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三种灵芝属真菌中灵芝酸的化学指纹图谱与抗增殖活性的相关性比较及化学计量学分析。

Comparative and chemometric analysis of correlations between the chemical fingerprints and anti-proliferative activities of ganoderic acids from three Ganoderma species.

机构信息

Key Laboratory of Plant Germplasm Enhancement and Specialty Agriculture, Wuhan Botanical Garden, Chinese Academy of Sciences, Wuhan, China.

The Sino-Africa Joint Research Centre, Chinese Academy of Sciences, Wuhan, China.

出版信息

Phytochem Anal. 2019 Jul;30(4):474-480. doi: 10.1002/pca.2830. Epub 2019 Apr 1.

Abstract

INTRODUCTION

Investigation on ganoderic acids (GAs) from different cultivars and origins of Ganoderma species, regarding to their composition, contents and bioactivities, will be of great importance for the development and quality control of Ganoderma-based healthcare products or drugs.

OBJECTIVE

Comparative and chemometric analysis of different Ganoderma species were conducted to reveal the correlations between their chemical fingerprints and anti-proliferative activities.

METHODOLOGY

Six Ganoderma samples with different origins and parts of fruiting body (pileus and stipe) were extracted with chloroform and enriched by a SPE-C18 cartridge. The eluents were used for high-performance liquid chromatography ultraviolet electrospray ionisation tandem mass spectrometry (HPLC-UV/ESI-MS/MS) analysis and cytotoxicity assay with three cancer cell lines (SGC-7901, HT-29 and Hep G2). Chemometric analysis was applied to correlate their chemical compositions and corresponding bioactivities.

RESULTS

Sixteen peaks (accounting for 70% of the total peak areas) were identified as GAs, and their contents ranged from 0.368 to 10.8 μg/g in various Ganoderma species. The extracts from three Ganoderma species had significant anti-proliferative activities (inhibitory rates ranged from 70.8% to 80.7%), and extracts from Lurongzhi showed remarkable inhibition to all three cancer cells (inhibitory rates range from 81.6% to 92.1%). Finally, chemometric analysis revealed that 3,7,12-trihydroxy-4,4,14-trimethyl-11,15-dioxochol-8-en-24-oic acid and 12-acetoxy-15-hydroxy-4,4,14-trimethyl-3,7,11-trioxochol-8-en-24-oic acid were the two compounds with most potential anti-proliferative activity for SGC-7901.

CONCLUSION

The correlations between chemical fingerprints and anti-proliferative activities of various Ganoderma species give remarkable insight into the true bioactive components of chemical markers for the quality assessment of the Ganoderma resources, and provide a good guidance for the study on the chemical spectrum-bioactivity relationship.

摘要

简介

研究不同品种和来源的灵芝中的灵芝酸(GAs),包括其组成、含量和生物活性,对于开发灵芝为基础的保健品或药物以及质量控制具有重要意义。

目的

对不同灵芝物种进行比较和化学计量学分析,以揭示其化学指纹图谱与抗增殖活性之间的相关性。

方法

用氯仿提取来自不同产地和菌盖和菌柄不同部位的 6 个灵芝样本,并用 SPE-C18 小柱进行富集。洗脱液用于高效液相色谱紫外电喷雾离子化串联质谱(HPLC-UV/ESI-MS/MS)分析,并对三种癌细胞系(SGC-7901、HT-29 和 Hep G2)进行细胞毒性测定。应用化学计量学分析来关联它们的化学成分和相应的生物活性。

结果

鉴定出 16 个峰(占总峰面积的 70%)为 GAs,其含量在不同灵芝物种中范围为 0.368 至 10.8μg/g。来自三种灵芝的提取物具有显著的抗增殖活性(抑制率范围为 70.8%至 80.7%),而来自鹿茸芝的提取物对所有三种癌细胞均表现出显著的抑制作用(抑制率范围为 81.6%至 92.1%)。最后,化学计量学分析表明,3,7,12-三羟基-4,4,14-三甲基-11,15-二氧代-8-烯-24-酸和 12-乙酰氧基-15-羟基-4,4,14-三甲基-3,7,11-三氧代-8-烯-24-酸是对 SGC-7901 具有最强潜在抗增殖活性的两种化合物。

结论

不同灵芝物种的化学指纹图谱与抗增殖活性之间的相关性为灵芝资源的化学标志物质量评估中的真正生物活性成分提供了重要的见解,并为化学谱-生物活性关系的研究提供了良好的指导。

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