小檗中原小檗碱类生物碱及其抗疟活性。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia Pub Date : 2025-06-13 DOI:10.1016/j.fitote.2025.106681

Wen-Hui Du, Ling Leng, Wei Chen, Long-Fei He, Gang Li, Zhu Qiu, Shu-Jun Fang, Yi-Ling Yang, Chao-Jiang Xiao, Bei Jiang

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引用次数: 0

摘要

三种新的原小檗碱生物碱berpruines A-C(1,2,4)，以及从95 % EtOH的小檗根提取物中分离出的六种已知化合物和一个分离产物(9)。通过对光谱数据（1D NMR、2D NMR、hremsims和CD）和理化性质的综合分析确定了它们的结构，并以植物中2,3,9,10,12五取代原小檗碱类生物碱的首个例子小檗碱C(4)为例进行了分析。化合物4、5、7、10具有显著的体外抗疟活性，IC50值分别为5.5、1.1、8.4、3.1 μM；化合物1、6、8具有中等的体外抗疟活性，IC50值为23.0 ~ 39.9 μM。此外，还对分离得到的原小檗碱类生物碱体外抗疟活性的构效关系进行了初步综述。

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Protoberberine alkaloids from Berberis pruinosa and their antimalarial activities.

Three new protoberberine alkaloids berpruines A-C (1, 2, and 4), along with six known compounds and one isolation artifact (9) from the 95 % EtOH extract of roots of Berberis pruinosa. Their structures were determined by the comprehensive analyses of the spectroscopic data (1D NMR, 2D NMR, HRESIMS, and CD) and physicochemical properties, and berpruine C (4) as the first example of 2,3,9,10,12 pentasubstituted protoberberine alkaloid from plants. Compounds 4, 5, 7, and 10 exhibited significant in vitro antimalarial activities with IC₅₀ values of 5.5, 1.1, 8.4, and 3.1 μM, and compounds 1, 6, and 8 exhibited moderate antimalarial activities with IC₅₀ values ranging from 23.0 to 39.9 μM. In addition, a summary of preliminary structure-activity relationship of isolated protoberberine alkaloids for in vitro antimalarial activity was described.

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来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

期刊介绍： Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.