of quality, especially concerning the amounts of volatile compounds in saffron samples. A specification for high-quality saffron of >20% crocins, >6% picrocrocin and not less than 0.3% of volatiles, calculated as sum of safranal, isophorone and ketoisophorone, was developed. Because no detailed pharmacological studies are available to explain the clinical effects of saffron for the treatment of cancer and depression, receptor binding studies were performed. Saffron extracts and crocetin had a clear binding capacity at the PCP binding side of the NMDA receptor and at the sigma(1) receptor, while the crocins and picrocrocin were not effective. These data could give biochemical support for the above-mentioned pharmacological effects of saffron.
藏红花提取物，即番红花（Crocus sativus L.）干燥的柱头，在癌症和抑郁症治疗的临床前和临床试验中应用越来越广泛。鉴于藏红花已知的质量问题，已开发并验证了基于RP(18) 2.5微米和整体式RP(18)材料的HPLC方法用于质量控制，包括对藏花素1至5、藏红花酸、苦藏花素及其降解产物顺式藏花素的定量分析。此外，GC-MS方法可用于检测和定量藏红花戊烷提取物中的挥发性化合物。这两种系统共同实现了对用于临床/临床前试验的藏红花药材和提取物的全面表征。为有效制备各自的参考标准品，开发了一种快速离心分配色谱（FCPC）方法，可高产率快速分离藏花素1、2、5和苦藏花素。使用这些色谱方法和参考标准品，对全球市场上的藏红花进行的代表性调查表明质量差异很大，尤其是藏红花样品中挥发性化合物的含量。制定了高质量藏红花的规格标准：藏花素含量>20%，苦藏花素含量>6%，挥发物（以藏红花醛、异佛尔酮和酮异佛尔酮的总和计算）不少于0.3%。由于尚无详细的药理学研究来解释藏红花治疗癌症和抑郁症的临床效果，因此进行了受体结合研究。藏红花提取物和藏红花酸在NMDA受体的PCP结合位点和sigma(1)受体处具有明显的结合能力，而藏花素和苦藏花素则无效。这些数据可为藏红花上述药理作用提供生化支持。
