Tian Yongqiang, Zhang Chunyun, Guo Mingquan
Key Laboratory of Plant Germplasm Enhancement and Specialty Agriculture, Wuhan Botanical Garden, Chinese Academy of Sciences, Moshan, Wuchang, Wuhan, 430074, China.
Graduate University of Chinese Academy of Sciences, Beijing, 100049, China.
BMC Complement Altern Med. 2017 Sep 12;17(1):460. doi: 10.1186/s12906-017-1966-y.
Alkaloids have been considered as the most promising bioactive ingredients in plant species from the genus Zanthoxylum. This study reports on the compositions and contents of the Zanthoxylum alkaloids (ZAs) from three Zanthoxylum species, and their potential anti-proliferation activities.
An HPLC-UV/ESI-MS/MS method was established and employed to analyze the alkaloids in different Zanthoxylum extracts. The common and unique peaks and their relative contents were summarized and compared to evaluate the similarity and dissimilarity of the three Zanthoxylum species. Meanwhile, inhibitory activity tests to four carcinoma cell lines, i.e., stomach tumor cells (SGC-7901), cervical tumor cells (Hela), colon tumor cells (HT-29) and Hepatic tumor cells (Hep G2), were carried out in vitro to evaluate the bioactivities of the ZAs.
Seventy peaks were detected in the crude total alkaloid samples, and 58 of them were identified. As a result, 13 common peaks were found in the extracts of all the three Zanthoxylum species, while some unique peaks were also observed in specific species, with 17 peaks in Z. simulans, 15 peaks in Z. ailanthoides and 11 peaks in Z. chalybeum, respectively. The comparison of the composition and relative contents indicated that alkaloids of benzophenanthridine type commonly present in all the three Zanthoxylum species with high relative contents among the others, which are 60.52% in Z. ailanthoides, 30.52% in Z. simulans and 13.84% in Z. chalybeum, respectively. In terms of activity test, Most of the crude alkaloids extracts showed remarkable inhibitory activities against various tumor cells, and the inhibitory rates ranged from 60.71 to 93.63% at a concentration of 200 μg/mL. However, SGC-7901 cells seemed to be more sensitive to the ZAs than the other three cancer cells.
The alkaloid profiles detected in this work revealed significant differences in both structures and contents among Zanthoxylum species. The inhibitory rates for different cancer cells in this study indicated that the potential anti-cancer activity should be attributed to quaternary alkaloids in these three species, which will provide great guidance for further exploring this traditional medicinal resource as new healthcare products.
生物碱被认为是花椒属植物中最具前景的生物活性成分。本研究报道了三种花椒属植物中花椒生物碱（ZAs）的组成、含量及其潜在的抗增殖活性。
建立了HPLC-UV/ESI-MS/MS方法并用于分析不同花椒提取物中的生物碱。总结并比较了共同峰和独特峰及其相对含量，以评估三种花椒属植物的异同。同时，对四种癌细胞系，即胃肿瘤细胞（SGC-7901）、宫颈肿瘤细胞（Hela）、结肠肿瘤细胞（HT-29）和肝肿瘤细胞（Hep G2）进行体外抑制活性试验，以评估ZAs的生物活性。
在粗总生物碱样品中检测到70个峰，其中58个峰被鉴定出来。结果，在所有三种花椒属植物的提取物中发现了13个共同峰，同时在特定物种中也观察到一些独特峰，在竹叶花椒中有17个峰，在樗叶花椒中有15个峰，在青花椒中有11个峰。组成和相对含量的比较表明，二苯并菲啶型生物碱在所有三种花椒属植物中普遍存在，且在其他生物碱中相对含量较高，在樗叶花椒中分别为60.52%，在竹叶花椒中为30.52%，在青花椒中为13.84%。在活性测试方面，大多数粗生物碱提取物对各种肿瘤细胞显示出显著的抑制活性，在浓度为200μg/mL时抑制率范围为60.71%至93.63%。然而，SGC-7901细胞似乎比其他三种癌细胞对ZAs更敏感。
本研究中检测到的生物碱谱揭示了花椒属植物在结构和含量上的显著差异。本研究中不同癌细胞的抑制率表明，潜在的抗癌活性应归因于这三个物种中的季铵生物碱，这将为进一步探索这种传统药用资源作为新型保健品提供重要指导。
