生物碱-单萜杂合体|广谱抗菌中药草珊瑚中发现具有抗神经炎活性的新骨架

中科院上海药物所岳建民院士团队从海南草珊瑚乙醇提取物的乙酸乙酯部位分离得到5个新的吲哚−单萜杂合体,其中,化合物4和5具有结构新颖的6/6/5/6/5-和6/6/6/6/5笼状骨架。
作者:小毅
时间:2023-08-17
阅读次数:416

草珊瑚 Sarcandra glabra (Thunb.) Nakai为金粟兰科草珊瑚属多年生常绿草本植物,又名九节风、竹节茶等,全株入药,药食同源,是苗族、傣族、壮族、瑶族等少数民族的常用药,是市售复方草珊瑚含片的君药。

Sarcandra glabra (Thunb.) Nakai, commonly known as sarcandra and also called "Jiu-jie-feng" and "Zhu-jie-cha" in China, is a perennial evergreen herbaceous plant belonging to the family Chloranthaceae. The entire plant is used for medicinal purposes and is considered as a medicinal-food homologous herb. It is commonly used by ethnic minorities in China such as the Miao, Dai, Zhuang, and Yao nations. Besides, sarcandra is the main ingredient of commercially available traditional Chinese medicine Sarcandra tablets.

草珊瑚性味苦、辛、平,归心、肝经,具有清热解毒、祛风活血、消肿止痛、抗菌消炎等功效。现代药理学研究表明草珊瑚富含黄酮类、萜类、香豆素类、酚酸类、挥发油类等化学成分,具有抗氧化、抗菌、抗炎、抗肿瘤、促进骨折愈合、调节免疫、降血糖血脂等药理活性,并且对胰腺癌、食道癌、肝癌等多种恶性肿瘤具有潜在抑制或辅助治疗作用。

Sarcandra glabra is characterized by a bitter, pungent, and neutral taste. It belongs to the heart and liver meridians according to traditional Chinese medicines. It is well-known for its therapeutic effects of clearing heat, detoxification, dispelling wind, promoting blood circulation, reducing swelling and relieving pain. It has been revealed by previous phytochemical investigations that the occurrence of contain flavonoids, terpenes, coumarins, phenolic acids, and volatile oils from S. glabra, which exhibit various bio-activities including antioxidant, antibacterial, anti-inflammatory, antihypertensive, lipid-lowering, anti-tumor, fracture healing promotion, and immune modulation. Furthermore, it has shown potential inhibitory or adjuvant therapeutic effects against various malignant tumors such as pancreatic cancer, esophageal cancer, and liver cancer.

为了进一步阐明草珊瑚属植物的药效成分,中科院上海药物所岳建民院士团队从海南草珊瑚乙醇提取物的乙酸乙酯部位分离得到5个新的吲哚−单萜杂合体,其中,化合物45具有结构新颖的6/6/5/6/5-6/6/6/6/5笼状骨架。通过核磁共振、X-单晶衍射、量子化学计算等手段鉴定了以上化合物的化学结构,并将其分别命名为sarglamides A−E(化合物1-5)。同时,该团队以白藜芦醇为阳性对照,在LPS-诱导的BV-2细胞炎症模型上测试了这些化合物的抗炎活性,结果表明化合物3-5具有较好的抗神经炎活性。

In order to deeply elucidate the active components of the genus Sarcandra, a team led by Academician Jian-min Yue from the Shanghai institute of materia medica, Chinese academy of sciences, isolated five new indole-diterpenoid hybrids from the ethyl acetate fraction of the extract of S. glabra collected in Hainan. Among them, compounds 4 and 5 possess structurally novel 6/6/5/6/5 and 6/6/6/6/5 cage-like frameworks, respectively. Their chemical structures were determined by nuclear magnetic resonance, X-ray single crystal diffraction, and quantum chemical calculations. These compounds were named sarglamides A-E (compounds 1-5), respectively. Additionally, their anti-inflammatory activities were evaluated in an LPS-induced BV-2 cell lines, using resveratrol as a positive control. The results showed that compounds 34 and 5 exhibited potential anti-neuroinflammatory activity.

 

岳院士团队的上述研究成果近日以“Sarglamides A−E, Indolidinoid−Monoterpenoid Hybrids with Anti-neuroinflammatory Activity from aSarcandra Species”为题在Organic Letters上发表。

These new findings have been published in Organic Letters titled Sarglamides A−E, Indolidinoid−Monoterpenoid Hybrids with Anti-neuroinflammatory Activity from a Sarcandra Species.

原文链接:

https://pubs.acs.org/doi/10.1021/acs.orglett.3c00196

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