Zhang Jian-Gang, Geng Chang-An, Huang Xiao-Yan, Chen Xing-Long, Ma Yun-Bao, Zhang Xue-Mei, Chen Ji-Jun
1 State Key Laboratory of Phytochemistry and Plant Resources in West China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
2 University of Chinese Academy of Sciences, Beijing 100049, PR China.
Eur J Mass Spectrom (Chichester). 2017 Feb;23(1):11-21. doi: 10.1177/1469066717694044. Epub 2017 Jan 1.
Uncaria rhynchophylla (Gou-Teng in Chinese) is officially documented in Chinese pharmacopoeia as one of the authentic sources for the crude drug of Gou-Teng which has long been used for mental and cardiovascular diseases. Indole alkaloids are the characteristic constituents responsible for the desired hypotensive effect; however, the psychiatric active constituents of Gou-Teng are still unclear. According to traditional Chinese medicine theory, only the hook-bearing stems of U. rhynchophylla are used as the crude materials for Gou-Teng, while its leaves and fruits are scarcely used. The present study aimed to compare the metabolic fingerprints of different parts (hooks, stems, leaves and fruits) of U. rhynchophylla by LC-DAD-MS/MS analysis and further evaluate their psychiatric activities on HEK293 cell line in vitro. A total of 38 constituents including 26 alkaloids, six flavonoids, two triterpenoids, two chlorogenic acid analogs and two other compounds were characterized. The different parts of U. rhynchophylla can be well differentiated from their chemical profiles. Leaves displayed the most potent activity on both MT and MT receptors, with agonistic rates of 39.7% and 97.6%. For 5-HT and 5-HT receptors, hooks showed the strongest activity with agonistic rates of 92.6% and 83.1%, respectively. This investigation provided valuable information for understanding the chemical divergence between different parts of U. rhynchophylla, and their substantial bases for psychiatric purposes.
钩藤在中国药典中被正式记载为传统中药钩藤的正品来源之一，长期以来用于治疗精神疾病和心血管疾病。吲哚生物碱是产生理想降压效果的特征性成分；然而，钩藤的精神活性成分仍不明确。根据传统中医理论，仅带钩的茎枝被用作钩藤的药材，而其叶和果实很少使用。本研究旨在通过LC-DAD-MS/MS分析比较钩藤不同部位（钩、茎、叶和果实）的代谢指纹图谱，并进一步在体外评估它们对HEK293细胞系的精神活性。共鉴定出38种成分，包括26种生物碱、6种黄酮类化合物、2种三萜类化合物、2种绿原酸类似物和2种其他化合物。钩藤的不同部位可以根据其化学特征很好地区分。叶对MT和MT受体均表现出最强的活性，激动率分别为39.7%和97.6%。对于5-HT和5-HT受体，钩表现出最强的活性，激动率分别为92.6%和83.1%。本研究为理解钩藤不同部位之间的化学差异及其精神活性的物质基础提供了有价值的信息。
