桄榔子皮黄酮类化合物的抗氧化、溶栓、抑菌和细胞毒活性

Seagufta Afrin, Abdul Muhit, H. Sohrab, C. M. Hasan, M. Ahsan
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引用次数: 1

摘要

采用桄榔子皮粗甲醇提取物分离次生代谢产物。通过各种色谱技术分离纯化了6个已知的天然化合物,鉴定出5个分离物为类黄酮衍生物,分别为pongachromene(1)、kanugin(2)、karanjin(3)、demethoxykanugin(4)、dimethoxypongapine(5)和1个三萜类化合物(6)。采用建立的方法对纯化的化合物以及粗甲醇提取物的石油醚、二氯甲烷和乙酸乙酯可溶性组分进行了生物活性评价。以丁基羟基茴香醚为对照品,采用DPPH自由基清除法研究其体外抗氧化活性。纯化合物中,卡兰金、去甲氧基卡兰金、二甲氧基卡兰金的IC50值分别为27.20±0.39 μg/mL和43.53±0.63 μg/mL,比标准化合物(23.87±0.09 μg/mL)具有显著的抗氧化活性。与标准链激酶(79.12%)相比,不同组分观察到轻度溶栓活性,凝块溶解范围为18.49%至29.35%。以阿奇霉素和酮康唑为标准,不同溶剂组分和纯分离物对被试微生物的抑菌带均为7.5 ~ 10.0 mm。在盐水对虾致死生物测定中,二氯甲烷、乙酸乙酯和甲醇可溶性组分的LC50值分别为0.67±0.05、0.61±0.13和0.56±0.10 μg/ml,显著高于标准他莫昔芬(LC50值为0.34±0.09 μg/ml)。
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Antioxidant, Thrombolytic, Antimicrobial and Cytotoxic Activities of Flavonoids Isolated from the Root Bark of Pongamia pinnata
The crude methanolic extract of the root bark of Pongamia pinnata was taken into consideration to isolate secondary metabolites. A total six known natural compounds were separated and purified by various chromatographic techniques and five isolates were identified as flavonoid derivatives such as pongachromene (1), kanugin (2), karanjin (3), demethoxykanugin (4), dimethoxypongapine (5) and the other is a triterpenoid (6). The pure compounds as well as petroleum ether, dichloromethane and ethyl acetate soluble fractions of crude methanolic extract were evaluated for bioactivities using established methods. In vitro antioxidant activity was studied by DPPH radical scavenging method using butylated hydroxyl anisole as standard. Among the pure compounds, kanugin and pongachromene showed significant antioxidant activity with the IC50 values of 27.20 ± 0.39 μg/mL and 43.53 ± 0.63 μg/ml, respectively as compared to the standard (23.87 ± 0.09 μg/ml), whereas karanjin, demethoxykanugin and dimethoxypongapine demonstrated moderate antioxidant activity. Mild thrombolytic activity was observed by different fractions with clot lysis ranging from 18.49 to 29.35% as compared to standard streptokinase (79.12%). The different solvent fractions and pure isolates showed very mild antimicrobial activity with zone of inhibition of 7.5 10.0 mm against the tested microorganisms using azithromycin and ketoconazole as standards. In the brine shrimp lethality bioassay, the dichloromethane, ethyl acetate, and methanol soluble fractions revealed significant lethality with LC50 values of 0.67 ± 0.05, 0.61 ± 0.13 and 0.56 ± 0.10 μg/ml, respectively as compared to standard tamoxifen (LC50 value 0.34 ± 0.09 μg/ml).
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