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从中国西南部的一种民族药用植物中提取的三种具有一氧化氮抑制活性的新化合物。

Three new compounds with nitric oxide inhibitory activity from , an ethnomedicinal plant from Southwest China.

作者信息

Gu Ronghui, Wang Yuehu, Wu Shibiao, Wang Yeling, Li Ping, Xu Li, Zhou Yue, Chen Ze'e, Kennelly Edward J, Long Chunlin

机构信息

1College of Life and Environmental Sciences, Minzu University of China, 27 Zhongguancun South Ave., Haidian, Beijing, 100081 People's Republic of China.

2Kunming Institute of Botany, Chinese Academy of Sciences, 132 Lanhei Road, Heilongtan, Kunming, 650201 People's Republic of China.

出版信息

BMC Chem. 2019 Apr 1;13(1):47. doi: 10.1186/s13065-019-0568-9. eCollection 2019 Dec.

DOI:10.1186/s13065-019-0568-9
PMID:31384795
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6661779/
Abstract

The medicinal plant has been used by the Zhuang ethnic people in mountainous areas of Southwest China to stop bleeding, invigorate blood circulation, and treat inflammation and wounds. In order to further explore its traditional medicinal uses, the phytochemical constituents of this species were examined. Three new compounds, the lignan tirpitzin (), the flavonoid tirpitzoside (), and the furan-glycoside tirpitziol (), along with five known compounds were isolated from the aerial part of for the first time. The structures of these compounds were elucidated by 1D and 2D NMR, LC/MS, IR spectrometric methods and compared with published data. The results of an in silico pharmacophore-based analysis showed potential targets of the new compounds, including ERBB2, IRAK4, LCK, JAK2, MAPK14, and MMP-12. These targets suggested that - may be involved with wound-healing and/or inflammation, leading to an in vitro assay of nitric oxide (NO) inhibition assays with lipopolysaccharide-induced BV-2 cells. All three new compounds displayed moderate NO inhibitory activity with the IC values of 14.97 ± 0.87, 26.63 ± 1.32, and 17.09 ± 2.3 μM, respectively.

摘要

这种药用植物在中国西南部山区的壮族人民中被用于止血、促进血液循环以及治疗炎症和伤口。为了进一步探索其传统药用价值，对该物种的植物化学成分进行了研究。从该植物地上部分首次分离出三种新化合物，即木脂素类的三裂叶素（）、黄酮类的三裂叶苷（）和呋喃糖苷类的三裂叶醇（），以及五种已知化合物。这些化合物的结构通过一维和二维核磁共振、液相色谱/质谱、红外光谱法进行了阐明，并与已发表的数据进行了比较。基于计算机模拟药效团分析的结果显示了这些新化合物的潜在靶点，包括表皮生长因子受体2（ERBB2）、白介素-1受体相关激酶4（IRAK4）、淋巴细胞特异性蛋白酪氨酸激酶（LCK）、 Janus激酶2（JAK2）、丝裂原活化蛋白激酶14（MAPK14）和基质金属蛋白酶-12（MMP-12）。这些靶点表明该植物可能与伤口愈合和/或炎症有关，从而对脂多糖诱导的BV-2细胞进行了一氧化氮（NO）抑制试验的体外测定。所有三种新化合物均表现出中等程度的NO抑制活性，IC50值分别为14.97±0.87、26.63±1.32和17.09±2.3μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/4863116bc3b4/13065_2019_568_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/190a753df157/13065_2019_568_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/aa1384c4cbef/13065_2019_568_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/4863116bc3b4/13065_2019_568_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/190a753df157/13065_2019_568_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/aa1384c4cbef/13065_2019_568_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a691/6661779/4863116bc3b4/13065_2019_568_Fig4_HTML.jpg

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