Megastigmane sesquiterpenoids from the pericarps of Trichosanthes kirilowii and their anti-complementary and anti-inflammatory activities

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia Pub Date : 2025-07-02 DOI:10.1016/j.fitote.2025.106715

Ji-Bin Zou , Jia-Ren Lyu , Leverne Wang , Shui-Yuan Yang , Yan Lu , Dao-Feng Chen

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引用次数: 0

Abstract

The pericarps of Trichosanthes kirilowii Maxim. (T. kirilowi) have been traditionally used in Chinese medicine for their heat-clearing properties. This study employed anti-complementary activity-guided fractionation and purification to isolate eleven compounds from the pericarps of T. kirilowi, including two new megastigmane sesquiterpenoids (6, 8), seven previously identified megastigmane sesquiterpenoids (1–5, 7, 9), and two known flavonoids (10,11). The structures were elucidated using spectroscopic techniques (NMR, HRESIMS, IR, and UV) and computational chemistry methods with CD spectroscopy. Biological evaluation demonstrated that four megastigmane sesquiterpenoids (3, 4, 5, 6) and two flavonoids (10, 11) exhibited both anti-complementary activities (CH₅₀ values ranging from 0.906 ± 0.075 mM to 4.933 ± 0.318 mM) and anti-inflammatory activities (inhibition rates: 14.30 ± 4.234 % to 72.87 ± 1.594 %). Furthermore, the new megastigmane sesquiterpenoid (6), featuring a 3-hydroxy-3-methylglutaryl (HMG) substituent, and the flavonoid glucoside (11) modulated cytokine levels in LPS-stimulated ANA-1 cells by reducing IL-6 and MCP-1 while increasing IL-10.

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栝槐果皮中大芪甲素倍半萜类化合物及其抗补体和抗炎活性

栝楼的果皮。（T. kirilowi）因其清热特性而被传统地用于中医。本研究采用抗互补活性引导分离纯化方法，从黄芪果皮中分离得到11个化合物，包括2个新的大芪甲素倍半萜类化合物（6,8），7个先前鉴定的大芪甲素倍半萜类化合物（1 - 5,7,9）和2个已知的黄酮类化合物（10,11）。利用波谱技术（NMR, hresms， IR和UV）和CD光谱计算化学方法对其结构进行了分析。生物学评价表明，4种大芪甲草氨酸倍半萜类化合物（3,4,5,6）和2种黄酮类化合物（10,11）具有抗互补活性（CH50值为0.906±0.075 mM ~ 4.933±0.318 mM）和抗炎活性（抑制率为14.30±4.234% ~ 72.87±1.594%）。此外，具有3-羟基-3-甲基戊二酰（HMG）取代基的新megastigmane倍半萜类化合物(6)和黄酮类糖苷（11）通过降低IL-6和MCP-1而增加IL-10来调节lps刺激的ANA-1细胞中细胞因子的水平。

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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.