Chen Wei-Di, Zhao Yun-Li, Dai Zhi, Zhou Zhong-Shun, Zhu Pei-Feng, Liu Ya-Ping, Zhao Li-Xing, Luo Xiao-Dong
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming, People's Republic of China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, People's Republic of China.
J Food Biochem. 2020 Dec;44(12):e13511. doi: 10.1111/jfbc.13511. Epub 2020 Oct 25.
The whole plant of Clerodendranthus spicatus (Thunb.) is one of popular functional food in south of China, named as "kidney tea" and used to ameliorate renal inflammation. In order to verify this potential function and explore the accurate compounds responsible for inflammation, the ethanol extract, fractions, and subfractions of this plant were prepared to evaluate anti-inflammation effect on xylene-induced acute inflammatory mice model, and the results indicated that two subfractions from EtOAc fraction show potential activities. Subsequent bioassay-guided isolation of the bioactive subfractions led to isolation of 25 compounds. Among them, compounds 2, 4, 5, 9-11, 13, 16, 17, and 20-22 inhibited the productions of pro-inflammation factors TNF-α, IL-1β, and IL-8 in lipopolysaccharide (LPS) -induced renal epithelia (HK-2) cells, respectively. Further anti-inflammation evaluation in vivo indicated that the major bioactive compounds 1, 2, 5-7, 17, 21, and 22 from C. spicatus were even better than aspirin. PRACTICAL APPLICATIONS: C. spicatus as a healthy tea has been available in the Chinese market and as a medicine for various disorders such as nephritis, rheumatism, inflammation, gout, and diabetes. Previous pharmacological investigation of the plant revealed the potential anti-inflammatory activities, but the material basis of anti-inflammatory activity remains to be elucidated. In our study, the anti-inflammatory fractions and compounds were obtained by the bioassay-guide isolation and the results showed that the highly oxygenated diterpenoids were major anti-inflammatory compounds, in which 1, 2, 5-7, 17, 21, and 22 were even better than aspirin. This information supported kidney tea as a functional food for treatment of renal inflammation reasonably and may add a new dimension to biological activity of this plant in the field of agriculture as a functional food were cultivated.
肾茶（Clerodendranthus spicatus (Thunb.)）全株是中国南方一种受欢迎的功能性食品，名为“肾茶”，用于改善肾脏炎症。为了验证这种潜在功能并探索导致炎症的具体化合物，制备了该植物的乙醇提取物、馏分和亚馏分，以评估其对二甲苯诱导的急性炎症小鼠模型的抗炎作用，结果表明乙酸乙酯馏分中的两个亚馏分具有潜在活性。随后，通过生物活性测定指导，对具有生物活性的亚馏分进行分离，得到了25种化合物。其中，化合物2、4、5、9 - 11、13、16、17以及20 - 22分别抑制了脂多糖（LPS）诱导的肾上皮（HK - 2）细胞中促炎因子TNF-α、IL-1β和IL-8的产生。进一步的体内抗炎评估表明，肾茶中的主要生物活性化合物1、2、5 - 7、17、21和22甚至比阿司匹林的效果更好。实际应用：肾茶作为一种健康茶饮已在中国市场有售，并且作为治疗各种疾病如肾炎、风湿、炎症、痛风和糖尿病的药物。此前对该植物的药理学研究揭示了其潜在的抗炎活性，但抗炎活性的物质基础仍有待阐明。在我们的研究中，通过生物活性测定指导分离得到了抗炎馏分和化合物，结果表明高度氧化的二萜类化合物是主要的抗炎化合物，其中1、2、5 - 7、17、21和22甚至比阿司匹林效果更好。这些信息合理地支持了肾茶作为治疗肾脏炎症的功能性食品，并可能为该植物作为功能性食品在农业领域的生物活性增添新的维度。
